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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Clopidogrel resistance: pharmacokinetic or pharmacogenetic?
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Clopidogrel resistance: pharmacokinetic or pharmacogenetic?

机译：氯吡格雷耐药性：药代动力学还是药代遗传学？

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Clopidogrel is important for the management of acute coronary syndromes and, along with aspirin, is recommended in the American College of Cardiology/American Heart Association guideline. It is also used along with aspirin, during the placement of coronary artery stents. Clopidogrel resistance was recognized in such procedures, as several patients did not have the anticipated platelet aggregation response to an ex vivo adenosine diphosphate challenge. From the EXCELSIOR study, which investigated the phenomenon, it was appreciated that it was present prior to treatment with clopidogrel and was therefore an intrinsic property of the patient's platelets. From other studies, it was appreciated that the patients who had clopidogrel resistance had a defective allele *2/ in the CYP2C19 gene. Furthermore, there was a dose response evident in that the homozygotes CYP2C19*2/*2 had platelets that responded even less well to clopidogrel than the heterozygotes CYP2C19*2 that responded less well than the wild-type homozygote. The involvement of the phenomenon with CYP2C19 led some to believe that it was a pharmacokinetic issue. However, the major oxidative metabolic pathway for clopidogrel by which the reactive intermediate is formed is CYP3A4. It is suggested that there is a linkage between a polymorphism of the platelet receptor P2Y12 and the polymorphism of CYP2C19.
机译：氯吡格雷对急性冠脉综合征的治疗很重要，在美国心脏病学会/美国心脏协会指南中推荐与阿司匹林一起使用。在放置冠状动脉支架期间，它也与阿司匹林一起使用。在这样的程序中，氯吡格雷耐药性得到了认可，因为几名患者没有对体外二磷酸腺苷激发的预期血小板聚集反应。从EXCELSIOR研究（该现象进行了调查）可以看出，它在使用氯吡格雷治疗之前就已存在，因此是患者血小板的固有特性。从其他研究中，可以理解氯吡格雷抵抗的患者在CYP2C19基因中有缺陷的等位基因* 2 /。此外，存在明显的剂量反应，纯合子CYP2C19 * 2 / * 2的血小板对氯吡格雷的反应甚至比杂合子CYP2C19 * 2的血小板要好于野生型纯合子。该现象与CYP2C19的参与使一些人认为这是一个药代动力学问题。但是，通过氯吡格雷形成反应性中间体的主要氧化代谢途径是CYP3A4。提示血小板受体P2Y12的多态性与CYP2C19的多态性之间存在联系。

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