Moliterno David J
Gill Heart Institute and Division of Cardiovascular Medicine, University of Kentucky, Lexington, Kentucky, USA.
J Interv Cardiol. 2008 Dec;21 Suppl 1:S18-24. doi: 10.1111/j.1540-8183.2008.00409.x.
Platelet activation and thrombin formation play significant roles in the pathophysiology of acute coronary syndrome. To overcome this pathophysiology, antiplatelet agents are utilized to decrease platelet aggregation and anticoagulants to decrease thrombin formation. Current antiplatelet agents are designed to inhibit various mediators of platelet activation, such as thromboxane A2 and adenosine diphosphate, and platelet-surface receptors (e.g., glycoprotein IIb/IIIa receptors). The rationale for upstream versus deferred administration of antiplatelet therapy in patients scheduled for percutaneous intervention and the current ACC/AHA guidelines for the management of patients with unstable angina/non-ST-segment myocardial infarction are discussed. The next-generation antiplatelet drugs are in various stages of clinical development, with unique differentiating mechanistic and pharmacokinetic properties. The newer P2Y12 thienopyridine receptor antagonists and protease receptor inhibitor are also examined, in addition to the rationale of various outcome studies evaluating the efficacy and safety of the different agents.
血小板活化和凝血酶形成在急性冠状动脉综合征的病理生理学中起重要作用。为克服这种病理生理状态，使用抗血小板药物来减少血小板聚集，并使用抗凝剂来减少凝血酶形成。目前的抗血小板药物旨在抑制血小板活化的各种介质，如血栓素A2和二磷酸腺苷，以及血小板表面受体（如糖蛋白IIb/IIIa受体）。讨论了计划进行经皮介入治疗的患者抗血小板治疗上游给药与延迟给药的基本原理，以及当前美国心脏病学会/美国心脏协会关于不稳定型心绞痛/非ST段抬高型心肌梗死患者管理的指南。新一代抗血小板药物正处于临床开发的不同阶段，具有独特的差异化作用机制和药代动力学特性。除了评估不同药物疗效和安全性的各种结果研究的基本原理外，还对新型P2Y12噻吩吡啶受体拮抗剂和蛋白酶受体抑制剂进行了研究。
