Tranexamic acid
Tranexamic acid: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Tranexamic acid
ATX code: B02AA02
Active ingredient: tranexamic acid (tranexamic acid)
Producer: Armavir biofactory, FKP (Russia)
Description and photo update: 2018-27-11
Prices in pharmacies: from 554 rubles.
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Tranexamic acid is a drug with antifibrinolytic action used for bleeding.
Release form and composition
Dosage form - solution for intravenous (intravenous) administration: transparent or almost transparent, from colorless to greenish-yellow (5 ml in glass ampoules; in a cardboard box 1, 2, 10, 20, 50 or 100 plastic trays or contoured cell packs containing 5 ampoules, and instructions for the use of Tranexamic acid).
Composition of 1 ml solution:
- active substance: tranexamic acid - 50 mg;
- auxiliary component: water for injection - up to 1 ml.
Pharmacological properties
Pharmacodynamics
Tranexamic acid is an antifibrinolytic agent, a competitive inhibitor of plasminogen activation and its subsequent transformation into plasmin protease (when used in high concentrations, it is uncompetitive).
It has a local and systemic hemostatic effect in bleeding, which is associated with an increase in fibrinolysis (with platelet pathologies, menorrhagia). Also, the substance has an anti-allergic and anti-inflammatory effect, which is ensured by the suppression of the formation of kinins and other active peptides that are involved in inflammatory and allergic reactions.
During experimental studies, it was confirmed that tranexamic acid has its own analgesic activity, in addition, its potentiating effect in relation to the analgesic activity of opioid analgesics is noted.
At a concentration of 1 mg / ml of blood, tranexamic acid does not aggregate platelets; at a concentration of up to 10 mg / ml of blood, it does not affect the number of platelets, blood clotting time or various clotting factors in whole / citrated blood in healthy patients. On the other hand, a substance at a concentration of both 1 mg / ml and 10 mg / ml of blood lengthens the thrombin time.
Pharmacokinetics
The substance in the tissues is distributed relatively evenly (except for the cerebrospinal fluid, in which the concentration is 10% of the plasma).
Tranexamic acid:
- penetrates the placental barrier; after administration of the drug to a pregnant woman at a dose of 10 mg / kg, its concentration in the umbilical cord blood can be quite high, about 0.03 mg / ml of fetal serum;
- passes through the blood-brain barrier;
- excreted in breast milk during lactation (reaches approximately 1% of the plasma concentration in the mother's blood);
- it is found in semen, while there is a decrease in fibrinolytic activity, however, the drug does not affect the migratory mobility of sperm;
- diffuses through the synovial membranes and into the articular fluid quickly (the concentration in the articular fluid corresponds to serum); biological T 1/2 (half-life) from the articular fluid is approximately 3 hours.
Initial V d (volume of distribution) - 9-12 liters.
Binds to plasma proteins (profibrinolysin) up to 3%.
In the blood, approximately 3% is associated with protein (plasminogen).
Antifibrinolytic concentration of tranexamic acid in different tissues is maintained for 17 hours, in plasma - up to 7-8 hours.
The substance is metabolized slightly. AUC (area under the concentration-time curve) has a three-phase form, T 1/2 in the terminal phase is 2 hours. The total renal clearance corresponds to plasma (7 l / h).
Excretion is carried out by the kidneys (the main route is glomerular filtration), more than 95% - for 12 hours unchanged. After intravenous administration of 10 mg / kg tranexamic acid, about 90% of the substance is excreted within 24 hours (by glomerular filtration). Two metabolites have been identified: deaminated and N-acetylated derivatives.
In patients with impaired renal function, there is a risk of drug accumulation.
Indications for use
- bleeding caused by generalized / local fibrinolysis, including metrorrhagia and menorrhagia, bleeding after surgery on the bladder and prostate gland, gastrointestinal bleeding (treatment);
- bleeding associated with surgical interventions in the nasal cavity, pharynx and mouth (tonsillectomy, adenoidectomy, tooth extraction), abdominal, thoracic and other major surgical interventions (including during cardiac surgery), gynecological surgery (treatment and prevention);
- obstetric and gynecological bleeding (treatment);
- bleeding caused by the use of fibrinolytic drugs (treatment).
Contraindications
Absolute:
- severe chronic renal failure (in patients with a glomerular filtration rate <30 mg / ml / 1.73 m 2), which is associated with the risk of accumulation of the substance;
- arterial / venous thrombosis, including a burdened history (in patients with deep vein thrombosis of the legs, pulmonary embolism, thrombosis of the intracranial vessels, etc.) in cases where it is impossible to combine use with anticoagulants;
- fibrinolysis associated with consumption coagulopathy (in patients with hypocoagulable stage of disseminated intravascular coagulation syndrome);
- violation of color vision (acquired);
- burdened history of seizures;
- subarachnoid hemorrhage, which is associated with the risk of developing cerebral edema, heart attack and cerebral ischemia;
- age up to 16 years - in the treatment of menorrhagia, up to 1 year - in all other cases;
- individual intolerance to the components of the drug.
