新型抗血小板药物的研究进展

Research Progress of new Antiplatelet Drugs

我国人口逐步老龄化,动脉硬化性血栓形成疾病是致死和致残的关键原因,特别是急性冠状动脉综合征(ACS)。此外脑卒中的危害也逐年增加。在动脉粥样硬化形成过程中血小板发挥主要作用,因此抗血小板药物是治疗的基石。环氧化酶-I受体抑制剂阿司匹林及噻吩吡啶类P2Y12受体拮抗剂氯吡格雷是临床常用的抗血小板药物,但它们各有缺陷,阿司匹林抗血小板作用相对较弱。氯吡格雷为前体药物,起效慢,而且疗效受多种药物影响,导致不同患者对药物反应存在差异性。因此降低出血风险和提高疗效成为研发新型抗血小板药物的目标,笔者从血小板黏附、活化和聚集机制到影响各个机制的新型抗血小板药物进行综述,尤其包括抗血小板作用新靶点药物。并针对心脑血管性疾病提供安全、有效的药物治疗进行展望。

In our country, the aging of the population is becoming more and more serious, and arterial thrombosis is the key cause of death and disability,especially acute coronary syndrome （ACS）. In addition,the risk of stroke increased year by year. Platelets play a major role in the formation of atheroselerosis, and antiplatelet drugs are the cornerstone of therapy. Cyclooxygenase-I inhibitor aspirin and thienopyridine P2Y12 receptor antagonist clopidogrel antiplatelet drugs is commonly used in clinical, but they have shortcomings, antiplatelet effect of aspirin is relatively weak. Clopidogrel is a prodrug, which is slow to take effect, and the effect is affected by many drugs. Therefore reduce the risk of bleeding and improve the efficacy of antiplatelet drugs become the research and development of new target, the author from the platelet adhesion, activation and aggregation mechanism to new antiplatelet drug effects of each mechanism are reviewed, especially including the antiplatelet effect of new target drugs. To provide a safe and effective drug therapy for cardiovascular and cerebrovascular diseases.