Department of Pharmaceutical and Biomedical Sciences, Raabe College of Pharmacy, Ohio Northern University, Ada, USA.
Ann Pharmacother. 2012 Jul-Aug;46(7-8):1047-53. doi: 10.1345/aph.1R025. Epub 2012 Jul 17.
To review the pharmacology, pharmacokinetics, efficacy, and safety profile of an oral modified-release (MR) formulation of tranexamic acid.
Literature was accessed through MEDLINE (1966-July 2012), Iowa Drug Information Service (1997-July 2012), and bibliographies of pertinent articles. Search terms included tranexamic acid, Lysteda, menorrhagia, menstrual blood loss, and heavy menstrual bleeding.
All available English-language abstracts and human studies were identified for review. Data provided by the manufacturer and the Food and Drug Administration were also evaluated. Efficacy was evaluated in 2 clinical trials, change in quality of life was evaluated in 3 clinical trials, and safety was evaluated in 4 clinical trials.
Tranexamic acid is a synthetic lysine analogue with antifibrinolytic activity. It interferes with the binding of plasminogen to fibrin, resulting in enhanced fibrin clot integrity. A novel MR formulation of oral tranexamic acid is approved for treatment of cyclic heavy menstrual bleeding. MR tranexamic acid is initiated at the beginning of heavy menstrual bleeding and can be taken for up to 5 days per cycle. Clinical trials show it to be safe and effective. Dosage adjustments are needed for women with renal insufficiency. Adverse effects are considered mild to moderate, with the most common being menstrual discomfort, headache, and back pain. The most significant safety concerns relate to the risk of thromboembolism.
MR tranexamic acid offers a new first-line therapy for patients with cyclic heavy menstrual bleeding. It is reported to be safe and effective. There are no labeled equivalents to MR tranexamic acid for cyclic heavy menstrual bleeding.
综述氨甲环酸口服控释制剂的药理学、药代动力学、疗效和安全性。
通过 MEDLINE（1966 年-2012 年 7 月）、爱荷华药物信息服务（1997 年-2012 年 7 月）和相关文章的参考文献检索文献。检索词包括氨甲环酸、Lysteda、月经过多、月经失血过多和经量过多。
所有可用的英文摘要和人类研究均被确定进行综述。还评估了制造商和美国食品和药物管理局提供的数据。在 2 项临床试验中评估了疗效，在 3 项临床试验中评估了生活质量的变化，在 4 项临床试验中评估了安全性。
氨甲环酸是一种合成的赖氨酸类似物，具有抗纤维蛋白溶解活性。它干扰纤溶酶原与纤维蛋白的结合，从而增强纤维蛋白凝块的完整性。一种新型的氨甲环酸口服控释制剂已被批准用于治疗周期性经量过多。控释氨甲环酸在月经出血过多的开始时开始服用，每个周期最多可服用 5 天。临床试验表明其安全有效。肾功能不全的妇女需要调整剂量。不良反应被认为是轻度至中度，最常见的是月经不适、头痛和背痛。最严重的安全问题与血栓栓塞风险有关。
控释氨甲环酸为周期性经量过多的患者提供了一种新的一线治疗方法。据报道，它安全有效。目前没有针对周期性经量过多的控释氨甲环酸的等效药物。
