Drug intelligence / Profile preview

cetirizine

Development stage
Approved
Lead developer
UCB
Modality
Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Cetirizine is a second-generation antihistamine used to treat symptoms of allergic rhinitis (hay fever), perennial and seasonal allergies, chronic idiopathic urticaria (hives), atopic dermatitis, and other allergic conditions. It works by selectively inhibiting peripheral histamine H1 receptor to block the action of histamine—a chemical responsible for allergy symptoms such as sneezing, itching, watery eyes, and runny nose. Cetirizine is a human metabolite of hydroxyzine with negligible anticholinergic or antiserotonergic activity and limited penetration into the brain compared to first-generation antihistamines. This results in fewer sedative effects but some drowsiness may still occur. Cetirizine was patented in 1983 and entered medical use in 1987; it is available as both prescription and over-the-counter formulations including tablets, chewables, liquids/gels/syrups/disintegrating tablets/capsules/eye drops[1][4][5][6][8].

Brand names
ZyrtecZyrtec AllergyChildren’s ZyrtecChildren’s Zyrtec AllergyChildren’s Zyrtec Chewable TabletsChildren’s Zyrtec HivesZerviate
Other names
cetirizine hydrochloride
02

Targets

HRH1 (Histamine H1 Receptor)

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