Axcel Nasatab

Chlorpheniramine maleate, paracetamol, pseudoephedrine hydrochloride.

Each tablet contains: Paracetamol 500 mg.
Chlorpheniramine Maleate 4mg.
Pseudoephedrine HCl 60mg.

Pharmacology: Mechanism of Action: Product contains a well-established analgesic - antipyretic - paracetamol; an antihistamine - chlorpheniramine maleate, and a decongestant - pseudoephedrine. This combination provides fast, effective symptomatic relief of headache, fever and pain, sinus and nasal congestion due to sinusitis or common cold.
Chlorpheniramine maleate is an alkylamine derivative with antihistamine and anticholinergic effects. It is one of the most potent of the antihistamines and is not so prone to producing drowsiness. It acts by competing with histamines for H(1)-receptor sites in the effector cells.
Pseudoephedrine is a stereoisomer of ephedrine and has a similar action, but with less CNS stimulation. It is a direct and indirect-acting sympathomimetic agent that provides vasoconstriction similar to that of ephedrine.
Pharmacokinetics: Chlorpheniramine Maleate is absorbed relatively slowly from the gastrointestinal tract, peak plasma concentrations occurring about 2.5 to 6 hours after administration by mouth. It appears to undergo considerable first-pass metabolism. About 70% of chlorpheniramine in the circulation is bound to plasma proteins. There is a wide inter-individual variation in the pharmacokinetics of chlorpheniramine: half-life ranging from 2 to 43 hours have been reported. Chlorpheniramine is widely distributed in the body, including passage into the CNS. It is extensively metabolised to desmethyl and didesmethylchlorpheniramine. Excretion is dependent on urinary pH and flow rate. A duration of action of 4 to 6 hours has been reported. Paracetamol is readily absorbed from the gastrointestinal tract with peak plasma concentrations occurring about 10 - 60 minutes after oral administration. It is distributed into most body tissues, crosses the placenta and is present in breast milk. Plasma - protein binding is negligible at usual therapeutic concentrations but increases with increasing concentrations. Paracetamol is metabolized predominantly in the liver and excreted in the urine mainly as the glucuronide and sulphate conjugates. Less than 5% is excreted as unchanged paracetamol. Pseudoephedrine is absorbed from the gastrointestinal tract. It is resistant to metabolism by monoamine oxidase and is largely excreted unchanged in the urine together with small amounts of its hepatic metabolite. It has a half-life of several hours. Small amount are excreted in the breast milk.

Symptomatic relief of headache, fever and pain, sinus and nasal congestion associated with sinusitis or common cold.

For adult only: 1 tablet to be taken, 3 or 4 times daily.

Symptoms of overdosage may vary from CNS depression to stimulation. Other signs and symptoms may include dizziness, tinnitus, ataxia, blurred vision, dry mouth, flushing and gastrointestinal symptoms. Acute hypertension or cardiovascular collapse with accompanying hypotension may occur. Treatment is symptomatic and supportive. The stomach should be emptied by aspiration and lavage. Convulsion may be controlled with diazepam given intravenously. Symptoms that may occur within 24 hours of overdosage of Paracetamol include nausea, vomiting, lethargy and sweating. Abdominal pain may be the first indication of liver damage. Hepatic failure, encephalopathy, coma and death may result. Toxicity following overdosage with paracetamol has been attributed to the metabolite, N-acetyl-p-benzoquinoneimine by mixed function oxidase enzyme in the liver and kidney. Acetylcysteine or methionine, are used as antidotes in paracetamol overdosage.

Contraindicated in patients hypersensitive to any of the active ingredients, or those with severe hypertension or severe coronary artery disease, and those taking MAO inhibitors, or within 14 days of taking them.

This preparation contains paracetamol. Do not take any other paracetamol containing medicines at the same time.

Use with caution in patients with narrow angle glaucoma, history of bronchial asthma, hyperthyroidism, cardiovascular diseases, prostatic hypertrophy, hypertension or diabetes mellitus. Preparation may cause drowsiness and dulling of mental alertness. Patients should be warned against driving and operating machinery. Preparation may also enhance the sedative effects of CNS depressants and alcohol. It should be given with care to patients with impaired kidney or liver function or those taking other drugs that affect the liver.
Use in Pregnancy & Lactation: There has been no specific data to establish the safe use of this product in pregnancy and lactation. Therefore, the product should be used only if the potential benefit justifies the potential risk to the fetus.

There has been no specific data to establish the safe use of this product in pregnancy and lactation. Therefore, the product should be used only if the potential benefit justifies the potential risk to the fetus.

Preparation contains an antihistamine, which may cause side-effects like sedation, lassitude, dizziness, hypotension, muscular weakness, incoordination, gastrointestinal disturbances, headache, blurred vision, tinnitus, elation or depression, irritability, anorexia, difficulty in micturition, dryness of the mouth, tightness of the chest, heaviness and weakness of the hands. Side effects due to paracetamol at therapeutic doses are rare. Epigastric distress or skin rash may occasionally occur. As for sympathomimetic agent, the side effects include fear, anxiety, restlessness, tremor, insomnia, confusion, irritability and psychotic states.

The absorption of Paracetamol may be accelerated by metoclopramide. The excretion may be affected and plasma concentrations altered when administered with probenecid. Chlorpheniramine maleate may enhance the sedative effects of CNS depressants including alcohol, barbiturates, hypnotics, opioid analgesics and anxiolytic sedatives. MAOIs may enhance the antimuscarinic effects of antihistamines. When sympathomimetics are given to patients receiving MAOIs, hypertensive reactions, including hypertensive crises may occur. The antihypertensive effects of methyldopa, mecamylamine, reserpine and veratrum alkaloids may be reduced by sympathomimetics. Beta-adrenergic-blocking agents may also interact with sympathomimetics. Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis. Antacids increase the rate of pseudoephedrine absorption; kaolin decreases it.

Keep container well closed. Store below 30°C. Protect from light.

Cough & Cold Preparations

R01BA52 - pseudoephedrine, combinations ; Belongs to the class of systemic sympathomimetic preparations used as nasal decongestants.

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