Adis, Auckland, New Zealand.
Drugs. 2012 Mar 26;72(5):585-617. doi: 10.2165/11209070-000000000-00000.
Tranexamic acid, a synthetic derivative of the amino acid lysine, is an antifibrinolytic agent that acts by binding to plasminogen and blocking the interaction of plasmin(ogen) with fibrin, thereby preventing dissolution of the fibrin clot. Tranexamic acid (Transamin®) is indicated in Japan for use in certain conditions with abnormal bleeding or bleeding tendencies in which local or systemic hyperfibrinolysis is considered to be involved. This article reviews the efficacy and tolerability of tranexamic acid in conditions amenable to antifibrinolytic therapy and briefly overviews the pharmacological properties of the drug. In large, randomized controlled trials, tranexamic acid generally significantly reduced perioperative blood loss compared with placebo in a variety of surgical procedures, including cardiac surgery with or without cardiopulmonary bypass, total hip and knee replacement and prostatectomy. In many instances, tranexamic acid also reduced transfusion requirements associated with surgery. It also reduced blood loss in gynaecological bleeding disorders, such as heavy menstrual bleeding, postpartum haemorrhage and bleeding irregularities caused by contraceptive implants. Tranexamic acid significantly reduced all-cause mortality and death due to bleeding in trauma patients with significant bleeding, particularly when administered early after injury. It was also effective in traumatic hyphaema, gastrointestinal bleeding and hereditary angioneurotic oedema. While it reduces rebleeding in subarachnoid haemorrhage, it may increase ischaemic complications. Pharmacoeconomic analyses predicted that tranexamic acid use in surgery and trauma would be very cost effective and potentially life saving. In direct comparisons with other marketed agents, tranexamic acid was at least as effective as ε-aminocaproic acid and more effective than desmopressin in surgical procedures. It was more effective than desmopressin, etamsylate, flurbiprofen, mefenamic acid and norethisterone, but less effective than the levonorgestrel-releasing intra-uterine device in heavy menstrual bleeding and was as effective as prednisolone in traumatic hyphaema. Tranexamic acid was generally well tolerated. Most adverse events in clinical trials were of mild or moderate severity; severe or serious events were rare. Therefore, while high-quality published evidence is limited for some approved indications, tranexamic acid is an effective and well tolerated antifibrinolytic agent.
氨甲环酸是一种氨基酸赖氨酸的合成衍生物，是一种抗纤维蛋白溶解剂，通过与纤溶酶原结合并阻止纤溶酶原与纤维蛋白的相互作用，从而防止纤维蛋白凝块溶解。氨甲环酸（Transamin®）在日本被批准用于某些具有异常出血或出血倾向的情况下，其中局部或全身纤维蛋白溶解被认为是涉及的。本文综述了氨甲环酸在可接受抗纤维蛋白溶解治疗的情况下的疗效和耐受性，并简要概述了该药物的药理学特性。在大型随机对照试验中，氨甲环酸通常与安慰剂相比，在各种手术中，包括伴有或不伴有体外循环的心脏手术、全髋关节和膝关节置换术和前列腺切除术，显著减少围手术期失血。在许多情况下，氨甲环酸还减少了与手术相关的输血需求。它还减少了妇科出血性疾病的出血，如月经过多、产后出血和避孕植入物引起的不规则出血。氨甲环酸显著降低创伤患者大出血的全因死亡率和因出血导致的死亡率，特别是在受伤后早期给予时。它在创伤性前房积血、胃肠道出血和遗传性血管神经性水肿中也有效。虽然它减少了蛛网膜下腔出血的再出血，但可能增加缺血性并发症。药物经济学分析预测，氨甲环酸在手术和创伤中的使用将非常具有成本效益，并且可能挽救生命。与其他已上市药物的直接比较表明，氨甲环酸在手术中与 ε-氨基己酸一样有效，在手术中比去氨加压素更有效。它比去氨加压素、氨甲苯酸、氟比洛芬、甲芬那酸和炔诺酮更有效，但在月经过多方面不如左炔诺孕酮释放宫内节育器有效，在创伤性前房积血方面与泼尼松龙一样有效。氨甲环酸通常耐受性良好。临床试验中的大多数不良事件为轻度或中度严重程度；严重或严重事件很少见。因此，虽然一些已批准的适应症的高质量已发表证据有限，但氨甲环酸是一种有效的且耐受性良好的抗纤维蛋白溶解剂。
