Transtat 500 Mechanism of Action

Pharmacotherapeutic group: Antihemorrhagics, Antifibrinolytics. ATC Code: B02AA02.
Pharmacology: Pharmacodynamics: Tranexamic acid is an antifibrinolytic compound which is a potent competitive inhibitor of the activation of plasminogen to plasmin. At much higher concentrations it is a non-competitive inhibitor of plasmin. The inhibitory effect of tranexamic acid in plasminogen activation by urokinase has been reported to be 6-100 times and by streptokinase 6-40 times greater than that of aminocaproic acid. The antifibrinolytic activity of tranexamic acid is approximately ten times greater than that of aminocaproic acid.
Pharmacokinetics: Absorption: Peak plasma Tranexamic acid concentration is obtained immediately after intravenous administration (500 mg). Then concentration decreases until the 6th hour. Elimination half-life is about 3 hours.
Distribution: Tranexamic acid administered parenterally is distributed in a two compartment model. Tranexamic acid is delivered in the cell compartment and the cerebrospinal fluid with delay. The distribution volume is about 33% of the body mass.
Tranexamic acid crosses the placenta, and may reach one hundredth of the serum peak concentration in the milk of lactating women.
Elimination: Tranexamic acid is excreted in urine as unchanged compound. 90% of the administered dose is excreted by the kidney in the twelve first hours after administration (glomerular excretion without tubular reabsorption).
Following oral administration, 1.13% and 39% of the administered dose were recovered after 3 and 24 hours respectively.
Plasma concentrations are increased in patients with renal insufficiency.