Fourth Stage Guide

Summer Training Guide
For
Fourth Stage
Pharmacy Students
‫ص َذقَ ٍخ‬
‫س ‪َ ٍِِْ :‬‬ ‫بد ا ْث ُِ آ َد ًَ ا ّْقَطَ َع َع ََئُُ إِال ٍِِْ صَال ٍ‬ ‫(إِ َرا ٍَ َ‬
‫ح ٌَ ْذ ُع٘ ىَُٔ)‬ ‫َجب ِسٌَ ٍخ ‪ ،‬أَ ْٗ ِع ْي ٌٍ ٌُ ْْزَفَ ُع ثِ ِٔ ‪ ،‬أَ ْٗ َٗىَ ٍذ َ‬
‫صبى ِ ٍ‬
‫حذٌش ّج٘ي ششٌف‬
‫إٕذاء‪.....‬‬
‫إىى ‪....‬‬
‫صٗجزً ٗأٗالدي (ٌبعش ٗحَضح)‪....‬‬
‫عيى ٍب أخزد ٍِ ٗقذ ٕ٘ ٍِ حقٌٖ ‪....‬‬
‫إٔذي عَـــــــــــــــــــيً ٕـــــــــــــــــــزا ‪....‬‬
‫ظٍبء‬
‫‪8102‬‬
‫رٍَٖـذ‬
‫ٌٍ‬
‫َِ اى َّش ِح ِ‬ ‫غ ٌِ هللاِ اى َّش ْح ِ‬ ‫ث ْ‬
‫ش ًذا)‬‫ع ٰى َٕ ْو أَرَّجِ ُعلَ َعيَ ٰى أَُْ رُ َعيِّ ََ ِِ ٍِ ََّب ُعيِّ َْذَ ُس ْ‬
‫(قَب َه ىَُٔ ٍُ٘ َ‬
‫ع٘سح اىنٖف اٌَخ ﴿‪﴾٦٦‬‬
‫ٌَضو اىزذسٌت اىصٍفً ىطالة اىَشحيخ اىشاثعخ فً ميٍبد اىصٍذىخ اىقغٌ‬
‫اىضبًّ ٍِ ٍزطيجبد اىزذسٌت اىصٍفً ثعذ رذسٌت اىَشحيخ اىضبىضخ ٗرأرً‬
‫إٍَزٔ ٍِ مُ٘ اىطبىت ٌذخو ٕزا اىقغٌ ٗقذ اعزنَو دساعخ عيٌ االدٌٗخ‬
‫مبٍال ٍع دساعخ صٍذىخ اىَجزَع ٗ قغَب ٍَٖب ٍِ اىصٍذىخ اىغشٌشٌخ‬
‫ٗثبىزبىً فأُ اغيت ٍب ٌشآ ٍِ ادٌٗخ ٗاٍشاض عزنُ٘ ٍَب عجق ىٔ‬
‫دساعزٖب ّظشٌب ٗعَيٍب فً اىنيٍخ‪...‬اُ اىطبىت فً ٕزٓ اىَشحيخ ٌنُ٘ قذ‬
‫اٗشل عيى اىزخشط‪ٗ ..‬ثبىزبىً فأُ االّخشاغ فً اج٘اء اىَْٖخ ٗاىزَبط‬
‫اىَجبشش ٍع عبىٌ االدٌٗخ ٗاى٘صفبد ٗاىَشظى ‪..‬رحذ اششاف اىصٍذىً‬
‫غجعب‪ٌ ..‬صجح ظشٗسح ٍيحخ ىيزٍٖؤ ىجٍئخ اىعَو مصٍذالًّ ٍغؤٗه عِ‬
‫صحخ ٗعالٍخ اىَشٌط‪ ..‬اُ ٕزا اىنزبة ٌعذ اعزنَبال ىنزبة (دىٍو اىزذسٌت‬
‫اىصٍفً‪ ..‬ىطالة اىَشحيخ اىضبىضخ فً ميٍبد اىصٍذىخ)‪..‬رٌ اىز٘عع ثٔ امضش‬
‫اّغجبٍب ٗاىَشحيخ اىذساعٍخ‪ ..‬غٍش اُ اىز٘عع ىٌ ٌخشط عِ اىز٘جٔ اىعبً‬
‫ىينزبة ٕٗ٘ رشمٍضٓ عيى (اىَعيٍ٘بد االعبعٍخ‪ٗ ..‬اىََٖخ‪ ..‬راد اىطبثع‬
‫اىعَيً ٗاىقبثو ىيزطجٍق) اىخبصخ ثنو ٍجَ٘عخ دٗائٍخ اٗ احذ ادٌٗزٖب‪ٗ...‬قذ‬
‫حبفظْب عيى اعي٘ة ٗرشرٍت دىٍو اىَشحيخ اىضبىضخ ٍِ ّبحٍخ رقغٌٍ اىفص٘ه‬
‫ٗرجٌ٘ت اىَجبٍٍع اىذٗائٍخ ٗعشض اىَعيٍ٘بد ٗاىجذاٗه اىَيحقخ اىخبصخ‬
‫ثأعَبء االدٌٗخ اىزجبسٌخ (االمضش شٍ٘عب) ٗاشنبىٖب اىصٍذالٍّخ ٗاىزً رَأل‬
‫ٍِ قجو اىطبىت اىَزذسة‪ ..‬إُ عَيً ٕزا قذ ال ٌخي٘ ٍِ قص٘ ٍس‪ٗ ،‬ىنِ ٗمَب‬
‫ت إّغبٌُ مزبثًب فً ٌ٘ ٍِٔ؛ إالَّ‬ ‫ٌق٘ه اىقبظً اىفبظو‪ ":‬إًِّّ سأٌذُ أَّّٔ ال ٌنزُ ُ‬
‫غُِ ‪ٗ ،‬ى٘ قُ ِّذ ًَ‬‫أحغِ‪ٗ ،‬ى٘ ِصٌ َذ مزا ىنبُ ٌُغزَح َ‬ ‫َ‬ ‫قب َه فً َغ ِذ ِٓ‪ :‬ى٘ ُغٍِّ َش ٕزا ىنبُ‬
‫ٕزا ىنبُ أفع َو‪ٗ ،‬ى٘ رُ ِشكَ ٕزا ىنبُ أجَ َو‪ٕٗ .‬زا ٍِِْ أعظَ ٌِ اى ِعجَ ِش‪ ٕ٘ٗ ،‬دىٍ ٌو‬
‫ش ِش "‪ٗ ..‬أخٍشا الثذ ٍِ اإلشبسح إىى إُ‬ ‫ص عيَى ُجَي ِخ اىجَ َ‬ ‫عيَى اعزٍال ِء اىَّْق ِ‬
‫ٕزا اىذىٍو قذ اعذ ىٍنُ٘ ٍغبعذا ىطيجزْب األعضاء فً اىزذسٌت اىصٍفً ٕٗ٘‬
‫ىٍظ ثذٌال عِ اىزذسٌت فً إي حبه اّغجبٍب ٍع اىحنَخ اىزعيٍٍَخ اىقبئيخ‪:‬‬
‫(قو ىً‪ٗ..‬ع٘ف أّغى‪..‬أسًّ ‪ٗ ..‬ع٘ف أرزمش ‪ ..‬أششمًْ ‪ٗ ..‬ع٘ف أرعيٌ)‪..‬‬
‫ٍِٗ اىيــــــــــــــــــٔ اىز٘فٍـــــــــــــــق‬
‫ظٍــــــبء‬
‫‪8102‬‬
Contents
Chapter's Title Page
number
0 Cardiovascular System 0
8 Gastro-intestinal System 82
3 Respiratory System 74
7 Central nervous system 28
5 Infections 47
2 Endocrine system 010
4 Genito-urinary system 080
2 Immune system and malignant disease 034
7 Nutrition and blood 072
01 Musculoskeletal and joint diseases 028
00 Eye 042
08 Ear, nose, and oropharynx 022
03 Skin 077
Chapter One: Cardiovascular System
1.1-Angiotensin-converting enzyme inhibitors (ACE inhibitors)
1-They inhibit ACE, thereby inhibiting the conversion of angiotensin I to
angiotensin II, a potent vasoconstrictor (1) .
2-Examples include (captopril, enalapril, fosinopril, imidapril, lisinopril,

moexipril, perindopril, quinapril, ramipril, and trandolapril) (2).
3-They act as vasodilators. The main uses of ACE inhibitors are in the
management of heart failure, hypertension, and myocardial infarction (3). In
addition, they are used for the prevention and treatment of diabetic nephropathy
(1)
.
4-Treat all patients with diabetes and hypertension with an ACE inhibitor or
angiotensin II receptor blockers (ARBs). Both classes provide nephroprotection
and reduced CV risk (4).
5-It may take several weeks before the full antihypertensive effects of ACEIs are
seen. Therefore, evaluating BP response 2 to 4 weeks after starting or changing the
dose of an ACEI is appropriate (5).
6-Renal function and electrolytes should be checked before starting ACE inhibitors
(or increasing the dose) and monitored during treatment (5). Patients with an
increase in serum creatinine of greater than 30% should have their ACEI therapy
temporarily discontinued (5) until further evaluation can be made (6).
7-Pronounced hypotension may occur at the start of therapy with ACE inhibitors
(first dose hypotension) (3). Therefore:
A-Therapy should be started with low doses followed by gradual titration as

tolerated to target doses (4).
B-For hypertension the first dose should preferably be given at bedtime (2).
8-Other adverse effects include persistent dry cough (3)(see ARBs below).
9-Angioedema is a serious potential complication of ACEi therapy. It occurs in

less than 1% of the population. Symptoms include lip and tongue swelling and
possibly difficulty breathing (4).
10-An ACEi, as well as an ARB or direct renin inhibitor, are absolutely

contraindicated in pregnancy (4).
1
ACE inhibitors
Scientific name Trade names Dosage form
1
Any extra notes:
1.2-Angiotensin II receptor blockers(ARBs).

1-They block the binding of angiotensin II to the AT1 receptor, thereby inhibiting
the effects of angiotensin II (1).
2-Examples include (Azilsartan, candesartan, eprosartan, irbesartan, losartan,

olmesartan, telmisartan , and valsartan)(sartans) (2).
3-They are used for hypertension, heart failure, diabetic nephropathy, and
myocardial infarction (1).
4-Imortant: unlike ACE inhibitors, they are less likely to cause the persistent
dry cough which can complicate ACE inhibitor therapy. They are therefore a
useful alternative for patients who have to discontinue an ACE inhibitor
because of persistent cough (2).
5-In select situations, the addition of ARBs to ACE-Is for patients with HF has
demonstrated additional incremental benefits and may be considered if aldosterone
antagonists are not indicated or tolerated (6).
6-Like ACE inhibitors, they may cause renal insufficiency, hyperkalemia, and
orthostatic hypotension (4).
7-Patients with a history of ACEi angioedema can be treated with an ARB when
needed (4).
2
Angiotensin II receptor blockers
1
Any extra notes:
1.3-Beta-adrenoceptor blocking drugs (beta-blockers)

1-Examples include (Atenolol, bisoprolol, carvedilol, metoprolol, nadolol,
oxprenolol, pindolol, and propranolol) (2).
2-Oxprenolol, and pindolol have intrinsic sympathomimetic activity (ISA); they

tend to cause less bradycardia than the other beta-blockers and may also cause
less coldness of the extremities (2).
3-Atenolol, and nadolol are the most water soluble; they are less likely to enter
the brain, and may therefore cause less sleep disturbance and nightmares. They are
excreted by the kidneys and dosage reduction is often necessary in renal
impairment (2).
4-Beta blockers are used in the management of:

A-Cardiovascular disorders such as hypertension, angina pectoris, cardiac
arrhythmias, myocardial infarction, and some of them are used for heart
failure (3).
B-They are also given to control symptoms of sympathetic overactivity,

anxiety states, hyperthyroidism, tremor and in the prophylaxis of migraine
(2, 3)
.
C-Some Beta blockers used as eye drops (e.g. timolol) to reduce raised intra-
ocular pressure in glaucoma (3).
5-Important:
A-Bisoprolol , carvedilol , metoprolol and nebivolol are the beta-blockers that
are used to treat heart failure (other beta- blokers are contraindicated) (2, 3).
3
B-When used for heart failure, β-blockers should be started in very low doses
with slow upward dose titration (2) (start low, go slow) (Doses should be
doubled no more often than every 2 weeks, as tolerated, until the target dose or
the maximally tolerated dose is reached) (4) e.g. :
Carvedilol start with 3.125 mg 6.25 mg 12.5 mg 25 mg) (2).
(2, 3)
C-When used in heart failure, carvedilol should be taken with food to
reduce the risk of hypotension (3).
6-Esmolol is a relatively cardioselective beta-blocker with a very short duration of

action, used intravenously for the short-term treatment of supraventricular
arrhythmias (2).
7-Sotalol, a non-cardioselective beta-blocker with additional class III anti-

arrhythmic activity, is used for prophylaxis in paroxysmal supraventricular
arrhythmias (2).
8-Important:
A-β-blockers are effective for reducing blood pressure but other
antihypertensives are usually more effective for reducing the incidence of
stroke, myocardial infarction, and cardiovascular mortality, especially in the
elderly (2). Therefore, β-blocker is no longer recommended as one of the
first-line treatment option for hypertension (5).
B-β-Blockers are only considered appropriate first-line agents to treat specific

compelling indications (e.g., post-MI and coronary artery disease) (4).
9-Beta-blockers can precipitate bronchospasm and should therefore usually be

avoided in patients with a history of asthma (2).
10-Atenolol, bisoprolol, metoprolol, and nebivolol, have less effect on the β2

(bronchial) receptors and are, therefore, relatively cardioselective. They have a
lesser effect on airways resistance but are not free of this side-effect (2).
11-Beta-blockers are also associated with fatigue, coldness of the extremities (may
be less common with those with ISA), and sleep disturbances with nightmares
(may be less common with the water-soluble beta-blockers) (2).
12-Beta-blockers can mask the signs and symptoms of hypoglycemia (such as

tachycardia) (except sweating). However, beta-blockers are not contra-indicated in
diabetes, although the cardioselective beta-blockers may be preferred (2, 5).
13-Abrupt cessation of β-blocker therapy may produce unstable angina, MI, or

even death in patients with coronary disease. In patients without heart disease,
abrupt discontinuation of β-blockers may be associated with tachycardia, sweating,
4
and generalized malaise in addition to increased BP. For these reasons, the dose
should always be tapered gradually over 1 to 2 weeks before discontinuation (4).
Beta-blockers
Scientific name Trade name Dosage form
1
Any extra notes:
1.4-Neprilysin inhibitors (Sacubitril)

1-Sacubitril (a neprilysin inhibitor) inhibits the breakdown of natriuretic peptides
resulting in varied effects including increased diuresis, natriuresis, and vasodilation
(2)
.
2-Neprilysin inhibitor must be combined with ARB. The combination of
valsartan with sacubitril [angiotension receptor- neprilysin inhibitor (ARNI)]
(entresto ®)is indicated for chronic heart failure with reduced ejection fraction
(systolic HF) (2).
3-Because of the risk of angioedema, patients should not start taking an ARNI
within 36 hours of taking their last ACE inhibitor dose (7).

1 Valsartan/sacubitril
Any extra notes:
5
1.5-Renin inhibitor
1-Aliskiren is a renin inhibitor that is licensed for the treatment of hypertension(2).
2-Aliskiren is an alternative therapy because of lack of long-term studies

evaluating CV event reduction and its significant cost (4).
3-Many of the cautions and adverse effects seen with ACE inhibitors and ARBs
apply to aliskiren. It is contraindicated in pregnancy due to known teratogenic
effects (4).

1
Any extra notes:
1.6-Calcium-channel blockers (CCBs)

1-CCBs include :
A-Dihydropyridine CCBs (examples amlodipine, nifedipine): They have a
greater selectivity for vascular smooth muscle than for heart and therefore
their main effect is vasodilatation (3).
B-Non-Dihydropyridine CCBs (examples diltiazem and verapamil): They

have a greater selectivity for heart than for vascular smooth muscle (3).
Diltiazem has a less negative inotropic effect than verapamil and significant
myocardial depression occurs rarely (2).
2-The main use of CCBs is in the management of angina pectoris and

hypertension (both types of CCBs) ; some are also used in cardiac arrhythmias
(non-dihydropyridine CCBs) (3). All are valuable in forms of angina associated
with coronary vasospasm (2).
3-Nimodipine is related to nifedipine but the smooth muscle relaxant effect

preferentially acts on cerebral arteries. Its use is confined to prevention and
treatment of vascular spasm following aneurysmal subarachnoid hemorrhage (2).
4-Verapamil is used also as prophylaxis of cluster headache. Nifedipine is also

indicated for Raynaud’s syndrome, postponement of premature labour, and
hiccup in palliative care (2).
5-Amlodipine and felodipine have a longer duration of action and can be given
once daily (2).
6
6-Side-effects associated with vasodilatation such as flushing and headache (which
become less obtrusive after a few days), and ankle swelling (which may respond
only partially to diuretics) are common (2). Constipation is the most common side-
effect of verapamil (2).
8-Verapamil and diltiazem should usually be avoided in heart failure (systolic

HF) because they may further depress cardiac function and cause clinically
significant deterioration (2).
9-Unlike in systolic HF, nondihydropyridine calcium channel blockers

(diltiazem and verapamil) may be useful in diastolic HF [HF with preserved
ejection fraction (HFpEF)] (6).
10-Nifedipine is a short acting, therefore it is commonly formulated as sustained

release formulation (long acting dosage form).
11-Amlodipine tablets from various suppliers may contain different salts (e.g.
amlodipine besilate, amlodipine maleate, and amlodipine mesilate) but the strength
is expressed in terms of amlodipine (base); tablets containing different salts are
considered interchangeable (2).
12-Different versions of modified-release preparations may not have the same

clinical effect. To avoid confusion between these different formulations of
nifedipine and diltiazem, prescribers should specify the brand to be dispensed (2).
13-Tablet membrane of (Tildiem retard ® and Adalat ® LA) may pass through
gastro-intestinal tract unchanged, but being porous has no effect on efficacy (2).
14-Grapefruit juice increases the concentration of (amlodipine, nifedipine,

verapamil, felodipine, and lercanidipine) (avoid) (2).
CCBs
1
7
Any extra notes:
1.7-Diuretics
1-The principal groups of diuretics are as follows (table 1-1).
Table 1-1: Types of diuretics

Diuretic type examples
Thiazide and related diuretics Hydrochlorothiazide, Chlortalidone
Loop Diuretics Furosemide, Bumetanide and Torasemide
Potassium (K+)-sparing diuretics Amiloride and triamterene
Aldosterone antagonist Spironolactone
Carbonic anhydrase inhibitors Acetazolamide (mainly for glaucoma)
Osmotic diuretics Mannitol (used in cerebral edema)
2-Diuretics promote the excretion of water and electrolytes by the kidneys. They
are used in the treatment of heart failure, hypertension and other diseases when
salt and water retention has resulted in edema (3).
3-Thiazides are the preferred type of diuretic for hypertension (4). Loop
diuretics produce a more potent diuresis, but a smaller decrease in peripheral
vascular resistance (PVR), and less vasodilation than thiazide diuretics (5).
4-The loop diuretics are more potent than thiazides, and retain their effectiveness
in renal insufficiency. Thus, in most patients with HF, loop diuretics are
preferred (5).
5-Thiazides are believed to lose their effectiveness when creatinine clearance

decreases to less than 30 mL/minute. Metolazone is an exception in that its
activity may be preserved in these patients (5). Unlike thiazides, loop diuretics
maintain their effectiveness in the presence of impaired renal function, although
higher doses may be necessary (4).
6-Potassium-sparing diuretics are weak antihypertensives when used alone.

Their primary use is in combination with another diuretic to counteract potassium-
wasting properties (4).
7-Because they do not alter disease progression or prolong survival, diuretics

are not required for HF patients without fluid retention (4).
8-Chlortalidone, a thiazide-related compound, has a longer duration of action than

the thiazides and may be given on alternate days to control edema. Metolazone is
particularly effective when combined with a loop diuretic (even in renal failure) (2).
8
9-Hydrochlorothiazide is more widely available in fixed-dose combination
products (5).
10-Xipamide and indapamide are chemically related to chlortalidone. Indapamide

is claimed to lower blood pressure with less metabolic disturbance, particularly
less aggravation of diabetes mellitus (2).
11-Spironolactone is of value in the treatment of edema and ascites caused by

cirrhosis of the liver; furosemide can be used as an adjunct. Low doses of
spironolactone are beneficial in moderate to severe heart failure (2).
12-Mannitol is an osmotic diuretic that can be used to treat cerebral edema and
raised intra-ocular pressure (2).
13-Diuretics ideally should be dosed in the morning if given once daily and in the
morning and afternoon if dosed twice daily to minimize the risk of nighttime
diuresis (4).
14-I.V Furosemide doses greater than 50 mg given by intravenous infusion only.

Give continuously in sodium chloride 0.9% ; glucose solutions are unsuitable (2).
15-Hypokalaemia can occur with both thiazide and loop diuretics. The risk of
hypokalaemia depends on the duration of action as well as the potency and is thus
greater with thiazides than with an equipotent dose of a loop diuretic (2).
16-Spironolactone is given after food (2). It has an anti-androgenic properties,

therefore:
A-It may cause side effects like gynecomastia (breast enlargement), and
impotence in men (3).
B- It has been used for its anti-androgenic properties in some cases of acne and
for women with hirsutism (hair on the face) (3).
17-In concentrations of 15% or greater, mannitol may crystallize when exposed to

low temperatures. Do not use a mannitol solution containing crystals. If such
crystallization occurs, the recommended procedure for resolubilization is to heat
the mannitol in a dry heat cabinet to 70 °C for flexible plastic containers with the
overwrap intact or to 80 °C for glass containers with vigorous shaking. The use of
a water bath is not recommended (8).
9
Diuretics
1
Any extra notes:
Note : Fixed-dose combination products

1-Several fixed-dose combination products are available , their use can reduce
the number of tablets or capsules taken by patients. This has been demonstrated
to improve adherence compared with using two separate single-drug
products. Improved adherence may increase the likelihood of achieving goal BP
values (3).
2-Most fixed-dose combinations include a thiazide diuretic. Other fixed-dose

combination products combine a CCB with either an ACEI or ARB (3).
Fixed-dose combination products

1
11
1.8-Lipid-regulating drugs
1-Lipid regulating drugs are used to modify blood lipid concentrations in the
management of dyslipidemias and for the reduction of cardiovascular risk (3).
2-The principal groups of lipid regulating drugs are (table 1-2) (2, 4):
Table 1-2: Types of lipid regulating drugs

Class Examples
1 Statins Atorvastatin, Fluvastatin, Pravastatin, Rosuvastatin,
and Simvastatin
2 Fibrates Bezafibrate, Ciprofibrate, Fenofibrate, and
Gemfibrozil
3 Nicotinic acid Acipimox, and Nicotinic acid.
derivatives
4 Bile acid sequestrants Colesevelam, Colestipol, and Colestyramine,
5 Absorption inhibitors Ezetimibe
6 Others Alirocumab, Evolocumab, Lomitapide ,
Mipomerson and Omega-3 fatty acid compounds
1.8.1- Statins
1-Statins are more effective than other lipid-regulating drugs at lowering LDL-
cholesterol concentration but they are less effective than the fibrates in reducing
triglyceride concentration (2).
2-Statins are used adjunct to diet and exercise for various dyslipidemias and for the
treatment of various dyslipidemia disorders in patients with no evidence of
cardiovascular disease (primary prevention) and in patients with documented
coronary artery disease (secondary prevention) (9).
3-Rosuvastatin and atorvastatin have the longest half-lives. The long half-life
also allows for administration at any time of day rather than at bedtime for
maximum effect, which is recommended for simvastatin, lovastatin, pravastatin,
and fluvastatin (5) (Cholesterol synthesis in the liver peaks during the early morning
(midnight to 3 a.m.) (3).
4-Relative LDL–lowering efficacy of statins are shown in table 1-3 (10).

Table 1-3: Relative LDL–lowering efficacy of statins (10).
11
high-intensity statin; moderate-intensity statin; lowers low-intensity statin;
lowers LDL by ≥ 50%. LDL-C by 30% to < 50%. lowers LDL by <30%.
5-The most common adverse effects reported include muscle pain and weakness
(myalgias), headache, GI symptoms, including dyspepsia, flatus, constipation, and
abdominal pain, and skin rashes. These symptoms are usually mild and often
dissipate with continued therapy (5).
6-Less common adverse effects include myopathy, elevated hepatic

transaminases, and diabetes (5).
7-Muscle toxicity can occur with all statins, however the likelihood increases with
higher doses. Therefore, advise patients to report promptly unexplained muscle
pain, tenderness, or weakness (2).
8-Liver enzymes should be measured before treatment, and repeated within 3

months and at 12 months of starting treatment, unless indicated at other times by
signs or symptoms suggestive of hepatotoxicity (2).
9-Grapefruit juice increases the concentration of simvastatin (avoid) (2).
1.8.2- Fibrates
1-Fibrates are mainly used for the treatment of hypertriglyceridemia (9).
2-Bezafibrate and fenofibrate are given with or just after food while gemfibrozil is
given 30 to 60 minutes before food (2).
1.8.3-Bile acid sequestrants (BAS)

1-Bile acid sequestrants effectively reduce LDL-cholesterol but can aggravate
hypertriglyceridaemia. Treatment with bile acid sequestrants may be appropriate if
statins and ezetimibe are inappropriate, and when LDL-cholesterol is severely
raised, for example in familial hypercholesterolaemia (2).
2-Older BAS (colestyramine, colestipol) are not well tolerated due to numerous GI
side effects and the unpleasant granular texture of the powder. Therefore,
colesevelam is currently the preferred agent (5).
3-Other uses:
A-Colesevelam is also approved by the FDA for use in type 2 diabetes to
improve glycemic control (5).
B-Colestyramine is also used for pruritus associated with partial biliary

obstruction and primary biliary cirrhosis. It also used for diarrhea associated
with Crohn‘s disease, ileal resection vagotomy, diabetic vagal neuropathy, and
radiation (2).
12
4-They interfere with the absorption of fat-soluble vitamins (supplements of
vitamins A, D, K, and folic acid may be required when treatment is prolonged) (2).
5-Colestyramine and colestipol may reduce or delay the absorption of

medications when co-administered. This can be minimized by administering other
medications 1 hour before or 4 hours after the resin dose (5).
6-Adminstarion:
A-Colesevelam tablet is given with or just after food (2).
B-Colestipol Granules: The contents of each sachet should be mixed with at

least 100 mL of water or other suitable liquid such as fruit juice or skimmed
milk. Alternatively it can be mixed with thin soups, cereals, yoghurt, or pulpy
fruits ensuring at least 100 mL of liquid is provided (2).
C-Colestyramine Powder :The contents of each sachet should be mixed with

at least 150 mL of water or other suitable liquid such as fruit juice, skimmed
milk, thin soups, and pulpy fruits with a high moisture content (2).
1.8.4-Cholesterol Absorption Inhibitor (Ezetimibe)

1-Ezetimibe may be used alone or in combination with a statin or fenofibrate
along with diet for the management of dyslipidemia, specifically to lower LDL-C.
In combination with a statin, it demonstrates an additive effect, enhancing LDL-C
lowering by an additional 10% to 20% (5).
2-Ezetimibe is taken without regard to meals (9).
1.8.5-Nicotinic acid derivatives

1-The value of nicotinic acid is limited by its side-effects, especially
vasodilatation. Acipimox seems to have fewer side-effects than nicotinic acid but
may be less effective in its lipid-regulating capabilities (2).
2-Nicotinic acid is used in combination with a statin if the statin alone cannot
adequately control dyslipidaemia (2). It lowers both cholesterol and triglyceride
concentrations by inhibiting synthesis; it also increases HDL-cholesterol (2).
3-Acipimox capsule is given with or just after food (2).
4-Nicotinic acid: Prostaglandin-mediated symptoms (such as flushing) can be

reduced by low initial doses taken with meals or, if patient taking aspirin, aspirin
dose should be taken 30 minutes before nicotinic acid (2).
1.8.6-Others
1-Lomitapide is used (orally) as an adjunct to dietary measures and other lipid-
regulating drugs for the treatment of homozygous familial hypercholesterolaemia.
dose to be taken at least 2 hours after evening meal (2).
13
2-Alirocumab and Evolocumab (lower LDL-C) are given subcutaneously.
These drugs are indicated as an adjunct to diet and maximally tolerated lipid-
lowering therapy for adults with heterozygous familial hypercholesterolemia or
patients who require additional lowering of LDL cholesterol (4).
3-Fish oil supplementation (omega-3 polyunsaturated fatty acids) may be most

useful in patients with hypertriglyceridemia, but its role in treatment is not well
defined (4) (there is no evidence that omega-3 fatty acid compounds reduce the risk
of cardiovascular disease) (2).
Lipid-regulating drugs
1
Any extra notes:
1.9-Nitrates
1-Nitrates are peripheral and coronary vasodilators used in the management of
angina pectoris, heart failure, and myocardial infarction (3).
2-Sublingual glyceryl trinitrate (GTN) is effective for providing rapid

symptomatic relief of angina. The aerosol spray provides an alternative method of
rapid relief of symptoms for those who find difficulty in dissolving sublingual
preparations (2).
3-If using the GTN spray, patient should apply the spray on or under the tongue
and not swallow or inhale it (5).
4-Patient education about sublingual glyceryl trinitrate (table 1-4)
14
Table 1-4: Patient education about sublingual glyceryl trinitrate
1-In the event of an acute attack, patients should be instructed to sit or lie down,
place the dose (spray or tablet) under the tongue, and not swallow the tablet.
Relief of pain should occur within 5 minutes (11). If the pain persists or is
unimproved 5 minutes after the first dose of GTN, the patient should call an
ambulance transport as they may be experiencing an MI. If patient needs more
than one tablet, he can take a maximum of three tablets in 15 minutes (5).
2-SL nitrates can also be used to prevent acute episodes if given 2 to 5 minutes
prior to activities known to produce angina; protection can last for up to 30
minutes with (4).
3-The tablets should be dispensed in the original, unopened manufacturer‘s
container and stored in the original brown bottle (5).
4-The bottle should be stored in a cool, dry place, but not refrigerated. The bottle
should be closed tightly after each opening (5).
5-GTN tablets should be supplied in glass containers of not more than 100 tablets
closed with a foil-lined cap, and containing no cotton wool wadding; they should
be discarded after 8 weeks in use (2).
6-Expiration dating should be monitored closely, and tablets should be replaced
immediately if they are exposed to excessive light, heat, moisture, or air (5).
5-Transdermal GTN patches, isosorbide dinitrate (ISDN) and isosorbide

mononitrate (ISMN) are most commonly prescribed for long-term prevention
(prophylaxis) of angina episodes (4).
6-ISMN is the primary metabolite of ISDN. To minimize the potential

development of nitrate tolerance, ISMN should be used in a twice-daily (the first
dose is taken on awakening and the second dose about 7 hours later) (5).
7-Modified release formulations of ISMN should only be given once daily (dose
to be taken in the morning), and used in this way do not produce tolerance (2).
8-Despite the availability of ISMN, oral ISDN is still commonly used. ISDN needs
to be dosed three times a day (7 AM, noon, and 5 PM ) (5). In the case of
modified release tablets of ISDN, the second of the two daily doses should be
given after about 8 hours rather than after 12 hours (2).
9-Common side effects of nitrate therapy include hypotension, dizziness, and

headache (5). Headache usually resolves after about two weeks of continued
therapy (4) and may be treated with acetaminophen (5).
10-Concomitant administration with phosphodiesterase type 5 inhibitors (within

24 hours for sildenafil and vardenafil, 48 hours for tadalafil) is contraindicated
due to the risk of life-threatening hypotension (5).
15
Nitrates
1
Any extra notes:
1.10-Antiplatelet drugs
1-Antiplatelet drugs reduce platelet aggregation and are used to prevent further
thromboembolic events in patients who have suffered myocardial infarction,
ischemic stroke or transient ischemic attacks, or unstable angina, and for primary
prevention of a thromboembolic event in patients at risk (3).
2-Antiplatelet drugs include aspirin, P2Y12 inhibitor antiplatelet [cangrelor (I.V),

clopidogrel, prasugrel, ticagrelor), dipyridamole, and Glycoprotein IIb/IIIa
inhibitors (Abciximab, eptifibatide and tirofiban) (2).
3-Aspirin is given following coronary bypass surgery. It is also used in atrial

fibrillation, for intermittent claudication, for stable angina and acute coronary
syndromes, for use following placement of coronary stents and for use in stroke (2).
4-Clopidogrel monotherapy may be an alternative when aspirin is contra-indicated,

for example in those with aspirin hypersensitivity (2).
5-Clopidogrel, in combination with low-dose aspirin, is also licensed for:

A-Acute coronary syndrome without ST-segment elevation; in these
circumstances the combination is given for up to 12 months (2). Aspirin is
continued indefinitely (4).
B-Acute myocardial infarction with ST-segment elevation; the combination is

licensed for at least 4 weeks, but the optimum treatment duration has not been
established (2). Aspirin is continued indefinitely (4).
C-In patients undergoing percutaneous coronary intervention (with the

placement of a coronary stent), clopidogrel is used as an adjunct with aspirin (2).
The recommended duration of P2Y12 inhibitors for a patient undergoing PCI is
at least 12 months for patients receiving either a bare metal or drug-eluting stent
(4)
. Aspirin therapy should continue indefinitely (2).
16
D-Clopidogrel is also licensed, in combination with low-dose aspirin, in
patients with atrial fibrillation (and at least one risk factor for a vascular
event), and for whom warfarin is unsuitable (2).
6-Both prasugrel and ticagrelor are more potent than clopidogrel. Prasugrel
has the fewest significant drug–drug interactions of the oral P2Y12 inhibitors (4).
7-Abciximab, eptifibatide, or tirofiban may be administered in patients with ST

segment elevation myocardial infarction (STEMI) undergoing primary PCI who
are treated with unfractionated heparin (UFH) (4).
8-Aspirin is also used as an analgesic and antipyretic (2).
9-Pregnant women who are at high risk of developing preeclampsia , or if they

have had hypertension during a previous pregnancy; these women are advised to
take aspirin once daily [unlicensed indication] from week 12 of pregnancy until
the baby is born (2).
10-Owing to an association with Reye’s syndrome, aspirin-containing

preparations should not be given to children under 16 years, unless specifically
indicated, e.g. for Kawasaki disease (2).
11-Contra-indications of aspirin include: Active peptic ulceration . bleeding

disorders (antiplatelet dose) . children under 16 years (risk of Reye‘s syndrome) .
haemophilia . previous peptic ulceration (analgesic dose) and cardiac failure
(analgesic dose) (2).
12-Aspirin is contraindicated in history of hypersensitivity to aspirin or any

other NSAID—which includes those in whom attacks of asthma, angioedema,
urticaria, or rhinitis have been precipitated by aspirin or any other NSAID (2).
13-Aspirin tablet commonly formulated as enteric coated tablet to decrease GIT

irritation.
Antiplatelet drugs
1
17
Any extra notes:
1.11-Anticoagulants
1-Anticoagulants are used in the treatment and prophylaxis of thromboembolic
disorders (3).
2-Different types of anticoagulants are available (table 1-5).
Table 1-5: Types of anticoagulants

Parenteral anticoagulants Oral anticoagulants
1 Unfractionated Heparin (UFH) 1 Warfarin
2 Low molecular weight heparins Direct Oral Anticoagulants
(LMWHs) (dalteparin, enoxaparin and (DOACs)
tinzaparin) Dabigatran, Rivaroxaban,
3 Parenteral direct thrombin inhibitor 2 apixaban , and edoxaban
(lepirudin, bivalirudin, argatroban, and
desirudin)
4 Fondaparinux
1.11.1-Unfractionated Heparin (UFH)

1-UFH can be administered via the intravenous (IV) or subcutaneous (SC) route (6).
2-For the treatment of Venous thromboembolism (VTE), UFH is generally

given as a continuous IV infusion (6).
3-The activated partial thromboplastin time (aPTT) is the most widely used test in
clinical practice to monitor UFH. Traditionally, therapeutic aPTT range is defined
as 1.5 to 2.5 times the control aPTT value (4).
4-Bleeding is the primary adverse effect associated with anticoagulant drugs.

