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

Masui, Takuya; Kusumi, Ichiro; Takahashi, Yoshito; Koyama, Tsukasa

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

Masui, Takuya; Kusumi, Ichiro; Takahashi, Yoshito et al.

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2006, 30(7), 1330-1333

Permalink : https://hdl.handle.net/2115/14722

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アクセス権	open access
URI	https://hdl.handle.net/2115/14722
タイトル	Effect of carbamazepine on the single oral dose pharmacokinetics of perospirone and its active metabolite
著者	Masui, Takuya ; Kusumi, Ichiro ; Takahashi, Yoshito ; Koyama, Tsukasa
著者名 Masui, Takuya
e-Rad_Researcher 30250426 著者名 Kusumi, Ichiro
著者名 Takahashi, Yoshito
著者名 Koyama, Tsukasa
言語	英語
キーワード	Atypical antipsychotics
	Carbamazepine
	Healthy subject
	Perospirone
	Pharmacokinetics
	Schizophrenia
発行日	2006-09-30
出版者	Elsevier B.V.
収録物名	Progress in Neuro-Psychopharmacology and Biological Psychiatry
巻(号)	30(7)
ページ	1330-1333
抄録	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.
資源タイプ	学術雑誌論文
出版タイプ	Accepted Manuscript
PISSN	0278-5846
関連情報	PMID 16600452
関連情報	URI http://www.sciencedirect.com/science/journal/02785846
関連情報 (isVersionOf)	出版社版DOI https://doi.org/10.1016/j.pnpbp.2006.02.012