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PHARMALOGY
Cetirizine dihydrochloride
CAS NO. 83881-51-1
 

Cetrizine Didihydrochloride Pharmocology

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.

Pharmacokinetics

Absorption

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of approximately 1 hour following oral administration of tablets, chewable tablets or syrup in adults. Comparable bioavailability was found between the tablet and syrup dosage forms. Comparable bioavailability was also found between the ZYRTEC tablet and the ZYRTEC chewable tablet taken with or without water. When healthy volunteers were administered multiple doses of cetirizine (10 mg tablets once daily for 10 days), a mean peak plasma concentration (Cmax) of 311 ng/mL was observed. No accumulation was observed.

A sympathomimetic amine that has a decongestant effect on the nasal mucosa. Its peripheral effects are similar to those of ephedrine and its central effects are similar to, but less intense than, those of amphetamines.^{01}

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Contains information from medical literature and expert advice from medical scientists, physicians, pharmacists, pharmacologists, and other professionally qualified physicians that goes beyond FDA-approved labeling.

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.

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