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New oral anticoagulants: their advantages and disadvantages compared with vitamin K antagonists in the prevention and treatment of patients with thromboembolic events

机译:新型口服抗凝药:与维生素K拮抗剂相比在预防和治疗血栓栓塞事件患者中的优缺点

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摘要

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.
机译:尽管发现并应用了许多肠胃外(普通和低分子量肝素)和口服抗凝维生素K拮抗剂(VKA)药物,但预防和治疗静脉和动脉血栓形成现象仍然是主要的医学挑战。此外,VKA是过去60年来唯一使用的口服抗凝剂。这项研究的主要目的是提供有关非维生素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与VKA相比的优缺点。 NOAC是对一种特定凝血因子(凝血酶(IIa)或活化因子X(Xa))具有选择性的新型直接作用药物。几种NOAC,例如达比加群(FIIa的直接抑制剂)和利伐沙班,阿哌沙班和edoxaban(Xa因子的直接抑制剂)已使用了至少5年,但可能使用了10年。与传统的VKA通过抑制维生素K依赖性因子的合成来阻止凝血过程不同,NOAC直接抑制关键的蛋白酶(因子IIa和Xa)。这些药物的重要适应症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纤颤的患者心脏和大脑中的动脉粥样硬化事件。它们不是固定的,并且可以使用各种剂量的强度。大多数研究报告说,与VKA相比,NOAC的优点多于弊,NOAC的最重要的优点包括安全性问题(即,大出血的发生率较低),使用方便,药物和食物的相互作用小,治疗范围广窗口,无需实验室监控。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具有更大的优势和更少的劣势。需要进行新的研究以进一步评估NOAC的功效。

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