Relative (Tranexamic acid is prescribed under medical supervision):
- the presence of a high risk of thrombosis (in patients with a history of thromboembolic events, with a burdened family history of thromboembolic diseases, a verified diagnosis of thrombophilia);
- hematuria associated with diseases of the renal parenchyma, bleeding from the upper urinary tract, which is associated with the risk of secondary mechanical obstruction of the urinary tract by a blood clot with the subsequent development of anuria;
- combined use with oral contraceptives, which is associated with a high risk of arterial thrombosis and venous thromboembolic complications;
- combined use with drugs of blood coagulation factors II, VII, IX and X in combination (prothrombin complex) or anti-inhibitory coagulant complex;
- combined use with anticoagulants;
- pregnancy and lactation.
Tranexamic acid, instructions for use: method and dosage
Tranexamic acid is injected intravenously by drop or jet slowly at a rate of 50 mg / min. Rapid administration of the drug should be avoided.
Dosage regimen in adult patients (the drug is administered from the moment bleeding occurs until it stops):
- bleeding after surgery on the bladder and prostate: 1000 mg 3 times a day;
- menorrhagia and metrorrhagia, gastrointestinal bleeding, bleeding associated with local fibrinolysis: 500 mg 2-3 times a day;
- bleeding associated with the use of fibrinolytic drugs: 10 mg / kg every 6-8 hours;
- bleeding associated with generalized fibrinolysis, obstetric-gynecological bleeding: 15 mg / kg every 6-8 hours.
Treatment and prevention of bleeding associated with surgery in adults (Tranexamic acid is used until bleeding stops every 6-8 hours):
- operations in the nasal cavity, pharynx and mouth, gynecological surgical interventions: 10-15 mg / kg;
- thoracic, abdominal and other major surgical interventions: 15 mg / kg.
When carrying out cardiac surgeries before the start of surgery, after induction of anesthesia, a loading dose of 15 mg / kg is administered, then during the entire operation - intravenous infusion at a rate of 4.5 mg / kg / h; it is recommended to inject 0.6 mg / kg of tranexamic acid into the heart-lung machine.
If necessary, prolonged hemostatic therapy (longer than 48 hours), the use of drugs in the form of tablets is indicated.
In children from 1 year of age, the experience of using Tranexamic acid is limited. The recommended daily dose for the treatment of bleeding associated with local / generalized fibrinolysis is 20 mg / kg.
Patients with mild to moderate impairment of renal excretory function require dose adjustment and frequency of drug administration. At a serum creatinine concentration of 120–249 µmol / L and a glomerular filtration rate of 60–89 ml / min / 1.73m 2, Tranexamic acid is administered at a dose of 15 mg / kg 2 times a day. At a serum creatinine concentration of 250-500 μmol / l and a glomerular filtration rate of 30-59 ml / min / 1.73m 2, the drug is administered in the same dose once a day.
Side effects
Possible adverse reactions [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare]:
- digestive system: often - vomiting, nausea, diarrhea (when the dose is reduced, the symptoms disappear);
- nervous system: rarely - convulsions, dizziness;
- immune system: very rarely - hypersensitivity reactions, including anaphylactic shock;
- skin: rarely - allergic skin reactions, including allergic dermatitis;
- vessels: rarely - a pronounced decrease in blood pressure (as a rule, this is associated with excessively rapid administration), thromboembolic complications; very rarely - venous / arterial thrombosis of various localization; with an unknown frequency - stroke, acute myocardial infarction, thrombosis of the cerebral and carotid arteries, deep vein thrombosis of the legs, pulmonary embolism, renal artery thrombosis with the development of cortical necrosis and acute renal failure, thrombosis of the central artery and retinal vein, coronary occlusion of aorta;
- organ of vision: rarely - visual impairments, including retinal vascular thrombosis, color perception disorders.
Overdose
Overdose cases of injectable tranexamic acid have not been described. There is limited information on overdose of pill formulations.
The main symptoms: orthostatic collapse (including dizziness when moving from horizontal to vertical), headache, dizziness, nausea, diarrhea, vomiting, orthostatic arterial hypotension. If there is a predisposition, the risk of thrombosis increases.
