Gemtranix 50 mg/ml 5 ml, 10 pcs.

Pharmacodynamics: Tranexamic acid is an antifibrinolytic agent specifically inhibiting the activation of profibrinolysin (plasminogen) and its conversion into fibrinolysin (plasmin). It has local and systemic hemostatic action in bleeding associated with increased fibrinolysis. In in vitro studies tranexamic acid in high concentrations reduced complement activity. Pharmacokinetics: Absorption Peak plasma concentration after intravenous administration (500 mg) is reached immediately and then the concentration gradually decreases. Distribution Binding to plasma proteins (plasminogen) of tranexamic acid is approximately 3%. The initial volume of distribution is approximately 9-12 liters. Tranexamic acid passes through the placenta. After an intravenous injection of 10 mg/kg in pregnant women, the concentration of tranexamic acid in serum is in the range of 10-53 µg/ml, while that in umbilical cord blood is in the range of 4-31 µg/ml. Tranexamic acid penetrates rapidly into the joint fluid and synovial membranes, with a delay into the cerebrospinal fluid. After intravenous injection of 10 mg/kg in patients undergoing knee surgery, the concentrations in synovial fluids were the same as in the corresponding serum samples. Tranexamic acid concentrations in breast milk were a hundredth of those observed in blood and a tenth of those observed in cerebrospinal and intraocular fluids. Tranexamic acid has been found in semen, where it inhibits fibrinolytic activity but does not affect sperm migration. Excretion Tranexamic acid is excreted with urine via glomerular filtration unchanged. Total renal clearance is equal to total plasma clearance (110-116 ml/min). The excretion of tranexamic acid is about 90% during the first 24 hours after intravenous administration of 10 mg/kg body weight. The elimination half-life (T1/2) is about 3 hours. Special groups Patients with renal insufficiency have increased plasma concentrations of tranexamic acid.

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 prostate and urinary tract surgery; – bleeding during surgical interventions in the nose, mouth and pharynx (adenoidectomy, tonsillectomy, tooth extraction); – bleeding during thoracic, abdominal and other extensive surgical interventions (including Obstetric and gynecologic bleeding (including bleeding during gynecologic surgical interventions); – bleeding caused by the use of fibrinolytic drugs.

Active ingredient

Tranexamic acid

Composition

Solution for intravenous administration as a clear, colorless solution. 1 ampoule tranexamic acid (in terms of dry substance) 250 mg Excipients: water d/i – up to 5 ml.

How to take, the dosage

Individual, depending on the clinical situation. A single dose for oral administration is 1-1.5 g, the frequency of use is 2-4 times/day, the duration of treatment is 3-15 days. The single dose for intravenous injection is 10-15 mg/kg. If repeated administration is necessary, the interval between each administration should be 6-8 hours. In case of impaired renal excretory function it is necessary to correct the dosage regimen: in creatinine blood serum levels of 120-250 µmol/l it is administered orally with 15 mg/kg, in vitro – 10 mg/kg 2 times/day; in creatinine serum levels of 250-500 µmol/l – orally and in vitro in the same single dose, 1 time/day; in creatinine serum levels more than 500 µmol/l – orally with 7.5 mg/kg, intravenously 5 mg/kg, multiple times per day.

Interaction

When concomitant use with hemostatic drugs and hemocoagulase activation of thrombosis is possible. The solution should not be added to blood products and solutions containing penicillin.Special clinical studies devoted to the study of interactions of tranexamic acid with other drugs have not been conducted. Tranexamic acid interferes with the pharmacological effect of fibrinolytic (thrombolytic) drugs. Combined oral contraceptives increase the risk of venous thromboembolic complications and arterial thrombosis (in particular, ischemic stroke and myocardial infarction). There is no experience in the use of tranexamic acid in women taking combined oral contraceptives. Since tranexamic acid has an antifibrinolytic effect, concomitant use with combined oral contraceptives may lead to an additional increase in the risk of thrombotic complications. Concomitant use of tranexamic acid with preparations of clotting factors II, VII, IX and X in combination [prothrombin complex] or anti-inhibitor coagulant complex increases the risk of thrombosis. There may be an increased risk of thrombotic complications (particularly myocardial infarction) when using tranexamic acid simultaneously with hydrochlorothiazide, desmopressin, ampicillin-sulbactam, ranitidine and nitroglycerin. When concomitant use with hemostatic drugs, activation of thrombosis is possible. Concomitant administration of tranexamic acid with anticoagulants should be carried out under strict medical supervision (experience of use is limited). Pharmaceutical drug interactions Tranexamic acid solution is compatible with most infusion solutions (0.9% sodium chloride solution, Ringer’s solution, 5% dextrose solution, dextrans). Tranexamic acid solution is compatible with unfractionated heparin. Tranexamic acid solution is pharmaceutically incompatible with urokinase, norepinephrine, dipyridamole, diazepam. Tranexamic acid solution should not be mixed with antibiotic solutions (penicillins, tetracyclines) and blood products.

