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Tranexamic Acid
- indication:For use in patients with hemophilia for short term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. It can also be used for excessive bleeding in menstruation, surgery, or trauma cases.
- pharmacologypharmacology:
- mechanism: Tranexamic acid competitively inhibits activation of plasminogen (via binding to the kringle domain), thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins, including the procoagulant factors V and VIII. Tranexamic acid also directly inhibits plasmin activity, but higher doses are required than are needed to reduce plasmin formation.
- toxicity: Oral LD<sub>50</sub> in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
- absorprion: Absorption of tranexamic acid after oral administration in humans represents approximately 30 to 50% of the ingested dose and bioavailability is not affected by food intake.
- halflife: Biological half-life in the joint fluid is about 3 hours.
- roouteelimination: Urinary excretion is the main route of elimination via glomerular filtration.
- volumedistribution: * 9 to 12 L
- clearance: * 110 - 116 mL/min