Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone
Melperone is an antipsychotic drug used for sleep induction [1, 4, 11]. Grözinger et al.  revealed an inhibitory effect of melperone on the hepatic cytochrome P450 2D6 (CYP2D6) catalyzed O-demethylation of dextromethorphan and of the antidepressant venlafaxine. We report an inhibitory effect of melperone on the metabolization of the antipsychotic risperidone, a substrate of CYP2D6 and CYP3A4 , and give further evidence for a melperone dependent inhibition of CYP2D6.
In all cases, blood was drawn 12 h after the last intake of medication, at steady state, defined by a constant dose over at least 7 days. Plasma concentrations were analyzed by standard procedures (mass spectroscopy, internal standard; Bioscientia, Ingelheim, Germany).
Individual one, a 19-year-old schizophrenic male, with a post psychotic lack of initiation, received 6 mg of risperidone per day. 50 mg of melperone per day were added for sleep induction. The initial risperidone plasma concentration of...
KeywordsRisperidone Metoprolol Venlafaxine Dextromethorphan Psychotic Depression
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