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Factor Xa inhibitors: a novel therapeutic class for the treatment of nonvalvular atrial fibrillation

机译:Xa因子抑制剂:用于治疗非瓣膜性心房颤动的新型治疗药物

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摘要

Atrial fibrillation is the most common cause of stroke. Treatment with anticoagulants in patients with atrial fibrillation reduces embolic complications of the disease including stroke. However, the commonly used anticoagulant has a narrow therapeutic index, requires routine monitoring, and has numerous drug and food interactions leading to less than optimal rates of adherence. Inhibition of clotting factor Xa has been evaluated as a potential target for anticoagulation therapy with the hypothesis that using target-specific therapy will alleviate some of the dosing variability observed with the vitamin K antagonist. Three factor Xa inhibitors are currently indicated for use in nonvalvular atrial fibrillation. Similar to the vitamin K antagonist, warfarin, all of the factor Xa inhibitors are administered orally. Rivaroxaban and edoxaban are dosed once daily while apixaban is dosed twice daily. All three agents have demonstrated noninferiority when compared with current standard treatment with warfarin for efficacy and safety outcomes. The therapeutic dose of factor Xa inhibitors vary based on renal function. Unlike warfarin, there are no currently available antidotes for the factor Xa inhibitors although this is an area of interest for current and future studies. In the event of a life-threatening bleed there are established management strategies to reverse the bleeding effects of the factor Xa inhibitors.
机译:心房纤颤是中风的最常见原因。在房颤患者中使用抗凝剂治疗可减少该疾病的栓塞并发症,包括中风。然而,常用的抗凝剂具有较窄的治疗指数,需要常规监测,并且具有多种药物和食物相互作用,导致达不到最佳的依从率。凝血因子Xa的抑制已被评估为抗凝疗法的潜在靶点,其假设是使用靶点特异性疗法将缓解维生素K拮抗剂观察到的某些剂量变异性。目前指出三因子Xa抑制剂可用于非瓣膜性房颤。与维生素K拮抗剂华法林类似,所有Xa因子抑制剂均口服给药。利伐沙班和依多沙班每天给药一次,而阿哌沙班每天给药两次。与目前使用华法林的标准疗法相比,所有三种药物均显示出非劣效性,从而提高了疗效和安全性。 Xa因子抑制剂的治疗剂量因肾功能而异。与华法林不同,Xa因子抑制剂目前没有可用的解毒剂,尽管这是当前和未来研究的重点领域。如果发生危及生命的流血,则已建立管理策略来逆转Xa因子抑制剂的流血作用。

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