Rikken Sem A O F, Storey Robert F, Andreotti Felicita, Clemmensen Peter, Ten Berg Jurriën M
Department of Cardiology, St. Antonius Hospital, Nieuwegein, The Netherlands.
School for Cardiovascular Diseases, Cardiovascular Research Institute Maastricht, Maastricht University Medical Center, Maastricht, The Netherlands.
Thromb Haemost. 2023 Feb;123(2):150-158. doi: 10.1055/s-0042-1753479. Epub 2022 Sep 8.
Oral inhibitors of the platelet P2Y receptor are indispensable in the treatment of ST-elevation myocardial infarction (STEMI), improving outcomes and even reducing mortality in some studies. However, these drugs are limited by delayed absorption and suboptimal platelet inhibition at the time of primary percutaneous coronary intervention. Despite efforts to achieve faster and more sustained platelet inhibition, strategies such as prehospital administration, higher loading doses, and crushed formulations have not led to improved coronary reperfusion. Parenteral glycoprotein IIb/IIIa inhibitors act sooner and are more potent than oral P2Y inhibitors, but their use has been limited by the increased risk of major bleeding and thrombocytopenia. Hence, there is a clinical need to refine drugs that deliver rapid, effective, yet safe platelet inhibition in the setting of STEMI. Novel parenteral antiplatelet drugs, such as cangrelor, selatogrel, and zalunfiban, have been recently developed to achieve rapid, potent antiplatelet effects while preserving hemostasis. We provide a description of currently available parenteral antiplatelet agents and of those in clinical development for prehospital administration in STEMI patients.
血小板P2Y受体口服抑制剂在ST段抬高型心肌梗死（STEMI）的治疗中不可或缺，在一些研究中可改善预后甚至降低死亡率。然而，这些药物存在吸收延迟以及在直接经皮冠状动脉介入治疗时血小板抑制效果欠佳的问题。尽管人们努力实现更快且更持久的血小板抑制，但诸如院前给药、更高负荷剂量以及碾碎制剂等策略并未带来冠状动脉再灌注的改善。胃肠外糖蛋白IIb/IIIa抑制剂起效更快且比口服P2Y抑制剂更有效，但其使用受到大出血和血小板减少风险增加的限制。因此，临床上需要优化在STEMI情况下能实现快速、有效且安全的血小板抑制的药物。新型胃肠外抗血小板药物，如坎格雷洛、塞拉托格雷和扎伦非班，最近已被研发出来，以在保持止血功能的同时实现快速、强效的抗血小板作用。我们描述了目前可用的胃肠外抗血小板药物以及正在进行临床开发用于STEMI患者院前给药的药物。
