Newer agents in antiplatelet therapy: a review.
Newer agents in antiplatelet therapy: a review.
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DOI：
10.2147/jbm.s25421
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发表时间：
2012
影响因子：
2
通讯作者：
Holinstat M
中科院分区：
文献类型：
--
作者：
Yeung J;Holinstat M
抗血小板治疗仍然是预防心肌梗死、缺血和中风等病理生理条件下异常血小板活化的主要方法。尽管抗血小板治疗方法有了显著的进步，但阿司匹林仍然是临床治疗的金标准。由于安全性、有效性和耐受性的限制，许多抗血小板抑制剂无法用于患者。在患者中观察到的出血风险增加和复发性动脉血栓形成的意外发生率阻碍了上级下一代抗血小板治疗的开发。由于代谢、起效时间和可逆性的变异性，药代动力学和药效学特征也限制了目前使用的许多抗血小板抑制剂的有效性。为解决其中一些缺点，开发新型抗血小板治疗的重点工作已经产生了大量潜在的抗血小板药物，这些药物靶向血小板中的酶（磷酸二酯酶、环氧合酶）、受体（嘌呤能、胰高血糖素、蛋白酶激活受体、血栓素）和糖蛋白（αIIbβ3、GPVI、vWF、GPIb）。对被证明上级阿司匹林的新型抗血小板治疗方法的验证和研究仍在进行中，应该会产生更好的药效学特征，与目前使用的方法相比，不良副作用更少。
Antiplatelet therapy remains the mainstay in preventing aberrant platelet activation in pathophysiological conditions such as myocardial infarction, ischemia, and stroke. Although there has been significant advancement in antiplatelet therapeutic approaches, aspirin still remains the gold standard treatment in the clinical setting. Limitations in safety, efficacy, and tolerability have precluded many of the antiplatelet inhibitors from use in patients. Unforeseen incidences of increased bleeding risk and recurrent arterial thrombosis observed in patients have hampered the development of superior next generation antiplatelet therapies. The pharmacokinetic and pharmacodynamic profiles have also limited the effectiveness of a number of antiplatelet inhibitors currently in use due to variability in metabolism, time to onset, and reversibility. A focused effort in the development of newer antiplatelet therapies to address some of these shortcomings has resulted in a significant number of potential antiplatelet drugs which target enzymes (phosphodiesterase, cyclooxygenase), receptors (purinergic, prostaglandins, protease-activated receptors, thromboxane), and glycoproteins (αIIbβ3, GPVI, vWF, GPIb) in the platelet. The validation and search for newer antiplatelet therapeutic approaches proven to be superior to aspirin is still ongoing and should yield a better pharmacodynamic profile with fewer untoward side-effects to what is currently in use today.