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首页> 外文期刊>Journal of Blood Medicine >Antiplatelet therapy in acute coronary syndromes: focus on ticagrelor
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Antiplatelet therapy in acute coronary syndromes: focus on ticagrelor

机译:急性冠脉综合征的抗血小板治疗:关注替卡格雷

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Abstract: The use of antiplatelet agents, specifically the thienopyridines, has become a standard of care in the approach to the patient presenting with an acute coronary syndrome. These drugs irreversibly inhibit the platelet by permanently binding to the surface P2Y12 receptor and blocking the downstream fibrinogen cross-linking between platelets, which leads to aggregation and thrombus. However, currently available therapeutic choices are limited by potential interaction with other medications, slow hepatic conversion to active metabolite, genetic resistance, and narrow therapeutic safety margin. In order to overcome these disadvantages, there has been an interest in developing alternatives to thienopyridines. Recent investigations have included ticagrelor, a reversible inhibitor of the P2Y12 platelet receptor, which appears to have overcome several drawbacks of the current thienopyridines. Its unique pharmacokinetic and pharmacodynamic profiles result in an inhibition of platelet aggregation that is rapid, high, consistent, and less susceptible to interpatient variability than currently available P2Y12 inhibitors. In addition, ticagrelor offers a potential mortality advantage not apparent with current agents. Although questions regarding the nature, magnitude, and clinical significance of several observed adverse effects (dyspnea and ventricular pauses) remain unanswered, it appears that ticagrelor may represent a significant advancement over currently available oral antiplatelet agents.
机译:摘要:抗血小板药物,特别是噻吩并吡啶类药物的使用,已成为治疗患有急性冠脉综合征的患者的标准治疗方法。这些药物通过永久结合至表面P2Y12受体并阻断血小板之间的下游纤维蛋白原交联而不可逆地抑制血小板,从而导致聚集和血栓形成。但是,当前可用的治疗选择受到与其他药物的潜在相互作用,肝向活性代谢物转化的缓慢,遗传抗性和狭窄的治疗安全性的限制。为了克服这些缺点,有兴趣开发噻吩并吡啶的替代物。最近的研究包括替卡格雷,P2Y12血小板受体的可逆抑制剂,它似乎已经克服了目前噻吩并吡啶类药物的几个缺点。其独特的药代动力学和药效学特征导致血小板聚集的抑制作用比现有的P2Y12抑制剂迅速,高,一致,并且不易受到患者间变异的影响。此外,替卡格洛具有潜在的死亡率优势,而目前的药物尚不明显。尽管关于几种观察到的不良反应(呼吸困难和心室停顿)的性质,大小和临床意义的问题仍未得到解答,但似乎替卡格雷已经优于目前口服的口服抗血小板药。

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