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Amikapron

Amikapron - General Information

Antifibrinolytic hemostatic used in severe hemorrhage.

 

Pharmacology of Amikapron

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).

 

Amikapron for patients

 

Amikapron Interactions

No information provided.

 

Amikapron 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.

 

Additional information about Amikapron

Amikapron 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.
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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Tranexamic Acid
Synonyms: Tranexamsaeure; tranexmic acid; Tranhexamic acid; Trans AMCHA; trans-Amcha; trans-Tranexamic acid; trans-4-aminomethylcyclohexane-1-carboxylic acid
Drug Category: Antifibrinolytic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Tranexamic Acid: Amcha; Amikapron; Amstat; Anvitoff; Carxamin; Cyclocapron; Cyklokapron; Emorhalt; Frenolyse; Mastop; Rikavarin; Rikavarin-S; Tamcha; Tranexan; Transamin; Trasamlon; Ugurol;
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 (Overdose): Oral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
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%).
Half Life: Biological half-life in the joint fluid is about 3 hours.
Dosage Forms of Amikapron: Solution Intravenous
Tablet Oral
Chemical IUPAC Name: 4-(aminomethyl)cyclohexane-1-carboxylic acid
Chemical Formula: C8H15NO2
Tranexamic Acid on Wikipedia: http://en.wikipedia.org/wiki/Tranexamic_acid
Organisms Affected: Humans and other mammals