The most common bleeding sites include the GI tract, urinary tract, and soft tissues
(4)
.
5-If major bleeding occurs, discontinue UFH immediately and give IV protamine
sulfate. Long-term UFH has been reported to cause alopecia, priapism,
hyperkalemia, and osteoporosis (4).
6-Heparin-induced thrombocytopenia (HIT) is a serious immune-mediated

problem that requires immediate intervention (discontinue heparin and initiate
alternative anticoagulation with a parenteral direct thrombin inhibitor) (4).
18
1.11.2-Low-Molecular-Weight Heparins
1-Advantages of LMWHs over UFH include: (A) predictable anticoagulation
dose response, (B) improved SC bioavailability, (C) dose-independent
clearance, (D) longer biologic half-life, E) lower incidence of
thrombocytopenia, and (F) less need for routine laboratory monitoring (4).
2-LMWHs can be easily administered in the outpatient setting, thus enabling the
treatment of VTE at home (6).
3-Because LMWH anticoagulant response is predictable when given SC, routine

laboratory monitoring is unnecessary (4).
4-As with other anticoagulants, bleeding is the most common adverse effect of
LMWH therapy, but major bleeding may be less common than with UFH. If major
bleeding occurs, administer protamine sulfate IV, although it cannot neutralize the
anticoagulant effect completely (4).
5-Thrombocytopenia can occur with LMWHs, but the incidence of HIT is three
times lower than with UFH (4).
1.11.3-Warfarin
1-Warfarin inhibits the production of vitamin K–dependent clotting factors (4).
Warfarin has no effect on circulating coagulation factors that have been previously
formed, and its therapeutic antithrombotic activity is delayed for 5 to 7 days (6).
2-Warfarin also inhibits the anticoagulant proteins C and S. Reductions in the

concentration of natural anticoagulants before the clotting factors are depleted can
lead to a paradoxical hypercoagulable state during the first few days of
warfarin therapy. It is for this reason that patients with acute thrombosis should
receive a fast-acting anticoagulant (heparin, LMWH, or fondaparinux) while
transitioning to warfarin therapy (6).
4-Monitor warfarin therapy by the international normalized ratio (INR); the

recommended target INR for treatment of VTE is 2.5, with an acceptable range of
2 to 3(4).
5-In patients with acute VTE, a rapid-acting anticoagulant (UFH, LMWH, or

fondaparinux) should be overlapped with warfarin for a minimum of 5 days and
until the INR is greater than 2 and stable (6).
6-Hemorrhagic complications ranging from mild to severe and life-

threatening can occur at any body site. The GI tract and nose are the most
frequent sites of bleeding. Intracranial hemorrhage is the most serious complication
and often results in permanent disability and death (4).
19
7-Because of the large number of food–drug and drug–drug interactions with
warfarin, close monitoring and additional INR determinations may be indicated
whenever other medications are initiated, or discontinued, or an alteration in
consumption of vitamin K–containing foods is noted (4).
8-Vitamin K is the antidote of warfarin (9).
1.11.4-Direct Oral Anticoagulants:

1-These currently include two categories, direct thrombin (factor IIa) inhibitor
(DTI) (dabigatran) and direct Xa inhibitors (rivaroxaban, apixaban, and
edoxaban) (12).
2-As compared to warfarin, these oral anticoagulants have a more rapid onset,
shorter half-life, wider therapeutic window, and more predictable
pharmacokinetics (12).
3-These features allow for sole oral therapy without the need for an overlapping
parenteral agent (with the exception of edoxaban for VTE), no need for titration
or dose adjustments in patients with normal renal function, and no need for
routine monitoring (12).
4-Compared to warfarin, the target-specific anticoagulants have a lower risk of

intracranial hemorrhage (12).
5-Issues of concern include the lack of antidotes, and risk of thrombosis due to
missed doses (12).
6-Idarucizumab is a monoclonal antibody fragment used to reverse dabigatran

anticoagulation (10).
1.11.5-Parenteral direct thrombin inhibitors

1-Several injectable DTIs are available including lepirudin, bivalirudin,
argatroban, and desirudin (6).
2-Parenteral DTIs are considered the drugs of choice for the treatment of VTE in
patients with a diagnosis or history of HIT (6).
1.11.6-Parenteral Xa inhibitor (Fondaparinux)

1-Fondaparinux is a safe and effective alternative to LMWH for treatment of
VTE. It is also is approved for prevention of VTE following orthopedic or
abdominal surgery (4).
2-Patients receiving fondaparinux do not require routine coagulation testing (4).
21
Anticoagulants
1
Any extra notes:
1.12-Anti-arrhythmic drugs
1-Anti-arrhythmic drugs can be classified clinically into those that act on
supraventricular arrhythmias (e.g. verapamil), those that act on both
supraventricular and ventricular arrhythmias (e.g. amiodarone), and those that act
on ventricular arrhythmias (e.g. lidocaine) (2) (table 1-6) (13).
Table 1-6: classification of Anti-arrhythmic drugs according to principal site

of action
21
2-Atropine is used for bradycardia and AV nodal blockade. In patients with
hemodynamically unstable or unresponsive to atropine, epinephrine or dopamine
may be administered (6).
3-Adenosine is the drug of choice for pharmacologic termination of paroxysmal

supraventricular tachycardia (PSVT) (6).
4-Hemodynamically stable torsades de pointes is often treated with I.V

magnesium (6).
5-Hemodynamically unstable PSVT, ventricular tachycardia, atrial fibrillation,

torsades de pointes, or ventricular fibrillation (already hemodynamically unstable)
should be terminated immediately using direct current cardioversion (DCC) (6).
6-Amiodarone is the most commonly used antiarrhythmic agent. It is used for rate
and rhythm control of atrial fibrillation and to treat and prevent ventricular
arrhythmias (9).
7-Although amiodarone is the most commonly used antiarrhythmic, it should be

reserved for patients with life-threatening arrhythmias due to its substantial
toxicity (9) (table 1-7) (2).
Table 1-7: Some amiodarone side effects (2)

Side effects Comments
Most patients taking amiodarone develop corneal microdeposits
Corneal (reversible on withdrawal of treatment); these rarely interfere with
1 microdeposits vision, but drivers may be dazzled by headlights at night. However, if
vision is impaired or if optic neuritis or optic neuropathy occur,
amiodarone must be stopped to prevent blindness and expert advice
sought
1-Amiodarone contains iodine and can cause disorders of thyroid
function; both hypothyroidism and hyperthyroidism can occur.
Thyrotoxicosis may be very refractory, and amiodarone should
Thyroid usually be withdrawn at least temporarily to help achieve control;
2 function treatment with carbimazole may be required. Hypothyroidism can be
treated with replacement therapy without withdrawing amiodarone if
it is essential; careful supervision is required.
2-Thyroid function tests should be performed before treatment and
then every 6 months.
1-Amiodarone is also associated with hepatotoxicity and treatment
Hepatotoxicity should be discontinued if severe liver function abnormalities or
clinical signs of liver disease develop.
3
2-Liver function tests required before treatment and then every 6
months.
4 Pulmonary Pneumonitis should always be suspected if new or progressive
toxicity shortness of breath or cough develops in a patient taking amiodarone.
5 Peripheral Fresh neurological symptoms should raise the possibility of
neuropathy peripheral neuropathy.
22
8-Because of the possibility of phototoxic reactions, patients taking amiodarone
should be advised to shield the skin from light during treatment and for several
months after discontinuing amiodarone; a wide-spectrum sunscreen to protect
against both long-wave ultraviolet and visible light should be used (2).
9-Digoxin is a cardiac glycoside that increases the force of myocardial contraction

(so used for HF) and reduces conductivity within the atrioventricular (AV) node
(so used for atrial fibrillation or flutter) (2).
10-Digoxin does not improve survival in patients with HF but does provide
symptomatic benefits only (4) (digoxin is added for patients who remain
symptomatic despite an optimal HF regimen consisting of an ACE inhibitor or
ARB, β-blocker, and diuretic (6). Digoxin is also prescribed routinely in patients
with HF and concurrent atrial fibrillation (AF) (5) to slow ventricular rate regardless
of HF symptoms (6).
11-Loading dose of digoxin (Rapid digitalization) is usually given for atrial

fibrillation or flutter (2) (Roughly half of the total loading dose administered as the
first dose, with the remaining portion divided and administered every 6–8 hours
initially) (9).
12-Sotalol is used for ventricular and supraventricular arrhythmias (2).
Anti-arrhythmic drugs
1
Any extra notes:
23
1.13-Miscellaneous cardiovascular drugs
1.13.1-Fibrinolytic drugs
1-Thrombolytic drugs are indicated for any patient with acute myocardial
infarction (STEMI) for whom the benefit is likely to outweigh the risk of
treatment (2).
2-Alteplase should be given within 6–12 hours of MI symptom onset, reteplase

and streptokinase within 12 hours of symptom onset, but ideally all should be
given within 1 hour; use after 12 hours requires specialist advice. Tenecteplase
should be given as early as possible and usually within 6 hours of symptom onset
(2)
.
3-Alteplase, streptokinase and urokinase can be used for other thromboembolic

disorders such as deep-vein thrombosis and pulmonary embolism (2).
4-Alteplase is also used for acute ischaemic stroke (2).
5-Urokinase is also licensed to restore the patency of occluded intravenous

catheters and cannulas blocked with fibrin clots (2).
1.13.2-Antifibrinolytic drugs
1-Fibrin dissolution can be impaired by the administration of tranexamic acid,
which inhibits fibrinolysis. It can be used to prevent bleeding or to treat bleeding
associated with excessive fibrinolysis (e.g. in surgery, dental extraction, and
obstetric disorders) and in the management of menorrhagia (2).
2-Tranexamic acid may also be used in hereditary angioedema, epistaxis, and in

thrombolytic overdose (2).
1.13.3-Vasodilator antihypertensives (Hydralazine, Minoxidil,

Sodium nitroprussid)
1-Vasodilators have a potent hypotensive effect (2).
2-Hydralazine (i.v infusion) is used for hypertensive emergencies (including

during pregnancy) (2).
3-Hydralazine is given by mouth as an adjunct to other antihypertensives for the

treatment of resistant hypertension but is rarely used; when used alone it causes
tachycardia and fluid retention (2).
4-Hydralazine in combination with nitrate is also used for heart failure

(patients who cannot tolerate an ACE inhibitor or ARB, or in whom they are
contra-indicated, may be given ISDN with hydralazine. The combination may be
considered in addition to standard therapy with an ACE inhibitor and a β-blocker
in patients who continue to remain symptomatic (2).
24
5-Sodium nitroprusside is given by i.v infusion to control severe hypertensive
emergencies when parenteral treatment is necessary (2).
6-Minoxidil should be reserved for the treatment of severe hypertension resistant

to other drugs (2).
1.13.4-Centrally acting antihypertensive drugs

1-Methyldopa is a centrally acting antihypertensive; it may be used for the
management of hypertension in pregnancy (2).
2-Clonidine has the disadvantage that sudden withdrawal of treatment may cause
severe rebound hypertension. (Note: Clonidine is also used for prevention of
recurrent migraine and prevention of vascular headache) (2).
1.13.5-Sympathomimetics (Inotropic sympathomimetics,

Vasoconstrictor sympathomimetics)
1-The profound hypotension of shock must be treated promptly to prevent tissue
hypoxia and organ failure. Volume replacement is essential to correct the
hypervolemia associated with hemorrhage and sepsis but may be detrimental in
cardiogenic shock (2).
2-Depending on hemodynamic status, cardiac output may be improved by the use

of sympathomimetic inotropes such as adrenaline/epinephrine, dobutamine or
dopamine (2).
3-In septic shock, when fluid replacement and inotropic support fail to maintain
blood pressure, the vasoconstrictor noradrenaline/norepinephrine may be
considered (2).
4-Midodrine is a sympathomimetic agent, which acts on peripheral α-adrenergic

receptors to increase arterial resistance, resulting in an increase in blood pressure.
It is indicated for severe orthostatic hypotension due to autonomic dysfunction
when corrective factors have been ruled out and other forms of treatment are
inadequate (2).
5-Metaraminol is a vasoconstrictor sympathomimetic indicated for acute

hypotension (2).
1.13.6-Coagulation proteins
1-Human prothrombin complex, Factor IX fraction, Factor VIIa, Factor VIII
fraction are used to treat hemorrhage especially that associated with congenital
deficiencies of these factor proteins (2).
25
1.13.7-Peripheral vasodilators (e.g. Cilostazol, Pentoxifylline)
1-Peripheral vascular disease can be either occlusive (e.g. intermittent
claudication) in which occlusion of the peripheral arteries is caused by
atherosclerosis, or vasospastic (e.g. Raynaud’s syndrome) (2).
2-Cilostazol is licensed for use in intermittent claudication to improve walking (2).
3-Pentoxifylline is another agent approved by the FDA for the treatment

intermittent claudication (limited role) (5) (Pentoxifylline is not established as
being effective for the treatment of intermittent claudication or Raynaud‘s
syndrome) (2).
1.13.8-Others antianginal agents

1-Ranolazine is an anti-ischemic agent. A key distinction between ranolazine and
traditional antianginal agents is that it has no appreciable effect on heart rate
and BP makes the drug useful in patients in need of further antianginal therapy
(who remain symptomatic while on standard angina pharmacotherapy) but who
have marginal BP or heart rates preventing titration of conventional antianginal
agents (5, 14).
2-Nicorandil a potassium-channel activator with a nitrate component, has both

arterial and venous vasodilating properties and is licensed for the prevention and
long-term treatment of angina. Nicorandil may produce additional symptomatic
benefit in combination with other antianginal drugs [unlicensed indication] (2).
3-Ivabradine lowers the heart rate by its action on the sinus node. It is licensed for
the treatment of angina in patients who are in normal sinus rhythm in combination
with a β-blocker, or when β-blockers are contraindicated or not tolerated (2).
Note: Ivabradine, in combination with standard therapy including a β-blocker

(unless contra-indicated or not tolerated), is also licensed for mild to severe stable
chronic heart failure in patients who are in sinus rhythm (2).
1.13.9-Drugs for pulmonary arterial hypertension

1-Ambrisentan, Epoprostenol, bosentan, iloprost , macitentan, Riociguat,
Selexipag, sildenafil, and tadalafil are licensed for the treatment of pulmonary
arterial hypertension (2).
2-Bosentan is also licensed to reduce the number of new digital ulcers in patients
with systemic sclerosis and ongoing digital ulcer disease (2).
26
Miscellaneous cardiovascular drugs
1
Any extra notes:
References
1-Michael AM, Jason. Frequently prescribed medications. Copyright © 2012 by Jones & Bartlett
Learning, LLC.
2-BNF 74.
3-Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical
Press 2009.
4-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 10th edition.
2017.
5-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical use of drugs,
11th ed., 2018.
6-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 4th edition. 2016.
7-Michael R. Updated Heart Failure Guidelines Highlight Role of Entresto, Corlanor. pharmacy
times. 2016.
8-Lawrence A. Trissel. Handbook on injectable drugs - 15th ed. 2009.
Learning, LLC
10-ACCP Updates in Therapeutics® 2018: The Pharmacotherapy Preparatory Review and
Recertification Course.
11-David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease Management.
8th edition. 2006.
12-Cooper, Daniel H.; Krainik,. Washington Manual of Medical Therapeutics, The, 34 Edition.
Copyright 2014 .
13-Helen Williams.V Arrhythmia : part 1. The pharmaceutical journal (VOL 271) (2003):368-
370.
14-Edward T. Bope, et al, eds. Conn‘s Current Therapy . Copyright 2018.
27
Chapter Two: Gastro-intestinal System
2.1-Drugs for Inflammatory bowel disease.

Notes:
1-Chronic inflammatory bowel diseases (IBD) include Crohn’s disease (CD)
and Ulcerative colitis (UC) (1). UC is confined to the rectum and colon, while CD
can involve any part of the gastrointestinal (GI) tract (2).
2-The major types of drug therapy used in IBD are aminosalicylates,

glucocorticoids, immunosuppressive agents (azathioprine, mercaptopurine,
cyclosporine, and methotrexate), antimicrobials (metronidazole and
ciprofloxacin), and monoclonal antibodies (1) [(infliximab, adalimumab,
golimumab, certolizumab, natalizumab and vedolizumab) (see chapter 9) (3).
2.1.1-Aminosalicylates
1-Aminosalicylates include Sulfasalazine [a combination of 5-aminosalicylic
acid, (‗5-ASA‘) and sulfapyridine (acts as a carrier and believed to be responsible
for many of the adverse reactions to sulfasalazine)], and the safer sulfa-free
compounds [mesalazine (mesalamine)(5-ASA), balsalazide (a pro-drug of 5-ASA)
and olsalazine (a dimer of 5-ASA)] (1, 2, 4).
2-The aminosalicylates are among the most commonly used drugs for inducing
and maintaining remission in patients with IBD (5).
3-Mesalazine can be used topically as an

enema, to treat left-sided disease, or as a
suppository for treatment of proctitis.
Mesalazine can be given orally in slow-
release formulations that deliver
mesalamine to the small intestine and colon
(2)
.
4-The extent of disease should be

considered when choosing the route of
administration. If the inflammation is
distal, a rectal preparation is adequate but if the inflammation is extended,
systemic medication is required (1).
5-Enemas or suppositories should be administered at bedtime, preferably after a

bowel movement (4).
6-Oral aminosalicylates for the treatment of ulcerative colitis are available in

different preparations and release forms. The preparation and dosing schedule
should be chosen taking into account the delivery characteristics and suitability
for the patient (1).
28
7-Sulfasalazine is contra-indicated in salicylate hypersensitivity (1). Unlike
sulfasalazine, sulfa-free compounds are safe to use for patients with sulfonamide
allergies (2).
8-Blood count should be performed and the drug stopped immediately if there is
suspicion of a blood dyscrasia (1).
9-Patients receiving aminosalicylates, and their carers, should be advised to report

any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that
occurs during treatment (Blood disorders) (1).
10-Regarding mesalazine:
A-If it is necessary to switch a patient to a different brand of mesalazine, the
patient should be advised to report any changes in symptoms (1).
B-The manufacturers of some mesalazine gastro-resistant and modified-release

medicines (Asacol MR tablets, Ipocol, Salofalk granules) suggest that
preparations that lower stool pH (e.g. lactulose) might prevent the release
of mesalazine (1).
C-Granules should be placed on tongue and washed down with water without
chewing (1).
11-Olsalazine is associated with a higher incidence of secretory diarrhea than

other aminosalicylates (5).
12-Balsalazide and Olsalazine are taken after food (1).
13-Note: sulfasalazine is also used for rheumatoid arthritis (it is one of the
Disease-Modifying Antirheumatic Drugs) (1).
Aminosalicylates
Scientific name Trade names Dosage form(s)
1
Any extra notes:
29
2.2-Proton pump inhibitors (PPIs)
1-Drug action: PPI suppresses gastric acid secretion by inhibition of the H+/K+-
ATPase in the gastric parietal cell (6).
2-PPIs are the most potent inhibitors of gastric acid secretion. PPIs include
omeprazole, lansoprazole, rabeprazole, pantoprazole, and esomeprazole (4).
3-PPIs are used for the treatments of gastric and duodenal ulcers; they are also
used in combination with antibacterials for the eradication of Helicobacter
pylori (a bacteria that is common cause of ulcer). PPIs can be used for the
treatment of dyspepsia and gastro-oesophageal reflux disease. They are also
used for the prevention and treatment of NSAID-associated ulcers (1).
4-A PPI can be used to reduce the degradation of pancreatic enzyme supplements
in patients with cystic fibrosis. They can also be used to control excessive secretion
of gastric acid in Zollinger–Ellison syndrome; high doses are often required (1).
5-Regimen for the eradication of Helicobacter pylori usually composed of PPI,

clarithromycin, and either amoxicillin or metronidazole for 10–14 days. This
regimen is called (triple therapy) (4).
(amoxicillin-containing regimen is preferred. In penicillin-allergic patients,
metronidazole is substituted for amoxicillin) (4).
6-Sequential therapy is a form of H. pylori eradication therapy in which the

antibiotics are administered in a sequence rather than together. Treatment typically
consists of a PPI and amoxicillin for 5 days followed by a PPI, clarithromycin, and
tinidazole (or metronidazole) for an additional 5 days (4).
7-PPIs are most effective when taken 30 to 60 minutes before meals (2).The once
daily dose usually given in the morning before meals. Large doses should be
given in 2 divided doses (1).
8-Various PPI dosage forms and formulations exist and include the enteric-coated
granules contained in gelatin capsules (omeprazole, esomeprazole, and
lansoprazole), and delayed release enteric-coated tablets (rabeprazole,
pantoprazole, omeprazole), delayed-release oral suspension (lansoprazole), and
an immediate-release formulation (omeprazole and sodium bicarbonate capsules
and powder for oral suspension). The enteric coating prevents degradation of the
drug in stomach acid (1). IV formulations are also available for some PPIs (1, 2).
Note: The sodium bicarbonate raises intragastric pH, permitting rapid absorption
of omeprazole from the duodenum (7). It should be taken on an empty stomach at
least 1 hour before a meal (4).
31
9-Special administration:
A-Orodispersible lansoprazole tablets should be placed on the tongue, allowed
to disperse and swallowed, or may be swallowed whole with a glass of water.
Alternatively, tablets can be dispersed in a small amount of water and
administered by an oral syringe or nasogastric tube (1).
B-Losec MUPS®: For administration by mouth, swallow whole, or disperse

Losec MUPS® tablets in water, or mix capsule contents or Losec MUPS®
tablets with fruit juice or yoghurt (1).
C-For patients who are unable to swallow the capsule or for pediatric
patients, there are several alternative administration methods available. The
contents of the delayed-release capsules can be mixed in applesauce or placed
in orange juice. If a patient has a nasogastric tube, the contents of an
omeprazole capsule can be mixed in 8.4% sodium bicarbonate solution.
Esomeprazole granules can be dispersed in water. Esomeprazole, omeprazole,
and pantoprazole are also available in a delayed-release oral suspension powder
packet, and lansoprazole is available as a delayed-release, orally disintegrating
tablet (4).
10-PPIs can increase the risk of fractures (particularly when used at high doses
for over a year in the elderly). Patients at risk of osteoporosis should maintain an
adequate intake of calcium and vitamin D and if necessary, receive other
preventative therapy (1).
11-Esomeprazole, and omeprazole are predicted to decrease the efficacy of

clopidogrel (By inhibiting clopidogrel conversion to its active form) (avoid )(1, 4) .
PPIs
Scientific names Trade name Dosage form
Any extra notes:
31
2.3-Histamine-2 Receptor Antagonists (H2RAs)
1-Drug action: H2RAs reduce gastric acid output as a result of histamine H2-
receptor blockade (1).
2-H2RAs include cimetidine, ranitidine, famotidine, and nizatidine (4).
3-H2RAs are used for the treatments of gastric and duodenal ulcers. They can be
used for the treatment of dyspepsia and gastro-oesophageal reflux disease (1).
4-Aspiration of gastric contents (Mendelson‘s syndrome) is a potential cause of

morbidity and mortality associated with anesthesia, especially in obstetrics and in
emergency surgery (8). H2RAs also reduce the risk of acid aspiration (1).
5-Cimetidine has been used alone or with an antihistamine (H1-antagonist) in

various skin disorders. H2RAs such as cimetidine and ranitidine have produced
improvement in certain types of urticaria (8).
6-Cimetidine inhibits several CYP450 isoenzymes, resulting in numerous drug

interactions (e.g., theophylline, warfarin, and clopidogrel) (4). Avoidance of the
combination, or a reduction in the dosage of these drugs may be required (8).
7-Ranitidine has less potential for hepatic CYP450 drug interactions, while
famotidine and nizatidine do not interact with drugs metabolized by the hepatic
CYP450 pathway (2).
8-Cimetidine has demonstrated weak antiandrogenic effects, and its use in high
doses has been associated with gynecomastia and impotence in men. This effect
is reversible with discontinuation of the medication or by switching to another
H2RA (2).
9-Regaeding H2RAs use for gastro-oesophageal reflux disease (GERD):

Tolerance to the gastric antisecretory effect may develop when H2RAs are
taken daily (versus as needed) and may be responsible for diminished efficacy.
Therefore, it is preferable to take an H2RA on an as needed basis rather than
regularly every day (7).
H2RAs
Scientific names Trade name Dosage form
32
Any extra notes:
2.4-Antacids:
1-Antacids are basic compounds that neutralize hydrochloric acid in the gastric
secretions. They are used in the symptomatic management of gastrointestinal
disorders associated with gastric hyperacidity such as dyspepsia, GERD, and
peptic ulcer disease (8).
2-Antacid agents include a variety of aluminum, magnesium, and calcium

products available as single and combination therapy preparations in multiple
dosage forms (6).
3-Antacids are best given when symptoms occur (i.e. when required) or are
expected, usually between meals and at bedtime (1). When taken 1 h after a meal,
antacids may act for up to 3 h compared with only 30 min–1 h if taken before
meals (9).
4-Liquids and powders generally provide faster relief and have greater
neutralizing capacity than tablets. Advantages of tablets over liquids include ease
of portability and administration (10). It might be appropriate for the patient to have
both; the liquid could be taken before and after working hours, while the tablets
could be taken during the day for convenience (9).
5-Tablets should not be swallowed whole; they should be chewed to initiate

disintegration or sucked to provide a relatively slow but sustained delivery of
antacid to the stomach (10).
6-Interactions:
A-Antacids can affect the absorption of a number of drugs (via chelation and
adsorption) (11). This interactions can usually be avoided when potentially
interacting drugs are separated by at least 2 hours (7).
B-Antacids also interact with enteric-coated tablets, capsules and granules

(Enteric coatings may be disrupted prematurely in the presence of antacids,
causing unwanted release of the drug in the stomach) (10).
7-Side effects of antacids:

A-AL-containing antacids tend to be constipating. Mg-containing antacids tend
to cause osmotic diarrhea and are useful in patients who are slightly
constipated. Thus combination products of AL and Mg salts cause minimum
bowel disturbances (9).
33
B-Antacids containing sod. Bicarbonate should be avoided in patients if
sodium intake should be restricted (e.g. in patient with heart failure,
hypertension,…..) (9) and during pregnancy (3).
C-Calcium carbonate: It acts quickly, has a prolonged action and is a potent

neutralizer of acid. It can cause acid rebound and, if taken over long periods at
high doses, can cause hypercalcaemia and so should not be recommended for
long-term use (9).
8-Other drugs that may be combined with antacid formulations include

simeticone, which acts as a defoaming agent to reduce excess gas in the stomach,
and alginates, which form a gel or foam on the surface of the stomach contents
thereby impeding reflux and protecting the oesophageal mucosa from acid
attack (8).
Antacids (including those combined with simethicone, and alginate)

Scientific names Trade names Dosage form
1
Any extra notes:
2.5-Laxatives:
1-Laxatives (purgatives or cathartics) promote defecation and are used in the
treatment of constipation and for bowel evacuation before investigational
procedures such as endoscopy or radiological examination, or before surgery (8)
to ensure the bowel is free of solid contents (1).
(10)
2-Laxatives can be classified into groups depending on their mode of action
(table 2-1).
34
Table 2-1: types of laxatives
Type of laxative Example(s) Approximate onset
of action
1-Stimulant laxative Senna, Bisacodyl, Sodium Oral:6-12hours (9)
picosulfate, and Glycerin (supp.) Rectal: within 1
hour (9)
2-Bulk-forming Methylcellulose, Bran , Sterculia 12 -24 hours, but
laxative and Ispaghula (Metamucil®) onset may be
delayed as long as
72 hours (7)
3-Lubricant (faecal Liquid paraffin 6-8 hours (7)
softeners)
4-Osmotic laxative Lactulose 1-2 days (9)
5-Othrs Linaclotide (guanylate cyclase-C receptor agonist).
Lubiprostone (chloride-channel activator), Prucalopride
(selective serotonin 5HT4-receptor agonist with
prokinetic properties) (1).
2.5.1-Stimulant laxatives:
1-Stimulant laxatives are thought to act mainly by stimulating the intestinal
mucosa to secrete water and electrolytes (12).
2-The main adverse effects of stimulant laxatives are griping and intestinal
cramps. Prolonged use may result in loss of colonic smooth muscle tone (10) .
However, many experts now believe that the risk of long-term use of stimulant
laxatives use have been overestimated and they are safe for daily use) (13).
3-Bisacodyl tablet is enteric-coated; therefore, it should be swallowed whole and

should not be taken within one hour of antacid or milk as this will lead to
dissolution of the coating and release of the drug into the stomach and cause
gastric irritation (10).
4-Senna is excreted via the kidney and may color the urine a yellowish-brown to
red color depending on its PH (12).
5-Senna is secreted in breast milk, and large dosages may cause increased gastric
motility and diarrhea in breastfed infants. Breastfeeding mothers should, therefore,
avoid this laxative (12). (However BNF-74 states that specialist sources indicate
suitable for use in breast-feeding in infants over 1 month (1)).
6-Usual Doses:
Bisacodyl 5 mg tab. Adult dose: usually 1-2 tablets (usually take at night to
produce the effect next morning).
While the dose of supp. Is one supp. (usually in the morning) (1, 10).
35
Senna tab. Adult dose: usually 2 tablets (usually take at night to produce the
effect next morning) (10, 11).
Glycerin suppositories: The patient should expect to have bowel movement
quickly (within one hour). Varying sizes are made: the 1 gm suppositories are
designed for infants, 2 gm for children and the 4 gm for adults (11).
2.5.2-Bulk-forming laxative:
1-Bulk laxatives are those that most closely resemble the normal physiological
mechanisms involved in bowel evacuation. Bulk laxatives work by swelling in the
gut and increasing faecal mass so that peristalsis is stimulated (13).
2-The laxative effect can take several days to develop (13).
3-Bulk laxatives should not be taken immediately before going to bed, because
there may be a risk of oesophageal blockage if the patient lies down directly after
taking them (10).
4-When recommending the use of a bulk laxative, the pharmacist should advise
that an increase in fluid intake would be necessary (13).
5-Adverse effects and disadvantages are relatively minor. They include:
–Risk of oesophageal and intestinal obstruction if preparations are not taken
with sufficient water.
– Abdominal distension and flatulence.
– They may not be suitable for patients who must restrict their fluid intake
severely (12).
6-Bulk-forming drugs are useful in controlling diarrhea associated with

diverticular disease (1).
2.5.3-Liquid paraffin:
Liquid paraffin is considered to have a limited usefulness as an occasional laxative
in situations where straining at stool must be avoided (for example, following an
operation or a myocardial infarction), but it has several drawbacks that make it
unsuitable for regular use (12) (it should never be recommended because other, safer
and more effective medications are available) (11):
-It can seep from the anus and cause irritation.
-It may interfere with the absorption of fat soluble vitamins.
-It is slightly absorbed into the intestinal wall, where it may set up foreign-body
granulomatous reactions.
-It may enter the lung through aspiration and cause lipoid pneumonia (12).
2.5.4-Lactulose:
1-It can be taken by all age group, have no drug interactions and can be safely used
in pregnancy (11). However, there are some factors that may deter patients from
using Lactulose: It may take 72 hours of regular dosing to produce an effect. It is
intensely sweet in taste which makes it more palatable for children, to whom it
can be given safely (10).
36
2-Adult laxative dose (1): 15 ml twice daily.
3-Serious adverse effects with lactulose are rare. Relatively minor side-effects
occur in about 20% of patients taking full doses and include flatulence, cramp and
abdominal discomfort, particularly at the start of treatment (12).
4-Lactulose syrup should be used with caution in diabetic patients because it

contains lactose and galactose (14).
5-Lactulose produces an osmotic diarrhea of low faecal pH, and discourages the
proliferation of ammonia-producing organisms. It is therefore useful in the
treatment of hepatic encephalopathy (1).
2.5.5-Product selection guidelines (table 2-2).
Table 2-2:Product selection guidelines

Patient Preferred laxative
Pregnant women Bulk-forming laxative. Lactulose may be used (1, 10, 13)
Breast-feeding mother Bulk-forming laxative, Lactulose (11)
Children Glycerin(supp.) (9), Lactulose (10)
Advanced age(elderly) Bulk-forming laxative, Also Lactulose and Glycerin
(supp.) are safe (7).
Laxatives (try to include the different types of laxatives )

Scientific name Trade names Type Dosage form(s)
1
Any extra notes:
37
2.6-Antidiarrhoeals
The priority in acute diarrhea is the prevention or reversal of fluid and electrolyte
depletion. This is particularly important in infants and elderly patients. Oral
rehydration preparations are used in the prevention or reversal of fluid and
electrolyte depletion. Severe depletion of fluid and electrolytes requires immediate
admission to hospital and urgent replacement (8).
2.6.1-Antimotility drugs
[Loperamide , Co-phenotrope (Diphenoxylate+Atropine)]
Note: Atropine is included at a subtherapeutic dose to discourage abuse
(unpleasant antimuscarinic effects will be experienced if higher than recommended
doses are taken)] (12).
1-Antimotility drugs are not recommended for acute diarrhea in young children (1).
In the UK, diphenoxylate hydrochloride is not licensed for children under 4 years
of age. In the UK, loperamide is not licensed for children under 4 years of age.
In the USA, loperamide is not recommended for children under the age of 2 years
(8)
.
2-Adult doses :
Loperamide: Initially 4 mg (2 tablets or capsules) , followed by 2 mg (1 tablet or
capsule) to be taken after each loose stool; usual dose 6–8 mg daily; maximum 16
mg per day (1).
Co-phenotrope: Initially 4 tablets, followed by 2 tablets every 6 hours until
diarrhea controlled (1).
2.6.2-Adsorbents (pectin +kaolin)
1-Adsorbents such as kaolin are not recommended for acute diarrheas (1).
2-Kaolin can form insoluble complexes with some drugs in the gastrointestinal
tract and reduce their absorption; oral doses should not be taken at the same
time (8).
Table 2-3:Amount of rehydration
2.6.3-Oral rehydration solution solution to be offered to patients (8).
(ORS) Age Quantity of solution (per
1-A premixed solutions (7) or watery stool)
sachets of powder for reconstitution Under 1 year 50 mL (quarter of a glass)
are available; these contain sodium 1–5 years 100 mL (half a glass)
as chloride and bicarbonate, 6–12 years 200 mL (one glass)
glucose and potassium (9). Adult 400 mL (two glasses
2-Only water should be used to make the solution and that boiled and cooled
water should be used for children < 1 year (9).
38
3-To avoid risk of possible exposure to further infection, the solution should be
discarded not later than 1 hour after reconstitution, or it may be kept for up to 24
hours if stored in a refrigerator (10).
4-Table 2-3 provides the volumes required per watery stool (9).
2.6.4-Probiotics (dietary supplement):

Probiotics are dietary supplements containing bacteria (including several
Lactobacillus species) that may promote health by enhancing the normal
microflora of the GI tract while resisting colonization by potential pathogens (5).
Probiotics have been shown to decrease the duration of infectious and
antibiotic-induced diarrhea (AAD) in adults and children (however; the use of
probiotics to treat and prevent AAD is controversial) (4).
2.6.5-Use of zinc in children with diarrhea:

Several large studies performed in developing countries have shown that daily
zinc supplementation in young children with acute diarrhea reduces both the
duration and severity of diarrhea. The WHO/UNICEF recommends that children
with acute diarrhea also receive zinc (10 mg of elemental zinc/day for infants
younger than 6 months; 20 mg of elemental zinc/day for older infants and children)
for 10 to 14 days (7, 13).
Antidiarrheals
1
Any extra notes:
2.7-Antispasmodics
1- Antispasmodics are drugs used for their relaxant action on smooth muscle. They
play a role in the management of gastrointestinal spasm and irritable bowel
syndrome (IBS) as well as other disorders associated with smooth muscle spasm
(8)
.
2-Antispasmodics include antimuscarinics (e.g. Hyoscine butylbromide). Other

antispasmodics (mebeverine, Alverine citrate, and peppermint oil) are used to
relieve pain in irritable bowel syndrome (1).
39
3-Conerning IBS (1):
A-Laxative (excluding lactulose as it may cause bloating) can be used to treat
constipation in IBS.
B-Loperamide is the first-line choice of anti-motility drug for relief of

diarrhea in IBS.
C-A low-dose tricyclic antidepressant, such as amitriptyline, can be used for

abdominal pain or discomfort as a second line option in patients who have not
responded to antispasmodics. A selective serotonin reuptake inhibitor may
be considered in those who do not respond to a tricyclic antidepressant.
Antispasmodics
1
Note: antichloinergics may be combined with benzodiazepine (librax®) or

phenothiazine (stelabid®) and they are used for gastrointestinal disorders
associated with anxiety; and for irritable bowel syndrome. Also they may be
combined with an analgesics.
Compound antichloinergics
Trade names Scientific name Dosage form
Librax®
Stelabid®
Antispasmine-
co®
Riabal-co®
Any extra notes:
41
2.8-Nausea and vomiting
1-Prochlorperazine, metoclopramide and domperidone are used to treat or
prevent nausea and vomiting (1).
2-Cinnarizine is used to prevent motion sickness where the dose is taken 2 hours
before travel then every 8 hours if required (1).
3-Domperidone has the advantage over metoclopramide and the

prochlorperazine of being less likely to cause central effects such as dystonic
reactions (a tetanus-like reaction) because it does not readily cross the blood-
brain barrier (1).
4-Granisetron and ondansetron (5HT3-receptor antagonists) are of value in the

management of nausea and vomiting in patients receiving cytotoxics and in
postoperative nausea and vomiting (1).
5-Dexamethasone has antiemetic effects and it is used in vomiting associated

with cancer chemotherapy. It can be used alone or with metoclopramide,
prochlorperazine, lorazepam, or a 5HT3-receptor antagonist (1).
6-Hyperemesis gravidarum (a severe nausea and vomiting during pregnancy) (4)

is a more serious condition, which requires regular antiemetic therapy,
intravenous fluid and electrolyte (1).
7-Domperidone, metoclopramide, 5HT3-receptor antagonists, and the

phenothiazines (except the antihistamine phenothiazine promethazine) are
ineffective in motion sickness (2).
8-I.V Metoclopramide doses should be administered as a slow bolus over at least

3 minutes. Oral liquid formulations should be given via an appropriately designed,
graduated oral syringe to ensure dose accuracy (1).
9-Metoclopramide dose: Adult (body-weight up to 60 kg): Up to 500 mcg/kg

daily in 3 divided doses. Adult (body-weight 60 kg and above): 10 mg up to 3
times (1).
10-Side effects:
A-Cinnarizine may cause drowsiness which may affect performance of skilled
tasks (e.g. cycling, driving) (1).
B-Domperidone is associated with a small increased risk of serious cardiac

side-effects (arrhythmia). Patients and their carers should be told how to
recognize signs of arrhythmia and advised to seek medical attention if
symptoms such as palpitation or syncope develop (1).
41
C-Metoclopramide can induce acute dystonic reactions involving facial and
skeletal muscle spasms and oculogyric crises. These dystonic effects are more
common in the young (especially girls and young women) and the very old;
they usually occur shortly after starting treatment with metoclopramide and
subside within 24 hours of stopping it (1).
Antiemetics
Scientific name Trade names Dosage form(s)
1
Any extra notes:
2.9-Anti-obesity drugs
1-Orlistat is a gastric and pancreatic lipase inhibitor that limits the absorption of
dietary fat (1).
2-It is used together with dietary modification in the management of obesity , i.e.
in patients with a BMI of 30 kg/m2 or greater. It may also be used in overweight
patients with a BMI of 27 kg/m2 or more if there are associated risk factors (such
as type 2 diabetes, hypertension) (1).
3-Orlistat is given in a usual dose of 120 mg orally three times daily, immediately
before, during, or up to 1 hour after meals. If a meal is missed or contains no
fat, the dose should be omitted (1).
4-Treatment with orlistat may also be used to maintain weight loss rather than to
continue to lose weight (1).
5-Discontinuation of treatment with orlistat should be considered after 12 weeks if

weight loss has not exceeded 5% since the start of treatment (1).
42
6-Orlistat may reduce the absorption of fat-soluble vitamins (A, D, E, and K)
and patients should take a multivitamin supplement that contains these vitamins.
The supplement should be taken once a day at least 2 hours before or after the
administration of orlistat, such as at bedtime (2).
7-Liraglutide (Saxenda®) [a glucagon-like peptide-1 (GLP-1) receptor agonist].

A-Liraglutide, is an injectable medication, FDA-approved for long-term
obesity management as an adjunct to lifestyle modification. When used for
obesity, the dose is titrated to 3 mg daily (2).
B-If the patient has not experienced ≥4% weight loss by 16 weeks after
initiating therapy, the drug should be discontinued (2).
C-It is also marketed under the brand name Victoza at a dose of 1.8 mg daily
for the treatment of type 2 diabetes (2).

Orlistat
Liraglutide
Any extra notes:
2.10-Local preparations for anal and rectal disorders

1-These products are used mainly for hemorrhoids and anal fissure (1).
2-They are usually formulated as ointments and creams or suppositories.

Ointments and creams can be used for internal and external hemorrhoids while
suppositories are used for internal hemorrhoids. However both are used twice
daily (morning and evening) and after each bowel movement (9).
3-Many people prefer suppositories, but these products are often not effective
because they tend to slip into the rectum and melt, thus bypass the anal canal
where the medication is needed. In general ointments and creams are preferred
over suppositories (13).
4-When used intrarectally, the ointment may be inserted using an applicator or

finger but the applicator is preferred because it can reach an area where the
finger cannot reach. The applicator should be lubricated by the ointment before
insertion (5).
43
5-Topical preparations that contain a combination of local anaesthetics,
corticosteroids, astringents, lubricants, and antiseptics are available. They can
offer symptomatic relief of local pain and itching (1).
6-Long-term use of corticosteroid creams can cause ulceration or permanent

damage due to thinning of the perianal skin and should be avoided (1).
Local preparations for anal and rectal disorders

1
Any extra notes:
2.11-Liver disorders (and related conditions), exocrine pancreatic

insufficiency.
1-Ursodeoxycholic acid is a naturally occurring bile acid. It is used for the
dissolution of cholesterol-rich gallstones in patients with functioning gallbladders.
Ursodeoxycholic acid is also used in primary biliary cirrhosis (8) (It slows disease
progression) (1).
2-Terpenes (Borneol with camphene, cineole, menthol, menthone and pinene)

(Rowachol® Capsule) are used for Biliary disorders (to be taken before food) (1).
3-Exocrine pancreatic insufficiency can result from chronic pancreatitis, cystic

fibrosis, obstructive pancreatic tumours, coeliac disease, Zollinger-Ellison
syndrome, and gastrointestinal or pancreatic surgical resection.
Exocrine pancreatic insufficiency is characterized by reduced secretion of
pancreatic enzymes into the duodenum. The main clinical manifestations are
maldigestion and malnutrition, associated with low circulating levels fat-soluble
vitamins. Patients also present with gastro-intestinal symptoms such as diarrhea,
abdominal cramps and steatorrhoea (1).
4-Pancreatic enzyme replacement therapy with pancreatin is the mainstay of

treatment for exocrine pancreatic insufficiency.
44
Pancreatin contains the three main groups of digestive enzymes: lipase, amylase
and protease. These enzymes respectively digest fats, carbohydrates and proteins
so that they can be absorbed and utilized by the body. Pancreatin should be
administered with meals and snacks (or immediately before or after food) (1).

