Transtat 500

Each film-coated tablet contains: Tranexamic acid, BP 500 mg.
Excipients/Inactive Ingredients: Microcrystalline cellulose, low substituted hydroxypropyl cellulose, povidone K-30, croscarmellose sodium, colloidal silicon dioxide, purified talc, magnesium stearate, colorcoat FC4S white, isopropyl alcohol and purified water.

Pharmacotherapeutic group: Antihemorrhagics, Antifibrinolytics. ATC Code: B02AA02.
Pharmacology: Pharmacodynamics: Tranexamic acid is an antifibrinolytic compound which is a potent competitive inhibitor of the activation of plasminogen to plasmin. At much higher concentrations it is a non-competitive inhibitor of plasmin. The inhibitory effect of tranexamic acid in plasminogen activation by urokinase has been reported to be 6-100 times and by streptokinase 6-40 times greater than that of aminocaproic acid. The antifibrinolytic activity of tranexamic acid is approximately ten times greater than that of aminocaproic acid.
Pharmacokinetics: Absorption: Peak plasma Tranexamic acid concentration is obtained immediately after intravenous administration (500 mg). Then concentration decreases until the 6th hour. Elimination half-life is about 3 hours.
Distribution: Tranexamic acid administered parenterally is distributed in a two compartment model. Tranexamic acid is delivered in the cell compartment and the cerebrospinal fluid with delay. The distribution volume is about 33% of the body mass.
Tranexamic acid crosses the placenta, and may reach one hundredth of the serum peak concentration in the milk of lactating women.
Elimination: Tranexamic acid is excreted in urine as unchanged compound. 90% of the administered dose is excreted by the kidney in the twelve first hours after administration (glomerular excretion without tubular reabsorption).
Following oral administration, 1.13% and 39% of the administered dose were recovered after 3 and 24 hours respectively.
Plasma concentrations are increased in patients with renal insufficiency.

Short-term use for haemorrhage or risk of haemorrhage in increased fibrinolysis or fibrinogenolysis. Local fibrinolysis as occurs in the following conditions: Prostatectomy and bladder surgery; Menorrhagia; Epistaxis; Conisation of the cervix; Traumatic hyphaema; Hereditary angioneurotic oedema; Management of dental extraction in haemophiliacs.

Local fibrinolysis: The recommended standard dosage is 15-25 mg/kg bodyweight (i.e. 2-3 tablets) two to three times daily. For the indications listed as follows the following doses may be used.
Prostatectomy: Prophylaxis and treatment of haemorrhage in high risk patients should commence pre- or post-operatively; thereafter 2 tablets three to four times daily until macroscopic haematuria is no longer present.
Menorrhagia: Recommended dosage is 2 tablets 3 times daily as long as needed for up to 4 days. If very heavy menstrual bleeding, dosage may be increased. A total dose of 4 g daily (8 tablets) should not be exceeded. Treatment with Tranexamic Acid (Transtat) Film-coated tablets should not be initiated until menstrual bleeding has started.
Epistaxis: Where recurrent bleeding is anticipated oral therapy (2 tablets three times daily) should be administered for 7 days.
Conisation of the cervix: 3 tablets three times daily.
Traumatic hyphaema: 2-3 tablets three times daily. The dose is based on 25 mg/kg three times a day.
Hereditary angioneurotic oedema: Some patients are aware of the onset of the illness; suitable treatment for these patients is intermittently 2-3 tablets two to three times daily for some days. Other patients are treated continuously at this dosage.
Haemophilia: In the management of dental extractions 2-3 tablets every eight hours. The dose is based on 25 mg/kg.
Renal insufficiency: By extrapolation from clearance data relating to the intravenous dosage form, the following reduction in the oral dosage is recommended for patients with mild to moderate renal insufficiency. (See table.)

Click on icon to see table/diagram/image

Children's dosage: This should be calculated according to body weight at 25 mg/kg per dose. However, data on efficacy, posology and safety for these indications are limited.
Elderly patients: No reduction in dosage is necessary unless there is evidence of renal failure.
Method of administration: Oral.

