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Desirudin: A review of the pharmacology and clinical application for the prevention of deep vein thrombosis

机译:Desirudin:预防深静脉血栓形成的药理学和临床应用综述

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摘要

Direct thrombin inhibitors (DTIs) are an emerging class of anticoagulants in routine clinical practice, although they have been under investigation for quite some time. Desirudin (Iprivask ?, Canyon Pharmaceuticals?) is a recombinant hirudin derivative that directly inhibits free and fibrin-bound thrombin. Desirudin was the first DTI approved for deep vein thrombosis (DVT) prophylaxis in Europe (Revasc ?) and is the newest injectable DTI commercially available in the USA. Desirudin is one of the few nonheparin subcutaneous drugs that has demonstrable efficacy for DVT prophylaxis. Subcutaneous desirudin has been shown to be more effective than both subcutaneous unfractionated heparin and enoxaparin, with comparable bleeding rates in the prevention of DVT in patients undergoing elective hip replacement. Desirudin also offers the advantage of a fixed dosing regimen while being less immunogenic than unfractionated heparin. However, owing to its pharmacokinetic properties, patients with renal dysfunction require dosing modifications. The favorable profile shown with desirudin thus far will allow its clinical use to grow and will promote further investigation into broadening its clinical applications.
机译:直接凝血酶抑制剂(DTI)是常规临床实践中新兴的一类抗凝剂,尽管已经进行了相当长时间的研究。 Desirudin(Iprivask?,Canyon Pharmaceuticals?)是一种重组水rud素衍生物,可直接抑制游离的和结合血纤蛋白的凝血酶。 Desirudin是欧洲首个被批准用于预防深静脉血栓形成(DVT)的DTI(Revasc®),并且是在美国市售的最新可注射DTI。 Desirudin是为数不多的可预防DVT的非肝素皮下药物之一。皮下Desirudin已被证明比皮下普通肝素和依诺肝素更有效,出血选择性在预防行选择性髋关节置换术的DVT方面具有可比性。 Desirudin还具有固定剂量方案的优势,同时免疫原性比普通肝素要低。然而,由于其药代动力学特性,肾功能不全患者需要调整剂量。迄今为止,desirudin所显示的良好特性将使其临床应用得以发展,并将促进进一步研究以扩大其临床应用。

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