基因多态性对氨氯地平药代、药效的影响

Effects of polymorphic gene on the pharmacokinetics and pharmacodynamics of amlodipine

氨氯地平是二氢吡啶钙离子通道阻滞剂,临床上用于各种高血压和心绞痛的治疗,在体内经CYP3A5代谢而消除,其药代动力学不同于其他的二氢吡啶钙离子通道阻滞剂。由于CYP3A存在基因多态性而导致氨氯地平药代动力学的个体差异。为此,笔者查阅国内外相关文献对氨氯地平的临床应用与CYP3A5基因多态性对其药代动力学及药效学的影响进行综述,为临床参考基因多态性特征来确立氨氯地平正确合理的给药方案提供依据。

Amlodipine,1,4-Dihydropyridine calcium channel antagonists,prescribed in the management of angina and hypertension,act as substrates of CYP3A5,has a pharmacokinetic profile that differs from other dihydropyridines.It has been suggested that the CYP3A5＊3 allele contributes to the interindividual variability of CYP3A activity in vivo.This review aimed to summarize the clinical application of the amlodipine and the possible role of the genetic polymorphism CYP3A5 on the pharmacokinetics and pharmacodynamics of amlodipine and instruct the reasonable clinical application of amlodipine.