Signs and symptoms may include nausea, vomiting, orthostatic symptoms and/or hypotension, dizziness, headache and convulsions. Initiate vomiting, then stomach lavage, and charcoal therapy. Maintain a high fluid intake to promote renal excretion. There is a risk of thrombosis in predisposed individuals. Anticoagulant treatment should be considered.

Hypersensitivity to tranexamic acid or to any of the excipients.
Severe renal impairment because of risk of accumulation.
Active thromboembolic disease.
History of venous or arterial thrombosis.
Fibrinolytic conditions following consumption coagulopathy.
History of convulsions.

In case of haematuria of renal origin (especially in haemophilia), there is a risk of mechanical anuria due to formation of a ureteral clot.
In the long-term treatment of patients with hereditary angioneurotic oedema, regular eye examinations (e.g. visual acuity, slit lamp, intraocular pressure, and visual fields) and liver function tests should be performed.
Patients with irregular menstrual bleeding should not use Tranexamic Acid (Transtat) Film-coated tablets until the cause of irregular bleeding has been established. If menstrual bleeding is not adequately reduced by Tranexamic Acid (Transtat) Film-coated tablets, an alternative treatment should be considered.
Tranexamic acid should be administered with care in patients receiving oral contraceptives because of the increased risk of thrombosis.
Patients with a previous thromboembolic event and a family history of thromboembolic disease (patients with thrombophilia) should use Tranexamic Acid (Transtat) Film-coated tablets only if there is a strong medical indication and under strict medical supervision.
The blood levels are increased in patients with renal insufficiency. Therefore a dose reduction is recommended.
The use of tranexamic acid in cases of increased fibrinolysis due to disseminated intravascular coagulation is not recommended.
Patients who experience visual disturbance should be withdrawn from treatment.
Clinical experience with tranexamic acid in menorrhagic children under 15 years of age is not available.
Cases of convulsions have been reported in association with tranexamic acid treatment. In cardiac surgery, most of these cases were reported following intravenous (i.v.) injection of tranexamic acid in high doses.
This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially 'sodium-free'.
Effects on ability to drive and use machines: Tranexamic Acid (Transtat) Film-coated tablets has no or negligible influence on the ability to drive and use machines.

Pregnancy: Although there is no evidence from animal studies of a teratogenic effect, the usual caution with use of drugs in pregnancy should be observed.
Tranexamic acid crosses the placenta.
Lactation: Tranexamic acid passes into breast milk to a concentration of approximately one hundredth of the concentration in the maternal blood. An antifibrinolytic effect in the infant is unlikely.

Adverse events are listed as follows by system organ class and frequency. Frequencies are defined as: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100), rare (≥1/10,000 and <1/1000) and very rare (<1/10,000) including isolated reports, not known (cannot be estimated from the available data).
Immune system disorders: Very rare: Hypersensitivity reactions including anaphylaxis.
Eye disorders: Rare: Colour vision disturbances, retinal/artery occlusion.
Vascular disorders: Rare: Thromboembolic events. Very rare: Arterial or venous thrombosis at any sites.
Gastro-intestinal disorders: Very rare: Digestive effects such as nausea, vomiting and diarrhoea, may occur but disappear when the dosage is reduced.
Skin and subcutaneous tissue disorders: Rare: Allergic skin reactions.
Nervous system disorders: Frequency not known: Convulsions particularly in cases of misuse (refer to Contraindications and Precautions).
Please seek medical attention immediately at the first sign of any adverse drug reaction shall appear.

Tranexamic Acid (Transtat) Film-coated tablets will counteract the thrombolytic effect of fibrinolytic preparations.

Store at temperatures not exceeding 30°C.

Haemostatics

B02AA02 - tranexamic acid ; Belongs to the class of amino acid antifibrinolytics. Used in the treatment of hemorrhage.

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