Etamzilat injections. The ability to influence the reaction rate when driving a vehicle or working with other mechanisms

Name:

Name: Etamsylat (Etamsylatiim)

Indications for use:
Etamsylate is used to prevent and stop capillary (from the smallest vessels) bleeding in diabetic angiopathy (vascular disease associated with an increase in blood sugar levels); surgical interventions in otorhinolaryngology (tonsillectomy /removal of the palatine tonsils - tonsils/), microsurgical operations on the ear, etc.), ophthalmology (keratoplasty /surgical replacement of part of the cornea/, cataract removal, antiglaucomatous operations and other fine surgical interventions), dentistry (removal of cysts , granulomas, extraction / removal / of teeth, etc.), urology (after prostatectomy / removal of the prostate gland / etc.), in surgical and gynecological (especially during operations on highly vascularized / abundantly blood-supplied / tissues) practice, also in emergency cases of intestinal and pulmonary bleeding and hemorrhagic diathesis (increased bleeding).

Pharmachologic effect:
The drug increases the formation of high molecular weight mucopolysaccharides in the walls of capillaries (the smallest vessels) and increases the stability of capillaries, normalizes their permeability during pathological processes, improves microcirculation (blood flow through the smallest vessels of the organ); It also has a hemostatic (hemostatic) effect. The hemostatic effect is apparently associated with an activating effect on the formation of thromboplastin. The drug stimulates the formation of blood coagulation factor III, normalizes the adhesion (gluing rate) of platelets. The drug does not affect prothrombin time (an indicator of blood clotting time), does not have hypercoagulable properties (does not cause increased blood clotting) and does not contribute to the formation of thrombi (blood clots).

Etamsylate method of administration and dosage:
Prescribed intravenously, intramuscularly, subconjunctivally (under the outer shell of the eye), retrobulbarly (behind the eyeball) and orally.
The hemostatic effect of etamsylate develops after intravenous administration after 5-15 minutes, the maximum effect occurs after 1-2 hours, the effect lasts 4-6 hours or more. When administered intramuscularly, the effect occurs somewhat more slowly. When taken orally, the maximum effect is observed after 3 hours.
For prophylactic purposes, the product is administered intravenously or intramuscularly 1 hour before surgery in a dose of 2-4 ml (1-2 ampoules), which corresponds to 0.25-0.5 g of ethamsylate, or given orally 2-3 tablets (0.25 d) 3 hours before surgery. If necessary, 2-4 ml are administered intravenously during surgery. If there is a danger of bleeding after surgery, administer prophylactically from 4 to 6 ml (2-4 ampoules) per day or give from 6 to 8 tablets per day (evenly throughout the day).
For medicinal purposes (for bleeding), 2-4 ml are injected into a vein or intramuscularly at once, and then after 4-6 hours - 2 ml or 2 tablets are given.
Can be injected into a vein by drip, adding to regular solutions for infusion. Do not mix ethamsylate in the same syringe with other products.
In the treatment of metro- and menorrhagia (dysfunctional uterine bleeding), etamzilate is prescribed 0.5 g orally or 0.25 g parenterally (bypassing the digestive tract) every 6 hours for 5-10 days, then 0.25 g. orally 4 times every day or 0.25 g parenterally 2 times every day during hemorrhage (bleeding) and two subsequent cycles.
In the treatment of hemorrhagic diathesis (increased bleeding) and diseases of the blood system, the product is prescribed in courses of 1.5 g every day at regular intervals orally for 5-14 days. In severe cases, treatment begins with parenteral administration of 0.25-0.5 g 1-2 times every day for 3-8 days, and then administered orally.
For diabetic microangiopathies (damages of small blood vessels), in particular, for retinopathy with hemorrhages (damage to the vessels of the retina, accompanied by a violation of their integrity), etamsylate is prescribed in courses of 2-3 months, giving 1-2 tablets 3 times every day or injecting intramuscularly, 1 ampoule (2 ml) 2 times every day for 10-14 days.
1 ml of solution is injected subconjunctivally and retrobulbarly.

