Verapamil, but not Probenecid, Co-Administration Can Convert Desloratadine to a Sedating Antihistamine in Mice

Author(s): Anand Katta, Mugunthu Dhananjeyan, Crystal Bykowski, Paul Erhardt, Miles Hacker, Donald B. White, Kenneth Bachmann

Journal Name: Drug Metabolism Letters

Volume 1 , Issue 1 , 2007

Become EABM
Become Reviewer
Call for Editor


The possibility that non-sedating antihistamines could elicit sedation in mice due to drug-induced inhibition of brain PgP was evaluated by measuring the ability of desloratadine alone or in combination with verapamil to cause ataxia in mice. Also, the concentrations of desloratadine in plasma and in brain homogenates were measured by liquid chromatography- mass spectrometry. Relative to methylcellulose (control) treatment, verapamil plus desloratadine decreased rotarod performance of mice. Plasma concentrations of desloratadine appeared comparable in the mice treated with either desloratadine or verapamil plus desloratadine, however the rate of decline of desloratadine from brain tissue was slower in mice treated with verapamil plus desloratadine compared to mice treated with desloratadine only. These data suggest that inhibition of brain PgP can convert desloratadine to a sedating antihistamine in mice.

Keywords: PgP, desloratadine, antihistamines, pharmacokinetics, pharmacodynamics

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2007
Published on: 01 March, 2012
Page: [7 - 11]
Pages: 5
DOI: 10.2174/187231207779814391

Article Metrics

PDF: 19