首页> 外文期刊>Thrombosis and Haemostasis: Journal of the International Society on Thrombosis and Haemostasis >A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibitio
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A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibitio

机译:口服直接凝血酶抑制剂西美加群及其皮下形式美拉加群与达肝素相比在预防髋关节或膝关节置换术后血栓栓塞中的剂量范围研究:METHRO I. MElagatran用于抑制THRombin

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The novel, oral direct thrombin inhibitor, ximelagatran (formerly H 376/95), represents an advance in antithrombotic therapy through its oral availability. After oral administration, ximelagatran is converted to its active form, melagatran. Melagatran can also be administered subcutaneously (s.c.). The results from the first clinical study with ximelagatran are reported. In this randomized, parallel-group, controlled study, 103 patients scheduled for elective total hip or total knee replacement received s.c. melagatran (1, 2 or 4 mg bid) for 2 days commencing immediately before surgery, followed by oral ximelagatran (6, 12 or 24 mg bid) for 6-9 days. Another 33 patients received dalteparin 5000 IU s.c. once daily, started the evening before surgery, for 8-11 days. At bilateral venography, deep vein thrombosis was found in 20.5% (16/78) of patients who had received s.c. melagatran and oral ximelagatran and in 18.5% (5/27) of patients in the dalteparin group. The study did not evaluate a dose-response for efficacy, and no differences between the three dose levels of melagatran and ximelagatran were shown. No pulmonary embolism was diagnosed during treatment. Total bleeding in the s.c. melagatran plus oral ximelagatran groups showed no dose-response and was similar to that seen in the dalteparin group. The pharmacokinetic properties of melagatran in the surgery patients were consistent with those observed for healthy subjects, and the APTT ratio, which increased non-linearly with plasma melagatran concentration, showed a consistent concentration-effect relationship during the treatment period. Ximelagatran and melagatran were well tolerated. In conclusion, ximelagatran and its active form melagatran appear to be promising agents for the prevention of venous thromboembolism following orthopaedic surgery.
机译:新型口服直接凝血酶抑制剂西美加群(ximelagatran,原名H 376/95)通过其口服可用性代表了抗血栓治疗的新进展。口服给药后,西美加群转换为活性形式美加群。 Melagatran也可以皮下给药(s.c.)。首次报道了西美加群的临床研究结果。在这项随机,平行组,对照研究中,计划进行全髋关节置换或全膝关节置换的103例患者接受了皮下注射。术前立即开始服用美加仑(1、2或4 mg每日两次),然后口服西美加仑(6、12或24 mg每日两次)6-9天。另有33名患者接受达肝素5000 IU s.c.每天一次,在手术前的晚上开始,持续8-11天。在双侧静脉造影时,接受皮下注射的患者中有20.5%(16/78)的患者发现深静脉血栓形成。 melagatran和口服ximelagatran,达肝素组的患者占18.5%(5/27)。该研究未评估疗效的剂量反应,并且未显示美拉加群和西美加群的三种剂量水平之间的差异。治疗期间未诊断出肺栓塞。皮下出血美拉加群加口服西美加群组无剂量反应,与达肝素组相似。美拉加群在手术患者中的药代动力学特性与健康受试者观察到的一致,APTT比率随血浆美拉加群浓度呈非线性增加,在治疗期间表现出一致的浓度效应关系。 Ximelagatran和melagatran的耐受性良好。总之,西美加群及其活性形式美拉加群似乎是预防骨科手术后静脉血栓栓塞的有前途的药物。

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