Zhang Yan-Jiao, Li Mu-Peng, Tang Jie, Chen Xiao-Ping
Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha 410008, China.
Institute of Clinical Pharmacology, Hunan Key Laboratory of Pharmacogenetics, Central South University, Changsha 410078, China.
Int J Environ Res Public Health. 2017 Mar 14;14(3):301. doi: 10.3390/ijerph14030301.
Clopidogrel has significantly reduced the incidence of recurrent atherothrombotic events in patients with acute coronary syndrome (ACS) and in those undergoing percutaneous coronary intervention (PCI). However, recurrence events still remain, which may be partly due to inadequate platelet inhibition by standard clopidogrel therapy. Genetic polymorphisms involved in clopidogrel's absorption, metabolism, and the P2Y12 receptor may interfere with its antiplatelet activity. Recent evidence indicated that epigenetic modification may also affect clopidogrel response. In addition, non-genetic factors such as demographics, disease complications, and drug-drug interactions can impair the antiplatelet effect of clopidogrel. The identification of factors contributing to the variation in clopidogrel response is needed to improve platelet inhibition and to reduce risk for cardiovascular events. This review encompasses the most recent updates on factors influencing pharmacokinetic and pharmacodynamic responses to clopidogrel.
氯吡格雷已显著降低急性冠状动脉综合征（ACS）患者以及接受经皮冠状动脉介入治疗（PCI）患者的复发性动脉粥样硬化血栓形成事件的发生率。然而，复发事件仍然存在，这可能部分归因于标准氯吡格雷治疗对血小板的抑制不足。参与氯吡格雷吸收、代谢及P2Y12受体的基因多态性可能会干扰其抗血小板活性。最近的证据表明，表观遗传修饰也可能影响氯吡格雷的反应。此外，人口统计学、疾病并发症和药物相互作用等非遗传因素会削弱氯吡格雷的抗血小板作用。为了增强血小板抑制作用并降低心血管事件风险，需要确定导致氯吡格雷反应差异的因素。本综述涵盖了影响氯吡格雷药代动力学和药效学反应的因素的最新进展。
