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学科主题: 临床医学
题名:
Effect of CYP2D6, CYP3A5, and MDR1 Genetic Polymorphisms on the Pharmacokinetics of Risperidone and Its Active Moiety
作者: Xiang, Qian1; Zhao, Xia1; Zhou, Ying1; Duan, Jing Li1; Cui, Yi Min1
关键词: Risperidone ; Chinese ; CYP2D6 ; CYP3A5 ; MDR1
刊名: JOURNAL OF CLINICAL PHARMACOLOGY
发表日期: 2010-06-01
DOI: 10.1177/0091270009347867
卷: 50, 期:6, 页:659-666
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: MULTIDRUG-RESISTANCE GENE ; P-GLYCOPROTEIN ; IN-VITRO ; PLASMA-CONCENTRATIONS ; CLINICAL-RESPONSE ; 9-HYDROXYRISPERIDONE ; EXPRESSION ; VIVO ; SCHIZOPHRENIA ; INVOLVEMENT
英文摘要:

Clinical studies suggest that plasma levels of risperidone and its active moiety (risperidone + 9-hydroxyrisperidone) correlate with adverse drug effects. The aim of this study is to evaluate the pharmacogenetic variability in the disposition of risperidone and the active moiety in healthy Chinese subjects. A 2-mg single dose of risperidone is orally administered to 23 healthy Chinese subjects. The risperidone and 9-hydroxyrisperidone serum concentrations are measured. The polymorphic alleles of CYP2D6*10, CYP3A5*3, MDR1 C1236T, G2677T/A, and C3435T are determined in each subject. The mean maximum plasma concentration and area under the time-concentration curve extrapolated to infinity for risperidone are significantly higher in subjects possessing the CYP2D6*10 allele than in those with the CYP2D6*1/*1 and *1/*10 genotype. For active moiety, the subjects who carry both homozygous CYP2D6*10 and homozygous CYP3A5*3 have 98% higher area under the time-concentration curve extrapolated to infinity and 59% higher maximum plasma concentration compared with other CYP2D6 EM subjects. The MDR1 2677GA genotype may also play a role in risperidone pharmacokinetics. Further studies are needed to explore the impact of MDR1 2677GA and CYP3A5 polymorphisms on risperidone therapy.

语种: 英语
WOS记录号: WOS:000277705100005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/52018
Appears in Collections:北京大学第一临床医学院_药剂科_期刊论文

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作者单位: 1.Peking Univ Third Hosp, Beijing, Peoples R China
2.Peking Univ First Hosp, Dept Pharm, Beijing 100034, Peoples R China

Recommended Citation:
Xiang, Qian,Zhao, Xia,Zhou, Ying,et al. Effect of CYP2D6, CYP3A5, and MDR1 Genetic Polymorphisms on the Pharmacokinetics of Risperidone and Its Active Moiety[J]. JOURNAL OF CLINICAL PHARMACOLOGY,2010,50(6):659-666.
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