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1
Toxicity is a measure to the degree to which something is toxic or poisonous.
The study of poisons is known as toxicology. Toxicity can refer to the effect on a Metabolism based drug interactions: One notable system involved in metabolic
whole organism, such as a human or a bacterium or a plant, or to a substructure, drug interactions is the enzyme system comprising the cytochrome P450
such as a cell (cytotoxicity) or the liver. In the science of toxicology, the subject of oxidases. This system may be affected by either enzyme induction or enzyme
such study is the effect of an external substance or condition and its deleterious inhibition, as discussed in the examples below.
effects on living things: organisms, organ systems, individual organs, tissues, Enzyme induction - drug A induces the body to produce more of an enzyme
cells, subcellular units. A central concept of toxicology is that effects are dose- which metabolises drug B. This reduces the effective concentration of drug B,
dependent; even water – by itself not toxic – can lead to water intoxication when which may lead to loss of effectiveness of drug B. Drug A effectiveness is not
taken by a human in large enough doses, whereas for even a very toxic altered.
substance such as snake venom there is a dose for which there is no toxic effect Enzyme inhibition - drug A inhibits the production of the enzyme metabolising
detectable. drug B, thus an elevation of drug B occurs possibly leading to an overdose.
Drug interaction is a situation in which a substance e.g. another drug, affects the
activity of a drug, i.e. the effects are increased or decreased. Typically, interaction Bioavailability - drug A influences the absorption of drug B. The examples
between drugs come to mind (drug-drug interaction). However, interactions may described above may have different outcomes depending on the nature of the
also exist between drugs & foods (drug-food interactions), as well as drugs & drugs. For example, if Drug B is a prodrug, then enzyme activation is required for
herbs (drug-herb interactions). Drug interactions may be the result of various the drug to reach its active form. Hence, enzyme induction by Drug A would
processes that alter the the pharmacokinetics of the drug (ADME). Alternatively, increase the effectiveness of the drug B by increasing its metab olism to its active
drug interactions may be the result of the pharmacodynamic properties of the form. Enzyme inhibition by Drug A would decrease the effectiveness of Drug B.
drug, e.g. via the co -administration of a receptor antagonist and an agonist for the
same receptor.
2
Category Sample Drug Interaction Information Category Sample Drug Interaction Information
Nasal -Ask a doctor before use if you: have heart disease, high blood pressure, thyroid disease, Acid Reducers ( H2 -For products containing cimetidine, ask a doctor or pharmacist before use if you are :
Decongestants diabetes, or difficulty in urination due to an enlarged prostate gland Receptor taking theophylline(oral asthma drug), warfarin (blood thinning drug), or phenytoin
Nicotine -Ask a doctor before use if you: have high blood pressurenot controlled by medication; Antagonists) (seizure drug)
Replacement have heart disease or have had a recent heart attack or irregular heartbeat, since nicotine Antacids -Ask a doctor or pharmacist before use if you are: allergic to milk or milk products if the
Products can increase your heart rate product contains more than 5 grams lactose in a maximum daily dose;
-Ask a doctor or pharmacist before use if you are: taking a prescription drug for -Ask a doctor before use if you have: kidney disease
depression or asthma (your dose may need adjustment);
-Do not use: if you continue to smoke, chew tobacco, use snuff, or use othernicotine- Antiemetics -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers
containing products -Ask a doctor before use if you have: a breathing problem, such as emphysema or chronic
bronchitis; glaucoma; difficulty in urination due to an enlarged prostate gland
Nighttime -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers -When using this product: avoid alcoholicbeverages
Sleep Aids -Ask a doctor before use if you have: a breathing problem such as emphysema or chronic
bronchitis; glaucoma; difficulty in urination due to an enlarged prostate gland Antihistamines -Ask a doctor or pharmacist before use if you are taking: sedatives or tranquilizers ; a
-When using this product: avoid alcoholicbeverages prescription drug for high blood pressure or depression
-Ask a doctor before use if you have: glaucoma or difficulty in urination due to an
Pain Relievers -Ask a doctor before taking if you: consume three or more alcohol-containing drinks per
enlarged prostate; breathing problems, such as emphysema, chronic bronchitis, or asthma
day. (The following ingredients are found in different OTC pain relievers: acetaminophen, -When using this product: alcohol, sedatives, and tranquilizers may increase drowsiness;
aspirin, ibuprofen, ketoprofen, magnesium salicylate , and naproxen. Important to read the avoid alcoholic beverages
label of these products to learn about various drug interaction warnings for each ingredient.)
Antitussives -Ask a doctor or pharmacist before use if you are: taking sedatives or tranquilizers
Stimulants -When using this product: limit the use of foods, beverages, and other drugs that have (Cough Medicine) -Ask a doctor before use if you have: glaucoma or difficulty in urination due to an
caffeine. Too much caffeine can cause nervousness, irritability, sleeplessness, and occasional enlarged prostate gland
rapid heart beat; be aware that the recommended dose of this product contains about as much
caffeine as a cup of coffee Bronchodilators -Ask a doctor before use if you: have heart disease, high blood pressure, thyroid disease,
diabetes, or difficulty in urination due to an enlarged prostate gland;
Topical Acne -When using this product: increased dryness or irritation of the skin may occur immediate ly
Drugs following use of this product or if you are using other topical acne drugs at the same time. If Laxatives -Ask a doctor before use if you have: kidney disease and the laxative contains
this occurs, only one drug should be used unless directed by your doctor phosphates, potassium, or magnesium; stomach pain, nausea, or vomiting
A dose-response curve is a simple X-Y graph relating the amount of a drug Phase I and Phase II reactions are biotransformations of chemicals that
occur during drug metabolism.
or toxin given to the response of the organism to that drug. The curves are
usually qualitative , though they can use quantitative information. Phase I metabolism usually precedes Phase II, though not necessarily.
During these reactions, polar bodies are either introduced or unmasked,
The measured dose (usually in [[milligrams, micrograms , or grams per
kilogram of body-weight) is generally plotted on the X axis and the response which results in (more) polar metabolites of the original chemicals. Phase I
reactions may occur by oxidation, reduction or hydrolysis reactions. If the
is plotted on the Y axis. Commonly, it is the logarithm of the dose that is
metabolites of phase I reactions are sufficiently polar, they may be readily
plotted on the X axis, and in such cases the curve is typically sigmoidal , with
the steepest portion in the middle. The first point along the graph where a excreted at this point. However, many phase I products are not eliminated
rapidly and undergo a subsequent reaction in which an endogenous
response above zero is reached is usually referred to as a threshold -dose.
