Drug intelligence / Profile preview

chlorpheniramine

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

Chlorpheniramine is a first-generation alkylamine antihistamine primarily used to relieve symptoms of allergic conditions such as allergic rhinitis (hay fever), urticaria (hives), and other skin allergies. It acts as a competitive antagonist at the histamine H1 receptor on target cells in blood vessels and respiratory tract tissues. By blocking H1 receptors, it reduces the effects of endogenous histamine—such as vasodilation and increased capillary permeability—thereby alleviating symptoms like sneezing, runny nose, itching eyes/nose/throat/skin. Chlorpheniramine also has mild anticholinergic properties that can cause side effects such as dry mouth or drowsiness but is considered less sedating than some other first-generation antihistamines. It is available in various formulations including tablets (often as chlorpheniramine maleate), syrups, and injectables[1][3][5][6].

Brand names
Chlor-TrimetonPiritonAller-ChlorTeldrin
Other names
chlorphenaminechlorpheniraminumclorfenamina马来酸氯苯那敏氯苯那敏扑尔敏
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)NET (Norepinephrine Transporter)HRH1 (Histamine H1 Receptor)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

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