Therapy: hospitalization is indicated. Oral administration or parenteral administration of large amounts of fluid is recommended to enhance renal excretion. Monitoring of the amount of urine excreted, forced diuresis. In some cases, anticoagulant therapy is warranted. The antidote is unknown.
special instructions
Before using Tranexamic acid and during treatment, an ophthalmologist's consultation is required in order to determine visual acuity, color vision, fundus condition. In case of visual impairment, the drug is canceled.
Patients with hematuria caused by diseases of the renal parenchyma, Tranexamic acid is prescribed with caution. Under these conditions, intravascular fibrin deposition is often noted, which can lead to worsening of kidney damage. Antifibrinolytic therapy for massive bleeding from the upper urinary tract of any etiology increases the likelihood of blood clots in the ureter / renal pelvis and, consequently, the risk of developing anuria and secondary mechanical obstruction of the urinary tract.
The risk of thrombotic complications cannot be completely excluded, despite the lack of confirmation of a significant increase in the incidence of thrombosis in the course of clinical trials. Before using Tranexamic acid, an examination should be carried out to identify risk factors for thromboembolic complications.
The presence of blood in cavities, such as in the pleural cavity, urinary tract, and joint cavities, can cause an insoluble clot to form in them. It is associated with extravascular blood coagulation. Such a clot can be resistant to physiological fibrinolysis. Until the cause of dysmenorrhea is established, women with irregular menstrual bleeding should not be prescribed tranexamic acid. If there is an inadequate decrease in menstrual bleeding during therapy, alternative treatment should be considered.
Influence on the ability to drive vehicles and complex mechanisms
Tranexamic acid can cause visual impairment and dizziness, which should be taken into account in patients who plan to drive vehicles.
Application during pregnancy and lactation
Tranexamic acid is used with caution during pregnancy / lactation.
During preclinical studies, tranexamic acid did not have a teratogenic effect on animals. The safety profile in pregnant women has not been studied. The substance crosses the placenta and can be contained in the umbilical cord blood in concentrations close to that of the mother.
The development of an antifibrinolytic effect in an infant in cases where tranexamic acid is used by the mother during lactation is unlikely.
Pediatric use
It is contraindicated to use Tranexamic acid in the treatment of menorrhagia in patients under the age of 16 years. For all other indications, the drug is not used in children under 1 year of age.
With impaired renal function
Patients with severe chronic renal failure (with a glomerular filtration rate <30 mg / ml / 1.73 m 2) are contraindicated in Tranexamic acid.
Drug interactions
The use of tranexamic acid prevents the development of the pharmacological effect of thrombolytic (fibrinolytic) agents.
Combined oral contraceptives increase the likelihood of arterial thrombosis and venous thromboembolic complications (including ischemic stroke and myocardial infarction). Women who take combined oral contraceptives have no experience with tranexamic acid. Due to the antifibrinolytic effect of tranexamic acid, combined use with combined oral contraceptives may further increase the risk of thrombotic complications.
With the simultaneous use of blood coagulation factors II, VII, IX and X with drugs in combination or with an anti-inhibitory coagulant complex, the likelihood of thrombosis increases.
An increased risk of thrombotic complications (in particular, myocardial infarction) is possible when combined with desmopressin, hydrochlorothiazide, ampicillin-sulbactam, nitroglycerin and ranitidine.
When combined therapy with hemostatic agents, activation of thrombus formation is possible.
Tranexamic acid solution is compatible with unfractionated heparin, as well as with most infusion solutions, including 0.9% sodium chloride solution, Ringer's solution, 5% dextrose solution, dextrans, amino acid solutions.
Pharmaceutical incompatibility is noted with norepinephrine, urokinase, diazepam, dipyridamole.
It is impossible to mix tranexamic acid with antibiotic solutions (penicillins, tetracyclines) and blood products.
Analogs
Analogs of Tranexamic acid are: Stagemin, Traxara, Tranexam, Exacil, Troxaminat, Sanksamik, Trameston, Cyclohemal, Transamcha, Cyclocapron, etc.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tranexamic acid
Reviews of Tranexamic acid are few, since in most cases the drug is used in a hospital setting.
Price for Tranexamic acid in pharmacies
The price recommended in the state register for Tranexamic acid, solution for intravenous administration 50 mg / ml, 5 ml in an ampoule, 10 ampoules in a cardboard pack - 1060 rubles.
Tranexamic acid: prices in online pharmacies
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Drug name Price Pharmacy |
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Tranexamic acid - Solofarm solution for intravenous injection. 50mg / ml amp. 5ml 10 pcs 554 r Buy |
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Tranexamic acid 50 mg / ml solution for intravenous administration 5 ml 10 pcs. RUB 926 Buy |
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Tranexamic acid solution for intravenous administration 50mg / ml 5ml 10pcs 1036 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
