Das Pranab, Oliphant Carrie S, Beach Elizabeth, Thapa Rashmi
Assistant Professor, Division of Cardiology, Department of Internal Medicine, University of Tennessee Health Sciences Center, Memphis, Tennessee, USA;
J Blood Med. 2010;1:79-91. doi: 10.2147/JBM.S6596. Epub 2010 May 31.
The aspirin-clopidogrel combination is the current gold standard antiplatelet regimen following percutaneous coronary intervention and for the treatment of acute coronary syndrome. Despite the clinical benefit of this combination, patients continue to have vascular events. Another purinergic (P2Y(12)) receptor antagonist, prasugrel, became available last year. Although prasugrel is superior to clopidogrel in reducing clinical endpoints, a higher bleeding rate has been identified particularly in high-risk patients. Ticagrelor, a reversible P2Y(12) receptor antagonist currently being evaluated for approval, is also more potent than clopidogrel but has a similar bleeding risk. Two additional P2Y(12) antagonists are being investigated that will be available as an intravenous formulation. Apart from the P2Y(12) receptor antagonists, multiple other agents are being developed with unique mechanisms of platelet inhibition. These agents are being studied as an alternative to or in combination with clopidogrel. The antiplatelet agents currently under development include: thrombin receptor antagonists, phosphodiesterase inhibitors, a thromboxane-prostaglandin receptor antagonist, a serotonin receptor blocker, a platelet adhesion antagonist, nitric oxide-releasing aspirin, a glycoprotein VI antagonist, and a cyclooxygenase inhibitor. The purpose of this review is to describe the efficacy and safety profiles of the emerging antiplatelet agents and their role in the treatment of atherosclerotic cardiovascular diseases.
阿司匹林与氯吡格雷联合用药是目前经皮冠状动脉介入治疗后及治疗急性冠状动脉综合征的金标准抗血小板治疗方案。尽管该联合用药具有临床益处，但患者仍会发生血管事件。另一种嘌呤能（P2Y(12)）受体拮抗剂普拉格雷于去年上市。虽然普拉格雷在降低临床终点方面优于氯吡格雷，但已发现其出血率较高，尤其是在高危患者中。替格瑞洛是一种目前正在评估其获批情况的可逆性P2Y(12)受体拮抗剂，其效力也比氯吡格雷更强，但出血风险相似。另外两种P2Y(12)拮抗剂正在研究中，将制成静脉制剂。除了P2Y(12)受体拮抗剂外，还有多种其他药物正在研发，它们具有独特的血小板抑制机制。这些药物正在作为氯吡格雷的替代药物或与氯吡格雷联合使用进行研究。目前正在研发的抗血小板药物包括：凝血酶受体拮抗剂、磷酸二酯酶抑制剂、血栓素 - 前列腺素受体拮抗剂、5-羟色胺受体阻滞剂、血小板黏附拮抗剂、释放一氧化氮的阿司匹林、糖蛋白VI拮抗剂和环氧化酶抑制剂。本综述的目的是描述新型抗血小板药物的疗效和安全性概况及其在动脉粥样硬化性心血管疾病治疗中的作用。
