Tranexam, 500 mg 10 pcs

Antifibrinolytic agent.

Tranexamic acid specifically inhibits profibrinolysin (plasminogen) activation and its conversion into fibrinolysin (plasmin).

It has local and systemic hemostatic action during bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia).

Also tranexamic acid has anti-allergic and anti-inflammatory effect due to suppression of kinins and other active peptides involved in allergic and inflammatory reactions.

Indications

Short-term treatment of bleeding associated with increased fibrinolysis in the following pathological conditions: Prostatectomy; surgical interventions on the bladder; Menorrhagia; Nosebleed; Conization of the cervix; Traumatic hyphema (hemorrhage in the anterior chamber of the eye); Prevention and treatment of bleeding in patients with hemophilia who undergo minor surgery (including tooth extraction); Hereditary angioedema (prevention of exacerbations of the disease). Bleeding during pregnancy.

Pharmacological effect

Antifibrinolytic agent.

Tranexamic acid specifically inhibits the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin).

It has a local and systemic hemostatic effect for bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia).

Also, tranexamic acid, by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions, has anti-allergic and anti-inflammatory effects.

Special instructions

In patients with hereditary angioedema, before starting treatment, consultation with an ophthalmologist is necessary (determining visual acuity, color vision, condition of the fundus). During treatment, regular ophthalmological examination is necessary (including assessment of visual acuity and color perception, examination of the fundus with a slit lamp, measurement of intraocular pressure, assessment of visual fields). If visual impairment occurs during treatment with tranexamic acid, the drug must be discontinued. In patients with hereditary angioedema who have been receiving tranexamic acid for a long time, regular laboratory monitoring of liver function is necessary. Tranexamic acid preparations should be used with caution in hematuria caused by diseases of the renal parenchyma, since intravascular fibrin deposition is often observed in these conditions, which can aggravate renal damage. In addition, in cases of massive bleeding of any etiology from the upper urinary tract, antifibrinolytic therapy increases the risk of blood clots in the renal pelvis and/or ureter and, accordingly, secondary mechanical obstruction of the urinary tract and the development of anuria. Although clinical studies have not revealed a significant increase in the incidence of thrombosis, the risk of thrombotic complications cannot be completely excluded. Cases of the development of venous and arterial thrombosis and thromboembolism in patients receiving tranexamic acid have been described. In addition, cases of occlusion of the central retinal artery and central retinal vein have been reported. Several patients developed intracranial thrombosis during treatment with tranexamic acid. Accordingly, in patients with a high risk of developing 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 using tranexamic acid, an examination should be performed to identify risk factors for thromboembolic complications. The presence of blood in cavities, such as the pleural cavity, joint cavities and urinary tract (including the renal pelvis and bladder) can lead to the formation of an “insoluble clot” due to extravascular coagulation, which may be resistant to physiological fibrinolysis. Patients with irregular menstrual bleeding should not be prescribed tranexamic acid until the cause of dysmenorrhea is determined. If the amount of menstrual bleeding is inadequately reduced during treatment with tranexamic acid, alternative treatment should be considered. There is insufficient data on the effectiveness and safety of the use of tranexamic acid in the treatment of menorrhagia in patients under 15 years of age, so the drug should be used with caution. Tranexamic acid should be used with caution in women concomitantly taking combined oral contraceptives due to the increased risk of thrombosis (See section “Interaction with other drugs”). In patients with DIC who require treatment with tranexamic acid, therapy should be carried out under the close supervision of a physician experienced in treating this disease. Due to the lack of adequate clinical studies, the simultaneous use of tranexamic acid with anticoagulants should be under the close supervision of a specialist experienced in the treatment of bleeding disorders. If vision impairment occurs while taking tranexamic acid, you should stop taking the drug and consult a doctor.

Active ingredient

Tranexamic acid

Active components

Tranexamic acid

Composition

Composition per tablet: Active ingredient: tranexamic acid 500.0 mg. Excipients (core): microcrystalline cellulose, hyprolose, sodium carboxymethyl starch, talc, colloidal silicon dioxide, calcium stearate. Excipients (shell): hypromellose, titanium dioxide, talc, macrogol.

