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口服 P2Y12 受体抑制剂负荷剂量:粉碎还是不粉碎?

Loading with Oral P2Y12 Receptor Inhibitors: To Crush or Not to Crush?

机构信息

2nd Department of Cardiology, Attikon University Hospital, National and Kapodistrian University of Athens Medical School, Athens, Greece.

Department of Cardiology, General Hospital of Attica ''KAT'', Athens, Greece.

出版信息

Thromb Haemost. 2019 Jul;119(7):1037-1047. doi: 10.1055/s-0039-1688790. Epub 2019 May 12.

DOI:10.1055/s-0039-1688790
PMID:31079416
Abstract

Oral P2Y receptor inhibitors represent a mainstay treatment in patients with acute coronary syndrome and those undergoing percutaneous coronary intervention. In the setting of ST-elevation myocardial infarction, when early platelet inhibition is highly desirable, the onset of action of oral P2Y receptor inhibitors is, however, delayed, likely due to delayed drug absorption. Crushing the tablets, which are to be used for patient loading with an oral P2Y receptor inhibitor, has been shown to provide earlier platelet inhibition than standard, integral tablets administration. Chewed ticagrelor tablets may also result in a similar effect. Such findings should be interpreted with caution, mainly due to the small number of patients enrolled and the nature (pharmacodynamic/pharmacokinetic) of the respective studies. Furthermore, in patients with out-of-hospital cardiac arrest, who remain comatose, crushing tablets is commonly applied in clinical practice for platelet P2Y receptor inhibition. In this review, we focus on current evidence regarding the role of crushed P2Y receptor inhibitor pills, analyzing clinical scenarios where most of the promise exists along with future expectations from this type of formulation. Large randomized studies are needed to draw firm conclusions regarding the clinical benefit of 'crushing' over the usual 'not-crushing' practice.

摘要

口服 P2Y 受体抑制剂是急性冠状动脉综合征和经皮冠状动脉介入治疗患者的主要治疗方法。在 ST 段抬高型心肌梗死的情况下,早期抑制血小板非常重要,但口服 P2Y 受体抑制剂的作用起效较慢,可能是由于药物吸收延迟。研究表明,粉碎用于患者负荷剂量的口服 P2Y 受体抑制剂的片剂,比标准完整片剂给药能更早地抑制血小板。咀嚼替格瑞洛片剂也可能产生类似的效果。这些发现应谨慎解释,主要是因为纳入的患者数量较少,以及各自研究的性质(药效学/药代动力学)。此外,对于在院外心脏骤停后仍处于昏迷状态的患者,临床上通常会粉碎片剂以抑制血小板 P2Y 受体。在这篇综述中,我们重点关注关于粉碎 P2Y 受体抑制剂片剂作用的现有证据,分析存在最大希望的临床情况,以及这种剂型的未来预期。需要进行大型随机研究,才能就“粉碎”相对于常规“不粉碎”实践的临床获益得出明确结论。

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引用本文的文献

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J Am Heart Assoc. 2019 Dec 3;8(23):e014498. doi: 10.1161/JAHA.119.014498. Epub 2019 Nov 26.