Suppr超能文献

新兴抗凝剂。

Emerging anticoagulants.

机构信息

Department of Respiratory Medicine, Mercy University Hospital, Grenville Place, Cork, Ireland.

出版信息

Curr Med Chem. 2012;19(20):3388-416. doi: 10.2174/092986712801215847.

Abstract

Warfarin, heparin and their derivatives have been the traditional anticoagulants used for prophylaxis and treatment of venous thromboembolism. While the modern clinician is familiar with the efficacy and pharmacokinetics of these agents, their adverse effects have provided the impetus for the development of newer anticoagulants with improved safety, ease of administration, more predictable pharmacodynamics and comparable efficacy. Research into haemostasis and the coagulation cascade has made the development of these newer anticoagulants possible. These drugs include the factor Xa inhibitors and IIa (thrombin) inhibitors. Direct and indirect factor Xa inhibitors are being developed with a relative rapid onset of action and stable pharmacokinetic profiles negating the need for close monitoring; this potentially makes them a more attractive option than heparin or warfarin. Examples of direct factor Xa inhibitors include apixaban, rivaroxaban, otamixaban, betrixaban and edoxaban. Examples of indirect factor Xa inhibitors include fondaparinux, idraparinux and idrabiotaparinux. Direct thrombin inhibitors (factor IIa inhibitors) were developed with the limitations of standard heparin and warfarin in mind. Examples include recombinant hirudin (lepirudin), bivalirudin, ximelagatran, argatroban, and dabigatran etexilate. This review will discuss emerging novel anticoagulants and their use for the prophylaxis and management of venous thromboembolism, for stroke prevention in nonvalvular atrial fibrillation and for coronary artery disease.

摘要

华法林、肝素及其衍生物一直是用于预防和治疗静脉血栓栓塞症的传统抗凝剂。尽管现代临床医生熟悉这些药物的疗效和药代动力学,但它们的不良反应促使人们开发出具有更好安全性、更容易管理、更可预测的药效学和相当疗效的新型抗凝剂。对止血和凝血级联反应的研究使得这些新型抗凝剂的开发成为可能。这些药物包括 Xa 因子抑制剂和 IIa(凝血酶)抑制剂。直接和间接 Xa 因子抑制剂的开发具有相对较快的作用开始时间和稳定的药代动力学特征,无需密切监测;这使得它们比肝素或华法林更具吸引力。直接 Xa 因子抑制剂的例子包括阿哌沙班、利伐沙班、奥塔米沙班、贝曲沙班和依度沙班。间接 Xa 因子抑制剂的例子包括磺达肝素、依达肝素和依达肝素钠。直接凝血酶抑制剂(因子 IIa 抑制剂)是为了克服标准肝素和华法林的局限性而开发的。例子包括重组水蛭素(lepirudin)、比伐卢定、西米拉坦、阿加曲班和达比加群酯。这篇综述将讨论新兴的新型抗凝剂及其在预防和治疗静脉血栓栓塞症、预防非瓣膜性心房颤动中风和治疗冠心病方面的应用。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验