For most beneficial or recreational drugs, the desired effects are found at substrate combines with the newly incorporated functional group to form a
highly polar conjugate.
doses slightly greater than the threshold dose. At higher doses still, undesired
side effects appear and grow stronger as the dose increases. The stronger a Phase II reactions — usually known as conjugation reactions (e.g., with
glucuronic acid, sulfonates (commonly known as sulfation) , glutathione or
particular substance is, the steeper this curve will be. In quantitative
situations, the Y-axis usually is designated by percentages, which refer to the amino acids ) — are usually detoxication in nature, and involve the
interactions of the polar functional groups of phase I metabolites.
percentage of users registering a standard response (which is often death,
when the 50% mark refers to LD50).
3
A sedative is a substance that depresses the central nervous system (CNS), resulting
in calmness, relaxation, reduction of anxiety, sleepiness, slowed breathing, slurred
speech, staggering gait , poor judgment, and slow, uncertain reflexes. Sedatives may be Hypnotic drugs are a class of drugs that induce sleep (which differentiates
referred to as tranquilizers, depressants, anxiolytics, soporifics, sleeping pills, them from the sedative category), used in the treatment of severe insomnia
downers, or sedative-hypnotics. At high doses or when they are abused, many of and in surgical anesthesia. Often the treatment of insomnia will not begin
these drugs can cause unconsciousness (see hypnotic) and death. with drugs at all, however, as many (not all) hypnotic drugs are habit forming.
A physician will usually recommend alternative sleeping patterns and
exercise before prescribing medication for sleep. These drugs include:
Examples of sedatives Uncategorized sedatives Barbiturates
Antidepressants eszopiclone (Lunesta®) Benzodiazepines
mirtazapine (Remeron®) ramelteon (Rozerem®) Zolpidem
trazodone (Desyrel®) methaqualone (Sopor®, Quaalude®) Zaleplon
Barbiturates ethchlorvynol (Placidyl®) Zopiclone
secobarbital (Seconal®) chloral hydrate (Noctec ®) Eszopiclone
pentobarbital (Nembutal ®) meprobamate (Miltown ®)
amobarbital (Amytal ®) chloral hydrate
glutethimide ( Doriden ®)
Benzodiazepines ("minor tranquilizers") methyprylon (Noludar ®) Chlormethiazole
alprazolam (Xanax®) gamma-hydroxybutyrate (GHB) Antihistamines
diazepam (Valium®) ethyl alcohol (alcoholic beverage) Doxylamine
lorazepam (Atavan ®) diethyl ether (Ether) Promethazine
Herbal sedatives methyl trichloride (Chloroform) diphenhydramine.
catnip zopiclone (Imovane®, Zimovane ®)
Valerian (plant) chloral hydrate (Noctec ®)
Mandrake Alcohol is often tried as a hypnotic drug but it is not particularly effective.
zaleplon (Sonata®)
Kava Kava zolpidem (Ambien®)
Anti-Convulsants Antipsychotics are drugs used to treat psychosis (e.g. schizophrenia, mania
1 Aldehydes and delusional disorder. Antipsychotics also have some effects as mood
The anticonvulsants, sometimes also called
2 Aromatic allylic alcohols stabilizers , leading to their frequent use in treating mood disorder (particularly
antiepileptics, belong to a diverse group of
3 Barbiturates bipolar disorder) even when no signs of psychosis are present. Antipsychotics
pharmaceuticals used in prevention of the
4 Benzodiazepines are also referred to as neuroleptic drugs. The word neuroleptic is derieved
occurrence of epileptic seizures. The goal of
5 Bromides from Greek. 'Neuro ' refers to the nerves and 'lept' means 'to take hold of'. Thus
an anticonvulsant is to suppress the rapid and
6 Carbamates the word means 'taking hold of one's nerves' which implies their role in mood
excessive firing of neurons that start a
7 Carboxamides stabilization. There are currently two main types:
seizure. Failing this, a good anticonvulsant
8 Fatty acids 1. Typical antipsychotics ("major tranquilizers")
would prevent the spread of the seizure within
9 Fructose derivatives fluphenazine (Prolixin®)
the brain and offer protection against possible
10 Gaba analogs haloperidol (Haldol ®)
excitotoxic effects that may result in brain
11 Hydantoins thiothixene (Navane®)
damage. An excellent anticonvulsant would
12 Oxazolidinediones trifluoperazine (Stelazine®, Trifluoperaz®)
have few serious side effects. However, no
13 Propionates loxapine succinate (Loxitane®)
such drug exists.
14 Pyrimidinediones perphenazine (Etrafon®, Trilafon®)
15 Pyrrolidines prochlorperazine (Compazine®)
Many anticonvulsants block Sodium (Na+)
16 Succinimides 2. Atypical antipsychotics
channels , Calcium (Ca2+) channels, AMPA
17 Sulfonamides clozapine (Clozaril®)
receptors or NMDA receptors . Some
18 Triazines quetiapine (Seroquel®)
anticonvulsants inhibit the metabolism of
19 Ureas risperidone (Risperdal ®)
GABA or increase its release.
20 Valproylamides (amide ziprasidone (Geodon®) (some become tired, some get insomnia)
derivatives of valproate) olanzapine (Zyprexa®)
Anti-depressants
An antidepressant is a medication designed to treat or alleviate the
Monoamine oxidase inhibitors (MAOI) Harmaline, Iproclozide, Iproniazid , Isocarboxazid , Nialamide,
symptoms of clinical depression. Some antidepressants, notably the
Phenelzine, Selegiline, Toloxatone, Tranylcypromine
tricyclics , are commonly used off-label in the treatment of neuropathic pain,
whether or not the patient is depressed. Smaller doses are generally used for Reversibleinhibitor of monoamineoxidase A
Brofaromine, Moclobemide
(RIMA)
this purpose, and they often take effect more quickly. Many antidepressants
Dopamine reuptake inhibitor(DARI) Amineptine, Phenmetrazine, Vanoxerine, Modafinil
also are used for the treatment of anxiety disorders , and tricyclic
antidepressants are used in the treatment of chronic pain disorders such as Norepinephrine-dopamine reuptake inhibitors Bupropion
chronic functional abdominal pain (CFAP), myofascial pain syndrome, and
Norepinephrine reuptake inhibitor(NRI) or
post-herpetic neuralgia. (NARI)
Atomoxetine, Maprotiline, Reboxetine, Viloxazine
The main classes of antidepressants have similar efficacy, but the newer
Serotonin -norepinephrine reuptake inhibitor
types are generally regarded to have a more benign side -effect profile and (SNRI)
Duloxetine, Milnacipran , Venlafaxine
less risk of lethality if taken in overdose.