Ursodeoxycholic acid
Pancreatin
2.12- Administration of rectal suppositories and enemas (7) :
Suppositories
1-Gently squeeze the suppository to determine if it is firm enough to insert. Chill a soft
suppository by placing it in the refrigerator for a few minutes or by running it under cool
running water.
2-Remove the suppository from its wrapping.
3-Dip the suppository for a few seconds in lukewarm water to soften the exterior.
4-Lie on your left side with knees bent or in the knee-to-chest position (see drawings A and
B). Position A is best for self-administration of a suppository. Small children can be held in
a crawling position.
5-Relax the buttock just before inserting the suppository to ease insertion. Gently insert the
tapered end of the suppository high into the rectum. If the suppository slips out, it was not
inserted past the anal sphincter (the muscle that keeps the rectum closed).
6-Continue to lie down for a few minutes, and hold the buttocks together to allow the
suppository to dissolve in the rectum. The parent/caregiver may have to gently hold a
child's buttocks closed.
7-Remember that the medication is most effective when the bowel is empty. Try to avoid a
bowel movement after insertion of the suppository for up to 1 hour so that the intended
action can occur.
Enemas
1-If someone else is administering the enema, lie on your left side with knees bent or in the
knee-to-chest position (see drawings A and B). Position A is preferred for children older
than 2 years. If self-administering the enema, lie on your back with your knees bent and
buttocks raised (see drawing C). A pillow may be placed under the buttocks.
2-If using a concentrated enema solution, dilute solution according to the product
instructions. Prepare 1 pint (500 mL) for adults and 1/2 pint (250 mL) for children.
3-Lubricate the enema tip with petroleum jelly or other non-medicated ointment/cream.
Apply the lubricant to the anal area as well.
4-Gently insert the enema tip 2 (recommended depth for children) to 3 inches into the
rectum.
5-Allow the solution to flow into the rectum slowly. If you experience discomfort, the flow
is probably too fast.
6-Retain the enema solution until definite lower abdominal cramping is felt. The
parent/caregiver may have to gently hold a child's buttocks closed to prevent the solution
from being expelled too soon.
45
References
1-BNF 74.
11th ed., 2018.
3-Edward T. Bope, et al, eds. Conn‘s Current Therapy. Copyright 2018.
2017.
Learning, LLC.
7-American pharmacists association. Handbook of Non-prescription drugs: An Interactive
Approach to Self-Care. 18th edition. 2016.
Press 2009.
9-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the pharmacy . A guide
to the managements of common illness. 7th edition. 2014.
10-Nathan A. Non-prescription medicines. 4th edition. London: Pharmaceutical Press. 2010.
11-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 4th edition. 2017.
12-Nathan A. fasttrack. Managing Symptoms in the Pharmacy. Pharmaceutical Press. 2008.
13-Canadian American pharmacists association (CPhA). CTMA: Compendium of Therapeutics
for Minor Ailments. 2014.
14-Virginia P A. Pharmacotherapeutics for Advanced Practice A Practical Approach. 3rd
edition. 2013.
46
Chapter Three: Respiratory System
3.1-Respiratory system, drug delivery
3.1.1-Inhalation
1-This route delivers the drug directly to the airways; the dose required is smaller
than when given by mouth and side effects are reduced (1).
2-Inhaler devices include pressurized metered-dose inhalers (MDI), breath

actuated inhalers, and dry powder inhalers (DPI). Many patients can be taught
to use a pressurized MDI effectively but some patients, particularly the elderly and
children, find them difficult to use. Spacer devices can help such patients because
they remove the need to co-ordinate actuation with inhalation (1).
3-DPI may be useful in adults and children over 5 years who are unwilling or
unable to use a pressurized MDI. Alternatively, breath-actuated inhalers are
suitable for adults and older children (1).
4-On changing from a pressurized MDI to a DPI dry powder inhaler, patients
may notice a lack of sensation in the mouth and throat previously associated with
each actuation. Coughing may also occur (1).
5-Spacer devices remove the need for coordination between actuation of a

pressurized MDI and inhalation. Spacer devices are particularly useful for patients
with poor inhalation technique, for children, for patients requiring high doses of
inhaled corticosteroids, for nocturnal asthma, and for patients prone to candidiasis
with inhaled corticosteroids (1).
6-Nebulizers:
A-A nebulizer converts a solution of a drug into an aerosol for inhalation.
Solutions for nebulization are available for use in severe acute asthma or
COPD (1).
B-They are administered over 5–10 minutes from a nebulizer usually driven by
oxygen in hospital (1).
C-Nebulization may be carried out using an undiluted nebulizer solution or it

may require dilution beforehand. The usual diluent is sterile sodium chloride
0.9% (physiological saline) (1).
3.1.2-Oral
The oral route is used when administration by inhalation is not possible. Systemic
side-effects occur more frequently when a drug is given orally rather than by
inhalation (1).
47
3.1.3-Parenteral
Drugs such as β2 agonists, corticosteroids, and aminophylline can be given by
injection in acute severe asthma when administration by nebulization is inadequate
or inappropriate (1).
An example of a metered A metered dose inhaler A metered dose inhaler attached

dose inhaler. attached to a spacer to a spacer device with a mask
device.
An example of a Breath actuated inhaler An example of an Accuhaler.

Turbohaler
Figure 3-1: Examples of respiratory system drug delivery devices (2).
48
3.1.4-Decice-specific patient counseling (2).
How to use a metered dose inhaler How to use a metered dose inhaler
with the aid of a spacer device
1. First assemble the spacer device if necessary as
directed by the manufacturer (with or without a
1. Remove the cap covering the mouthpiece and face mask).
check that there is no fluff or dirt in the 2. Remove the cap from the inhaler and insert the
mouthpiece. mouthpiece of the inhaler into the opening at the
2. Shake the inhaler. end of the spacer.
3. If the inhaler is new or has not been used for 3. Hold the spacer and inhaler together and shake.
some time it will need to be tested. To test: Hold 4. Breathe out.
the inhaler away from body. Press the top of the 5. Put the spacer mouthpiece in the mouth and seal
aerosol canister once. A fine mist should be with the lips.
puffed into the air. The inhaler is now ready to 6. Press the inhaler once and then breathe in and
use. out four or five times.
4. Tilt head back slightly. 7. Further doses may be taken waiting a few
5. Breathe out gently. seconds between puffs.
6. Place the mouthpiece in the mouth between the 8. Separate the spacer and inhaler. Replace the
teeth (do not bite). Close lips around the inhaler cap and store until next dose.
mouthpiece. How to use an Accuhaler
7. Start to breathe in slowly through the
1. With the Accuhaler mouthpiece facing you, slide
mouth, at the same time press down on
the lever away until it clicks. This will have loaded
the inhaler to release the medicine in to the lungs.
a dose ready for inhalation and the Accuhaler will
8. Hold breath for between 5 and 10 seconds, then
move the dose counter on.
breathe out slowly.
2. Hold the Accuhaler flat and breathe out
9. If a second dose is required, wait approximately
away from the inhaler.
30 seconds and repeat the process.
3. Seal lips around the Accuhaler mouthpiece and
10. Replace the cap and if the inhaler is a
inhale deeply.
corticosteroid inhaler, rinse the mouth out with
4. Remove inhaler from the mouth and hold
water.
breath as long as is comfortable.
5. Slide the thumb grip back towards you to
close the inhaler.
6. For further doses repeat above steps.
How to use a Turbohaler How to use a Breath actuated inhaler
1. Unscrew the cover and remove it.
2. Hold the Turbohaler upright with one hand and
with the other twist the grip in one direction as far
as it will go. 1. Shake the inhaler.
3. Now twist back as far as it will go – a click 2. Hold the inhaler upright and open the cap.
should be heard, showing the inhaler is primed 3. Breathe out, away from the inhaler.
and ready for use. 4. Put the mouthpiece in the mouth, seal lips
4. Breathe out gently. around the mouthpiece.
5. Place the mouthpiece between the lips and 5. Breathe in steadily through the mouthpiece.
breathe in through the mouth as deeply and as 6. Hold breath for about ten seconds.
hard as possible. 7. Keeping the inhaler upright, close the cap.
6. Remove the inhaler from the mouth and breathe 8. For further doses repeat the above steps.
out slowly.
7. Replace the cover.
8. Repeat the above steps if more than one puff is
required.
49
3.2-Drugs used for asthma and/or Chronic Obstructive Pulmonary
Disease (COPD)
Drugs used for asthma and COPD are summarized in table 3-1. Stepwise approach
for managing asthma in adults is shown in figure 3-1.
Table 3-1: Drugs used for asthma and/or COPD

Class Example(s) Route
Salbutamol (called albuterol Systemic
1 Bronchodilators β2-agonists in USA) terbutaline, and
Formoterol and salmeterol inhaled
Antimuscarinic Ipratropium, and Tiotropium Inhaled
Methylxanthines Theophylline and as Systemic
aminophylline
2 Corticosteroids Inhaled CS Beclometasone, Inhaled
(CS) Mometasone, Budesonide,
Fluticasone.
Systemic CS Prednisolone, Systemic
Hydrocortisone
3 Leukotriene Receptor Antagonists zileuton, montelukast and Oral
(Leukotriene Modifiers) zafirlukast
4 Mast Cell Stabilizers Cromolyn sodium Inhaled
5 Immunosuppresants (monoclonal Omalizumab, and S.C
antibodies) Mepolizumab injection
Reslizumab I.V
infusion
6 Phosphodiesterase type-4 inhibitor Roflumilast Oral
Figure 3-1: Stepwise approach for managing asthma in adults.

(3)
*Beclometasone dipropionate (BDP) or equivalent .
51
3.2.1-Beta2-adrenoceptor agonist
1-Inhaled Short-Acting β2-Agonists (SABAs) [e.g., salbutamol and
terbutaline)
A-SABAs are the most effective agents for reversing acute airway obstruction
caused by bronchoconstriction and are the drugs of choice for acute symptom
relief (asthma or COPD) (4).
B-SABA used on as required base (5).
B-SABAs inhaled immediately before exertion reduces exercise-induced

asthma (1).
2-Inhaled Long-Acting β2-Agonists (LABAs): Salmeterol and formoterol

A-Regular use of beta2 agonists is mainly restricted to LABAs in patients also
requiring anti-inflammatory prophylactic treatment; a SABA should still be
used as required (5).
B-LABAs provide up to 12 hours of bronchodilation after a single dose (4).
C-LABAs are indicated for chronic treatment of asthma and COPD (4).
D-Salmeterol should not be used for the relief of an acute symptom relief; it has
a slower onset of action than salbutamol or terbutaline (1, 4).
E-Formoterol is licensed for short-term symptom relief and for the prevention
of exercise-induced bronchospasm; its speed of onset of action is similar to
that of salbutamol (1).
3-Adverse effects of β2-agonists include tachycardia, tremor, and hypokalemia,

which are usually not troublesome with inhaled dosage forms (4).
4-Note : The β2-agonists (by i.v infusion) salbutamol and terbutaline are licensed
for inhibiting uncomplicated premature labour between 22 and 37 weeks of
gestation to permit a delay in delivery of up to 48 hours (1).
Beta2-adrenoceptor agonist
1
51
Any extra notes:
3.2.2-Corticosteroids
1-Corticosteroids are potent anti-inflammatory agents and are available in inhaled,
oral, and injectable dosage forms (4).
2-Inhaled Corticosteroids:
A-ICS are the preferred therapy for all forms of persistent asthma in all age
groups (4). In COPD, ICS may reduce exacerbations when given in combination
with an inhaled LABA (1).
B-Although some beneficial effect is seen within 12 hours of administration of

an ICS, 2 weeks of therapy is necessary to see significant clinical effects (4).
C-Local adverse effects of ICS include oral candidiasis, cough, and

dysphonia. The incidence of local adverse effects can be reduced by using a
spacer device and by having the patient rinse the mouth with water and
expectorate after using the ICS (4).
D-Budesonide has the most safety data in humans and is the preferred ICS
during pregnancy (4).
3-Systemic Corticosteroids
A-Prednisone, prednisolone, and methylprednisolone are systemic
corticosteroids. These medications are the cornerstone of treatment for acute
asthma and COPD exacerbations not responding to an inhaled SABA (4).
B-Because of serious potential adverse effects, systemic corticosteroids are

avoided as long-term controller medication for asthma, if possible. Systemic
corticosteroids are only used in patients who have failed other therapies (4)
(should normally be taken as a single dose in the morning to reduce the
disturbance to circadian cortisol secretion) (1).
C-Chronic systemic corticosteroids should be avoided in COPD

management because of questionable benefits and high risk of toxicity (6).
4-Combination of inhaled corticosteroids and long-acting bronchodilators

(fluticasone plus salmeterol or budesonide plus formoterol) is associated with
greater improvements than either agent alone and makes administration of both
drugs more convenient (6).
52
Inhaled Corticosteroids (including combination products)
1
Any extra notes:
3.2.3- Antimuscarinic:
1-Two antimuscarinic medications are available: ipratropium bromide and
tiotropium bromide (4).
2-Inhaled ipratropium bromide indicated as (as needed) as an adjunctive therapy

in severe acute asthma, for short-term relief in mild COPD, and for COPD
exacerbations not completely responsive to β2-agonists alone (1, 4, 6).
3-Combination of both SABA with ipratropium provides added symptomatic

relief and improvements in pulmonary function (Combivent ® contains
salbutamol and ipratropium in an MDI for therapy of COPD) (6).
3-Tiotropium bromide is a long-acting inhaled antimuscarinic available in a DPI

and Respimat. It is use as a long-term maintenance treatment for patients with
asthma (via Respimat) and COPD (via Respimat and DPI) (1, 4).
Inhaled Antimuscarinic (including combination products)

1
53
Any extra notes:
3.2.4-Leukotriene Receptor Antagonists (LTRAs) (Leukotriene Modifiers):

1-The available drugs are (zileuton, montelukast and zafirlukast) (4). They are
indicated for asthma prophylaxis. In addition, montelukast is used for symptomatic
relief of seasonal allergic rhinitis in patients with asthma (1).
2-Although these agents offer the convenience of oral administration, they are
significantly less effective than low ICS doses (4).
3-They are not used to treat acute asthma exacerbations and must be taken on a
regular basis, even during symptom-free periods (6).
4-Montelukast is given once daily in the evening (1).
A-The chewable tablet is taken on an empty stomach. This means an hour

before food or 2 hours after food (1).
B-Granules may be swallowed or mixed with cold, soft food (not liquid) and
taken immediately (1).
Leukotriene Receptor Antagonists

1
Any extra notes:
3.2.5-Methylxanthines:
1-Theophylline causes bronchodilation. Its use is limited because of lower
efficacy, a narrow therapeutic index with potentially life threatening toxicity, and
multiple clinically important drug interactions (4).
2-Methylxanthines must be taken systemically (orally or IV). Sustained-release

theophylline is the preferred oral preparation and is used for chronic asthma
or COPD (1, 6). Theophylline is given by injection as aminophylline (due to
54
increased solubility) for severe acute asthma or severe acute exacerbation of
COPD (1, 6).
3- Phyllocontin Continus ® Forte tablets are for smokers and other patients where
theophylline half-life is shorter (1).
4-For intravenous injection, give very slowly over at least 20 minutes (1).
5-The rate of absorption from modified release preparations can vary

between brands. If a prescription for a modified-release oral aminophylline
preparation does not specify a brand name, the pharmacist should contact the
prescriber and agree the brand to be dispensed. Additionally, it is essential that a
patient discharged from hospital should be maintained on the brand on which that
patient was stabilized as an inpatient (1).
6-Directions for administration of theophylline modified release capsules (e.g.

slo-phyllin ®): In adults Swallow whole with fluid or swallow enclosed granules
with soft food (e.g. yoghurt). In children Contents of the capsule (enteric-coated
granules) may be sprinkled on to a spoonful of soft food (e.g. yoghurt) and
swallowed without chewing (1).
7-Modified-release theophylline tablet should be taken with or just after food (1).
Methylxanthines
1
Any extra notes:
3.2.6-Mast Cell Stabilizers:

1-Sodium cromoglicate (mast cell stabilizer) (by inhalation) is indicated for
prophylaxis of mild persistent asthma in children and adults (6).
2-Other uses:
A-Sodium cromoglicate and nedocromil sodium may also have a role in
allergic conjunctivitis; sodium cromoglicate is used also in allergic rhinitis (1).
B-Sodium cromoglicate is used also (orally as a capsule) for allergy-related

diarrhea [food allergy (in conjunction with dietary restriction)]. Capsules may
55
be swallowed whole or the contents dissolved in hot water and diluted with cold
water before taking. To be taken 30 to 60 minutes before food (1).
Mast Cell Stabilizers

1
Any extra notes:
3.2.7-Immunosuppresants monoclonal antibodies

1-Omalizumab (S.C. injection) is an anti-IgE monoclonal antibody. It is used as
prophylaxis of severe persistent allergic asthma. It is also used for chronic
spontaneous urticaria in patients who have had an inadequate response to H1
antihistamine treatment (1).
2-Mepolizumab (S.C. injection) and Reslizumab (I.V. infusion) reduce the

production and survival of eosinophils. They are indicated as an add on
treatment for severe refractory eosinophilic asthma (1).
Immunosuppresants monoclonal antibodies

1
Any extra notes:
3.2.8-Phosphodiesterase type-4 inhibitor

1-Roflumilast is used as an adjunct to bronchodilators for the maintenance
treatment of patients with severe COPD associated with chronic bronchitis
and a history of frequent exacerbations (1).
56
3.3-Antihistamines
1-Antihistamines are used in the treatment of nasal allergies (they reduce
rhinorrhoea and sneezing)(antihistamines are frequently used in combination
preparations for the treatment of coughs and colds). Antihistamines are also used
to treat urticarial rashes, pruritus, and insect bites and stings (5).
2-The antihistamines may be classified into :
A-Sedating antihistamines: older antihistamines that are associated with

troublesome sedative and antimuscarinic effects. Example are (chlorphenamine
(chlorpheniarmine), clemastine, cyproheptadine, Hydroxyzine, ketotifen,
(5)
diphenhydramine, and dimethindene maleate ) . Drowsiness is a major
problem with the sedating antihistamines and those affected should not drive
or operate machinery (5). Drowsiness may diminish after a few days of
treatment (1).
B-Non-sedating antihistamines: are newer antihistamines, they generally

cause little or no drowsiness (5). Example are (acrivastine, bilastine, cetirizine,
desloratadine, fexofenadine, levocetirizine , loratadine , and mizolastine) (1).
[Although drowsiness is rare, nevertheless patients should be advised that it can
occur and may affect performance of skilled tasks (e.g. cycling or driving);
alcohol should be avoided. If drowsiness occurs, it may diminish after a few
days of treatment] (1).
3-Because of their antimuscarinic actions (like urinary retention), the sedating

antihistamines should be used with caution in conditions such prostatic
hyperplasia. Antimuscarinic adverse effects are not a significant problem with the
non-sedating antihistamines (5).
4-There is little evidence that any one of the older, ‘sedating‘ antihistamines is
superior to another and patients vary widely in their response (1).
5-Antihistamines are more effective when taken 1to 2 hours before anticipated
exposure to the offending allergen (6).
6-Important : Cyproheptadine has been widely used as an appetite stimulant,

but in the long-term appears to have little value in producing weight gain and such
use is no longer generally recommended (5).
7-Diphenhydramine has pronounced sedative properties and may be used as a

hypnotic in the short-term management of insomnia (taken before bedtime) (5).
57
Antihistamines
1
10
Any extra notes:
3.4-Cough preparations
Notes :
1-Children under 6 years should not be given OTC cough and cold medicines
containing the listed ingredients in (table 3-2) (1).
Table 3-2: Over the counter cough and cold medicines for children (1)
1-Children under 6 years should not be given OTC cough and cold medicines
containing the following ingredients:
-Brompheniramine, chlorphenamine, diphenhydramine, doxylamine,
promethazine, or triprolidine (antihistamines);
-Dextromethorphan or pholcodine (cough suppressants);
-Guaifenesin (expectorants);
-Phenylephrine, pseudoephedrine, ephedrine, oxymetazoline, or
xylometazoline (decongestants).
2-Sympathomimetics (e.g. pseudoephedrine and phenylphrine) are commonly

included in cough and cold remedies for their bronchodilator and decongestant
58
actions. They may be useful if the patient has blocked nose as well as cough,
but they can increase the BP ,stimulate the heart, and alter the diabetic control (9) ;
therefore they are not recommended for patients with : Coronary artery diseases
(Angina, MI, ….), hypertension, diabetes mellitus, and hyperthyroidism (7).
3.4.1-Cough suppressants (Antitussive):

1-Codeine, Pholcodeine and dextromethorphan are used for dry cough.
Although all three may be effective, dextromethorphan and pholcodeine have a
lower risk of constipation and dependence developing. In addition, both
pholcodeine and codeine can cause drowsiness whereas dextromethorphan is non-
sedating in most people (7).
2-The FDA recommended that the use of codeine-containing cough medicines

should be contraindicated in children younger than 18 years (8).
3-Side effects: even at OTC doses codeine can cause constipation and at high
doses, respiratory depression (9), therefore it is best avoided in patients with
impaired respiratory function e.g. asthma (10).
4-Codeine is well known as a drug of abuse and sales must be refused because of
knowledge or likelihood of abuse (9).
5-Generally dextromethorphan is considered non-sedating and has fewer side

effects and thought to have a low potential for abuse (11).
6-Sedating antihistamines are used as the cough suppressant component of many

compound cough preparations on sale to the public; all tend to cause drowsiness
which may reflect their main mode of action (1).
3.4.2-Expectorants and Mucolytics

1-Expectorants and mucolytics are used for wet cough. Examples of expectorant is
glyceryl guaiacolate (also called Guaifenesin) and examples of is Mucolytics is
bromohexine.
3.4.3-Lozenges
1-Nonmedicated lozenges may reduce cough by decreasing throat irritation (10).
They may contain ingredients such as honey and lemon, or glycerol. They are
thought to coat the pharyngeal mucosa, soothing inflammation and reducing
irritation, and can be used to treat both productive and non-productive coughs
(7)
.
2-They are considered to be safe in children and pregnant women (9) but should
not be given to children under three years of age because of the risk of choking (7).
If recommended they should be given 3-4 times daily (12).
59
Cough preparations
1
Any extra notes:
3.5-Orally administered nasal decongestants

1-Orally administered nasal decongestants like pseudoephedrine, phenylphrine
and ephedrine constrict the dilated blood vessels of the nose (12).
2-The sympathomimetics are usually combined with antihistamine (13).
Orally administered nasal decongestants

1
61
Any extra notes:
2.6-Mucolytics for cystic fibrosis

1-Dornase alfa (by inhalation of nebulized solution) is used to reduce sputum
viscosity in patients with cystic fibrosis (1).
2-Nebulized hypertonic sodium chloride (3–7%) is used to mobilize lower

respiratory tract secretions in mucus consolidation (e.g. cystic fibrosis) (1).
3-Nebulized hypertonic sodium chloride solution (3%) is used for mild to

moderate acute viral bronchiolitis in infants (1).
4-Mannitol administered by inhalation (inhalation of powder), improves mucus

clearance and is licensed for the treatment of cystic fibrosis as an add-on therapy
to standard care (1).

1
Any extra notes:
References
1-BNF 74.
2-Christopher A Langley, Dawn Belcher. Applied Pharmaceutical Practice. Pharmaceutical Press. 2009.
3-Nicholas A. Boon, Nicki R. Colledge and Brian R. Walker. Davidson's Principles and Pracrtice of
Medicines . 22nd Edition 2014.
5-Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press
2009.
6-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 10th edition. 2017.
7-Sarah Marshall . Over-the-counter advice for coughs. The Pharmaceutical Journal (Vol 278) 20
January 2007 . page:85-88
8-The U.S. Food and Drug Administration (FDA). FDA Drug Safety Communication: FDA requires
labeling changes for prescription opioid cough and cold medicines to limit their use to adults 18 years and
older. 2018.
9-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the pharmacy . A guide to the
managements of common illness. 7th edition. 2014.
10-American pharmacists association. Handbook of Non-prescription drugs: An Interactive Approach to
Self-Care. 18th edition. 2016.
11-Nathan A. fasttrack. Managing Symptoms in the Pharmacy. Pharmaceutical Press. 2008.
61
Chapter Four : Central Nervous System
Note: many of the CNS drugs (like antipsychotics, antidepressant,

antiepileptics, anxiolytics, hypnotics, opioid analgesics) can cause drowsiness,
thereby affecting the ability to drive and operate hazardous machinery and patients
should be warned about this.
4.1-Drugs for dementia

1-In dementia, there is a is a deterioration memory, judgement, language and
communication. Alzheimer’s disease is the most common cause of dementia
and accounts for over half of all patients; about one-third of dementia cases
are due to vascular disease (1).
2-Donepezil, galantamine, and rivastigmine are the main cholinesterase

inhibitors. All have produced modest improvement in patients with mild to
moderately severe disease (1). Acetylcholinesterase inhibitors can cause unwanted
cholinergic side-effects (2).
3-When switching from one cholinesterase inhibitor to another, 1 week washout is

generally sufficient (3).
4-Memantine is a glutamate receptor antagonist; it is licensed for treating

moderate to severe Alzheimer‘s disease (2).
5-Rivastigmine and galantamine are given with or just after meal (2).
Drugs for dementia

1
Any extra notes:
4.2-Epilepsy and other seizure disorders

1-Antiepileptic drug (AEDs) include : Brivaracetam, Carbamazepine,
Clonazepam, Ethosuximide, Ezogabine, Felbamate, Gabapentin, Lacosamide,
Lamotrigine, Levetiracetam, Oxcarbazepine, Phenobarbital or Primidone,
62
Phenytoin, Pregabalin, Tiagabine, Topiramate, Valproate, Vigabatrin and
Zonisamide (2, 3).
2-If it is felt desirable for a patient to be maintained on a specific

manufacturer’s product. This advice relates only to antiepileptic drug use for
treatment of epilepsy; it does not apply to their use in other indications (2).
3-Usually, therapy is initiated at lower and gradually increased over 3 or 4

weeks to an effective dose (3).
4-Phenytoin metabolism is capacity-limited, so that a small changes in doses
result in large changes in serum concentrations. The patient is at risk of sudden
toxicity if too large a dose increase is made (4).
5-Adverse effects of AEDs (4).

A-Two types of adverse effects occur with AEDs: dose-related and
idiosyncratic.
B-For many AEDs, common dose-related adverse effects include sedation,

ataxia, and diplopia (If a patient has a job that requires mental alertness, it is
best to choose an AED that is less likely to cause sedation (e.g., lamotrigine).
C-Idiosyncratic adverse effects will almost always result in the AED being
discontinued. Rash, hepatotoxicity, and hematologic toxicities are the most
common idiosyncratic reactions seen with AEDs.
D-Chronic Adverse Reactions : One chronic adverse effect that is of concern

is osteoporosis. Carbamazepine, phenytoin, Phenobarbital , oxcarbazepine, and
valproate have all been shown to decrease bone mineral density, even after only
6 months of treatment. Patients taking these drugs for longer than 6 months
should take supplemental calcium and vitamin D.
6-Drug–drug interactions (3, 4).

AEDs are associated with many different drug interactions:
A-Phenobarbital, phenytoin, primidone, and carbamazepine are potent

inducers of various cytochrome P-450 (CYP450) isoenzymes, increasing the
clearance of other drugs metabolized through these pathways.
B-Valproic acid inhibits many hepatic enzyme systems and displaces some
drugs from plasma albumin.
C-Felbamate and topiramate can act as inducers with some isoforms and
inhibitors with others.
7-Withdrawal of AEDs is done slowly (4).

63
8-Acetazolamide, a carbonic anhydrase inhibitor, has a specific role in treating
epilepsy associated with menstruation. Piracetam is used as adjunctive treatment
for cortical myoclonus (2).
9-Seizures lasting longer than 5 minutes should be treated urgently with

intravenous lorazepam (repeated once after 10 minutes if seizures recur or fail to
respond) (2). Other drugs used for convulsive status epilepticus are: phenytoin,
fosphenytoin, phenobarbital, thiopental, midazolam, or a non-barbiturate
anaesthetic such as propofol (2).
10-Other uses: another indications for some AEDs are: neuropathic pain, migraine
prophylaxis, trigeminal neuralgia, bipolar disorder, and anxiety disorder (2).
Antiepileptic drugs
1
Any extra notes:
4.3-Hypnotics and anxiolytics

1-Hypnotics are used for patients with insomnia, while anxiolytics are used for
patients with anxiety (2).
2-Prescribing of these drugs is widespread but dependence and tolerance occur.

This may lead to difficulty in withdrawing the drug (2).
3-Hypnotics and anxiolytics should be reserved for short courses to alleviate acute
conditions after causal factors have been established (2).
64
4-Benzodiazepines (e.g. Alprazolam, diazepam, Chlordiazepoxide, Lorazepam)
are the most commonly used anxiolytics and hypnotics (2).
5-Short-acting hypnotics (e.g. Loprazolam, lormetazepam, and temazepam) are

preferable in patients with sleep onset insomnia, when sedation the following day
is undesirable, or when prescribing for elderly patients (2).
6-Long-acting hypnotics (e.g. diazepam) are indicated in patients with poor sleep
maintenance (e.g. early morning waking) that causes daytime effects, when an
anxiolytic effect is needed during the day, or when sedationthe following day is
acceptable (2).
7-Zaleplon, zolpidem, and zopiclone are non-benzodiazepine hypnotics (2).
8-Melatonin is a pineal hormone; it is licensed for the short-term treatment of

insomnia in adults (2).
9-Benzodiazepine anxiolytics can be effective in alleviating anxiety states (2).
10-Beta-blockers do not affect psychological symptoms of anxiety, such as worry,

tension, and fear, but they do reduce autonomic symptoms, such as palpitation and
tremor (2).
11-Nonbenzodiazepine antianxiety agents for generalized anxiety disorder include

(3)
: A-Antidepressants. B-Anticonvulsant (Pregabalin).
C-Atypical antipsychotic (Quetiapine).
Hypnotics and anxiolytics

1
Any extra notes:
65
4.4-Antipsychotic drugs (for treatment of schizophrenia)
1-First-generation antipsychotic drugs include for example : Chlorpromazine,
Fluphenazine, Haloperidol, Loxapine, Perphenazine, Thioridazine, and
Trifluoperazine (3).
2-Second-generation antipsychotics (SGAs) include for example: Amisulpride,

Aripiprazole, Clozapine, Lurasidone, Olanzapine, Paliperidone, Quetiapine,
Risperidone (2).
3-Side effects of antipsychotic drugs:

A-Side-effects caused by antipsychotic drugs are common and contribute
significantly to non-adherence to therapy (2).
B-Side effects of antipsychotic drugs include: Extrapyramidal symptoms,

hyperprolactinaemia, sexual dysfunction, arrhythmias, hyperglycaemia, weight
gain and blood dyscrasias (2).
C-SGAs are said to cause few or no acutely occurring extrapyramidal side

effects, minimal or no propensity to cause tardive dyskinesia (TD), and less
effect on serum prolactin than the first-generation antipsychotics (FGAs).
Clozapine is the only SGA that fulfills all these criteria (3).
D-SGAs have less neurologic side effects, especially effects on movement, but
they have increased risk for metabolic side effects, including weight gain,
hyperlipidemias, and diabetes mellitus (3).
4-Other uses (2):

A-Some antipsychotic drugs can be used for the treatment of nausea and
vomiting, choreas, and motor tics.
B-Chlorpromazine and haloperidol can be used for intractable hiccup.
C-Benperidol is used in deviant antisocial sexual behavior but its value is not
established.
D-Antipsychotic drugs can be used with caution for the short-term treatment of
severe agitation and restlessness in the elderly.
5-Long-acting depot injections antipsychotic are used for maintenance therapy

especially when compliance with oral treatment is unreliable. Depot
antipsychotics are administered by deep intramuscular injection at intervals of 1 to
4 weeks (2).
6-Warning: Owing to the risk of contact sensitization, pharmacists, nurses, and

other health workers should avoid direct contact with chlorpromazine; tablets
should not be crushed and solutions should be handled with care (2).
66
Antipsychotics (Both typical and Atypical antipsychotics)
1
Any extra notes:
4.5-Antidepressant drugs
1-Currently available classes of antidepressant medications are shown in table 4-
1(3).
Table 4-1: Antidepressant drugs (2, 3).

Class of Antidepressant Example(s)
1 Selective serotonin reuptake Citalopram, Escitalopram, Fluoxetine,
inhibitors (SSRIs) Fluvoxamine, Paroxetine, Sertraline
2 Tricyclic antidepressants Amitriptyline, Desipramine, Dosulepin ,
(TCAs) and tetracyclic Doxepin, Lofepramine, Imipramine,
antidepressants Nortriptyline, Mianserin (tetracyclic),
Trimipramine
3 Norepinephrine and dopamine Bupropion
reuptake inhibitor (NDRI)
4 Mixed serotonergic effects Nefazodone, Trazodone, Vilazodone,
(Mixed 5-HT) Vortioxetine
5 Serotonin and α2-adrenergic Mirtazapine
antagonist
6 Monoamine oxidase inhibitors Phenelzine, Selegiline, Tranylcypromine
(MAOIs)
7 Melatonin receptor agonist Agomelatine
8 Noradrenaline reuptake Reboxetine
inhibitors
9 Serotonin and noradrenaline re- Duloxetine, Venlafaxine
uptake inhibitors.
67
2-There is little to choose between the different classes of antidepressant drugs in
terms of efficacy (2).
3-Regarding SSRIs:
A-SSRIs are generally chosen as first-line antidepressants because of their
safety in overdose and improved tolerability compared with earlier agents. The
SSRIs produce fewer sedative, anticholinergic, and cardiovascular adverse
effects than the TCAs and are less likely to cause weight gain than the TCAs (3).
B-In the treatment of depression the usual initial dose of fluoxetine is 20 mg

once daily; US product information recommends giving this dose in the
morning (5).
C-Some SSRIs are also used as part of the management of generalized anxiety
disorder, obsessive-compulsive disorder, panic disorders and bulimia nervosa.
Fluoxetine is also used in the treatment of premenstrual syndrome (2, 5).
D-The most common adverse effects associated with this class of agents
include GI complaints, insomnia, restlessness, headache, and sexual
dysfunction (6).
4-Regarding TCAs:
A-TCAs are antidepressants, but their use has diminished because of the
availability of equally effective therapies that are safer on overdose and
better tolerated (3).
B-TCAs have α-adrenergic blockade, antihistaminic effects, and anticholinergic

effects, which lead to orthostasis, sedation, and anticholinergic symptoms,
respectively. They also lead to cardiotoxic effects (6).
C-Some TCAs are used in the management treatment for neuropathic pain,
migraine prophylaxis, anxiety disorders and in nocturnal enuresis in
children (2, 6).
5-Duloxetine is also used in the treatment of generalized anxiety disorder,

treatment of diabetic peripheral neuropathic, and the treatment of moderate to
severe stress urinary incontinence in women (5).
6-The use of antidepressants has been linked with suicidal thoughts and
behavior. Patients should be monitored for suicidal behavior, self-harm, or
hostility, particularly at the beginning of treatment or if the dose is changed (2).
68
Antidepressant drugs
1
4.6-Drugs used in parkinsonism

1-The primary objective of drug therapy is to enhance dopaminergic activity
within the damaged areas of the basal ganglia, and this is achieved in various
ways (table 4-2) (7).
Any extra notes:
Table 4-2: Drugs used in parkinsonism (7).
69
2-Regarding Levodopa and Carbidopa/Levodopa:
A-L-dopa, the most effective drug available. Ultimately, all Parkinson disease
(PD) patients will require L-dopa (3).
B-The immediate response to levodopa is often dramatic, but the long-term

use is limited by the development of motor fluctuations. The most common
of these is the wearing-off effect (8).
C-Wearing off occurs when patients experience recurrence of symptoms

before the next dose of medication (9). Possible options to solve such problem
include (4): Carbidopa/L-dopa needs to be given more frequently or the
addition of the COMT inhibitor entacapone or the MAO-B inhibitor
rasagiline or a dopamine agonist (e.g., pramipexole, ropinirole) (3).
D-Another complication of L-dopa therapy is dyskinesia [an involuntary

choreiform movements (too much movement )involving the neck, trunk, and
extremities (lower/upper)]. Possible options to solve such problem include:
The use of lower individual doses of L-dopa (with an increase in dosage
frequency) or addition of amantadine (3).
3-Regarding dopamine Agonists:

A-The ergot derivative (bromocriptine, Pergolide, Cabergoline) and the
nonergots (safer) pramipexole , rotigotine , and ropinirole are beneficial
adjuncts in patients with limited clinical response to L-dopa (3).
B-In younger patients (e.g., age <65 years) with milder disease, the initiation
of a dopamine agonist is preferred. In older patients (e.g., age >65 years)
with PD, it may be more appropriate to initiate treatment with levodopa
instead of a dopamine agonist (10).
4-Regarding Catechol-O-Methyltransferase (COMT) Inhibitors:

A-Tolcapone, entacapone and opicapone are used only in conjunction with
carbidopa/L-dopa. Thus, ―on‖ time is increased (2, 3).
B-Tolcapone can cause hepatotoxicity. There is no evidence of

hepatotoxicity from entacapone (3).
C-Entacapone may discolor the urine (2).
5-Regarding Monoamine Oxidase Type-B (MAO-B) Inhibitors

A-Selegiline is a first-generation MAO-B inhibitor. Selegiline is metabolized
to the amphetamine derivatives, which have been implicated in producing
side effects such as insomnia and vivid dreaming (11). So it is not given in the
evening because excess stimulation from metabolites can cause insomnia.
The orally disintegrating tablet formulation dissolves in the mouth on contact
with saliva and undergoes pregastric absorption (this minimizes the effect of
71
first-pass and reduces the production of amphetamine-based metabolites)
(10)
.
B-Rasagiline is a second-generation selective inhibitor of MAO-B. It is more

potent inhibitor of MAO-B than selegiline, and it is not metabolized into
amphetamine-based metabolites (10).
C-Safinamide is another (new) monoamine-oxidase-B inhibitor (2).
6-Regarding anticholinergic medications:

A-Anticholinergics [e.g. procyclidine, and trihexyphenidyl (benzhexol)] are
more helpful in alleviating tremor and rigidity than bradykinesia. However,
they are poorly tolerated by elderly patients owing to their cognitive side
effects (12).
B-Their use is mostly restricted to patients with tremor that is intractable to

levodopa treatment (8).
7-Regarding amantadine:
A-Aamantadine has been found to have antidyskinesia effects, the finding has
shifted its use from use as monotherapy in early disease to that of an adjunctive
agent in managing levodopa-induced dyskinesias (10, 11).
B-It is also used for post-herpetic neuralgia (2).
Antiparkinsonian drugs
1
Any extra notes:
4.7-Analgesics
4.7.1-Non-steroidal anti-inflammatory drugs (NSAIDs).
See chapter Nine.
71
4.7.2-Paracetamol
1-Paracetamol has analgesic and antipyretic effects but no anti-inflammatory
effect. Paracetamol is a suitable analgesic for children (2).
2-Over-dosage with paracetamol is particularly dangerous as it may cause

hepatic damage (2).
3-Patient should be advised not to take more than 1g (usually 2 tablet of 500 mg)
at any one time. And not take more than 8 tablets (4 gm) in 24 hours (2).
4-Compound analgesic preparations containing paracetamol with a low dose of

an opioid analgesic (e.g. 8 mg of codeine phosphate per compound tablet) are
commonly used, but the advantages have not been substantiated. The low dose of
the opioid may be enough to cause opioid side-effects (in particular, constipation)
and can complicate the treatment of overdosage yet may not provide significant
additional relief of pain (2).
Paracetamol (Including compound analgesic preparations)

1
Any extra notes:
4.7.3-Opioid analgesics
1-Opioid analgesics are usually used to relieve moderate. Repeated
administration may cause dependence and tolerance (2).
2-Opioids such as codeine or dextropropoxyphene are used in the treatment of less

severe pain, and are often combined with non-opioid analgesics such as aspirin,
other NSAIDs, or paracetamol (5).
72
3-More potent opioids such as morphine are used in severe acute and chronic pain,
including cancer pain (5).
4-Tramadol produces has fewer of the typical opioid side-effects (notably, less
respiratory depression, less constipation and less addiction potential (2).
(Note: However, tramadol is abused by some Iraqi addicts).
5-The most common side-effects include nausea and vomiting (particularly in

initial stages), and constipation (2).
6-Opioids should be used with caution in patients with impaired respiratory

function (avoid in chronic obstructive pulmonary disease) and asthma (avoid
during an acute attack) (2).
Opioid analgesics
1
Any extra notes:
4.7.4-Neuropathic pain
1-Neuropathic pain, occurs as a result of damage to neural tissue (2).
2-Neuropathic pain is generally managed with a tricyclic antidepressant (e.g.

amitriptyline ) or with certain antiepileptic drugs (carbamazepine, gabapentin,
and pregabalin) (2).
3-Neuropathic pain may respond to opioid analgesics (2).
4-Capsaicin (topical) is licensed for neuropathic pain (but the intense burning
sensation during initial treatment may limit use) (2).
4.7.5-Antimigraine drugs
4.7.5.1-Treatment of acute migraine
1-Treatment of a migraine attack should be guided by response to previous
treatment and the severity of the attacks. A simple analgesic such as aspirin,
paracetamol preferably in a soluble or dispersible form) or a NSAID is often
effective (2).
73
(Peristalsis is often reduced during migraine attacks the medication may not
be sufficiently well absorbed to be effective; dispersible or effervescent
preparations are therefore preferred) (2).
2-Concomitant antiemetic treatment may be required (2) (e.g. cyclizine in

migril®). (migraine attack is usually associated with nausea).
3-If treatment with an analgesic is inadequate, an attack may be treated with a

specific antimigraine compound such as a 5HT1-receptor agonist (‗triptan’) (like
almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan,
and zolmitriptan) (2).
4-The value of ergotamine for migraine is limited by its side-effects, it is best

avoided (2).
4-Triptans and ergotamine are contra-indicated in ischemic heart disease (2).
Note : Very important: The maximum recommended doses of ergotamine

preparations should not be exceeded (should not exceed the maximum dose per
attack, the maximum dose per day as well as the maximum dose per week).
Triptans and ergotamine

1
Any extra notes:
4.7.5.2-Prophylaxis of migraine
1-Where migraine attacks are frequent, preventive treatment for migraine should
be considered (2).
2-Drugs that are used for Prophylaxis of migraine include:

A-The beta-blockers (e.g. propranolol is the most commonly used) (2).
B-Tricyclic antidepressants, and antiepileptics (topiramate, sodium valproate,

valproic acid, and gabapentin ) are also effective for preventing migraine (2).
C-Pizotifen is of limited value and may cause weight gain (2).

