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Pharmacology: In physiological and pathologic conditions, fibrinolysis affects enhancement of vascular permeability, and relevant to the development, progression and healing of hemorrhage, allergy and other biological reactions induced by plasmin. Tranexamic acid inhibits the activity of plasmin, thereby exhibiting antihemorrhagic, antiallergic and anti-inflammatory effects.
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 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 eg, 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.
Antiallergic and Anti-Inflammatory Action: Tranexamic acid inhibits plasmin-induced production of kinins and other active peptides, that cause enhancement of vascular permeability, allergy and inflammatory lesions (as demonstrated in guinea pigs and rats).
Clinical Studies: Hemostatic Action: A hemostatic effect of Transamin was observed in 2063 out of 2802 patients (73.6%) (capsule and tablet) and in 594 out of 709 patients (83.8%) (ampoule) with a bleeding tendency caused by diseases eg, leukemia, aplastic anemia and purpura, which are considered to be associated with systemic hyperfibrinolysis, or abnormal bleeding eg, pulmonary, nasal, vaginal and renal hemorrhage, prostatic hemorrhage (ampoule only), and intra- and postoperative bleeding.
Antiallergic and Anti-Inflammatory Actions: Skin Disorders: Capsule/Tablet: Transamin was effective for symptoms eg, pruritus, swelling and erythema in 135 out of 223 patients (60.5%) in an open-labeled clinical study conducted to evaluate its effect on skin disorders (eg, eczema and similar conditions, urticaria, drug eruptions and toxidermia).
In a double-blind comparative study conducted to evaluate the effects of Transamin on pruritus, redness, swelling and other symptoms in 67 patients with skin disorders (eczema and similar conditions, drug eruptions and toxidermia), 35 patients were assigned to Transamin and 32 to placebo. The efficacy rate (good to excellent responses) was 62.9% (22 cases) for Transamin vs 31.3% (10 cases) for placebo (p<0.05).
Ampoule: Symptoms of skin disorders eg, eczema and similar conditions or urticaria, etc improved in 220 out of 283 patients (77.7%). Otorhinolaryngological Diseases: Capsule/Tablet: In an open-labeled clinical study performed on 168 patients with tonsillitis, laryngopharyngitis, stomatitis and gingivitis, the effects against pain, swelling and redness, etc were observed in 119 patients (70.8%).
In a double-blind comparative study performed to determine effects of Transamin in 168 patients with otorhinolaryngological diseases (eg, acute pharyngolaryngitis, acute tonsillitis, stomatitis), 84 patients were assigned to Transamin and 84 to placebo. The efficacy rate (good to excellent responses) was 52.4% (44 cases) for Transamin vs 26.2% (22 cases) for placebo (p<0.05).
Pharmacokinetics: Blood Concentration: Capsule/Tablet: When a single dose of tranexamic acid was administered orally to healthy adults, the pharmacokinetic parameters were as shown as follows: Pharmacokinetic Parameters After a Single Oral Dose of Tranexamic Acid (n=5): Tmax: 2-3 hrs; Cmax: 5.5 mcg/mL (capsule), 6 mcg/mL (tablet); t½: 3.3 hrs.
Blood concentration-time profile after a single oral dose of tranexamic acid. Capsule: See Figure 1.
Click on icon to see table/diagram/imageTablet: See Figure 2.
Click on icon to see table/diagram/imageAmpoule: When a single dose of 500 mg tranexamic acid was administered IM or 1000 mg was administered IV to healthy adults, the time plasma concentration were as follows: See Figure 3.
Click on icon to see table/diagram/imagePharmacokinetic parameters after a single IV or IM dose of tranexamic acid are as follows: 500-mg Dose (IM): Tmax: 0.5 hr; Cmax: 21.2 mcg/mL; t½: 2 hrs.
1000-mg Dose (IV): Cmax: 60 mcg/mL (15 min after administration); t½: 1.9 hrs; Vd: 42.4 L.
Distribution: Reference Information (Animal Study):
Capsule/Tablet: When a single dose of 14C-tranexamic acid was administered orally to rats, the concentration in most organs reached peak values as well as the blood concentration after 2 hrs.
Levels in kidney and liver were higher, and those of other organs were lower than that of the blood.
Ampoule: When 14C-tranexamic acid was administered IV or IM to mice, the distribution in the tissue was highest in the liver, kidneys and pulmonary, followed by pancreas, adrenals, spleen, prostate, colon, uterus, heart and muscle. Levels in the brain were low.
Metabolism and Excretion: Capsule/Tablet: When a single dose (250 or 500 mg) of tranexamic acid was administered orally to healthy adults, it was rapidly absorbed and about 40-70% of the administered dose was excreted as unchanged form in the urine within 24 hrs.
Ampoule: When a single dose of 500 mg tranexamic acid was administered IM or 1000 mg was administered IV to healthy adults, it was rapidly absorbed, and about 80% and 76% of the administered dose, was respectively, excreted as unchanged form in the urine within 24 hrs of administration.
