Anaxyl 500

Generic

Tranexamic Acid

 

Indications

Anaxyl® capsule and injection are indicated in –

1.  Haemorrhage associated with excessive fibrinolysis. Local fibrinolysis may occur in the
   conditions e.g. prostatectomy and bladder surgery, menorrhagia, epistaxis, conisation of
   cervix, management of dental extraction in patients with coagulopathies, ulcerative colitis,
   haematuria and gastrointestinal haemorrhage.
2. General fibrinolysis as in prostatic and pancreatic cancer; after thoracic and other major
   surgery; in obstetrical complications such as abruptio placentae and post-partum
   haemorrhage; in leukaemia and liver diseases and in connection with thrombolytic therapy
   with streptokinase.
3. In prophylaxis of hereditary angioneurotic oedema.

 

Pharmacology

PHARMACOLOGICAL ACTIONS: Tranexamic acid has a strong inhibitory effect on the activation of plasminogen, i.e. the conversion of plasminogen to plasmin, in the fibrinolytic system.The half life is 1-2 hours. Plasma protein binding is 3% at therapeutic plasma levels. The plasma protein binding seems fully accounted by its binding to plasminogen. Tranexamic acid is excreted unchanged in the urine.

PHARMACOKINETICS: Tranexamic acid is rapidly absorbed from the gastrointestinal tract. Maximum serum levels are reached within 2-3 hours. After oral administration, about 40% of the dose is excreted in the urine during the first 24 hours. After intravenous administration 45% of the dose is excreted in the urine during the first day.

 

Dosage & Administration

Adults-

• The usual dose: 500-1000 mg 3 times daily.
• For prophylaxis: The mean recommended daily doses are 0.5-1 gm orally, 500 mg by the parenteral (intravenous or intramuscular) route.
• For therapy of hemorrhagic manifestations: the oral dose increases to 1-3 gm given in divided doses: in cases of particular seriousness and urgency, begin by injecting an ampoule (500 mg) slowly by intravenous route and administer the necessary subsequent oral doses.

Children-

• For prophylaxis: For every kg of body weight from 5-10 mg are orally administered daily in divided doses.
• For therapeutic purposes: The oral doses are doubled (from 10 to 20 mg/kg), while the intravenous and intramuscular treatment is begun with 10 mg/kg (=0.5 ml every 5 kg) by the slow intravenous route, continuing the oral administration up to the required dose. Where it is more convenient (e.g. in small babies) the ampoules, diluted in a little sweetened water, maybe orally administered instead of the Capsules.

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

 

Interaction

Clinically important interactions have not been observed with Tranexamic Acid. Because of the absence of interaction studies, simultaneous treatment with anticoagulants must take place under the strict supervision of a physician experienced in this field.

 

Contraindications

Active thromboembolic disease, such as deep vein thrombosis, pulmonary embolism and cerebral thrombosis Subarachnoid haemorrhage Hypersensitivity to Tranexamic acid or any of the ingredients.

 

Side Effects

Dose-dependent, gastrointestinal discomfort is the most commonly reported undesirable effect, but it is usually of mild and temporary in nature. Allergic skin reactions have been reported as an uncommon undesirable effect. Hypotension may occur after fast injection.

 

Pregnancy & Lactation

Pregnancy: Tranexamic acid crosses the placenta. Clinical experience of use in pregnant women is limited. Animal studies have not supplied any evidence of an increased incidence of fetal damage.

Lactation: Tranexamic acid is excreted into breast milk, but it is not likely to influence the child at therapeutic doses.

 

Precautions & Warnings

Tranexamic Acid should be used with caution in patients with renal impairment. The dose should be reduced beacause of high risk of accumulation. Caution should also be exercised in case of massive haematuria (avoid if risk of ureteric obstruction), disseminated intravascular coagulation (patient must be under the supervision of a physician experienced in treating this disorder), irregular menstrual bleeding (cause should be established before initiating therapy). Drugs with actions on haemostasis should be given with caution to patients on antifibrinolytic therapy.

 

Therapeutic Class

Anti-fibrinolytic drugs, Haemostatic drugs

 

Storage Conditions

Store at a cool and dry place, protected from light and moisture.

 

Pharmaceutical Name

ACI Limited