血小板聚集是由于其表面GpIIb/IIIa 受体偶联相关,因此出现了特异性GpIIb/IIIa受体拮抗剂替罗非班。但GpIIb/IIIa受体 偶联也受P2Y12受体影响。波立维通过选择性抑制二磷酸腺苷(ADP)与血小板P2Y12受体受体结合,从而阻断ADP介导的糖蛋白GPⅡb/Ⅲa复合物的活化,减少血小板之间的相互粘附,降低血栓形成的风险。
比波立维更早的药物噻吩吡啶存在时间很短即被淘汰,目前均为二代噻吩吡啶类药物,包括氯吡格雷,普拉格雷,三者均需进过肝内酶代谢后产生生物活性。而非噻吩吡啶类药物坎格雷洛,为无活性前体药,可静脉直接使用,因此常用于ACS行PCI患者。替格瑞洛另一种非噻吩吡啶药物,入体内后仍需肝脏转换,为口服制剂。几种药物特点见下图:
美国胸科医师协会(ACCP)2023年更新了围手术期抗血小板指南,并给出一张简洁明了的图,详细指南如下:
(1)小手术例如皮肤科,眼科,牙科等小手术,如仅服用ASA 或P2Y12抑制剂,可不停用,如合用ASA和P2Y12,可停用其中任何一种。
(2)In patients receiving ASA who are undergoing elective non-cardiac surgery, wesuggest ASA continuationover ASA interruption. In patients receiving ASA therapy who are undergoing elective surgery and require ASA interruption, we suggeststopping ASA <7 daysinstead of 7 to 10 days before the surgery. In patients receiving clopidogrel who are undergoing an elective non-cardiac surgery, we suggeststopping clopidogrel 5 daysinstead of 7 to 10 days before the surgery,stopping ticagrelor 3 to 5 daysinstead of 7 to 10 days before the surgery,stopping prasugrel 7 daysinstead of 7 to 10 days before the surgery.In patients who require antiplatelet drug interruptionwe suggest to resume antiplatelet drugs <24 hoursinstead of > 24 hours after the surgery/procedure.不建议在术前停用阿司匹林(颅内手术,脊柱手术除外),如必须停用,可停用<7天,如服用波立维,只需停用五天,替卡格雷只需停用3-5天,普拉格雷停用7天,并在手术结束后24小时即可恢复使用)
(3)围手术期没必要监测血小板功能
(4)In patients receiving ASA and a P2Y12 inhibitor with coronary stents placed within the last 6 to 12 weeks who are undergoing an elective surgery, we suggest either continuation of both antiplatelet agents or stopping one antiplatelet agent within 7 to 10 days of surgery. within the last 3 to 12 months and are undergoing an elective surgery, we suggest stopping the P2Y12 inhibitor prior to surgery over continuation of the P2Y12 inhibitor。冠脉支架植入后6-12周患者服用双抗,建议停用其中一种药物7-10天,也可不必停药。冠脉支架植入后3-12月,建议停用P2Y12抑制剂
(5)In patients with coronary stents who require continued dual antiplatelet therapy, we suggest delaying an elective surgery/procedure over not delaying the surgery/procedure. In patients with coronary stents who require interruption of antiplatelet drugs for an elective surgery, we suggest against routine bridging therapy with a glycoprotein IIb/IIIa inhibitor, cangrelor, or LMWH over routine use of bridging therapy(择期手术患者不能停用双抗者,建议延期手术。如必须手术,不建议使用IIb/IIIa受体拮抗剂,低分子肝素等桥接,而使用常规肝素桥接)
Anesthesiology最新一期综述概括了上述所有ADP抑制剂的作用特点以及围手术期出血如何处理,全文链接点击阅读原文。
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