Chlorphenamine Maleate Tablet: Each tablet contains 4 mg Chlorphenamine Maleate.
Chlorphenamine Maleate Syrup: Each teaspoonful (5 mL) contains Chlorphenamine Maleate 2 mg.
Pharmacology: Pharmacodynamics: Chlorphenamine antagonises competitively the effects of histamine on H1-receptors and also has weak antimuscarinic and moderate antiserotonin and local anaesthetic actions. It penetrates the brain and causes stimulation or sedation in animals.
Pharmacokinetics: Chlorphenamine maleate is almost completely absorbed after administration by mouth, peak plasma concentrations occurring at about 2.5 to 6 hours. The drug is widely distributed including passage into the CNS, with a volume of distribution of between 1 and 10L/KG. About 70% of chlorphenamine in the circulation is protein-bound. Chlorpheniramine undergoes some first pass metabolism and enterohepatic recycling. Chlorphenamine is extensively metabolised, principally to inactive desmethylated metabolites which are excreted primarily in the urine, together with about 35% unchanged drug. Only trace amounts are excreted in the faeces. The mean elimination half life has been reported to be about 30 hours, with mean values ranging from 2 to 43 hours.
The antihistaminic action of Chlorphenamine Maleate provides effective prophylaxis and treatment for allergic disorders such as hay fever, urticaria, angioneurotic edema, vasomotor rhinitis, bronchial asthma, contact dermatoses, food and drug allergy, insect bites, serum sickness, transfusion reactions and anaphylactic shock. Chlorphenamine Maleate is useful as well in the prophylaxis and control of motion sickness and in the management of coughs of allergic origin.
Chlorphenamine Maleate 4 mg is convenient for case where symptoms are not severe enough to require the parenteral route of administration and for maintenance requirement. Adult 4 mg every 4-6 hours as needed (Maximum 24 mg daily).
Chlorphenamine Maleate Syrup is readily accepted by children and adults who prefer liquid medication. Ephedrine sulfate is an effective decongestant and bronchial relaxant-counter acts many histamine effects.
Adult 4 mg every 4-6 hours as needed (Maximum 24 mg daily).
Children 6-12 years: 2 mg every 6-8 hours a day as needed not to exceed 12 mg a day.
Or as prescribed by physician.
Overdosage with chlorphenamine is associated with antimuscarinic, extrapyramidal, gastrointestinal and CNS effects. In infants and children, CNS stimulation predominates over CNS depression, causing ataxia, excitement, tremors, psychosis, hallucinations and convulsions. Hyperpyrexia may also occur. Other symptoms of overdosage in children include dilated pupils, dry mouth, facial flushing. Deepening coma and cardiorespiratory collapse may follow, and even death. In adults CNS depression is more common with drowsiness, coma and convulsions, progressing to respiratory failure or possibly cardiovascular collapse including arrhythmias.
In severe overdosage the stomach should be emptied. Activated charcoal has been given as have saline laxatives. Convulsions may be controlled with diazepam or phenytoin, although it has been suggested that CNS depressants should be avoided. Other treatment is supportive and symptomatic and may include artificial respiration, external cooling for hyperpyrexia and intravenous fluids. Vasopressors such as noradrenaline or phenylephrine may be used to counteract hypotension. Forced diuresis, peritoneal dialysis or haemodialysis appear to be of limited benefit.
The anticholinergic properties of chlorphenamine are intensified by monoamine oxidase inhibitors (MAOIs). The tablets are therefore contraindicated in patients who have been treated with MAOIs within the last fourteen days.
This medicine should be given with caution to patients with epilepsy, severe cardiovascular disorders, liver disorders, glaucoma, urinary retention, prostatic enlargement, pyloroduodenal obstruction, asthma, bronchitis, bronchiectasis, thyrotoxicosis and severe hypertension.
Special care should be taken when using chlorphenamine maleate in children and the elderly as they are more prone to developing neurological anticholinergic effects.
Warning: May cause drowsiness. If affected do not drive or operate machinery. Avoid alcoholic drink.
If symptoms do not go away within 5 days talk to a pharmacist or doctor.
Although most antihistamines should be avoided by patients with porphyria, chlorpheniramine maleate has been used and is thought to be safe.
Chlorphenamine Maleate shares with all antihistamine preparations side effects which are rarely serious and disappear with continued therapy. Drowsiness and hypnosis may occur. The cardiovascular, gastrointestinal and other systems may also be affected. Allergic reactions to antihistamines have been known to occur with topical application. Allergy to Chlorphenamine maleate is contraindication to its use. CNS stimulation instead of depression may occur with Chlorphenamine maleate.
This medicine may enhance the sedative effects of alcohol, hypnotics, anxiolytics, sedatives, opioid analgesics and neuroleptics.
The antimuscarinic effects of chlorphenamine are enhanced by other antimuscarinic drugs and both antimuscarinic and sedative effects are enhanced by monoamine oxidase inhibitors (concurrent therapy with which is contraindicated) and tricyclic antidepressants.
Metabolism of phenytoin may be inhibited by chlorpheniramine with the possible development of phenytoin toxicity.
Store at temperatures not exceeding 30°C.
R06AB04 - chlorphenamine ; Belongs to the class of substituted alkylamines used as systemic antihistamines.
Antamin syr 2 mg/5 mL
60 mL x 1's
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