74
D-Botulinum toxin type A is licensed for the prophylaxis of headaches in
adults with chronic migraine (2).
Prophylaxis of migraine
1
Any extra notes:
4.8-Drugs for vertigo and tinnitus

Betahistine is an analogue of histamine licensed for vertigo, tinnitus, and hearing
loss associated with Ménière's disease. Antihistamines (such as cinnarizine), and
phenothiazines (such as prochlorperazine) are also used (2).
Any extra notes:
4.9-Drugs for Attention deficit hyperactivity disorder (ADHD)

1-Pharmacologic therapy can be divided into two categories, stimulants and
nonstimulants.
A-Stimulants include methylphenidate, dexmethylphenidate,
dextroamphetamine–amphetamine (amphetamine salts), dextroamphetamine,
and lisdexamfetamine (4).
B-Nonstimulant medications include atomoxetine, bupropion, clonidine, and

guanfacine (4).
2-Psychostimulants are the most effective agents in treating ADHD (2).
75
3-In preschool-aged children, methylphenidate can be added to the patient‘s
treatment if behavioral modification monotherapy is not sufficient in managing
ADHD symptoms (4).
Drugs for ADHD

1
Any extra notes:
4.10-Drugs for mania and hypomania

1-Antipsychotic drugs (normally olanzapine, quetiapine , or risperidone) are
useful in acute episodes of mania and hypomania; if the response to antipsychotic
drugs is inadequate, lithium or valproate may be added (2).
2-Lithium salts are used in the prophylaxis and treatment of mania, hypomania
and depression in bipolar disorder (manic-depressive disorder), and in the
prophylaxis and treatment of recurrent unipolar depression (2).
3-Valproate is used for the treatment of manic episodes associated with bipolar
disorder. Carbamazepine may be used for the prophylaxis of bipolar disorder
(manic-depressive disorder) in patients unresponsive to a combination of other
prophylactic drugs (2).
Drugs mania and hypomania

1
Any extra notes:
76
4.11-Dugs used for substance dependence
1-Drugs used for substance dependence are summarized in table 4-3 (2).
Table 4-3: Drugs used for substance dependence (2)

Substance Drugs used
1-Acamprosate and naltrexone are effective treatments for
Alcohol relapse prevention in patients with alcohol dependence;
1 dependence disulfiram is an alternative.
2-Nalmefene is licensed for the reduction of alcohol

consumption.
Bupropion (oral tablet) , and varenicline (oral tablet)
2 Nicotine Nicotine replacement therapy (Gum, Lozenges, Patches,
dependence Nasal spray, Inhalator, Sublingual tablets, Mouth (oral)
spray, and Orodispersible tablets).
3 Opioid Methadone, Buprenorphine and (Buprenorphine/naloxone)
dependence are used as substitution therapy in opioid dependence.
2-Full description of NRT usage guideline (Community Pharmacy A Guide to the

Management of Minor Ailments. By Dr. Dheyaa Jabbar Kadhim)
Drugs used for substance dependence

1
Any extra notes:
4.12-Miscellaneous drugs
1-Botulinum toxin type A (muscle relaxants, peripherally acting) is used for (2):
A-Treatment of focal spasticity (including hand and wrist disability associated
with stroke)
B-Blepharospasm, hemifacial spasm, spasmodic torticollis.
C-Severe hyperhidrosis of the axillae
D-Prophylaxis of headaches in adults with chronic migraine.
E-Temporary improvement of moderate to severe wrinkles between the
eyebrows in adults under 65 years.
F-Ankle disability due to lower limb spasticity associated with stroke.
77
G-Management of bladder dysfunctions.
H-Temporary improvement of moderate to severe crow‘s feet
2-Tetrabenazine is indicated for movement disorders due to Huntington‘s chorea,

senile chorea, and related neurological conditions (2).
3-Risperidone and aripiprazole are FDA label approved for the treatment of
irritability, consisting primarily of physical aggression and severe tantrum
behavior associated with autism (13).
Any extra notes:
References
Press 2009.
2-BNF-74.
2017.
Press 2009.
7-Russell J Greene, Norman D Harris . Pathology and Therapeutics for Pharmacists : A basis for
clinical pharmacy practice third edition . 2008 by pharmaceutical press.
9-Michele A. Faulkner. Early Versus Delayed Diagnosis and Treatment of Parkinson‘s Disease:
What You Need To Know . Us pharmacist. December, 2008.
11th ed., 2018.
11- David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease
Management. 8th edition.
12-Maxine A. Papadakis, et al, eds. Current Medical Diagnosis & Treatment, 56th Edition 2017
13- ACCP Updates in Therapeutics® 2015: Pediatric Pharmacy Preparatory Review Course.
78
Chapter Five : Infections
5.1-Antibacterials
5.1.1-Aminoglycosides
1-These include amikacin, gentamicin, neomycin, streptomycin, and tobramycin
(1)
.
2-All are bactericidal and active against some Gram-positive and many Gram-
negative organisms. Tobramycin has similar activity to gentamicin. It is slightly
more active against Ps. aeruginosa (1).
3-The aminoglycosides are not absorbed from the gut and must therefore be
given by injection for systemic infections (1). Neomycin sulfate may be given
orally to reduce the bacterial population of the colon prior to bowel surgery or in
hepatic failure (1).
4-Once daily administration of aminoglycosides is more convenient than multiple

daily dose regimens (1).
5-The important side-effects are ototoxicity, and nephrotoxicity (1).
6-Streptomycin is used mainly for tuberculosis (2nd line drug) and for brucellosis
(1)
.
Aminoglycosides
1
Any extra notes:
5.1.2-Carbapenems
1-These include imipenem (with cilastatin), ertapenem and meropenem (1).
2-The carbapenems are beta-lactam antibacterials with a broad-spectrum of

activity which includes many Gram-positive and Gram-negative bacteria, and
anaerobes (1).
79
3-Imipenem is partially inactivated by enzymatic activity and is therefore
administered in combination with cilastatin, a specific enzyme inhibitor (1).
4-Meropenem has less seizure-inducing potential and can be used to treat central
nervous system infection (1).
Carbapenems
1
Any extra notes:
5.1.3-Cephalosporins
1-Classification (table 5-1) (1, 2)
Table 5-1: Cephalosporins (1, 2)

Groups Examples
1 First-generation Cefalexin and cefadroxil
2 Second -generation Cefuroxime
3 Third-generation Cefotaxime, ceftazidime ceftriaxone, cefixime,
cefpodoxime
4 Fourth-generation Cefepime
5 Fifth-generation Ceftaroline
2-They have more broad-spectrum antimicrobial activity than penicillins,

activity that broadens in spectrum when moving from first- to fourth-generation
agents (3). In general the activity against gram negative bacteria is increase and the
activity against gram positive bacteria is decrease when we move from first to third
generations cephalosporins (2).
3-Some important properties for specific agents (table 5-2) (1, 2):
Table 5-2: Properties for specific cephalosporins

Drug Properties
Ceftriaxone Has a longer half-life (may be given once daily).
Ceftazidime Has good activity against pseudomonas.
Cefixime Oral third-generation cephalosporin.
Cefpodoxime Oral third-generation cephalosporin (must be given after
food).
81
4-The principal side-effect of the cephalosporins is hypersensitivity and about
0.5–6.5% of penicillin-sensitive patients will also be allergic to the cephalosporins.
Patients with a history of immediate hypersensitivity to penicillin should not
receive a cephalosporin (contraindicated) (1).
5-Note : important: when given by an intravenous injection, most of these drugs

should be given over at least 5 minutes or by intravenous infusion after mixing
with a compatible fluid (arrhythmias following rapid injection reported) (1).
6-Important:
A-Ceftriaxone should not to be given simultaneously with infusion fluids
containing Ca, even by different infusion lines. May be infused sequentially
with infusion fluids containing Ca if flush with NaCl 0.9% between infusions or
give infusions by different infusion lines at different sites (1).
B-In neonate (28 days of age or younger) at least 48 hours must elapse from
the last dose of ceftriaxone and the use of any Ca-containing solutions (4).
Cephalosporins
1
Any extra notes:
5.1.4-Glycopeptide antibiotic
1-The glycopeptide teicoplanin and vancomycin have bactericidal activity against
aerobic and anaerobic Gram-positive bacteria including multi-resistant
staphylococci (1).
2-Teicoplanin is similar to vancomycin, but has a significantly longer duration of

action, allowing once daily administration and is associated with a lower
incidence of nephrotoxicity than vancomycin (1).
81
3-Injection of (teicoplanin and vancomycin) can be used to prepare solution for
oral administration (for Clostridium difficile infection) (1).
4-Vancomycin is typically administered by slow IV infusion. More rapid infusion

rates can cause the red man syndrome, which is a histamine-mediated reaction
that is typically manifested by flushing and redness of the upper body (5).
Glycopeptide
1
Any extra notes:
5.1.5-Lincosamides (lincomycin and clindamycin)

1-Active against Gram-positive cocci, and also against many anaerobes (1). The
main indication for the use of lincosamides is now in the treatment of severe
anaerobic infections (2).
2-Clindamycin is much better absorbed from the GIT than lincomycin. They
both penetrate well into bone and have been used successfully in osteomyelitis (2).
3-The capsules should be taken with a glass of water (2).
4-They have also been used topically in the treatment of acne vulgaris (2).
5-Important: Patients should discontinue immediately and contact doctor if

diarrhea develops (1) (Lincosamides are reported to produce diarrhea. In some
patients severe antibiotic-associated or pseudomembranous colitis may develop
during therapy or up to several weeks after it, and has proved fatal) (2).
Lincosamides
1
Any extra notes:
82
5.1.6-Macrolides
1-These include erythromycin, azithromycin and clarithromycin (1).
2-This class of antibiotics has activity against gram-positive cocci, including

streptococci and staphylococci, and some upper respiratory gram-negative
bacteria, but minimal activity against enteric gram-negative rods (5).
3-Azithromycin has a long half-life and once daily dosage is recommended (1).
4-Important : Azithromycin capsules must be given on an empty stomach (an

hour before food or 2 hours after food) while azithromycin tablet and
suspension are given without regard to meal (1).
5-Clarithromycin is usually given twice daily. And it is one of the component of

triple therapy for eradication of H. pylori (a bacteria that cause ulcer) (1).
6-Spiramycin is also a macrolide which is used for the treatment of toxoplasmosis

(1)
.
7-Gastro-intestinal side-effects are mild and less frequent with azithromycin and
clarithromycin than with erythromycin (1).
Macrolides
1
Any extra notes:
5.1.7-Monobactam
1-Aztreonam is monobactam antibiotic with an antibacterial spectrum limited to
Gram-negative aerobic bacteria including Pseudomonas aeruginosa, Neisseria
meningitidis, and Haemophilus influenzae (1).
83
Any extra notes:
5.1.8-Metronidazole and tinidazole

1-They are active against anaerobic bacteria and protozoa (Entamoeba
histolytica, giardia lamblia). Tinidazole is similar to metronidazole but has a
longer duration of action(2).
2-Metronidazole and tinidazole tablets are taken with or after food (1, 2).
3-Tinidazole may be given at a dose of 2 g (4 tablets) for some vaginal and GIT
infections (2).
4-They can produce nausea and an unpleasant metallic taste (2).
5-When given with alcohol, metronidazole and tinidazole may provoke a

disulfiram-like reaction in some patients (2).

1
Any extra notes:
5.1.9-Penicillins
1-Classification of penicillins (table 5-3) (1)
Table 5-3: Classification of penicillins

Penicillin groups Examples
1 Natural penicillins Benzylpenicillin and phenoxymethylpenicillin
2 Penicillinase-resistant Flucloxacillin, cloxacillin
penicillins
3 Broad-spectrum Amoxixillin, ampicillin
penicillins
4 Antipseudomonal Piperacillin (combined with the beta-lactamase
penicillins inhibitor tazobactam), Ticarcillin (combined with
the beta-lactamase inhibitor clavulanic acid)
84
2-Penicillins vary between agents with broad antimicrobial spectra and more
narrow-spectrum agents (1).
3-Ampicillin and amoxicillin are active against certain gram-positive and gram-
negative organisms but are inactivated by penicillinases (1).
4-Both piperacillin and ticarcillin have a broad spectrum of activity against a

range of Gram-positive and Gram-negative bacteria, and anaerobes. High doses
may lead to hypernatremia (owing to sodium content of preparations) (1).
5-Co-amoxiclav consists of amoxicillin with the beta-lactamase inhibitor

clavulanic acid. Clavulanic acid inactivates beta-lactamases, making the
combination active against beta-lactamase-producing bacteria that are resistant to
amoxicillin (1).
6-Various combinations between amoxicillin and clavulanic acid are presents

(table 5-4):
Table 5-4: Amoxicillin-Clavulanic acid combinations

Combinations Dosage form Notes
156 ( 125 +31) suspension
312 ( 250 + 62) suspension
457( 400 + 57) suspension Given twice daily(every 12 hours)
375 ( 250 + 125) Tablet
625( 500 + 125) Tablet
1000 ( 875 +125) Tablet Given twice daily(every 12 hours)
600 (500 + 100) Injection For intravenous injection only
1200 (1000 + 200) Injection For intravenous injection only
7-The most important side-effect of the penicillins is hypersensitivity which

causes rashes and anaphylaxis and can be fatal (1).
8-Ampicillin, flucloxacillin and cloxaciliin must be given on an empty stomach

(This means an hour before food or 2 hours after food) while amoxicillin
maybe taken without regard to meal (1).
9-For the eradication of H. pylori (a bacteria that cause ulcer), amoxicillin is given
with clarithromycin and a proton pump inhibitor; usual doses of amoxicillin for
the eradication of H. pylori is 1 g twice daily (or less commonly 500 mg three
times daily) (1, 2).
85
Penicillins
1
Any extra notes:
5.1.10-Quinolones
1-These include Nalidixic acid, Norfloxacin, Ciprofloxacin, Gatifloxacin,
Ofloxacin, Levofloxacin, Moxifloxacin (1, 2).
2-Nalidixic acid and norfloxacin are effective in uncomplicated urinary-tract

infections (1).
3-Ciprofloxacin is active against both Gram-positive and Gram-negative bacteria.

It is particularly active against Gram-negative bacteria. Ciprofloxacin can be
used for infections like respiratory tract infections (but not for pneumococcal
pneumonia), urinary-tract infections, and infections of the gastro-intestinal system
(including typhoid fever) (1).
4-Respiratory fluoroquinolones: Levofloxacin, moxifloxacin, and gemifloxacin

have improved coverage of streptococci but generally less gram-negative activity
than ciprofloxacin (except levofloxacin, which does cover P. aeruginosa) (5).
5-When the benefits of treatment outweigh the risks (arthropathy has developed
in weight-bearing joints in young animals), ciprofloxacin is licensed for use in
children for severe infections (6).
6-Nalidixic acid should be avoided in infants less than 3 months old (1, 2).
7-Administration
A-Norfloxacin should be taken on an empty stomach (1).
B-Important: Ciprofloxacin and Norfloxacin should not be taken with dairy

products (interfere with the absorption) (1, 2).
86
8-Driving and skilled tasks: Quinolones may impair performance of skilled tasks
(e.g. driving) (1).
9-Quinolones cause acute haemolytic anaemia when taken by individuals with

Glucose 6-phosphate dehydrogenase (G6PD) deficiency (1).
10-Di- and trivalent cations: Greatly decrease fluoroquinolone absorption (3).

Concomitant administration with aluminum- or magnesium-containing antacids,
oral iron, oral calcium, and oral zinc preparations can markedly impair absorption
of all orally administered fluoroquinolones (6).
Quinolones
1
Any extra notes:
5.1.11-Sulfonamides and trimethoprim

1-Sulfamethoxazole and trimethoprim are used in combination (as co-
trimoxazole) because of their synergistic activity. Trimethoprim is also used
alone particularly in the treatment of infections of the urinary and respiratory tracts
(2)
.
2-It is commonly used for treating sinusitis, otitis media, bronchitis, prostatitis, and
UTIs (5).
3-Co-trimoxazole should not generally be given to infants below 6 weeks of age

because of the risk of kernicterus. Co-trimoxazole should be avoided by people
with G6PD deficiency (2).
4-All patients should be asked whether they are allergic to "sulfa drugs" (5).
5-Co-trimoxazole in high dosage is the drug of choice for the treatment of mild to
moderate pneumocystis pneumonia (1).
87
1
Any extra notes:
5.1.12-Tetracyclines (like Tetracycline, and Doxycycline)

1-The tetracyclines are broad-spectrum antibiotics (1). Doxycycline has longer
duration than tetracycline and may be given once or twice daily.
2-Common indications for doxycycline include: genital Chlamydia, acne, and

brucellosis (in combination with rifampicin) (1).
3-Important : Oral administration:

A-Tetracycline must be given on an empty stomach (this means an hour
before food or 2 hours after food) while doxycycline is given during meals
(1)
.
B-Capsules (of both drugs) should be swallowed whole with plenty of fluid
while sitting or standing (1) (because it may cause oesophageal irritation).
4-Deposition of tetracyclines in growing bone and teeth (by binding to calcium)

causes staining, and they should not be given to children under 12 years, or to
pregnant or breast-feeding women (1).
5-They may cause photosensitivity: Patients should be advised to avoid exposure

to sunlight or sun lamps (1).
6-Di- and trivalent cations: Greatly decrease absorption of tetracyclines (3).
Tetracyclines
1
Any extra notes:
88
5.1.13-Antituberculosis drugs
1-First-line agents form the core of initial regimens for the treatment of TB.
Currently, isoniazid, rifampicin (rifampin), pyrazinamide, and ethambutol are
considered first-line agents. In specific situations, rifabutin and rifapentine may be
considered first-line agents (7).
2-Second-line drugs available for infections caused by resistant organisms, or

when first-line drugs cause unacceptable side-effects, include aminosalicylic acid
, amikacin, capreomycin, cycloserine, newer macrolides (e.g. azithromycin and
clarithromycin), moxifloxacin, bedaquiline and delamanid (1).
3-Treatment of active TB includes two phases:

A-The Initial phase: Iisoniazid (INH), rifampin, pyrazinamide, and
ethambutol for the initial phase of two months (5).
B-Continuation phase: combination of two medications, usually consisting

of rifampin and INH four months four months (for a total of 6 months of
treatment) (5).
4-Isoniazid is the preferred drug for treating latent TB infection. Generally,

isoniazid alone is given for 9 months. Rifampin for 4 months can be used when
isoniazid resistance is suspected or when the patient cannot tolerate isoniazid (8).
5-Pyridoxine (vitamin B6) may be used with INH to prevent sensory neuropathy
(5)
.
6-Rifampicin in combination with doxycycline is also used for Brucellosis. It also

used for prevention of secondary case of meningococcal meningitis (used for 2
days)(1).
7-Isoniazid must be taken 30 to 60 minutes before food. Rifampicin is Taken on

an empty stomach (an hour before food or 2 hours after food)
8-Important : Rifampicin causes a harmless orange-red discoloration of the

urine, faeces, sweat, saliva, sputum, tears, and other body fluids (2).
9-Ethambutol ocular toxicity (color blindness, loss of visual acuity, optic

neuritis) : The patients should be advised to discontinue therapy immediately if
they develop deterioration in vision and promptly seek further advice (1).
89
Antituberculosis drugs
1
Any extra notes:
5.1.14-Other antibacterials (Table 5-5):
Table 5-5: Other antibacterials

Antibacterials comments
1-It is a potent broad spectrum antibiotic (1).
2-Associated with serious hematological side-effects (aplastic
1 Chloramphenicol anaemia) when given systemically and should therefore be reserved
for the treatment of life-threatening infections (1).
1-It is active against a range of Gram-positive and Gram-negative
(1)
2 Fosfomycin .
2-A single 3 gm dose is used for acute uncomplicated lower
urinary-tract infections (1).
3 Fusidic acid 1-Narrow spectrum antibiotics used for staphylococcal infections
(1)
.
2-The oral suspension is given after food (1).
4 Linezolid Active against Gram-positive bacteria including methicillin
resistant Staphylococcus aureus (MRSA) (1).
1-Poorly absorbed from the gastro-intestinal tract, and, therefore,
Rifaximin should not be used to treat systemic infections (1).
5 2-Used for reduction in recurrence of hepatic encephalopathy (1).
1-Nitrofurantoin is used in the treatment and prophylaxis urinary-
tract infections (UTI) (2).
2-It is given orally, with food or milk (2).
6 Nitrofurantoin 3-Important: Any prophylactic dose of antibiotic for UTI
should be given at bedtime (2).
4-Nitrofurantoin may cause a brownish discoloration of the urine
(2)
.
7 Dapsone Used for dermatitis herpetiformis, leprosy and Pneumocystis
jirovecii (1).
91
5.2-Antifungal drugs
1-Examples of systemic antifungal drugs are listed in table (5-6) (1).
Table 5-6: Systemic antifungal drugs (1).

Class Examples
1 Echinocandin Nidulafungin, Caspofungin, Micafungin,
antifungals
2 Polyene antifungals Amphotericin B, Nystatin.
3 Triazole antifungals Fluconazole, Isavuconazole, Itraconazole,
Posaconazole, Voriconazole
4 Others Flucytosine, Griseofulvin
2-Fluconazole 150 mg as a single oral dose may be used for vaginal candidiasis.
While for recurrent vulvovaginal candidiasis: Initially 150 mg every 72 hours for 3
doses, then 150 mg once weekly for 6 months (1).
3-Lipid formulations of amphotericin are significantly less toxic and are

recommended when the conventional formulation of amphotericin is contra-
indicated because of toxicity, especially nephrotoxicity or when response to
conventional amphotericin is inadequate (1).
4-Echinocandin antifungals are only active against Aspergillus spp. and Candida
spp (1).
5-Itraconazole can be administered as intermittent ‗pulse’ therapy (1).
6-Concerning griseofulvin (Important) :

A-Griseofulvin is contra-indicated in pregnancy and women should not
become pregnant during, or within 1 month of stopping therapy. also men
should avoid fathering a child during and for at least 6 months after
administration (1, 2).
B-Absorption of griseofulvin from the GIT is enhanced by reducing the particle

size or when given with a fatty meal (should be given with or after meals) (2).
C-Duration of therapy is dependent on the site of the infection and may

extend to a number of months (1) (2 to 8 weeks for infections of the hair and
skin, up to 6 months for infections of the fingernails, and 12 months or more for
infections of the toenails) (2).
D-It may impair performance of skilled tasks (e.g. driving) (1).
E-Griseofulvin use has been superseded by newer antifungals, particularly for

nail infections (1).
91
7-Nystatin is used for oral, oropharyngeal, and perioral infections by local
application in the mouth (1) (will be discussed later). And it may be given orally
for the treatment of intestinal candidiasis (2).
8-Itraconazole capsule must be given after food. While Oral solution is taken
on an empty stomach (an hour before food or 2 hours after food) (1).
9-Voriconazole tablet and suspension are taken on an empty stomach (an hour
before food or 2 hours after food) (1).
10-Bone marrow depression can occur with flucytosine which limits its use (1).
Systemic antifungal drugs

1
Any extra notes:
5.3-Anthelmintics
1-The most common anthelmintics drugs available in Iraq are mebendazole and
albendazole.
2-Other anthelmintics are Ivermectin, Levamisole, and Praziquantel (1).
3-For the treatment of pinworms (Enterobius vermicularis):

A-Mebendazole is the drug of choice for treating threadworm infection in
patients of all ages over 2 years. It is given as a single dose of 100 mg; as
reinfection is very common, a second dose may be given after 2 weeks (1).
B-Albendazole may also be given as a single dose of 400 mg; as reinfection

is very common, a second dose may be given after 2 weeks (2).
92
4-In the treatment of echinococcosis (hydatid disease), albendazole is given orally
with meals in a dose of (400 mg twice daily for 3 months) (10).
5-Mebendazole is effective against Ascaris lumbricoides and is generally

considered to be the drug of choice; the usual dose is 100 mg twice daily for 3
days (1).
Anthelmintics
1
Any extra notes:
5.4-Antiprotozoal drugs
5.4.1-Amoebicides
1-Amoebicides [Metronidazole, Tinidazole (discussed previously)] and
Diloxanide furoate.
2-Diloxanide furoate, is a luminal amoebicide acting principally in the bowel

lumen and is used in the treatment of intestinal amoebiasis. It is given alone in the
treatment of asymptomatic cyst passers (patients with E. histolytica cysts in the
faeces) or following an amoebicide that acts in the tissues, such as metronidazole,
in patients with invasive amoebiasis (1, 2) and the usual course is of 10 days (2).
3-Flatulence is the most common adverse effect during treatment with diloxanide
furoate (2).

1
Any extra notes:
5.4.2-Drugs for toxoplasmosis (Spiramycin)

1-Congenital toxoplasmosis is not a problem in women who have Toxoplasma
antibody before conception (2). If toxoplasmosis is acquired in pregnancy,
transplacental infection may lead to severe disease in the fetus (1).
93
2-Spiramycin may reduce the risk of transmission of maternal infection to the
fetus (1). Spiramycin (3 g daily in divided doses) should be given until term (10).
Note: 1 g = 3,000,000 units.
Any extra notes:
5.4.3-Leishmaniacides
1-Sodium stibogluconate (Pentostam®), is used for visceral leishmaniasis (kala-
azar) and for extensive cutaneous leishmaniasis (1).
2-It is given by injection (I.M or I.V) for 28 days in visceral leishmaniasis and
for 20 days in cutaneous infection (1).
3-I.V injections must be given slowly over 5 minutes (to reduce risk of local
thrombosis) and stopped if coughing or substernal pain occur. Injection should be
filtered immediately before administration using a filter of 5 microns or less (1).
Any extra notes:
5.4.4-Antimalarials
Drugs used for treatment or of prophylaxis malaria are listed in table 5-7 (11).
Table 5-7: Antimalarials (11).

Drugs used for treatment of malaria Drugs used for malaria prophylaxis
1-Artesunate 1-Atovaquone/proguanil
2-Artemether with lumefantrine 2-Chloroquine phosphate
3-Atovaquone/proguanil 3-Doxycycline
4-Chloroquine Phosphate 4-Hydroxychloroquine
5-Clindamycin 6-Doxycycline 5-Mefloquine
7-Hydroxychloroquine 6-Primaquine phosphate
8-Mefloquine 9-Primaquine phosphate 7-Sulfadoxine/pyrimethamine
10-Quinidine gluconate r
11-Quinine sulfate
12-Tetracycline
94
5.5-Antiviral drugs
5.5.1- Hepatitis
The most common types of viral hepatitis include hepatitis: A (HAV), B (HBV), C
(HCV), D (HDV), and E (HEV).
1- There is no specific treatment for HEV or HAV infection (10, 11).
2-Treatment of acute Hepatitis B is supportive (In rare instances of severe

acute hepatitis B, treatment with oral antiviral agents is required) (9).
3-Treatment of Chronic Hepatitis B:

A-Not all chronic HBV patients are candidates for treatment (12). The indication
for treatment is a high viral load in the presence of active hepatitis [as
demonstrated by elevated serum transaminases and/or histological evidence of
inflammation and fibrosis] (10).
B-Available drugs for the treatment of HBV:

Interferon alfa-2b, pegylated interferon alfa-2a (Peg-IFN), and direct-acting
antiviral agents (orally) (lamivudine , telbivudine , entecavir, adefovir and
tenofovir) (10, 11).
C-Entecavir and tenofovir are potent antivirals with a high barrier to genetic
resistance, and so are the most appropriate first-line agent (10).
D-Monotherapy with Peg-IFN, tenofovir, or entecavir are options for the

initial treatment of chronic hepatitis B. If the response is inadequate a change in
treatment should be considered (1).
E-If drug-resistant hepatitis B virus emerges during treatment, another antiviral

drug to which the virus is sensitive should be added (1).
F-IFN-based therapies are typically administered for a predefined duration (48

weeks), whereas direct-acting antiviral agents are used until a specific end
point is achieved. For HBeAg-positive patients, treatment is recommended until
HBeAg seroconversion and an undetectable HBV viral load are achieved and
for 6 months of additional treatment (8, 11).
4-Interferon alfa has been used for treatment of HDV (11).
5-Some patients with acute HCV may be treated. The same regimens used for
chronic HCV are recommended for treatment (12).
6-Treatment of chronic HCV:

A-The recommended treatment regimen depends upon the genotype. The
length of treatment is based on the treatment regimen and patient-specific
95
factors such as previous experience with HCV treatment and presence of
cirrhosis (12).
B-Available drugs are:

Indirect-acting antivirals (IAAs): Pegylated Interferon (IFN) Alfa-2a/b and
Ribavirin. These agents have had limited therapeutic success and have been
largely replaced by direct-acting antivirals (DAAs) (13).
Direct-acting antivirals (DAAs): [Simeprevir, Paritaprevir (boosted with

ritonavir), Ledipasvir, Ombitasvir, Sofosbuvir, Dasabuvir, Daclatasvir,
velpatasvir , Grazoprevir, elbasvir, voxilaprevir].
C-Treatment success rates with DAAs greatly increased, and treatment

duration decreased (usually 8-12 weeks) (12, 13). Table 5-8: summarized some
the indications for DAAs for HBV.
Table 5-8: Indications for DAAs for HBV

Drugs Indication(s)
1 Sofosbuvir/ ledipasvir (with or without Genotype 1, 4, 5, or 6 infection (1,
13)
ribavirin)
2 Sofosbuvir/velpatasvir (with or All 6 genotypes (1, 13)
without ribavirin)
3 Sofosbuvir and daclatasvir (with or Genotype 1 , 3 or 4 infection (1, 13)
without ribavirin)
4 Sofosbuvir and simeprevir (with or Genotype 1 or 4 infection (1, 13)
without ribavirin)
5 sofosbuvir, / velpatasvir/voxilaprevir All 6 genotypes (13)
6 Ombitasvir/ paritaprevir/ ritonavir and Genotype 1 infection (1, 13)
Dasabuvir (with or without ribavirin)
7 Ombitasvir/paritaprevir/ ritonavir Genotype 4 (1)
(with ribavirin)
8 Grazoprevir/elbasvir (with or without Geonotypes 1 or 4 infection (1, 13)
ribavirin)
Drugs for viral hepatitis

1
96
Any extra notes:
5.5.2- Herpes virus infections

Antivral agents for herpes virus infections are aciclovir, famciclovir, valaciclovir,
foscarnet (use for simplex virus infection unresponsive to aciclovir in
immunocompromised patients; it is toxic and can cause renal impairment) (1).
5.5.2.1-Herpes simplex infections

1-Herpes infection of the mouth and lips and in the eye is generally associated with
herpes simplex virus serotype 1 (HSV-1). Genital infection is most often
associated with HSV-2 and also HSV-1 (1).
2-Treatment of herpes simplex infection should start as early as possible and

usually within 5 days of the appearance of the infection (1).
3-In individuals with good immune function, mild infection of the eye (ocular
herpes) and of the lips (herpes labialis or cold sores) is treated with a topical
antiviral drug (1).
4-Severe infection, neonatal herpes infection or infection in immunocompromized

individuals requires treatment with a systemic antiviral drug (1).
5.5.2.2-Varicella-zoster infections
1-Neonates with chickenpox should be treated with a parenteral antiviral to
reduce the risk of severe disease (1).
2-Chickenpox in otherwise healthy children between 1 month and 12 years is

usually mild and antiviral treatment is not usually required (1).
3-Chickenpox is more severe in adolescents and adults than in children.

Antiviral treatment is generally recommended in immunocompromized patients
and those at special risk (e.g. because of severe cardiovascular or respiratory
disease or chronic skin disorder); in such cases, an antiviral is given for 10 days
with at least 7 days of parenteral treatment (1).
4-In herpes zoster (shingles) systemic antiviral treatment can reduce the severity
and duration of pain, reduce complications, and reduce viral shedding (1).
5-Treatment with the antiviral should be started within 72 hours of the onset of
rash and is usually continued for 7–10 days (1).
97
Drugs for herpes simplex infections
1
Any extra notes:
5.5.3- Cytomegalovirus infection

1-Ganciclovir is related to aciclovir but it is more active against cytomegalovirus
(CMV); it is also much more toxic (myelosuppression) than aciclovir (1).
2-Valaciclovir is licensed for prevention of cytomegalovirus disease following

renal transplantation (1).
3-Valganciclovir is licensed for the initial treatment and maintenance treatment

of CMV retinitis in AIDS patients. It is also licensed for preventing CMV disease
following solid organ transplantation from a cytomegalovirus-positive donor (1).
Drugs for cytomegalovirus infection

1
Any extra notes:
5.5.4-Influenza
1-Oseltamivir below and zanamivir are most effective for the treatment of
influenza if started within a few hours of the onset of symptoms; they are licensed
for use within 48 hours of the first symptoms (1) (table 5-9).
2-Antiviral medications can be used to prevent influenza (1) (table 5-9).

Table 5-9: Indications and duration of use of oseltamivir and zanamivir (1).
Oseltamivir (Tamiflu) Zanamivir (Relenza)

Treatment Daily for 5 days Daily for 5 days
Post-exposure Daily for 10 days Daily for 10 days
prophylaxis of influenza
Prevention of influenza Daily for up to 28 days For up to 6 weeks
during an epidemic
98
5.5.5-Respiratory syncytial virus
1-Ribavirin is licensed for administration by inhalation for the treatment of
severe bronchiolitis caused by the respiratory syncytial virus (RSV) in infants,
especially when they have other serious diseases (1).
2-Palivizumab is a monoclonal antibody licensed for preventing serious lower

respiratory-tract disease caused by respiratory syncytial virus in children at high
risk of the disease (e.g. those with chronic lung disease, congenital heart disease)
(1)
.
Any extra notes:
5.5.6-HIV infection
1-Drugs used for HIV infection are listed in table 5-10.
Table 5-10: drug for Drugs used for HIV infection (1, 8).
Class Examples
1 Integrase inhibitors Dolutegravir, Elvitegravir, Raltegravir,
2 Fusion inhibitors Enfuvirtide
3 Non-nucleoside reverse Efavirenz, Etravirine, Nevirapine, Rilpivirine,
transcriptase inhibitor
4 Nucleoside reverse f Abacavir, Didanosine, Emtricitabine,
transcriptase inhibitors Lamivudine, Stavudine, Tenofovir, Zidovudine
5 Protease inhibitors Fosamprenavir, Atazanavir, Darunavir,
Indinavir, Lopinavir, Nelfinavir, Ritonavir,
Saquinavir, Tipranavir
6 Coreceptor inhibitor Maraviroc
2-Treatment includes a combination of drugs known as ‗highly active

antiretroviral therapy‘ (HAART) (1).
2-Treatment of HIV-1 infection is initiated with 2 nucleoside reverse

transcriptase inhibitors and either a non-nucleoside reverse transcriptase
inhibitor, or a boosted protease inhibitor, or an integrase inhibitor (1).
3-The regimens of choice contain tenofovir and emtricitabine with either:

A-Efavirenz. Or
99
B-Ritonavir boosted atazanavir. OR
C-Rritonavir-boosted darunavir. OR
D-Raltegravir (1).
4-Alternative regimens contain abacavir and lamivudine with either:

A-lopinavir with ritonavir. OR
B-Ritonavir-boosted fosamprenavir.OR
C-Nevirapine. OR
D-Rilpivirine (1).
Drugs used for HIV infection

1
Any extra notes:
References
1-BNF-74.
Press 2009.
3- Michael AM, Jason. Frequently prescribed medications. Copyright © 2012 by Jones &
Bartlett Learning, LLC.
4-Lawrence A. Trissel. Handbook on injectable drugs - 15th ed. 2009.
5-Cooper, Daniel H.; Krainik,. Washington Manual of Medical Therapeutics, The, 34 Edition.
Copyright 2014.
6-BNF-For children 2017-18.
8th edition. 2006.
2017.
9-Dan L. Longo, et al, eds. Harrison's Principles of Internal Medicine, 19th Edition. Copyright ©
2015 by the McGraw-Hill Companies, Inc.
10-Nicholas A. Boon, Nicki R. Colledge and Brian R. Walker. Davidson's Principles and
Pracrtice of Medicines . 22nd Edition 2014.
13-The Evolving Management of Hepatitis C Virus. Us pharmacist . 2015.
111
Chapter Six : Endocrine System
6.1-Drugs used in diabetes
6.1.1-Oral Antidiabetics
Note: they are given for type II diabetes.
1-Classification and administration with respect to food (table 6-1) (1, 2) :
Table 6-1: Classification and administration of oral antidiabetics

Groups Example(s) Administration
1 Sulphonylureas Glibenclamide, With food
Gliclazide, Glimepiride
2 Biguanides Metformin Take with or just after
food
3 dipeptidylpeptidase- Alogliptin, Linagliptin, Without regard to meal
4 inhibitors Sitagliptin, Saxagliptin,
Vildagliptin
4 Thiozolidinediones Pioglitazone Without regard to meal
5 Meglitinides Nateglinide, Within 30 minutes before
Repaglinide meals
Tablets should be chewed
with first mouthful of
6 Alpha-glucosidase Acarbose food or swallowed whole
inhibitor with a little liquid
immediately before food.
7 Sodium-glucose Canagliflozin,
cotransporter dapagliflozin, Before first meal
2 (SLGT2) inhibitors empagliflozin
2-Treatment guidelines suggest metformin as initial therapy (3). The current

recommendation is to start metformin therapy at diagnosis (4). The sustained-
release preparation will last 24 hours if given with the evening meal. Sustained-
release preparations have fewer GI side effects (5).
3-Glimepiride or extended-release glipizide, may be the preferred sulfonylureas

for their relatively low risk of hypoglycemia, convenient once-daily dosing (5).
4-Rapid-acting secretagogues (meglitinides) may be used instead of sulfonylureas

in patients who develop late postprandial hypoglycemia on a sulfonylurea or
patients with irregular meal schedules (6).
5-Insulin secretagogues (sulphonylureas and meglitinides), DPP-IV inhibitors, α-

glucosidase inhibitors, and SLGT2 inhibitors begin to lower the plasma glucose
immediately, whereas the glucose-lowering effects of the biguanides and
thiazolidinediones are delayed by weeks (3).
111
6-Adverse effects:
A-The primary side effects of the sulfonylureas and Meglitinides (glinides)
are hypoglycemia and weight gain (2).
B-The primary side effects of metformin GIT disturbances (anorexia, nausea,

vomiting, and diarrhea); and there may be weight loss (7). To minimize GI side
effects, metformin should be initiated at 500 mg twice a day or 850 mg once a
day, to be taken with food, followed by weekly increases in 500 mg increments
or 850mg increases every 2 weeks (2).
C-Hypoglycaemia is rare with a biguanide given alone, although it may

occur if other contributing factors or drugs are present (7).
D-The most commonly reported side effects with dipeptidylpeptidase-4

inhibitors is the increased risk of infection (2).
7-Metformin can be used in pregnancy for both preexisting and gestational

diabetes. Glibenclamide can be used during the second and third trimesters of
pregnancy in women with gestational diabetes (1).
8-Important : Metformin is used for the symptomatic management of polycystic

ovary syndrome [PCOS]. Metformin helps to normalize menstrual cycle
(increasing the rate of spontaneous ovulation), and may improve hirsutism (1).
Oral Antidiabetics (including combined products)

1
10
112
Any extra notes:
6.1.2-Parenteral anti-diabetes agents

Parenteral anti-diabetes agents include: insulins, GLP-1 receptor agonists (incretin
mimetic) and amylin mimetic (8).
6.1.2.1-Insulins
1-All patients with type 1 DM require insulin (8). It is also needed for type 2
diabetes when other methods have failed to achieve good control, and
temporarily in the presence of intercurrent illness or peri-operatively. Pregnant
women with type 2 diabetes may be treated with insulin (1).
2-Commercially available insulin products differ in their the pharmacokinetics

(5)
.(table 6-2) (3).
Table 6-2: Summary of characteristics of insulins (4)
3-Regular insulin has a relatively slow onset of action when given

subcutaneously; requiring injection 30 minutes prior to meals (8).
4-Lispro, aspart, and glulisine insulins are analogs that are more rapidly
absorbed, peak faster, and have shorter durations of action than regular
insulin. This permits more convenient dosing within 10 minutes of meals (rather
than 30 minutes prior), produces better efficacy in lowering postprandial blood
glucose than regular insulin in type 1 DM, and minimizes delayed postmeal
hypoglycemia (8).
5-Neutral protamine hagedorn (NPH): is intermediate-acting. It is prepared by

a process in which protamine is conjugated with regular insulin, producing a
product with a delayed onset but extended duration of action (9).
113
6-Glargine, degludec and detemir are long-acting ―peakless‖ human insulin
analogs that result in less nocturnal hypoglycemia than NPH insulin when given
at bedtime (8).
7-Insulin glargine and insulin degludec are given once daily and insulin detemir
is given once or twice daily according to individual requirements (1).
8-Biphasic insulins (biphasic isophane insulin, biphasic insulin aspart, biphasic

insulin lispro) are pre-mixed insulin preparations containing various combinations
of short acting insulin (regular insulin or rapid-acting insulin analogue) and an
intermediate-acting insulin (1).
9-Insulin is generally given by subcutaneous injection; the injection site should

be rotated to prevent local side effects (1, 7). Short-acting insulins (regular
insulin or rapid-acting insulin analogue) can also be given by I.V route for
urgent treatment (1).
10-The primary sites used for injecting

insulin are the lateral thigh, abdomen
and upper arm. Many practitioners
recommend using the abdominal area
because absorption from this site is least
affected by exercise and is the most
predictable (2).
11-Stability and Storage (see the

product's leaflet also)
A-Insulin is typically refrigerated,
though most vials are good for 28 days
at room temperature (9).
B-In practice, most patients store vials currently in use at room temperature
because injection of cold insulin is uncomfortable (2).
C-All unopened, extra vials or pen devices should be stored in the refrigerator
(2◦–8◦C) (2).
D-Insulin should not be used if it has been frozen or exposed to temperatures

>37◦C (2).
E-Insulin preparations should be protected from light (7).
12-Adminstarion of insulin S.C with a syringe (called insulin syringe) is still the
most common method of insulin administration.
114
13-Insulin pen devices are also available for
injecting insulin. Pen devices are often preferred as
they make insulin administration much easier,
especially for patients who need to take their insulin
doses away from home. They also can increase
dosing accuracy (2).
14-Insulin pump consists of a pump that can

programmed to deliver
predetermined amounts of
insulin [i.e., regular, or
rapid (mostly)] from a
reservoir to a
subcutaneously inserted
(2)
catheter or needle .
15-The dose of insulin is

expressed as units.
16-Hypoglycemia and
weight gain are the most
common adverse effects of insulin (8).
Insulin preparations
1
Any extra notes:
115
6.1.2.2-Glucagon-like peptide-1 receptor agonists
1-Glucagon-like peptide-1 receptor agonists, albiglutide, dulaglutide, exenatide,
liraglutide and lixisenatide should be reserved for combination therapy when other
treatment options for type 2 DM have failed (1).
2-Liraglutide (Saxenda®) was also approved for long-term obesity management
as an adjunct to lifestyle modification (2) (see chapter 2).
3-The main side effects of GLP-1 agonist therapy include nausea, vomiting, and
diarrhea. These GI adverse effects tend to lessen over time (9).
Glucagon-like peptide-1 receptor agonists

1
Any extra notes:
6.1.3-Diabetic complications (Table 6-2)
Table 6-2: Recommended drug(s) for some diabetic complications

Complications Recommended drug(s)
1 Cardiovascular disease ACE inhibitor, low dose aspirin and a
lipid-regulating drug (1).
2 Diabetic nephropathy ACE inhibitor or ARBs (1).
Gabapentin, pregabalin, carbamazepine,
Painful neuropathy opioid analgesics, Duloxetine,
amitriptyline, Nortriptyline, and
(1)
Capsaicin cream .
Diabetic Diabetic diarrhea Doxycycline or metronidazole.
3 neuropathy Octreotide may be useful in
(8)
unresponsive cases .
Gastroparesis Metoclopramide or erythromycin may
be helpful (8).
Orthostatic Fludrocortisone (8), Midodrine (1).
hypotension
Erectile dysfunction sildenafil, vardenafil, tadalafil (8).
4 Diabetic retinopathy Intravitreal anti-vascular endothelial growth
(proliferative retinopathy) factor (VEGF) therapy (ranibizumab) (8).
116
6.1.4-Hypoglycaemia
1-In hypoglycemia, if sugar cannot be given by mouth, glucagon can be given by
injection (1).
2-Alternatively, glucose intravenous infusion 20% may be given intravenously into
a large vein through a large-gauge needle. Glucose intravenous infusion 10% may
also be used but larger volumes are needed. Glucose intravenous infusion 50% is
not recommended because of the higher risk of extravasation injury and because
administration is difficult (1).
3-Diazoxide, administered by mouth, is useful in the management of patients with

chronic hypoglycemia from excess endogenous insulin secretion, either from an
islet cell tumor or islet cell hyperplasia. It has no place in the management of acute
hypoglycemia (1).

