Syrup Presentation

Each 5 ml contains :
Ambroxol Hydrochloride IP        7.5 mg

Ambroxol is indicated as "secretolytic therapy" in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe freely and deeply. When administered orally onset of action occurs after about 30 minutes. The breakdown of acid mucopolysaccharide fibers makes the sputum thinner and less viscous and therefore more easily removed by coughing. Although sputum volume eventually decreases, its viscosity remains low for as long as treatment is maintained.

Indications

• Acute respiratory tract diseases with impaired formation of secretions, particularly in acute exacerbations of chronic bronchitis, asthmatic bronchitis, bronchial asthma and bronchiectasis.

The following additional indications are also present in some local markets:

• Ambroxol hydrochloride treatment of respiratory disorders associated with viscid mucus such as: Pneumonia, otitis media, sinusitis, nasopharyngitis, secretolytic therapy for relieving cough in acute and chronic disorders of the respiratory tract associated with pathologically thickened mucus and impaired mucus transport.

Pharmacology

Mechanism of Action

Ambroxol is the active metabolite of bromhexine. Ambroxol causes an increase in secretion in the respiratory tract. It promotes surfactant production and stimulates ciliary activity. These effects assist the flow of mucus and its removal (mucociliary clearance).
An improvement in mucociliary clearance was demonstrated in clinical pharmacological studies. The increase in secretion and mucociliary clearance facilitate expectoration and reduce the cough.

Pharmacokinetics

Absorption: Ambroxol is rapidly absorbed (70-80%) after oral administration. The time to reach peak plasma concentration is approximately 2 hours. The absolute bio-availability of oral domperidone is low (approximately 15%) due to first-pass hepatic and intestinal metabolism.
Distribution: The distribution half-life of ambroxol is around 1.3 hours.
Metabolism: Metabolite is dibromoanthranilic acid (activity unspecified).
Excretion: Excretion is 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 is biphasic, with an alpha half-life of 1.3 hours and a beta half-life of 8.8 hours.

Drug Interactions

Antitussives: Concomitant administration of antitussives may impair the expectoration of liquefied bronchial mucus due to inhibition of the cough reflex and cause congestion of secretions.
Antibiotics: After using ambroxol the concentrations of the antibiotics amoxicillin, cefuroxime and erythromycin in bronchial secretions and sputum are increased.
Pregnancy and Lactation: Preclinical studies as well as extensive clinical experience after the 28th week have shown no evidence of ill-effects during pregnancy. Nonetheless, the usual precautions regarding the use of drugs during pregnancy, especially during the first trimester, should be observed. The drug enters breast milk, but is not likely to affect the infant when therapeutic doses are used.

Side Effects

• Mild upper gastro-intestinal side effects (primarily pyrosis, dyspepsia, and occasionally nausea, vomiting) have been reported.
• Allergic reactions have occurred rarely, primarily skin rashes.

Contraindications

• Should not be used in patients known to be hypersensitive to ambroxol or other components of the formulation.

Renal Impairment: In severe renal impairment ambroxol must only be used under medical supervision. The secretolytic effect of ambroxol is supported by adequate fluid intake.
Hepatic Impairment: In severe hepatic impairment ambroxol must only be used under medical supervision.

Precautions

• Syrup contains sucrose and sorbitol, oral drops contain sorbitol and modified-release capsules contain sucrose. Patients with fructose intolerance should not take this medicine. A mild laxative effect may also occur.
• Syrup contains methyl and propyl hydroxybenzoate (parabens) which may cause allergic reactions (possibly delayed).
• Syrup and oral drops contain Ponceu 4R (E 124) which may cause allergic reactions.

Over Dosage

Symptoms and Signs: Manifestations of poisoning are so far unknown in humans.
Treatment: Symptomatic treatment is recommended.