Involvement of CYP3A4 in the Metabolism of Bromperidol in vitro

Authors: Sato S.¹; Someya T.¹; Shioiri T.¹; Koitabashi T.²; Inoue Y.³

Source: Basic & Clinical Pharmacology & Toxicology, Volume 86, Number 3, 1 March 2000 , pp. 145-148(4)

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Abstract:

In this study, human cytochrome P450 isoenzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4) expressed in a cell line were used to elucidate their roles in the metabolism of bromperidol. We found that CYP3A4 catalyzes the N-dealkylation of bromperidol and its metabolite, reduced bromperidol. CYP3A4 also catalyzes the dehydration of bromperidol to bromperidol 1,2,3,6-tetrahydropyridine, metabolizes bromperidol to bromperidol pyridinium, and catalyzes the oxidation of reduced bromperidol back to bromperidol. CYP1A2, CYP2C19, and CYP2D6 do not catalyze these reactions.

Document Type: Original article

Affiliations: 1: Department of Psychiatry, Niigata University School of Medicine, Niigata, 2: Department of Psychiatry, National Saigata Hospital, Niigata, and 3: Pharmacokinetics, Kyushu Laboratories, Pharmaceutical Research Division, Yoshitomi Pharmaceutical Industries Ltd, Fukuoka, Japan

Publication date: 2000-03-01

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