1
Any extra notes:
6.2-Thyroid and antithyroid drugs

6.2.1-Thyroid hormone
1-Thyroid hormone [thyroxine (levothyroxine)] is used in hypothyroidism (1).
(Hypothyroidism is readily treated by lifelong replacement therapy with
thyroxine) (7).
2-Thyroxine dose preferably taken at least 30 minutes before breakfast (1).

(taking levothyroxine at bedtime results in somewhat higher serum T 4 and lower
TSH levels. Therefore, the administration timing for levothyroxine should be kept
constant) (4).
3-Levothyroxine is the drug of choice for pregnant women (8).

1
Any extra notes:
117
6.2.2-Antithyroid drugs
1-Thionamides:
A-Thionamides (carbimazole, methimazole and propylthiouracil) are
effective in treating hyperthyroidism (2).
B-Antithyroid drug therapy should continue for 12 to 24 months to induce a
long-term remission (8).
C-Propylthiouracil is drug of choice during the first trimester of pregnancy,

during the second and third trimesters, methimazole (hence carbimazole) is
the drug of choice (8).
D-Pruritic maculopapular rashes, arthralgias, and fevers occur in up to 5% of

patients and may occur at greater frequency with higher doses and in children.
Rashes often disappear spontaneously but, if persistent, may be managed with
antihistamines (8).
E-Agranulocytosis is one of the serious adverse effects of thionamide therapy

that occurs within the first 3 months of therapy is agranulocytosis. Routine
monitoring is not recommended because of its sudden onset (8). Warn patient or
carers to tell doctor immediately if sore throat, mouth ulcers, bruising, fever,
malaise, or non-specific illness develops (1).
2-Radioactive sodium iodide (131 I) solution is used increasingly for the treatment
of thyrotoxicosis at all ages, particularly where medical therapy or compliance is a
problem, in patients with cardiac disease, and in patients who relapse after
thyroidectomy (1).
3-Iodine has been used as an adjunct to antithyroid drugs for 10 to 14 days before
partial thyroidectomy; however, there is little evidence of a beneficial effect (1).
4-Propranolol is useful for rapid relief of thyrotoxic symptoms (1). Propranolol has
been used in conjunction with iodine to prepare mildly thyrotoxic patients for
surgery. The thyroid gland is rendered less vascular thus making surgery easier (1).
Any extra notes:
118
6.3-Corticosteroids
1-The corticosteroids are used in physiological doses for replacement therapy in
adrenal insufficiency. Pharmacological doses are used when anti-inflammatory
or immunosuppressant effects are required (7) (for so many different diseases).
2-Cortisone and hydrocortisone have very appreciable mineralocorticoid (or
sodium-retaining) properties relative to their glucocorticoid (or antiinflammatory)
properties, prednisolone have considerably less, and others, such as betamethasone
and dexamethasone, have none or virtually none (7).
3-As a rough guide, the approximate equivalent doses of the main corticosteroids
in terms of their glucocorticoid (or anti-inflammatory) properties alone, are:
Betamethasone 0.75 Mg = Cortisone Acetate 25 Mg = Dexamethasone 0.75 Mg

= Hydrocortisone 20 Mg = Methylprednisolone 4 Mg = Prednisolone 5 Mg =
Prednisone 5 Mg = Triamcinolone 4 Mg (7).
4-Important:
A-The use of pharmacological doses of corticosteroids suppresses the
endogenous secretion of steroids by the anterior pituitary (7).
B-The adrenal suppression is less when the corticosteroid is given as a single

dose in the morning, and even less if this morning dose is given on alternate
days or less frequently (7).
C-Sudden withdrawal or reduction in dosage, may precipitate acute

adrenocortical insufficiency (7).
D-Gradual withdrawal of systemic corticosteroids is required for example :

-Patient who received more than 40 mg prednisolone (or equivalent)
daily for more than 1 week (1).
-Patient who received more than 3 weeks‘ treatment (1).
5-Corticosteroids have numerous side effects including nearly all body systems.
A-Most Common: Gastrointestinal irritation, increased appetite, nervousness/
restlessness, weight gain, acne, glucose intolerance (transient), lipid
abnormalities (transient) (10).
B-Rare/Severe/Important: Lower resistance to infections, adrenal suppression,

rounding out of the face, hirsutism, glaucoma, osteoporosis, peptic ulceration
(10)
.
6- Important: Corticosteroids (especially dexamethasone) are frequently abused

in Iraq. (prolonged use of glucocorticoids have a dramatic effect on body fat
distribution, resulting in the characteristic appearance of moon face) (7).
119
Corticosteroids
1
Any extra notes:
6.4-Disorders of bone metabolism

1-Osteoporosis occurs most commonly in postmenopausal women and in those
taking long-term oral corticosteroids (glucocorticosteroids) (1).
2-Two main classes of medications are available for osteoporosis: antiresorptives,

which decrease bone resorption, and anabolics, which promote bone
formation (5).
3-Those at risk of osteoporosis should maintain an adequate intake of calcium and

vitamin D and any deficiency should be corrected by increasing dietary intake or
taking supplements (1). Calcium carbonate is the salt of choice. It should be
ingested with meals to enhance absorption (5). Calcium citrate need not be taken
with meals (5).
4-Bisphosphonates (Alendronic acid, Ibandronic acid, Pamidronate disodium,

Risedronate sodium, Sodium clodronate, and Zoledronic acid)
A-Bisphosphonates are first-line therapy for osteoporosis in both men and

women (1).
111
B- Bisphosphonates must be administered carefully to optimize clinical benefit
and minimize adverse GI effects. Each oral tablet should be taken in the
morning with at least (180 mL) of plain water (not coffee, juice, mineral water,
or milk) at least 30 minutes (60 minutes for oral ibandronate) before consuming
any food, supplements, or medications. An exception is delayed-release
risedronate, which is administered immediately after breakfast with at least
(120 mL) of plain water (8).
C-The patient should remain upright (sitting or standing) for at least 30

minutes after alendronate and risedronate and 1 hour after ibandronate
administration to prevent esophageal irritation and ulceration (8).
D-If a patient misses a weekly dose, it can be taken the next day. If more
than 1 day has elapsed, that dose is skipped until the next scheduled
ingestion. If a patient misses a monthly dose, it can be taken up to 7 days
before the next scheduled dose (8).
E-Weekly, monthly and quarterly dosing may increase compliance with taking
bisphosphonate (5, 8).
F-I.V. Zoledronic is approved for once-yearly treatment of postmenopausal

osteoporosis, and administered once every other year to prevent osteoporosis
(5)
.
G-Bisphosphonates are also used in the treatment of Paget‘s disease,

hypercalcaemia of malignancy, and in bone metastases in breast cancer (1).
5-Denosumab (SC) is first-line therapy and should be considered in patients who

are unable to tolerate bisphosphonates (9).
6-Hormone therapies (estrogen with or without a progestogen) are not

recommended solely for osteoporosis but have positive bone effects when used
for other indications (8).
7-Raloxifene is an estrogen agonist on bone receptors but an antagonist at

breast receptors, is recommended as alternative therapy after bisphosphonates,
denosumab, or teriparatide (9).
8-Calcitonin is an endogenous hormone released from the thyroid gland when

serum calcium is elevated (8). Calcitonin is considered a last-line agent for the
treatment of osteoporosis (9).
9-Testosterone is not FDA indicated for osteoporosis (8).
10-Teriparatide and abaloparatide are (human parathyroid hormone related

peptide analog) (anabolic therapies) indicated (by s.c route) for osteoporosis (8).
111
Drugs for osteoporosis
1
Any extra notes:
6.5-Sex hormones
6.5.1-Female sex hormones
6.5.1.1-Hormone replacement therapy (HRT)
1-Hormone replacement therapy (HRT) with small doses of an oestrogen (e.g.
estradiol, estrone, estriol , ethinylestradiol) (together with a progestogen in women
with a uterus to reduces the risk of endometrial cancer) is appropriate for
alleviating menopausal symptoms such as vaginal atrophy or vasomotor
instability (1) [Vasomotor symptoms include hot flashes (sensation of heat that
typically begins in the face and chest and quickly spreads), night sweats].
2-Methods of progestogen administration:

A-Cyclic Estrogen and Progestogen: Estrogen is administered daily, and
progestogen is administered for 12 to 14 days of the month. The disadvantage
of this method of administration is the return of monthly menses in
approximately 90% of women 1 to 2 days following the last progestogen dose.
Women may view this scheduled bleeding as an advantage to this method of
administration as it limits spotting or soiling of undergarments (9)
B-Continuous Combined Estrogen and Progestogen: Estrogen and

progestogen are administered daily and result in endometrial atrophy.
Therefore, women do not experience a withdrawal bleed but may experience
unanticipated breakthrough bleeding or spotting during the month.
Although this may sound more appealing than a withdrawal bleed, women may
view the unpredictable bleeding or spotting as a disadvantage to this type of
administration (9)
3-Menopausal atrophic vaginitis may respond to topical vaginal oestrogen

(chapter 7) preparation used for a few weeks and repeated if necessary (1).
4-An oestrogen may be given orally or transdermaly (avoids 1st-pass effect) (1).
112
5-Clonidine may be used to reduce vasomotor symptoms in women who cannot
take an oestrogen, but clonidine may cause unacceptable side-effects (1).
Hormone replacement therapy (HRT)

1
Any extra notes:
6.5.1.2-Progestogens
1-Progestogens and drugs with progestogenic actions (e.g. dydrogesterone and
medroxyprogesterone and norethisterone) may be used in menstrual disorders
such as dysmenorrhoea and menorrhagia associated with dysfunctional uterine
bleeding (1, 3).
2-Progestogens may also be used in the management of endometriosis (3).
3-Progestogens may be used as contraceptive. Progestogens sometimes are used

with oestrogens for HRT (see above) (3).
4-Important: Progestogens have been used for the prevention of spontaneous

abortion in women with a history of recurrent miscarriage (habitual abortion) but
there is no evidence of benefit and they are not recommended for this purpose
(1)
.
5-Ulipristal is a progesterone receptor modulator with a partial progesterone

antagonist effect (1).
A-Ulipristal is used in the pre-operative treatment of moderate to severe
symptoms of uterine fibroids (1).
B-It is also used as an hormonal emergency contraceptive (1).
C-Ulipristal (up to four courses) is recommended in patients with heavy

menstrual bleeding associated with uterine fibroids (1).
Progestogens
1
113
2
Any extra notes:
6.5.2- Male sex hormones

1-The primary indication for androgens (e.g. Mesterolone, testosterone or its
esters) is as replacement therapy in male hypogonadal disorders caused by either
pituitary or testicular disorders (7).
2-Androgens are useless as a treatment of impotence and impaired

spermatogenesis unless there is associated hypogonadism (1).
3-The testosterone esters are usually formulated as oily solutions for

intramuscular use to give a prolonged duration of action (3).
Male sex hormones

1
Any extra notes:
6.5.3-Anti-androgens
1-Cyproterone acetate is an anti-androgen. It is used for the control of libido in
severe hypersexuality or sexual deviation in men. Cyproterone acetate may be used
with ethinylestradiol in women for the control of acne and hirsutism (7). It is given
after food (1).
2-Cyproterone acetate is also licensed for use alone in patients with metastatic
prostate cancer (1).
3-Fatigue and lassitude may be produced by the drug which may impair
performance of skilled tasks (e.g. driving) (1).
114
Any extra notes:
6.5.4-Anabolic steroids
1-Nandrolone is an anabolic steroid with some androgenic. It is usually given in
the form of oily intramuscular injections as an anabolic after debilitating
illness (7).
2-Important: The protein-building properties of anabolic steroids have not proved

beneficial in the clinical setting. Their use as body builders or tonics is unjustified;
some athletes abuse them (1).
3-Anabolic steroids have been given for osteoporosis in women but they are no
longer advocated for this purpose (1).

1
Any extra notes:
6.6-Hypothalamic and anterior pituitary hormones and

antioestrogens
6.6.1-Anti-oestrogens
1-Clomifene (clomiphene) :
A-Clomifene is the most widely used drug in the treatment of female with
anovulatory infertility (1, 7).
B-The usual oral dose is 50 mg of clomifene citrate daily for 5 days starting
within about 5 days of onset of menstruation (preferably on 2nd day). If
ovulation does not occur, a course of 100 mg daily for 5 days may be given (1, 7).
C-Patients should be warned that there is a risk of multiple pregnancy (rarely

more than twins) (1).
2-Tamoxifen (7) :
A-Tamoxifen is an oestrogen antagonist with actions similar to those of
clomifene citrate.
B-It is used in the treatment of breast cancer.
115
C-Tamoxifen is also used to stimulate ovulation in women with anovulatory
infertility.
Anti-oestrogens
1
Any extra notes:
6.6.2-Gonadotrophins
Follicle-stimulating hormone (FSH) and luteinizing hormone (LH) together,
follicle-stimulating hormone alone, or chorionic gonadotrophin, are used in the
treatment of infertility in women with proven hypopituitarism or who have not
responded to clomifene (1).
Gonadotrophins
1
Any extra notes:
6.6.3-Growth hormone
1-Growth hormone (Recombinant Human Growth Hormone somatropin) is used
to treat deficiency of the hormone in children and in adults (1).
2-Pegvisomant is a highly selective growth hormone receptor antagonist

indicated for the treatment of acromegaly (1).
116
6.7-Antidiuretic hormone disorders
6.7.1-Posterior pituitary hormones
1-Vasopressin (antidiuretic hormone, ADH) is used in the treatment of pituitary
(‗cranial‘) diabetes insipidus as is its analogue desmopressin (1).
2-Desmopressin is more potent and has a longer duration of action than

vasopressin; unlike vasopressin it has no vasoconstrictor effect (It is given by
mouth or intranasally for maintenance therapy) (1).
3-Other uses:
A-Desmopressin may also have a role in nocturnal enuresis. Patients being
treated for primary nocturnal enuresis should be warned to limit fluid intake to
minimum from 1 hour before dose until 8 hours afterwards; and to stop
taking desmopressin during an episode of vomiting or diarrhea (until fluid
balance normal) (1).
B-Desmopressin is also used to boost factor VIII concentration in mild to

moderate haemophilia and in von Willebrand‘s disease (1).
C-Terlipressin, a derivative of vasopressin, is used to control variceal

bleeding in portal hypertension in patient with liver cirrhosis (1).
6.7.2-Antidiuretic hormone antagonists

Demeclocycline and Tolvaptan (a vasopressin V2-receptor antagonist) can be
used in the treatment of hyponatraemia resulting from inappropriate secretion of
antidiuretic hormone (1).
Drugs for antidiuretic hormone disorders

Any extra notes:
6.8-Other endocrine drugs

6.8.1-Bromocriptine and other dopaminergic drugs
1-Bromocriptine is a stimulant of dopamine receptors in the brain; it also inhibits
release of prolactin by the pituitary. Cabergoline has actions and uses similar to
those of bromocriptine, but its duration of action is longer (1)(it is usually given
once weekly).
117
2-Uses:
A-Bromocriptine, inhibits the secretion of prolactin from the anterior pituitary
and is used in the treatment of prolactinoma (prolactin-secreting pituitary
adenomas) and endocrinological disorders associated with hyperprolactinaemia,
including amenorrhoea, galactorrhoea, and infertility in both men and
women (7).
B-Growth hormone secretion may be suppressed by bromocriptine in some

patients with acromegaly (7).
C-Because of its dopaminergic activity bromocriptine is also used in the

management of Parkinson’s disease (7).
D-Bromocriptine is also approved for type 2 diabetes mellitus (8).
3-Adverse Effects:
A-Nausea is the most common adverse effect at the beginning of treatment
with bromocriptine, but vomiting, dizziness, and orthostatic hypotension may
also occur. Syncope has followed initial doses (7).
B-Adverse effects are generally dose-related and may therefore be more

frequent with the higher doses (7).
C-Nausea may be reduced by gradual increase of the dose, taking

bromocriptine with food; domperidone (chapter 1) may also be given at least
1 hour before bromocriptine, for the first few days of therapy (7).
D-Excessive daytime sleepiness and sudden onset of sleep can occur with
dopamine-receptor agonists. Patients starting treatment with these drugs should
be warned of the risk and of the need to exercise caution when driving or
operating machinery. Those who have experienced excessive sedation or
sudden onset of sleep should refrain from driving or operating machines until
these effects have stopped occurring (1).
4-Concerning cabergoline: Dispense in original container (contains desiccant) (1).

(a desiccant is a hygroscopic substance that induces or sustains a state of dryness
(desiccation) in its vicinity)
Bromocriptine and other dopaminergic drugs

1
118
Any extra notes:
6.8.2-Drugs affecting gonadotrophins

6.8.2.1-Danazol
1-Danazol inhibits pituitary gonadotrophins (follicle stimulating hormone and
luteinising hormone); it combines androgenic activity with antioestrogenic and
antiprogestogenic activity. It is used mainly for the treatment of endometriosis
(1)
. (Endometriosis is a condition affecting women mainly in their reproductive
years, and caused by endometrial tissue developing outside the uterine cavity) (1).
2-Other uses of danazol are for severe pain and tenderness in benign fibrocystic
breast disease not responding to other treatment and for hereditary angioedema (1).
3-Cetrorelix and ganirelix are luteinizing hormone releasing hormone

antagonists, which inhibit the release of gonadotrophins (LH and FSH). They are
used in the treatment of infertility by assisted reproductive techniques (1).
Any extra notes:
6.8.2.2-Gonadorelin analogues
1-Administration of gonadorelin analogues [buserelin, goserelin, leuprorelin,
nafarelin, and triptorelin (which are more potent and have a longer duration of
action)] produces an initial phase of stimulation; continued administration is
followed by down-regulation of gonadotrophin-releasing hormone receptors,
thereby reducing the release of gonadotrophins (follicle stimulating hormone and
luteinising hormone) which in turn leads to inhibition of androgen and oestrogen
production (1, 7).
2-Gonadorelin analogues are used in the treatment of endometriosis, and prostate

cancer (1).
3-Other uses include the treatment of precocious puberty, infertility, anaemia due
to uterine fibroids (together with iron), breast cancer, and before intra-uterine
surgery. Use of leuprorelin and triptorelin for 3 to 4 months before surgery reduces
the uterine volume, fibroid size and associated bleeding (1).
119
Any extra notes:
6.9-Cushing’s Syndrome
1-Most types of Cushing‘s syndrome are treated surgically. Metyrapone has
been found helpful in controlling the symptoms of the disease (1).
2-Ketoconazole An imidazole derivative which acts as a potent inhibitor of

cortisol and aldosterone synthesis is used for treatment of endogenous Cushing‘s
syndrome [dizziness and somnolence may affect the performance of skilled tasks
(e.g. driving)] (1).
Any extra notes:
References
1-BNF 74.
2-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical use of drugs, 11th ed.,
2018.
3-Dan L. Longo, et al, eds. Harrison's Principles of Internal Medicine, 19th Edition. Copyright © 2015 by
the McGraw-Hill Companies, Inc.
4-Maxine A. Papadakis, et al, eds. Current Medical Diagnosis & Treatment, 56th Edition 2017 .
6-American Diabetes Association . Standards of Medical Care in Diabetes 2018. Diabetes Care Volume
41, Supplement 1, January 2018. Pages: S1-S159.
7-Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press
8-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 10th edition. 2017.
9-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 4th edition. 2016. by The McGraw-
Hill Companies
Learning, LLC
121
Chapter Seven : Genito-urinary System
7.1-Drugs for genito-urinary disorders
7.1.1-Drugs for benign prostatic hyperplasia (BPH):

1-The alpha1-selective alpha blockers (like: alfuzosin, doxazosin, tamsulosin and
terazosin) relax smooth muscle in BPH producing an increase in urinary flow-rate
and an improvement in obstructive symptoms (1).
2-The 5α-reductase inhibitors (finasteride and dutasteride)(decreases the

conversion of testosterone to the more active form) (reduce prostate volume,
although this takes a number of months) (2).
So : α1-blokers can produce rapid symptomatic relief only (not affect the prostate
volume) while 5α-reductase inhibitors reduce prostate volume but this effect is
delayed. Therefore both drugs may be used together.
3-Tamsulosin, may be used also for expulsion of lower ureteral stones (for both
male and female)(2).
4-α1-blokers can cause orthostatic hypotension which may be severe and produce
syncope after the initial dose. This reaction can be avoided by starting treatment
with a low dose, preferably at night )(2). Patient should be warned to lie down if
symptoms such as dizziness, fatigue or sweating develop, and to remain lying
down until they abate completely (1).
5-Tamsulosin and silodosin, third-generation α1-adrenergic antagonists, are

selective for prostatic α1A receptors. Therefore, they do not cause peripheral
vascular smooth muscle relaxation and associated hypotension (3).
6-Important:
A-Women of childbearing potential should avoid handling crushed or
broken tablets of finasteride or leaking capsules of dutasteride (1).
B-Dutasteride and finasteride are excreted in semen and use of a condom is

recommended if sexual partner is pregnant or likely to become pregnant (1).
7-In the treatment androgenetic alopecia in men, finasteride is given orally in a

low dose (1 mg daily) while the dose used for BPH is 5 mg daily.
8-Tadalafil (5 mg daily) is approved to treat the signs and symptoms of benign

prostatic hyperplasia (1).
121
5α-reductase inhibitors
1
α1-blokers
1
Any extra notes:
7.1.2-Urinary incontinence
(UI)
1-UI occurs as a result of
overfunctioning or
underfunctioning of the urethra,
bladder, or both. Urethral
underactivity is known as stress
UI. Bladder overactivity is
known as Urge UI (bladder
muscle is overactive and contracts
inappropriately) (3).
2-The antimuscarinic oxybutynin has direct smooth muscle relaxant properties

and has been most widely used for Urge UI (1).
3-A modified-release preparation of oxybutynin hydrochloride is effective and has

fewer side effects; a transdermal patch is also available (1).
4-Tolterodine, and the newer antimuscarinic drugs (darifenacin, fesoterodine,

solifenacin, and trospium) are also licensed for Urge Urinary Incontinence (3).
122
5-Mirabegron a β3-adrenergic agonist alternative to anticholinergic/antimuscarinic
drugs for managing Urge UI (3).
6-Stress incontinence is generally managed by non-drug methods (specific type

of exercise) . Duloxetine (chapter 4) can be added and is licensed for the treatment
of moderate to severe stress incontinence in women (1).
Drugs for urinary incontinence

1
Any extra notes:
7.1.3-Nocturnal enuresis
1-Children are generally expected to be dry by a developmental age of 5 years,
and historically it has been common practice to consider children for treatment
only when they reach 7 years; however, symptoms may still persist in a small
proportion by the age of 10 years (1).
2-Initially, advice should be given on fluid intake, diet, toileting behavior. For
children who do not respond to this advice (more than 1–2 wet beds per week), an
enuresis alarm should be the recommended (1).
3-Combined treatment with desmopressin, or the use of desmopressin alone, is

recommended if the initial alarm treatment is unsuccessful or it is no longer
appropriate or desirable (1).
4-Treatment with oral or sublingual desmopressin is recommended for children

over 5 years of age when alarm use is inappropriate or undesirable, or when rapid
or short-term results are the priority (for example, to cover periods away from
home) (1).
5-Desmopressin (chapter 6), an analogue of vasopressin, is used for nocturnal

enuresis; it is given by oral or by sublingual administration. Particular care is
needed to avoid fluid overload. Treatment should not be continued for longer than
3 months without interrupting treatment for 1 week for full re-assessment (1).
123
6-Important : Desmopressin should not be given intranasally for nocturnal
enuresis due to an increased incidence of side-effects (1).
7-To reduce the risk of water intoxication, children should drink no more than
240 mL of fluid from 1 hour before to 8 hours after administration of desmopressin
(4)
.
8-Tricyclic antidepressants (see chapter 4 ) such as imipramine, are used but

relapse is common after withdrawal. Initial treatment should continue for 3
months; further courses can be considered following a medical review every 3
months (1).
Drugs for urinary incontinence

1
Any extra notes:
7.1.4-Drugs for erectile dysfunction

1-Phosphodiesterase type-5 inhibitors: Avanafil, Sildenafil, tadalafil and
vardenafil are licensed for the treatment of erectile dysfunction (ED)(1).
2-Tadalafil is a longer-acting drug. It can be used as required, but can also be used
as a regular lower daily dose to allow for spontaneous (rather than scheduled)
sexual activity or in those who have frequent sexual activity (2).
3-They have no effect on the penis in the absence of sexual stimulation (2).
(Adequate sexual stimulation is needed to trigger the events leading to erection) (5).
4-Adverse effects most commonly reported are related vasodilatation and

include Headache and flushing. Also common are visual disturbances such as
blurred vision (2).
5-Phosphodiesterase type-5 inhibitors may potentiate the hypotensive effects of

nitrates, and are therefore contra-indicated in patients receiving such drugs (2).
6-Adminstraion
A-Onset of effect of sildenafil (but not tadalafil or vardenafil ) may be delayed
if taken with food (1).
124
B-Dose to be taken (Avanafil: 15–30 minutes, sildenafil: 1 hour, tadalafil: at
least 30, and vardenafil 25–60 minutes) before sexual activity (1).
7-Important :
A-Sildenafil, and tadalafil are licensed for the treatment of pulmonary arterial
hypertension (for both male and female) (1).
B-Tadalafil (5 mg daily) is approved to treat the signs and symptoms of benign

prostatic hyperplasia (1).
8-Intracavernosal, intraurethral or topical application of alprostadil

(prostaglandin E1) is recommended as second-line therapy under careful medical
supervision (1).
Drugs for erectile dysfunction

1
Any extra notes:
7.1.5-Premature ejaculation
1-Dapoxetine is a short-acting selective serotonin re-uptake inhibitor indicated for
premature ejaculation to be taken approximately 1–3 hours before sexual activity
(1)
.
2-Dapoxetine –induced postural hypotension and syncope: Patients should be

advised to maintain hydration and to sit or lie down until prodromal symptoms
such as nausea, dizziness, and sweating abate (1).

1
Any extra notes:
125
7.1.6-Other preparations for urinary disorders
7.1.6.1-Alkalinisation of urine
1-The alkalinizing action may relieve the discomfort of cystitis caused by lower
urinary tract infections (1).
2-Prevention of uric acid stones is also an indication for alkalinization of urine

(2)
.
3-Potassium Citrate, Sodium citrate and sodium bicarbonate are used for this
purpose (1).
Drugs for Alkalinisation of urine

1
Any extra notes:
7.1.6.2-Phenazopyridine and Rowatinex®

1-Phenazopyridine exerts an analgesic effect on the mucosa of the urinary tract and
is used to provide symptomatic relief of pain and irritability in conditions such as
cystitis and prostatitis, and urethritis. It is given after food (2). It cause
discoloration of urine.
2-Important : If phenazopyridine is given with an antibacterial for the treatment

of urinary-tract infections, treatment should usually not exceed 2 days (2)
(Urinary analgesics may mask signs and symptoms of UTIs not responding to
antimicrobial therapy) (3).
3-A terpene mixture (Rowatinex®) is claimed to be of benefit in urolithiasis

(stone) for the expulsion of calculi (1). It is given before food (1).
126
Any extra notes:
7.1.6.3-Bladder instillations and urological surgery

1-Aqueous chlorhexidine can be used in the management of common infections of
the bladder but it is ineffective against most Pseudomonas spp (1).
2-Sterile sodium chloride solution 0.9%p. (physiological saline) is usually

adequate and is preferred as a mechanical irrigant (1).
3-Continuous bladder irrigation with amphotericin may be of value in mycotic

infections in adults (1).
4-Bladder instillations of doxorubicin and mitomycin are used for recurrent

superficial bladder tumours (1).
5-Instillation of epirubicin is used for treatment and prophylaxis of certain forms

of superficial bladder cancer (1).
6-Instillation of BCG (Bacillus Calmette-Guérin), is licensed for the treatment of

primary or recurrent bladder carcinoma in-situ and for the prevention of
recurrence following transurethral resection (1).
7.2-Preparations for vaginal and vulval conditions

7.2.1-Topical Hormone replacement therapy (HRT) for vaginal atrophy
A cream containing an oestrogen may be applied on a short-term basis to improve
the vaginal epithelium in menopausal atrophic vaginitis (1).
Scientific name Trade names(if available) Dosage form
Any extra notes:
7.2.2- Vaginal and vulval infections

Guideline for applying vaginal products (pessaries or vaginal cream) (6):
127
1.Wash hands with soapy water before
using the pessaries/cream.
2.Remove any external foil or plastic
packaging from the pessary and
applicator.
3.If an applicator is provided, load the
applicator as directed by the
manufacturer.
4.Stand with one leg on a chair or lie
down with knees bent and legs apart.
5.Press the applicator plunger to insert
the pessary or cream into the vagina
(see the figure ). If no applicator is provided, insert the pessary as high into the
vagina as is comfortable by pushing gently but firmly in an upwards and
backwards direction using the middle finger. (If pregnant, do NOT use an
applicator to insert pessaries; insert using finger method.)
6.If an applicator is used, wash it ready for next use.
7.Wash hands once more.
7.2.2.1-Vaginal fungal infections

1-Vaginal candidiasis is treated primarily with antifungal pessaries or cream
inserted high into the vagina (including during menstruation) (1).
2-Single-dose preparations offer an advantage when compliance is a problem

(1)
.
3-Imidazole drugs (clotrimazole, econazole, and miconazole) are effective against

candida in short courses of 1 to 14 days according to the preparation used;
treatment can be repeated if initial course fails to control symptoms or if symptoms
recur (1).
4-Most internal preparations should be administered at night (this give the drug
time to be absorbed, and eliminate the possibility of accidental loss which is more
likely to occur if the person is mobile) (7).
5-Oral treatment of vaginal infection (e.g. with fluconazole or itraconazole) is

also effective (1).
6-Vaginal antifungal can be used during the menstrual period. If desired, wait
and treat the infection after the menses end. Do not, however, interrupt a course
of therapy because of the beginning of period (8).
128
Antifungals for Vaginal Fungal infections
Scientific name Trade Dosage Treatment course
names form
1
Any extra notes:
7.2.2.2-Other infections
1-Trichomonal infections commonly involve the lower urinary tract as well as the
genital system and need systemic treatment with metronidazole or tinidazole (1).
2-Bacterial infections with Gram-negative organisms are particularly common in

association with gynecological operations and trauma. Metronidazole is effective
against certain Gram-negative organisms, especially Bacteroides spp. and can be
used prophylactically in gynecological surgery (1).
3-Clindamycin cream and metronidazole gel are indicated for bacterial

vaginosis (1).
4-Vaginal preparations intended to restore normal acidity may prevent recurrence

of vaginal infections and permit the re-establishment of the normal vaginal flora (1).
5-The antiviral drugs aciclovir, famciclovir, and valaciclovir can be used in the
treatment of genital infection due to herpes simplex virus (1).
Any extra notes:
129
7.3-Drugs used in obstetrics
7.3.1-Tocolytics (Myometrial relaxants)
1-Tocolytics inhibit uterine contractions and are used in premature labour to
delay early delivery (2).
2-The oxytocin receptor antagonist, atosiban, is licensed for the inhibition of

uncomplicated premature labour between 24 and 33 weeks of gestation. Atosiban
may be preferable to a beta2 agonist because it has fewer side effects (2).
3-The dihydropyridine CCB nifedipine is also used and has fewer side-effects than
a beta2 agonist (2).
4-The beta2 agonists salbutamol and terbutaline are licensed for inhibiting
uncomplicated premature labour between 22 and 37 weeks of gestation to permit a
delay in delivery of up to 48 hours. Oral therapy is no longer recommended (2).
Any extra notes:
7.3.2-Induction and augmentation of labour

1-Oxytocin is administered by slow intravenous infusion, using an infusion pump,
to induce or augment labour (1).
2-Dinoprostone is available as vaginal tablets, pessaries and vaginal gels for the
induction of labour (1).
3-Misoprostol is given orally or vaginally for the induction of labour (1).
Drugs for Induction and augmentation of labour

1
Any extra notes:
131
7.3.3-Termination of pregnancy
1-Gemeprost, a prostaglandin administered vaginally as pessaries, is suitable for
the medical induction of late therapeutic abortion (1).
2-The prostaglandin misoprostol is given by mouth, buccally, sublingually, or

vaginally, to induce medical abortion (1).
3-Pre-treatment with mifepristone can facilitate the process of medical abortion.

It sensitizes the uterus to subsequent administration of a prostaglandin and,
therefore, abortion occurs in a shorter time and with a lower dose of prostaglandin
(1)
.
Drugs for Termination of pregnancy

1
Any extra notes:
7.3.4-Prevention and treatment of uterine hemorrhage

1-If the uterus fails to contract adequately after delivery (uterine atony), or if
retained placental remnants prevent retraction of the placental bed, postpartum
hemorrhage may occur. These two causes account for about 80% of cases of
postpartum hemorrhage (2).
2-Postpartum hemorrhage may be fatal to the mother unless promptly dealt with,
and management generally involves:
• removal of the placenta if it has not been expelled.
• the use of oxytocics to contract the uterus.
• transfusion if blood loss is severe.
3-Parenteral oxytocin, or an ergot alkaloid (ergometrine or methylergometrine),

is the oxytocic generally used to control bleeding due to uterine atony (2).
4-Carboprost has an important role in severe postpartum hemorrhage

unresponsive to ergometrine maleate and oxytocin (1).
5-Misoprostol can be used in postpartum hemorrhage when oxytocin, ergometrine

maleate, and carboprost are not available or are inappropriate (1).
131
Any extra notes:
7.4-Hormonal contraceptives
7.4.1-Combined oral contraceptives (COCs)
1-COCs are a combination of estrogen (prevent the development of the dominant
follicle) and progestin (prevent ovulation) (5).
2-The COCs are available in a variety of cycle lengths.

The most common is the 28-day pack that contains 21
days of active pills (pills that contain estrogen and
progestin) followed by 7 days of placebo pills (to
minimize confusion) the patient takes one pill daily. After
taking the last pill of a 28-day pack, the patient should
begin a new pack the next day (5).
3-Combined oral contraceptives containing a fixed amount of an oestrogen and a

progestogen in each active tablet are termed ‗monophasic’; those with varying
amounts of the two hormones are termed ‗phasic’ (1).
4-Phased preparations are generally reserved for women who either do not have
withdrawal bleeding or who have breakthrough bleeding with monophasic
products (1).
5-A transdermal patch and a vaginal ring, both containing an oestrogen with a
progestogen, are also available (1).
6-The majority of combined oral contraceptives contain ethinylestradiol as the

oestrogen component; mestranol and estradiol are also used (1).
7-The combination of ethinylestradiol with either (desogestrel, drospirenone or

gestodene) may be considered for women who have side-effects (such as acne,
headache, depression, breast symptoms, and breakthrough bleeding) with other
progestogens (1).
8-Dosing for the Drug Class:

A-In the first-day start method, women take the first pill on the first day of
the next menstrual cycle (3).
132
B-If reasonably certain woman is not pregnant, first course can be started on
any day of cycle—if starting on day 6 of cycle or later, additional precautions
(barrier methods) necessary during first 7 days (1).
C-Each tablet should be taken at approximately same time each day; if

delayed, contraceptive protection may be lost (1).
D-21-day combined preparations, 1 tablet daily for 21 days; subsequent

courses repeated after a 7-day interval (during which withdrawal bleeding
occurs) (1).
E-Every day (ED) combined preparations, 1 active tablet daily for 21 days,
followed by 1 inactive or iron tablet daily for 7 days; subsequent courses
repeated without interval (withdrawal bleeding occurs when inactive tablets
being taken) (1, 9).
9-Interactions:
Women using combined hormonal contraceptive patches, vaginal rings or oral
tablets who require enzyme inducing drugs or griseofulvin should be advised
to change to a reliable contraceptive method that is unaffected by enzyme-
inducers, such as some parenteral progestogen-only contraceptives or intra-
uterine devices. This should be continued for the duration of treatment and for
four weeks after stopping (1).
10-COCs have benefits aside from pregnancy prevention that include treatment of
acne, hirsutism, premenstrual syndrome (PMS), menstrual cycle regulation (5).
11-Missed pill
A-The critical time for loss of contraceptive protection is when a pill is omitted
at the beginning or end of a cycle (which lengthens the pill-free interval) (1).
B-If a woman forgets to take a pill, it should be taken as soon as she

remembers, and the next one taken at the normal time (even if this means taking
2 pills together) (1).
C-A missed pill is one that is 24 or more hours late. If a woman misses only
one pill, she should take an active pill as soon as she remembers and then
resume normal pill-taking. No additional precautions are necessary (1).
D-If a woman misses 2 or more pills (especially from the first 7 in a packet),
she may not be protected. She should take an active pill as soon as she
remembers and then resume normal pill-taking. In addition, she must either
abstain from sex or use an additional method of contraception such as a condom
for the next 7 days. If these 7 days run beyond the end of the packet, the next
packet should be started at once, omitting the pill-free interval (or, in the case
of everyday (ED) pills, omitting the 7 inactive tablets) (1).
133
E-Emergency contraception is recommended if 2 or more combined oral
contraceptive tablets are missed from the first 7 tablets in a packet and
unprotected intercourse has occurred since finishing the last packet (1).
12-Diarrhea and vomiting:

A-Vomiting and persistent, severe diarrhea can interfere with the absorption of
combined oral contraceptives. If vomiting occurs within 2 hours of taking a
combined oral contraceptive another pill should be taken as soon as possible (1).
B-In cases of persistent vomiting or severe diarrhea lasting more than 24

hours, additional precautions should be used during and for 7 days after
recovery (1).
C-If the vomiting and diarrhea occurs during the last 7 tablets, the next pill-
free interval should be omitted (in the case of ED tablets the inactive ones
should be omitted) (1).
7.4.2-Progestogen-only contraceptives
7.4.2.1-Oral progestogen-only contraceptives
1-Advantages
A-Oral progestogen-only preparations may offer a suitable alternative when
oestrogens are contra-indicated (including those patients with venous
thrombosis or a past history of venous thrombosis) (1).
B-Confusion with pill taking is minimized because there is no placebo week

and all 28 pills in each pack are the same (5).
2-Disadvantages
A-Important: They must be taken even more regularly than COCs, they are
taken as one tablet daily, on a continuous basis, starting on day 1 of cycle and
taken at the same time each day (if delayed by longer than 3 hours
contraceptive protection may be lost) (5, 8).
B-They may have a higher failure rate than combined preparations(1) (0.3%
- 8%) (5).
3-Interactions:
The efficacy of oral progestogen-only preparations is reduced by enzyme-
inducing drugs or griseofulvin and an alternative contraceptive method,
unaffected by the interacting drug, is recommended during treatment with an
interacting drug and for at least 4 weeks afterwards (1).
7.4.2.2-Parenteral progestogen-only contraceptives

1-Injectable Medroxyprogesterone acetate is given as a 150-mg intramuscular
injection(5) repeated every 12 weeks (1).
134
7.4.3-Emergency hormonal contraception
1-Hormonal emergency contraceptives include levonorgestrel and ulipristal ;
either drug should be taken as soon as possible after unprotected intercourse to
increase efficacy (1).
2-Levonorgestrel is effective if taken within 72 hours (3 days) of unprotected

intercourse. Ulipristale, is effective if taken within 120 hours (5 days) of
unprotected intercourse (1).
7.4.4-Use of oral contraceptives during breast-feeding

1-The American College Of Gynecology (ACOG) recommends waiting at least
6weeks before starting any estrogen-containing contraceptive regardless of
breast-feeding status (By this time, the increased risk of thrombosis that occurs
during pregnancy should be reduced to baseline). However, COCs have been
reported to decrease milk quantity and quality. Therefore, many providers suggest
avoiding COCs in women who are exclusively breastfeeding (5).
2-For non–breast-feeding women, a progestin-only contraceptive may be used

immediately postpartum and 6 weeks postpartum if solely breast-feeding and in
some cases 3 weeks postpartum if partially breast-feeding (5).
Hormonal contraceptives
1
Any extra notes:
135
7.5-Spermicidal contraceptives (nonoxinol ‘9’)
1-Nonoxynol-9, a surfactant that destroys the cell membranes of sperm, is the most
commonly used spermicide (4).
2-Nonoxynol-9 is available in a variety of forms, including a cream, foam, film,

gel, suppository, and tablet (4).
3-To be used most effectively, spermicides must be placed in the vagina not more
than 1 hour prior to sexual intercourse, and they must come in contact with the
cervix (4).
4-Spermicides may be used alone, with a barrier method, or adjunctively with

other forms of contraceptives to provide additional protection against unwanted
pregnancy (4). However, they are generally considered relatively ineffective when
used as the sole method of contraception, and such use is not recommended (2).

