Department of Emergency Medicine, Beth Israel Deaconess Medical Center, WCC-2, Boston, MA 02215, USA.
J Med Toxicol. 2011 Dec;7(4):281-7. doi: 10.1007/s13181-011-0178-y.
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.
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，用于预防非瓣膜性心房颤动患者的栓塞性中风。达比加群具有可预测抗凝反应的药代动力学特征，不经过 CYP450 代谢，药物相互作用和药物食物相互作用较少，且不需要频繁监测凝血参数。临床医生正在迅速将该药物作为华法林治疗的替代品开具处方。然而，目前还没有可靠的治疗药物可用于逆转达比加群引起的出血并发症。到目前为止，尚无可靠的证据来指导出血并发症的管理；管理应从尽可能控制出血开始，如果需要，输注红细胞。预计输注新鲜冰冻血浆并不能帮助控制出血。对于输注凝血因子 VIIa 和凝血酶原复合物浓缩物，仅有有限和混杂的数据；对于这些治疗方法，以及对于由于达比加群导致的危及生命或密闭空间出血的透析，也应予以考虑。我们介绍了一篇综述文章，其中回顾了这种新型口服抗凝剂的药代动力学、临床试验文献和共识指南。
