PROSTATECTOMY: 5-10 ml by slow intravenous injection every eight hours (the first injection being given during the operation) for the first three days after surgery thereafter 1-1.5 gm orally three to four times daily until macroscopic haematuria is no longer present. For the indications listed below the following doses are recommended. The recommended standard dose is 1 to 1.5 gm or 5-10 ml by slow intravenous injection at a rate of 1 ml/minute, two to three times daily. Intravenous administration is necessary only if it is difficult to give adequate doses by mouth. Consider EEG monitoring of patients with a history of seizure. Off-target antagonism of GABA(A) receptors may be associated with the development of convulsions and hyperexcitability following tranexamic acid administration - the risk appears higher with improper administration or administration during cardiovascular surgery. 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). 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. At much higher concentrations it behaves as a noncompetitive inhibitor of plasmin similar to aminocaproic acid, a similar antifibrinolytic which is 10-fold less potent. Tranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. After intravenous administration 45% of the dose is excreted in the urine during the first day. After oral administration, about 40% of the dose is excreted in the urine during the first 24 hours. Maximum serum levels are reached within 2-3 hours. PHARMACOKINETICS: Tranexamic acid is rapidly absorbed from the gastrointestinal tract. Tranexamic acid is excreted unchanged in the urine. The plasma protein binding seems fully accounted by its binding to plasminogen.

Plasma protein binding is 3% at therapeutic plasma levels. the conversion of plasminogen to plasmin, in the fibrinolytic system.The half life is 1-2 hours.

PHARMACOLOGICAL ACTIONS: Tranexamic acid has a strong inhibitory effect on the activation of plasminogen, i.e.

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