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心血管疾病中的P2Y拮抗剂——在预防缺血事件与引发出血之间寻求最佳平衡

P2Y Antagonists in Cardiovascular Disease-Finding the Best Balance Between Preventing Ischemic Events and Causing Bleeding.

作者信息

Fernando Himawan, McFadyen James D, Wang Xiaowei, Shaw James, Stub Dion, Peter Karlheinz

机构信息

Atherothrombosis and Vascular Biology Laboratory, Baker Heart and Diabetes Institute, Melbourne, VIC, Australia.

Department of Medicine, Monash University, Melbourne, VIC, Australia.

出版信息

Front Cardiovasc Med. 2022 May 12;9:854813. doi: 10.3389/fcvm.2022.854813. eCollection 2022.

DOI:10.3389/fcvm.2022.854813
PMID:35647068
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9133423/
Abstract

Dual antiplatelet therapy comprising of aspirin and oral P2Y receptor antagonists are an established cornerstone of therapy in acute coronary syndromes and percutaneous coronary intervention. As a result, the platelet P2Y receptor remains a key therapeutic target in cardiovascular medicine since pharmacological antagonists were first developed in the 1990's. With a greater understanding of platelet biology and the role played by the P2Y receptor in the amplification of platelet activation and thrombus formation, there has been progressive refinement in the development of P2Y receptor antagonists with greater potency and consistency of antiplatelet effect. However, challenges remain in the utilization of these agents particularly in balancing the need for greater protection from ischemic events whilst minimizing the bleeding risk and present a real opportunity for the institution of individualized medicine. Future drug developments will provide clinicians with greater avenues to achieve this.

摘要

由阿司匹林和口服P2Y受体拮抗剂组成的双联抗血小板治疗是急性冠状动脉综合征和经皮冠状动脉介入治疗中既定的治疗基石。因此,自20世纪90年代首次开发出药理拮抗剂以来,血小板P2Y受体仍然是心血管医学中的关键治疗靶点。随着对血小板生物学以及P2Y受体在血小板活化和血栓形成放大过程中所起作用的深入了解,P2Y受体拮抗剂的开发不断取得进展,其抗血小板作用的效力和一致性更强。然而,在使用这些药物时仍存在挑战,尤其是在平衡预防缺血事件的需求与将出血风险降至最低之间,这为个体化医疗的实施提供了切实机会。未来的药物开发将为临床医生提供更多实现这一目标的途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a42/9133423/b2e91de6e2cf/fcvm-09-854813-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a42/9133423/2bb3613502bf/fcvm-09-854813-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a42/9133423/b2e91de6e2cf/fcvm-09-854813-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a42/9133423/2bb3613502bf/fcvm-09-854813-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a42/9133423/b2e91de6e2cf/fcvm-09-854813-g002.jpg

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