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西洛他唑与直接经皮冠状动脉介入治疗:虚幻还是较好的选择?

Cilostazol and primary-PCI: mirage or good alternative?

机构信息

Department of Cardiovascular Medicine, Catholic University of the Sacred Heart, Rome, Italy.

出版信息

Curr Vasc Pharmacol. 2012 Jul;10(4):468-71. doi: 10.2174/157016112800812854.

DOI:10.2174/157016112800812854
PMID:22329616
Abstract

Oral anti-platelet agents targeting the platelet P2Y12 receptor are an integral component of treating patients undergoing percutaneous coronary interventions. Advancements in the design of stents and catheters are pushing the technique towards treatment of high risk lesions whose failure would expose patients to catastrophic events. Success of these complex procedures largely lays on efficacy of anti-platelet drugs and the limitation of stent restenosis and/or thrombosis. Clopidogrel has been the most commonly used agent in this respect worldwide. However, there are certain shortcomings of clopidogrel, the most important of which is the wide response variability of platelet inhibition. Thus, clinicians are facing challenges in treating patients where high inhibition of platelets is necessary and the response to clopidogrel may be insufficient. In the last few years, cilostazol, a phosphodiesterase (PDE) 3 inhibitor, has been tested in the setting of acute coronary syndromes: it exerts not only anti-platelet actions, but also pleiotropic effects, including inhibition on neointimal hyperplasia, therefore preventing both stent restenosis and thrombosis. Therefore, cilostazol may be considered, on top of our current anti-platelet therapy, as a potential candidate to achieve optimal platelet inhibition especially in patients undergoing primary-PCI (p-PCI) or high risk procedures. This review will focus on the pharmacological characteristics of cilostazol and the initial evidences that support the use of this drug in the setting of p-PCI.

摘要

针对血小板 P2Y12 受体的口服抗血小板药物是治疗接受经皮冠状动脉介入治疗患者的重要组成部分。支架和导管设计的进步正在推动该技术治疗高危病变,如果这些病变治疗失败,患者将面临灾难性事件。这些复杂手术的成功在很大程度上取决于抗血小板药物的疗效以及支架再狭窄和/或血栓形成的限制。氯吡格雷在这方面是世界范围内使用最广泛的药物。然而,氯吡格雷存在一定的缺陷,最重要的是血小板抑制的广泛反应变异性。因此,临床医生在治疗需要高度抑制血小板且对氯吡格雷反应可能不足的患者时面临挑战。在过去的几年中,磷酸二酯酶(PDE)3 抑制剂西洛他唑已在急性冠状动脉综合征中进行了测试:它不仅具有抗血小板作用,而且还具有多种作用,包括抑制内膜增生,从而预防支架再狭窄和血栓形成。因此,西洛他唑除了我们目前的抗血小板治疗外,还可以被视为一种潜在的候选药物,特别是在接受直接经皮冠状动脉介入治疗(p-PCI)或高危手术的患者中,以实现最佳的血小板抑制。本文综述将重点介绍西洛他唑的药理学特征,并支持在 p-PCI 中使用该药的初步证据。

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Cilostazol and primary-PCI: mirage or good alternative?西洛他唑与直接经皮冠状动脉介入治疗:虚幻还是较好的选择?
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Cilostazol reduces the progression of carotid intima-media thickness without increasing the risk of bleeding in patients with acute coronary syndrome during a 2-year follow-up.在一项为期2年的随访中,西洛他唑可减缓急性冠脉综合征患者颈动脉内膜中层厚度的进展,且不会增加出血风险。
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Cilostazol could ameliorate platelet responsiveness to clopidogrel in patients undergoing primary percutaneous coronary intervention.西洛他唑可改善接受直接经皮冠状动脉介入治疗患者的血小板对氯吡格雷的反应性。
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Optimizing of thienopyridine therapy by multiple electrode platelet aggregometry in clopidogrel low responders undergoing PCI.经皮冠状动脉介入治疗中氯吡格雷低反应者应用多电极血小板聚集仪优化噻吩吡啶治疗。
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Use of cilostazol in percutaneous coronary interventions.西洛他唑在经皮冠状动脉介入治疗中的应用。
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引用本文的文献

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The efficacy and safety of cilostazol as an alternative to aspirin in Chinese patients with aspirin intolerance after coronary stent implantation: a combined clinical study and computational system pharmacology analysis.西洛他唑作为冠状动脉支架植入术后阿司匹林不耐受的中国患者替代阿司匹林的疗效和安全性:一项联合临床研究和计算系统药理学分析。
Acta Pharmacol Sin. 2018 Feb;39(2):205-212. doi: 10.1038/aps.2017.85. Epub 2017 Sep 21.
2
Cilostazol Induces PGI2 Production via Activation of the Downstream Epac-1/Rap1 Signaling Cascade to Increase Intracellular Calcium by PLCε and to Activate p44/42 MAPK in Human Aortic Endothelial Cells.西洛他唑通过激活下游Epac-1/Rap1信号级联反应诱导前列环素I2生成,从而通过磷脂酶Cε增加细胞内钙,并激活人主动脉内皮细胞中的p44/42丝裂原活化蛋白激酶。
PLoS One. 2015 Jul 16;10(7):e0132835. doi: 10.1371/journal.pone.0132835. eCollection 2015.
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Effects of cilostazol on the progression and regression of symptomatic intracranial artery stenosis: it reduces the risk of ischemic stroke.西洛他唑对有症状颅内动脉狭窄进展和转归的影响:它降低缺血性卒中风险。
Neural Regen Res. 2015 Apr;10(4):667-72. doi: 10.4103/1673-5374.155443.