1
Any extra notes:
References
1-BNF-74.
Press 2009.
3-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 10th Edition.
2017.
4-Marie A. Chisholm-Burns. Pharmacotherapy Principles & Practice. 4th edition. 2016.
11th ed., 2018.
6-Christopher A Langley, Dawn Belcher. Applied Pharmaceutical Practice. Pharmaceutical
Press. 2009.
Learning, LLC
136
Chapter Eight: Immune System and Malignant Disease
8.1-Immunosuppressants
1-Immunosuppressants with their indication are shown in table 8.1 (1).
Table 8.1: Immunosuppressants with their indication(s) (1)

Immunosuppressants Indication(s)
1 Azathioprine Rheumatoid arthritis, suppression of transplant
rejection, severe refractory eczema, inflammatory
bowel disease, myasthenia gravis and autoimmune
conditions
2 Ciclosporin Severe acute ulcerative colitis, rheumatoid
arthritis, atopic dermatitis, psoriasis, organ
transplantation, nephrotic syndrome
3 Sirolimus Prophylaxis of organ rejection in kidney allograft
recipients
4 Tacrolimus Prophylaxis of organ rejection
5 Canakinumab Acute gout
6 Basiliximab Prophylaxis of acute organ rejection
7 Belimumab Systemic lupus erythematosus
8 Mycophenolate mofetil Prophylaxis of organ rejection
9 Belatacept Prophylaxis of organ rejection
8.2-Drugs for multiple sclerosis

Drugs used for multiple sclerosis are listed in table 8.2 (2).
Table 8-2. Treatment of multiple sclerosis (2).

Conditions Medications
1 Acute episode, including relapse Methylprednisolone, Prednisone,
Dexamethasone
2 Relapse prevention, first-line Interferon β-1 a, Interferon β -1 b
treatment Glatiramer, Fingolimod,
Teriflunomide, Dimethylfumarate
3 Relapse prevention for disease Natalizumab, Fingolimod
activity despite use of first-line Teriflunomide, Dimethylfumarate
treatment Alemtuzumab, Mitoxantrone
4 High disease activity (typically with Natalizumab, Alemtuzumab
multiple gadolmium-enhancing
lesions on MRI.
8.3-Malignant disease
8.3.1-Antineoplastic monoclonal antibodies
Antineoplastic monoclonal antibodies with their indication(s) are listed in table 8-3
(1)
.
137
Table 8.3: Antineoplastic monoclonal antibodies with their indication(s) (1)
Antineoplastic Indication(s)
monoclonal antibodies
1 Bevacizumab Colorectal cancer, breast cancer, renal cell
carcinoma, lung cancer, [ovarian, fallopian tube,
or peritoneal cancer].
2 Blinatumomab Relapsed or refractory Philadelphia chromosome
negative acute lymphoblastic leukemia
3 Brentuximab vedotin Hodgkin‘s disease, Relapsed or refractory
systemic anaplastic large cell lymphoma
4 Catumaxomab Treatment of malignant ascites in patients with
epithelial cell adhesion molecule (EpCAM)
positive carcinomas
5 Cetuximab Colorectal cancer, squamous cell cancer of
the head and neck
6 Daratumumab Multiple myeloma
7 Elotuzumab Multiple myeloma
8 Ipilimumab Treatment of melanoma
9 Necitumumab Squamous non-small-cell lung cancer
10 Nivolumab Melanoma, non-small cell lung cancer, renal cell
carcinoma
11 Obinutuzumab Chronic lymphocytic leukaemia
12 Ofatumumab Chronic lymphocytic leukaemia (CLL)
13 Panitumumab Colorectal cancer
14 Pembrolizumab Melanoma
15 Pertuzumab Breast cancer
16 Ramucirumab Gastric cancer or gastrooesophageal junction
adenocarcinoma
17 Rituximab Rheumatoid arthritis, follicular non-Hodgkin‘s
lymphoma, diffuse large B-cell non-Hodgkin‘s
Lymphoma, chronic lymphocytic leukaemia,
18 Siltuximab Multicentric Castleman‘s disease (MCD)
19 Trastuzumab Breast cancer, gastric cancer.
8.3.2-General Side-effects of cytotoxic drugs

General Side-effects of cytotoxic drugs are (1):
A-Extravasation of intravenous drugs B-Oral mucositis
C-Tumour lysis syndrome D-Hyperuricaemia E-Bone-marrow suppression
F-Alopecia G-Thromboembolism H-Nausea and vomiting
8.3.3-Alkylating agents (Antineoplastics)

Alkylating agents with their indication(s) are listed in table 8-4 (1).
138
Table 8.4: Alkylating agents with their indication(s) (1)
Alkylating agents Indication(s)
1 Bendamustine Treatment of chronic lymphocytic leukaemia,| Treatment of
non-Hodgkin‘s lymphoma, Treatment of multiple myeloma
2 Busulfan Chronic myeloid leukaemia,
3 Carmustine Multiple myeloma , Non-Hodgkin‘s lymphomas , Brain
tumours
4 Chlorambucil Some lymphomas and chronic leukaemias
5 Cyclophosphamide Rheumatoid arthritis, Used mainly in combination with other
agents for treating a wide range of malignancies, including
some ukaemias, lymphomas, and solid tumours
6 Dacarbazine Metastatic melanoma | Soft-tissue sarcomas (combination
therapy) | Hodgkin‘s disease (combination therapy)
7 Estramustine Prostate cancer
8 Ifosfamide Malignant disease
9 Lomustine Hodgkin‘s disease resistant to conventional therapy ,
Malignant melanoma , Certain solid tumours
10 Melphalan Multiple myeloma, Polycythaemia vera, Localised malignant
melanoma of the extremities , Localised soft-tissue sarcoma
of the extremities
11 Temozolomide glioblastoma multiforme, malignant glioma
12 Thiotepa Conditioning treatment before haematopoietic stem cell
transplantation in the treatment of haematological disease or
solid tumours, in combination with other chemotherapy
13 Treosulfan Ovarian cancer
14 Daunorubicin Acute myelogenous leukaemia , Acute lymphocytic
Leukaemia, Advanced AIDS-related Kaposi‘s sarcoma
15 Doxorubicin Acute leukaemias , Hodgkin‘s lymphoma , Non-Hodgkin‘s
lymphoma, Some solid tumours including breast cancer,
Some papillary bladder tumours (bladder instillation) ,
Recurrent superficial bladder tumours (bladder instillation) ,
Transitional cell carcinoma (bladder instillation) , Carcinoma
in situ (bladder instillation), For AIDS-related Kaposi‘s
sarcoma in patients with low CD4 count and extensive
mucocutaneous or visceral disease , Advanced ovarian
cancer when platinum-based chemotherapy has failed ,
Progressive multiple myeloma (in combination with
bortezomib) in patients who have received at least one prior
therapy and who have undergone or are unsuitable for bone-
marrow transplantation, Monotherapy for metastatic breast
cancer in patients with increased cardiac risk
16 Epirubicin Treatment of breast cancer, Treatment and prophylaxis of
certain forms of superficial bladder cancer
17 Idarubicin Acute non-lymphocytic leukaemias, Advanced breast cancer
18 Mitoxantrone Metastatic breast cancer , Non-Hodgkin‘s lymphoma , Adult
acute non-lymphocytic leukaemia , Non-resectable primary
hepatocellular carcinoma
19 Pixantrone Treatment of refractory or multiply relapsed aggressive non-
Hodgkin B-cell lymphomas
139
8.3.4-Antimetabolites (Antineoplastics)
Antimetabolites with their indication(s) are listed in table 8-5 (1).
Table 8.5: Antimetabolites with their indication(s) (1)

Antimetabolites Indication(s)
1 Azacitidine Treatment of intermediate-2 and high-risk
myelodysplastic syndromes, chronic
myelomonocytic leukaemia, and acute myeloid
leukaemia
2 Capecitabine Colon cancer, colorectal cancer , gastric cancer,
breast cancer,
3 Cladribine B-cell chronic lymphocytic leukaemia , Hairy cell
leukaemia
4 Clofarabine acute lymphoblastic leukaemia
5 Cytarabine Acute myeloblastic leukaemia, Lymphomatous
meningitis
6 Decitabine Acute myeloid leukaemia
7 Fludarabine Ttreatment of advanced B-cell chronic lymphocytic
leukaemia (CLL)
8 Fluorouracil Treatment of some solid tumours including
gastrointestinal tract cancers and breast cancer, In
combination with folinic acid in advanced colorectal
cancer
9 Gemcitabine Non-small cell lung cancer, pancreatic cancer,
epithelial ovarian cancer, breast cancer
10 Mercaptopurine IBD, Acute leukaemias , Chronic myeloid
leukaemia
11 Methotrexate Crohn‘s disease, rheumatoid arthritis, Neoplastic
diseases, Severe psoriasis
12 Nelarabine T-cell acute lymphoblastic leukaemia and T-cell
lymphoblastic lymphoma
13 Pemetrexed Malignant pleural mesothelioma, non-small cell
lung cancer.
14 Tegafur with gastric cancer
gimeracil and oteracil
15 Tioguanine Acute leukaemia , Chronic myeloid leukaemia
16 Trifluridine with colorectal cancer,
tipiracil
17 Bleomycin Squamous cell carcinoma | Metastatic germ cell
cancer , Non-Hodgkin‘s lymphoma
18 Mitomycin Recurrent superficial bladder tumours (bladder
instillation)
19 Pentostatin Hairy cell leukaemia
8.3.5-Plant alkaloids (Antineoplastics)

Plant alkaloids with their indication(s) are listed in table 8-6 (1).
141
Table 8.6: Plant alkaloids with their indication(s) (1)
Plant alkaloids Indication(s)
1 Trabectedin Soft-tissue sarcoma, ovarian cancer
8.3.6-Platinum compounds (Antineoplastics)

Platinum compounds with their indication(s) are listed in table 8-7 (1).
Table 8.7: Platinum compounds with their indication(s) (1)

Platinum compounds Indication(s)
1 Carboplatin Ovarian cancer and lung cancer
2 Cisplatin Treatment of testicular, lung, cervical, bladder,
head and neck, and ovarian cancer
3 Oxaliplatin Colorectal cancer, colon cancer
8.3.7-Podophyllotoxin derivatives (Antineoplastics)

Podophyllotoxin derivatives with their indication(s) are listed in table 8-8 (1).
Table 8.8: Podophyllotoxin derivatives with their indication(s) (1)

Podophyllotoxin Indication(s)
derivatives
1 Etoposide Small cell carcinoma of the bronchus, the
lymphomas and testicular cancer
8.3.8-Taxanes (Antineoplastics)
Taxanes with their indication(s) are listed in table 8-9 (1).
Table 8.9: Taxanes with their indication(s) (1)

Taxanes Indication(s)
1 Cabazitaxel Prostate cancer
2 Docetaxel Breast cancer, non-small cell lung cancer, prostate
cancer, gastric adenocarcinoma, squamous cell
carcinoma of the head and neck
3 Paclitaxel Ovarian cancer, breast cancer, non-small cell lung
cancer, AIDS-related Kaposi‘s sarcoma,
adenocarcinoma of the pancreas, breast cancer,
8.3.9-Topoisomerase I inhibitors (Antineoplastics)

Topoisomerase I inhibitors with their indication(s) are listed in table 8-10 (1).
Table 8.10: Topoisomerase I inhibitors with their indication(s) (1)

Topoisomerase I Indication(s)
inhibitors
1 Irinotecan Colorectal cancer, adenocarcinoma of the pancreas,
2 Topotecan Ovarian cancer, carcinoma of the cervix
141
8.3.10- Vinca alkaloids (Antineoplastics)
Vinca alkaloids with their indication(s) are listed in table 8-11 (1).
Table 8.11: Vinca alkaloids with their indication(s) (1)

Vinca alkaloids Indication(s)
1 Vinblastine sulfate Variety of cancers including leukaemias,
lymphomas, and some solid tumours (e.g. breast and
lung cancer)
2 Vincristine sulfate Variety of cancers including leukaemias,
lung cancer)
3 Vindesine sulfate Variety of cancers including leukaemias,
lung cancer)
4 Vinflunine Treatment of advanced or metastatic transitional cell
carcinoma of the urothelial tract
5 Vinorelbine Advanced breast cancer, Advanced non-small cell
lung cancer
8.3.11- Other Antineoplastics

Other Antineoplastics with their indication(s) are listed in table 8-12 (1).
Table 8.12: Other Antineoplastics with their indication(s) (1)

Other Antineoplastics Indication(s)
1 Arsenic trioxide Acute promyelocytic leukaemia
2 Asparaginase Acute lymphoblastic leukaemia
3 Crisantaspase Acute lymphoblastic leukaemia
4 Eribulin breast cancer
5 Hydroxycarbamide Treatment of chronic myeloid leukaemia |
(Hydroxyurea) Treatment of
cancer of the cervix, Sickle-cell disease
6 Mitotane Adrenocortical carcinoma
7 Panobinostat Multiple myeloma
8 Pegaspargase Acute lymphoblastic leukaemia
9 Procarbazine Hodgkin‘s lymphoma
10 Raltitrexed Colorectal cancer
11 Olaparib Serous epithelial ovarian, fallopian tube, or
primary peritoneal cancer
12 Venetoclax Chronic lymphocytic leukaemia,
13 Vismodegib basal cell carcinoma
8.3.12-Retinoid and related drugs (Antineoplastics)

Retinoid and related drugs with their indication(s) are listed in table 8-13 (1).
142
Table 8.13: Retinoid and related drugs with their indication(s) (1)
Retinoid and related Indication(s)
drugs
1 Bexarotene Skin manifestations of cutaneous T-cell lymphoma
2 Tretinoin Acute promyelocytic leukaemia
8.3.13-Drugs for cytotoxic drug-induced side effects

Drugs for cytotoxic drug-induced side effects are listed in table 8-14 (1).
Table 8.17: Drugs for cytotoxic drug-induced side effects (1)

Drugs Indication(s)
1 Dexrazoxane Prevention of chronic cumulative cardiotoxicity
caused by doxorubicin or epirubicin, Anthracycline
extravasation
2 Palifermin Management of oral mucositis in patients with
haematological malignancies
3 Mesna Cytotoxic induced urothelial toxicity
4 Folinic acid Prevention of methotrexate-induced adverse
effects, As an antidote to methotrexate, Adjunct to
fluorouracil in colorectal cancer
5 Levofolinic acid Prevention of methotrexate-induced adverse
effects, As an antidote to methotrexate, Adjunct to
fluorouracil in colorectal cancer
6 Rasburicase Prophylaxis and treatment of acute hyperuricaemia,
before and during initiation of chemotherapy
8.3.14- Hormonal Antineoplastics

8.3.14.1-Anti-androgens Antineoplastics
Anti-androgens antineoplastics with their indication(s) are listed in table 8-15 (1).
Table 8.15: Anti-androgens Antineoplastics with their indication(s) (1).

Anti-androgens Indication(s)
Antineoplastics
1 Abiraterone acetate Prostate cancer
2 Bicalutamide Prostate cancer
3 Enzalutamide Prostate cancer
4 Flutamide Prostate cancer
8.3.14.2-Oestrogens antineoplastics
Oestrogens antineoplastics with their indication(s) are listed in table 8-16 (1).
Table 8.16: Oestrogens antineoplastics with their indication(s) (1)

Oestrogens Indication(s)
Antineoplastics
1 Diethylstilbestrol Breast cancer in postmenopausal women, Prostate
cancer
143
8.3.14.3-Anti-gonadotrophin releasing hormones antineoplastics
Anti-gonadotrophin releasing hormones antineoplastics with their indication(s) are
listed in table 8-17 (1).
Table 8.17: Anti-gonadotrophin releasing hormones antineoplastics with

their indication(s) (1)
Anti-gonadotrophin releasing Indication(s)
hormones
1 Degarelix Prostate cancer
8.3.14.4-Somatostatin analogues (antineoplastics)

Somatostatin analogues (antineoplastics) with their indication(s) are listed in table
8-18 (1).
Table 8.18: Somatostatin analogues antineoplastics with their indication(s)

(1)
Somatostatin analogues Indication(s)

1 Lanreotide Acromegaly, Neuroendocrine (particularly
carcinoid) tumours, gastroenteropancreatic
neuroendocrine tumours, Thyroid tumours
2 Octreotide Symptoms associated with carcinoid tumours
with features of carcinoid syndrome, VIPomas,
glucagonomas, Acromegaly, Prevention of
complications following pancreatic surgery,
Acromegaly, Neuroendocrine (particularly
carcinoid) tumour, Reduce intestinal secretions
in palliative care, Reduce vomiting due to
bowel obstruction in palliative care
3 Pasireotide Cushing‘s disease when surgery has failed or is
inappropriate
8.3.14.5-Progestogens antineoplastics
Progestogens antineoplastics with their indication(s) are listed in table 8-19 (1).
Table 8.19: Progestogens antineoplastics with their indication(s) (1)

Progestogens antineoplastics Indication(s)
1 Megestrol acetate Breast cancer
8.3.14.6-Anti-oestrogens antineoplastics
Anti-oestrogens antineoplastics with their indication(s) are listed in table 8-20 (1).
Table 8.20: Anti-oestrogens antineoplastics with their indication(s) (1)

Anti-oestrogens antineoplastics Indication(s)
1 Fulvestrant Breast cancer
2 Tamoxifen Breast cancer, Anovulatory infertility
3 Toremifene Breast cancer
144
8.3.14.7-Aromatase inhibitors antineoplastics
Aromatase inhibitors antineoplastics with their indication(s) are listed in table 8-21
(1)
.
Table 8.21: Aromatase inhibitors antineoplastics with their indication(s) (1)

Aromatase inhibitors antineoplastics Indication(s)
1 Anastrozole Breast cancer
2 Exemestane Breast cancer
3 Letrozole Breast cancer
8.3.15-Immunotherapy antineoplastics
Immunotherapy antineoplastics with their indication(s) are listed in table 8-22 (1).
Table 8.22: Immunotherapy antineoplastics with their indication(s) (1)

Immunotherapy Indication(s)
antineoplastics
1 Talimogene herparepvec Melanoma
2 Interferon alfa Chronic myelogenous leukaemia (as monotherapy or in
combination with cytarabine), Hairy cell leukaemia, Follicular
lymphoma, Lymph or liver metastases of carcinoid tumour,
Chronic hepatitis B, Chronic hepatitis C,| Adjunct to surgery in
malignant melanoma , Maintenance of remission in multiple
myeloma
3 Aldesleukin Metastatic renal cell carcinoma
4 Bacillus Calmette-Guérin Bladder instillation for the treatment of primary or recurrent
bladder carcinoma and for the prevention of recurrence
following transurethral resection
5 Histamine Maintenance therapy, in combination with aldesleukin, in
dihydrochloride patients with acute myeloid leukaemia in first remission
6 Mifamurtide Osteosarcoma
7 Lenalidomide Multiple myeloma
8 Pomalidomide Multiple myeloma
9 Thalidomide Multiple myeloma
8.3.16-Proteasome inhibitors antineoplastics

Proteasome inhibitors antineoplastics with their indication(s) are listed in table 8-
23 (1).
Table 8.23: Proteasome inhibitors antineoplastics with their indication(s) (1)

Proteasome inhibitors Indication(s)
antineoplastics
1 Bortezomib Multiple myeloma,
2 Carfilzomib Multiple myeloma
3 Ixazomib Multiple myeloma
145
8.3.17-Protein kinase inhibitors antineoplastics
Protein kinase inhibitors antineoplastics with their indication(s) are listed in table
8-24 (1).
(1)
Table 8.24: Protein kinase inhibitors antineoplastics with their indication(s)
Protein kinase Indication(s)
inhibitors
antineoplastics
1 Afatinib Non-small cell lung cancer
2 Axitinib Renal cell carcinoma
3 Bosutinib Chronic myeloid leukaemia
4 Cabozantinib Medullary thyroid carcinoma
5 Ceritinib Non-small cell lung cancer
6 Cobimetinib Melanoma
7 Crizotinib Non-small cell lung cancer
8 Dabrafenib Melanoma
9 Dasatinib Chronic myeloid leukaemia, Acute lymphoblastic leukaemia
10 Erlotinib Non-small cell lung cancer
11 Everolimus Renal cell carcinoma, neuroendocrine tumours of pancreatic origin, breast
cancer, Liver transplantation, Renal transplantation , Heart transplantation,
Subependymal giant cell astrocytoma associated with tuberous sclerosis
complex, Renal angiomyolipoma associated with tuberous sclerosis complex
12 Gefitinib Non-small cell lung cancer
13 Ibrutinib Chronic lymphocytic leukaemia, Treatment of Waldenstr m‘s
macroglobulinaemia
14 Idelalisib Chronic lymphocytic leukaemia, Treatment of follicular lymphoma
15 Imatinib Chronic myeloid leukaemia, acute lymphoblastic leukaemia, gastro-intestinal
stromal tumours, Treatment of myelodysplastic/ myeloproliferative diseases,
dermatofibrosarcoma protuberans
16 Lapatinib Breast cancer
17 Lenvatinib Renal cell carcinoma, thyroid carcinoma
18 Nilotinib Chronic myeloid leukaemia
19 Osimertinib Non-small-cell lung cancer
20 Palbociclib Breast cancer
21 Pazopanib Rrenal cell carcinoma,
22 Ponatinib Chronic myeloid leukaemia, acute lymphoblastic leukaemia
23 Regorafenib Colorectal cancer, gastrointestinal stromal tumours
24 Ruxolitinib Treatment of disease-related splenomegaly or symptoms in patients with
primary myelofibrosis, postpolycythaemia vera myelofibrosis, or post-
essential thrombocythaemia myelofibrosis
25 Sorafenib Renal cell carcinoma, thyroid carcinoma, hepatocellular carcinoma
26 Sunitinib Gastro-intestinal stromal tumours, renal cell carcinoma, pancreatic
neuroendocrine tumours
27 Temsirolimus Renal cell carcinoma, mantle cell lymphoma
28 Trametinib Melanoma
29 Vandetanib Medullary thyroid cancer
30 Vemurafenib Melanoma
31 Nintedanib Idiopathic pulmonary fibrosis
146
8.3.18-Vascular endothelial growth factor inhibitors antineoplastics
Vascular endothelial growth factor inhibitors antineoplastics with their
indication(s) are listed in table 8-25 (1).
Table 8.25: Vascular endothelial growth factor inhibitors antineoplastics

with their indication(s) (1)
Vascular endothelial growth factor Indication(s)
inhibitors antineoplastics
1 Aflibercept Colorectal cancer
References
1-BNF-74
2-Maxine A. Papadakis, et al, eds. Current Medical Diagnosis & Treatment, 56th Edition 2017 .
147
Chapter Nine: Nutrition and Blood
9.1-Iron deficiency anaemia
Treatment with an iron preparation is justified only in the presence of a
demonstrable iron-deficiency state. Prophylaxis with an iron preparation may be
appropriate in some conditions (1).
9.1.1-Oral iron
1-The oral dose of elemental iron for iron-deficiency anaemia should be 100 to
200 mg daily (1). Table 9-1: Iron content of different iron
salts (1).
2-When the hemoglobin is in the
normal range, treatment should be
continued for a further 3 months
to replenish the iron stores (1).
3-The iron content of various

iron salts is tabulated in the table
9-1 (1).
4-Oral iron preferably taken on

an empty stomach because food, especially dairy products, decreases the
absorption by 40% to 50% (2). (However, many patients must take iron with food
because they experience GI upset when iron is administered on an empty stomach)
(3)
.
5-The patient should be told that oral iron therapy produces dark stools (2).
6-Oral iron preparations sometimes produces gastrointestinal irritation and

abdominal pain with nausea and vomiting. Adverse effects can be reduced by
giving it with or after food (rather than on an empty stomach) or by beginning
therapy with a small dose and increasing gradually (4).
7-Important: Oral Liquid preparations containing iron salts should be well

diluted with water and swallowed through a straw to prevent discoloration of
the teeth (4).
8-Modified-release preparations of iron have no therapeutic advantage and

should not be used (1).
9-Iron should be stored in a safe place, inaccessible to young children.

Accidental ingestion of even small amounts (three to four tablets) of oral iron can
cause serious consequences in small children1 (2).
10-Some oral preparations contain ascorbic acid to aid absorption of the iron but
the therapeutic advantage of such preparations is minimal (2).
148
11-Preparations containing iron and folic acid are used during pregnancy in
women who are at high risk of developing iron and folic acid deficiency (1).
Oral iron (including combination products)

1
Any extra notes:
9.1.2-Parenteral iron
1-Parenteral iron (e.g. iron dextran, iron sucrose) is generally reserved for use
when oral therapy is unsuccessful because the patient cannot tolerate oral iron, or
does not take it reliably, or if there is continuing blood loss, or in malabsorption (1).
2-Parenteral iron may also have a role in the management of chemotherapy-

induced anaemia. Many patients with chronic renal failure who are receiving
hemodialysis also require parenteral iron (1).
3-Depending on the preparation used, parenteral iron is given as a total dose or in

divided doses (1).
3-With the exception of patients with severe renal failure receiving haemodialysis,
parenteral iron does not produce a faster hemoglobin response than oral iron
provided that the oral iron preparation is taken reliably and is absorbed adequately
(1)
.
4-Anaphylactoid reactions occur in less than 1% of patients treated with

parenteral iron therapy and are more commonly associated with iron dextran
than with iron sucrose (2). If an anaphylactic – like reaction occurs, it generally
responds to i.v epinephrine, diphenhydramine, and corticosteroids (3).
5-In Iraq, iron dextran is given most commonly by IM route. In these cases,
undiluted drug should be administered using a Z-track technique to avoid
149
staining the skin. (The skin should be pulled laterally before injection; then the
drug is injected and the skin is released to avoid leakage of dextran into the
subcutaneous tissue) (2).
6-Test dose for iron dextran: the recommendation is differs between UK and
USA:
A-USA: Because of the potential for anaphylaxis with iron dextran, an IM or
IV test dose should be given. The test dose for adults is 25 mg of iron dextran.
A period of 1 hour or longer should elapse before the remaining portion of the
initial dose be given. Subsequent use of test doses should be considered during
iron dextran therapy but is not required (2).
B-UK: Test doses are no longer recommended and caution is needed with
every dose of intravenous iron (1).
Parenteral iron
1
Any extra notes:
9.2-Epoetins
1-Epoetins (recombinant human erythropoietins) are used to treat the anaemia
associated with erythropoietin deficiency in chronic renal failure, and to shorten
the period of symptomatic anaemia in patients receiving cytotoxic chemotherapy
(1)
.
2-Darbepoetin alfa is a derivative of epoetin; it has a longer half-life and can be

administered less frequently than epoetin (1).
3-Methoxy polyethylene glycol-epoetin beta is a continuous erythropoietin

receptor activator that is licensed for the treatment of symptomatic anaemia
associated with chronic kidney disease. It has a longer duration of action than
epoetin (1).
4-Important:
A-Overcorrection of hemoglobin concentration in patients with chronic
kidney disease may increase the risk of death and serious cardiovascular
events, and in patients with cancer may increase the risk of thrombosis and
related complications(1).
151
B-The hemoglobin concentration should be maintained within the range 10–12
g/100mL (1).
Epoetins
1
Any extra notes:
9.3-Megaloblastic anaemia
Most megaloblastic anaemias result from a lack of either vitamin B12 or folate
and treated accordingly (1).
9.4-Sickle-cell anaemia
Hydroxycarbamide (Hydroxyurea) can reduce the frequency of crises and the
need for blood transfusions in sickle-cell disease (1).
9.5-Glucose 6-phosphate dehydrogenase (G6PD) deficiency

1-Individuals with G6PD deficiency are susceptible to developing acute
hemolytic anaemia when they take a number of common drugs (table 9-2) (1).
Table 9-2: Drugs with definite and possible risk of hemolysis in some G6PD-
deficient individuals (1).
Drugs with definite risk of hemolysis in most Drugs with possible risk of
G6PD-deficient individuals hemolysis in some G6PD-
deficient individuals
. Dapsone and other sulfones (higher doses for
dermatitis herpetiformis more likely to cause problems) . Aspirin (acceptable up to a dose
. Methylthioninium chloride of at least 1 g daily in most G6PD-
. Niridazole deficient individuals)
. Nitrofurantoin . Chloroquine (acceptable in acute
. Pamaquin malaria and malaria
. Primaquine (30 mg weekly for 8 weeks has been found chemoprophylaxis)
to be without undue harmful effects in African and . Menadione, water-soluble
Asian people) derivatives (e.g. menadiol sodium
. Quinolones (including ciprofloxacin, moxifloxacin, phosphate)
nalidixic acid, norfloxacin, and ofloxacin). . Quinidine (acceptable in acute
. Rasburicase malaria)
. Sulfonamides (including co-trimoxazole; some . Quinine (acceptable in acute
sulfonamides, e.g. sulfadiazine, have been tested and malaria)
found not to be hemolytic in many G6PD-deficient . Sulfonylureas
individuals)
151
9.6-Folic acid
1-Prevention of neural tube defects (NTD):
A-Folic acid supplements taken before and during pregnancy can reduce the
occurrence of neural tube defects (4).
B-For women of child-bearing potential at high risk

of having a pregnancy affected by NTD ( e.g. if they
have had a previous pregnancy affected by a neural
tube defect), the dose of folic acid is 4 or 5 mg daily
starting before pregnancy (in the USA the
recommendation is 4 weeks before) and continued
through the first trimester (until week 12 of pregnancy)
(4)
.
C-For women at a low risk of having a child with a NTD the dose is 400
micrograms daily and continued through the first trimester (until week 12 of
pregnancy) (4).
2-Other indications for folic acid include (1):

A-Folate-deficient megaloblastic anaemia.
B-Prevention of methotrexate-induced side-effects (dose to be taken on a

different day to methotrexate dose).
C-Prophylaxis of folate deficiency in dialysis.

Folic acid
Any extra notes:
9.7-Iron overload
1-Deferasirox and Deferiprone are oral iron chelators, while desferrioxamine is
an iron chelator parenterally (i.v or s.c). They promote Iron excretion and
indicated for conditions associated with iron overload (e.g. thalassaemia major) (1).
2-Iron excretion induced by desferrioxamine is enhanced by administration of

ascorbic acid (vitamin C) daily by mouth; it should be given separately from food
since it also enhances iron absorption (1).
3-Desferrioxamine is also indicated for iron poisoning (1).
152
4-Adminstartion of Deferasirox:
A-For dispersible tablets, manufacturer advises tablets should be dispersed in
100–200mL of water, orange juice, or apple juice; if necessary any residue
should be resuspended in a small volume of water or juice then administered;
do not chew or swallow whole (1).
B-For film-coated tablets, manufacturer advises tablets may be crushed and

sprinkled on to soft food (yoghurt or apple sauce), then administered
immediately (1).
Iron chelators
1
Any extra notes:
9.8-Drugs for neutropenia

1-Recombinant human granulocyte-colony stimulating factor (rhG-CSF) (e.g.
filgrastim , lenograstim , pegfilgrastim and lipegfilgrastim) stimulates the
production of neutrophils and may reduce the duration of chemotherapy-
induced neutropenia and thereby reduce the incidence of associated sepsis (1).
2-Pegfilgrastim and lipegfilgrastim derivatives have longer duration of action (1).
Granulocyte-colony stimulating factors

1
Any extra notes:
9.9-Minerals and Electrolyte

9.9.1-Calcium supplements
1-Calcium salts are used in the management of hypocalcaemia and calcium
deficiency states resulting from dietary deficiency or ageing (4).
153
2-Intravenous calcium (e.g. calcium gluconate) salts are also used to reverse the
toxic cardiac effects of potassium in the emergency treatment of severe
hyperkalemia (calcium act to protect the heart from hyperkalemia) (4).
3-Intravenous calcium gluconate is given by slow intravenous injection or

infusion (risk of arrhythmias if given too rapidly) (1).
4-Calcium carbonate or acetate are effective phosphate binders and are given
orally (with food) to reduce phosphate absorption from the gut in patients with
hyperphosphataemia; this is particularly relevant to patients with chronic renal
failure (4).
5-Oral calcium supplements can also be used as an adjunct in the management of

osteoporosis (4).
9.9.2-Phosphate-binding agents
1-Calcium-containing preparations are used as phosphate-binding agents in
the management of hyperphosphataemia complicating renal failure (1).
2-Sevelamer and Lanthanum is licensed for the treatment of hyperphosphataemia

in patients with chronic kidney disease (2).
9.9.3-Potassium
1-Potassium salts are used for the prevention and treatment of hypokalaemia (4).
2-An intravenous potassium salt (KCL) may be required in severe acute

hypokalaemia (4).
3-When i.v potassium is added to i.v fluid, it is important to mix thoroughly; if

the solutions are not thoroughly mixed a concentrated layer of potassium chloride
may form (layering effect) owing to differences in density. If such a mixture is
administered it may have a serious effect (1).
4-Calcium or sodium polystyrene sulfonate are cation exchange resins given (by
mouth or by rectum) to treat hyperkalemia associated with anuria or severe
oliguria, and in dialysis patients (1).
9.9.4-Zinc
1-Zinc supplement is used for zinc deficiency (1).
2-Zinc supplements have been shown to reduce the incidence, intensity, or duration
of acute diarrhea in children in developing countries (see chapter 2) .
3- Zinc prevents the absorption of copper in Wilson’s disease (4).
154
9.9.5-Magnesium
Magnesium is indicated for (1):
1-Hypomagnesaemia.
2-Emergency treatment of serious arrhythmias (torsade de pointes).
3-Severe acute asthma.
4-Prevention and treatment of seizures in pre-eclampsia.
5-Rapid bowel evacuation (by mouth).
9.9.6-Selenium
Selenium deficiency can occur as a result of inadequate diet or prolonged
parenteral nutrition. A selenium supplement should not be given unless there is
good evidence of deficiency (1).
Minerals and Electrolyte

1
Any extra notes:
9.10-Vitamins
9.10.1-Vitamin A:
1-Vitamin A, a fat-soluble vitamin, is essential for growth, for the development
and maintenance of epithelial tissue, and for vision (4).
2-Vitamin A is used in the treatment and prevention of vitamin A deficiency.

