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血小板抑制剂的进展:靶点是 P2Y12 受体。

Progress in platelet blockers: the target is the P2Y12 receptor.

机构信息

Cardiovascular and Thoracic Section, Department of Anesthesiology and Critical Care, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA.

出版信息

J Cardiothorac Vasc Anesth. 2013 Jun;27(3):620-4. doi: 10.1053/j.jvca.2013.01.008.

DOI:10.1053/j.jvca.2013.01.008
PMID:23672863
Abstract

The considerable progress in P2Y12-platelet blockers has important perioperative implications due to a family of novel agents beyond clopidogrel. Although prasugrel is more potent than clopidogrel due to more efficient hepatic metabolism, it is limited clinically by its irreversibility and bleeding risks. Ticagrelor, as the first approved direct and reversible oral P2Y12 blocker, still is limited clinically by its novel side-effect profile. Intravenous reversible P2Y12 blockade is possible now with both cangrelor and elinogrel, although both agents are still in clinical development. Furthermore, elinogrel offers the possibility of both oral and parenteral P2Y12 blockade with a single agent. Future trials likely will continue to evaluate and compare the safety and efficacy of these agents in multiple clinical settings, including the perioperative period.

摘要

由于除氯吡格雷以外的新型药物家族,P2Y12 血小板抑制剂取得了相当大的进展,这对围手术期具有重要意义。虽然普拉格雷由于更有效的肝脏代谢作用比氯吡格雷更有效,但由于其不可逆性和出血风险,在临床上受到限制。替卡格雷洛作为第一个被批准的直接、可逆的口服 P2Y12 抑制剂,由于其新颖的副作用谱,在临床上仍然受到限制。现在可以使用坎格瑞洛和依诺格雷洛进行静脉内可逆的 P2Y12 阻断,但这两种药物仍处于临床开发阶段。此外,依诺格雷洛有可能通过单一药物同时进行口服和静脉内 P2Y12 阻断。未来的试验可能会继续评估和比较这些药物在多个临床环境中的安全性和疗效,包括围手术期。

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