Available in the form of tablets in blisters of 100 pieces per package and in the form of a solution for injection. The tablets have a biconvex shape, white, with a dosage of 0.05 g for kittens and 0.25 g for adults.

Composition of the drug and release form

Ampoules are designed for intravenous and intramuscular use. A cardboard box contains 20 or 50 ampoules with a dosage: 1 ml - 5% solution, 2 ml - 12.5% ​​solution.

The tablets and solution contain the active component ethamsylate. The additional substances are:

• Injections: purified water, sodium disulfite and sodium bicarbonate;
• Tablets: lactose, povidone K25, citric acid and magnesium stearate.

Pharmacological properties

Dicynone is a hemostatic drug that improves platelet adhesion. With active exposure to substances, their quantity does not increase, the plasma remains in a normal state. Etamsylate also affects the capillaries and blood vessels of the pet, strengthening and increasing their stability. Thanks to this, the bleeding slows down significantly and the cat loses less blood.

Indications for use

The use of Etamsylate is necessary for capillary or parenchymal bleeding, thrombocytopathy or thrombocytopenia. It is also used for preventive purposes after surgery or for hemorrhagic syndrome, reducing heavy bleeding and eliminating hemostasis disorders.

Rules for the use of the drug

Instructions for use of Etamsylate for cats, available in the package, describe methods of using the drug in the form of tablets and solution. The tablets must be given orally in fractional form, ¼ twice a day, diluted with water in a teaspoon.

The solution is administered by injection intramuscularly. As a rule, cats resist strongly, so it is better to do the procedure with an assistant. It is recommended to give the injection in the thigh or shoulder, taking into account several nuances:

• The muscle for injection must be completely relaxed;
• There is no need to disinfect before injecting;
• The syringe should be directed at a slight angle;
• The needle and syringe must be sterile and should not be touched with hands;
• The depth of needle entry should not exceed 1 cm.

The dosage of Etamzilate intramuscularly for a cat is 0.1 ml per 1 kg of animal weight twice a day. For prevention, you can inject once.

Contraindications and side effects

The main contraindications for use are tumor diseases of blood vessels and capillaries. It is also prohibited to use the drug if you are lactose intolerant or have diabetes. In the presence of renal failure, impaired thrombus formation, or urolithiasis, giving Etamzilat to a cat is contraindicated. This also applies to individual intolerance to the main or auxiliary substances in the composition of the medicine.

With proper treatment and compliance with the dosage, the drug is well tolerated. However, cats may experience some side effects:

• Low blood pressure;
• Dizziness, vomiting, stomach pain in the cat;
• Allergic reactions in the form of swelling, redness of the skin or mucous membranes.

Storage conditions and shelf life

Etamsylate must be stored in a dry place, protected from children and animals, at a temperature of no more than +24ºC. The shelf life of the drug is 3 years from the date of manufacture. Used or expired tablets and ampoules are disposed of along with household waste.

Etamzilate pharmacology belongs to the group of antihemorrhagic drugs. The drug is available in the form of tablets and solution for injection, which is a clear, colorless liquid. The main substance of the drug is ethamsylate, each ampoule of which contains 250 milligrams of this component.

Etamsylate is a medicine used to prevent or stop bleeding. It has the properties to influence the process of interaction between endothelium and platelets (the first stage of hemostasis).

It promotes:

• increasing platelet adhesiveness;
• normalizing the stability of the capillary wall, which helps reduce its permeability;
• inhibiting the synthesis of prostaglandins, which cause the destruction of red blood cells, relaxation and increased permeability of the smallest vessels.

As a result, there is a significant reduction in the volume and rate of bleeding.

Pharmacokinetic characteristics

After the first injections of the drug, doctors note, on average, after 10 minutes the onset of the hemostatic effect, the maximum peak of which occurs after an hour. At the same time, the maximum concentration of the substance in the blood is determined (subject to a dosage of 0.5 grams).

90% of the main component binds to proteins. More than half of the administered dose leaves the body within 24 hours in the form of an unchanged molecule. This drug can cross the blood-placental barrier, but there is no information about its possible passage into breast milk.

