Etamsylate

General characteristics. Structure:

Acting substances: 125 mg of etamsylate.         

Excipients: sodium of a sulfite feast (sodium disulphite), sodium sulfite anhydrous (sodium sulfite), disodium salt of ethylene diamine, tetraacetic acid (Trilonum of B) (эдетат dinatrium), water for injections.

Etamsylate is haemo static lekartsvenny drug.

Pharmacological properties:

Pharmacodynamics. Styptic action is based on strengthening of interaction between an endothelium and thrombocytes. Increases adhesion of thrombocytes, stabilizes walls of capillaries, reducing, thus, their permeability, slows down synthesis of prostaglandins causing disaggregation of thrombocytes, a vazodilatation and increase in permeability of capillaries that reduces a bleeding time and reduces blood losses. Increases the speed of formation of primary blood clot and strengthens its retraction, practically does not influence the level of fibrinogen and a prothrombin time. Recovers patholologically the changed bleeding time. Does not influence normal parameters of system of a hemostasis. The haemo static effect at intravenous administration of solution of Etamsylate occurs in 5-15 minutes, the maximum effect - in 1 - 2 hour, action proceeds within 4-6 hours. At intramuscular introduction the haemo static effect occurs in 30-60 minutes

Pharmacokinetics. Drug is well absorbed at intramuscular introduction, poorly contacts proteins of plasma and uniform elements of blood. Etamsylate is evenly distributed in various bodies and fabrics (depends on extent of their blood supply). The drug elimination half-life after intravenous administration makes 1,9 hours, after intramuscular introduction - 2,1 hours. In 5 minutes after intravenous administration kidneys allocate 20-30% of the administered drug, completely - in 4 hours. Effective concentration in blood - 0,05-0,02 mg/ml. Drug is removed from an organism mainly with urine, in insignificant quantity with bile

Indications to use:

Capillary bleedings of various etiology, especially if bleeding is caused by damage of an endothelium: prevention and a stop of bleedings in time and after surgeries on well vaskulyarizovanny fabrics in otolaryngology, gynecology, obstetrics, urology, stomatology, ophthalmology and plastic surgery; prevention and treatment of capillary bleedings of various etiology and localization: a hamaturia, a metrorrhagia, primary menorrhagia, a menorrhagia at women with intrauterine contraceptives, nasal bleedings, bleeding of gums.

Route of administration and doses:

Etamsylate is entered intravenously, intramusculary, in ophthalmology subkonjyunktivalno and retrobulbarno. Etamsylate can be entered intravenously kapelno into 5% solution of glucose or in isotonic solution of sodium of chloride.

Adult: with the preventive purpose at operative measures the drug is administered intravenously or intramusculary in 1 hour prior to operation in a dose of 0,25-0,5 g (2-4 ml of 12,5% of solution), if necessary during operation - in a dose of 0,25-0,5 g (2-4 ml of 12,5% of solution), at danger of postoperative bleeding - 0,5-0,75 g (4-6 ml of 12,5% of solution) within a day.

To children: if necessary intraoperatsionno Etamsylate is entered intravenously at the rate of 8-10 mg/kg of body weight. For a bleeding stop Etamsylate is entered intravenously or intramusculary by 0,25-0,5 g (2-4 ml of 12,5% of solution) then each 4-6 hours on 0,25 g (2 ml of 12,5% of solution) within 5-10 days.

At treatment метрот - menorrhagias Etamsylate each 6-8 hours within 5-10 days appoint in a single dose 0,25 g (2 ml of 12,5% of solution) intravenously or intramusculary.

At a diabetic miakroangiopatiya Etamsylate is entered intramusculary within 10-14 days in a single dose of 0,25-0,5 g by three times a day.

In ophthalmology Etamsylate is entered subkonjyuktivalno or retrobulbarno - in a dose of 0,125 g (1 ml of 12,5% of solution).

Features of use:

It is required to be careful from patients at whom thrombosis or a thrombembolia was ever observed.

Drug is inefficient at patients with reduced number of thrombocytes. At the gemoryoragichesky complications connected with overdose of anticoagulants it is recommended to ispolzoyovat specific antidotes.

Use of etamsylate at patients with the broken indicators of coagulant system of blood is possible, but it has to be added with administration of the drugs eliminating the revealed deficit or defect of factors of coagulant system.

Safety of use of etamsylate at pregnancy is not established. Etamsylate should be applied during pregnancy only in those cases if the potential advantage for mother exceeds possible risk for a fruit It is necessary to stop breastfeeding during treatment of mother the drug Etamsylate.

Side effects:

Headache, dizziness, face reddening, allergic rash, paresthesias of the lower extremities, lowering of arterial pressure.

Interaction with other medicines:

It is impossible to mix Etamsylate with other medicines. Administration of drug in a dose of 10 mg/kg of body weight in 1 hour prior to administration of solutions of dextrans with an average molecular weight of 30000-40000 Da prevents anti-aggregation action of the last; administration of etamsylate after solutions of dextrans has no haemo static effect. Perhaps sochetayony Egamzilata with aminocapronic acid and sodium Menadionum bisulphite.

Contraindications:

Acute porphyria, hemoblastosis at children, hypersensitivity to any ingredient of drug; thrombosis; thromboembolism.

With care - at bleedings against the background of overdose of anticoagulants, pregnancy.

Storage conditions:

Period of validity 4 years. After a period of validity not to apply In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 125 mg/ml. On 2 ml in ampoules. On 5 ampoules place in blister strip packagings. On 1, 2 blister strip packagings stack in a pack from a cardboard. On 10 ampoules in a pack from a cardboard. The pack is pasted over with the label - a parcel post from paper label or coated. Put the application instruction, a knife in each pack ampoule or the scarificator ampoule ceramic. When using ampoules with notches, points or rings the knife ampoule does not invest.