Ambroxol

Drug class
Pharmacokinetics

Mechanisms of
Action

Clinical Uses

Indication

Contraindication

Interaction
Adverse Effect

Expectorants, active mucolytic agent

OOA: 30 minutes
Absorption:
Ambroxol hydrochloride is rapidly absorbed (70-80%) after oral
administration. The time to reach peak plasma concentration is
approximately 2 hours.
Distribution:
The distribution half-life of ambroxol hydrochloride is around 1.3 hours.
Metabolism:
Metabolite is dibromoanthranilic acid (activity unspecified).
Excretion:
Primarily via the kidneys. Renal clearance (rate) is approximately 53
ml/minute; approximately 5-6% of a dose is excreted unchanged in the
urine. The elimination half-life of ambroxol hydrochloride is biphasic, with
an alpha half-life of 1.3 hours and a beta half-life of 8.8 hours.
Ambroxol is an active N-desmethyl metabolite of
the mucolytic, bromhexine. Its mucolytic activity by which it facilitates
breakdown of acid mucopolysaccharide fibres in the mucous making it
thinner and less viscous and, therefore, easy for expectoration; it
stimulates the ciliary activity thereby improving mucokinesis (transport of
mucous); it stimulates production of pulmonary surfactant, a substance
found to play a major role in the lung host defense mechanism, thereby
further protecting against lung inflammation and infection; also exhibits
anti-inflammatory and antioxidant activity. When administered orally,
onset of action occurs after about 30 minutes.
tracheobronchitis, emphysema with bronchitis pneumoconiosis, chronic
inflammatory pulmonary conditions, bronchiectasis, bronchitis with
bronchospasm asthma
Acute and chronic diseases of respiratory tract, with symptoms of thick
mucus retention. Bronchitis, bronchial asthma, bronchiecstasia and
silicosis.
Hypersensitivity to any of the component of the product or its parent
compounds. It is also contraindicated in patients with completely impaired
renal function and with gastric ulceration.
Nausea, headache and gastrointestinal disorders have been observed
rarely. Other toxic effects include skin irritation, eye irritation and
respiratory tract irritation. Ingestion of large doses may cause
gastrointestinal tract irritation with decreased motility or constipation,
ulceration or bleeding from the stomach or duodenum, and peritonitis. It
may affect behaviour/CNS (tremor, convulsions, ataxia and somnolence),
respiration (dyspnoea, respiratory stimulation), the liver, blood (changes
in white blood cell count) and the urinary system. Occasional
gastrointestinal side effects may occur but these are normally mild.

Dosage
Adults: daily dose of 30 mg (one Ambroxol tablet )to 120 mg (4 Ambroxol
tablets) taken in 2 to 3 divided doses
Children up to 2 years: half a teaspoonful Ambroxol syrup twice daily

Children 2 - 5 years: half a teaspoonful Ambroxol syrup 3 times daily

Children over 5 years: One teaspoonful Ambroxol syrup 2-3 times daily.
Preparations
available
Pregnancy category

it is advisable to avoid use during the first trimester of pregnancy.

Pseudoephedrine
Drug class

Description

Vasoconstrictor Agents
Adrenergic Agents
Sympathomimetics
Central Nervous System Agents
Bronchodilator Agents
Nasal Decongestants
An alpha- and beta-adrenergic agonist that may also enhance release of
norepinephrine. It has been used in the treatment of several disorders
including asthma, heart failure, rhinitis, and urinary incontinence, and for
its central nervous system stimulatory effects in the treatment of
narcolepsy and depression

Structure

Pharmacodynamics

Pharmacokinetic

Mechanisms of
Action

Indication

Toxicity

a sympathomimetic agent, structurally similar to ephedrine, used to

relieve nasal and sinus congestion and reduce air-travel-related otalgia in
adults. The salts pseudoephedrine hydrochloride and pseudoephedrine
sulfate are found in many over-the-counter preparations either as singleingredient preparations, or more commonly in combination with
antihistamines and/or paracetamol/ibuprofen. pseudoephedrine only
serves to relieve nasal congestion commonly associated with colds or
allergies.
Absorption: almost completely absorbed from the GI tract
Metabolism: hepatic
Half life 9-16 hours
acts directly on both alpha- and beta-adrenergic receptors. Through direct
action on alpha-adrenergic receptors in the mucosa of the respiratory
tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine
relaxes bronchial smooth muscle by stimulating beta2-adrenergic
receptors. pseudoephedrine releasing norepinephrine from its storage
sites, an indirect effect.
nasal congestion, sinus congestion, Eustachian tube congestion, and
vasomotor rhinitis, and as an adjunct to other agents in the optimum
treatment of allergic rhinitis, croup, sinusitis, otitis media, and
tracheobronchitis. Also used as first-line therapy of priapism
nervousness, restlessness, and insomnia. Rare adverse reactions include
difficult/painful urination, dizziness/lightheadedness, heart palpitations,