Indications

Instructions for use describe that the drug Etamzilate is recommended for the prevention and control of bleeding that occurs in the capillaries. This is especially true for cases of bleeding, which is caused by pathological conditions and processes in the endothelium.

Such cases include:

• preventive and therapeutic measures during and after surgical interventions on various organs and parts of the patient’s body;
• hematuria;
• metrorrhagia;
• primary hypermenorrhea;
• bleeding from the nose or gums;
• prevention of periventricular bleeding in babies born prematurely.

Contraindications

The main prohibitions on the use of the drug Etamzilat include:

• allergy to the main or auxiliary components of the drug;
• bronchial asthma;
• porphyria in the acute period;
• thromboembolism and thrombosis;
• hemoblastomosis in young patients.

Interaction

Clinical studies revealed the following:

• etamsylate inactivates vitamin B1;
• if etamsylate is administered 60 minutes before the use of rheopolyglucin, the antiplatelet effect is prevented, and if after, the hemostatic effect is prevented;
• it is allowed to combine Ethazilate with other drugs in this group;
• If mixed with saline, the drug must be administered immediately.

It is forbidden to mix Etamsylate with sodium bicarbonate and sodium lactate. Also, you should not use the same syringe to administer ethamsylate and other medications.

special instructions

Before starting to use the drug, it is important to rule out other causes that cause bleeding.

If there is no effect from using the drug during excessive or prolonged menstruation, you need to make sure that the bleeding is not caused by various pathological processes, which include fibrous formations in the uterus.

It is prescribed very carefully to patients if they have thrombosis or thromboembolism.

If a patient has a situation of unstable blood pressure or hypotension, then when administering Etamsylate intravenously, medical personnel should be as attentive as possible and monitor the patient’s well-being.

In case of a reduced platelet count, the use of this drug is not advisable.

When hemorrhagic complications occur caused by taking very large doses, it is important to take a specific antidote as quickly as possible.

Patients who have disorders in blood coagulation parameters are allowed to take the drug only if they additionally administer medications that have the properties of relieving the deficiency of these parameters.

Therapeutic doses can affect the results of tests for determining creatinine, namely, they reduce.

If the injection solution changes color during dilution, its administration is strictly prohibited.

Very often, the patient develops allergies and bronchospasm due to the presence of substances such as sodium metabisulfite and sodium sulfite.

Kidney pathologies

Clinical studies on the safety and effectiveness of this drug in patients with renal failure have not been conducted. It is worth considering that the kidneys are involved in the process of eliminating Etamzilate. For this reason, the dose of the drug is reduced.

Pregnancy and lactation

There is not enough information about the lack of influence of the main component of the drug on the mother’s body and her fetus. There is a strict ban on administering the medicine in the first months of pregnancy. During the rest of the period, it is important to consider the risk-benefit ratio.

In case of urgent need to administer Etamzilat during lactation, the child should be transferred to artificial feeding.

Speed ​​reaction

Ethamsylate has no effect on the reaction rate. It is important to remember that in some cases you may feel dizzy. This must be taken into account when driving a car or working with other complex mechanisms.

Dosage

Etamsylate in ampoules is used for intravenous or intramuscular administration. The maximum effective dose ranges from 10 to 20 mg per kilogram of patient weight per day. It should be entered 3 - 4 times. Most often it corresponds to 4 to 8 ampoules per day. The children's dosage is half the adult dosage.

60 minutes before surgery, 1 or 2 ampoules are injected into a vein or muscle. Doctors also use the drug during surgery. After the procedure is completed, the drug is used every 5 hours until the risk of bleeding completely disappears.

For newborn children, a dosage of 10 milligrams per kilogram of baby’s weight is used. Therapy should be started within 120 minutes after birth.

The drug can be used topically. Most often this occurs during tooth extraction. To do this, moisten a gauze cloth with the solution and apply it to the desired location. At this time, you can use IM or IV administration of the drug.

