CYP2D6基因多态性及对美托洛尔代谢的影响

中国临床药理学与治疗学 ›› 2011, Vol. 16 ›› Issue (9): 1059-1064.

CYP2D6基因多态性及对美托洛尔代谢的影响

熊丹, 熊玉卿

南昌大学医学院临床药理研究所,南昌 330006,江西

收稿日期:2011-06-01 修回日期:2011-08-08 出版日期:2011-09-26 发布日期:2011-10-11
通讯作者: 熊玉卿,女,教授,博士生导师,主要从事药代动力学方向研究。Tel: 0791-6360654 E-mail: xiongyuqing2009@hotmail.com
作者简介:熊丹,女,硕士研究生,从事药代动力学研究。Tel: 13970941341 E-mail: 05xiongdan@163.com
基金资助:
国家十一五科技重大专项“建立新药研发安全监测信息化技术平台”子课题“构建I期临床试验研究和风险监测的信息化监管技术平台”(2009ZX09309-003-02)

Polymorphism of CYP2D6 gene and the influence on the metabolism of metoprolol

XIONG Dan, XIONG Yu-qing

Institute of Clinical Pharmacology, Medical College of Nanchang University, Nanchang 330006, Jiangxi, China

Received:2011-06-01 Revised:2011-08-08 Online:2011-09-26 Published:2011-10-11

摘要/Abstract

摘要： CYP2D6是一种重要的P450系氧化代谢酶,主要参与多种重要药物的代谢。CYP2D6基因多态性会引起药物代谢有显著的个体和种族差异。美托洛尔为选择性β₁受体阻滞剂,临床应用上存在巨大个体差异,主要在肝脏经多条途径代谢,大约70%的代谢由CYP2D6介导,CPY2D6基因多态性对美托洛尔代谢有较大影响。本文从CYP2D6的基因多态性及它对美托洛尔代谢的影响这两方面作一综述。

关键词: 美托洛尔, CYP2D6, 基因多态性, 药物代谢

Abstract: As one of major cytochrome P450s, CYP2D6 is responsible for the metabolism of many important drugs. Genetic polymorphism of CYP2D6 is the basis of lager interindividual and racial variability in the metabolism of drug. Metoprolol is a selective β₁-adrenoceptor antagonist, there is an obvious individual difference in clinic. It is metabolized in the liver, in vivo data indicate that approximately 70% of the metabolism of metoptolol depends upon CYP2D6. Genetic polymorphism of CYP2D6 have a great influence on the metabolism of metoprolol. Here we summarize the polymorphism of CYP2D6 gene and the influence on the metabolism of metoprolol.

Key words: Metoprolol, CYP2D6, Gene polymorphism, Drug metabolism

中图分类号:

R969.1

熊丹, 熊玉卿. CYP2D6基因多态性及对美托洛尔代谢的影响[J]. 中国临床药理学与治疗学, 2011, 16(9): 1059-1064.

XIONG Dan, XIONG Yu-qing. Polymorphism of CYP2D6 gene and the influence on the metabolism of metoprolol[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2011, 16(9): 1059-1064.

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