Cheer Susan M, Dunn Christopher J, Foster Rachel
Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 1311, New Zealand.
Drugs. 2004;64(13):1479-502. doi: 10.2165/00003495-200464130-00006.
Tinzaparin sodium (tinzaparin; innohep) is a low molecular weight heparin (LMWH) formed by the enzymatic degradation of porcine unfractionated heparin (UFH). In clinical trials, once-daily subcutaneous (SC) tinzaparin was effective and generally well tolerated in the prophylaxis and treatment of thromboembolic disease. SC tinzaparin 75 anti-Xa IU/kg/day showed similar thromboprophylactic efficacy to adjusted-dosage oral warfarin in patients undergoing total hip arthroplasty; in patients undergoing knee replacement, the incidence of deep vein thrombosis (DVT) was significantly lower with tinzaparin. The drug had similar efficacy to equivalent-dosage SC enoxaparin sodium in orthopaedic surgery. In patients undergoing general surgery, SC tinzaparin 3500 anti-Xa IU/day was of equivalent thromboprophylactic efficacy to SC UFH 5000IU twice daily. Encouraging preliminary results have been obtained with tinzaparin in the prevention of DVT in patients with complete motor paralysis. In the initial treatment of acute proximal DVT and pulmonary embolism, SC tinzaparin 175 anti-Xa IU/kg/day was at least as effective as adjusted-dosage intravenous (IV) UFH. In the outpatient treatment of venous thromboembolism, tinzaparin has demonstrated similar efficacy to dalteparin sodium (dalteparin) and warfarin. Tinzaparin was effective in preventing clotting in haemodialysis circuits; the anticoagulant efficacy of tinzaparin in patients undergoing haemodialysis was similar to that of SC dalteparin and similar to or less than (although in this case the tinzaparin dose was too low for sufficient anticoagulant efficacy) that of IV UFH. Advantages of tinzaparin over UFH and warfarin include ease of administration and lack of need for laboratory monitoring. Tinzaparin is more cost effective than UFH in the treatment of established thromboembolic disease, and home-based treatment with tinzaparin may offer greater cost benefits than hospital-based therapy. Tinzaparin is well tolerated, including in elderly patients and those with renal impairment receiving long-term treatment. Incidences of major bleeding complications were low and reports of heparin-induced thrombocytopenia were infrequent in clinical studies. In conclusion, tinzaparin is a valuable LMWH in the prophylaxis and management of thromboembolic disease.
替扎肝素钠（替扎肝素；Innohep）是一种低分子量肝素（LMWH），由猪源普通肝素（UFH）经酶解降解而成。在临床试验中，每日一次皮下注射（SC）替扎肝素在预防和治疗血栓栓塞性疾病方面有效且一般耐受性良好。在接受全髋关节置换术的患者中，皮下注射75抗Xa国际单位/千克/天的替扎肝素与调整剂量的口服华法林具有相似的血栓预防效果；在接受膝关节置换术的患者中，替扎肝素治疗的深静脉血栓形成（DVT）发生率显著更低。在骨科手术中，该药物与等效剂量的皮下注射依诺肝素钠疗效相似。在接受普通外科手术的患者中，皮下注射3500抗Xa国际单位/天的替扎肝素与每日两次皮下注射5000国际单位的普通肝素具有等效的血栓预防效果。替扎肝素在预防完全性运动麻痹患者的DVT方面已取得了令人鼓舞的初步结果。在急性近端DVT和肺栓塞的初始治疗中，皮下注射175抗Xa国际单位/千克/天的替扎肝素至少与调整剂量的静脉注射（IV）普通肝素一样有效。在静脉血栓栓塞症的门诊治疗中，替扎肝素已证明与达肝素钠（达肝素）和华法林疗效相似。替扎肝素在预防血液透析回路凝血方面有效；在接受血液透析的患者中，替扎肝素的抗凝效果与皮下注射达肝素相似，且与静脉注射普通肝素相似或更低（尽管在此情况下替扎肝素剂量过低，无法达到足够的抗凝效果）。替扎肝素相对于普通肝素和华法林的优势包括给药方便且无需实验室监测。在治疗已确诊的血栓栓塞性疾病方面，替扎肝素比普通肝素更具成本效益，并且在家中使用替扎肝素治疗可能比在医院治疗具有更大的成本效益。替扎肝素耐受性良好，包括老年患者和接受长期治疗的肾功能不全患者。在临床研究中，严重出血并发症的发生率较低且肝素诱导的血小板减少症的报告较少。总之，替扎肝素是预防和管理血栓栓塞性疾病的一种有价值的低分子量肝素。