Special Instructions

The drug should be used strictly on the basis of indications and in accordance with the specified method of administration: – the solution is administered intravenously very slowly; – tranexamic acid should not be administered intramuscularly. Before and during treatment with tranexamic acid it is necessary to consult an ophthalmologist (determination of visual acuity, color vision, fundus condition). If there are visual disturbances during treatment with tranexamic acid, the drug should be discontinued. Tranexamic acid preparations should be used with caution in hematuria caused by kidney parenchyma diseases, because in these conditions there is often intravascular deposition of fibrin, which may aggravate kidney damage. In addition, in cases of massive bleeding of any etiology from the upper urinary tract, antifibrinolytic therapy increases the risk of blood clot formation in the renal pelvis and/or ureter and, accordingly, secondary mechanical obstruction of the urinary tract and development of anuria. Although the clinical studies have not shown a significant increase in the incidence of thrombosis, but the risk of thrombotic complications can not be completely excluded. Cases of venous and arterial thrombosis and thromboembolism have been described in patients receiving tranexamic acid. In addition, cases of central retinal artery occlusion and central retinal vein occlusion have been reported. Several patients developed intracranial thrombosis during treatment with tranexamic acid. Accordingly, in patients with a high risk of thrombosis (history of thromboembolic complications, cases of thromboembolism in relatives, verified diagnosis of thrombophilia) tranexamic acid should be used only if absolutely necessary and under strict medical supervision. Before the use of tranexamic acid, an examination aimed at identifying risk factors of thromboembolic complications should be performed. The presence of blood in cavities such as the pleural cavity, joint cavities and urinary tract (including the renal pelvis and bladder) may lead to the formation of an “insoluble clot” due to extravascular clotting, which may be resistant to physiological fibrinolysis. Patients with irregular menstrual bleeding should not be prescribed tranexamic acid until the cause of dysmenorrhea is established. If menstrual bleeding volume is inadequately reduced during tranexamic acid treatment, alternative treatment should be considered. The efficacy and safety of tranexamic acid in the treatment of menorrhagia in patients under 16 years of age have not been established. Tranexamic acid should be used with caution in women simultaneously taking combined oral contraceptives due to an increased risk of thrombosis. In patients with DIC syndrome who require tranexamic acid treatment, therapy should be carried out under the close supervision of a physician experienced in the treatment of this disease. Tranexamic acid may be administered to such patients only if the patient has symptoms of predominant activation of the fibrinolytic system with acute severe bleeding. Such patients, in general, are characterized by such hematological profile data: shortening of euglobulin clot lysis time. prolongation of prothrombin time, decreased plasma concentrations of fibrinogen, factors V and VIII, plasminogen and its activators, alpha-2 macroglobulin; normal plasma concentrations of factor II (prothrombin), factors VIII and X; increased plasma concentration of fibrin degradation products; normal platelet count. It is assumed that the underlying disease does not modify individual indicators of the hematological profile. In such acute cases a single injection of tranexamic acid in a dose of 1000 mg is often enough to stop bleeding. The prescription of tranexamic acid for DIC syndrome should be made only in the presence of relevant laboratory data and after the examination of these data by a specialist. Due to the lack of adequate clinical studies, concomitant use of tranexamic acid with anticoagulants should be performed under close supervision of a specialist experienced in the treatment of blood clotting disorders. If during the use of tranexamic acid visual impairment is observed, it is necessary to stop taking the drug and consult a physician.

Contraindications

– Hypersensitivity to tranexamic acid or other components of the drug; – Severe chronic renal failure (glomerular filtration rate [GFR] less than 30 mg/mL/1.73m2) due to the risk of cumulation; – Venous or arterial thrombosis at present or in the history (deep leg vein thrombosis, pulmonary thromboembolism, intracranial thrombosis, etc.).) when simultaneous therapy with anticoagulants is impossible; – fibrinolysis due to consumption coagulopathy (hypocoagulation stage of disseminated intravascular coagulation syndrome [DIC]); – convulsions in anamnesis; – acquired color vision disorder; – subarachnoid hemorrhage (due to the risk of cerebral edema, ischemia and cerebral infarction); – treatment of menorrhagia in patients under 16 years of age (no experience of use); – age less than 1 year (no experience of use).

Side effects

Digestive system: decreased appetite, nausea, diarrhea, heartburn. CNS disorders: drowsiness, color vision disorders. Allergic reactions: including skin rash, itching.

Similarities

Tranexam, Ciclogemal