1. Name Of The Medicinal Product
Tranexamic Acid 500mg Tablets.
2. Qualitative And Quantitative Composition
Each tablet contains 500mg Tranexamic Acid.
For excipients, see 6.1.
3. Pharmaceutical Form
Tablet.
White, capsule shaped tablet embossed with 'T500' on one side and a break line on the other side.
4. Clinical Particulars
4.1 Therapeutic Indications
Tranexamic Acid 500mg Tablets are indicated for short term use for haemorrhage or risk of haemorrhage in those with increased fibrinolysis or fibrinogenolysis. Local fibrinolysis as occurs in the following conditions:
1. | a) Prostatectomy and bladder surgery
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2. | Management of dental extraction in haemophiliacs. |
3. | Hereditary angioneurotic oedema. |
4.2 Posology And Method Of Administration
Route of administration: Oral.
Adults:
Local Fibrinolysis: The recommended standard dose is 15-25mg/kg bodyweight (i.e. 2-3 tablets) two to three times daily. For the indications listed below the following doses may be used:
1a | Prostatectomy: Prophylaxis and treatment of haemorrhage in high risk patients should commence per- or post-operatively with tranexamic acid injection; thereafter 2 tablets three to four times daily until macroscopic haematuria is no longer present. |
1b | 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 4g daily (8 tablets) should not be exceeded. Treatment with Tranexamic acid should not be initiated until menstrual bleeding has started. |
1c | Epistaxis: When repeated bleeding is anticipated oral therapy (2 tablets three times daily) should be administered for 7 days. |
1d | Cervix Conisation: 3 tablets three times daily. |
1e | Traumatic Hyphaema: 2-3 tablets 3 times daily. The dose is based on 25mg/kg three times a day. |
2. | Haemophilia: In the management of dental extractions 2-3 tablets every eight hours. The dose is based on 25mg/kg. |
3. | Hereditary angioneurotic oedema: Some patients are aware of the onset of 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. |
Children:
This should be calculated according to bodyweight at 25mg/kg per dose at the adult dosing frequencies.
Elderly:
No reduction in dosage is necessary unless there is evidence of renal failure (see guidelines below).
Renal Impairment
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:
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4.3 Contraindications
Hypersensitivity to tranexamic acid or any of the other ingredients.
Active thromboembolic disease.
Severe renal failure because of risk of accumulation.
4.4 Special Warnings And Precautions For Use
Caution is advised in treating those with massive haematuria from the upper urinary tract, especially in haemophiliacs, as there have been some cases of ureteric obstruction.
The blood levels are increased in patients with renal insufficiency. Therefore a dose reduction is recommended (see Section 4.2, Posology and Method of Administration).
In those patients requiring long term administration of tranexamic acid, such as those with hereditary angioneurotic oedema, regular eye examinations (e.g. visual acuity, slit lamp, intraocular pressure, visual fields) and liver function tests should be performed.
Patients with irregular menstrual bleeding should not use tranexamic acid until the cause of irregular bleeding has been established. If menstrual bleeding is not adequately reduced by Tranexamic Acid Tablets, an alternative treatment should be considered.
Patients with a previous thromboembolic event and a family history of thromboembolic disease (patients with thrombophilia) should use Tranexamic Acid Tablets only if there is a strong medical indication and under strict medical supervision.
The use of tranexamic acid in cases of increased fibrinolysis due to disseminated intravascular coagulation is not recommended.
Clinical experience with Tranexamic Acid Tablets in menorrhagic children under 15 years of age is not available.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Tranexamic Acid will counteract the thrombolytic effect of fibrinolytic preparations.
4.6 Pregnancy And Lactation
Pregnancy: There is no evidence from animal studies that tranexamic acid has any teratogenic effect, however, 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.
4.7 Effects On Ability To Drive And Use Machines
Tranexamic Acid has no or negligible influence on the ability to drive and use machines.
4.8 Undesirable Effects
Gastrointestinal disorders (nausea, vomiting, diarrhoea) may occur but disappear when the dosage is reduced.
Rare instances of colour vision disturbances have been reported. Patients who experience disturbance of colour vision should be withdrawn from treatment.
Rare cases of thromboembolic events have been reported.
Rare cases of allergic skin reactions have also been reported.
4.9 Overdose
No cases of overdosage have been reported. Symptoms may be nausea, vomiting, orthostatic symptoms and/or hypotension. 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.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
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.
5.2 Pharmacokinetic Properties
Following oral administration, 1.13% and 39% of the administered dose were recovered after 3 and 24 hours respectively. Tranexamic acid administered parenterally is distributed in a two-compartment model. Tranexamic acid crosses the placenta, and may reach one hundredth of the serum peak concentration in the milk of lactating women. Tranexamic acid crosses the blood brain barrier.
Following intravenous administration, the biological half-life of tranexamic acid has been determined to be 1.9 hours and 2.7 hours.
5.3 Preclinical Safety Data
No additional information.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Microcrystalline cellulose
Hydroxypropyl cellulose L-HPC LH11
Purified talc
Hydrogenated vegetable Oil
Magnesium stearate
Silica, colloidal anhydrous
Povidone
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
3 years.
6.4 Special Precautions For Storage
Do not store above 25°C. Store in the original container.
6.5 Nature And Contents Of Container
Blister strips of aluminium foil and PVC/PVdC, 12 tablets per blister.
Pack size of 60.
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
7. Marketing Authorisation Holder
Sandoz Ltd
Woolmer Way
Bordon
Hampshire
GU35 9QE
8. Marketing Authorisation Number(S)
PL 04416/0391
9. Date Of First Authorisation/Renewal Of The Authorisation
12 March 2003
10. Date Of Revision Of The Text
June 2007
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