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心血管疾病和缺血性卒中中的替格瑞洛抵抗

Ticagrelor Resistance in Cardiovascular Disease and Ischemic Stroke.

作者信息

He Song, Lin Yapeng, Tan Quandan, Mao Fengkai, Chen Kejie, Hao Junli, Le Weidong, Yang Jie

机构信息

Department of Neurology, The First Affiliated Hospital of Chengdu Medical College, Chengdu 610072, China.

International Clinical Research Center, Chengdu Medical College, Chengdu 610072, China.

出版信息

J Clin Med. 2023 Feb 1;12(3):1149. doi: 10.3390/jcm12031149.

Abstract

Ticagrelor, acting as a reversible platelet aggregation inhibitor of P2Y12 receptors (P2Y12R), is regarded as one of the first-line antiplatelet drugs for acute cardiovascular diseases. Though the probability of ticagrelor resistance is much lower than that of clopidogrel, there have been recent reports of ticagrelor resistance. In this review, we summarized the clinical application of ticagrelor and then presented the criteria and current status of ticagrelor resistance. We further discussed the potential mechanisms for ticagrelor resistance in terms of drug absorption, metabolism, and receptor action. In conclusion, the incidences of ticagrelor resistance fluctuated between 0 and 20%, and possible mechanisms mainly arose from its absorption and receptor action. Specifically, a variety of factors, such as the drug form of ticagrelor, gut microecology, and the expression and function of P-glycoprotein (P-gp) and P2Y12R, have been shown to be associated with ticagrelor resistance. The exact mechanisms of ticagrelor resistance warrant further exploration, which may contribute to the diagnosis and treatment of ticagrelor resistance.

摘要

替格瑞洛作为一种P2Y12受体(P2Y12R)的可逆性血小板聚集抑制剂,被视为急性心血管疾病的一线抗血小板药物之一。尽管替格瑞洛抵抗的发生率远低于氯吡格雷,但近期已有关于替格瑞洛抵抗的报道。在本综述中,我们总结了替格瑞洛的临床应用,随后阐述了替格瑞洛抵抗的标准及现状。我们进一步从药物吸收、代谢及受体作用方面探讨了替格瑞洛抵抗的潜在机制。总之,替格瑞洛抵抗的发生率在0%至20%之间波动,其可能机制主要源于药物吸收及受体作用。具体而言,多种因素,如替格瑞洛的药物剂型、肠道微生态以及P-糖蛋白(P-gp)和P2Y12R的表达与功能,已被证明与替格瑞洛抵抗相关。替格瑞洛抵抗的确切机制有待进一步探索,这可能有助于替格瑞洛抵抗的诊断与治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/920f/9918175/77026871ed5f/jcm-12-01149-g001.jpg

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