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Old and New Anticoagulant Agents for the Prevention and Treatment of Patients with Ischemic Stroke

机译:预防和治疗缺血性中风患者的新旧抗凝剂

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摘要

Vitamin K antagonists are the only oral anticoagulants available and are considered as well-established treatment to prevent a first stroke or a recurrent stroke in patients with atrial fibrillation. The difficulties in the routine management of these patients cause an underuse of vitamin K antagonists. For long-term use, there is a need for safer and more effective oral anticoagulants that do not require routine monitoring of coagulation. Recently, new drugs have been developed and there are a number of clinical trials for the primary and secondary prevention of stroke in atrial fibrillation. The new anticoagulants that are being investigated target factor Xa or thrombin. The factor Xa inhibitors include indirect inhibitors such as idraparinux and biotinylated idraparinux that inhibit factor Xa by potentiating antithrom-bin. Also being investigated are apixaban and rivaroxaban, orally active agents that inhibit factor Xa directly. Direct thrombin inhibitors include ximelagatran and dabigatran etexilate. Although ximelagatran was withdrawn early because of liver toxicity, it provided convincing evidence that new oral anticoagulants have the potential to replace warfarin. However, even if these new drugs prove superior to dose-adjusted warfarin, their benefits must be substantial (retaining high efficacy with added safety and convenience) to offset their increased Cost.
机译:维生素K拮抗剂是唯一可用的口服抗凝剂,被认为是预防房颤患者中风或复发性中风的行之有效的治疗方法。这些患者常规治疗的困难导致维生素K拮抗剂使用不足。对于长期使用,需要更安全,更有效的口服抗凝剂,而无需常规监测凝血。最近,已经开发出新药,并且有许多临床研究可用于对心房纤颤中风的一级和二级预防。正在研究的新型抗凝剂靶向Xa因子或凝血酶。 Xa因子抑制剂包括间接抑制剂,例如伊曲帕林和生物素化的伊曲帕林,它们通过增强抗凝血酶来抑制Xa因子。还正在研究直接抑制因子Xa的口服活性剂apixaban和rivaroxaban。直接凝血酶抑制剂包括西美加群和达比加群酯。尽管西美加群由于肝毒性而提前撤出,但它提供了令人信服的证据,表明新的口服抗凝药有可能替代华法林。然而,即使这些新药被证明优于剂量调整的华法林,其益处也必须是实质性的(保持高疗效并增加安全性和便利性)以抵消其增加的成本。

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