Selective serotonin reuptake inhibitor(SSRI) Alaproclate , Etoperidone, Citalopram, Escitalopram, Fluoxetine,
Mechanism of action: The therapeutic effects of antidepressants are Fluvoxamine, Paroxetine, Sertraline, Zimelidine
believed to be related to an effect on neurotransmitters , particularly by
Selective serotonin reuptake enhancer (SSRE)
inhibiting the monoamine transporter proteins of serotonin and Tianeptine
norepinephrine. SSRI’s specifically prevent the reuptake of serotonin Tricyclicantidepressants (TCA) Amitriptyline, Amoxapine, Butriptyline, Clomipramine,
(thereby increasing the level of serotonin in synapses of the brain), whereas Desipramine, Dibenzepin , Dothiepin , Doxepin , Imipramine,
earlier monoamine oxidase inhibitors (MAOIs) blocked the destruction of Iprindole, Lofepramine, Melitracen , Nortriptyline, Opipramol,
Protriptyline, Trimipramine
neurotransmitters by enzymes which normally break them down. Tricyclic
Tetracyclic antidepressants
antidepressants (TCAs ) prevent the reuptake of various neurotransmitters , Maprotiline, Mianserin , Nefazodone, Trazodone
including serotonin, norepinephrine, and dopamine. Noradrenergic and specific serotonergic
antidepressant (NaSSA) Mirtazapine
4
Adrenergic Agents bind with adrenergic receptors (or adrenoceptors),
which are a class of G protein-coupled receptors that are targets of the
catecholamines. Adrenergic receptors specifically bind their endogenous
3.0. Autonomic [3 Qs] ligands , the catecholamines adrenaline and noradrenaline (also called
epinephrine and norepinephrine in the USA), and are activated by these. Many
cells possess these receptors, and the binding of an agonist will generally
3.1. Adrenergics cause the cell to respond in a fight-or-flight manner. For instance, the heart rate
will increase and the pupils will dilate, energy will be mobilized, and blood flow
3.2. Cholinergics diverted from other organs to skeletal muscle.
Indirect
Amphetamine – Tyramine
Acting
Mixed Ephedrine
Action:
Beta blockers are a class of drugs used for various indications, but
Alpha blockers (also called alpha-adrenergic blocking agents) constitute a particularly for the management of cardiac arrhythmias and cardioprotection
variety of drugs which block a1 -adrenergic receptors in arteries and smooth after myocardial infarction.
muscles. Beta blockers block the action of endogenous catecholamines, epinephrine
(adrenaline) and norepinephrine (noradrenaline) in particular, on ß-adrenergic
receptors , part of the sympathetic nervous system which mediates the "fight
Indications: These drugs may be used to treat: or flight" response. There are three known types of beta receptor, designated
•benign prostatic hyperplasia (BPH) ß1, ß2 and ß3. ß1-Adrenergic receptors are located mainly in the heart,
•high blood pressure (hypertension). This is not typically the drug of choice kidney, and adipose tissue. ß2-Adrenergic receptors are located mainly in the
unless the patient also has BPH. heart, lung, GI tract, liver, pancreas, and skeletal muscle. The role and
•symptoms of non inflammatory chronic pelvic pain syndrome, a type of location of ß3-receptors is less well-defined.
prostatitis. As a side effect they may reduce blood pressure and result in
lightheadedness. Indications for beta blockers include:
Hypertension
Examples of alpha blockers: Alpha blockers include: Angina
•Doxazosin (Cardura) Cardiac arrhythmia
•Prazosin (Minipress ) Congestive heart failure
•Phenoxybenzamine Myocardial infarction
•Phentolamine (Rogitine) Glaucoma
•Tamsulosin (Flomaxtra/Flomax) Migraine prophylaxis
•Alfuzosin (Uroxatral) Symptomatic control (tachycardia , tremor) in anxiety and hyperthyroidism
•Terazosin (Hytrin) Essential tremor
Phaeochromocytoma, in conjunction with a-blocker
5
Beta-Blocking Drugs
Non-selective agents ß1-Selective agents
Alprenolol Acebutolol
Carteolol
Levobunolol
Atenolol
Betaxolol
4.0. Cardiovascular [4 Qs]
Mepindolol
Metipranolol
Bisoprolol
Esmolol
4.1. Cardiac glycosides
Nadolol
Oxprenolol
Metoprolol
Nebivolol
4.2. Antiarrhythmics
Penbutolol
Pindolol
Mixed a1/ß-adrenergic antagonists
Carvedilol
4.3. Antihypertensives - diuretics
Propranolol
Sotalol
Celiprolol
Labetalol
4.4. Anti-anginal agents
Timolol ß2-Selective agents
Butoxamine (weak a-adrenergic
4.5. Anticoagulants, coagulants &
agonist activity) antihyperlipidemics
Cardiac glycosides are drugs used in the treatment of congestive heart failure Antiarrhythmic agents are used to suppress fast rhythms of the heart (cardiac
arrhythmias), such as atrial fibrillation, atrial flutter, ventricular tachycardia, and
and cardiac arrhythmia. These glycosides are found as secondary metabolites
in several plants, but also in some animals. Some of these compounds ventricular fibrillation. Suppression is often done to relieve the symptoms that may
be associated with the loss of the atrial component to ventricular filling (atrial kick )
(ouabain and some frog poisons) are used in Africa as arrow-poisons for
hunting. Cardiac glycosides work by inhibiting the Na+/K+ pump. They do this that is due to atrial fibrillation or flutter. In individuals with ventricular arrhythmias,
antiarrhythmic agents are often still in use to suppress arrhythmias. If these drugs
by stabilizing the E2-P transition state of the Na+/K+ pump. This inhibition
fail it may lead to implantation of an implantable cardioverter-defibrillator (ICD).
increases the amount of Ca++ ions available for contraction of the heart
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muscle, improves cardiac output and reduces distention of the heart. T hey
5 main classes in the Vaughan Williams system of antiarrhythmic agents:
have an antiarrhythmic effect by prolonging the refractory period of the AV
node (Atrioventricular node), reducing the number of impulses reaching the Class I agents interfere with the sodium (Na+) channel.
