Description
Tranexamic Acid Pharmacodynamics
Antifibrinolytic agent is a competitive (at high concentrations – non-competitive) inhibitor of plasminogen activation and its conversion into plasmin. It has local and systemic hemostatic action in bleeding associated with increased fibrinolysis. Tranexamic acid also has analgesic, anti-allergic and anti-inflammatory effects due to inhibition of kinins and other active peptides involved in allergic and inflammatory reactions. Tranexamic acid at a concentration of 1 mg/ml does not aggregate platelets in vitro, and at concentrations up to 10 mg/ml does not affect platelet counts, clotting time or various clotting factors in whole blood, or nitrate blood in a healthy person. On the other hand, tranexamic acid at both 1 mg/ml and 20 mg/ml blood concentrations prolongs thrombin time.
Indications
Prevention and treatment of bleeding due to generalized or localized fibrinolysis in adults and children 1 year and older, including:
– menorrhagia and metrorrhagia;
– Gastrointestinal bleeding;
– bleeding after surgical interventions on the prostate and bladder:
– bleeding during surgical interventions in the nose, mouth and pharynx (adenoidectomy, tonsillectomy, tooth extraction),
– Bleeding during thoracic, abdominal and other major surgical interventions (including cardiac surgery);
– Obstetric and gynecologic bleeding (including bleeding during gynecologic surgical interventions);
– bleeding caused by the use of fibrinolytic drugs. Contraindications
Contraindications
– Hypersensitivity to tranexamic acid or other components of the drug;
– Severe chronic renal insufficiency (glomerular filtration rate [GFR| less than 30 mg/ml/1.73 m2) due to the risk of cumulation;
– venous or arterial thrombosis, current or anamnesis (deep vein thrombosis of the lower extremities, pulmonary embolism, intracranial thrombosis, etc.) with the possibility of concurrent therapy with anticoagulants;
– fibrinolysis due to consumption coagulopathy (hypocoagulable stage of disseminated intravascular coagulation syndrome [DIC]);
– history of seizures;
– acquired color vision disorder;
– subarachnoid hemorrhage (due to the risk of cerebral edema, ischemia, and cerebral infarction);
– treatment of menorrhagia in patients under the age of 16 years (no experience of use);
-children under 1 year of age (no experience).
Dosage and administration method
- Intravenously by drip or stream slowly; infusion rate 1 ml/min.
- Rapid intravenous administration should be avoided!
- Adult patients
- Treatment of menorrhagia and metrorrhagia. gastrointestinal bleeding: 500 mg 2-3 times a day from the time of bleeding until it stops;
- Treatment of bleeding after surgical interventions on the prostate and urinary tract: 1000 mg 3 times a day until the bleeding stops;
- Prophylaxis and treatment of bleeding during operative interventions in the cavity of the nose, mouth and pharynx: 10-15 mg/kg of body weight every 6-8 hours until bleeding stops; Prophylaxis and treatment of bleeding during thoracic, abdominal and other major operative interventions: 15 mg/kg of body weight every 6-8 hours until bleeding stops;
- Prevention and treatment of bleeding during cardiac surgery: a loading dose of 15 mg/kg after induction of anesthesia prior to surgery, followed by intravenous infusion at a rate of 4.5 mg/kg/hour during the entire operation; tranexamic acid at a dose of 0.6 mg/kg in a heart-lung machine is recommended;
- Treatment of obstetric and gynecologic bleeding (including bleeding during gynecologic surgical procedures): 15 mg/kg body weight every 6-8 hours from the time of bleeding until it stops;
- Treatment of bleeding caused by the use of fibrinolytic drugs: 10 mg/kg of body weight every 6-8 hours from the development of bleeding until the bleeding stops.
- In case of necessity of prolonged (more than 48 hours) hemostatic therapy it is recommended to use tranexamic acid preparations in tablet dosage form.
- Children over 1 year of age.
- The experience of using tranexamic acid preparations in children is limited.
- Recommended dose for treatment of bleeding caused by local and generalized fibrinolysis is 20 mg/kg/day.
- Administration in special groups of patients Patients with impaired renal function
- In patients with mild to moderate renal excretory dysfunction it is necessary to correct the dose and the administration frequency of tranexamic acid (See Table 1). Table 1. Correction of dosing regimen
- Serum creatinine concentration Glomerular filtration rate (GFR) Tranexamic acid dosage
- 120 – 249 μmol/l (1.36-2.82 mg/dL) 60 – 89 ml/min/1.73 m2 15 mg/kg body weight 2 times daily
- 250 to 500 μmol/l (2.83 to 5.66 mg/dL) 30 to 59 mL/min/1.73 m2 15 mg/kg of body weight once daily
- Impaired liver function
- No dose adjustment is required in patients with hepatic impairment.
- Elderly patients
- No dose adjustment is required in elderly patients in the absence of renal impairment.
