Transamin Mechanism of Action

PHARMACOLOGY: In physiological and pathologic conditions, fibrinolysis affects enhancement of vascular permeability and relevant to the development, progression and healing of hemorrhage induced by plasmin. Tranexamic acid inhibits the activity of plasmin, thereby exhibiting antihemorrhagic effects.
1. 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 inhibits fibrinolysis induced by plasmin. In addition, in the presence of antiplasmins such as α₂-macroglobulin in the plasma, the antifibrinolytic action of tranexamic acid is even further strengthened.
2. Hemostatic action: When the blood level of plasmin is abnormally elevated, various phenomena occur such as inhibition of platelet aggregation and decomposition of coagulation factors.
Even a slight elevation in the blood level of plasmin specifically induces fibrinolysis. Tranexamic acid is considered to exhibit a hemostatic effect by inhibiting fibrinolysis in common types of hemorrhage.
Tablet: CLINICAL STUDIES: Hemostatic Action: A hemostatic effect of Transamin was observed in 2,063 out of 2,802 patients (73.6%) with a bleeding tendency caused by diseases such as leukemia, aplastic anemia and purpura, which are considered to be associated with systemic hyperfibrinolysis or abnormal bleeding, such as pulmonary hemorrhage, vaginal hemorrhage, renal bleeding and intraoperative and postoperative bleeding.
PHARMACOKINETICS: 1. Blood concentration: The concentration in the blood, when 1,000 mg and 2,000 mg of tranexamic acid were administered orally to healthy adults, reached peak values 7 μg/ml and 14.4 μg/ml within 2-3 hours after administration.
When a single dose of tranexamic acid was administered orally to healthy adults, the pharmacokinetic parameters were as shown as follows. (See Table 2 and figure.)

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2. Distribution: Reference information (animal study): When a single dose of ¹⁴C-tranexamic acid was administered orally to rats, the concentration in most organs reached the peak values as well as the blood concentration after 2 hours. Levels in kidney and liver were higher and those of other organs were lower than that of the blood.
3. Metabolism and excretion: When a single dose (250 mg or 500 mg) of tranexamic acid was administered orally to healthy adults, it was rapidly absorbed and about 40 to 70% of the administered dose was excreted as unchanged form in the urine within 24 hours.