Class II agents are anti-sympathetic nervous system agents (all: beta blockers ).
ventricles. Cardiac output is restored but atrial fibrillation or atrial flutter are not
abolished. Examples of plants producing cardiac glycosides: Class III agents affect potassium (K+) efflux.
Class IV agents affect the AV node.
- Strophanthus - ouabain g/k/e-strophanthin
- Digitalis lanata and Digitalis purpurea - digoxin, digitoxin Class V agents work by other or unknown mechanisms.
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Digoxin is a cardiac glycoside extracted from the foxglove plant, digitalis. Its class Ia:Ajmaline , Disopyramide, Prajmaline, Procainamide, Quinidine, Sparteine
class Ib: Aprindine, Lidocaine , Mexiletine, Tocainide
corresponding aglycone is digoxigenin. Digoxin is widely used in the treatment
class Ic:Encainide, Flecainide, Lorcainide, Moricizine, Propafenone
of various heart conditions, namely atrial fibrillation, atrial flutter and congestive
class II: various Beta blockers
heart failure that cannot be controlled by other medication. Digoxin
class III:Amiodarone, Bretylium tosilate, Bunaftine, Dofetilide, Ibutilide
preparations are commonly marketed under the trade name Lanoxin.
class IV: various Calcium channel blockers
class V:Adenosine, Digoxin
Antihypertensives:
1.1 Diuretics Anti-anginal agents: for treatment of angina pectoris, a symptom of ischaemic
heart disease. Drugs used are:
1.2 Anti-adrenergics
1.3 Calcium channel blockers 1. nitrates such as nitroglycerin (glyceryl trinitrate) or pentaerythritol tetranitrate
1.4 ACE inhibitors These drugs cause vasodilation of the venous capacitance vessels by simulating
the endothelium-derived relaxing factor (EDRF). Used to relieve both exertional and
1.5 Angiotensin II receptor antagonists
1.6 Aldosterone antagonists vasospastic angina by allowing venous pooling, reducing the pressure in the
ventricles and so reducing wall tension and oxygen requirements in the heart.
1.7 Vasodilators
1.8 Centrally acting adrenergic drugs Short-acting nitrates are used to abort angina attacks that have occurred, while
longer-acting nitrates are used in the prophylactic management of the condition.
1.8.1 Adrenergic neuron blockers
1.9 Herbals provoking hypotension ---------------------
2. beta blockers , either cardioselectives such as acebutolol or metoprolol , or non-
1. Diuretics: help the kidneys eliminate excess salt and water from the body's cardioselectives such as oxprenolol or sotalol
These drugs are used in the prophylaxis of exertional angina by reducing the work
tissues and blood. There are several types including:
-Loop diuretics: (bumetanide, ethacrynic acid, furosemide, torsemide) the heart is allowed to perform below the level that would provo ke an angina attack.
They cannot be used in vasospastic angina and can precipitate heart failure.
-Thiazides: (chlortalidone, epitizide, hydrochlorothiazide & chlorothiazide)
----------------------
-Thiazide-like diuretics: (indapamide, metolazone)
-Potassium-sparing diuretics : (amiloride; triamterene) 3. calcium channel blockers , either Class I agents (e.g., verapamil), Class II agents
(e.g., amlodipine, nifedipine), or the Class III agent diltiazem.
(NOTE: evidence suggest that by lowering blood pressure. Evidenc e suggests that These drugs are Calcium ion antagonists and are used for treatment of exertional &
vasospastic angina. In vitro, they dilate coronary & peripheral arteries. T hey have
reduction of the blood pressure by 5-6 mmHg can decrease the risk of stroke by
40%, of coronary heart disease by 15-20%, and reduces the likelihood of dementia, negative inotropic & chronotropic effects, decreasing afterload, improving
myocardial efficiency, reducing heart rate & improving coronary blood flow.
heart failure, and mortality from cardiovascular disease.)
6
Acenocoumarol, Clorindione, Dicumarol
Vitamin K
(Dicoumarol}, Diphenadione, Ethyl biscoumacetate,
antagonists:
Phenprocoumon, Phenindione, Tioclomarol, Warfarin
An anticoagulant is a substance that prevents coagulation; that is, it stops Heparin group Antithrombin III, Bemiparin , Dalteparin, Danaparoid,
(Platelet aggregation Enoxaparin, Heparin, Nadroparin, Parnaparin ,
blood from clotting. Anticoagulants are given to people to stop thrombosis
(blood clotting inappropriately in the blood vessels). This is useful in primary and inhibitors): Reviparin, Sulodexide, Tinzaparin
secondary prevention of deep vein thrombosis , pulmonary embolism, Abciximab, Acetylsalicylic acid (Aspirin), Aloxiprin,
myocardial infarctions and strokes in those who are predisposed. Beraprost, Ditazole, Carbasalate calcium,
1. Vitamin K antagonists: Oral anticoagulants are a class of pharmaceuticals Other platelet
Cloricromen, Clopidogrel, Dipyridamole,
aggregation
that act by antagonizing the effects of vitamin K. It is important to note that they Epoprostenol , Eptifibatide, Indobufen, Iloprost,
take at least 48 to 72 hours for the anticoagulant effect to develop fully. In cases inhibitors:
Picotamide, Prasugrel , Ticlopidine, Tirofiban,
when an immediate effect is required, heparin must be given concomitantly. Treprostinil, Triflusal
The most important oral anticoagulants are Warfarin (Coumadin). Heparin and Alteplase, Ancrod, Anistreplase, Brinase, Drotrecogin
derivative substances: Heparin is a biological substance, usually made from Enzymes: alfa, Fibrinolysin, Protein C, Reteplase, Saruplase ,
pig intestines. It works by activating antithrombin III, which blocks thrombin from Streptokinase, Tenecteplase, Urokinase
clotting blood.
