二氢吡啶类钙拮抗剂药物基因组学的研究进展

二氢吡啶类钙拮抗剂是临床常用的一类降压药。临床使用过程中,疗效受到患者基因组学特征的影响。细胞色素P450(CYP3A)酶、P-糖蛋白(P-gp)和乳腺癌耐药蛋白(BCRP)转运体参与了药物体内处置过程,而CACNA1C受体是发挥药效的关键。大量临床研究结果表明,它们的基因多态性对该类药物的药动学和药效学会产生较大影响。本文在查阅近年来国内外文献基础上,就酶、转运体和受体的基因多态性对二氢吡啶类钙拮抗剂药动和药效的影响研究进展进行了综述,为临床用药提供参考。

Advances in pharmacogenomics of dihydropyridine calcium antagonists

Dihydropyridine calcium antagonists are a class of antihypertensive drugs commonly used in clinical practice.During clinical use,the efficacy is influenced by the pharmacogenomic characteristics of the patient.The CYP3A enzyme,P-gp and BCRP transporters are involved in the disposition of drug in vivo,and the CACNA1C receptor is the key to drug efficacy.A large number of clinical studies have shown that their genetic polymorphisms have a greater impact on the pharmacokinetics and pharmacodynamics of these drugs.In this paper,we consulted the recent domestic and foreign literatures and reviewed the research progress of the effects of gene polymorphisms of enzymes,transporters and receptors on the pharmacokinetics and pharmacodynamics of dihydropyridine calcium antagonists,and provides reference for clinical use.