Cetirizine, a Novel Antihistamine

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Cetirizine, an oxidative metabolite of hydroxyzine, is a cyclizine class H1-receptor antagonist with diminished CNS activity currently under investigation. It has a novel pharmacokinetic profile with a 9-hour half-life, lower volume of distribution and total body clearance, minimal metabolism and essentially renal excretion. Minimal binding to CNS receptors has been demonstrated in animal models. In contrast to its parent compound and diphenhydramine, cetirizine has an effect comparable to placebo on psychomotor function and multiple sleep latency tests. Inhibition of histamine-induced bronchospasm and mild bronchodilation has also been demonstrated. U.S. and European clinical trials have affirmed its safety and efficacy in histamine-associated disorders.