2. Direct thrombin inhibitors: Another type of anticoagulant is the direct Direct thrombin Argatroban, Bivalirudin, Dabigatran, Desirudin,
thrombin inhibitors . Current members of this class include argatroban, lepirudin, inhibitors: Hirudin, Lepirudin, Melagatran, Ximelagatran
and bivalirudin. Other Dabigatran, Defibrotide, Dermatan sulfate,
antithrombotics: Fondaparinux, Rivaroxaban
Non-medicinal: Citrate, EDTA , Oxalate
7
A local anesthetic is a drug that reversibly
inhibits the propagation of signals along
nerves. When it is used on specific nerve Amino esters
pathways, effects such as analgesia (loss of Adverse reactions to local anesthetics are not infrequent, but true
Benzocaine
pain sensation) and paralysis (loss of muscle allergyis very rare. Non-allergic reactions may resemble allergy in
Chloroprocaine
power) can be achieved. Clinical local their manifestations. In some cases, skin tests and provocative
Cocaine
anesthetics belong to one of two classes:
Procaine challenge may be necessary to establish a diagnosis of allergy. There
aminoamide and aminoester local
Amino amides are also cases of allergy to paraben derivatives, which are often
anesthetics. These so-called synthetic local
anesthetics are structurally related to cocaine . Bupivacaine added as preservatives to local anesthetic solutions.
Local anesthetic drugs act mainly by inhibiting Levobupivacaine ---------------------------
sodium influx through sodium-specific ion Lidocaine Methemoglobinemia: The systemic toxicity of prilocaine is
channels in the neuronal cell membrane, in Mepivacaine comparatively low, however its metabolite, o-toluidine, is known to
particular the voltage-gated sodium channels. Prilocaine cause methemoglobinemia. As methemoglobinemiareduces the
When the influx of sodium is interrupted, an amount of hemoglobin that is available for oxygen transport, this side
Ropivacaine
action potential cannot arise and signal effect is potentially life-threatening. Therefore dose limits for prilocaine
conduction is inhibited. Local anesthetics are Septocaine
should be strictly observed. Prilocaine is not recommended for use in
weak bases and are usually formulated as the Combinations
hydrochloride salt to render them water- Lidocaine/prilocaine (EMLA) infants.
soluble. Acidosis such as caused by wound
infection partly reduces the action of local
anesthetics because of reduced ability to
cross the cell membrane.
Brand
An antibiotic is a drug that kills or slows the growth of bacteria . They have no Class Generic Name Common Uses Side Effects
Names
effect against viruses, fungi, or parasites. Antibiotics are generally small
molecules with a molecular weight less than 2000 kd. They are not enzymes. Aminoglycosides Amikacin Amikin
Some antibiotics have been derived from mold, for example the penicillin
Gentamicin Garamycin
class. Antibiotics can be categorized based on their target specificity: 'narrow-
spectrum' antibiotics target particular types of bacteria, such as Gram- Kanamycin Infections caused by Hearing loss
negative or Gram-positive bacteria, while 'wide -spectrum' antibiotics affect a Gram-negative bacteria, Vertigo
Neomycin
larger range of bacteria. The effectiveness of individual antibiotics varies with such as Escherichia coli Kidney
Netilmicin and Klebsiella damage
the location of the infection, the ability of the antibiotic to reach the site of
infection, and the ability of the bacteria to resist or inactiva te the antibiotic.
Streptomycin
Some antibiotics actually kill the bacteria (bactericidal), whereas others
merely prevent the bacteria from multiplying (bacteriostatic ). Antibiotics can Tobramycin Nebcin
also be classified by the organisms against which they are effec tive, and by Carbacephem
the type of infection in which they are useful, which depends on the Loracarbef Lorabid
sensitivities of the organisms that most commonly cause the infection and the
Carbapenems Ertapenem
concentration of antibiotic obtainable in the affected tissue.
Imipenem/
Primaxin
Cilastatin
Meropenem
8
Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics
Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics
Brand
Class Generic Name Common Uses Side Effects
Names
Cephalosporins Cefadroxil Duricef Class Generic Name Brand Names Common Uses Side Effects
Gastrointestinal upset and diarrhea
(First generation)
Cefazolin Ancef Nausea (if alcohol taken concurrently)
Allergic reactions Glycopeptides
Cephalexin Keflex Teicoplanin
Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics Antibiotics
Brand
Class Generic Name Common Uses Side Effects
Names Class Generic Name Brand Names Common Uses Side Effects
Sulfonamides Mafenide Others Chloramphenicol Chloromycetin
Sulfacetamide Ethambutol
Nausea, vomiting, and
diarrhea Fosfomycin
Sulfamethizole
Urinary tract infections Allergy (including skin Furazolidone
Sulfanilimide (archaic) (except sulfacetamide rashes)
and mafenide); Crystals in urine Isoniazid
Sulfasalazine mafenide is used Kidney failure Linezolid Zyvox
Sulfisoxazole topically for burns Decrease in white blood
cell count Metronidazole Flagyl
Trimethoprim Sensitivity to sunlight Nitrofurantoin Macrodantin
Trimethoprim- Platensimycin
Sulfamethoxazole Bactrim
(Co-trimoxazole ) Pyrazinamide
9
Antifungals work by exploiting differences between mammalian and fungal cel ls
Use or misuse of antibiotics may result in the development of antibiotic to kill off the fungal organism without significantly harming the host. Unlike
resistance by the infecting organisms, similar to the development of pesticide bacteria, both fungi and humans are eukaryotes. The basic structure of fungal
resistance in insects. Evolutionary theory of genetic selection requires that as cells and human cells is nearly identical. This means it is more difficult to find a
close as possible to 100% of the infecting organisms be killed off to avoid target for an antifungal medication to attack that does not also exist in the
selection of resistance; if a small subset of the population survives the infected organism. Consequently, some of the side-effects of systemic anti -
treatment and is allowed to multiply, the average susceptibility of this new fungals can be life -threatening. Classes include:
population to the compound will be much less than that of the original 1. Polyene antibiotics: bind with sterols in the fungal cell wall, principally
population, since they have descended from those few organisms which ergosterol and this causes the cell's contents to leak out and the cell di es. Animal
survived the original treatment. This survival often results from an inheritable cells have cholesterol instead of ergosterol and are less susceptible: Nystatin ;
resistance to the compound which was infrequent in the original population Amphotericin B; Natamycin ; Rimocidin; Filipin; Pimaricin.
