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新型抗血小板药物:为何需要它们。

New antiplatelet agents: why they are needed.

机构信息

Immunohematology and Transfusion Center, Department of Pathology and Laboratory Medicine, University Hospital of Parma, Italy.

出版信息

Eur J Intern Med. 2009 Dec;20(8):733-8. doi: 10.1016/j.ejim.2009.09.005. Epub 2009 Oct 1.

DOI:10.1016/j.ejim.2009.09.005
PMID:19892299
Abstract

Despite recent advances in the treatment of acute coronary syndromes (ACS), including dual antiplatelet therapy with aspirin and a thienopyridine during the acute phase and for secondary prevention, this condition remains a leading cause of morbidity and mortality. The limitations of the currently available antiplatelet agents have triggered the development of newer drugs. In this review we summarize the mechanisms of actions and results of current clinical trials of novel antiplatelet agents. These include prasugrel, a thienopyridine prodrug which has a mechanism similar to that of clopidogrel but superior pharmacokinetic features; ticagrelor, a non-thienopyridine that binds reversibly to the platelet P2Y(12) receptor; cangrelor, an intravenously administered analog of ticagrelor; the thrombin receptor antagonist SCH 53048; and terutroban (S18886), a thromboxane A(2) receptor inhibitor.

摘要

尽管急性冠状动脉综合征 (ACS) 的治疗方法最近有所进展,包括在急性期和二级预防中使用阿司匹林和噻吩吡啶的双联抗血小板治疗,但这种情况仍然是发病率和死亡率的主要原因。目前可用的抗血小板药物存在局限性,这促使开发了新型药物。在这篇综述中,我们总结了新型抗血小板药物的作用机制和当前临床试验结果。这些药物包括普拉格雷,一种噻吩吡啶前体药物,其作用机制与氯吡格雷相似,但药代动力学特征更优;替卡格雷洛,一种可逆结合血小板 P2Y(12)受体的非噻吩吡啶药物;坎格雷洛,替卡格雷洛的静脉内类似物;血栓素受体拮抗剂 SCH 53048;和替罗非班(S18886),一种血栓素 A(2)受体抑制剂。

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New antiplatelet agents: why they are needed.新型抗血小板药物:为何需要它们。
Eur J Intern Med. 2009 Dec;20(8):733-8. doi: 10.1016/j.ejim.2009.09.005. Epub 2009 Oct 1.
2
Ticagrelor--a new platelet aggregation inhibitor in patients with acute coronary syndromes. An improvement of other inhibitors?替格瑞洛--急性冠脉综合征患者的新型血小板聚集抑制剂。能改善其他抑制剂吗?
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New antiplatelet drugs: beyond aspirin and clopidogrel.新型抗血小板药物:超越阿司匹林和氯吡格雷。
Int J Clin Pract. 2009 May;63(5):776-89. doi: 10.1111/j.1742-1241.2009.02058.x.
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Update on antiplatelet therapy in acute coronary syndromes: what do new drugs bring into clinical practice?急性冠脉综合征的抗血小板治疗进展:新药为临床实践带来了什么?
Am J Cardiovasc Drugs. 2009;9 Suppl 1:13-7. doi: 10.2165/1153164-S0-000000000-00000.
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Clinical overview of promising nonthienopyridine antiplatelet agents.有前景的非噻吩并吡啶类抗血小板药物的临床概述
Am Heart J. 2008 Aug;156(2 Suppl):S23-8. doi: 10.1016/j.ahj.2008.06.006.
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[Novel agents in antiplatelet therapy].[抗血小板治疗中的新型药物]
Turk Kardiyol Dern Ars. 2010 Jul;38(5):369-78.
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Advances in antiplatelet therapy: agents in clinical development.抗血小板治疗的进展:处于临床开发阶段的药物
Am J Cardiol. 2009 Feb 2;103(3 Suppl):40A-51A. doi: 10.1016/j.amjcard.2008.11.023.
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New antiplatelet agents and the role of platelet function testing in acute coronary syndromes.新型抗血小板药物与血小板功能检测在急性冠脉综合征中的作用。
Clin Ther. 2013 Aug;35(8):1064-8. doi: 10.1016/j.clinthera.2013.07.429.
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Novel antiplatelet agents in development: prasugrel, ticagrelor, and cangrelor and beyond.正在研发的新型抗血小板药物:普拉格雷、替格瑞洛和坎格瑞洛及其他。
Am J Ther. 2009 Sep-Oct;16(5):451-8. doi: 10.1097/MJT.0b013e318187de4f.
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Advances in antiplatelet therapy for ACS and PCI.急性冠状动脉综合征和经皮冠状动脉介入治疗的抗血小板治疗进展
J Interv Cardiol. 2008 Dec;21 Suppl 1:S18-24. doi: 10.1111/j.1540-8183.2008.00409.x.

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