Bhanwra Sangeeta, Ahluwalia Kaza
Department of Pharmacology, Government Medical College and Hospital, Chandigarh, India.
J Pharmacol Pharmacother. 2014 Jan;5(1):12-4. doi: 10.4103/0976-500X.124409.
Cardiovascular diseases are still the most important cause of morbidity and mortality worldwide and anti-thrombotic treatment is widely used as a result. The currently used drugs include heparin and its derivatives, vitamin K antagonists, though efficacious, have their own set of limitations like unpredictable pharmacokinetic profile, parenteral route (with heparin and its derivatives only), narrow therapeutic window, and constant laboratory monitoring for their efficacy and safety. This lead to the development of novel factor Xa inhibitors which could be given orally, have predictable dose response relationship and are associated with lesser hemorrhagic complications. They include rivaroxaban, apixaban, and edoxaban among others. Apixaban has currently been approved for use in patients undergoing total knee or hip replacement surgery and to prevent stroke in patients with atrial fibrillation. Many trials are ongoing for apixaban to firmly establish its place in future, among the anti-thrombotic drugs.
心血管疾病仍然是全球发病和死亡的最重要原因,因此抗血栓治疗被广泛应用。目前使用的药物包括肝素及其衍生物、维生素K拮抗剂,尽管这些药物有效,但它们有自身一系列局限性,如不可预测的药代动力学特征、仅肝素及其衍生物为肠胃外给药途径、治疗窗窄以及需要持续进行实验室监测以评估其疗效和安全性。这促使了新型Xa因子抑制剂的研发,这类抑制剂可以口服,具有可预测的剂量反应关系,且出血并发症较少。其中包括利伐沙班、阿哌沙班和依度沙班等。阿哌沙班目前已被批准用于接受全膝关节或全髋关节置换手术的患者,以及预防心房颤动患者的中风。目前正在进行许多关于阿哌沙班的试验,以在未来的抗血栓药物中稳固确立其地位。