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Canadian Pharmacy |
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Mechanism of Action
Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its
principal effects are mediated via selective inhibition of peripheral H1
receptors. The antihistaminic activity of cetirizine has been clearly documented
in a variety of animal and human models. In vivo and ex vivo animal models
have shown negligible anticholinergic and antiserotonergic activity. In
clinical studies, however, dry mouth was more common with cetirizine than
with placebo. In vitro receptor binding studies have shown no measurable
affinity for other than H1 receptors. Autoradiographic studies with radiolabeled
cetirizine in the rat have shown negligible penetration into the brain.
Ex vivo experiments in the mouse have shown that systemically administered
cetirizine does not significantly occupy cerebral H1 receptors. |
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Zyrtec Articles |
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