angrelor -扩大急性冠脉综合征患者的治疗选择。

Cardiology journal Pub Date : 2024-01-01 Epub Date: 2023-11-15 DOI:10.5603/cj.96076
Jacek Kubica, Piotr Adamski, Sławomir Dobrzycki, Robert Gajda, Mariusz Gąsior, Marek Gierlotka, Miłosz Jaguszewski, Jacek Legutko, Maciej Lesiak, Eliano P Navarese, Piotr Niezgoda, Małgorzata Ostrowska, Tomasz Pawłowski, Agnieszka Tycińska, Julia M Umińska, Adam Witkowski, Robert Gil
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引用次数: 0

摘要

angrelor是唯一的静脉注射P2Y12受体拮抗剂。它是一种三磷酸腺苷类似物,选择性地、直接地、可逆地结合血小板P2Y12受体,发挥其抗聚集作用。canrelor的特点是线性,剂量依赖的药代动力学和快速起效,提供超过90%的有效血小板抑制。angrelor被内皮内核苷酸酶快速代谢;因此,它的半衰期为2.9 - 5.5分钟,其抗血小板作用在60 - 90分钟内消退。来自三个关键的cangrelor试验(CHAMPION PLATFORM, CHAMPION PCI和CHAMPION PHOENIX)的数据表明,cangrelor以轻度出血为代价,降低了经皮冠状动脉介入治疗过程中围手术期血栓并发症的风险。其独特的药理学特性使其克服了口服P2Y12受体抑制剂的局限性,主要与这些药物的生物利用度延迟和降低以及抗血小板作用有关,这在急性冠脉综合征的情况下经常观察到。理论上从angrelor获益最多的患者亚组包括口服P2Y12受体拮抗剂的药代动力学和药效学最受干扰的患者,即st段抬高型心肌梗死患者、接受阿片类药物治疗的患者、轻度治疗性低温患者或心源性休克患者。如果手术患者需要桥接,Cangrelor也可能有用。根据目前的指南,在急性和稳定的情况下,P2Y12受体inhibitor-naïve患者接受经皮冠状动脉介入治疗时,可以考虑使用cangrelor。
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Cangrelor - Expanding therapeutic options in patients with acute coronary syndrome.

Cangrelor is the only intravenous P2Y12 receptor antagonist. It is an adenosine triphosphate analog that selectively, directly, and reversibly binds to the platelet P2Y12 receptors exerting its antiaggregatory effect. Cangrelor is characterized by linear, dose-dependent pharmacokinetics and rapid onset of action providing potent platelet inhibition exceeding 90%. Cangrelor is rapidly metabolized by endothelial endonucleotidase; thus, its half-life is 2.9 to 5.5 min, and its antiplatelet effect subsides within 60 to 90 min. Data originating from three pivotal cangrelor trials (CHAMPION PLATFORM, CHAMPION PCI, and CHAMPION PHOENIX) indicate that cangrelor reduces the risk of periprocedural thrombotic complications during percutaneous coronary intervention at the expense of mild bleedings. Its unique pharmacological properties allow it to overcome the limitations of oral P2Y12 receptor inhibitors, mainly related to the delayed and decreased bioavailability and antiplatelet effect of these agents, which are often observed in the setting of acute coronary syndrome. Subgroups of patients who could theoretically benefit the most from cangrelor include those in whom pharmacokinetics and pharmacodynamics of oral P2Y12 receptor antagonists are most disturbed, namely patients with ST-segment elevation myocardial infarction, those treated with opioids, with mild therapeutic hypothermia, or in cardiogenic shock. Cangrelor could also be useful if bridging is required in patients undergoing surgery. According to the current guidelines cangrelor may be considered in P2Y12 receptor inhibitor-naïve patients undergoing percutaneous coronary intervention in both acute and stable settings.

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