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Drugs. 2014 Feb;74(2):243-62. doi: 10.1007/s40265-013-0174-4.
Rivaroxaban (Xarelto(®)), an oral direct factor Xa inhibitor, is approved for the initial treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE), as well as the prevention of recurrent DVT and PE. It is administered at a fixed oral dose and does not require routine coagulation monitoring. In the EINSTEIN-DVT and EINSTEIN-PE trials, in over 8,000 patients with DVT and/or PE, a single-drug approach with rivaroxaban was shown to be noninferior to standard therapy consisting of subcutaneous enoxaparin sodium overlapping with and followed by an oral dose-adjusted vitamin K antagonist (enoxaparin-VKA) with regard to the incidence of symptomatic recurrent venous thromboembolism (VTE) after 3, 6 or 12 months of treatment. Rivaroxaban was generally well tolerated in patients with DVT or PE, with no significant between-group differences in clinically relevant bleeding between the rivaroxaban and enoxaparin-VKA groups. Notably, rivaroxaban was associated with a significantly lower rate of major bleeding compared with enoxaparin-VKA when EINSTEIN-DVT and EINSTEIN-PE data were pooled. Pharmacoeconomic analyses indicated that rivaroxaban may be a cost-effective alternative to enoxaparin-VKA for the treatment of DVT or PE and prevention of recurrent VTE. Extended prophylaxis with rivaroxaban reduced the incidence of symptomatic recurrent VTE to a greater extent than placebo in the EINSTEIN-Extension trial, but was associated with a non-significant increase in the risk of clinically relevant bleeding compared with placebo. In conclusion, rivaroxaban is a reasonable alternative to standard therapy for the treatment of DVT and PE, and as extended thromboprophylaxis.
利伐沙班(拜瑞妥(®)),一种口服直接 Xa 因子抑制剂,已获准用于深静脉血栓形成(DVT)和肺栓塞(PE)的初始治疗,以及 DVT 和 PE 的复发预防。它采用固定的口服剂量给药,不需要常规凝血监测。在 EINSTEIN-DVT 和 EINSTEIN-PE 试验中,在 8000 多名 DVT 和/或 PE 患者中,与包括皮下依诺肝素钠重叠并用和随后用口服剂量调整维生素 K 拮抗剂(依诺肝素-VKA)的标准治疗相比,利伐沙班单一药物治疗在治疗后 3、6 或 12 个月时的症状性复发性静脉血栓栓塞症(VTE)发生率方面非劣效。在 DVT 或 PE 患者中,利伐沙班总体耐受性良好,利伐沙班组和依诺肝素-VKA 组之间在临床上有意义的出血方面没有显著的组间差异。值得注意的是,当将 EINSTEIN-DVT 和 EINSTEIN-PE 数据汇总时,与依诺肝素-VKA 相比,利伐沙班与显著较低的大出血发生率相关。药物经济学分析表明,利伐沙班可能是替代依诺肝素-VKA 治疗 DVT 或 PE 和预防复发性 VTE 的一种具有成本效益的选择。在 EINSTEIN-Extension 试验中,利伐沙班的扩展预防治疗在更大程度上降低了症状性复发性 VTE 的发生率,而与安慰剂相比,其临床上有意义的出血风险增加无统计学意义。总之,利伐沙班是标准治疗 DVT 和 PE 的合理替代药物,也是扩展血栓预防的合理替代药物。