Revision Year: 2020 Publisher: Chelonia Healthcare Limited, 11 Boumpoulinas Street, 3rd Floor, 1060 Nicosia, Cyprus
ATC Code: R06AB04
Chlorphenamine is a potent antihistamine (H1-antagonist).
Antihistamines diminish or abolish the actions of histamine in the body by competitive reversible blockade of histamine H1-receptor sites on tissues. Chlorphenamine also has anticholinergic activity.
Antihistamines act to prevent the release of histamine, prostaglandins and leukotrienes and have been shown to prevent the migration of inflammatory mediators. The actions of chlorphenamine include inhibition of histamine on smooth muscle, capillary permeability and hence reduction of oedema and wheal in hypersensitivity reactions such as allergy and anaphylaxis.
Chlorphenamine is well absorbed from the gastro-intestinal tract, following oral administration. The effects develop within 30 minutes, are maximal within 1 to 2 hours and last 4 to 6 hours. The plasma half-life has been estimated to 12 to 15 hours.
Chlorphenamine is metabolised to the monodesmethyl and didesmethyl derivatives. About 22% of an oral dose is excreted unchanged in the urine. Only traces amounts have been found in the faeces.
No additional data of relevance.
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