Influence of quinidine, fluvoxamine, and ketoconazole on the enantioselective pharmacokinetics of citalopram in rats.(Clinical report)

Canadian Journal of Physiology and Pharmacology | November 1, 2008| | Copyright

Introduction

Citalopram (CITA), a drug used for the treatment of depression, is available as a racemic mixture or as the pure enantiomer (+)-(S)-CITA. Its antidepressive action is related to (+)-(S)-CITA and to its metabolite (+)-(S)-demethylcitalopram (DCITA) (Baumann et al. 2002; Hyttel et al. 1992). Sanchez et al. (2003) reported that the (-)-(R)-CITA enantiomer inhibits the anxiolytic effect of (+)-(S)-CITA in rats. In humans, the metabolism of CITA depends on CYP2C, CYP2D, CYP3A, monoamine oxidases A and B, and aldehyde oxidase (Brosen and Naranjo 2001). The ...

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