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Pharmacodynamics: In physiological conditions, fibrinolysis affects enhancements of vascular permeability and relevant to the development, progression and healing of hemorrhage, allergy and other biological reaction induced by plasmin.
Antiplasmin action: Tranexamic acid inhibits the binding of plasmin or plasminogen to fibrin by strongly binding to the lysine binding site (LBS), of fibrin, which is also the binding site for plasmin and plasminogen. Therefore, tranexamic acid strongly inhibit fibrinolysis induced by plasmin. In addition, in the presence of antiplasmins eg. α2-macroglobulin in the plasma, the antifibrinolytic action of tranexamic acid is even further strengthened.
Hemostatic Action: When the blood level of plasmin is abnormally elevated, various phenomena occur e.g., inhibition of platelet aggregation and decomposition of coagulation factors, occur. Even slight elevation in the blood level of plasmin specifically induces fibrinolysis. Tranexamic acid is considered to exhibit hemostatic effects by inhibiting fibrinolysis in common hemorrhages.
Anti-allergic and anti-inflammatory: Tranexamic acid inhibits plasmin-induced production of kinin and other active peptides, that cause enhancement of vascular permeability, allergy and anti-inflammatory lesions (as demonstrated in guinea pigs and rats).
Pharmacokinetics: Absorption: Peak plasma Tranexamic Acid Injection concentration is obtained immediately after IV administration (500mg). Then concentration decreases until the 6th hour. Elimination half-life is about 3 hours.
Distribution: Tranexamic Acid Injection is delivered in the cell compartment and the cerebrospinal fluid with delay. The distribution volume is about 33% of the body mass.
Elimination: Tranexamic Acid Injection 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). Plasma concentrations are increased in patients with renal insufficiency.
