Etamsylate - instructions for use, doses, side effects, contraindications

Hemostatic agent. It also has angioprotective and proaggregant action. Stimulates the formation of platelets and their exit from the bone marrow. Hemostatic action due to activation of thromboplastin formation at the site of damage to small vessels and a decrease in the formation in the endothelium of prostacyclin vessels PgI2, promotes an increase in adhesion and aggregation of platelets, which ultimately leads to a halt or reduction of 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 vasoconstrictive action. Recovers pathologically altered bleeding time. The hemostasis does not influence the normal parameters of the system.

Hemostatic effect with intravenous administration of (iv) solution etamzilate occurs in 5-15 minutes, the maximum effect is manifested after 1-2 hours. The action lasts for 4-6 hours, then within 24 hours weaken. With intramuscular injection (in / m), the haemostatic effect occurs in 30-60 minutes.

Pharmacokinetics:

The drug is well absorbed by intramuscular injection, weakly binds to plasma proteins and shaped elements of the blood. The therapeutic concentration in the blood is 0.05-0.02 mg / ml. Etamsylate evenly distributed in various organs and tissues (depends on the degree of their blood supply). The half-life of the drug after intravenous administration is 1.9 hours, after intramuscular injection - 2.1 hours. 5 minutes after intravenous injection, 20-30% of the injected drug is excreted by the kidneys, it is completely eliminated through 4 hours.The drug is excreted from the body mainly by the kidneys (in unchanged form), in an insignificant quantity with bile.

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 the dental, urological, ophthalmic, otorhinolaryngological practice, intestinal, renal, pulmonary hemorrhage, metro- and menorrhagia in fibroids, etc.), secondary bleeding against thrombocytopenia and thrombocytopathy, hypocoagulation, hematuria, intracranial hemorrhage (including in newborns and premature infants), nasal bleeding against a background of arterial hypertension, hemorrhage due to the use of drugs, hemorrhagic diathesis (including the disease of Verlhof, Willebrand-Jurgens, thrombocytopathy), diabetic microangiopathy (hemorrhagic iabeticheskaya retinopathy, retinal hemorrhage repeated, hemophthalmus).

Contraindications:

Hypersensitivity to etamzilate, sodium metabisulphite and / or sodium sulfite, or other components of the drug, acute porphyria,hemoblastosis in children, bronchial asthma, pregnancy and the period of breastfeeding.

Carefully:

Thrombosis, a history of thromboembolism, a tendency to arterial hypotension and unstable blood pressure, impaired renal function (no experience of clinical use), bleeding against a background of an overdose of anticoagulants.

Pregnancy and lactation:

Limited clinical data on the possible use of the drug Etamsylate in pregnant women. Etamsylate penetrates through placental barrier, its insignificant concentration is contained in the maternal and umbilical cord blood.

Application of the drug Etamsylate during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

There is no data on the release of etamzilate in breast milk. Therefore, when prescribing the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding.

Dosing and Administration:

Intravenous, intramuscular, in ophthalmology - subconjunctival and retrobulbar. Etamsylate can be administered intravenously drip in a 5% solution of glucose or in a 0.9% solution of sodium chloride.The prepared solution is administered immediately.

Adults: with the preventive purpose for surgical interventions, the drug is administered intravenously or intramuscularly 1 hour before the operation at a dose of 250-500 mg (2-4 ml of the solution), if necessary during the operation - intravenously at a dose of 250-500 mg (2-4 ml of solution) , with the danger of postoperative bleeding - intravenously or intramuscularly at a dose of 500-750 mg (4-6 ml of solution) evenly during the day after the operation.

For children: if necessary during the operation the drug is administered intravenously at the rate of 8-10 mg / kg body weight.

To stop bleeding, the drug is administered intravenously or intramuscularly 250-500 mg (2-4 ml of solution), then every 4-6 hours for 250 mg (2 ml of solution) for 5-10 days.

In the treatment of metro- and menorrhagia, the drug is prescribed in a single dose of 250 mg (2 ml solution) intravenously or intramuscularly every 6-8 hours for 5-10 days. With diabetic microangiopathy, the drug is administered intramuscularly in a single dose of 250-500 mg 3 times a day for 10-14 days.