In the presence of pathology in the liver and kidneys, Etamzilat is used extremely carefully.

Overdose

There have been no reports of accidental or deliberate overdose. First aid for the development of this condition is symptomatic treatment.

Adverse reactions

During various studies, it turned out that Etamzilat has a certain effect on the patient’s body, which consists in the development of:

• dizziness;
• tides;
• thromboembolism;
• decrease in pressure;
• nausea and vomiting;
• diarrhea;
• abdominal pain;
• allergies;
• hives;
• itching;
• anaphylactic shock;
• agranulocytosis;
• neutropenia;
• thrombocytopenia;
• asthenia;
• temperature rise;
• bronchospasm.

It is worth noting that the negative effects of the drug are quite weak and can go away on their own.

Storage

To maintain the therapeutic effect, it is necessary not to exceed the temperature of 25 degrees in the room where the drug is located.

The shelf life of the drug is indicated on the packaging, each ampoule, and blister of tablets and is 36 months. After this period, the use of the medicine is prohibited and it must be destroyed.

Price

The average price for Etamzilat in ampoules is 80-85 rubles, and in tablets - about 100 rubles for 50 pieces.

In order to buy Etamzilat ampoules or tablets, you must contact your doctor and write a prescription, which will indicate the dose, frequency of administration or administration, and duration of therapy. Only a correctly executed document gives the patient the right to purchase the drug.

Analogs

An imported analogue of the drug Etamzilate is Dicinone, which is also available in ampoules and tablets.

Dosage form:  solution for intravenous and intramuscular administration Compound:

1 ml of the drug contains:

active substance: etamsylate 125.0 mg.

Excipients: sodium disulfite 4.0 mg, disodium edetate 0.1 mg, water for injection up to 1 ml.

Description: Transparent colorless or slightly colored liquid. Pharmacotherapeutic group:hemostatic agent ATX:  

B.02.B.X.01 Etamsylate

Pharmacodynamics:

The drug increases the formation of high molecular weight mucopolysaccharides in the walls of capillaries and increases the stability of capillaries, normalizes their permeability during pathological processes, improves microcirculation; has a hemostatic effect. The hemostatic effect is due to the activation of thromboplastin formation at the site of damage to small vessels. The drug stimulates the formation of blood coagulation factor III and normalizes platelet adhesion. The drug does not affect the level of fibrinogen and prothrombin time, does not have hypercoagulable properties and does not contribute to the formation of thrombi (blood clots).

Pharmacokinetics:

After intravenous administration, it begins to act within 5-15 minutes. Maximum effect 1 hour after dosing. The effect of the drug lasts for 4-6 hours. After administration of 500 mg, the maximum plasma concentration is reached after 10 minutes (50 μg/ml).

The plasma half-life after intravenous administration is approximately 2 hours. evenly distributed in various organs and tissues (depending on the degree of their blood supply).

The drug is well absorbed when administered intramuscularly and weakly binds to plasma proteins and blood cells. When administered intramuscularly, the hemostatic effect occurs within 30-60 minutes. The half-life from blood plasma after intramuscular administration is 2.1 hours.

Penetrates through the placental barrier and into breast milk.

About 72% of the administered dose is excreted unchanged through the kidneys during the first 24 hours.

Indications:

Prevention and treatment of capillary bleeding of various etiologies:

During and after surgical interventions on all well-vascularized tissues in dental, otorhinolaryngological, gynecological, urological, ophthalmological practice, obstetrics and plastic surgery;

Hematuria, metrorrhagia, primary menorrhagia, menorrhagia in women with intrauterine contraceptives, nosebleeds, bleeding gums;

Diabetic microangiopathy (hemorrhagic diabetic retinopathy, repeated retinal hemorrhage, hemophthalmos);

Intracranial hemorrhages in newborns and premature infants.

Contraindications:

Hypersensitivity to the components of the drug;

Hypersensitivity to sodium bisulfite;

Acute porphyria;

Hemoblastosis in children (lymphoblastic and myeloblastic leukemia);

Thromboembolism, thrombosis;

Breastfeeding period.

