Department of Pharmacy Services, Henry Ford Hospital, Detroit, MI 48202, USA.
Am J Health Syst Pharm. 2013 May 15;70(10 Suppl 1):S12-21. doi: 10.2146/ajhp130041.
To describe the pharmacologic agents and strategies used for urgent reversal of warfarin and the target-specific oral anticoagulants dabigatran, rivaroxaban, and apixaban.
To reverse the anticoagulant effects of warfarin in patients who are bleeding or need surgery, exogenous vitamin K (phytonadione) may be used in combination with another, shorter-acting intervention, such as fresh frozen plasma (FFP), prothrombin complex concentrate (PCC), recombinant factor VIIa, or activated PCC (aPCC). Three-factor PCC contains factors II, IX, and X in an inactivated form, and four-factor PCC also includes factor VII in an inactivated form. No four-factor PCC products are available in the United States, but aPCC, which contains the same four factors with factor VII provided in an activated form, is available. The intervention depends on the International Normalized Ratio, presence of bleeding, and need for and timing of surgery. Research suggests that clotting factor concentrates are more effective than FFP alone for warfarin reversal. These products also may be useful for reversing the effects of target-specific oral anticoagulants, but limited efficacy and safety data are available to support their use. The risks and benefits associated with these products need to be weighed before their use for reversal of dabigatran, rivaroxaban, or apixaban. Additional clinical data are needed to clearly define the role of concentrated clotting factor products in reversal and to determine the optimal clotting factor concentrate product and dose for urgent reversal of oral anticoagulation.
Phytonadione and clotting factor concentrates appear to have a role for reversal of warfarin, and limited evidence suggests that clotting factor concentrates could have a role in reversal of target-specific oral anticoagulants in an emergency situation.
描述用于紧急逆转华法林以及达比加群、利伐沙班和阿哌沙班这 3 种靶向特定口服抗凝剂的药理学药物和策略。
为逆转正在出血或需要手术的华法林抗凝患者的抗凝作用，可联合使用外源性维生素 K（叶绿醌）与另一种起效更快的干预措施，如新鲜冰冻血浆（FFP）、凝血酶原复合物浓缩物（PCC）、重组 VII 因子或活化 PCC（aPCC）。三因子 PCC 以失活形式包含因子 II、IX 和 X，四因子 PCC 还包含失活形式的因子 VII。美国尚无四因子 PCC 产品，但可获得含有以激活形式提供的相同四因子加因子 VII 的 aPCC。干预措施取决于国际标准化比值、出血情况以及手术的必要性和时间。研究表明，与 FFP 单独使用相比，凝血因子浓缩物更有助于逆转华法林的抗凝作用。这些产品对于逆转靶向特定口服抗凝剂的作用可能也有一定效果，但目前仅有有限的疗效和安全性数据支持其使用。在使用这些产品逆转达比加群、利伐沙班或阿哌沙班之前，需要权衡其相关风险和获益。需要更多的临床数据来明确凝血因子浓缩物产品在逆转中的作用，并确定用于紧急逆转口服抗凝的最佳凝血因子浓缩物产品和剂量。
叶绿醌和凝血因子浓缩物似乎在逆转华法林方面具有一定作用，且有限的证据表明，在紧急情况下，凝血因子浓缩物可能在逆转靶向特定口服抗凝剂方面具有一定作用。
