Hull Russell D, Gersh Meryl H
University of Calgary , Calgary, Alberta , Canada.
Curr Med Res Opin. 2015 Feb;31(2):197-210. doi: 10.1185/03007995.2014.975786. Epub 2014 Oct 30.
Venous thromboembolism (VTE), comprising deep vein thrombosis (DVT) and pulmonary embolism (PE), is a major cause of morbidity, mortality, and healthcare expenditure. Anticoagulant therapy is recommended for at least 3 months in patients with acute VTE to prevent recurrence. Conventional anticoagulants are associated with inherent limitations including route of administration, required monitoring and dose adjustments, potential for food-drug and drug-drug interactions, unpredictable pharmacokinetics and pharmacodynamics, and possible severe adverse events.
This manuscript reviews the pharmacology of the novel oral anticoagulants (NOACs), and analyzes the differences in phase 3 clinical trial designs, outcomes, and specific patient populations investigated for the treatment of acute and prevention of secondary VTE.
A literature search was performed in PubMed using the key words dabigatran, apixaban, rivaroxaban, edoxaban, and venous thromboembolism in PubMed. The search included all years, English language, and peer-reviewed articles relating to phase 3 clinical trials, subanalyses, and meta-analyses of these NOACs for the treatment of acute VTE and secondary prevention.
NOACs have demonstrated comparable efficacy and comparable or superior safety in large, randomized clinical trials in the treatment and prevention of VTE compared with conventional therapy. New oral anticoagulants, including the direct thrombin (dabigatran etexilate) and direct factor Xa inhibitors (rivaroxaban, apixaban, and edoxaban), have advantages over conventional agents such as oral administration at fixed doses, predictable pharmacokinetics and pharmacodynamics, minimal potential for food-drug and drug-drug interactions, and lack of required monitoring.
NOACs offer additional oral anticoagulation treatment options for patients with VTE.
静脉血栓栓塞症（VTE）包括深静脉血栓形成（DVT）和肺栓塞（PE），是发病、死亡及医疗费用的主要原因。对于急性VTE患者，推荐进行至少3个月的抗凝治疗以预防复发。传统抗凝剂存在固有局限性，包括给药途径、需要监测和剂量调整、食物-药物及药物-药物相互作用的可能性、不可预测的药代动力学和药效学，以及可能出现的严重不良事件。
本文综述新型口服抗凝剂（NOACs）的药理学，并分析用于治疗急性VTE和预防继发性VTE的3期临床试验设计、结果及所研究的特定患者群体之间的差异。
在PubMed中使用关键词达比加群、阿哌沙班、利伐沙班、依度沙班和静脉血栓栓塞症进行文献检索。检索涵盖所有年份、英文以及与这些NOACs治疗急性VTE和二级预防的3期临床试验、亚组分析和荟萃分析相关的同行评审文章。
在治疗和预防VTE的大型随机临床试验中，与传统治疗相比，NOACs已证明具有相当的疗效和相当或更优的安全性。新型口服抗凝剂，包括直接凝血酶抑制剂（达比加群酯）和直接Xa因子抑制剂（利伐沙班、阿哌沙班和依度沙班），相对于传统药物具有优势，如固定剂量口服给药、可预测的药代动力学和药效学、食物-药物及药物-药物相互作用的可能性极小，且无需监测。
NOACs为VTE患者提供了额外的口服抗凝治疗选择。