Carefully:

History of thrombosis, thromboembolism; bleeding due to an overdose of anticoagulants, pregnancy.

Pregnancy and lactation:

In animal studies, the teratogenic effect of ethamsylate was not revealed. In clinical studies, no fetotoxic effect of ethamsylate was observed. However, given the insufficient clinical experience, the use of etamsylate during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.

There are no data on the penetration of ethamsylate into breast milk. When prescribing the drug during lactation, breastfeeding should be stopped.

Directions for use and dosage:

Intravenously, intramuscularly.

Etamsylate can be administered intravenously in a 5% glucose solution or in an isotonic sodium chloride solution.

The optimal daily dose of ethamsylate for adults is 10-20 mg/kg body weight per day, divided into 3-4 doses, as an intramuscular or slow intravenous injection.

If mixed with saline, it should be used immediately.

For adults: during surgical interventions, 250-500 mg is administered intravenously or intramuscularly 1 hour before surgery; during surgery, 250-500 mg is administered intravenously; if necessary, this dose can be repeated again. After surgery, 250-500 mg is administered every 6 hours until the risk of bleeding disappears.

For children: The daily dose is 10-15 mg/kg body weight, divided into 3-4 doses.

In neonatology: administered intramuscularly or intravenously at a dosage of 12.5 mg per kg of body weight (0.1 ml = 12.5 mg). Treatment should begin within the first 2 hours after birth.

When treating metromenorrhagia, the drug is prescribed in a single dose of 250 mg (2 ml of 12.5% ​​solution) intravenously or intramuscularly every 6-8 hours for 5-10 days.

For diabetic microangiopathy, the drug is administered intramuscularly for10-14 days in a single dose of 250-500 mg three times a day. Side effects:

Allergic reactions, headache, dizziness, paresthesia of the lower extremities, decreased systolic blood pressure, flushing of the facial skin, nausea, heartburn, heaviness in the epigastric region, hyperthermia, skin rashes.

Overdose:

No cases of ethamsylate overdose have been reported to date.

Interaction:

Etamsylate is pharmaceutically incompatible (in the same syringe) with other drugs.

Ethamsylate solution is incompatible with sodium bicarbonate injection and sodium lactate solution.

Administration of the drug at a dose of 10 mg/kg body weight 1 hour before the administration of dextran solutions with an average molecular weight of 30,000-40,000 prevents the antiplatelet effect of the latter; administration of ethamsylate after dextran solutions does not have a hemostatic effect. A combination of ethamsylate with aminocaproic acid and menadione sodium bisulfite is possible.

Special instructions:

For use in medical institutions only.

Before starting treatment, other causes of bleeding should be excluded.

If the solution becomes colored, it should not be used.

The drug can be used topically (for example, in the case of a skin graft, after tooth extraction, etc.): a sterile swab or napkin is soaked in the solution and applied to the wound.

Caution is required in patients who have ever experienced thrombosis or thromboembolism. The drug is ineffective in patients with a low platelet count. For hemorrhagic complications associated with an overdose of anticoagulants, it is recommended to use specific antidotes. The use of etamsylate in patients with impaired blood coagulation system parameters is possible, but it should be supplemented by the administration of drugs that eliminate the identified deficiency or defect of coagulation factors.

The drug contains sodium bisulfite, which in rare cases can cause severe hypersensitivity reactions (including anaphylactic shock) and bronchospasm.

If hyperthermia occurs, treatment should be discontinued.

Impact on the ability to drive vehicles. Wed and fur.:

Etamsylate does not affect the ability to drive a car or operate other machinery.

active substance: etamsylate;

1 tablet contains etamsylate 250 mg;

Excipients: calcium hydrogen phosphate dihydrate, sodium metabisulfite (E 223), potato starch, povidone, calcium stearate.

Dosage form

Pills.

Pharmacotherapeutic group

Hemostatic agents for systemic use. Angioprotectors. ATC code B02B X01.

