Enantioselective disposition of venlafaxine and its metabolite o-desmethylvenlafaxine in rats

Author:

Dubey Sunil K1,Anand Amit1,Saha Ranendra N1

Affiliation:

1. Department of Pharmacy, Birla Institute of Technology & Science, Pilani, India

Abstract

Aim: The study was conducted to understand enantioselective pharmacokinetic of venlafaxine (VEN) and o-desmethylvenlafaxine (ODV) using enantioselective HPLC method. The R-enantiomer of VEN is a potent inhibitor of both serotonin and noradrenaline reuptake, whereas the S-enantiomer is more selective in inhibiting serotonin reuptake. Enantiomers of ODV also inhibit noradrenaline and serotonin reuptake. Materials & methods: Study was carried out in wistar rats after oral administration of 120 mg/kg dose of racemic VEN. Results: Plasma concentrations of S (+) VEN were found to be higher than those of R (-) VEN. Plasma concentrations of S (+) ODV were found to be higher than those of R (-) ODV. Conclusion: A significant difference in most of the pharmacokinetic parameters was observed between the enantiomers of VEN in rat plasma.

Publisher

Future Science Ltd

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