Pregnancy

In preclinical studies, tranexamic acid did not have a teratogenic effect. Adequate and strictly controlled studies of the effectiveness and safety of tranexamic acid in pregnant women have not been conducted. Tranexamic acid crosses the placenta and may be present in cord blood in concentrations close to maternal levels. Because animal reproduction studies do not always predict reactions in humans, tranexamic acid should be used during pregnancy only when absolutely necessary. Tranexamic acid passes into breast milk (the concentration of the drug in milk is about 1% of the concentration in the mother’s blood plasma). The development of an antifibrinolytic effect in an infant is unlikely. However, caution should be exercised when using tranexamic acid in nursing mothers.

Contraindications

Hypersensitivity to tranexamic acid or other components of the drug; Severe chronic renal failure (glomerular filtration rate [GFR] less than 30 mg/ml/1.73 m2) due to the risk of accumulation; Venous or arterial thrombosis currently or in history (deep vein thrombosis of the legs, pulmonary embolism, thrombosis of intracranial vessels, etc.) if simultaneous anticoagulant therapy is impossible; Fibrinolysis due to consumption coagulopathy (hypocoagulable stage of disseminated intravascular coagulation syndrome [DIC]); history of seizures; Acquired color vision impairment; Subarachnoid hemorrhage (due to the risk of developing cerebral edema, ischemia and cerebral infarction); Children up to 3 years of age (solid dosage form).

Side Effects

The incidence of adverse drug reactions is determined in accordance with the WHO classification: very often (>1/10), often (>1/100, ≤1/10), infrequently (>1/1000, ≤1/100), rarely (>1/10000, ≤1/1000), very rarely (less than 1/10000), frequency unknown (cannot be determined by available data). Gastrointestinal disorders: often – nausea, vomiting, diarrhea (symptoms disappear when the dose is reduced). Disorders of the skin and subcutaneous tissues: rarely – allergic skin reactions, including allergic dermatitis. Disorders of the organ of vision: rarely – visual disturbances, including impaired color perception, thrombosis of retinal vessels. Vascular disorders: rarely – thromboembolic complications, marked decrease in blood pressure (usually due to excessively rapid intravenous administration, in exceptional cases – after oral administration); very rarely – arterial and venous thrombosis of various locations; frequency unknown – acute myocardial infarction, cerebral artery thrombosis, carotid artery thrombosis, stroke, deep vein thrombosis of the legs, pulmonary embolism, renal artery thrombosis with the development of cortical necrosis and acute renal failure, occlusion of coronary artery bypass graft, thrombosis of the central artery and retinal vein. Immune system disorders: very rarely – hypersensitivity reactions, including anaphylactic shock. Nervous system disorders: rarely – dizziness, convulsions (usually with intravenous administration).

Interaction

When combined with hemostatic drugs and hemocoagulase, activation of thrombus formation is possible.

Overdose

Data on drug overdose are not provided.

Prescribing

Hemostatic agent

Complete set of goods

Film-coated tablets 500 mg. 10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

1, 2, 3, 5 blister packs along with instructions for use are placed in a cardboard pack.

Functional features

Absorption after oral administration of doses in the range of 0.5-2 g is 30-50%. The time of onset of maximum concentration when taken orally 0.5, 1 and 2 g is 3 hours, the maximum concentration is 5, 8 and 15 mcg/ml, respectively.

Connection with plasma proteins (profibrinolysine) – less than 3%.

Distributed relatively evenly in tissues (with the exception of cerebrospinal fluid, where the concentration is 1/10 of the plasma concentration); penetrates the placental barrier into breast milk (about 1% of the concentration in maternal plasma).

It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect sperm migration. The initial volume of distribution is 9-12 l. Antifibrinolytic concentration in various tissues lasts 17 hours, in plasma – up to 7-8 hours.

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

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

Two metabolites of tranexamic acid have been identified: N-acetylated and deaminated derivatives. If renal function is impaired, there is a risk of accumulation of tranexamic acid.

Storage conditions

At a temperature not exceeding 30 °C. Keep out of the reach of children.

Shelf life

3 years. Do not use after expiration date.

Manufacturer

Obninsk HFC, Russia