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P2Y12受体拮抗剂之间转换的药效学及临床意义:实践考量

Pharmacodynamic and clinical implications of switching between P2Y12 receptor antagonists: considerations for practice.

作者信息

Bagai Akshay, Chua Doson, Cohen Eric A, Saw Jacqueline, Verma Subodh, Vijayaraghavan Ram, Welsh Robert, Fitchett David

机构信息

From the *Terrence Donnelly Heart Centre, St. Michael's Hospital, University of Toronto, Toronto, ON, Canada; †St. Paul's Hospital, University of British Columbia, Vancouver, BC, Canada; ‡Sunnybrook and Women's Health Sciences Center, University of Toronto, Toronto, ON, Canada; §Vancouver General Hospital, University of British Columbia, Vancouver, BC, Canada; ¶Division of Cardiac Surgery, Keenan Research Centre for Biomedical Science, Li Ka Shing Knowledge Institute of St. Michael's Hospital, University of Toronto, Toronto, ON, Canada; ‖Rouge Valley Health System, Toronto, ON, Canada; and **Mazankowski Heart Institute, University of Alberta, Edmonton, Canada.

出版信息

Crit Pathw Cardiol. 2014 Dec;13(4):156-8. doi: 10.1097/HPC.0000000000000030.

Abstract

Dual antiplatelet therapy with aspirin and a P2Y12 receptor antagonist, either clopidogrel or the newer more potent agents prasugrel or ticagrelor, is standard therapy in patients receiving a coronary stent and those with a recent acute coronary syndrome. Switching antiplatelet drug regimen may be required in some patients for efficacy, safety, adherence, and cost considerations. However, there are potential concerns when switching from one agent to another that gaps in effective antiplatelet inhibition could lead to thrombotic events, and overlap of agents might cause excessive platelet inhibition thereby increasing the risk of bleeding. This review considers pharmacodynamic and clinical data to guide clinicians when switching between antiplatelet drugs is considered. Loading dose of the new agent should be considered in nearly all situations to avoid any possible gap in adequate platelet inhibition, as overlap of the 2 agents is unlikely to result in bleeding in excess of that with the more potent drug.

摘要

对于接受冠状动脉支架植入术的患者以及近期发生急性冠状动脉综合征的患者,阿司匹林联合一种P2Y12受体拮抗剂(氯吡格雷或更新的、效力更强的药物普拉格雷或替格瑞洛)进行双重抗血小板治疗是标准疗法。出于疗效、安全性、依从性和成本等方面的考虑,部分患者可能需要更换抗血小板药物方案。然而,从一种药物转换为另一种药物时存在一些潜在问题,有效的抗血小板抑制作用出现间隙可能会导致血栓形成事件,而药物重叠可能会导致血小板过度抑制,从而增加出血风险。本综述探讨药效学和临床数据,以指导临床医生在考虑更换抗血小板药物时做出决策。几乎在所有情况下都应考虑使用新药的负荷剂量,以避免足够的血小板抑制出现任何可能的间隙,因为两种药物重叠不太可能导致出血超过使用效力更强药物时的出血情况。

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