Unit for Medication Outcomes Research and Education, School of Pharmacy, University of Tasmania, Hobart, Australia.
Cardiovasc Ther. 2010 Oct;28(5):278-86. doi: 10.1111/j.1755-5922.2010.00209.x. Epub 2010 Jul 14.
Atrial fibrillation (AF) is the most commonly occurring arrhythmia, and is a condition of both significant clinical and economic importance. An antithrombotic agent is considered mandatory as part of the management in most patients with AF. It has been conclusively demonstrated that long-term anticoagulation therapy can significantly reduce the risk of stroke in patients with nonvalvular AF. While vitamin K antagonists (VKAs) such as warfarin are highly effective, they possess numerous limitations that curtail their use, or make their use challenging for clinicians and patients. A new generation of anticoagulants are being investigated in phase III clinical trials in patients with AF. One or more of these agents have the potential to either replace or act as alternatives to VKA therapy in AF. This group includes the direct thrombin inhibitor, dabigatran, the direct factor Xa inhibitors rivaroxaban, apixaban, and edoxaban, and finally, the vitamin K analogue, tecarfarin. Additional agents are being developed in phase I or II clinical trials. The direct thrombin and factor Xa inhibitors are generally small, synthetic molecules with predictable pharmacokinetics, a predictable pharmacodynamic effect, few drug interactions and do not require routine therapeutic drug monitoring. These new anticoagulants may well represent a new era in anticoagulation. However, they do possess their own limitations and will present new challenges for clinicians.
心房颤动(AF)是最常见的心律失常,是一种具有重要临床和经济意义的疾病。大多数 AF 患者的治疗方案中都需要使用抗血栓药物。已经明确证实,长期抗凝治疗可以显著降低非瓣膜性 AF 患者的中风风险。虽然维生素 K 拮抗剂(VKAs)如华法林具有高度疗效,但它们存在许多限制,限制了它们的使用,或使临床医生和患者难以使用。新一代抗凝剂正在 AF 患者的 III 期临床试验中进行研究。这些药物中的一种或多种有可能替代或替代 VKA 治疗 AF。这组药物包括直接凝血酶抑制剂达比加群、直接因子 Xa 抑制剂利伐沙班、阿哌沙班和依度沙班,以及最后一种维生素 K 类似物替卡格雷。其他药物正在 I 期或 II 期临床试验中开发。直接凝血酶和因子 Xa 抑制剂通常是小分子、合成分子,具有可预测的药代动力学、可预测的药效学效应、较少的药物相互作用,且不需要常规治疗药物监测。这些新型抗凝剂可能代表着抗凝治疗的新时代。然而,它们确实存在自身的局限性,也将给临床医生带来新的挑战。