Vitamin A has also been used to treat various skin disorders including acne
and psoriasis (4).
3-In view of evidence suggesting that high levels of vitamin A may cause birth
defects (teratogenic), women who are (or may become) pregnant are advised not
to take vitamin A supplements ( except on the advice of a doctor ); nor should
they eat liver (1).
(The American College of Obstetricians and Gynecologists has recommended that
women who are pregnant or planning pregnancy should ensure that any vitamin
supplements they take contain a daily dose of vitamin A of no more than 5000
units. The Australian Adverse Drug Reactions Advisory Committee has advised
155
women in this category to avoid vitamin A supplements and to not exceed the
recommended daily allowance of 2500 units from all sources) (4).
9.10.2-Vitamin B Substances (table 9-3)
Table 9-3: Vitamin B substance and their uses

Vit. B Scientific name Uses
B1 Thiamine Thiamine is used in the treatment and prevention
of thiamine deficiency (4).
B2 Riboflavin Riboflavin is used in the treatment and prevention
of riboflavin deficiency (4).
-Pyridoxine is used in the treatment and
prevention of pyridoxine deficiency states (4).
B6 Pyridoxine -Prevention of isoniazid-induced neuropathy (4).
-Treatment of premenstrual syndrome (4).
-Indicated in both idiopathic acquired and
hereditary sideroblastic anaemias (1).
-Vitamin B12 is used in the treatment and
B12 Cobalamins prevention of vitamin B12 deficiency (4).
- Treatment of B12- deficient megaloblastic
anaemias (4).
9.10.3-Vitamin C (Ascorbic acid)

Vitamin C (ascorbic acid) therapy is essential in scurvy. Claims that vitamin C
ameliorates colds or promotes wound healing have not been proved (1).
9.10.4-Vitamin D
1-The term Vitamin D is used for a range of compounds which possess the
property of preventing or curing rickets. They include ergocalciferol (calciferol,
vitamin D2 ), colecalciferol (vitamin D3 ), alfacalcidol (1-α
hydroxycholecalciferol), and calcitriol (1,25-dihydroxycholecalciferol) (1).
2-Vitamin D requires hydroxylation by the kidney to its active form, therefore the
hydroxylated derivatives alfacalcidol or calcitriol should be prescribed if
patients with severe renal impairment require vitamin D therapy (1).
3-Preparations containing calcium with Vitamin D are available for the

management of combined calcium and vitamin D deficiency (1).
9.10.5-Vitamin E
1-Vitamin E is used in the treatment and prevention of vitamin E deficiency (4).
2-Vitamin E has been tried for various other conditions but there is little
scientific evidence of its value (1).
156
9.10.6-Vitamin K
1-Vitamin K is necessary for the production of blood clotting factors (1).
2-Vitamin K compounds are used in the treatment and prevention of hemorrhage

associated with vitamin K deficiency (4).
3-Because vitamin K is fat soluble, patients with fat malabsorption, especially in

biliary obstruction or hepatic disease, may become deficient. Menadiol sodium
phosphate is a water-soluble synthetic vitamin K derivative that can be given
orally to prevent vitamin K deficiency in malabsorption syndromes (1).
9.10.7-Multivitamin preparations
1-It is generally considered that healthy persons eating a normal balanced diet
should have no need for vitamin supplementation (4).
2-Supplementation should concentrate on groups of people at risk of deficiency

such as pregnant and lactating women, who need calcium, folic acid, and iron; and
certain groups who need vitamin D. A multivitamin supplement might be
considered for some groups such as the elderly and those with reduced calorie
intake (4).
Vitamins
1
10
11
157
Any extra notes:
9.11-Nutrition
9.11.1-Intravenous nutrition
1-When adequate feeding through the alimentary tract is not possible, nutrients
may be given by intravenous infusion (1).
2-Indications for this method include preparation of undernourished patients for

surgery, chemotherapy, or radiation therapy; severe or prolonged disorders of the
gastro-intestinal tract; major surgery, trauma, or burns; prolonged coma or refusal
to eat; and some patients with renal or hepatic failure (1).
3-Parenteral nutrition requires the use of a solution containing amino acids,

glucose, fat, electrolytes, trace elements, and vitamins (1).
9.11.2-Enteral nutrition
1-Enteral nutrition (EN) is defined as delivery of nutrients via the gastrointestinal
(GI) tract in a liquid form by a tube (5).
2-EN may be indicated in a variety of conditions or disease states. For example (3):
A-Patients who have neurologic disorders, such as a cerebrovascular accident.
B-Facial or jaw injuries, or lesions of the oral cavity or esophagus).
C-Extreme prematurity (2).
Nutrition
Trade names Composition
1
Any extra notes:
9.12-Fluid management
Solutions of electrolytes are given intravenously, to meet normal fluid and
electrolyte requirements or to replace substantial deficits or continuing losses (1).
158
1-Crystalloids are intravenous fluids that can contain water, sodium (Na+),
chloride (Cl), and other electrolytes. Lactated Ringer solution is a crystalloid that
contains mostly Na+ and Cl–, but also lactate, potassium (K+), and calcium (Ca2+)
(6)
.
2-Dextrose 5% (D5W) is also a crystalloid, but it should not be used for fluid
resuscitation because of the smaller amount of fluid that remains in the
intravascular compartment (6).
3-Colloids include packed red blood cells, pooled human plasma (5% albumin,
25% albumin, and 5% plasma protein fraction), semisynthetic glucose polymers
(dextran), and semisynthetic hydroxyethyl starch (hetastarch) (6).
4-Distribution of intravenous fluid (Table 9-4) (6).
Table 9-4: Distribution of Intravenous Fluid (6).
5-Fluid resuscitation
A-Crystalloids (0.9% sodium chloride or lactated Ringer solution) are
recommended for fluid resuscitation in hypovolemia. Lactated Ringer solution
is historically preferred in surgery and trauma patients, but no evidence
suggests superiority over normal saline for fluid resuscitation. The lactate in
lactated Ringer solution is metabolized to bicarbonate, and it can theoretically
be useful for metabolic acidosis (6).
B-Colloids can be considered after fluid resuscitation with crystalloid (usually

4–6 L) has failed to achieve hemodynamic goals or after clinically significant
edema limits the further administration of crystalloid (6).
6-Maintenance intravenous fluids:

1-Maintenance intravenous fluids are indicated in patients who are unable to
tolerate oral fluids (6).
2-The goal of maintenance intravenous fluids is to prevent dehydration and to

maintain a normal fluid and electrolyte balance (6).
159
3-A typical maintenance intravenous fluid is D5W with 0.45% sodium chloride
plus 20–40 mEq of potassium chloride per liter (6).
7-I.V sodium bicarbonate is used for severe metabolic acidosis, sodium

bicarbonate can be given intravenously (1).
8-Intravenous glucose solutions (5%) are used mainly to replace water deficit.
Glucose solutions are also used to correct and prevent hypoglycemia and to
provide a source of energy in those too ill to be fed adequately by mouth. Glucose
solutions are given in regimens with calcium and insulin for the emergency
management of hyperkalemia (1).
Fluids
Trade names Composition
1
Any extra notes:
9.13-Miscellanous drugs
1-Eculizumab is indicated to reduce thrombotic microangiopathy in atypical
hemolytic uraemic syndrome and reduce hemolysis in paroxysmal nocturnal
haemoglobinuria (1).
2-Anagrelide is indicated for Essential thrombocythaemia. Eltrombopag and

Romiplostim are indicated thrombocytopenia (1).
3-Cinacalcet reduces parathyroid hormone which leads to a decrease in serum

calcium concentrations (used for Secondary hyperparathyroidism in patients with
end stage renal disease on dialysis, and treatment of hypercalcaemia in parathyroid
carcinoma/primary hyperparathyroidism in patients where parathyroidectomy is
inappropriate (1).

1
161
Any extra notes:
9.14-Drugs used in metabolic disorders

Drugs used in certain metabolic disorders are summarized in table 9-5 (1).
Table 9-5: Drugs used in metabolic disorders (1).

Metabolic disorders Drug
1 Acute porphyrias Haem arginate
2 Fabry‘s disease Agalsidase alfa
3 carnitine deficiency [primary (inborn Levocarnitine
errors of metabolism) or secondary (in
haemodialysis patients)]
4 Gaucher‘s disease Imiglucerase, Velaglucerase alfa
5 Homocystinuria Betaine
6 Mucopolysaccharidosis Elosulfase alfa, Idursulfase,
Laronidase
7 Nephropathic cystinosis Mercaptamine (Cysteamine)
8 Niemann-Pick type C disease Miglustat
9 Pompe disease Alglucosidase alfa
10 Tyrosinaemia type I Nitisinone
Hyperammonaemia due to Carglumic acid
11 Urea cycle N-acetylglutamate synthase
disorders deficiency
Long-term treatment of urea Sodium phenylbutyrate
cycle disorders
12 Wilson‘s disease Penicillamine, Zinc acetate
References
1-BNF-74.
11th ed., 2018.
2017.
Press 2009.
161
Chapter Ten: Musculoskeletal and Joint Diseases
10.1-Drugs for Rheumatoid arthritis (RA) , Osteoarthritis (OA), and

other related disorders
1-The following medication classes are prescribed commonly for the treatment of
RA:
A-Non-steroidal anti-inflammatory drugs (NSAIDs).
B-Glucocorticoids.
C-Conventional synthetic Disease-Modifying Antirheumatic Drugs

(csDMARDs). Commonly used agents include methotrexate (MTX),
sulfasalazine, hydroxychloroquine, and leflunomide (1, 2).
D-Biologic DMARDs.
E-Targeted synthetic DMARDs (tsDMARDs) (Tofacitinib) (1).
2-DMARDs are the mainstay of RA treatment (3). It is important to start

DMARDs as soon as possible after disease onset (1) (within the first 3 months of
diagnosis) (3).
4-Because DMARDs may take 2 to 6 months to reach full effect, NSAIDs and
sometimes glucocorticoids can be used in the interim to reduce pain and swelling
(2)
.
5-Biologic DMARDs are indicated in RA patients who have failed an adequate trial
of csDMARD therapy or in combination with csDMARDs in patients with early,
aggressive disease (1).
6-The following medications are used for the treatment of OA (1):

A-Acetaminophen
B-NSAIDs
C-Topical Therapies (Capsaicin, NSAIDs)
E-Duloxetine and tramadol
F-Glucosamine and Chondroitin
G-Intraarticular (IA)Therapy (corticosteroids, hyaluronic acid derivatives).
10.1.1-Conventional synthetic DMARDs

1-Regular monitoring of DMARD therapy is essential because of the risk of liver
and haematological toxicity (4). (e.g. liver function test to detect hepatotoxicity
and complete blood count (CBC) to detect bone marrow suppression) (1).
162
2-Tthe patient is warned to report immediately the onset of any feature of blood
disorders (e.g. sore throat, bruising, and mouth ulcers), liver toxicity (e.g. nausea,
vomiting, abdominal discomfort, and dark urine) (5).
3-Concerning Methotrexate:
A-Methotrexate (MTX) is the most commonly used DMARD because of its
oral, once-weekly administration, well defined safety profile (when monitored
appropriately), demonstrated efficacy, and low cost (2, 3).
B-Other uses for MTX include: IBD, neoplastic diseases, and severe psoriasis
(5)
.
C-It is usually given once weekly (Note that the dose is a weekly dose) (5).
D-In patients taking MTX for non-malignant conditions, folic acid (5 mg/week)
given on a different day from the methotrexate, may help to reduce the frequency
of such side-effects (5).
E-Withdraw treatment if stomatitis develops—may be first sign of gastro-

intestinal toxicity (5).
F-Folinic acid following methotrexate administration helps to prevent

methotrexate-induced mucositis and myelosuppression. Treatment with folinic
acid (as calcium folinate) may be required in acute toxicity (5).
G-Pulmonary toxicity may be a special problem in rheumatoid arthritis (patient

to seek medical attention if dyspnoea, cough or fever); monitor for symptoms at
each visit—discontinue if pneumonitis suspected (5).
4-Concerning hydroxychloroquine:
A-Periodic ophthalmologic examinations are necessary for patients taking
hydroxychloroquine for early detection of reversible retinal toxicity (1) (refer to
ophthalmologist if visual acuity changes) (5).
B-Patient should not take antacids for at least 4 hours before or after
hydroxychloroquine to reduce possible interference with hydroxychloroquine
absorption (5).
C-To avoid excessive dosage in obese patients, the dose of

hydroxychloroquine should be calculated on the basis of ideal body-weight (5).
D-Hydroxychloroquine should be taken with or just after meal (5).
5-Concerning Leflunomide:
A-A loading dose for 3 days may result in therapeutic response within the first
month (1).
163
B-Patients should be advised not to drink alcohol for as long as they are
receiving Leflunomide (5).
C-Washout Procedure: The active metabolite persists for a long period; to aid
drug elimination in case of serious adverse effect, or before starting another
DMARD, or before conception, stop treatment and give either colestyramine or
charcoal, activated. Procedure may be repeated as necessary (5).
6-Concerning Penicillamine:
A-In addition to RA, it is used also for cystinuria (therapeutic and prophylaxis),
aids the elimination of copper ions in Wilson’s disease (hepatolenticular
degeneration), and for autoimmune hepatitis (used rarely; after disease
controlled with corticosteroids) (5).
B-Patients who are hypersensitive to penicillin may react rarely to penicillamine

(5)
.
C-Proteinuria, associated with immune complex nephritis, occurs in up to 30%

of patients, but may resolve despite continuation of treatment; treatment may be
continued provided that renal function tests remain normal, oedema is absent,
and the 24-hour urinary excretion of protein does not exceed 2 g (5).
D-Rashes are a common side-effect. Those that occur in the first few months of
treatment disappear when the drug is stopped and treatment may then be re-
introduced at a lower dose level and gradually increased (5).
E-Loss of taste can occur about 6 weeks after treatment is started but usually
returns 6 weeks later irrespective of whether treatment is discontinued (5).
F-Nausea may occur but is not usually a problem provided that penicillamine is
taken before food (30 to 60 minutes before food) or on retiring and that low
initial doses are used and only gradually increased (5).
10.1.2-Targeted Synthetic DMARDs (tsDMARDs)

Tofacitinib is an oral (this is an advantage) Janus kinase (JAK) inhibitor for
treatment of moderate to severe RA. It can be used as a monotherapy or in
combination with methotrexate or another cs DMARD (2, 3).
164
DMARDs
1
Any extra notes:
10.1.3-Non-steroidal anti-inflammatory drugs (NSAIDs)

1-NSAIDs have analgesic, anti-inflammatory, and antipyretic properties.
NSAIDs are used for the relief of mild to moderate pain, minor febrile conditions,
and for acute and chronic inflammatory disorders such as osteoarthritis, and
rheumatoid arthritis (6).
2-Some NSAIDs are applied topically for the relief of muscular and rheumatic
pain, and some (like diclofenac) are used in ophthalmic preparations for ocular
inflammatory disorders (5).
3-In single doses NSAIDs have analgesic activity. In regular full dosage NSAIDs
have both a lasting analgesic and an anti-inflammatory effect (5).
4-Differences in anti-inflammatory activity between NSAIDs are small, but there is

considerable variation in individual response and tolerance to these drugs. About
60%of patients will respond to any NSAID; of the others, those who do not
respond to one may well respond to another (5).
5-Pain relief starts soon after taking the first dose and a full analgesic effect
should normally be obtained within a week, whereas an anti-inflammatory effect
may not be achieved (or may not be clinically assessable) for up to 3 weeks. If
appropriate responses are not obtained within these times, another NSAID should
be tried (5).
165
6-The commonest adverse effects of NSAIDs are generally GI disturbances,
such as GI discomfort. These are usually mild and reversible but in some patients
peptic ulceration and severe GI bleeding may occur (6).
7-They vary in their selectivity for inhibiting different types of cyclo-oxygenase

(COX); selective inhibitors of COX-2 (Celecoxib, etoricoxib and parecoxib) is
associated with less GI intolerance. This advantage may be lost in patients who
require concomitant low-dose aspirin (5).
Aceclofenac, Diclofenac, Etodolac, Ibuprofen, Indometacin, Ketoprofen,
Mefenamic Acid, Meloxicam, Naproxen, Piroxicam, Sulindac and Tenoxicam are
examples of non-selective COX-2inhibitors (5).
8-The combination of a NSAID and low-dose aspirin can increase the risk of
GI side-effects; this combination should be used only if absolutely necessary (5).
9-Systemic as well as local effects of NSAIDs contribute to GI damage; taking

oral formulations with milk or food, or using enteric-coated formulations, or
changing the route of administration may only partially reduce symptoms such
as dyspepsia (5).
10-Patients at risk of GI ulceration (including the elderly), who need NSAID

treatment should receive gastroprotective treatment (5) (e.g. PPIs) (3).
11-All NSAID use (including COX-2 selective inhibitors) can, to varying degrees,
be associated with a small increased risk of thrombotic events (e.g. myocardial
infarction and stroke); however, the greatest risk may be in those receiving high
doses long term. COX-2 selective inhibitors, diclofenac (150mg daily) are
associated with an increased risk of thrombotic events. The increased risk for
diclofenac (and hence aceclofenac) is similar to that of licensed doses of etoricoxib
(5)
.
12-Naproxen appears to have the lowest incremental cardiovascular risk of the

nonselective NSAIDs (3).
13-It is preferable to avoid NSAIDs in patients with active or previous gastro-

intestinal ulceration or bleeding and patients with a history of hypersensitivity to
aspirin or any other NSAID. Celecoxib is contra-indicated in patients with
sulfonamide sensitivity (5).
14-NSAIDs should be used with caution in patients with asthma , and

hypertension (it cause sodium and water retention) (6).
15-Important : Use of more than one NSAID together should be avoided

because of the increased risk of adverse effects (6).
166
16-Indometacin use associated with a high incidence of side-effects including
headache, dizziness [may affect performance of skilled tasks (e.g. driving)], and
GI disturbances. Mefenamic acid has occasionally been associated with diarrhea
which require discontinuation of treatment. Piroxicam has more GI side effects
than most other NSAIDs, and is associated with more frequent serious skin
reactions. (5).
17-Accordig to its leaflet, Olfen® 50/100mg rectocaps is given before meals.
NSAIDs
1
10
11
12
Any extra notes:
10.1.4-Glucosamine and Chondroitin

1-The glucosamine sulfate and chondroitin sulfate are dietary supplements (1).
Both compounds are found naturally in the body and are essential to the formation
of cartilage (7).
167
2-The combination is believed to have a synergistic effect by stimulating
cartilage production(glucosamine) and inhibiting its destruction (chondroitin) (7)
but convincing evidence for this effect is lacking (2).
3-Indicated for symptomatic relief of mild to moderate osteoarthritis of the knee

(5)
.
4-Glucosamine and/or chondroitin lack uniform efficacy and are not preferred
treatment options (1) (any true clinical value remains to be shown)(2)
(Glucosamine is not recommended for the treatment of osteoarthritis) (5).
Glucosamine and Chondroitin

1
Any extra notes:
10.1.5-Intraarticular (IA) hyaluronic acid derivatives

1-Hyaluronic acid derivatives are intended to improve elasticity and viscosity of
synovial Fluid (8).
2-They are indicated for the treatment of knee OA when treatment failure to other
therapies occurs (8). However, IA hyaluronic acid is not routinely recommended
for knee OA pain (1) (are not recommended) (5). Injections do not provide clinically
meaningful improvement and may be associated with serious adverse events (e.g.,
increased pain, joint swelling, and stiffness) (1).
3-Administration typically consists of weekly injections for 3 to 5 weeks,

depending on the specific product (3). Most benefits are seen after the last dose (8).
4-A new hyaluronan preparation (Monovisc) has been developed, containing 4 or

5 times the amount of hyaluronan used in the usual knee injection.. It is designed
to treat the symptoms of osteoarthritis with only one injection. The approach, if
effective, would simplify the procedure especially for ―needle shy‖ patients (2).
168
Hyaluronic acid derivatives
1
Any extra notes:
10.1.6-Biologic DMARDs
1-Five of the available biologic agents are inhibitors of TNF-α: infliximab,
etanercept , adalimumab, golimumab, and certolizumab (9). Non-TNF agents are:
Abatacept, anakinra, tocilizumab, Secukinumab, and rituximab (1).
2-These drugs are administered parenterally (Sc or I.V)
3-Although biological treatment is more effective than standard DMARD therapy,

treatment costs are significantly greater. Because of this, many countries have set
guidelines restricting their use (4).
4-Although generally well tolerated, biological therapies increase the risk of

serious infections due to suppression of the immune response (4).
A-In general, Biologic agents should be avoided in patients with serious

infections (3). (Tuberculosis has also been noted, and a tuberculin skin test and
chest radiograph should be obtained before beginning therapy) (4).
B-Biologic agents should be at least temporarily discontinued in patients who

develop infections while on therapy until the infection is cured. Live vaccines
should not be given to patients taking biologic agents (1).
5-Heart failure (HF) is a relative contraindication for anti-TNF agents due to

reports of increased cardiac mortality and HF exacerbations. Patients with New
York Heart Association class III or IV and an ejection fraction of 50% or less should
not use anti-TNF therapy (1).
6-Apremilast is a phosphodiesterase type-4 inhibitor used for psoriatic arthritis (and

plaque psoriasis) (5).
7-Other indications for the biological agents are summarized in table 10-1 (5).
169
Table 10-1: Other indications for biological agents
Drug Other indications
1 Adalimumab plaque psoriasis, IBD (UC and CD), acne inversa, Uveitis,
Ankylosing spondylitis, axial spondyloarthritis, and psoriatic
arthritis
2 Certolizumab Ankylosing spondylitis, axial spondyloarthritis, psoriatic
pegol arthritis
3 Etanercept Ankylosing spondylitis , plaque psoriasis, axial
spondyloarthritis , psoriatic arthritis
4 Golimumab ulcerative colitis, ankylosing spondylitis, psoriatic arthritis
5 Infliximab IBD (UC and CD), Ankylosing spondylitis, plaque psoriasis,
Plaque psoriasis
6 Rituximab Lymphoma (Hodgkin‘s, and non-Hodgkin‘s), chronic
lymphocytic leukaemia, granulomatosis with polyangiitis
(Wegener‘s) and microscopic polyangiitis.
Biological agents
1
Any extra notes:
10.2-Drugs for hyperuricemia and gout

10.2.1-Acute attacks of gout
1-Nonsteroidal anti-inflammatory drugs (NSAIDs), colchicine, and
corticosteroids are considered first-line monotherapy for acute attacks (3).
2-Treatment should commence within 24 hours of the onset of an attack (1).
171
3-Acute attacks of gout are usually treated with NSAIDs (5). Doses at the higher
end of the therapeutic range (i.e. large doses) are often needed (3). Following
resolution of the attack, tapering of NSAID therapy may be considered (1).
10.2.1.1-Colchicine
1-Colchicine is highly effective in relieving acute gout attacks but it is used
infrequently today because of its low therapeutic index (1, 3).
2-Oral colchicine causes dose-dependent GI adverse effects (nausea, vomiting,

and diarrhea). Non-GI adverse effects include neutropenia and neuromyopathy,
which may be worsened in patients taking other myopathic drugs (e.g., statins) or
in those with renal insufficiency (1).
3-Colchicine should not be used concurrently with macrolide antibiotics

(especially clarithromycin) because reduced biliary excretion may lead to
increased plasma colchicine levels and toxicity (1).
4-Colchicine is also used for short-term prophylaxis during initial therapy with
allopurinol and uricosuric drugs (5).
10.2.2-Long-term control of gout

1-After the first attack of acute gout, prophylactic pharmacotherapy is
recommended if patients have two or more attacks per year. Other indications
include presence of tophi, chronic kidney disease, or history of urolithiasis (1).
2-Urate-lowering therapy can be started during an acute attack if anti-

inflammatory prophylaxis has been initiated. The guidelines recommend low-dose
oral colchicine or low-dose NSAIDs as first-line prophylactic therapies (1).
Continue prophylaxis until at least 1 month after hyperuricaemia corrected
(usually for first 3 months) to avoid precipitating an acute attack (5).
10.2.2.1-Xanthine oxidase inhibitors (Allopurinol, Febuxostat)

1-Xanthine oxidase inhibitors reduce uric acid by impairing conversion of
hypoxanthine to xanthine and xanthine to uric acid. They are the most widely
prescribed agents for long-term prevention of recurrent gout attacks (1).
2-Allopurinol:
A-Mild adverse effects of allopurinol include skin rash, GI problems, headache,
and urticaria (1).
B-Allopurinol should not be taken with ampicillin owing to increased risk of

rash (2).
C-It also used for the prophylaxis of (hyperuricaemia associated with cancer
chemotherapy, uric acid and calcium oxalate renal stones) (5).
171
D-Take allopurinol with food to minimize GI upset (10).
3-Febuxostat :
A-Febuxostat is a nonpurine xanthine oxidase inhibitor. Due to differences in
chemical structure, febuxostat would not be expected to cross-react in
patients with a history of allopurinol hypersensitivity syndrome (3).
B-It is also used for prophylaxis and treatment of acute hyperuricaemia with
initial chemotherapy for hematologic malignancies (5).
10.2.2.2-Uricosuric Drugs
1-Uricosurics (such as probenecid or sulfinpyrazone) are considered second-line
treatment (2).
2-Patients with a history of urolithiasis should not receive uricosurics. Starting

with low, maintaining adequate urine flow and alkalinization of the urine
during the first several days of therapy may decrease likelihood of uric acid stone
formation (1).
3-Lesinurad is a selective uric acid reabsorption inhibitor. It is approved as

combination therapy with a xanthine oxidase inhibitor for treatment of
hyperuricemia associated with gout in patients who have not achieved target serum
uric acid levels with xanthine oxidase inhibitor monotherapy (1).
10.2.2.3-Pegloticase
1-Pegloticase is a recombinant form of uricase bound to polyethylene glycol
that is approved for the treatment of chronic gout refractory to other therapy (3).
3-Pegloticase should be limited to patients with severe gout with tophi or

nephropathy that has not responded to other agents because of significant adverse
effects, including anaphylaxis (in up to 5% of patients) that mandates
pretreatment with antihistamines and corticosteroids, and its high cost (3).
Drugs for hyperuricemia and gout

1
Any extra notes:
172
10.3-Intra-articular corticosteroid injections
1-Corticosteroids (e.g. Methylprednisolone, Triamcinolone) are injected locally for
an anti-inflammatory effect. They are given by intra-articular injection (5) (e.g.in
case of RA, OA or gout) (1) to relieve pain, increase mobility, and reduce deformity
in one or a few joints; they can also provide symptomatic relief while waiting for
DMARDs to take effect (5).
2-Specific instructions are given to the patient to refrain from weight-bearing

activity for 3 days, except getting up for meals and going to the bathroom (2).
Local corticosteroid injections

1
Any extra notes:
10.4-Neuromuscular disorders
1-Anticholinesterases (Neostigmine, Pyridostigmine)
A-They prolong the action of acetylcholine by inhibiting the action of the
enzyme acetylcholinesterase and are used for myasthenia gravis (5).
B-Muscarinic side-effects of anticholinesterases include increased sweating,

increased salivary and gastric secretions, increased gastro-intestinal and uterine
motility, and bradycardia (5).
C-Pyridostigmine is preferable to neostigmine because of its smoother action

and the need for less frequent dosage. It is particularly preferred in patients
whose muscles are weak on waking (5).
D-Note: Corticosteroids are used when anticholinesterases do not control

symptoms completely (5).
2-Skeletal muscle relaxants:

A-The skeletal muscle relaxants are used for the relief of chronic muscle
spasm or spasticity associated with multiple sclerosis or other neurological
damage; they are not indicated for spasm associated with minor injuries (5).
173
B-Baclofen, diazepam, and tizanidine act principally on the central nervous
system. While dantrolene has a peripheral site of action; cannabis extract has
both a central and a peripheral action (5).
C-The dose of baclofen should be increased slowly to avoid the major side-
effects of sedation and muscular hypotonia (other adverse events are
uncommon) (5).
D-The dose of dantrolene should be increased slowly. Muscle-relaxant doses

of benzodiazepines are similar to anxiolytic doses (5).
E-Drowsiness due to (Baclofen, tizanidine) may affect performance of skilled

tasks (e.g. driving) (5).
F-Note: Baclofen is given orally and by intrathecal injection. It is given with

or just after food. Baclofen is also indicated for hiccup due to gastric distension
(in palliative care) (5).
G-Dantrolene (i.v) also indicated for malignant hyperthermia (5).
3-The neuroprotective drug (Riluzole) is given orally to extend life in patients

with amyotrophic lateral sclerosis (ALS) (5).
4-Quinine salts such as quinine sulfate are effective in reducing the frequency of
nocturnal leg cramps by about 25% in ambulatory patients; however, because of
potential toxicity, quinine is not recommended for routine treatment and should not
be used unless cramps cause regular disruption to sleep (5).
Drugs for neuromuscular disorders

1
Any extra notes:
174
10.5-Drugs for extravasation
1-Extravasation injury follows leakage of drugs or intravenous fluids from the
veins or inadvertent administration into the subcutaneous or subdermal tissue. It
must be dealt with promptly to prevent tissue necrosis (5).
2-Acidic or alkaline preparations and those with an osmolarity greater than that of
plasma can cause extravasation injury. Cytotoxic drugs commonly cause
extravasation injury (5).
3-Placing a glyceryl trinitrate patch distal to the cannula may improve the
patency of the vessel in patients with small veins or in those whose veins are prone
to collapse (5).
4-Hyaluronidase is an enzyme that temporarily reducing the tissues more readily

permeable to injected fluids (6). Spreading the extravasation substance involves
administering hyaluronidase (infiltrated into affected area as soon as possible after
extravasation) (5).
5-Note: in addition to extravasation, hyaluronidase is indicated for hematoma

and to enhance permeation of (SC or IM injections, local anaesthetics, and
ophthalmic local anesthetic) (5).

1
Any extra notes:
References
2017.
4-Nicholas A. Boon, Nicki R. Colledge and Brian R. Walker. Davidson's Principles and Practice
of Medicines .22nd Edition 2014.
5-BNF-74.
Press 2009.
8th edition. 2006.
8-Leon Shargel , Alan H. Mutnick . Comprehensive pharmacy review. 8th edition 2013.
11th ed., 2018.
10-Michael AM, Jason. Frequently prescribed medications. Copyright © 2012 by Jones &
Bartlett Learning, LLC.
175
Chapter Eleven: Eye
11.1-Administration of drugs to the eye
1-Administration guideline for eye drops and ointments are shown below (1):
How to use eye drops How to use eye ointment

1. Wash hands with soapy water. 1. Wash hands with soapy water.
2. If necessary, clean the eyes with boiled and 2. Clean your eye if necessary (as with eye
cooled water and a tissue (one tissue for each drops)
eye) to remove any discharge or remaining 3. Sit in front of a mirror.
wateriness (do not use cotton wool as it may 4. Remove the cap from the eye ointment
leave fibres behind that may irritate the eye). tube. Applying the ointment (see figure):
3. Shake the bottle of drops if necessary. Some 5. Gently pull down the lower eyelid,
eye drops are suspensions and will need shaking; forming a pocket between the lid and the eye.
if applicable, this direction will be on the label. 6. Hold the tube above the eye without
4. Remove the cap from the bottle. touching it.
5. Either sit down or lie down and tilt the head 7. Gently squeeze the tube and place about 1
backwards so that you are looking at the ceiling. cm of ointment into the pocket, starting from
6. Gently pull down the lower eyelid with a nearest the nose to the outer edge.
finger to make a pocket between the eye and the 8. Twist the wrist to break the strip of
lower lid. ointment from the tube.
7. Look upwards. 9. Close the eye and blink to help spread the
8. Rest the dropper bottle on the forehead above eye ointment over the eyeball. Body
the eye (see figure). temperature will help to melt the ointment so
9. Squeeze one drop inside the lower eyelid (do that it will spread over the surface of the eye.
not allow the dropper tip to touch the eye). 10. Vision will be blurred for a few
10. Close the eye and gently blot away any moments. Keep blinking and the vision will
excess drops on a clean tissue. clear.
11. Apply slight pressure to the inner corner of 11. Wipe away excess ointment using a clean
the eye for about 30 seconds. This will prevent tissue.
the drops running down the tear duct and into the 12. Replace the cap of the tube.
back of the throat, avoiding any unpleasant after 13. Remember to discard any remaining
taste and also minimizing any absorption into the ointment four weeks after opening.
body, reducing the risk of possible side-effects.
12. Replace the cap on the bottle.
13. Remember to discard any remaining drops
four weeks after opening.
176
2-Important: one drop is all that is needed. Instillation of more than one drop
should be discouraged because it may increase systemic side-effects (2).
3-When two different eye-drop preparations are used at the same time of day,
dilution and overflow may occur when one immediately follows the other. The
patient should therefore leave an interval of at least 5 minutes between the two
(2)
. (The interval should be extended when eye drops with a prolonged contact time,
such as gels and suspensions, are used) (2).
4-Very important : If using a suspension, shake well before instilling. If using

the suspension with another dosage form, place the suspension drop last,
because it has prolonged retention time in the tear film (1).
Note : most steroid eye drops present as a suspension.
5-Important: If both drop and ointment therapy are indicated, instill the drops
at least 10 minutes before the ointment so that the ointment does not become a
barrier to the drops' penetrating the tear film or cornea (3).
6-Important: Discard or replace eye drop bottles 30 days after the sterility safety
seal is opened (unless stated otherwise by manufacturer). The manufacturer's
expiration date does not apply once the seal is broken (3).
7-Important: Some eye drops (like latanoprost (Xalatan®) need to be stored at

refrigerator.
8-Patients should be warned not to drive or perform other skilled tasks until
vision is clear after using eye drops or eye ointments (2).
9-It is common to use drops during the day and then use eye ointment in the
evening or at night upon retiring when the blurring of vision will be less
inconvenient (4).
10-Contact lenses and drug treatment: In general, patients should be counseled

not to place any ophthalmic solution, suspension, gel, or ointment into the eye
when contact lenses are in place (3). The lenses should be removed before drop
instillation and not worn during the period of treatment (2).
11-Pressure on the lacrimal punctum for at least a minute after

applying eye drops reduces nasolacrimal drainage and therefore
decreases systemic absorption from the nasal mucosa (2).
12-Certain eye drops, e.g. amphotericin, ceftazidime ,

cefuroxime, colistimethate sodium, desferrioxamine mesilate, dexamethasone,
gentamicin, and vancomycin can be prepared aseptically from material
supplied for injection (2).
177
11.2-Antibacterials eye preparations
1-Bacterial eye infections are generally treated topically with eye drops and eye
ointments. Systemic administration is sometimes appropriate in blepharitis (2).
2-Common antibacterials available as an eye preparations include (2):

A- Chloramphenicol.
B- Quinolones: ciprofloxacin, levofloxacin, moxifloxacin, and ofloxacin.
C- Aminoglycosides : gentamicin, neomycin , and tobramycin
D- Polymyxin B.
E- Fusidic acid.
3-Many antibacterial preparations are also combined with a corticosteroid (see

corticosteroid below) (2).
4-Frequency of application depends on the severity of the infection and the

potential for irreversible ocular damage; antibacterial eye preparations are usually
administered as follows (2):
A-Eye drops, apply 1 drop at least every 2 hours then reduce frequency as
infection is controlled and continue for 48 hours after healing (2).
B-Eye ointment, apply either at night (if eye drops used during the day) or 3–4
times daily (if eye ointment used alone) (2).
Antibacterials alone
1
6-
Any extra notes:
178
11.3-Antivirals and antifungals
1-Commonly used antivirals are aciclovir (acyclovir) or ganciclovir for hrpes
simplex infections. Aciclovir eye ointment is used in combination with systemic
treatment for ophthalmic zoster (2).
2-Fungal infections of the cornea are rare. Antifungal preparations for the eye are
not generally available. Treatment will normally be carried out at specialist centers
(2)
.
Antivirals
Any extra notes:
11.4-Corticosteroids and other anti-inflammatory preparations

1-Commonly used corticosteroids are : Betamethasone, Dexamethasone,
Fluorometholone, Hydrocortisone, and Prednisolone (2).
2-They are used to treat inflammatory eye conditions. Topical corticosteroids are
applied frequently for the first 24–48 hours; once inflammation is controlled, the
frequency of application is reduced (2).
3-They may be combined with anti-infective (2).
4-An intravitreal implant containing dexamethasone or fluocinolone are also

available for certain eye conditions (2).
5-Steroid glaucoma’ can follow the use of corticosteroid eye preparations in

susceptible individuals; a ‗steroid cataract’ can follow prolonged use (2).
6-Other anti-inflammatory preparations used for the topical treatment of

inflammation and allergic conjunctivitis include sodium cromoglicate (sodium
cromoglycate), and nedocromil sodium. Lodoxamide eye drops are used for
allergic conjunctival conditions including seasonal allergic conjunctivitis (2).
7-NSAIDs:
A- NSAIDs eye drops such as diclofenac, flurbiprofen , and ketorolac are used
for the prophylaxis and treatment of inflammation, pain, and other symptoms
associated with ocular surgery or laser treatment of the eye (2).
179
B-Diclofenac sodium and flurbiprofen are also used to prevent miosis during
ocular surgery (2).
C-Diclofenac eye drops may be used for seasonal allergic conjunctivitis (2).
D-Contra-indicated in patients with a history of hypersensitivity to aspirin or

any other NSAID (2).
8-Eye drops containing antihistamines, such as azelastine or ketotifen can be used

for allergic conjunctivitis (2).
Corticosteroids
1
2 Eye drop
Antibacterials with corticosteroids

1
Other anti-inflammatory preparations

1 Sodium cromoglicate
NSAIDs
1
181
Antihistamines alone
1
Any extra notes:
11.5-Decongestants and decongestants-antihistamine combination (5).

1-Such preparation may be intended for the treatment of allergic conjunctivitis.
2-Common decongestants-antihistamine combination is (Naphazoline-

Antazoline).
Decongestants and decongestants-antihistamine combination

1
Any extra notes:
11.6-Drugs for dry eye (tear deficiency) (artificial tears).

1-Hypromellose (hydroxypropylmethylcellulose) is the traditional choice of
treatment for tear deficiency. It may need to be instilled frequently (e.g. hourly) for
adequate relief. Polyvinyl alcohol is also used for dry eye (2).
2-Preparations containing a longer-acting polymer, known as carbomer, have a

much longer retention time in the eye and symptom relief is obtained with
significantly fewer instillations (6).
3-Eye ointments containing a paraffin can be used to lubricate the eye surface,
especially in cases of recurrent corneal epithelial erosion. They may cause
temporary visual disturbance and are best suited for application before sleep (2).
181
They are, however, a useful adjunct to artificial tears if used at bedtime (6).
4-Preservatives (nearly always 0.01% benzalkonium chloride) can damage the

corneal epithelium. If a patient is likely to be using artificial tears for a long
time, a preservative-free preparation should be considered (7) [Some of these
products may be available as pack that contain single dose eye drops (e.g. 28 or
30 single dose eye drops that contain small volume usually 0.4 mL and each drop
is intended for single use only)].
5-Sodium hyaluronate eye drops are also used in the management of tear
deficiency (2).
6-Sodium chloride 0.9% drops are sometimes useful in tear deficiency, and can be
used as ‗comfort drops‘ by contact lens wearers, and to facilitate lens removal.
They are also used to irrigate the eye (2).
7-Ciclosporin eye drop [to be applied to the affected eye(s) at bedtime]is licensed
for severe keratitis in patients with dry eye disease, which has not improved
despite treatment with tear substitutes (2).
Drugs for dry eye

1
Any extra notes:
11.7-Antiglaucoma Drugs
1-Glaucoma characterized by a loss of visual field associated with cupping of the
optic disc and optic nerve damage. While glaucoma is generally associated with
raised intra-ocular pressure (IOP), it can occur when IOP is within the normal
range (2).
2-The most common form of glaucoma is primary open-angle glaucoma, where

drainage of the aqueous humour is restricted. Patients with ocular hypertension are
at high risk of developing primary open-angle glaucoma (2).
182
3-Acute angle-closure glaucoma occurs when the outflow of aqueous humour
from the eye is obstructed; it is a medical emergency that requires urgent reduction
of IOP to prevent loss of vision (2).
4-Drugs that reduce intra-ocular pressure by different mechanisms are available

for managing glaucoma (2).
5-Antiglaucoma drugs include (table 11-1) (2):

Table 11-1: Antiglaucoma drugs (2)
Pharmacological class Examples
1 Topical beta-blockers Betaxolol, Carteolol, levobunolol, and Timolol
2 Prostaglandin analogues Latanoprost, tafluprost, travoprost and
and prostamides bimatoprost
3 The carbonic anhydrase Acetazolamide (systemic administration),
inhibitors Brinzolamide (Topical), and dorzolamide
(Topical)
4 Parasympathomimetic Pilocarpine
5 Sympathomimetics Apraclonidine, Brimonidine
(selective α2- agonists)
Note: The osmotic diuretics, intravenous hypertonic mannitol or glycerol by mouth

are useful short-term ocular hypotensive drugs (2).
6-Acetazolamide is given by mouth or by i.v injection. It is used as an adjunct to

other treatment for reducing IOP. Acetazolamide is not generally recommended for
long-term use (2).
7-Sometimes, it may be necessary to combine two or more of these drugs to

control intra-ocular pressure (2).
8-Topical β-blockers:
A-Are typically administered twice daily (8).
B-Tachyphylaxis may occur in 20% to 50% of patients on monotherapy with a

β-blocker, resulting in the need for a different agent or combination therapy (8).
C-Systemic absorption can follow topical application to the eyes; consider side
effects listed for systemically administered beta blockers (2).
5-Prostaglandin analogues:
A-Are usually applied once daily, preferably in the evening (2) and should
not be increased to twice daily, as this may decrease effectiveness (8).
B-Patients receiving latanoprost or tafluprost should be instructed to

refrigerate unopened medication. Once open latanoprost can stored at room
183
temperature for 6 weeks. Tafluprost single-use containers can be stored at room
temperature for up to 28 days (8).
C-Prostaglandin analogues may cause, darkening, thickening and lengthening

of eye lashes (2) ( reversible upon stopping treatment) (9).
D-Changes in eye color: Before initiating treatment, patients should be warned

of a possible change in eye color as an increase in the brown pigment in the iris
can occur, which may be permanent; particular care is required in those with
mixed colored irides and those receiving treatment to one eye only (2).
E-Patients should also be advised to avoid repeated contact of the eye drop
solution with skin as this can lead to hair growth or skin pigmentation (2).
6-Apraclonidine usually used for maximum 1 month (Short-term adjunctive

treatment) (2).
7-Acetazolamide is a sulfonamide derivative; blood disorders, rashes, and other

sulfonamide-related side effects occur occasionally.
Acetazolamide, brinzolamide, and dorzolamide are contra-indicated if history of
sulfonamide hypersensitivity. Acetazolamide is also used for epilepsy (2).
Antiglaucoma drugs (single drug and combined preparations)

1
Any extra notes:
184
11.8-Drugs for retinal disorders
1-Available pharmacological option(s) for different retinal disorders are listed in
table 11-2 (2).
Table 11-2: Drugs for retinal disorders (2)

Retinal disorders Available pharmacological option(s)
1 Age-related macular (Aflibercept, pegaptanib and ranibizumab) (vascular
degeneration endothelial growth factor inhibitors)
2 Macular edema Fluocinolone acetonide, Aflibercept,
Dexamethasone, and Ranibizumab,
3 Optic neuropathy Idebenone (nootropic and antioxidant)
4 Vitreomacular Ocriplasmin (recombinant proteolytic enzymes)

traction
2-Admistration method (table 11-3) (2):
Table 11-3: Administration method (2)

Drug Administration method
1 Aflibercept Intravitreal injection
2 Pegaptanib Intravitreal injection
3 Ranibizumab Intravitreal injection
4 Fluocinolone acetonide Intravitreal injection
5 Idebenone By mouth
6 Ocriplasmin Intravitreal injection
Drugs for retinal disorders

1
Any extra notes:
185
11.9- Miscellaneous ophthalmological products
11.9.1-Mydriatics and cycloplegics
1-Antimuscarinics dilate the pupil and paralyse the ciliary muscle. Short-acting,
relatively weak mydriatics, such as tropicamide (lasts for 4–6 hours), facilitate the
examination of the fundus (Funduscopy) of the eye (be applied 20 minutes
before examination). Longer acting options include cyclopentolate (action up to 24
hours) or atropine sulfate (action up to 7 days) (2).
2-Phenylephrine is used for mydriasis in diagnostic or therapeutic procedures;

mydriasis occurs within 60–90 minutes and lasts up to 5–7 hours (2).
3-Mydriatics and cycloplegics are used in the treatment of anterior uveitis,

usually as an adjunct to corticosteroids (2).
11.9.2-Antiseptics and disinfectants

