Tranexamic Acid (3 brand names, 3 dosage forms, 3 routes)
Available dosage forms: SOLUTION, INJECTABLE, TABLET.
Routes of administration: INTRAVENOUS, INJECTION, ORAL.
Brand Names
- CYKLOKAPRON
- LYSTEDA
- TRANEXAMIC ACID
Related Health Topics
Related Conditions
Indications and Usage
Tranexamic acid tablets are indicated for the treatment of cyclic heavy menstrual bleeding in females of reproductive potential [see Clinical Studies (14)].
Drug Interactions
No drug-drug interaction studies were conducted with tranexamic acid tablets.
Mechanism of Action
Tranexamic acid is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure. The antifibrinolytic effects of tranexamic acid are mediated by reversible interactions at multiple binding sites within plasminogen. Native human plasminogen contains 4 to 5 lysine binding sites with low affinity for tranexamic acid (K d= 750 µmol/L) and 1 with high affinity (K d= 1.1 µmol/L). The high affinity lysine site of plasminogen is involved in its binding to fibrin. Saturation of the high affinity binding site with tranexamic acid displaces plasminogen from the surface of fibrin. Although plasmin may be formed by conformational changes in plasminogen, binding to and dissolution of the fibrin matrix is inhibited.
Overdosage
There are no known cases of intentional overdose with tranexamic acid tablets and no subjects in the clinical program took more than 2 times the prescribed amount of tranexamic acid tablets in a 24-hour period (>7800 mg/day). However, cases of overdose of tranexamic acid have been reported. Based on these reports, symptoms of overdose may include gastrointestinal (nausea, vomiting, diarrhea); hypotensive (e.g., orthostatic symptoms); thromboembolic (arterial, venous, embolic); visual impairment; mental status changes; myoclonus; or rash. No specific information is available on the treatment of overdose with tranexamic acid tablets. In the event of overdose, employ the usual supportive measures (e.g., clinical monitoring and supportive therapy) as dictated by the patient’s clinical status.