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Effect of CYP2D6, CYP3A5, and MDR1 Genetic Polymorphisms on the Pharmacokinetics of Risperidone and Its Active Moiety
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
2010-06-01
DOI10.1177/0091270009347867
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
引用统计
被引频次:48[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52018
专题北京大学第一临床医学院_药剂科
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
推荐引用方式
GB/T 7714
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.
APA Xiang, Qian,Zhao, Xia,Zhou, Ying,Duan, Jing Li,&Cui, Yi Min.(2010).Effect of CYP2D6, CYP3A5, and MDR1 Genetic Polymorphisms on the Pharmacokinetics of Risperidone and Its Active Moiety.JOURNAL OF CLINICAL PHARMACOLOGY,50(6),659-666.
MLA Xiang, Qian,et al."Effect of CYP2D6, CYP3A5, and MDR1 Genetic Polymorphisms on the Pharmacokinetics of Risperidone and Its Active Moiety".JOURNAL OF CLINICAL PHARMACOLOGY 50.6(2010):659-666.
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