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

The drug has a haemostatic effect, the mechanism of which is due to the activation of thromboplastin formation at the site of damage to small vessels and a decrease in the formation of prostacyclin vessels in the endothelium. This helps increase the adhesion, and then the aggregation of platelets, which, at eventually, leads to a halt or decrease in bleeding. Etamsylate stimulates the formation of platelets from megakaryocytes and their exit from the bone marrow, accelerates the formation of tissue thromboplastin, promotes an increase in the rate of formation of the primary thrombus at the site of injury and enhance its retraction.

The drug strengthens education at wall capillaries mucopolysaccharides with a large molecular weight, increases the resistance of capillaries, normalizes the permeability of the latter in pathological processes and improves microcirculation.

Against the background of Etamzilat treatment, pathologically altered parameters of hemostasis are restored, for example, bleeding time, but this preparation does not influence the normal parameters of the hemostasis system.

The haemostatic effect with intravenous (iv) Etamzilate is 5-15 minutes, the maximum effect after 1-2 hours, the effect lasts for 4-6 hours. With intramuscular (intramuscular) administration, the haemostatic effect occurs after 30- 60 min.

Pharmacokinetics:

It is well absorbed with both in / m and / in the introduction. After intravenous or intravenous administration of etamzilate at a dose of 500 mg, its concentration in plasma after 1 hour is 30 μg / ml. 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). The elimination half-life after intravenous administration is 1.9 hours, and after IM is 2.1 hours, respectively. Binding to plasma proteins is 95%. Etamsylate is not metabolized and is excreted from the body in an unchanged form mainly by the kidneys (> 80%), partially excreted through the intestine.

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, otolaryngological practice, intestinal,renal, pulmonary hemorrhage, metro- and menorrhagia in fibromyoma, etc.), secondary bleeding against thrombocytopenia and thrombocytopathy, hypocoagulation, hematuria, intracranial hemorrhage (including in newborns and premature infants), nasal bleeding against arterial hypertension, bleeding due to drug use, hemorrhagic diathesis (including Werlhof, Willebrand-Jurgens disease, thrombocytopathy), diabetic microangiopathy (hemorrhagic diabetic retinopathy, repeated bleeding in the retina, g ophthalmia).

Contraindications:

Hypersensitivity to any of the components of the drug, thrombosis, thromboembolism, acute porphyria, hemoblastosis in children, lactation.

Carefully:When bleeding against a background of an overdose of anticoagulants, thrombosis or thromboembolism in the anamnesis, pregnancy.

Caution is prescribed to patients with heart rhythm disturbances and angina pectoris.

Pregnancy and lactation:

The safety of the drug in pregnant women is not established. Etamsylate should be used during pregnancy only if the potential benefit to the mother exceeds the possible risk to the fetus.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Etalesylate is used iv, in / m, in ophthalmology is administered subconjunctivalally or retrobulbarno.

Etamsylate can be injected intravenously in a 5% solution of dextrose or in a 0.9% solution of sodium chloride.

Adults: for prophylactic purposes for surgical interventions, the drug is administered iv or IM for 1 h before the operation at a dose of 0.25-0.5 g (2-4 ml of 12.5% solution), if necessary during surgery - in dose of 0.25-0.5 g (2-4 ml of 12.5% solution), with the danger of postoperative bleeding, prophylaxis is introduced - 0.5-0.75 g (4-6 ml of 12.5% solution) within 24 hours .

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

To stop bleeding Etamsylate injected intravenously or intramuscularly with 0.25-0.5 g (2-4 ml of a 12.5% solution), after which every 4 to 6 hours, 0.25 g (2 ml 12.5% solution) for 5-10 days.

When treating metrorrhagia and menorrhagia Etamsylate appoint a single dose of 0.25 g (2 ml of 12.5% solution) intravenously or intramuscularly every 6-8 hours for 5-10 days.

With diabetic microangiopathy Etamsylate administered intramuscularly during 10-14 days in a single dose of 0.25-0.5 g three times a day.

In ophthalmology Etamsylate injected subconjunctivally or retrobulbarno - in a dose of 0.125 g (1 ml of 12.5 % solution).

Side effects:

Possible headache, dizziness, hyperemia of the facial skin, a decrease in systolic blood pressure, paresthesia of the lower extremities, allergic reactions, nausea, heartburn, a feeling of heaviness in the epigastric region.

Overdose:

There is no evidence of an overdose of the drug.

Interaction:

Solution Etamsylate can not be mixed in one syringe with other drugs.

With simultaneous application with rheopoliglukin, the effects of both drugs are completely inhibited.

Administration of the drug at a dose of 10 mg / kg body weight 1 hour prior to administration of solutions of dextrans with an average molecular weight of 30,000-40000 Da prevents the antiplatelet effect of the latter; the administration of etamzilate after solutions of dextrans does not exert a haemostatic effect.

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

Special instructions:

Care must be taken in patients who have ever had thrombosis or thromboembolism.

The drug is ineffective in patients with a reduced number of platelets.

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

Etalesylate is prescribed only as an auxiliary and, mainly, in the violation of the platelet-vascular component of hemostasis.

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

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

During the period of treatment, it is not recommended to drive vehicles and engage in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular injection, 125 mg / ml.

Packaging:

When produced at OOO "Experimental Plant" GNTSLS ", Ukraine.

2 ml in ampoules.

10 ampoules together with instructions for use and a scarifier with an ampoule or a cutting ceramic disc in a pack of cardboard with a cardboard splitter. If an ampoule has a fracture ring or a fracture point, an ampoule scriber or a ceramic cutting disc in a pack

Storage conditions:

Store in a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.

Terms leave from pharmacies.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N 015534/01

Date of registration:18.03.2009

The owner of the registration certificate:EXPERIMENTAL FACTORY ГНЦЛС, ООО EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

Manufacturer: & nbsp

EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

Information update date: & nbsp05.10.2015

Illustrated instructions

Instructions

Etamsylate (Etamsylate)