Gender-dependent influence of bupropion on the activity of hepatic cytochrome P450 2D2 in rats

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Authors

ZAHRADNÍKOVÁ Lucia ZENDULKA Ondřej JUŘICA Jan MCCASKEY HADAŠOVÁ Eva

Year of publication 2008
Type Article in Periodical
Magazine / Source Activitas Nervosa Superior
MU Faculty or unit

Faculty of Medicine

Citation
Field Pharmacology and pharmaceutical chemistry
Keywords cytochrome P450; bupropion
Description One of the most important enzymatic systems participating in drug metabolism is cytochrome P450 (CYP450). CYP450 consists of many isoforms which activity of is influenced by numerous endogenous (e.g. gender, pathophysiological status, age) and exogenous factors (e.g. xenobiotical inhibitors and inducers). Although bupropion is not metabolized by CYP 2D6 (human ortologue of rat CYP2D2), there is certain potential for interaction when bupropion is co-administered with other drugs metabolized by this isoenzyme, too. The aim of the present study was to determine the influence of gender and administration of bupropion on the CYP450 isoform 2D2 (CYP2D2) activity. As selective markers of the metabolic activity of CYP2D2 dextromethorphan (DEM) and its metabolite dextrorphane (DOR) were used. In animals treated with bupropion compared to control animals administered with saline the inhibitory effect of bupropion was expressed as a decrease of DOR in the 30th, 60th and 120th minutes of perfusion.
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