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首页> 外文期刊>Current Pharmaceutical Design >Direct Thrombin Inhibitors for the Treatment of Acute Coronary Syndromes and During Percutaneous Coronary Interventions
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Direct Thrombin Inhibitors for the Treatment of Acute Coronary Syndromes and During Percutaneous Coronary Interventions

机译:直接凝血酶抑制剂治疗急性冠状动脉综合征和经皮冠状动脉介入治疗期间

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摘要

As acute coronary syndromes are principally sustained by plaque complication and subsequent thrombus formation, anticoagulant therapy plays a central role in avoiding ischemic events; its main targets are thrombin activity and generation. Despite its limitations, such as its scarce ability to activate bound thrombin and its unpredictable pharmacological response, heparin is the most widely uzed drug for this purpose. Direct thrombin inhibitors are biologically superior to heparin principally because they inhibit clot-bound and circulating thrombin without interacting with other plasma proteins. Their clinical role in acute coronary syndromes and during coronary intervention has been tested in several trials.nnThis article overviews the principal trials involving active-site direct thrombin inhibitors in acute coronary syndrome and during coronary intervention and compares their efficacy and safety with unfractionated heparin. It also describes ongoing trials and analyzes further clinical developments such as their use in addition to the glycoprotein IIb/IIIa inhibitors and the potential advantage possible with new agents orally administered.
机译:由于急性冠脉综合征主要由斑块并发症和随后的血栓形成所维持,因此抗凝治疗在避免缺血事件中起着核心作用。它的主要目标是凝血酶活性和生成。尽管有其局限性,例如缺乏激活结合凝血酶的能力和不可预测的药理作用,肝素仍是使用最广泛的为此目的使用的药物。直接凝血酶抑制剂在生物学上优于肝素,主要是因为它们抑制凝块结合和循环的凝血酶而不与其他血浆蛋白相互作用。在一些试验中已经测试了它们在急性冠状动脉综合征中的临床作用。nn本文概述了涉及活性部位直接凝血酶抑制剂在急性冠脉综合征和冠状动脉介入治疗中的主要试验,并比较了普通肝素的疗效和安全性。它还描述了正在进行的试验并分析了进一步的临床发展,例如除糖蛋白IIb / IIIa抑制剂外的使用以及口服新药可能带来的潜在优势。

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