Active substanceEtamsylateEtamsylate
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  • Dosage form: & nbspsolution for injection and external application
    Composition:1 ml of the preparation contains:

    active substance: Ethazylate 125.0 mg;

    Excipients: sodium disulfite 2.5 mg, sodium sulfite 1.0 mg, disodium edetate 0.5 mg, water for injection up to 1.0 ml.

    Description:Transparent colorless or slightly yellowish liquid.
    Pharmacotherapeutic group:hemostatic agent
    ATX: & nbsp

    B.02.B.X.01   Etamsylate

    Pharmacodynamics:

    Hemostatic agent; has also an angioprotective and proaggregant effect. Stimulates the formation of platelets and their exit from the bone marrow. Hemostatic action due to activation of thromboplastin formation at the site of small vessel damage and decreased formation of prostacyclin vessels in the endothelium (PgI2), promotes an increase in adhesion and aggregation of platelets, which ultimately leads to stopping or reducing bleeding. Increases the rate of formation of the primary thrombus and enhances its retraction, practically does not affect the concentration of fibrinogen and prothrombin time. Doses of more than 2-10 mg / kg do not lead to greater severity of the effect. With repeated injections, thrombus formation is intensified.

    Possessing anti-hyaluronidase activity and stabilizing ascorbic acid, it prevents destruction and promotes the formation in the capillary wall of mucopolysaccharides with a large molecular weight, increases the resistance of capillaries, reduces their fragility; normalizes permeability in pathological processes.

    Reduces the yield of fluid and diapedesis of blood elements from the vascular bed, improves microcirculation.

    Does not have hypercoagulable properties. Does not have vasoconstrictive action.

    Recovers pathologically altered bleeding time. The hemostasis does not influence the normal parameters of the system.

    Hemostatic effect with intravenous (iv) introduction of etamzilate occurs in 5-15 minutes, the maximum effect is manifested in 1-2 hours. The effect lasts for 4-6 hours, then within 24 hours gradually weakens; with intramuscular (in / m) introduction, the effect comes somewhat slower.

    After the course treatment, the effect persists for 5-8 days, gradually weakening.
    Pharmacokinetics:

    It is well absorbed with the / m introduction. The therapeutic concentration in the blood is 0.05-0.02 mg / ml. It is evenly distributed in various organs and tissues (depends on the degree of their blood supply). It weakly binds to plasma proteins and formed elements of blood. Quickly excreted from the body, mainly by the kidneys (unchanged), and also with bile. Half-life (T1/2) after the / m introduction - 2.1 hours, after the / in - 1.9 hours.After 5 minutes after intravenous administration of the kidneys, 20-30% of the injected drug is released, completely eliminated after 4 hours.

    Indications:

    Prophylaxis and stopping of bleeding: parenchymal and capillary bleeding (including traumatic, in surgery with operations on highly vascularized organs and tissues, surgical interventions in dental, urological, ophthalmic, otorhinolaryngological practice, intestinal, renal, pulmonary hemorrhage, metro- and menorrhagia in fibromyoma, etc.), secondary bleeding against thrombocytopenia and thrombocytopathy, hypocoagulation, hematuria, intracranial hemorrhage (including neonates and neonates (hemorrhagic diabetic retinopathy, hemorrhagic diabetic retinopathy, retinal hemorrhage, haemophthalmia), hemorrhagic diathesis (including the disease of Verlhof, Villebrand-Jurgens, thrombocytopathy), diabetic microangiopathy (hemorrhagic diabetic retinopathy, repeated haemorrhage to the retina, hemophthalmus).

    Contraindications:

    Hypersensitivity, thrombosis, thromboembolism, acute porphyria, pregnancy, lactation.

    Carefully:

    When bleeding against the background of an overdose of anticoagulants. Caution is necessary (despite the absence of induction of thrombosis) in the administration of etamzilate to patients with thrombosis or thromboembolism in history.

    Dosing and Administration:

    Intravenous and intramuscular. In ophthalmic practice - retrobulbarno. Solution for injection can be used externally - a sterile swab impregnated with the drug, superimposed on the wound.

    Adults: at operative interventions prophylactically ethamylate administered intravenously or intramuscularly for 1 hour before surgery - 0.25-0.5 g as needed - 0.25-0.5 g intravenously during surgery and prophylactically - 0.5-0.75 g intravenously or intramuscularly evenly 3 -4 times during the day - after the operation.

    For children: if necessary during the operation - intravenously 8-10 mg / kg.

    Diabetic microangiopathy (Haemorrhagic diabetic retinopathy, retinal hemorrhage repeated, hemophthalmus) - 0.25-0.35 g intramuscularly 3 times per day or 0.125 g of 2 times a day for 2-3 months.

    Side effects:

    Headache, dizziness, hyperemia of the facial skin, a decrease in systolic blood pressure, paresthesia of the lower extremities, allergic reactions.

    Overdose:

    It is possible to intensify the manifestations of the described adverse reactions (headache, dizziness, facial skin hyperemia, decreased systolic blood pressure, paresthesia of the lower extremities).

    Interaction:

    Pharmaceutically incompatible (in one syringe) with other drugs.

    Introduction at a dose of 10 mg / kg for 1 hour before dextrans (average molecular weight 30-40 kDa) prevents their antiaggregant effect; the administration after does not have a haemostatic effect.

    It is acceptable to combine with aminocaproic acid and menadione sodium bisulfite.

    Special instructions:

    When hemorrhagic complications associated with an overdose of anticoagulants, it is recommended to use specific antidotes.

    The use of etamzilate in patients with impaired blood coagulation indexes is possible, but it must be supplemented by the introduction of drugs that eliminate the revealed deficiency or defect factors of the coagulation system.

    Form release / dosage:

    Solution for injection and external application, 125 mg / ml.

    Packaging:

    2 ml each into neutral glass ampoules of grade НС-1 or НС-3.

    For 10 ampoules, together with instructions for medical use and a scapegrator, the ampoule is placed in a cardboard box withsepta from cardboard, or 5 or 10 ampoules are placed in a contour mesh box made of a polyvinyl chloride film.

    When using ampoules with a notch or a fracture ring, the scarifier is not inserted.

    For 1 or 2 contour cell pack of polyvinylchloride film together with instructions for medical use put in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008602/09
    Date of registration:LSR-008602/09
    Date of cancellation:2009-10-28
    The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia
    Manufacturer: & nbsp
    Representation: & nbspESKOM NPK, OAOESKOM NPK, OAO
    Information update date: & nbsp05.10.2015
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