New oral anticoagulants clinical application progress
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摘要: 抗凝药是通过抑制或阻断机体生理性凝血机制的某些环节而遏止血液凝聚的药物,临床主要用于血栓栓塞性疾病的预防和治疗。传统口服抗凝药可同时干扰凝血机制中的多个靶点,以华法林为代表。尽管华法林在血栓栓塞性疾病的预防和治疗方面效果明确,但是,在临床使用过程中出现了诸多弊端严重影响了医患双方的积极性。与传统口服抗凝药物相比,新型口服抗凝药物(new oral anticoagulants, NOACs)是通过抑制凝血酶促反应中特定凝血因子的路径预防和治疗血栓,主要包括凝血酶抑制剂(达比加群酯)和凝血因子Ⅹa抑制剂(利伐沙班、啊哌沙班、依杜沙班、Ⅲ期临床研究中的贝曲西班),NOACs具有起效快、代谢迅速、无需常规监测凝血指标、与药物食物相互作用较少、出血(尤其是颅内出血)等并发症发生率较低等优点,目前,已广泛应用于非瓣膜性心房颤动的抗凝治疗、深静脉血栓的防治、急性冠脉综合征的二级预防等疾病的治疗中。因此NOACs得以开展更多的临床研究,进一步明确了其适应证、剂量的调整及范围、如何优化个体用药等实际问题,使得NOACs走在了时代的前沿,为需要抗凝的患者提供更多的选择,制定最佳的治疗方案。以下就NOACs的药物特性及临床研究进展做简要综述,希望可以为临床规范使用NOACs提供借鉴。Abstract: Anticoagulants are drugs that prevents blood coagulation by inhibiting or blocking certain parts of the organism's physiological coagulation mechanism, which are mainly used in the prevention and treatment of thromboembolic diseases. Traditional oral anticoagulants can interfere with multiple targets in the coagulation mechanism, represented by warfarin. Although warfarin has remarkable advantages on the prevention and treatment of thromboembolic disease, the disadvantages of it also limited the popularity among both doctors and patients in clinical practise. Compared with traditional oral anticoagulants, New oral anticoagulants (NOACs) inhibit blood coagulation pathways in particular of the clotting factors, for example thrombin inhibitors (dabigatran etexilate) and blood coagulation factor X inhibitors (rivaroxaban apixaban; edoxaban; the Ⅲ clinical study of betrixaban), NOACs work fast, metabolic quickly, do without regular monitoring of blood coagulation indexes, interact less with food and drug, risk less bleeding events, especially intracranial hemorrhage. At present, NOACs have been widely used in nonvalvular atrial fibrillation of anticoagulant therapy, prevention of deep vein thrombosis and the secondary prevention of acute coronary syndrome. So more clinical studies about NOACs were conducted to further define the scope of its indications, dosage adjustment, optimization of individual application. These new progress makes the new oral anticoagulants walking in the forefront of the times, provided more choices to make the best treatment plans for patients in need of anticoagulation. Here we provide a brief overview in the drug characteristics and clinical research progress of NOACs to promote standardized application of NOACs.
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Key words:
- New oral anticoagulants /
- Dabigatran etexilate /
- Rivaroxaban /
- Apixaban /
- Edoxaban
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