Clinical Trials Unit, London School of Hygiene and Tropical Medicine, London, UK.
Département des maladies des voies respiratoires, Hôpital Foch, Suresnes, France.
Int J Gynaecol Obstet. 2022 Jun;158 Suppl 1(Suppl 1):40-45. doi: 10.1002/ijgo.14201.
To review available data on tranexamic acid (TXA) plasma concentration needed to inhibit fibrinolysis and the time to achieve this concentration when giving TXA by different routes in humans. To identify ongoing trials assessing alternatives to intravenous TXA administration.
We updated two previous systematic reviews by searching MEDLINE, EMBASE, OviSP, and ISI Web of Science from database inception to July 2021. We also searched the WHO International Clinical Trials Registry Platform for ongoing trials to July 2021. Titles and abstracts were screened for relevant trials. Two reviewers independently reviewed and agreed the trials to be included.
Plasma TXA concentrations over 10 mg/L provide near maximal inhibition of fibrinolysis, with concentrations over 5 mg/L providing partial inhibition. Oral TXA tablets take about 1 h to reach a plasma concentration of 5 mg/L in postpartum women. Studies in healthy volunteers and shocked trauma patients show that intramuscular TXA achieves a plasma level of over 10 mg/L within 15 min. One trial is ongoing to determine the pharmacokinetics of intramuscular and oral solution TXA in pregnant women.
Intramuscular TXA in healthy volunteers and shocked trauma patients reaches therapeutic concentration rapidly. Oral TXA tablets take too long to reach the minimum therapeutic concentration in postpartum women.
回顾在人体中通过不同途径给予氨甲环酸（TXA）时，达到抑制纤维蛋白溶解所需的 TXA 血浆浓度数据，并确定达到该浓度所需的时间。确定正在评估 TXA 静脉给药替代方案的试验。
我们通过检索 MEDLINE、EMBASE、OviSP 和 ISI Web of Science 数据库，更新了之前的两项系统评价，检索时间为数据库建立至 2021 年 7 月。我们还在世界卫生组织国际临床试验注册平台上搜索了截至 2021 年 7 月正在进行的试验。筛选标题和摘要以确定相关试验。两名审查员独立审查并同意纳入的试验。
血浆 TXA 浓度超过 10mg/L 可提供接近最大程度的纤维蛋白溶解抑制，浓度超过 5mg/L 可提供部分抑制。产后妇女口服 TXA 片剂约 1 小时即可达到 5mg/L 的血浆浓度。在健康志愿者和休克创伤患者的研究中，肌内注射 TXA 在 15 分钟内达到超过 10mg/L 的血浆水平。一项试验正在进行中，以确定孕妇肌内注射和口服溶液 TXA 的药代动力学。
健康志愿者和休克创伤患者的肌内 TXA 迅速达到治疗浓度。口服 TXA 片剂在产后妇女中达到最低治疗浓度需要太长时间。
