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五糖。新型抗凝剂。

Pentasaccharides. The new anticoagulants.

作者信息

Abdel-Razeq Hikmat

机构信息

Department of Medicine, King Fahad Armed Forces Hospital, PO Box 9862, Jeddah 21159, Kingdom of Saudi Arabia.

出版信息

Saudi Med J. 2004 Aug;25(8):983-90.

Abstract

Venous thromboembolism VTE remains a common but preventable disease. The last decade has witnessed major advances in VTE treatment and prophylaxis. Low molecular weight heparins LMWH became the agents of choice in the treatment of deep venous thrombosis DVT and are increasingly used in the treatment of stable pulmonary embolism PE. Increasing focus on simplicity and efficacy has led to the discovery of the synthetic pentasaccharides, substances that specifically inhibit factor Xa activity, producing an antithrombotic effect without affecting other coagulation factors or platelets. Fondaparinux, the first pentasaccharide introduced into the market, was first tried as a prophylactic agent against VTE in patients undergoing major orthopedic procedures, such as hip fracture, total hip and knee replacements, such approach appeared to be more effective than LMWH. Fondaparinux was also used, with promising results, in prophylaxis in patients undergoing major abdominal surgery and high risk medical patients. Pentasaccharides were recently tried in the treatment of both DVT and PE. The largest clinical investigation program ever undertaken in this therapeutic area, has shown that pentasaccharides are as safe and as effective as either unfractionated heparin UFH or LMWH, with the added convenience of once daily injection, no need for monitoring the anticoagulant effect and no major side effects such as thrombocytopenia. Therefore, the efficacy, the safety profile and the added convenience for both patients and physicians alike, will probably keep pentasaccharides as the front runner among new anticoagulants of the future. This article focuses on the use of fondaparinux as a prophylactic agent against VTE in patients undergoing major orthopedic and abdominal surgery along with high risk medical patients; it will also discuss the recent promising data on its use to treat active DVT and PE.

摘要

静脉血栓栓塞症(VTE)仍然是一种常见但可预防的疾病。过去十年见证了VTE治疗和预防方面的重大进展。低分子量肝素(LMWH)成为治疗深静脉血栓形成(DVT)的首选药物,并越来越多地用于治疗稳定型肺栓塞(PE)。对简单性和有效性的日益关注导致了合成五糖的发现,这些物质特异性抑制因子Xa活性,产生抗血栓作用而不影响其他凝血因子或血小板。磺达肝癸钠是第一种投放市场的五糖,最初在接受重大骨科手术(如髋部骨折、全髋关节和膝关节置换)的患者中作为预防VTE的药物进行试验,这种方法似乎比LMWH更有效。磺达肝癸钠也用于接受重大腹部手术的患者和高危内科患者的预防,效果良好。五糖最近也被尝试用于治疗DVT和PE。在这一治疗领域进行的有史以来最大规模的临床研究项目表明,五糖与普通肝素(UFH)或LMWH一样安全有效,而且具有每日一次注射的便利性,无需监测抗凝效果,也没有血小板减少等主要副作用。因此,其疗效、安全性以及对患者和医生双方而言额外的便利性,可能会使五糖在未来新型抗凝剂中保持领先地位。本文重点介绍磺达肝癸钠在接受重大骨科和腹部手术的患者以及高危内科患者中作为预防VTE药物的应用;还将讨论其用于治疗活动性DVT和PE的近期有前景的数据。

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