but is now much more frequent in the descendants thus selected entirely 2. Imidazoles and triazoles: inhibit the enzyme cytochrome P450 14a-
from those originally infrequent resistant organisms. demethylase. This enzyme converts lanosterol to ergosterol, and is required in
An abscess caused by methicillin-resistant Staphylococcus aureus bacteria fungal cell wall synthesis and block steroid synthesis in humans. Imidazoles:
(MRSA). By 1984 half of the people with active tuberculosis in the United Miconazole; Ketoconazole; Clotrimazole ; Econazole; Mebendazole; Bifonazole ;
States had a strain that resisted at least one antibiotic. In certain settings, Butoconazole ; Fenticonazole; Isoconazole; Oxiconazole ; Sertaconazole;
such as hospitals and some child-care locations, the rate of antibiotic Sulconazole; Thiabendazole; Tiaconazole. Triazoles: Fluconazole; Itraconazole;
resistance is so high that the normal, low cost antibiotics are virtually useless Ravuconazole; Posaconazole; Voriconazole.
for treatment of frequently seen infections. The situation is worsened by the 3. Allylamines: inhibit enzyme squalene epoxidase, an enzyme required for
fact that genes coding for antibiotic resistance can be transferred between ergosterol synthesis: Terbinafine (Lamisil ); Amorolfine; Naftifine ; Butenafine.
bacteria, making it possible for bacteria never exposed to an an tibiotic to 4. Echinocandin: inhibit the synthesis of glucan in the cell wall, probably via the
acquire resistance from those which have. enzyme 1,3-ß glucan synthase: Anidulafungin; Caspofungin ; Micafungin
5. Others: Flucytosine is an antimetabolite; Griseofulvin binds to polymerized
microtubules and inhibits fungal mitosis; Fluocinonide; Gentian Violet
Antiviral drugs are a class of medication used specifically for treating Anti-influenza agents Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir
viral infections. Most of the antivirals now available are designed to help
deal with HIV, herpesvirus, which is best known for causing cold sores but Abacavir, Didanosine, Emtricitabine , Lamivudine, Stavudine,
NRTIs
actually covers a wide range of diseases, and the hepatitis B and C Zalcitabine, Zidovudine
viruses, which can cause liver cancer. Researchers are now worki ng to
extend the range of antivirals to other families of pathogens.
NtRTIs Tenofovir
The emergence of antivirals is the product of a greatly expanded
Anti-
knowledge of the genetic and molecular function of organisms, al lowing
retroviral
biomedical researchers to understand the structure and function of drugs NNRTIs Efavirenz, Delavirdine, Nevirapine
viruses, major advances in the techniques for finding new drugs, and the
intense pressure placed on the medical profession to deal with the human Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir,
immunodeficiency virus (HIV), the cause of the deadly acquired PIs Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir
immunodeficiency syndrome ( AIDS) epidemic. Though no one could
Fusion
sensibly claim that AIDS has been a benefit to humankind, it has certainly inhibitors
Enfuvirtide
done much to advance the state of antiviral technology.
Adefovir, Fomivirsen, Imiquimod, Inosine,Interferon,
Other antiviral agents
Podophyllotoxin, Ribavirin, Viramidine
10
The endocrine system consists of several glands, that secrete hormones directly
into the blood rather than into a duct system. To be classified as a hormone, a
chemical must be produced by an organ, be released (in small amo unts) into the
blood, and be transported by the blood to a distant organ to exe rt its specific
function. This definition holds for most ‘classical ’ hormones, but there are also
paracrine mechanisms (chemical communication between cells within a tissue or
organ), autocrine signals (a chemical that acts on the same cell), and intracrine
7.0. Endocrines and signals (a chemical that acts within the same cell). Three class es of hormone:
1. Amines: such as norepinephrine, epinephrine, and dopamine, are derived from
Immunosuppressants [2 Qs] single amino acids, in this case tyrosine. Thyroid hormones such as 3,5,3’-
triiodothyronine (T3) and 3,5,3’,5’-tetraiodothyronine (thyroxine, T4) make up a
subset of this class because they derive from the combination of two iodinated
tyrosine amino acid residues.
2. Peptides and Proteins: consist of three (in the case of thyrotropin-releasing
hormone) to more than 200 (in the case of follicle-stimulating hormone ) amino acid
residues and can have molecular weights as large as 30,000. All hormones
secreted by the pituitary gland are peptide hormones, as are leptin from
adipocytes , ghrelin from the stomach, and insulin from the pancreas.
3. Steroids: are derivatived from cholesterol and are subdivided into those with an
intact steroid nucleus (gonadal and adrenal steroids) and those with a broken
steroid nucleus (vitamin D). Steroid horomones include estrogen and
progesterone from the ovary, testosterone from the testes, and cortisol and
aldosterone from the adrenal gland.
Immunosuppressive drugs or immunosuppressants are drugs that are used Glucocorticoids: glucocorticoids are used to suppress various allergic,
in immunosuppressive therapy to inhibit or prevent activity of the immune inflammatory, and autoimmune disorders. They are also administered as
system. Clinically they are used to: posttransplantory immunosuppressants to prevent the acute transplant rejection
prevent the rejection of transplanted organs and tissues (e.g. bone marrow, and graft-versus-host disease. Nevertheless, they do not prevent an infection and
heart, kidney, liver) also inhibit later reparative processes. These drugs suppress the cell-mediated
treatment of autoimmune diseases or diseases that are most likely of immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3,
autoimmune origin (e.g. rheumatoid arthritis , myasthenia gravis, systemic lupus IL-4, IL-5, IL-6, IL-8 and TNF-?, the most important of which is the IL-2. Smaller
erythematosus, Crohn's disease, and ulcerative colitis). cytokine production reduces the T cell proliferation. Glucocorticoids also suppress
These drugs are not without side effects and risks. Because the majority of them the humoral immunity, causing B cells to express smaller amounts of IL-2 and of
act non-selectively, the immune system loses its ability to successfully resist IL-2 receptors . This diminishes both B cell clone expansion and antibody synthesis.
infections and spreading of malignant cells. There are also other side effects, Antiinflammatoryeffects
like hypertension, dyslipidemia, hyperglycemia, peptic ulcers , liver and kidney Glucocorticoids influence all types of inflammatory events, no matter what thei r
injury. The immunosuppressive drugs also interact with other medicines and cause. They induce the lipocortin-1 (annexin-1) synthesis, which then binds to cell
affect their metabolism and action. membranes preventing the phospholipase A2 from coming into contact with its
substrate arachidonic acid. This leads to diminished eicosanoid production. The
Immunosuppressive drugs can be classified into four groups and others: cyclooxygenase (both COX -1 and COX -2) expression is also suppressed,
glucocorticoids potentiating the effect.
cytostatics Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space,
antibodies where it binds to the leukocyte membrane receptors and inhibits various
drugs acting on immunophilins inflammatory events: epithelial adhesion , emigration, chemotaxis , phagocytosis ,
other drugs respiratory burst and the release of various inflammatory mediators (lysosomal
enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from
neutrophils , macrophages and mastocytes .