Contraindication

Adverse Effect

Interaction

Preparations
available
Pregnancy category

IBUPROFEN
Drug class

Description

headache, increased sweating, nausea/vomiting, trembling, troubled

breathing, unusual paleness, and weakness
contraindicated for use in patients:
with known hypersensitivity or idiosyncratic reaction to
pseudoephedrine (or any of the other ingredients in the product);
with severe hypertension or coronary artery disease;
taking monoamine oxidase inhibitors (MAOIs) or who have taken
MAOIs within the previous 14 days.
cardiovascular stimulation elevated blood pressure, tachycardia or
arrhythmias
central nervous system (CNS) stimulation restlessness, insomnia,
anxiety, tremors and (rarely) hallucinations
skin rashes and urinary retention
Antidepressant medication eg tricyclic antidepressants and
monoamine oxidase inhibitors (MAOIs) may cause a serious increase
in blood pressure or hypertensive crisis
other sympathomimetic agents, such as decongestants, appetite
suppressants and amphetamine-like psychostimulants may cause an
increase in blood pressure and additive effects
methyldopa and -blockers may cause an increase in blood pressure
urinary acidifiers enhance elimination of pseudoephedrine
urinary alkalinisers decrease elimination of pseudoephedrine
Oral: 30, 60 mg tablets; 60 mg capsules; 15, 30 mg/5 mL syrups; 7.5
mg/0.8 mL drops
Oral extended-release: 120, 240 mg tablets, capsules
Category B2:
should be used in pregnancy only if the potential benefits to the patient
are weighed against the possible risk to the foetus.

Anti-inflammatory Agents
Cyclooxygenase Inhibitors
Analgesics
Analgesics, Non-Narcotic
Antipyretics
Nonsteroidal Anti-inflammatory Agents (NSAIAs)
a propionic acid derivative, is a prototypical nonsteroidal antiinflammatory drugs (NSAID) with analgesic and antipyretic properties.

Structure

Pharmacodynamics

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID), with analgesic

and antipyretic properties. Ibuprofen has pharmacologic actions similar to
those of other prototypical NSAIAs, which are thought to act through
inhibition of prostaglandin synthesis.

Pharmacokinetic

Mechanisms of
Action

Indication

Toxicity

Contraindication

Adverse Effect

Interaction
Preparations
available

Dosage

~ 80% absorbed from GI tract

Time to reach peak plasma concentration = 47 minutes (suspension)
(conventional tablets)

Protein binding

90-99% to whole human plasma and site II of purified albumin, bindin

linear at concentrations exceeding 20 mcg/ml.

Route of
elimination

rapidly metabolized and eliminated in the urine.

Half life

2-4 hours

Absorption

Ibuprofen is a non-selective inhibitor of cyclooxygenase, an enzyme

invovled in prostaglandin synthesis via the arachidonic acid pathway.
inhibition cylooxygenase-2 (COX-2) which decreases the synthesis of
prostaglandins involved in mediating inflammation, pain, fever and
swelling.
Antipyretic effects may be due to action on the hypothalamus,
resulting in an increased peripheral blood flow, vasodilation, and
subsequent heat dissipation.
rheumatoid arthritis, juvenile rheumatoid arthritis and osteoarthritis. May
be used to treat mild to moderate pain and for the management of
dysmenorrhea. May be used to reduce fever. Has been used for treating
ankylosing spondylitis, gout and psoriatic arthritis. May reduce pain, fever
and inflammation of pericarditis. May be used IV with opiates to relieve
moderate to severe pain. Ibuprofen lysine may be used IV to treat patent
ductus arteriosus (PDA) in premature neonates.
Most common symptoms of overdose are abdominal pain, nausea,
vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and
insomnia. Other symptoms include headache, loss of consciousness,
tinnitus, CNS depression, convulsions and seizures. May rarely cause
metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure,
dyspnea, respiratory depression, coma, acute renal failure, and apnea
(primarily in very young pediatric patients).
Patient with nasal polyps, angioedema, and bronchospastic reactivity to
aspires
systemic lupus erythematosus
May cause peripheral edema and fluid retention. Use caution in patients
with congestive heart failure or severe uncontrolled hypertension. May
cause dyspepsia, heartburn, nausea, vomiting, anorexia, diarrhea,
constipation, stomatitis, flatulence, bloating, epigastric pain, and
abdominal pain. Peptic ulcer and GI bleeding have been reported. May
also cause dizziness, headache and nervousness. Acute renal failure
accompanied by acute tubular necrosis has been reported.
with aspirin may decrease the total anti-inflammatory effect
Capsul 200 mg,
IV 100mg/ml,
Suspension 100mg/5 ml, 40 mg/ml
Tablet 200 mg, 400 mg, 600 mg, 800 mg,
Chewable tablet 50mg, 100 mg
analgesic dose: oral dose (< 2400 mg/d),
topical cream into fascia and muscle
postsurgical dental pain: liquid gel preparation 400 mg