2024-03-28T20:00:40Zhttps://eprints.lib.hokudai.ac.jp/dspace-oai/requestoai:eprints.lib.hokudai.ac.jp:2115/147222022-11-17T02:08:08Zhdl_2115_20040hdl_2115_121Effect of carbamazepine on the single oral dose pharmacokinetics of perospirone and its active metaboliteMasui, TakuyaKusumi, IchiroTakahashi, YoshitoKoyama, TsukasaAtypical antipsychoticsCarbamazepineHealthy subjectPerospironePharmacokineticsSchizophrenia493.7Perospirone 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.Elsevier B.V.Journal Articleapplication/pdfhttp://hdl.handle.net/2115/14722https://eprints.lib.hokudai.ac.jp/dspace/bitstream/2115/14722/1/PNP%26BP30-7.pdf0278-5846Progress in Neuro-Psychopharmacology and Biological Psychiatry307133013332006-09-30enginfo:pmid/16600452info:doi/10.1016/j.pnpbp.2006.02.012author