Antibodies: are used as a quick and potent immunosuppression method to prevent the acute
Cytostatics: inhibit cell division. And include the alkylating agents and antimetabolites. In rejection reaction.
immunotherapy, they are used in smaller doses than in the treatment of malignant diseases. 1. Polyclonal antibodies: Heterologous polyclonal antibodies are obtained from the serum of
They affect the proliferation of both T cells and B cells. animals (e.g. rabbit , horse) and injected with the patient's thymocytes or lymphocytes. The
1. Alkylating agents: are used in immunotherapy are nitrogen mustards antilymphocyte (ALG) and antithymocyte antigens (ATG) are being used. They are part of the
(cyclophosphamide), nitrosoureas, platinum compounds and others. Cyclophosphamide is steroid-resistant acute rejection reaction and grave aplastic anemia treatment. However, they are
probably the most potent immunosuppressive compound. In small doses, it is very efficient in primarily added to other immunosuppressives to diminish their dosage and toxicity. They also
the therapy of systemic lupus erythematosus, autoimmune hemolytic anemias, Wegener's allow transition to cyclosporine therapy. These agents inhibit T lymphocytes and cause their lysis,
which is both complement mediated cytolysis and cell-mediated opsonization followed by removal
granulomatosis and other immune diseases. High doses cause pancytopenia and
of reticuloendothelial cells from the circulation in the spleen and liver]]. In this way, polyclonal
hemorrhagic cystitis.
antibodies inhibit cell-mediated immune reactions, including graft rejection, delayed
2. Antimetabolites: interfere with the synthesis of nucleic acids. These include: hypersensitivity (i.e. tuberculin skin reaction), and the graft-versus-host disease (GVHD), but
folic acid analogues, such as methotrexate; purine analogues such as azathioprine and influence thymus-dependent antibody production. Because of a high immunogenicity of polyclonal
mercaptopurine; pyrimidine analogues and protein synthesis inhibitors. antibodies, almost all patients have an acute reaction to the treatment. It is characterized by fever,
(1) Methotrexate: is a folic acid analogue. It binds dihydrofolate reductase and prevents rigor episodes and even anaphylaxis. Later during the treatment, some patients develop serum
synthesis of tetrahydrofolate. It is used in the treatment of autoimmune diseases (for exampl e sickness or immune complex glomerulonephritis. Serum sickness arises 7-14 days after the
rheumatoid arthritis) and in transplantations. therapy has begun. The patient suffers from fever, joint pain and erythema that can be soothed
(2) Azathioprine and Mercaptopurine: are is extensively used to control transplant rejection with the use of steroids and analgesics. Urticaria (hives) can also be present. It is possible to
reactions. It is nonenzymatically cleaved to mercaptopurine, that acts as a purine analogue diminish their toxicity by using highly purified serum fractions and intravenous administration in
and an inhibitor of DNA synthesis. Mercaptopurine itself can also be administered directly. the combination with other immunosuppressants, for example calcineurin inhibitors, cytostatics
By preventing the clonal expansion of lymphocytes in the induction phase of the immune and cortisteroids. The most frequent combination is to simultaneously use antibodies and
response, it affects both the cell and the humoral immunity. cyclosporine. Patients gradually develop a strong immune response to these drugs, reducing or
(3) Cytotoxic antibiotics eliminating their effectiveness.
Among these, dactinomycin is the most important. It is used in kidney transplantations. Other 2. Monoclonal antibodies: are directed towards exactly defined antigens. Therefore, they cause
fewer side effects. Especially significant are the IL-2 receptor (CD25) and CD3 directed
cytotoxic antibiotics are anthracyclines, mitomycin C, bleomycin, mitramycin.
antibodies. They are used to prevent the rejection of transplant ed organs, but also to track
changes in the lymphocyte subpopulations. It is reasonable to expect similar new drugs in the
future.
11
3. T-cell receptor directed antibodies Drugs acting on immunophilins
Cyclosporin: Together with tacrolimus, cyclosporin is a calcineurin inhibitor. It has been in use since
OKT3 (R) is presently the only approved anti-CD3 antibody. It is a mouse anti-CD3 monoclonal
1983 and is one of the most widely used immunosuppressive drugs. It is a fungal peptide, composed
antibody of the IgG2a type that prevents T-cell activation and proliferation by binding the T-cell
of 11 amino acids. Cyclosporin is thought to bind to the cytosolic protein cyclophilin (an immunophilin)
receptor complex present on all differentiated T cells. As such, it is one of the most potent
of immunocompetent lymphocytes, especially T-lymphocytes. This complex of ciclosporin and
immunosuppressive substances and is clinically used to control the steroid and/or polyclonal
cyclophilin inhibits calcineurin, which under normal circumstances induces the transcription of
antibodies resistant acute rejection episodes. For acting more specifically than polyclonal
interleukin-2. The drug also inhibits lymphokine production and interleukin release, leading to a
antibodies, it is also used preventively in transplantations. Presently, the OKT3's action
reduced function of effector T-cells.
mechanism is not yet sufficiently understood. It is known that the molecule binds TCR/CD3, the T-
Cyclosporin is used in the treatment of acute rejection reactions, but has been increasingly
cell receptor complex. During the first few administrations, this binding non-specifically activates T
substituted with newer immunosuppressants, as it is nephrotoxic.
cells, leading to a serious syndrome 30 to 60 minutes later. It is characterized by fever, myalgia,
headache and artralgia. In some cases, it progresses to a life-threatening reaction of the Tacrolimus (Prograf(TM): is a bacterial product (Streptomyces tsukubaensis). It is a macrolide
cardiovascular system and the central nervous system needing a lengthy therapy. Past this lactone and acts by inhibiting calcineurin. The drug is used particularly in the liver and kidney
period, CD3 (R) blocks the TCR - antigen binding and causes conformation change or the transplantations, although in some clinics it is used in heart, lung and heart/lung transplants. It binds
removal of the entire TCR3/CD3 from the T-cell surface. This lowers the number of T cells, to an immunophilin, followed by the binding of the complex to calcineurin and the inhibition of its
perhaps by sensitising them for the uptake by the reticular epithelial cells. The cross-binding of phosphatase activity. In this way, it prevents the passage of G0 into G1 phase. Tacrolimus is more
CD3 molecules also activates an intracellular signal, causing the T cells' anergy or apoptosis, potent than cyclosporin and has less pronounced side effects.
