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Name: Tranexamic Acid
PubChem Compound ID: 1549136
Description: Antifibrinolytic hemostatic used in severe hemorrhage.
Molecular formula: C8H15NO2
Molecular weight: 157.21 g/mol
1197-18-8; ZINC01542907
Name: Tranexamic Acid
Name (isomeric): DB00302
Drug Type: small molecule
Description: Antifibrinolytic hemostatic used in severe hemorrhage.
Tranhexamic acid; Tranexamsaeure; Trans AMCHA; trans-Tranexamic acid; trans-Amcha; trans-4-aminomethylcyclohexane-1-carboxylic acid; tranexmic acid
Brand: Amcha, Cyclocapron, Frenolyse, Transamin, Amstat, Anvitoff, Ugurol, Cyklokapron, Carxamin, Rikavarin-S, Emorhalt, Trasamlon, Tranexan, Mastop, Tamcha, Amikapron, Rikavarin
Category: Antifibrinolytic Agents
CAS number: 1197-18-8
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.
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 vitr...
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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 activit...
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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.
Protein binding: The plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen (does not bind serum albumin).
Biotransformation: Only a small fraction of the drug is metabolized (less than 5%).
Route of elimination: Urinary excretion is the main route of elimination via glomerular filtration.
Half Life: Biological half-life in the joint fluid is about 3 hours.
Clearance: 110 - 116 mL/min
Toxicity: Oral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
Affected organisms: Humans and other mammals