Tranexam, 500 mg 10 pcs

Interaction

When used in combination with hemostatic drugs and hemocoagulase, it is possible to activate thrombosis.

Special Instructions

In patients with hereditary angioedema, a consultation with an ophthalmologist (visual acuity, color vision, fundus condition) is necessary before treatment begins. Regular ophthalmologic examinations (including assessment of visual acuity and color perception, examination of the fundus with a slit lamp, measurement of intraocular pressure, assessment of visual fields) are necessary during treatment. If visual disturbances occur during treatment with tranexamic acid, the drug should be discontinued. In patients with hereditary angioedema receiving tranexamic acid preparations for a long time, regular laboratory monitoring of liver function is required. Tranexamic acid preparations should be used with caution in hematuria caused by kidney parenchyma diseases, because in these conditions intravascular fibrin deposition is often observed, 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 revealed 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. There are insufficient data on the effectiveness and safety of tranexamic acid in the treatment of menorrhagia in patients under 15 years of age, so the drug should be used with caution. Caution should be exercised when using tranexamic acid in women simultaneously taking combined oral contraceptives due to the increased risk of thrombosis (See section “Interaction with other medicinal products”). In patients with DICH who require treatment with tranexamic acid, therapy should be carried out under the close supervision of a physician experienced in the treatment of this disease. Due to the lack of adequate clinical studies, concomitant use of tranexamic acid with anticoagulants should be carried out under the 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.

Synopsis

Oblong biconvex white film-coated tablets. On cross section the core is white or white with a creamy or grayish tint.

Features

Oral absorption of doses in the range of 0.5-2 g is 30-50%. Time of maximum concentration on oral administration of 0.5, 1 and 2 g is 3 hours, maximum concentration is 5, 8 and 15 mcg/ml, respectively.

Binding with plasma proteins (profibrinolysin) is less than 3%.

It is fairly evenly distributed in tissues (exception is cerebrospinal fluid where the concentration is 1/10 of plasma concentration); it penetrates through placental barrier and into breast milk (about 1% of mother plasma concentration).

Detected in seminal fluid, where it reduces fibrinolytic activity, but does not affect sperm migration. The initial volume of distribution is 9-12 liters. Antifibrinolytic concentration in various tissues persists for 17 h, in plasma – up to 7-8 h.

Little is metabolized. The area curve has a three-phase shape with a half-life of 3 hours in the final phase.

Total renal clearance is equal to plasma clearance (7 l/h). It is excreted by kidneys (main route – glomerular filtration) – more than 95% unchanged during the first 12 hours.

Two metabolites of tranexamic acid were identified: N-acetylated and deaminated derivative. In case of impaired renal function there is a risk of cumulation of tranexamic acid.

Contraindications

Hypersensitivity to tranexamic acid or other drug components; 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 thrombosis, pulmonary thromboembolism, intracranial thrombosis, etc.).) when concomitant therapy with anticoagulants is impossible; Fibrinolysis due to consumption coagulopathy (hypocoagulation stage of disseminated intravascular coagulation syndrome [DIC]); Seizures in the history; Acquired color vision disorder; Subarachnoid hemorrhage (due to the risk of brain edema, ischemia and cerebral infarction); Children under 3 years old (solid dosage form).

Side effects

The incidence of adverse drug reactions is defined according to the WHO classification: very common (>1/10), common (>1/100, ≤1/10), infrequent (>1/1000, ≤1/100), rare (>1/10000, ≤1/1000), very rare (<1/10000), frequency unknown (cannot be established from available data). Gastrointestinal disorders: common - nausea, vomiting, diarrhea (symptoms disappear with dose reduction). Skin and subcutaneous tissue disorders: rare - skin allergic reactions, including allergic dermatitis. Visual disorders: rare - visual disturbances, including color perception disorders, retinal vascular thrombosis. Vascular disorders: rare - thromboembolic complications, marked decrease in blood pressure (usually due to excessively rapid intravenous administration, in exceptional cases - after oral administration); very rare - arterial and venous thrombosis of various localizations; frequency unknown - acute myocardial infarction, cerebral artery thrombosis, carotid artery thrombosis, stroke, deep vein thrombosis in legs, pulmonary embolism, renal artery thrombosis with development of cortical necrosis and acute renal failure, aortocoronary shunt occlusion, central artery and retinal vein thrombosis. Immune system disorders: very rare - hypersensitivity reactions, including anaphylactic shock. Nervous system disorders: rarely - dizziness, seizures (usually when administered intravenously).

Overdose

There are no data on overdose of the drug.

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Pregnancy use

In preclinical studies tranexamic acid had no teratogenic effects. Adequate and strictly controlled studies of efficacy and safety of tranexamic acid in pregnant women have not been conducted. Tranexamic acid penetrates the placenta and may be present in umbilical cord blood at concentrations close to maternal concentration. Because reproductive studies in animals do not always predict reactions in humans, tranexamic acid should only be used during pregnancy if absolutely necessary. Tranexamic acid penetrates into breast milk (concentration of the drug in milk is about 1% of the concentration in maternal plasma). Development of antifibrinolytic effect in the infant is unlikely. Nevertheless, caution should be exercised when using tranexamic acid in nursing mothers.

Similarities

Cyclogemal