1. Name Of The Medicinal Product
Tranexamic Acid 500mg Tablets
2. Qualitative And Quantitative Composition
Each tablet contains Tranexamic Acid 500 mg as the active ingredient.
For excipients, see 6.1
3. Pharmaceutical Form
Film-coated tablets
White film-coated oblong tablets, marked on one side, FW291.
4. Clinical Particulars
4.1 Therapeutic Indications
Tranexamic acid is an antifibrinolytic agent, which competitively inhibits the activation of plasminogen to plasmin.
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
4.2 Posology And Method Of Administration
Route of administration: Oral.
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 below the following doses may be used:
Ia. Prostatectomy: Prophylaxis and treatment of haemorrhage in high risk patients should coinnience per- or post-operatively with an injectable form of Tranexamic acid; thereafter 2 tablets three to four times daily until macroscopic haematuria is no longer present.
Ib. 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.
Ic. Epistaxis: Where recurrent bleeding is anticipated oral therapy (2 tablets three times daily) should be administered for 7 days.
Id. Conisation of the cervix: 3 tablets three times daily.
Ie. Traumatic hyphaema: 2-3 tablets three times daily. The dose is based on 25 mg/kg three times a day.
2. Haemophilia: In the management of dental extractions 2-3 tablets every eight hours. The dose is based on 25 mg/kg.
3. 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.
Children's dosage:
This should be calculated according to body weight at 25 mg/kg per dose.
Elderly patients:
No reduction in dosage is necessary unless there is evidence of renal failure (see guidelines below).
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.
Serum creatinine (µmol/l) Dose Tranexamic acid
120-249 15mg/kg body weight twice daily.
250-500 15 mg/kg body weight/day.
4.3 Contraindications
Tranexamic acid is contraindicated in patients with a history of thromboembolic disease.
Known hypersensitivity to tranexamic acid or any of the excipients, see 6.1.
Severe renal failure because of risk of accumulation.
4.4 Special Warnings And Precautions For Use
In massive haematuria from the upper urinary tract (especially in haemophilia) since, in a few cases, ureteric obstruction has been reported.
When disseminated intravascular coagulation is in progress.
In the long-term treatment of patients 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, 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 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 information on renal insufficiency is contained in section 4.2.
The use of tranexamic acid in cases of increased fibrinolysis due to disseminated intravascular coagulation is not recommended.
Clinical experience with tranexamic acid 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
Although there is no evidence from animal studies of a teratogenic effect, the usual caution with the 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
None
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.
There have been rare cases of retinal/artery occlusion 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
There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the Summary of Product Characteristics.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Core
Microcrystalline cellulose
Croscarmellose sodium
Talc
Magnesium stearate
Colloidal anhydrous silica
Povidone K90
Coating
Methacrylate polymers
Titanium dioxide (E171)
Talc
Magnesium stearate
Macrogol 8000
Vanillin
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
24 months.
6.4 Special Precautions For Storage
Do not store above 25°C.
Store in the original packaging.
6.5 Nature And Contents Of Container
Blister packs of PVC film with aluminium foil backing containing 60 tablets.
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
7. Marketing Authorisation Holder
Goldshield Pharmaceuticals Ltd
NLA Tower
Croydon
CRO OXT
United Kingdom
8. Marketing Authorisation Number(S)
PL 12762/0129
9. Date Of First Authorisation/Renewal Of The Authorisation
25 February 2004
10. Date Of Revision Of The Text
06/10/2010
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