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氯吡格雷是一种无活性的前体药物,进入体内后需要通过细胞色素P450(主要是细胞色素P450 2C19即CYP2C19)氧化为活性代谢物而发挥其抗血小板作用。越来越多的研究发现CYP2C19某些基因多态性(主要是细胞色素P450*2)与氯吡格雷的活性代谢产物减少,血小板抑制程度减轻,及主要不良心血管事件及支架内血栓增加有关。现就细胞色素P450多态性对氯吡格雷的药代动力学、药效动力学与临床终点事件的影响,及对细胞色素P450等位基因携带者的处理最新研究进展进行综述。
Clopidogrel is an inactive prodrug that enters the body and exerts its anti-platelet effect upon its oxidation into an active metabolite by cytochrome P450 (mainly CYP2C19, a cytochrome P450 2C19). More and more studies have found that some CYP2C19 genetic polymorphisms (mainly cytochrome P450 * 2) are associated with decreased active metabolites of clopidogrel, reduced platelet inhibition, and major adverse cardiovascular events and increased stent thrombosis . Now on the cytochrome P450 polymorphism of clopidogrel pharmacokinetics, pharmacodynamics and clinical endpoints, as well as on the handling of cytochrome P450 allele carriers the latest research progress are reviewed.