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Effect of carbamazepine on the single oral dose pharmacokinetics of perospirone and its active metabolite

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Title: Effect of carbamazepine on the single oral dose pharmacokinetics of perospirone and its active metabolite
Authors: Masui, Takuya Browse this author
Kusumi, Ichiro Browse this author →KAKEN DB
Takahashi, Yoshito Browse this author
Koyama, Tsukasa Browse this author
Keywords: Atypical antipsychotics
Healthy subject
Issue Date: 30-Sep-2006
Publisher: Elsevier B.V.
Journal Title: Progress in Neuro-Psychopharmacology and Biological Psychiatry
Volume: 30
Issue: 7
Start Page: 1330
End Page: 1333
Publisher DOI: 10.1016/j.pnpbp.2006.02.012
PMID: 16600452
Abstract: Perospirone is a serotonin 5-HT2A and dopamine D2 receptor antagonist which originated in Japan. It has been shown that perospirone is metabolized to ID-15036 mainly by CYP3A4 based on an in vitro study. To investigate the metabolism of perospirone in humans, the authors measured the concentration of perospirone and ID-15036 after a single oral dose of perospirone (8 mg) in 10 healthy male subjects, before and during coadministration of carbamazepine, known as a potent inducer of CYP3A4. Before carbamazepine coadministration, the peak plasma concentrations ± SD of perospirone and ID-15036 were 4.0 ± 4.3 and 11.7 ± 7.1 ng/ml, respectively. During carbamazepine coadministration, the concentration of perospirone was decreased below the detection limit, and that of ID-15036 was 6.0 ± 1.7 ng/ml. The concentrations of perospirone and ID-15036 were influenced significantly by the treatment with carbamazepine, and this was probably attributable to the induction of CYP3A4. This study provided an in vivo evidence of involvement of CYP3A4 in the metabolism of perospirone.
Type: article (author version)
Appears in Collections:医学院・医学研究院 (Graduate School of Medicine / Faculty of Medicine) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 増井 拓哉

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