Desloratadine: A preclinical and clinical overview

Drugs of Today
P. NormanX. Rabasseda

Abstract

A new competitive histamine H(1)-receptor antagonist with superior binding affinity at this receptor as compared with other common antihistamines, desloratadine is the active metabolite of loratadine, the most extensively used agent of this class. Under development for the treatment of allergic rhinitis and urticaria and currently awaiting regulatory approval in the United States, desloratadine was recently approved and became commercially available in Europe for the treatment of allergic disease. Desloratadine is at least 50-fold more potent in vitro and appears to be 10-fold more potent in vivo than loratadine. The new antihistamine is metabolized to 3-hydroxydesloratadine, which retains biological activity. Absorption of orally administered desloratadine is dose proportional, and desloratadine achieves steady-state concentrations after approximately 5 doses with once-daily administration. This is consistent with mean half-life values of 24-27 h and a 24-h dosing interval. The absorption of desloratadine is not affected by food and there are no clinically relevant drug-drug interactions. In randomized, double-blind, placebo-controlled clinical trials, a single 5 mg dose of desloratadine conferred significant relief of seasona...Continue Reading

Citations

Jul 11, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R RamanathanJ E Patrick
Mar 1, 2006·Expert Opinion on Drug Safety·Bruce PrennerBarry Lutsky
Oct 28, 2004·Rapid Communications in Mass Spectrometry : RCM·Yaru SongYi-Ming Liu
Jul 27, 2011·Environmental Toxicology and Pharmacology·Izabela Sadowska-WodaEdyta Bieszczad-Bedrejczuk

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