新型口服抗凝药:与维生素K拮抗剂相比,它们在预防和治疗血栓栓塞事件患者中的优缺点。
New oral anticoagulants: their advantages and disadvantages compared with vitamin K antagonists in the prevention and treatment of patients with thromboembolic events.
作者信息
Mekaj Ymer H, Mekaj Agon Y, Duci Shkelzen B, Miftari Ermira I
机构信息
Institute of Pathophysiology, Faculty of Medicine, University of Prishtina, Prishtina, Kosovo ; Department of Hemostasis and Thrombosis, National Blood Transfusion Center of Kosovo, Prishtina, Kosovo.
Clinic of Neurosurgery, Faculty of Medicine, University of Prishtina, Prishtina, Kosovo, Prishtina, Kosovo.
出版信息
Ther Clin Risk Manag. 2015 Jun 24;11:967-77. doi: 10.2147/TCRM.S84210. eCollection 2015.
Despite the discovery and application of many parenteral (unfractionated and low-molecular-weight heparins) and oral anticoagulant vitamin K antagonist (VKA) drugs, the prevention and treatment of venous and arterial thrombotic phenomena remain major medical challenges. Furthermore, VKAs are the only oral anticoagulants used during the past 60 years. The main objective of this study is to present recent data on non-vitamin K antagonist oral anticoagulants (NOACs) and to analyze their advantages and disadvantages compared with those of VKAs based on a large number of recent studies. NOACs are novel direct-acting medications that are selective for one specific coagulation factor, either thrombin (IIa) or activated factor X (Xa). Several NOACs, such as dabigatran (a direct inhibitor of FIIa) and rivaroxaban, apixaban and edoxaban (direct inhibitors of factor Xa), have been used for at least 5 years but possibly 10 years. Unlike traditional VKAs, which prevent the coagulation process by suppressing the synthesis of vitamin K-dependent factors, NOACs directly inhibit key proteases (factors IIa and Xa). The important indications of these drugs are the prevention and treatment of deep vein thrombosis and pulmonary embolisms, and the prevention of atherothrombotic events in the heart and brain of patients with acute coronary syndrome and atrial fibrillation. They are not fixed, and dose-various strengths are available. Most studies have reported that more advantages than disadvantages for NOACs when compared with VKAs, with the most important advantages of NOACs including safety issues (ie, a lower incidence of major bleeding), convenience of use, minor drug and food interactions, a wide therapeutic window, and no need for laboratory monitoring. Nonetheless, there are some conditions for which VKAs remain the drug of choice. Based on the available data, we can conclude that NOACs have greater advantages and fewer disadvantages compared with VKAs. New studies are required to further assess the efficacy of NOACs.
尽管已发现并应用了多种胃肠外(普通肝素和低分子肝素)和口服抗凝药物维生素K拮抗剂(VKA),但静脉和动脉血栓形成现象的预防和治疗仍然是重大的医学挑战。此外,VKA是过去60年来唯一使用的口服抗凝剂。本研究的主要目的是展示非维生素K拮抗剂口服抗凝剂(NOAC)的最新数据,并基于大量近期研究分析其与VKA相比的优缺点。NOAC是新型直接作用药物,对一种特定凝血因子具有选择性,即凝血酶(IIa)或活化因子X(Xa)。几种NOAC,如达比加群(FIIa的直接抑制剂)和利伐沙班、阿哌沙班和依度沙班(因子Xa的直接抑制剂),已使用至少5年,但可能长达10年。与传统VKA通过抑制维生素K依赖性因子的合成来预防凝血过程不同,NOAC直接抑制关键蛋白酶(因子IIa和Xa)。这些药物的重要适应证是预防和治疗深静脉血栓形成和肺栓塞,以及预防急性冠状动脉综合征和心房颤动患者心脏和脑部的动脉粥样硬化血栓形成事件。它们并非固定剂量,有多种不同强度的剂量可供选择。大多数研究报告称,与VKA相比,NOAC的优点多于缺点,NOAC最重要的优点包括安全性问题(即大出血发生率较低)、使用方便、药物与食物相互作用较小、治疗窗宽且无需实验室监测。尽管如此,在某些情况下VKA仍然是首选药物。根据现有数据,我们可以得出结论,与VKA相比,NOAC具有更多优点和更少缺点。需要进行新的研究以进一步评估NOAC的疗效。