Tranexamic Acid BP 500 mg in 5 ml for Injection.

Tranexamic Acid BP 500 mg in 5 ml for Injection.

Tranexamic Acid BP 500 mg in 5 ml for Injection.

Pharmacotherapeutic group: Antihaemorrhagics, Antifibrinolytics, Amin oacids. ATC code: B02AA02

Tranexamic acid exerts an anti haemorrhagic activity by inhibiting the fibrinolytic properties of plasmin.

A complex involving tranexamic acid, plasminogen is constituted; the tranexamic acid being linked to plasminogen when transformed into plasmin.

The activity of the tranexamic acid-plasmin complex on the activity on fibrin is lower than the activity of free plasmin alone.

In vitro studies showed that high tranexamic dosages decreased the activity of complement.

Therapeutic indications

Tranexamic acid is indicated in adults and children from one year in prevention and treatment of haemorrhages due to general or local fibrinolysis.

Specific indications include:

Haemorrhage caused by general or local fibrinolysis such as:

  • Menorrhagia and metrorrhagia.
  • Gastrointestinal bleeding.

Haemorrhagic urinary disorders, further to prostate surgery or surgical procedures affecting the urinary tract,Ear Nose Throat surgery (adenoidectomy, tonsillectomy, dental extractions).

Gynaecological surgery or disorders of obstetric origin.

Thoracic and abdominal surgery and other major surgical intervention such as cardiovascular surgery.

Management of haemorrhage due to the administration of a fibrinolytic agent.

Posology and method of administration

Adults: Unless otherwise prescribed, the following doses are recommended:

  1. Standard treatment of local fibrinolysis: 0.5 g (1 ampoule of 5 mL) to 1 g (1 ampoule of 10 mL or 2 ampoules of 5 mL) tranexamic acid by slow intravenous injection or infusion (= 1 mL/minute) two to three times daily
  2. Standard treatment of general fibrinolysis: 1 g (1 ampoule of 10 mL or 2 ampoules of 5 mL) tranexamic acid by slow intravenous injection or infusion (= 1 mL/minute) every 6 to 8 hours, equivalent to 15 mg/kg body weight (BW)
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Renal impairment: In renal insufficiency leading to a risk of accumulation, the use of tranexamic acid is contraindicated in patient with severe renal impairment. For patients with mild to moderate renal impairment, the dosage of tranexamic acid should be reduced according to the serum creatinine level:

Serum creatinine micromol/Lmg/10 mLDose IVAdministration
120 to 2491.35 to 2.8210 mg/kg BWEvery 12 hours
250 to 5002.82 to 5.6510 mg/kg BWEvery 24 hours
> 500> 5.655 mg/kg BWEvery 24 hours

Hepatic impairment: No dose adjustment is required in patient with hepatic impairment.

Paediatric population: In children from 1 year, for current approved indications, the dosage is in the region of 20 mg/kg/day. However, data on efficacy, posology and safety for these indications are limited. The efficacy, posology and safety of tranexamic acid in children undergoing cardiac surgery have not been fully established.

Elderly: No reduction in dosage is necessary unless there is evidence of renal failure.

Method of administration

The administration is strictly limited to slow intravenous injection or infusion of maximum 1 mL per minute.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients.
  • Acute venous or arterial thrombosis.
  • Fibrinolytic conditions following consumption coagulopathy except in those with predominant activation of the fibrinolytic system with acute severe bleeding.
  • Severe renal impairment (risk of accumulation).
  • History of convulsions.
  • Intrathecal and intraventricular injection, intracerebral application (risk of cerebral oedema and convulsions).

Special warnings and precautions for use

The indications and method of administration indicated above should be followed strictly:

  • Intravenous injections or infusions should be given very slowly (maximum 1 mL per minute).
  • Tranexamic acid should not be administered by the intramuscular route.

Convulsions: Cases of convulsions have been reported in association with tranexamic acid treatment. In coronary artery bypass graft (CABG) surgery, most of these cases were reported following intravenous (IV.) injection of tranexamic acid in high doses. With the use of the recommended lower doses of tranexamic acid, the incidence of postoperative seizures was the same as that in untreated patients.

Visual disturbances: Attention should be paid to possible visual disturbances including visual impairment, vision blurred, impaired colour vision and if necessary the treatment should be discontinued. With continuous long-term use of tranexamic acid, regular ophthalmologic examinations (eye examinations including visual acuity, colour vision, fundus, visual field etc.) are indicated. With pathological ophthalmic changes, particularly with diseases of the retina, the physician must decide after consulting a specialist on the necessity for the long-term use of tranexamic acid in each individual case.

Haematuria: In case of haematuria from the upper urinary tract, there is a risk for urethral obstruction.

Thromboembolic events: Before use of tranexamic acid, risk factors of thromboembolic disease should be considered. In patients with a history of thromboembolic diseases or in those with increased incidence of thromboembolic events in their family history (patients with a high risk of thrombophilia), tranexamic acid should only be administered if there is a strong medical indication after consulting a physician experienced in haemostaseology and under strict medical supervision.

Tranexamic acid should be administered with care in patients receiving oral contraceptives because of the increased risk of thrombosis.

Disseminated intravascular coagulation: Patients with disseminated intravascular coagulation (DIC) should in most cases not be treated with tranexamic acid. If tranexamic acid is given it must be restricted to those in whom there is predominant activation of the fibrinolytic system with acute severe bleeding. Characteristically, the haematological profile approximates to the following: reduced euglobulin clot lysis time; prolonged prothrombin time; reduced plasma levels of fibrinogen, factors V and VIII, plasminogen fibrinolysin and alpha-2 macroglobulin; normal plasma levels of P and P complex; i.e. factors II (prothrombin), VIII and X; increased plasma levels of fibrinogen degradation products; a normal platelet count.

Interaction with other medicinal products and other forms of interaction

No interaction studies have been performed. Simultaneous treatment with anticoagulants must take place under the strict supervision of a physician experienced in this field. Medicinal products that act on haemostasis should be given with caution to patients treated with tranexamic acid. There is a theoretical risk of increased thrombus-formation potential, such as with oestrogens. Alternatively, the antifibrinolytic action of the drug may be antagonised with thrombolytic drugs.

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Fertility, pregnancy and lactation

Women of childbearing potential: Women of childbearing potential have to use effective contraception during treatment.

Pregnancy: There are no or limited amount of data from the use of tranexamic acid in pregnant women. As a result, although studies in animals do not indicate teratogenic effects, as precaution for use, tranexamic acid is not recommended during the first trimester of pregnancy.

Limited clinical data on the use of tranexamic acid in different clinical haemorrhagic settings during the second and third trimesters did not identify deleterious effect for the foetus. Tranexamic acid should be used throughout pregnancy only if the expected benefit justifies the potential risk.

Breast-feeding: Tranexamic acid is excreted in human milk. Therefore, breast-feeding is not recommended.

Fertility: There are no clinical data on the effects of tranexamic acid on fertility.

Effects on ability to drive and use machines

No studies have been performed on the ability to drive and use machines.

Overdose

No case of overdose has been reported.

Signs and symptoms may include dizziness, headache, hypotension, and convulsions. It has been shown that convulsions tend to occur at higher frequency with increasing dose.

Management of overdose should be supportive.

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