- Cough and cold, Allergic rhinitis
Mechanism of Action
Guaiphenesin a plant product which enhances the bronchial secretion and reduce its viscosity, allowing ciliary movement to carry the loosened secretions upward toward the pharynx. The increased flow of less viscous secretions promotes ciliary action and changes a dry, unproductive cough to one that is more productive and less frequent.
Phenylephrine is a sympathomimetic amine that acts predominantly on α-adrenergic receptors. It is mainly used to treat nasal congestion, .It causes vasoconstriction in the mucosa of the respiratory tract leads to decreased oedema and increased drainage of sinus cavities, hence providing relief from stuffy nose and sinus pressure.
Ambroxol hydrochloride comes in the category of mucokinetic, they are the drugs that reduce the cough viscosity and facilitates its removal by coughing.Menthol provides relief with cooling sensation in pain, sore throat. They are useful in cough due to irritation of the pharyngeal mucosa above the epiglottis, and act by increasing the flow of saliva, the best natural demulcent, which produces protective and soothing effect.
- Should be used in caution with patients with gastric ulcer.
- Use cautiously with pregnancy, lactation, and persistent coughs.
- Use drug with caution in patients with cirrhosis or other liver disease.
- It should not be used in patients hypersensitive to any active ingredient.
- It should not be used in patients severe hypertension, ventricular tachycardia,
Warning & Precautions
- Monitor patient for dizziness and excessive drowsiness. If noted, hold therapy and notify health care provider.
- Use with caution in elderly patients, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Monoamine oxidase inhibitors may increase the anti cholinergic effects of Chlorpheniramine.
Allergic reactions such as skin rash, nettle-rash, and angioneurotic oedema are possible. Under the prolonged administration in large doses pain in epigastrial area, nausea, vomiting can appear
Ambroxol Hydrochloride should be given cautiously to patients with gastric and duodenal ulceration or convulsive disorders. Patients with hepatic and renal insufficiency should take it with caution
- Drowsiness due to Chlorpheniramine.
Overdosage may induce ventricular extrasystoles and short paroxysms of ventricular tachycardia, a sensation of fullness in the head and tingling of the extremities.
Should an excessive elevation of blood pressure occur, it may be immediately relieved by an α– adrenergic blocking agent (e.g., phentolamine).
Pharmacodynamics:The combination is well established in patients with cold and cough.
Ambroxol:Absorption: Ambroxol 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 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.
Guaiphenesin:Absorption: Guaiphenesin is well absorbed from the gastro-intestinal tract following oral administration, although limited information regarding its pharmacokinetics is available. After the administration of 600 mg Guaiphenesin to healthy adult volunteers, the Cmax was approximately 1.4ug/ml, with tmax occurring approximately 15 minutes after drug administration.
Distribution: No information is available on the distribution of Guaiphenesin in humans.
Metabolism and elimination: Guaiphenesin appears to undergo both oxidation and demethylation. Following an oral dose of 600 mg guaifenesin to 3 healthy male volunteers, the t½ was approximately 1 hour and the drug was not detectable in the blood after approximately 8 hours. Pharmacokinetics in Renal/Hepatic Impairment: There have been no specific studies of Guaiphenesin in subjects with renal or hepatic impairment. Caution is therefore recommended when administering this product to subjects with severe renal or hepatic impairment.
Chlorpheniramine Maleate:Absorption and distribution: It is absorbed relatively slowly from the gastrointestinal tract, with peak plasma concentrations occurring about 2.5 to 6 hours after oral administration. Chlorpheniramine appears to undergo considerable first-pass metabolism. Bioavailability is low, values of 25 to 50% having been reported. About 70% of chlorpheniramine in the circulation is bound to plasma proteins. There is wide inter-individual variation in the pharmacokinetics of chlorpheniramine; half-life values ranging from 2 to 43 hours have been reported. Chlorpheniramine is widely distributed in the body and enters the CNS.
Metabolism: Chlorpheniramine maleate is metabolised extensively. Metabolites include desmethyl- and didesmethylchlorpheniramine. Unchanged drug and metabolites are excreted primarily in the urine; excretion is dependent on urinary pH and flow rate. Only trace amounts have been found in the faeces.
Excretion: A duration of action of 4 to 6 hours has been reported; this is shorter than may be predicted from pharmacokinetic parameters.
Phenyleprine Maleate:Oral absorption of Phenylephrine (HCl) is found to be 73% ±2. Volume of distribution is found to be 340 litre . Presystemic metabolism is noted to be 60% and metabolism is reported Hepatic. Renal Excretion accounts for < 20 % and plasma half life is 2 - 3 hr.
The preparation should not be used after the expiry date.
Keep it out of reach of children