Department of Medicine, McMaster University and Henderson Research Centre, Hamilton, Ontario, Canada.
Thromb Haemost. 2010 Jan;103(1):62-70. doi: 10.1160/TH09-07-0434. Epub 2009 Oct 26.
Although currently available anticoagulants are effective for the prevention and treatment of thromboembolic disorders, they have several drawbacks. Low-molecular-weight heparins and fondaparinux produce a predictable level of anticoagulation that obviates the need for coagulation monitoring, but they must be given parenterally, which renders them inconvenient for long-term use. Vitamin K antagonists, such as warfarin, are administered orally, but produce a variable anticoagulant response because genetic polymorphisms, dietary vitamin K intake and multiple drug-drug interactions affect their metabolism. Consequently, coagulation monitoring and frequent dose adjustments are needed to ensure that a therapeutic level of anticoagulation is achieved. This is burdensome for patients and physicians, and costly for the healthcare system. These limitations have prompted the development of new oral anticoagulants that target thrombin or factor Xa and can be given in fixed doses without coagulation monitoring. This paper focuses on the new oral anticoagulants in the most advanced stages of development.
尽管目前可用的抗凝剂在预防和治疗血栓栓塞性疾病方面非常有效，但它们也存在一些缺点。低分子量肝素和磺达肝癸钠可产生可预测的抗凝水平，从而无需进行凝血监测，但它们必须通过注射给药，这使得它们不方便长期使用。维生素 K 拮抗剂，如华法林，可口服给药，但由于遗传多态性、饮食中维生素 K 摄入和多种药物相互作用会影响其代谢，因此会产生不同的抗凝反应。因此，需要进行凝血监测和频繁调整剂量，以确保达到治疗性抗凝水平。这对患者和医生来说都是一种负担，对医疗保健系统来说也是一种成本。这些局限性促使开发了新的口服抗凝剂，这些抗凝剂可靶向凝血酶或因子 Xa，并可在无需凝血监测的情况下给予固定剂量。本文重点介绍处于最先进开发阶段的新型口服抗凝剂。
