University of Florida, College of Medicine-Jacksonville, Jacksonville, Florida 32209, USA.
Rev Esp Cardiol. 2010 Jan;63(1):60-76. doi: 10.1016/s1885-5857(10)70010-4.
Platelet P2Y12 receptor antagonism with clopidogrel has represented a major advancement in the pharmacological management of patients with atherothrombotic disease, in particular those with acute coronary syndromes and undergoing percutaneous coronary interventions. Despite the benefit associated with clopidogrel therapy in these high risk settings, laboratory and clinical experience have led to identify some of its caveats, among which its wide range of platelet inhibitory response is the most relevant. Genetic, cellular and clinical factors are implied in variability in response to clopidogrel. Importantly, pharmacodynamic findings have shown to have important prognostic implications, underscoring the need for more optimal antiplatelet treatment strategies. The aim of this manuscript is to provide an overview on the current status and future directions in P2Y12 receptor antagonism, with particular emphasis on interindividual variability in response to clopidogrel and strategies, including novel antiplatelet agents, to improve platelet P2Y12 inhibition.
血小板 P2Y12 受体拮抗剂氯吡格雷在抗动脉粥样硬化血栓形成疾病的药理学治疗方面取得了重大进展，特别是在急性冠脉综合征和经皮冠状动脉介入治疗的患者中。尽管氯吡格雷治疗在这些高危人群中具有益处，但实验室和临床经验发现了其一些局限性，其中最相关的是其广泛的血小板抑制反应。遗传、细胞和临床因素与氯吡格雷的反应变异性有关。重要的是，药效学发现表明具有重要的预后意义，强调需要更优化的抗血小板治疗策略。本文旨在概述 P2Y12 受体拮抗剂的现状和未来方向，特别强调氯吡格雷反应的个体间变异性和改善血小板 P2Y12 抑制的策略，包括新型抗血小板药物。