In ophthalmology, the drug is administered subconjunctivalally or retrobulbarno in a dose of 125 mg (1 ml solution).

The solution can be applied topically (a sterile tampon is impregnated and applied to the wound).

Side effects:

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000), and very rarely (<1/10000), including individual message.

From the digestive tract

Often: nausea, heaviness in the epigastric region.

From the skin and subcutaneous tissues

Often: skin rash;

Frequency unknown: hyperemia of the facial skin.

From the nervous system

Often: headache;

Frequency unknown: dizziness, paresthesia of the lower extremities.

From the side of the cardiovascular system

Rarely: thromboembolism, marked decrease in arterial pressure.

On the part of the blood and lymphatic system

Rarely: agranulocytosis, neutropenia, thrombocytopenia.

From the side of the musculoskeletal system

Rarely: arthralgia.

From the immune system

Rarely: allergic reactions.

Other

Often: asthenia;

Rarely: fever.

Driving in the preparation of sodium metabisulphite is able in rare cases to cause severe hypersensitivity reactions and bronchospasm.If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

There is no evidence of an overdose of the drug.

Interaction:

Pharmaceutically incompatible (in one syringe) with other medications. Administration of the drug at a dose of 10 mg / kg body weight 1 hour prior to the administration of solutions of dextrans with an average molecular weight of 30,000-40,000 prevents the antiaggregative effect of the latter; the administration of etamzilate after solutions of dextrans does not exert a haemostatic effect.

Possible combination of the drug with aminocaproic acid and menadione sodium bisulfite.

Thiamin (vitamin B1) is inactivated by sodium metabisulphite, which is part of the drug.

Laboratory and experimental data

In therapeutic doses ethamylate can reduce the level of creatinine in the blood when determined by the enzymatic method. It is recommended to use Popper's classical method to determine creatinine, since ethamylate does not affect the results of determining the concentration of creatinine by this method.

Special instructions:

Before starting treatment, other causes of bleeding should be ruled out. Care must be taken in patients who have ever had thrombosis or thromboembolism. When hemorrhagic complications associated with an overdose of anticoagulants, it is recommended to use specific antidotes. The use of etamzilate in patients with disturbed parameters of the coagulation system of blood is possible, but it must be supplemented by the introduction of drugs that eliminate the revealed deficiency or defect factors of the coagulation system.

Because of the increased risk of arterial hypotension (pronounced decrease in blood pressure) with parenteral use of the drug should be careful in patients with unstable blood pressure or a tendency to arterial hypotension.

A drug Etamsylate as an antioxidant contains sodium metabisulphite, which can cause allergic reactions, nausea diarrhea in patients with increased sensitivity to it. Allergic reactions can be expressed and manifest with anaphylactic shock and / or life-threatening attacks of suffocation.Frequency of occurrence is unknown, however such pathological reaction is observed more often in patients with bronchial asthma. If such an allergic reaction occurs, the drug should be discontinued immediately. In case of skin reactions or fever, discontinue treatment and consult a doctor, as this may be a manifestation of a hypersensitivity reaction.

Clinical studies of the use of etamzilate preparations in patients with impaired liver and kidney function have not been performed, therefore caution should be exercised when using etamzilate in this category of patients. As ethamylate excreted by the kidneys, it is necessary to reduce the dose of the drug Etamsylate in patients with renal insufficiency.

Effect on the ability to drive transp. cf. and fur:

During the period of application of the drug, care should be taken when operating vehicles, mechanisms and when dealing with other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 125 mg / ml.

Packaging:

To 2 ml in glass syringes of neutral glass with Luer Lock lock, with a hard cap and accessories. 1 syringe per contour cell packaging made of polyvinyl chloride or polyethylene terephthalate film. On 1 contour acheikova packing together with a needle injecting and the instruction on application in a pack from cardboard box.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004457

Date of registration:12.09.2017

Expiration Date:12.09.2022

The owner of the registration certificate:FARMZASCHITA NPC, FSUE FARMZASCHITA NPC, FSUE Russia

Manufacturer: & nbsp

FARMZASCHITA NPC, FSUE Russia

Information update date: & nbsp03.10.2017

Illustrated instructions

Instructions

Etamsylate (Etamsylate)