Capsule: Each capsule contains: Tranexamic acid 500 mg.
Tranexamic acid is an anti-fibrinolytic agent used mainly in the treatment and prophylaxis of haemorrhage associated with excessive fibrinolysis. It is given by mouth, by slow intravenous injection, or limited to gastrointestinal disturbances, hypotension has occurred, particularly after rapid intravenous infusion.
Injection: Each mL contains Tranexamic Acid Ph. Eur. 100 mg; Water for Injection USP q.s.; Excipients q.s.
Each mL of the sterile solution for intravenous injection contains 100 mg Tranexamic Acid. Its Chemical Name is trans-4-(aminomethyl) cyclohexanecarboxylic acid.
Molecular Formula: C8H15NO2.
Molecular Weight: 157.2.
Pharmacology: Injection: Tranexamic acid is an antifibrinolytic agent that inhibits the activation of plasminogen to plasmin (fibrinolysin-enzyme that degrades fibrin clots), fibrinogen, and other plasma proteins, including the procoagulant factors V and VIII. And at much higher concentrations, a noncompetitive inhibitor of plasmin ie, have 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. 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).
Plasma protein binding is 3% at the therapeutic plasma levels. The plasma protein binding seems fully accounted for by its binding to plasminogen. Tranexamic acid is excreted unchanged in the urine.
Approximately 90% of an intravenously administered Tranexamic acid dose is excreted largely unchanged in the urine within 24 hours.
Pharmacokinetics: Capsule: Tranexamic acid is rapidly absorbed from the gastrointestinal tract: absorption is 30 to 50%. It is widely distributed throughout the body, diffuses across the placenta and has been detected in breast milk. It has a plasma elimination half-life of about 2 hours. It is excreted in the urine mainly as unchanged drug.
Capsule: It is used in the treatment and prophylaxis of haemorrhage associated with excessive fibrinolysis. It is also used in the prophylaxis of hereditary angioedema.
Injection: Tranexamic acid is indicated in haemorrhage or risk of haemorrhage, increased fibrinolysis or fibrinogenolysis, general fibrinolysis as in prostatic and pancreatic cancer, after thoracic and other major surgery; in obstetrical complications such as abruption placentae and post-partum haemorrhage; in leukemia and liver diseases and in connection with thrombolytic therapy with streptokinase. Also in hereditary angioneurotic oedema.
1 to 1.5 g (or 15 to 25 mg/kg body weight) twice to four times a day or as prescribed by the physician.
5-10 mL by slow intravenous injection at a rate of 1 mL/minute, two to three times daily. For the indications listed as follows the following doses are recommended.
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.
Tranexamic acid injection may be applied topically to the nasal mucosa of patients suffering from epistaxis. This can be done by soaking a gauze strip in the solution, and then packing the nasal cavity.
Dental Surgery in Patients with Haemophilia:
For short-term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy. Immediately before surgery, 10 mg per kg body-weight should be given intravenously.
1.0 g (10 mL) by slow intravenous injection three to four times daily. With fibrinolysis in conjunction with diagnosed, increased intravascular coagulation i.e. defibrillation syndrome, an anticoagulant such as heparin may be given with caution.
Dosage in renal insufficiency:
For patients with impaired renal function there is a risk of drug accumulation therefore the dose should be reduced with respect to the renal function. (See table.)
Click on icon to see table/diagram/image
Injection: Active thromboembolic disease, such as deep vein thrombosis, pulmonary embolism and cerebral thrombosis.
Subarachnoid hemorrhage, the limited clinical experience shows that a reduced risk for rebleeding is offset by an increase in the rate of cerebral ischemia.
Hypersensitivity to Tranexamic acid or to any of the ingredients.
Patients with acquired defective color vision, since this prohibits measuring one endpoint that should be followed as a measure of toxicity.
Capsule: Should not be used in patients with active intravenous clotting because of the risk of thrombosis. Patients with a predisposition to thrombosis are also at risk if given anti-fibrinolytic therapy.
Haemorrhage due to disseminated intravenous coagulation should therefore not be treated with anti-fibrinolytic compounds unless the condition is predominantly due to disturbances in fibrinolytic mechanisms; tranexamic acid has been used when the latter conditions are met, but with careful monitoring and anti-coagulant cover.
Injection: Patients with irregular menstrual bleeding should not use Tranexamic acid until the cause of the irregularity has been established. If menstrual bleeding is not adequately reduced by Tranexamic acid, an alternative treatment should be considered.
Patients with a high risk of thrombosis (a previous thromboembolic event and a family history of thromboembolic disease) should use Tranexamic acid only if there is a strong medical indication and under strict medical supervision.
Patients with disseminated intravascular coagulation (DIC), who require treatment with Tranexamic acid, must be under the strict supervision of a physician experienced in treating this disorder.
The blood levels are increased in patients with renal insufficiency. Therefore a dose reduction is recommended, see Dosage & Administration. In haematuria from the upper urinary tract blood clots can, in a few cases, lead to ureteric Obstruction.
In the long-term treatment of patients, regular eye examination should be performed. The preparation should not be used in patients with acquired defective colour vision. If a colour vision disorder should occur during the course of treatment, the drug should be discontinued.
No retinal changes have been reported or established in eye examination performed on patient treated with Tranexamic acid over periods ranging from several weeks to months. For patients who are to receive continual treatment with Tranexamic acid for several weeks and ophthalmological examination is advised (including visual acuity, colour vision, eyegrounds, field of vision etc.) if possible before commencing treatment and at regular intervals during treatment.
Injection: Use in Pregnancy: Tranexamic acid crosses the placenta. Clinical experience of use in pregnant women is limited. Usual caution with the use of drugs in pregnancy should be observed.
Use in Lactation: Tranexamic acid passes into breast milk to a concentration of approximately 100 of the concentration in the maternal blood. An antifibrinolytic effect in the infant is unlikely.
Injection: Pregnancy: Tranexamic acid crosses the placenta. Clinical experience of use in pregnant women is limited. Usual caution with the use of drugs in pregnancy should be observed.
Lactation: Tranexamic acid passes into breast milk to a concentration of approximately 100 of the concentration in the maternal blood. An antifibrinolytic effect in the infant is unlikely.
Tranexamic acid appears to be well tolerated. It can produce dose-related gastro-intestinal disturbances. Hypotension has occurred particularly after rapid intravenous administration. Thrombotic complications have been reported in patients receiving tranexamic acid, but these are usually a consequence of its inappropriate use.
Dose dependent gastro-intestinal disorders (nausea, vomiting, diarrhea) may occur but disappear when the dosage is reduced. Rapid intravenous injection may cause dizziness and/or hypotension. Rare cases of thromboembolic events have been reported.
Injection: The solution for injection may be mixed with the following solutions: isotonic sodium chloride; isotonic glucose; 20% fructose; 10% invertose; dextran 40; dextran 70; Ringer's solution.
Tranexamic acid may be mixed with Heparin.
Tranexamic acid should not be added to blood for transfusion or to injections containing penicillin.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Capsule: Store at temperatures not exceeding 30°C.
Injection: Store at a temperature not exceeding 25°C.
Shelf-Life: 24 months.
B02AA02 - tranexamic acid ; Belongs to the class of amino acid antifibrinolytics. Used in the treatment of hemorrhage.
Cap 500 mg x 100's. Soln for inj (amp) 100 mg/mL (clear, colourless, free from visible extraneous particulate matter) x 5 mL x 5's.