Indications:- Cough decongestant formula
Dextromethorphan and Chlorpheniramine Suspension
Dextromethorphan & Chlorpheniramine
SUSPENSION PRESENTATION:
Each 5 ml contains:
Dextromethorphan Hydrobromide IP 10mg
Chlorpheniramine Maleate IP 4mg
This combination medicine of Dextromethorphan hydrobromide and Chlorpheniramine maleate is used to treat various symptoms of sneezing, runny nose, and cough caused by the common cold. Dextromethorphan acts as a cough suppressant affecting the signals in the brain that trigger cough reflex while Chlorpheniramineis a histamine H1 antagonist.
Dextromethorphan Hydrobromide-
- Cough (not caused by smoking, asthma, or emphysema)
Chlorpheniramine Maleate-
- Allergy
- Hay fever
- Common cold
- Asthma
- Rhinitis
Dextromethorphan Hydrobromide-
Dextromethorphan is a dextrorotatory isomer of levomethorphan, a semisynthetic morphine derivative that binds to and acts a a potent blocker of N-methyl-d-aspartate (NMDA) glutamatergic receptor, and an agonist to the opioid sigma 1 and sigma 2 receptors, also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.
Chlorpheniramine Maleate-
Chlorpheniramine competes with the histamine H1 receptor sites on smooth muscle of the bronchi, GI tract, uterus, and large blood vessels; they bind to cellular receptors, preventing access of histamine, thereby suppressing histamine-induced allergic symptoms. They don’t directly alter histamine or its release. This therefore blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Dextromethorphan Hydrobromide-
After being rapidly absorbed from the gastrointestinal tract it is converted into the active metabolite dextrorphan in the liver by the cytochrome P450 enzyme CYP2D6 and exerts its antitussive effect in 15-30 minutes after oral administration. The duration of action is approximately 3-6 hours with conventional dosage forms. Dextromethorphan and its metabolites are excreted via the kidney. Depending on the metabolism phenotype up to 11% may be excreted unchanged or up to 100% as demethylated conjugated morphinan compounds. In the first 24 hours after dosing, less than 0.1% is eliminated in the feces.
Chlorpheniramine Maleate-
Chlorpheniramine is rapidly and well absorbed from the GI tract. Food in the stomach delays absorption but doesn’t affect its bioavailability. It is distributed extensively into the body; the drug is about 72% protein-bound. And is largely metabolised in GI mucosal cells and liver (first-pass effect) via Cytochrome P450 (CYP450) enzymes. The elimination half-life of chlorpheniramine varies between 13.9 and 43.4 hours in adults; drugs and metabolites are excreted in urine.
- dizziness
- feeling nervous, restless and excited
- constipation
- drowsiness
- dry mouth, nose, or throat
- blurred vision
- nausea
- abdominal discomfort
This combination is contraindicated in individuals:
- Having a prior severe hypersensitivity reaction or allergic to dextromethorphan or history of hypersensitivity to chlorpheniramine maleate or antihistamines or any other ingredients of the preparations.
- With, or at risk of developing, respiratory failure (e.g those with chronic obstructive airways disease or pneumonia, or during an asthma attack or an exacerbation of asthma).
- Who are being treated or have been treated with monoamine oxidase inhibitors (MAOIs) within the past 14 days. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine. Anticholinergic properties of chlorpheniramine are intensified by MAOIs.
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