Brands, Medical Use, Clinical Data
Drug Category
Dosage Forms
- Tablets containing 500 mg of tranexamic acid
- Sterile solution for intravenous injection containing 100 mg tranexamic acid
Brands / Synonyms
Amcha; Amikapron; Amstat; Anvitoff; Carxamin; Cyclocapron; Cyklokapron; Emorhalt; Frenolyse; Mastop; Rikavarin; Rikavarin-S; Tamcha; Tranexamic acid EP/JP/CP; Tranexamsaeure; Tranexan; tranexmic acid; Tranhexamic acid; Trans AMCHA; trans-Amcha; trans-Tranexamic acid
; Transamin; Trasamlon; Ugurol
Indications
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.
Pharmacology
Tranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. Tranexamic acid is a competitive inhibitor of plasminogen activation, and at much higher concentrations, a noncompetitive inhibitor of plasmin, i.e., actions similar to aminocaproic acid. Tranexamic acid is about 10 times more potent in vitro than aminocaproic acid. Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. Tranexamic acid in a concentration of 1 mg per mL does not aggregate platelets in vitro. In patients with hereditary angioedema, inhibition of the formation and activity of plasmin by tranexamic acid may prevent attacks of angioedema by decreasing plasmin-induced activation of the first complement protein (C1).
Mechanism of Action
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.
Absorption
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.
Toxicity
Oral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
Biotrnasformation / Drug Metabolism
Only a small fraction of the drug is metabolized (less than 5%).
Contraindications
CYKLOKAPRON Tablets and Injection are contraindicated:
1. In patients with acquired defective color vision, since this prohibits measuring one endpoint that
should be followed as a measure of toxicity.
2. In patients with subarachnoid hemorrhage. Anecdotal experience indicates that cerebral edema and
cerebral infarction may be caused by CYKLOKAPRON in such patients.
3. In patients with active intravascular clotting.
Drug Interactions
No information provided.
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