基因多态性对钙离子通道阻滞剂类抗高血压药物药动学及-药学进展.PDFVIP

PROGRESS IN PHARMACEUTICAL SCIENCES 2014,38 11 :819-823 ( ) 819 基因多态性对钙离子通道阻滞剂类抗高血压药物 药动学及疗效的影响 喻子眈 1,2 ，王永庆 2*，龚晓健 1** （1. 中国药科大学药理学教研室，江苏 南京 210009；2. 南京医科大学第一附属医院临床药理研究室，江苏 南京 210029） [ 摘要 ] ·钙离子通道阻滞剂是常用的一种高血压治疗药物，其中又以二氢吡啶类钙离子通道阻滞剂为主要代表，常见的有硝苯地平、氨氯地平、 非洛地平等。然而，不同的患者个体对此类抗高血压药物可产生不同的降压效果，这种差异是环境和遗传共同作用的结果。基因多态性决 定了药物代谢酶、转运体以及作用受体的差异，是导致药物疗效差异的重要原因之一。综述药物代谢酶、转运体和作用受体的基因多态性 对钙离子通道阻滞剂类抗高血压药物的药动学和疗效的影响。 [ 关键词 ] 钙离子通道阻滞剂；基因多态性；药动学；抗高血压疗效；个体差异 [ 中图分类号 ] R972.4 [ 文献标志码 ] A [ 文章编号 ] 1001-5094（2014）11-0819-05 Effect of Genetic Polymorphisms on Pharmacokinetics and Efficacy of Calcium Channel Blockers as Antihypertensives:an Review 1,2 2 1 YU Zidan , WANG Yongqing , GONG Xiaojian ( 1. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China; 2. Research Division of Clinical Pharmacology, The first Affiliated Hospital with Nanjing Medical University, Nanjing 210029, China) [Abstract] Calcium channel blockers, especially dihydropyridine calcium channel blockers, such as nifedipine, amlodipine, felodipine and so on, are widely used in the therapy of hypertension. It has been revealed that there is the interindividual variation of efficacy among these antihypertensives in hypertension patients which is the result of variety of genetic and environmental factors and genetic polymorphisms and determines the difference of metabolic enzymes, transporters and receptors for the drugs, thus becoming one of the main reasons for the variation of efficacy of the drugs. The impact of genetic polymorphisms of the metabolic enzy