COLDKRIS Capsule Ref.[115642] Active ingredients: Chlorphenamine

Source: Registered Drug Product Database (NG)  Publisher: Krishat Pharma Industries Limited, KM 15, Lagos-Ibadan Expressway, Ibadan, Oyo State, NIGERIA, Email: info@krishatpharma.com, Company contacts details: operations@krishatpharma.com

5.1. Pharmacodynamic properties

ATC code: R06AB04

Mechanism of action

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.

Pharmacodynamic effects

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.

5.2. Pharmacokinetic properties

Absorption

Chlorphenamine is well absorbed from the gastrointestinal tract and following oral administration the effects develop within 30 minutes, and are maximal within 1 to 2 hours and last about 4 to 6 hours. The plasma half life has been estimated to be 12 to 15 hours.

Distribution

The drug is widely distributed throughout the body including the CNS.

Biotransformation

The main site of metabolic transformation is in the liver. Chlorphenamine is metabolised to the monodesmethyl and didesmethyl derivatives. About 22% of an oral dose is excreted unchanged in the urine.

Elimination

Little if any is excreted unchanged in the urine; most appears there as degradation products that are almost completely excreted within 24 hours. The drug is eliminated more rapidly by children than by adults.

5.3. Preclinical safety data

NA.

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