Povidone-iodine eye drop may be used as an antiseptics before ocular surgery (2).
11.9.3-Motics (parasympathomimetics)
Acetylcholine chloride irrigation (powder and solvent) is used for during some
eye surgery requiring rapid complete miosis (2).
11.9.4-Local anaesthetics
1-Oxybuprocaine and tetracaine (eye drops) are widely used topical local
anaesthetics. Tetracaine produces a more profound anesthesia and is suitable for
use before minor surgical procedures, such as the removal of corneal sutures (2).
2-Lidocaine, with or without adrenaline/epinephrine is injected into the eyelids for

minor surgery (2).
Miscellaneous ophthalmological products

1
Any extra notes:
186
References
Press. 2009.
2-BNF-74.
11th ed., 2018.
6-Lucy C. Titcomb .Eye disorders : Over-the-counter ophthalmic preparations. The
Pharmaceutical Journal .Vol 264 No 7082 p212-218 February 5, 2000 .
7-Marvyn Elton .Ocular conditions from A to Z (i). The Pharmaceutical Journal .17 February
2007 (Vol 278) 195-198.
Press 2009.
187
Chapter Twelve: Ear, Nose, and Oropharynx
12.1-Drugs acting on the ear
12.1.1-Administration of ear drop:
How to use ear drops and sprays (1, 2)

1. Wash hands with soapy water.
2. Clean and dry the ear gently with a facecloth.
3. If necessary, shake the bottle of drops or spray.
Some drops and sprays are suspensions
and will need shaking; if applicable, this direction
will be on the label.
4. Warm the ear drops or spray by holding the
bottle in the hand for a few minutes.
5. Remove the lid.
6. Lie down on side with the affected ear
uppermost (or tilt the head to one side).
7. Gently pull the ear lobe backward and upward to
open the ear canal (see drawing A). If the patient is
a child younger than 3 years old, pull the ear
backward and downward (see drawing B).
8. Drop the drops or spray into the ear canal.
9. Gently massage just in front of the ear.
10. Stay lying down or with the head tilted for five
minutes to allow the medication to run down the
ear canal.
11. Return to the upright position and wipe away
any excess medication.
12. Repeat if necessary in the other ear.
13. Replace the lid.
188
12.1.2-Treatment of otitis externa
1-Otitis externa is a general term used to describe inflammation of the skin of
the external auditory canal that may be due to infection with bacteria, viruses, or
fungi or secondary to skin disorders such as eczema (3).
2-Otitis externa may be acute or chronic. The treatment of both acute and chronic
otitis externa includes thorough cleansing and the use of appropriate
antibacterial ear drops, with or without a corticosteroid, even though some
have doubted the value of topical antibacterials (3).
3-Solution of acetic acid 2% acts as an antifungal and antibacterial in the external

ear canal. It may be used to treat mild otitis externa but in severe cases an anti-
inflammatory preparation with or without an anti-infective drug is required (4).
4-Ear drops containing aminoglycosides, such as gentamicin, neomycin, or

framycetin, or polymyxins should not be used when the ear drum is perforated
because of the risk of ototoxicity (3).
Ear products for otitis externa

(Corticosteroids, Anti-infective, and combination products)
1
6-
7-
Any extra notes:
12.1.3-Treatment of Acute Bacterial Otitis Media

1-Pain of otitis media should be treated with oral analgesics. Acetaminophen or a
NSAID, such as ibuprofen, should be offered early to relieve pain of acute otitis
media (5).
189
2-Watchful waiting antibiotic prescriptions (prescription given to the patient but
only filled if symptoms persist or worsen within 48–72 hours after diagnosis) are
approaches used to decrease antimicrobial use. These approaches should only be
considered in otherwise healthy children (6).
3-Guidelines recommend the use of antibiotics in otitis media. Antibiotics

shorten the course of the disease and may prevent complications (7).
4-Amoxicillin (High-dose amoxicillin 80–90 mg/kg/day because higher middle

ear fluid concentrations can overcome pneumococcal penicillin resistance) or
amoxicillin/ clavulinic acid continue to be the drugs of choice (5-7).
5-Alternative choices include cephalosporins or macrolide antibiotics. If there is

no improvement after three days, switching antibiotics should be considered (7).
12.1.4-Removal of ear wax (cerumen)

A-Nonpharmacologic Therapy
1-The only recommended nonpharmacologic method of removing cerumen is to
use a wet, wrung-out washcloth draped over a finger (2). (The common use of
cotton-tipped swabs to remove earwax is ineffective and potentially dangerous) (8).
B-Pharmacologic Therapy (Cerumunolytics)

1-Constituents of cerumenolytic products include fixed and volatile oils (olive,
arachis, almond and camphor oils), glycerol, docusate, and urea hydrogen peroxide
(9)
.
2-The manufacturers docusate (dioctyl sodium sulpho-succinate) recommend that

adults and children use enough ear drops to fill the affected ear then place a
small plug of cotton wool in the ear and repeat for two consecutive nights (10).
3-Sodium bicarbonate ear drop should be instilled two to three times a day for up
to 3 days (10).
Cerumunolytics
1
Any extra notes:
191
12.2-Drugs acting on the nose
12.2.1- Administration of nasal preparations (1).
How to use nasal drop How to use nasal sprays

1. Gently blow the nose to clear the nostrils. 1. Gently blow nose to clear nostrils.
2. Wash hands. 2. Wash hands with soapy water before using
3. Shake the bottle of drops. Some are the spray.
suspensions and will need shaking; if 3. Gently shake the spray. Some are suspensions
applicable, this direction will be on the and will need shaking; if applicable, this direction
label. will be on the label.
4. Remove the lid from the bottle. If the lid 4. Remove the cap from the spray.
includes an integral dropper draw some 5. Tilt head slightly forward (look down at
liquid into the dropper. feet).
5. Position the head as shown in figure 6. Close one nostril; gently press against the
below. The easiest way to do this is to lie on side of the nose with one finger.
a bed with your head hanging over the edge. 7. Insert tip of nasal spray into open nostril
Bending forward or kneeling is an and slowly breathe in through the open
alternative but maintaining the position for 2 nostril, and while breathing in squeeze the
minutes after using the drops is more spray to deliver one dose. It is important to
difficult. Tilting the head back is not a keep the spray upright (do not sniff hard as
suitable position as the drops will not cover the spray will travel straight to the back of
the upper surface of the nostril. the throat, failing to deposit any medication
6. Drop the required number of drops into in the nostril).
each nostril. The intention is to spread the 8. Remove spray from the nose and breathe
drop(s) evenly over the surface of the out through the mouth. Tilt head backwards
nostril. Do not allow the dropper to touch for about a minute to prevent the liquid spray
the nose. running out of the nose.
7. Stay in this position for 2 minutes to 9. Repeat in other nostril as directed.
prevent the drops running out of the nose 10. Replace cap on spray.
and down the back of the throat. 11. Try not to blow nose for several minutes
8. Replace the lid. after using the spray.
191
Note:
1-Nasal sprays are preferable for adults and children aged over 6 years
because spray has a faster onset of action and cover a large surface area (11).
2-Nasal drops are preferable for children aged below 6 years because their
nostrils are not sufficiently wide to allow effective use of sprays. (But the drops
cover a limited surface area and easily swallowed which increase the possibility of
systemic effects) (11).
12.2.2-Drugs used in nasal allergy

12.2.2.1-Corticosteroids (intranasal)
1-Nasal preparations containing corticosteroids (beclometasone, betamethasone,
budesonide, fluticasone, mometasone, and triamcinolone) are used for more
persistent symptoms of allergic rhinitis (4).
2-In seasonal allergic rhinitis (e.g. hay fever), treatment should begin 2 to 3
weeks before the season commences and may have to be continued for several
months (4).
3-Some patients improve within a few days, but peak response may require 2 to
3 weeks (5).
4-The dosage may be reduced once a response is achieved (5).
5-Blocked nasal passages should be cleared with a decongestant or saline

irrigation before administration to ensure adequate penetration of the spray (5).
Intranasal corticosteroids
1
Any extra notes:
12.2.2.3-Topical nasal decongestants

1-Intranasal sympathomimetics (nasal drops and sprays) such as phenylephrine,
naphazoline, oxymetazoline, and xylometazoline may be useful for short-term
treatment (usually not longer than 7 days) to relieve severe nasal congestion (3, 4).
192
2-Topical nasal decongestants (sympathomimetics) can be recommended for those
patients in whom systemic (oral) decongestants are less suitable (11).
3-Sodium chloride 0.9% given as nasal drops or spray may relieve nasal
congestion by helping to liquefy mucous secretions (4).
4-If topical; (drops or sprays) decongestants are to be recommend, the pharmacist

should advice the patients not to use the product for longer than 7 days
because rebound congestion (Rhinitis medicamentosa) (11).
5-Many treatment options have been proposed for rhinitis medicamentosa

including slow reduction in the use of decongestant, a switch to inhaled
corticosteroids or an abrupt discontinuation. Abrupt cessation is effective but it
is difficult because the patients will be congested for several days or weeks (12).
Note: some of these product may present in two concentrations (one for children
and one for adults).
Topical nasal decongestants

1
Any extra notes:
12.2.2.4-The topical antihistamine, Mast-cell stabilizers, and Antimuscarinics

1-The topical antihistamine azelastine is useful for controlling breakthrough
symptoms in allergic rhinitis. Topical antihistamines are considered less effective
than topical corticosteroids but probably more effective than cromoglicate (4).
2-Caution patients using intranasal azelastine about potential for drowsiness

because systemic availability is approximately 40% (5).
3-Mast-cell stabilizers such as sodium cromoglicate available as nasal drop or

spray and used as prophylaxis of allergic rhinitis (4).
193
4-It is preferably to start sodium cromoglicate 1 week before the hay fever
season is likely to begin and then used continuously (11) (but it is less effective) (4).
5-Ipratropium bromide available as intranasal spray for Rhinorrhoea associated

with allergic and non-allergic rhinitis (4).
Any extra notes:
12.3-Drugs acting on the oropharynx

12.3.1-Oropharyngeal fungal infections
1-Topical antifungals for oropharyngeal fungal infections (thrush) include nystatin
as an oral suspension drop and miconazole (as an oral gel) (4).
2-Concerning miconazole oral gel: treatment should be continued for at least 7

days after lesions have healed or symptoms have cleared, to be administered
after meals, retain near oral lesions before swallowing (4).
3-Concerning nystatin oral drop: continued for 48 hours after lesions have
resolved (4).
Topical antifungals for oropharyngeal fungal infections

1
Any extra notes:
194
12.3.2-Mouthwashes and gargles
1-Mouthwashes (e.g. those containing Chlorhexidine, Hydrogen peroxide,
Hexetidine, Sodium bicarbonate with sodium chloride) are used for general oral
hygiene (4).
2-Chlorhexidine (antiseptic and disinfectant) (3):

A-Can be used as a mouthwash, spray or gel for (oral hygiene and plaque
inhibition , oral candidiasis, gingivitis , and management of aphthous ulcers) (4).
B-Rinse or gargle 10 mL twice daily (rinse or gargle for about 1 minute). It may
cause reversible brown staining of teeth (4).
C-Chlorhexidine may be incompatible with some ingredients in toothpaste,

causing an unpleasant taste in the mouth; rinse the mouth thoroughly with water
between using toothpaste and chlorhexidine-containing products (4).
Mouthwashes and gargles

1
Any extra notes:
12.3.3-Oral ulceration and inflammation

1-Ulceration of the oral mucosa may be caused by trauma (physical or chemical),
recurrent aphthae, infections, carcinoma, dermatological disorders, nutritional
deficiencies, gastro-intestinal disease, hematopoietic disorders, and drug therapy
(Chemotherapy induced mucositis) (4).
2-Secondary bacterial infection may be a feature of any mucosal ulceration. Use of

a chlorhexidine mouthwash is often beneficial and may accelerate healing of
recurrent aphthae (4).
3-Topical corticosteroid therapy may be used for some forms of oral ulceration.
In the case of aphthous ulcers it is most effective if applied in the ‗prodromal‘
phase (4).
195
5-Doxycycline rinsed in the mouth may be of value for treatment of recurrent
aphthous ulceration (by mouth using dispersible tablet: 100 mg 4 times a day
usually for 3 days, dispersible tablet can be stirred into a small amount of water
then rinsed around the mouth for 2–3 minutes, it should preferably not be
swallowed). Low-dose doxycycline is licensed as an adjunct to scaling and root
planing for the treatment of periodontitis (4).
6-Local analgesics [e.g. anesthetics like lidocaine] have a limited role in the
management of oral ulceration. When applied topically their action is of a
relatively short duration so that analgesia cannot be maintained continuously
throughout the day. The main indication for a topical local analgesic is to relieve
the pain of otherwise intractable oral ulceration particularly when it is due to major
aphthae (4).
7-Flurbiprofen (lozenges) is a NSAID licensed for the relief of sore throat (4).
8-Benzydamine (NSAID) mouthwash or spray may be useful in reducing the

discomfort associated with a variety of ulcerative conditions (4).
9-Mucositis occurs as a nonspecific effect of chemotherapy and radiation

therapy on the basal epithelium of the mouth. Equal portions of lidocaine,
diphenhydramine, and magnesium-containing or aluminum-containing antacids
can be used for their anesthetic and astringent properties. Many institutions
compound mouthwash products containing these ingredients as well as antibiotics,
nystatin, or corticosteroids (13).
Oral ulceration and inflammation (corticosteroids, NSAID, local

anaesthetics)
1
Any extra notes:
196
12.3.4-Fluoride
1-Availability of adequate fluoride confers significant resistance to dental
caries. It is now considered that the topical action of fluoride (paste, mouthwash)
on enamel and plaque is more important than the systemic effect (tablet, oral drop)
(4)
.
2-When the fluoride content of drinking water is less than 700 micrograms per litre
(0.7 parts per million), daily administration of fluoride tablets or drops provides
suitable supplementation. Systemic fluoride supplements should not be prescribed
without reference to the fluoride content of the local water supply (4).
3-Directions for administration

A-With oral use: Tablets should be sucked or dissolved in the mouth and taken
preferably in the evening (4).
B-With oral (topical) use: For mouthwash, rinse mouth for 1 minute and then
spit out (4).
C-Toothpaste: Avoid drinking or rinsing mouth for 30 minutes after use (4).
Fluoride
1
Any extra notes:
12.3.5-Treatment of dry mouth (xerostomia)

1-Dry mouth may be caused by drugs with antimuscarinic (anticholinergic) side-
effects, by diuretics, by irradiation of the head and neck region or by damage to or
disease of the salivary glands (4).
2-Patients with a persistently dry mouth may develop a burning or scalded

sensation and have poor oral hygiene; they may develop increased dental caries,
periodontal disease, and oral infections (particularly candidiasis) (4).
3-Dry mouth may be relieved in many patients by simple measures such as

frequent sips of cool drinks or sucking pieces of ice or sugar-free fruit
pastilles. Sugar-free chewing gum stimulates salivation in patients with residual
salivary function (4).
4-Artificial saliva can provide useful relief of dry mouth (4).

197
5-Pilocarpine tablets are licensed for the treatment of xerostomia following
irradiation for head and neck cancer and for dry mouth and dry eyes
(xerophthalmia) in Sjögren‘s syndrome. They are effective only in patients who
have some residual salivary gland function, and therefore should be withdrawn if
there is no response (4).
Products for dry mouth

1
Any extra notes:
References
Press. 2009.
Press 2009.
4-BNF-74.
2017.
7-Andreoli and carpenter‘s. Cecil essentials of medicine 9th edition. 2016.
8-W. Steven Pray, Gabriel E. Pray .Treating Minor Ear Problems. US Pharm. 2012;37(5):16-23.
11-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the pharmacy . A
guide to the managements of common illness. 7th edition. 2014.
12- Canadian American pharmacists association (CPhA). CTMA: Compendium of Therapeutics
for Minor Ailments. 2014.
11th ed., 2018.
198
Chapter Thirteen: Skin
13.1-Common Skin Diseases by Body Location
Common Skin Diseases by Body Location are shown in table 13-1 (1)
Table 13-1: Common Skin Diseases by Body Location (1).
12.2-Dermatologic Drug Delivery Systems

1-Dermatologic formulations are available in a variety of forms: solutions,
suspensions or shake lotions, powders, lotions, emulsions, gels, creams, ointments,
and aerosols. Each dermatologic delivery vehicle has specific characteristics and
uses based on the type, relative acuteness, and location of the lesion (1) (table 13-2).
2-Powders are used mainly in intertriginous areas (e.g., groin, under the breasts,
or in skin folds) to decrease friction, which can cause mechanical irritation. They
also are useful in the treatment of tinea pedis (athlete‘s foot), tinea cruris (jock
itch), and diaper dermatitis (diaper rash) (1).
3-Lotions are suspensions or solutions of powder in a water vehicle. They are

especially advantageous in the treatment of conditions characterized by significant
inflammation and tenderness. In these situations, creams or ointments may cause
pain on application. Also, lotions are useful for hairy areas of the body and scalp
(1)
.
4-Gels are most useful when applied to hairy areas or other areas such as the
face or scalp, where it is considered cosmetically unacceptable to have the residue
of a vehicle remain on the skin (1).
5-Creams are the most commonly used vehicle in dermatology. The most
common mistake made by patients when applying creams is that they use too
much or do not rub them in fully. Generally, if the cream can be seen on the skin
after application, the patient has made one or both of these application mistakes (1).
6-Ointments are most useful on chronic lesions, relieving dryness, brittleness,

and protecting fissures owing to their occlusive properties. They should not be
199
used on acutely inflamed lesions. Ointments should not be applied to intertriginous
or hairy areas because they tend to trap heat and promote maceration. Ointments
are greasy and may be cosmetically unacceptable (1).
7-Collodions are painted on the skin and allowed to dry to leave a flexible film
over the site of application (2).
Table 13-2: Appropriate Dermatologic Vehicle Selection Across the Range of

Dermatologic Lesions (1).
13.3-Anti-infective skin preparations

13.3.1-Antibacterial preparations
1-Topical antibacterials (3)(e.g. neomycin, metronidazole, polymyxins, silver
sulfadiazine, bacitracin, mupirocin, and retapamulin) (2) and antiseptics may be
useful for superficial skin infections, but antibacterials should only be used short
term because of the risks of inducing bacterial resistance and contact allergy (3).
2-To minimize the development of resistant organisms it is advisable to limit the

choice of antibacterials applied topically to those not used systemically (2).
3- Silver sulfadiazine is used in the treatment of infected burns (2).
4-In the community, acute impetigo (caused by Staphylococcusaureus) on small

areas of the skin may be treated by short-term topical application of fusidic acid.
Mupirocin should be used only to treat meticillin-resistant Staphylococcus aureus.
If the impetigo is extensive or longstanding, an oral antibacterial such as
flucloxacillin (or clarithromycin in penicillin allergy) should be used (2).
5-Metronidazole is used topically for rosacea and to reduce the odor associated
with anaerobic infections (2).
6-Cellulitis, a rapidly spreading deeply seated inflammation of the skin and

subcutaneous tissue, requires systemic antibacterial treatment (2).
211
Topical antibacterials
1
Any extra notes:
13.3.2-Antifungal preparations
1-Most localized fungal infections are treated with topical preparations (2).
2-Important: To prevent relapse, local antifungal treatment should be continued

for 1–2 weeks after the disappearance of all signs of infection (2).
3-Topical antifungal include: The imidazole antifungals (clotrimazole, econazole,

ketoconazole, tioconazole and miconazole), Terbinafine, tolnaftate, nystatin,
griseofulvin, amorolfine, and compound benzoic acid ointment (Whitfield‘s
ointment).
4-Pityriasis versicolor can be treated with ketoconazole shampoo (apply once

daily for maximum 5 days, leave preparation on for 3–5 minutes before rinsing) (2).
5-Antifungal treatment may not be necessary in asymptomatic patients with tinea

infection of the nails. If treatment is necessary, a systemic antifungal is more
effective than topical therapy (2).
6-Combination products of an antifungals and corticosteroids are available to

treat fungal infection associated with inflammation.
211
Antifungal preparations (including Combination products)
1
Any extra notes:
13.3.3-Antiviral preparations
1-Aciclovir cream can be used for the treatment of initial and recurrent labial
herpes simplex infections (cold sores) (2).
Important : Aciclovir is best applied at the earliest possible stage, usually when
prodromal changes of sensation are felt in the lip and before vesicles appear
(2)
.
2-Penciclovir cream is also licensed for the treatment of herpes labialis; it needs to
be applied more frequently than aciclovir cream (2).
3-Systemic treatment is necessary for buccal or vaginal infections and for herpes
zoster (shingles) (2).
Antiviral preparations
Any extra notes:
212
13.3.4-Parasiticidal preparations
13.3.4.1-Scabies
1-Permethrin is used for the treatment of scabies (apply 5% preparation over
whole body then wash off after 8–12 hours); malathion can be used if permethrin
is inappropriate (apply preparation over whole body, and wash off after 24 hours)
(2)
.
2-Benzyl benzoate is an irritant and should be avoided in children; it is less

effective than malathion and permethrin (2).
3-Ivermectin by mouth has been used, in combination with topical drugs, for the
treatment of hyperkeratotic (crusted) scabies that does not respond to topical
treatment alone; further doses may be required (2).
4-All members of the affected household should be treated simultaneously.

Treatment should be applied to the whole body including the scalp, neck, face, and
ears. Particular attention should be paid to the webs of the fingers and toes and
lotion brushed under the ends of nails (2).
5-It is now recommended that malathion and permethrin should be applied

twice, one week apart; in the case of benzyl benzoate in adults, up to 3
applications on consecutive days may be needed. It is important to warn users to
reapply treatment to the hands if they are washed (2).
6-The itch and eczema of scabies persists for some weeks after the infestation has
been eliminated and treatment for pruritus and eczema may be required.
Application of crotamiton can be used to control itching after treatment with more
effective acaricides (2).
7-A topical corticosteroid may help to reduce itch and inflammation after scabies
has been treated successfully; however, persistent symptoms suggest that scabies
eradication was not successful. Oral administration of a sedating antihistamine
at night may also be useful (2).
Preparations for scabies

1
213
Any extra notes:
13.3.4.2-Head lice
1-Head lice infestation (pediculosis) should be treated using lotion or liquid
formulations (shampoos are diluted too much in use to be effective) (2).
2-A contact time of 8–12 hours or overnight treatment is recommended for lotions
and liquids (2).
3-In general, a course of treatment for head lice should be 2 applications of

product 7 days apart to kill lice emerging from any eggs that survive the first
application. All affected household members should be treated simultaneously (2).
4-Dimeticone is effective against head lice ; it is less active against eggs and
treatment should be repeated after 7 days. Malathion, an organophosphorus
insecticide, is an alternative, but resistance has been reported (2).
Drugs for Head lice

Scientific Trade Dosage Application
name names form
1
Any extra notes:
13.4-Preparations for minor cuts and abrasions

Cetrimide is used to treat minor cuts and abrasions. The effervescent effect of
hydrogen peroxide is used to clean minor cuts and abrasions (2).
Any extra notes:
214
13.5-Skin cleansers, and antiseptics
1-Wound cleansing is required to remove any dirt or foreign bodies and to remove
exudate and slough (pus and necrotic tissue). This helps to prevent infection and
aids healing. Commonly used cleansing solutions are sodium chloride 0.9%,
hypochlorite, hydrogen peroxide, povidone-iodine, and chlorhexidine (3).
2-Hydrogen peroxide, an oxidising agent, can be used in solutions of up to 6% for

skin disinfection, such as cleansing and deodorizing wounds and ulcers (2).
3-For irrigating ulcers or wounds, lukewarm sterile sodium chloride 0.9% solution
is used (2).
4-Potassium permanganate solution 1 in 10000, a mild antiseptic with astringent

properties, can be used for exudative eczematous areas; treatment should be
stopped when the skin becomes dry.
5-Alcohol (Indications: skin preparation before injection). (Cautions : flammable;

avoid broken skin) (2).
6-Wound dressings and packing preparations help to protect the wound and
provide the correct environment for wound healing. Some also help by absorbing
exudates (3). (e.g. sofra-tulle®).
Skin cleansers, and antiseptics

1
Any extra notes:
215
13.6-Emollients and Barrier preparations
1-Emollients (like Soft Paraffin) soothe, smooth and hydrate the skin and are
indicated for all dry or scaling disorders (like eczema) (2).
2-Barrier preparations often contain water-repellent (e.g. Zinc oxide, castor oil).
They are used on the skin around stomas, bedsores, and pressure areas in the
elderly where the skin is intact (2).
3-Notes concerning napkin rash (2) :

A-The first line of treatment is to ensure that nappies are changed frequently.
The rash may clear when left exposed to the air and a barrier preparation can be
helpful.
B-If the rash is associated with a fungal infection, an antifungal cream such
as clotrimazole cream is useful.
C-A mild corticosteroid such as hydrocortisone 1% is useful in moderate to

severe inflammation. The barrier preparation is applied after the corticosteroid
preparation.
D-Preparations containing hydrocortisone should be applied for no more

than a week.
Emollients and Barrier preparations (including preparations for napkin

rash)
1 Zinc oxide
2 Zinc and castor oil
Any extra notes:
13.7-Topical local anaesthetics and antipruritics

1-An emollient may be of value where the pruritus is associated with dry skin (2).
2-Preparations containing crotamiton are sometimes used but are of uncertain

value. Preparations containing calamine are often ineffective (2).
216
3-Topical antihistamines and local anaesthetics are only marginally effective and
occasionally cause sensitization. For insect stings and insect bites, a short
course of a topical corticosteroid is appropriate. Short-term treatment with an
oral sedating antihistamine may help in insect stings where sedation is desirable
(2)
.
4-Calamine preparations are of little value for the treatment of insect stings or
bites (2).
5-Topical preparation containing doxepin 5%p is licensed for the relief of pruritus
in eczema; it can cause drowsiness [may affect performance of skilled tasks (e.g.
driving)] and there may be a risk of sensitization (2).
Topical local anaesthetics and antipruritics

1
Any extra notes:
13.8-Topical Corticosteroids
1-Topical corticosteroids are used for the treatment of inflammatory conditions
of the skin (other than those arising from an infection), in particular eczema,
contact dermatitis, insect stings (2).
2-Topical corticosteroids are not recommended in the routine treatment of urticaria

(2)
.
3-Application:
A-Topical corticosteroids should be applied no more than twice daily.
Increasing the application from twice daily to four times daily does not produce
superior responses, and may lead to increased frequency of topical and systemic
adverse effects (1).
B-One fingertip unit (approximately 500 mg) is sufficient to

cover an area that is twice that of the flat adult handprint
(palm and fingers). (2).
217
4-Preparations should be rubbed in thoroughly and, when possible, applied while
the skin is moist (e.g., after bathing and drying off). Hydration of the skin
increases percutaneous absorption and the resultant therapeutic effect of topical
steroids (1).
5-Children, especially infants, are particularly susceptible to side-effects. A

mild corticosteroid such as hydrocortisone 1% ointment or cream is useful for
treating nappy rash and for atopic eczema in childhood. A moderately potent
or potent corticosteroid may be appropriate for severe atopic eczema on the limbs,
for 1–2 weeks only, switching to a less potent preparation as the condition
improves (2).
6-Thinning of the skin, telangiectasia (a visible permanent dilatation of small

Cutaneous blood vessels), localized fine hair growth, hypopigmentation, and
striae (pink, red or purple lines or bands) can result from repeated application of
topical corticosteroids (1).
7-Mild corticosteroids are generally used on the face. Potent corticosteroids should
generally be avoided on the face (2).
8-When topical treatment has failed, intralesional corticosteroid injections may be

used (2).
9-Topical corticosteroid preparation potencies (Table 13-3) (3).
Table 13-3: potencies of topical corticosteroid (3).
218
Topical Corticosteroids (including Combination products)
Scientific name Trade names Dosage form potencies
1
Any extra notes:
13.9-Preparations for psoriasis

1-Psoriasis is a chronic inflammatory skin disorder characterized by enhanced
epidermal proliferation leading to erythema, scaling, and thickening of the skin
(3)
.
2-There are several types of psoriasis including guttate, flexural, pustular, and
erythrodermic, but chronic plaque psoriasis (psoriasis vulgaris) is the most
common form. In chronic plaque psoriasis the areas most commonly affected are
the extensor sides of the knees, elbows, and hands, and the scalp and sacrum (3).
3-There is no cure and treatment is designed to induce a remission or suppress

disease to a tolerable level (3).
4-Drug therapy for psoriasis are summarized in table 13-4 (1).
5-Topical drugs are the treatment of first choice for chronic plaque psoriasis.
Psoriasis refractory to topical therapy may respond to systemic drugs (3).
6-Ointments are the most occlusive and most potent formulations because of
enhanced penetration into the dermis. Patients may prefer the less greasy creams or
lotions for daytime use (4).
219
Table 13-4: Drug therapy for psoriasis (1, 2)
Topical Agents for the Agents for the Treatment of
Treatment of Psoriasis Severe Psoriasis
1 Emollients 1 Psoralens plus UVA (PUVA)
2 Keratolytics (salicylic acid, urea, Acitretin, Alitretinoin
α-hydroxy acids [i.e., glycolic and 2
lactic acids])
3 Topical corticosteroids 3 Methotrexate
4 Coal tar 4 Cyclosporine
5 Anthralin Immunomodulators (etanercept,
6 Calcipotriene and calcitriol 5 infliximab, adalimumab, golimumab,
7 Tazarotene secukinumab, ixekizumab)
8 Ultraviolet B (UVB)
7-Calcipotriol and tacalcitol are analogues of vitamin D that affect cell division
and differentiation (2).
8-Topical tacrolimus and pimecrolimus have a role in the treatment of psoriasis.

They are indicated also for atopic eczema (2).
9-Acitretin;
A-It is a metabolite of etretinate, is a retinoid (vitamin A derivative) (2).
B-Acitretin is teratogenic. In women with a potential for child-bearing, the

possibility of pregnancy must be excluded before treatment and effective
contraception must be used during treatment and for at least 3 years afterwards
(2)
.
C-Monitor serum-triglyceride, serum-cholesterol, and liver function before
and during treatment (2).
D-Taken with or just after meal. Patient should protect the skin from
sunlight—even on a bright but cloudy day (2).
Preparations for psoriasis (including both topical and systemic products)

1
211
Any extra notes:
13.10-Acne and rosacea

13.10.1-Acne
1-Mild to moderate acne is generally treated with topical preparations. Systemic
treatment with oral antibacterials is generally used for moderate to severe acne or
where topical preparations are not tolerated or are ineffective or where application
to the site is difficult (2).
2-Severe acne is usually treated with oral isotretinoin (2).
3-Concerning topical preparations:

A-Topical preparations for acne include : Benzoyl peroxide, azelaic acid,
topical retinoid and topical antibacterials (2).
B- It is usual to start with a lower strength and to increase the concentration of

benzoyl peroxide gradually (to minimize skin irritation) (2).
C-benzoyl peroxide can bleach clothing and bedding. If it is applied at night,

white sheets and pillowcases are best used and patients can be advised to wear
an old T-shirt or shirt to minimize damage to good clothes (5).
D-Topical tretinoin, its isomer isotretinoin, and adapalene (a retinoid-like

drug), are useful for treating mild to moderate acne. Patients should be warned
that some redness and skin peeling can occur initially but settles with time (2).
E-Topical retinoids should be applied at night, a half hour after cleansing (4).
F-Important : Topical retinoids are contra-indicated in pregnancy; women

of child-bearing age must use effective contraception (2).
G-Topical antibacterials are probably best reserved for patients who wish to
avoid oral antibacterials or who cannot tolerate them. Topical preparations of
erythromycin and clindamycin are effective for inflammatory acne (2).
4-Systemic antibiotics (doxycycline, tetracycline, erythromycin, ciprofloxacin,

trimethoprim-sulfamethoxazole, and trimethoprim alone) are standard therapy for
moderate and severe acne and treatment-resistant inflammatory acne (2, 4).
5-Cyprindiol (cyproterone acetate with ethinylestradiol) contains an anti-

androgen. It is licensed for use in women with moderate to severe acne that has not
responded to topical therapy or oral antibacterials, and for moderately severe
211
hirsutism (although it is an effective hormonal contraceptive, it should not be used
solely for contraception) (2).
6-Oral retinoid for acne:

A-The retinoid isotretinoin reduces sebum secretion. It is used for the systemic
treatment of nodulo-cystic, severe acne, scarring, acne which has not responded
to an adequate course of a systemic antibacterial, or acne which is associated
with psychological problems (2).
B-Isotretinoin is a toxic. It is given for at least 16 weeks; repeat courses are not
normally required (2).
C-Side-effects of isotretinoin include severe dryness of the skin and mucous

membranes, nose bleeds, and joint pains (2).
D-The drug is teratogenic. Women must practise effective contraception for at

least 1 month before starting treatment, during treatment, and for at least 1
month after stopping treatment (2).
7-Spironolactone in higher doses is an antiandrogenic compound. Doses of 50 to

200 mg have been shown to be effective in acne (4).
13.10.2-Rosacea
1-The pustules and papules of rosacea respond to
topical azelaic acid, topical ivermectin or to topical
metronidazole . Alternatively oral administration of
tetracycline, doxycycline or erythromycin
can be used (2).
2-Topical brimonidine tartrate is licensed for the

treatment of facial erythema in rosacea (2).
Topical and oral preparations for acne and Rosacea

1
212
Any extra notes:
13.11-Preparations for warts and calluses

1-Salicylic acid is a useful keratolytic which may be considered first-line for wart
(Apply daily, treatment may need to be continued for up to 3 months); it is also
suitable for the removal of corns and calluses (2).
2-Lactic acid is included in some preparations with salicylic acid. However, there
is no evidence to support greater efficacy when lactic acid is added (6).
3-Advise patient to apply carefully to wart and to protect surrounding skin (e.g.
with soft paraffin or specially designed plaster); rub wart surface gently with file or
pumice stone once weekly (2).
4-Other treatment options for wart are formaldehyde, glutaraldehyde,

cryotherapy and silver nitrate (2).
5-The treatment of external anogenital warts is by topical application of

podophyllin or Imiquimod (2).
Preparations for warts and calluses

1
Any extra notes:
13.12-Sunscreen preparations
1-Sunscreen preparations contain substances that protect the skin against UVA
and UVB radiation, but they are no substitute for covering the skin and avoiding
sunlight (2).
213
2-The sun protection factor (SPF) provides guidance on the degree of protection
offered against UVB; for example, a SPF of 8 should enable a person to remain 8
times longer in the sun without burning (2).
3-All products should be applied 20 minutes before exposure to the sun, and
reapplied every 2 to 4 hours and after swimming to ensure maximum protection (6).
4-Sunscreen must be applied to all exposed areas of the body including the nose
ad lips but avoid contact with eye (7).
Sunscreen preparations
Scientific name Trade names Dosage form SPF
1
Any extra notes:
13.13-Hair conditions
13.13.1-Androgenetic alopecia
1-Finasteride is licensed for the treatment of androgenetic alopecia in men.
Continuous use for 3–6 months is required before benefit is seen, and effects are
reversed 6–12 months after treatment is discontinued (2).
2-Topical application of minoxidil (1mL twice daily) may stimulate limited hair
growth in a small proportion of adults but only for as long as it is used (2).
3-Minoxidil is available in 2% and 5% concentrations (6). The 2% and 5%

products are approved for use in both men and women (7).
Preparations for androgenetic alopecia

1
Any extra notes:
214
13.13.2-Hirsutism
1-Topical eflornithine can be used as an adjunct to laser therapy for facial
hirsutism in women (2).
2-Co-cyprindiol may be effective for moderately severe hirsutism. Metformin

hydrochloride is an alternative in women with polycystic ovary syndrome.
Systemic treatment is required for 6–12 months before benefit is seen (2).
Preparations for hirsutism

1
Any extra notes:
13.13.3-Dandruff and seborrhoeic dermatitis

1-Ketoconazole shampoo is used for seborrhoeic dermatitis and dandruff (leave
preparation on for 3–5 minutes before rinsing ) (treatment: Apply twice weekly
for 2–4 weeks) (Prophylaxis: Apply every 1–2 weeks). Selenium sulfide
shampoo is also used (2).
2-Cradle cap in infants may be treated with olive oil applications overnight,
followed by using a baby shampoo the next morning (6). Ketoconazole has been
shown to be effective (8).
13.14-Antiperspirants
1-Hyperhidrosis (excessive sweating) can be generalized or focal, affecting the
palms of the hands, soles of the feet, or axillae (3).
2-Drug therapy should be tried initially but is often ineffective in severe cases.
Aluminium salts, such as aluminium chloride or aluminium chlorohydrate in
alcoholic solvents applied topically, may be successful in milder forms of focal
hyperhidrosis (3).
Antiperspirants (if available )

1
Any extra notes:
215
References
11th ed., 2018.
2-BNF-74.
Press 2009.
2017.
5-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the pharmacy . A guide
to the managements of common illness. 7th edition. 2014.
216
217

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7 Central nervous system 28

2 Endocrine system 010

4 Genito-urinary system 080

2 Immune system and malignant disease 034

7 Nutrition and blood 072

01 Musculoskeletal and joint diseases 028

08 Ear, nose, and oropharynx 022

2-Examples include (captopril, enalapril, fosinopril, imidapril, lisinopril,

A-Therapy should be started with low doses followed by gradual titration as

9-Angioedema is a serious potential complication of ACEi therapy. It occurs in

10-An ACEi, as well as an ARB or direct renin inhibitor, are absolutely

Any extra notes:

1.2-Angiotensin II receptor blockers(ARBs).

2-Examples include (Azilsartan, candesartan, eprosartan, irbesartan, losartan,

Any extra notes:

1.3-Beta-adrenoceptor blocking drugs (beta-blockers)

2-Oxprenolol, and pindolol have intrinsic sympathomimetic activity (ISA); they

4-Beta blockers are used in the management of:

B-They are also given to control symptoms of sympathetic overactivity,

6-Esmolol is a relatively cardioselective beta-blocker with a very short duration of

7-Sotalol, a non-cardioselective beta-blocker with additional class III anti-

B-β-Blockers are only considered appropriate first-line agents to treat specific

9-Beta-blockers can precipitate bronchospasm and should therefore usually be

10-Atenolol, bisoprolol, metoprolol, and nebivolol, have less effect on the β2

12-Beta-blockers can mask the signs and symptoms of hypoglycemia (such as

13-Abrupt cessation of β-blocker therapy may produce unstable angina, MI, or

Any extra notes:

1.4-Neprilysin inhibitors (Sacubitril)

Scientific name Trade name Dosage form

Any extra notes:

2-Aliskiren is an alternative therapy because of lack of long-term studies

Scientific name Trade name Dosage form

Any extra notes:

1.6-Calcium-channel blockers (CCBs)

B-Non-Dihydropyridine CCBs (examples diltiazem and verapamil): They

2-The main use of CCBs is in the management of angina pectoris and

3-Nimodipine is related to nifedipine but the smooth muscle relaxant effect

4-Verapamil is used also as prophylaxis of cluster headache. Nifedipine is also

8-Verapamil and diltiazem should usually be avoided in heart failure (systolic

9-Unlike in systolic HF, nondihydropyridine calcium channel blockers

10-Nifedipine is a short acting, therefore it is commonly formulated as sustained

12-Different versions of modified-release preparations may not have the same

14-Grapefruit juice increases the concentration of (amlodipine, nifedipine,

Table 1-1: Types of diuretics

5-Thiazides are believed to lose their effectiveness when creatinine clearance

6-Potassium-sparing diuretics are weak antihypertensives when used alone.

7-Because they do not alter disease progression or prolong survival, diuretics

8-Chlortalidone, a thiazide-related compound, has a longer duration of action than

10-Xipamide and indapamide are chemically related to chlortalidone. Indapamide

11-Spironolactone is of value in the treatment of edema and ascites caused by

14-I.V Furosemide doses greater than 50 mg given by intravenous infusion only.

16-Spironolactone is given after food (2). It has an anti-androgenic properties,

17-In concentrations of 15% or greater, mannitol may crystallize when exposed to

Any extra notes:

Note : Fixed-dose combination products

2-Most fixed-dose combinations include a thiazide diuretic. Other fixed-dose

Fixed-dose combination products

Table 1-2: Types of lipid regulating drugs

4-Relative LDL–lowering efficacy of statins are shown in table 1-3 (10).

6-Less common adverse effects include myopathy, elevated hepatic

8-Liver enzymes should be measured before treatment, and repeated within 3

9-Grapefruit juice increases the concentration of simvastatin (avoid) (2).