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2010年上市的两种新型抗凝剂——达比加群酯和利伐沙班:预期进展——引发的问题

[Two new anticoagulants available in 2010--Dabigatran Etexilate and Rivaroxaban: expected progresses--raised problems].

作者信息

Samama M, Conard J, Horellou M-H, Le Flem L, Guinet C, Depasse F

机构信息

Service d'hématologie, hôtel-Dieu, AP-HP, 1 place du parvis-Notre-Dame, Paris, France.

出版信息

Ann Pharm Fr. 2010 Nov;68(6):359-69. doi: 10.1016/j.pharma.2010.08.001. Epub 2010 Oct 29.

DOI:10.1016/j.pharma.2010.08.001
PMID:21073994
Abstract

After having been used for decades, heparins (unfractionated heparin [UFH] or low molecular weight heparins [LMWH]) and vitamin K antagonists (VKA), which are only parenterally active or which are responsible for frequent iatrogenicity respectively, have to face the competition of new anticoagulant drugs targeting either factor Xa or factor IIa (thrombin). Rivaroxaban (Xarelto(®)) and Dabigatran Etexilate (Pradaxa(®)) are the two leading components. They are more convenient to use and do not require routine coagulation monitoring. They are already marketed for venous thromboembolism prevention in major orthopaedic surgery. Although manufacturers claim that no biological monitoring is required, these two compounds may interfere in routine coagulation tests such as PT or aPTT, and in esoteric assays such as anti-Xa activity (the results of which are usually expressed in international anti-Xa units either UFH or LMWH unit) for Rivaroxaban or anti-IIa activity for Dabigatran Etexilate. Noteworthy is the fact that, in the case of these new anticoagulant drugs, results should be expressed in active product units (nanogram per millilitre of Rivaroxaban or Dabigatran). The new anticoagulants are associated with a bleeding risk comparable to that of VKA and heparins.

摘要

在使用了数十年后,肝素(普通肝素[UFH]或低分子量肝素[LMWH])以及维生素K拮抗剂(VKA),前者仅具有肠外活性,后者则分别导致频繁的医源性问题,它们不得不面对针对Xa因子或IIa因子(凝血酶)的新型抗凝药物的竞争。利伐沙班(拜瑞妥®)和达比加群酯(泰毕全®)是两种领先的药物成分。它们使用起来更方便,且无需常规凝血监测。它们已被用于预防大型骨科手术中的静脉血栓栓塞。尽管制造商声称无需进行生物学监测,但这两种化合物可能会干扰常规凝血试验,如PT或活化部分凝血活酶时间(aPTT),以及一些特殊检测,如利伐沙班的抗Xa活性检测(其结果通常以国际抗Xa单位表示,即UFH或LMWH单位)或达比加群酯的抗IIa活性检测。值得注意的是,对于这些新型抗凝药物,结果应以活性产品单位(每毫升利伐沙班或达比加群的纳克数)表示。新型抗凝药物的出血风险与VKA和肝素相当。

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Ann Pharm Fr. 2010 Nov;68(6):359-69. doi: 10.1016/j.pharma.2010.08.001. Epub 2010 Oct 29.
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