Product Information
Registration Status: ActiveCYKLOKAPRON TABLET 500mg is approved to be sold in Singapore with effective from 1989-09-03. It is marketed by PFIZER PTE LTD, with the registration number of SIN02487P.
This product contains Tranexamic Acid 500mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Pfizer Italia S.r.l. in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Antifibrinolytic hemostatic used in severe hemorrhage. [PubChem]
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.
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.
Pharmacokinetics
- 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.
- Distribution
- * 9 to 12 L
- Metabolism
- Only a small fraction of the drug is metabolized (less than 5%).
- Elimination
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.
Active Ingredient/Synonyms
Acide tranexamique | Acido tranexamico | Acidum tranexamicum | Tranexamsaeure | Tranexmic acid | Tranhexamic acid | Trans AMCHA | trans-4-(Aminomethyl)cyclohexanecarboxylic acid | trans-4-aminomethylcyclohexane-1-carboxylic acid | trans-Amcha | trans-Tranexamic acid | Tranexamic Acid |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.