Indications

Prevention and control of hemorrhages in superficial and internal capillaries of various etiologies, especially if the bleeding is caused by damage to the endothelium:

• prevention and treatment of bleeding during and after surgical operations in otolaryngology, gynecology, obstetrics, urology, dentistry, ophthalmology and plastic surgery;
• prevention and treatment of capillary bleeding of various etiologies and localization: hematuria, metrorrhagia, primary hypermenorrhea, hypermenorrhea in women with intrauterine contraceptives, nosebleeds, bleeding gums.

Contraindications

Hypersensitivity to etamsylate or any other component of the drug. Acute porphyria, increased blood clotting, thrombosis, thromboembolism.

Pregnancy or breastfeeding period. Hemoblastosis (lymphatic and myeloid leukemia, osteosarcoma) in children.

Treatment can begin after ruling out the presence of fibrous formations of the uterus.

Directions for use and doses

Apply internally. Take the tablets during or after meals. The daily dose for adults is 1-2 tablets 3-4 times a day. In severe cases, the dose is 3 tablets 3-4 times a day.

For menorrhagia, 3-4 tablets per day are prescribed, starting from the 5th day from the expected start of menstruation until the 5th day of the next menstrual cycle.

After surgery, take 1-2 tablets every 6 hours until the risk of bleeding disappears.

The daily dose for children is half the dose for adults.

Adverse reactions

Nervous system: rarely - headache, dizziness, flushing, paresthesia in the legs.

Digestive tract: nausea, vomiting, diarrhea, epigastric pain.

Respiratory system: bronchospasm.

The immune system: rarely - allergic reactions, fever, skin rash, a case of angioedema has been described.

Endocrine system: very rarely - acute porphyria.

Musculoskeletal system: rarely - back pain.

All side effects are mild and transient.

Children treated with etamsylate to prevent bleeding in acute lymphatic and myeloid leukemia were more likely to have severe leukopenia.

Overdose

There are no data on overdose of etamsylate.

Use during pregnancy or breastfeeding

The safety of the drug during pregnancy has not been established. During treatment with the drug, breastfeeding should be stopped.

Children

The drug is used for children over 6 years of age. Not prescribed to children with hemoblastosis.

Features of application

Use with caution in patients who have previously experienced thrombosis or thromboembolism. The drug is ineffective if the platelet count is low.

Before starting treatment, other causes of bleeding should be excluded.

Treatment with etamsylate for patients with impaired blood coagulation parameters must be supplemented with the introduction of drugs that eliminate the detected deficiency or defect of blood coagulation factors.

The ability to influence the reaction rate when driving a vehicle or working with other mechanisms

Caution is required when working with vehicles or machinery, as dizziness may occur.

Interaction with other drugs and other types of interactions

Taking rheopolyglucin during administration prevents the anti-aggregation effects of the latter; taking it after administration of rheopolyglucin does not have a hemostatic effect. Combination with aminocaproic acid and vikasol is acceptable.

Pharmacological properties

Pharmacodynamics. Etamsylate is a means to prevent and stop bleeding. It affects the first stage of the hemostasis mechanism (the interaction between the endothelium and platelets). Etamsylate increases platelet adhesiveness, normalizes the stability of capillary walls, thus reducing their permeability, inhibits the biosynthesis of prostaglandins, which cause platelet disaggregation, vasodilation and increased capillary permeability. As a result, bleeding time is significantly reduced and blood loss is reduced.

Pharmacokinetics. Etamsylate is almost completely absorbed from the gastrointestinal tract, reaching peak serum concentrations 4 hours after administration.

Approximately 72% of the administered dose is excreted unchanged in the urine during the first 24 hours. Etamzilate penetrates the placental barrier and into breast milk.

Basic physical and chemical properties

tablets are white or almost white, flat-cylindrical, scored and chamfered.

Best before date

Storage conditions

No special storage conditions are needed. To protect from moisture and light, store in original packaging.

Keep out of the reach of children!

Package

10 or 50 tablets in a blister; 1 blister in a pack.

Vacation category

On prescription.

Manufacturer.

PJSC "Lugansk Chemical and Pharmaceutical Plant".