Source: Health Products Regulatory Authority (ZA) Publisher: Biotech Laboratories (Pty) Ltd, Ground Floor, Block K West, Central Park, 400 16<sup>th</sup> Street, Randjespark, Midrand 1685, South Africa, Tel. nr: 011 848 3050
Pharmacological Classification: 8.1 Coagulants, haemostatics
Pharmacotherapeutic group: Antihaemorrhagics, antifibrinolytics, amino acids
ATC Code: B02AA02
Tranexamic acid exerts an anti-haemorrhagic activity by inhibiting the fibrinolytic properties of plasmin.
A complex involving tranexamic acid, plasminogen is constituted; the tranexamic acid being linked to plasminogen when transformed into plasmin.
The activity of the tranexamic acid-plasmin complex on the activity on fibrin is lower than the activity of free plasmin alone.
In vitro studies showed that high tranexamic dosages decreased the activity of complement.
Peak plasma concentrations of tranexamic acid are obtained rapidly after a short intravenous infusion after which plasma concentrations decline in a multi-exponential manner.
The plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen. Tranexamic acid does not bind to serum albumin. The initial volume of distribution is about 9 to 12 litres.
Tranexamic acid passes through the placenta. Following administration of an intravenous injection of 10 mg/kg to 12 pregnant women, the concentration of tranexamic acid in serum ranged 10-53 microgram/ml while that in cord blood ranged 4-31 microgram/ml. Tranexamic acid diffuses rapidly into joint fluid and the synovial membrane. Following administration of an intravenous injection of 10 mg/kg to 17 patients undergoing knee surgery, concentrations in the joint fluids were similar to those seen in corresponding serum samples. The concentration of tranexamic acid in a number of other tissues is a fraction of that observed in the blood (breast milk, one hundredth; cerebrospinal fluid, one tenth; aqueous humor, one tenth). Tranexamic acid has been detected in semen where it inhibits fibrinolytic activity but does not influence sperm migration.
It is excreted mainly in the urine as unchanged medicine. Urinary excretion via glomerular filtration is the main route of elimination. Renal clearance is equal to plasma clearance (110 to 116 ml/min). Excretion of tranexamic acid is about 90 % within the first 24 hours after intravenous administration of 10 mg/kg body weight. Elimination half-life of tranexamic acid is approximately 3 hours.
Plasma concentrations increase in patients with renal failure.
No specific pharmacokinetic study has been conducted in children.
No non-clinical study was performed.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.