Pharmacology of Drug-Tranexamic Acid

Mechanism of Action

Tranexamic acid exerts antifibrinolytic effect by forming a reversible complex with plasminogen through the lysine binding site of fibrin and thus displaces the plasminogen from the fibrin surface ; preventing the binding of plasmin to fibrinogen or fibrin monomers. It inhibits the activation of plasminogen (i.e. formation of plasmin). It also acts as a weak non competitive inhibitor of plasmin and blocks it`s action on fibrin.

Pharmaco Kinetics
Absorption: About 40% is absorbed orally. Distribution: Widely distributed in the body. Excretion: Excreted mainly as unchanged drug.

Half Life
2 hours

Adverse Effects
1.Nausea 2.Diarrhoea 3.Gastrointestinal problems 4.Headache 5.Hypotension 6.Giddiness 7.Thrombophlebitis at injected vein 8.Impairment of Colour vision

1.Thromboembolic disorders 2.Subarachnoid haemorrhage 3.Massive upper urinary tract haemorrhage 4.Colour vision disorders 5.Thrombophlebitis 6.Hepatic impairment 7.Severe renal impairment

Special Precautions
1.Avoid rapid I.V. administration 2.Lower dosage adjustment is required in renal impairment 3.Monitor liver functioning during long term use


Breast Feeding
Use with caution

Old Age
Use with caution

1.Surgical procedures 2.Menorrhagia 3. Metrorrhagia 4.Post partum haemorrhage 5.Haemorrhage after abortion 6.Haemorrhage due to contraceptive device insertion 7.Tooth extractions and haemorrhage in other dental procedures 8.Epistaxis 9.Haemoptysis 10.Gastrointestinal bleeding 11.Prostatectomy 12.Tonsillectomy 13.Fibrinolysis 14.Ocular trauma 15.Orthopedic surgery 16.Cardiovascular surgery

Oral: 3 to 4gm/day in 3 to 4 divided doses or 15 to 25mg/kg body wt. 3 to 4 times daily. I.V.: 1.5 to 3gm/day in 3 divided doses or 10 to 15mg/kg body wt. 3 times daily. Administered as slow I.V. injection or as continuous infusion; at a rate of 25 to 50mg/kg/day.

Store below 25 degree C. and protects from light. Keep out of reach of children.

Over Dose
Treatment is supportive and symptomatic. Remove drug from the body by induced emesis, gastric lavage and administer activated charcoal to reduce absorption. Maintain adequate diuresis with the aid of fluids and diuretics.