unless they receive another signal through a costimulatory molecule. CD3 antibodies also shift the Sirolimus (Rapamune(Tm), Rapamicin): Sirolimus is a macrolide lactone, produced by the
balance from Th1 to Th2 cells. actinomycetes Streptomyces hygroscopicus. It is used to prevent rejection reactions. Although it is a
IL-2 receptor directed antibodies: is an important immune system regulator necessary for the structural analogue of tacrolimus, it acts somewhat differently and has different side effects. Contrary
clone expansion and survival of activated lymphocytes T. Its eff ects are mediated by the trimer to cyclosporine and tacrolimus that affect the first phase of the T lymphocyte activation, sirolimus
cell surface receptor IL-2a, consisting of the a, ß and ? chains. The IL-2a (CD25, T-cell activation affects the second one, namely the signal transduction and their clonal proliferation. It binds to the
antigen, TAC) is expressed only by the already activated T lymphocytes. Therefore, it is of special same receptor (immunophilin) as tacrolimus, however the produced complex does not inhibit
significance to the selective immunosuppressive treatment and the research has been focused on calcineurin, but another protein. Therefore, sirolimus acts synergistically with cyclosporine and, in
the development of effective and safe anti-IL-2 antibodies. By the use of the recombinant gene combination with other immunosuppressants, has few side effects. Indirectly it inhibits several T
technology, the mouse anti-Tac antibodies have been modified leading to the presentation of two lympohocyte kinases and phosphatases, preventing the transmission of signal into their activity and
himeric mouse/human anti-Tac antibodies in the year 1998: basiliximab (Simulect (R)) and the transition of the cell cycle from G1 to S phase. Similarly, it prevents the B cell differentiation to the
plasma cells, which lowers the quantity of IgM, IgG and IgA antibodies produced. It acts
daclizumab (Zenapax (R)). These drugs act by binding the IL-2a receptor's a chain, preventing
immunoregulatory.
the IL-2 induced clonal expansion of activated lymphocytes and shortening their survival. They
are used in the profilaxis of the acute organ rejection after the bilateral kidney transplantation,
Other drugs
Interferons: IFN-ß suppresses the production of Th1 cytokines and the activation of
monocytes. It is used to slow down the progression of multiple sclerosis. IFN-? is able to trigger
lymphocytic apoptosis.
Opioids: Prolonged use of opioids may cause immunosuppression by inhibiting the migration
of leukocytes.
TNF binding proteins: A TNF -a (tumor necrosis factor alpha) binding protein is a monoclonal
antibody or a circulating receptor such as infliximab (Remicade®), etanercept (Enbrel ®), or 8.0. Analgesics [5 Qs]
adalimumab (Humira®) that binds to TNF - a and prevent it from inducing the synthesis of IL- 1
and IL- 6 and the adhesion of lymphocyte activating molecules. They are used in the treatment
of rheumatoid arthritis, ankylosing spondylitis, Crohn's disease and psoriasis.
8.1. Opioids
TNF or the effects of TNF are also suppressed by various natural compounds, including
curcumin (an ingredient in turmeric) and catechins (in green tea). 8.2. Non-opioids, NSAIDs
These drugs may raise the risk of contracting tuberculosis or inducing a latent infection to
become active. Infliximab and adalimumab have label warnings stating that patients should be
evaluated for latent TB infection and treatment should be initiated prior to starting therapy with
them.
Mycophenolate: Mycophenolic acid acts as a non-competitive, selective and reversible
inhibitor of inosine monophosphate dehydrogenase (IMPDH), which is a key enzyme in the de
novo guanosine nucleotide synthesis. In contrast to other human cell types, ly mphocytes B and
T are very dependent on this process.
[edit] Small biological agents
FTY720 is a new synthetic immunosuppressant, currently in phase 3 of clinical trials. It
increases the expression or changes the function of certain adhesion molecules ( a4/ß7
integrin) in lymphocytes, so they accumulate in the lymphatic tissue (lymphatic nodes) and their
number in the circulation is diminished. In this respect, it dif fers from all other known
immunosuppressants.
12
Analgesics
Opioids : Buprenorphine, Butorphanol , Codeine,
Dextropropoxyphene, Dihydrocodeine, Fentanyl , 9.0. Antihistamines and
Diamorphine (Heroin), Hydrocodone,
Hydromorphone, Ketobemidone, Morphine,
Autocoids [2 Qs]
Nalbuphine, Oxycodone, Oxymorphone,
Pentazocine, Pethidine (Meperidine), Tramadol
Salicylic acid Aspirin (Acetylsalicylic Acid), Diflunisal,
and Ethenzamide
derivatives:
Pyrazolones: Aminophenazone, Metamizole, Phenazone
Anilides: Paracetamol (acetaminophen), Phenacetin
Others: Ziconotide, Tetrahydrocannabinol
Antihistamines (H1 receptor antagonists): Widely used for hay fever, mild
allergic reactions and additive with other CNS depressants
Four common: Dipheniramine (Benedryl ); Chlorphenhydramine (ClorTrimeton);
Promethazine (Phenegan); Loratidine (Claritin)
Pharmacologic effects: H1 blocking effects include: Capillary permeability is
blocked producing reduced edema; Blocks dilation of vascular smooth muscle;
Blocks some bronchoconstriction; Suppresses the itching and pain
The End
&
Other effects: CNS depression (Sominex, Nytol); Anticholinergic ; Antiemetic
(Dramamine, Bonine);
Adverse reactions: Undesirable CNS depression. Sedative effect cancelled out
when combined with decongestant (adrenergic agonist). CNS stimul ation can
occur in a few cases. More common in children, elderly with larger doses.
Newer nonsedating H1 blockers (Clariton) produce less sedation. Xerostomia
Toxicity: More common due to easy accessibility in OTC preparations
Death can result.
Uses: Control seasonal hay fever; Relieve itching, edema and erythema
Some topical anesthetic effect; To prevent and treat motion sickness
Preop sedation and antiemetic effects; OTC sleep aids.
Good Luck
13
The conjugation of glucuronic acid
to a drug by the liver is an example
of a:
A. Cytochrome P450 reaction
B. Transformation reaction
C. Phase I activation reaction
D. Phase II inactivation reaction
14
15
16