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Dabigatran: Review of Pharmacology and Management of Bleeding Complications of This Novel Oral Anticoagulant

机译:达比加群:这种新型口服抗凝药的药理学和出血并发症的管理的回顾。

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摘要

Dabigatran (Pradaxa) is a competitive direct thrombin inhibitor approved by the US FDA for prevention of embolic stroke in patients with nonvalvular atrial fibrillation. Dabigatran has a pharmacokinetic profile that produces predictable anticoagulation responses, does not undergo CYP 450 metabolism, has few drug–drug and drug–food interactions, and does not require frequent laboratory monitoring of clotting parameters. Clinicians are rapidly prescribing this agent as a replacement for warfarin therapy. However, no therapeutic agent has been accepted to reliably reverse the hemorrhagic complications of dabigatran. As of yet, there is no solid evidence to guide management of bleeding complications; management should start with local control of bleeding when possible and transfusion of pRBCs if needed. Transfusion of FFP would not be expected to help control bleeding. Limited and mixed data exist for transfusion of factor VIIa and prothrombin complex concentrates; these therapies should be considered as well as dialysis, which will increase elimination in patients with life-threatening or closed-space bleeding due to dabigatran. We present an article that reviews the pharmacokinetics, clinical trial literature, and consensus guidelines regarding this novel oral anticoagulant.
机译:达比加群(Pradaxa)是一种竞争性直接凝血酶抑制剂,已获得美国FDA批准,用于预防非瓣膜性房颤患者的栓塞性中风。达比加群的药代动力学特征可产生可预测的抗凝反应,不进行CYP 450代谢,药物-药物和药物-食品的相互作用少,不需要对凝结参数进行频繁的实验室监测。临床医生正在迅速开出这种药物来替代华法林疗法。然而,尚未接受任何治疗剂来可靠地逆转达比加群的出血并发症。到目前为止,尚无确凿的证据来指导出血并发症的治疗。处理应从局部控制出血开始,如有必要,应输注pRBC。 FFP的输血不会帮助控制出血。对于因子VIIa和凝血酶原复合物浓缩物的输血,存在有限和混合的数据。这些疗法应与透析同时考虑,这将增加因达比加群而危及生命或封闭空间出血的患者的清除。我们提出了一篇文章,综述了有关这种新型口服抗凝药的药代动力学,临床试验文献和共识指南。

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