Pharmacokinetics and bioavailability of tranexamic acid

Abstract

Tranexamic acid 1 g was given intravenously to three healthy volunteers. Plasma concentrations decayed in three monoexponential phases. Most elimination took place during the first eight hours, giving an apparent elimination half-life of approximately two hours. Plasma clearance ranged between 110-116 ml/min. The urinary recovery of tranexamic acid exceeded 95% of the dose. Ten healthy volunteers were given tranexamic acid 2 g orally on an empty stomach, and together with a meal. Food had no influence on the absorption of tranexamic acid, as judged by comparison of the peak plasma concentration, the time required to reach the peak, the AUC from zero to six hours, and the urinary excretion data. The oral bioavailability of tranexamic acid, calculated from 24 h urinary excretion after oral and intravenous administration, was 34% of the dose.

The Antifibrinolytic Drug Tranexamic Acid Reduces Liver Injury and Fibrosis in a Mouse Model of Chronic Bile Duct Injury

“…This analysis yielded a plasma concentration of approximately 0.2 mg/l TA, roughly 16 hours after the last dose of drug. This is similar to levels observed at this time after administration of a therapeutic dose of TA in humans (Eriksson et al, 1974;Pilbrant et al, 1981).…”

“…Thus, one mechanism whereby TA treatment could reduce ANIT-induced liver injury is by inhibiting plasmin-mediated fibrinolysis, thereby stabilizing hepatic fibrin deposits. Our results indicate that plasma TA levels in TA-treated mice sufficiently prolonged clot lysis ex vivo, consistent with inhibition of plasmin, and were similar to those observed in TA-treated humans (Eriksson et al, 1974;Pilbrant et al, 1981). Although TA treatment probably sustained hepatic fibrin deposition in ANIT-treated mice, we were unable to detect a significant increase in hepatic fibrin deposition in ANIT-treated mice given TA.…”

Efficacy of Tranexamic acid in Reducing Blood Loss During Maxillofacial Trauma Surgery–A Pilot Study

“…maintain a therapeutically effective concentration between 5 mg/ dl. Though 30% of the intravenous dose of 10 mg/kg of TXA was detected in the urine during the first hour after administration and the total excretion rose to 45% after 3 hours, approximately 55% remains in circulation upto 24 hours [29]. Therefore maxillofacial trauma surgery does not require a continuous infusion since post operative haemorrhage is of lesser concern than management of immediate haemorrhage in order to clear the airway.…”

An ionizable chromophoric reagent for the analysis of primary amine-containing drugs by capillary electrophoresis

“…The plasma levels of TA in five patients collected at 0.5 h after dosing were in the range of 327-497 mM. Plasma levels of 515-547 mM were reported [18] 5 min after intravenous bolus of 1000 mg TA. The proposed method seems simple for monitoring TA in plasma since HPLC analysis of TA in blood usually needs complicate procedures [19,20].…”