Etamsylate (Tablets, Solution) Instructions for Use
ATC Code
B02BX01 (Etamsylate)
Active Substance
Etamsylate (Rec.INN registered by WHO)
Clinical-Pharmacological Group
Hemostatic agent. Thromboplastin formation activator
Pharmacotherapeutic Group
Hemostatic agents; vitamin K and other hemostatic agents; other systemic hemostatic agents
Pharmacological Action
A hemostatic agent that also has angioprotective and proaggregant effects. It stimulates the formation of platelets and their release from the bone marrow.
The hemostatic effect, due to the activation of thromboplastin formation at the site of damage to small vessels and a decrease in the formation of prostacyclin PgI2 in the vascular endothelium, contributes to increased platelet adhesion and aggregation, which ultimately leads to the cessation or reduction of bleeding.
It increases the rate of primary thrombus formation and enhances its retraction, practically without affecting the concentration of fibrinogen and prothrombin time. Doses greater than 2-10 mg/kg do not lead to a greater severity of the effect. With repeated administrations, thrombus formation is enhanced.
Possessing antihyaluronidase activity and stabilizing ascorbic acid, it prevents the destruction and promotes the formation of high molecular weight mucopolysaccharides in the capillary wall, increases capillary resistance, reduces their fragility, and normalizes permeability in pathological processes.
It reduces the leakage of fluid and diapedesis of formed blood elements from the vascular bed and improves microcirculation. It does not have a vasoconstrictive effect. It restores the pathologically altered bleeding time.
It does not affect the normal parameters of the hemostasis system. The hemostatic effect after intravenous administration of etamsylate occurs within 5-15 minutes, the maximum effect is manifested after 1-2 hours.
The action lasts for 4-6 hours, then gradually weakens over 24 hours; with intramuscular administration, the effect occurs after 30-60 minutes.
Pharmacokinetics
Etamsylate is well absorbed after intramuscular administration, weakly binds to plasma proteins and formed blood elements. Cmax in plasma after intramuscular and intravenous administration at a dose of 500 mg is reached after 10 minutes and is 30-50 µg/ml. The therapeutic concentration in blood is 0.05-0.02 mg/ml. Etamsylate is evenly distributed in various organs and tissues (depending on the degree of their blood supply).
After oral administration, it is rapidly and almost completely absorbed. Cmax in plasma after a dose of 500 mg is reached after 4 hours and is 15 µg/ml.
Binding to plasma proteins is about 95%.
It penetrates the placental barrier almost completely. It is not known whether Etamsylate is excreted in breast milk.
It is excreted from the body mainly by the kidneys (unchanged), in small amounts with bile. T1/2 after oral administration is about 3.7 hours, after intravenous administration – 1.9 hours, after intramuscular administration – 2.1 hours.
It is excreted from the body mainly by the kidneys (unchanged), in small amounts with bile: after oral administration – 72% within 24 hours; 5 minutes after intravenous administration – 20-30% of the dose, completely – after 4 hours.
Indications
Prevention and cessation of bleeding: parenchymal and capillary bleeding (including traumatic, in surgery during operations on highly vascularized organs and tissues, during surgical interventions in dental, urological, ophthalmological, otolaryngological practice, intestinal, renal, pulmonary bleeding, metrorrhagia and menorrhagia with fibroids and others), secondary bleeding against the background of thrombocytopenia and thrombocytopathy, hypocoagulation, hematuria, intracranial hemorrhage (including in newborns and premature infants), nosebleeds against the background of arterial hypertension, bleeding caused by medication, hemorrhagic diathesis (including Werlhof’s disease, Willebrand-Jürgens disease, thrombocytopathy), diabetic microangiopathy (hemorrhagic diabetic retinopathy, repeated retinal hemorrhage, hemophthalmos).
ICD codes
| ICD-10 code | Indication |
| D68.0 | Von Willebrand’s disease |
| D69.1 | Qualitative platelet defects |
| D69.3 | Idiopathic thrombocytopenic purpura |
| H35.6 | Retinal hemorrhage |
| H36.0 | Diabetic retinopathy |
| H44.8 | Other disorders of globe (including hemophthalmos) |
| I62.9 | Intracranial hemorrhage (nontraumatic) unspecified |
| K92.2 | Gastrointestinal hemorrhage, unspecified |
| N92.0 | Excessive and frequent menstruation with regular cycle (menorrhagia, polymenorrhea) |
| N92.1 | Heavy and frequent menstruation with irregular cycle (menometrorrhagia, metrorrhagia) |
| N93 | Other abnormal uterine and vaginal bleeding |
| P52 | Intracranial nontraumatic hemorrhage of fetus and newborn |
| R04.0 | Epistaxis |
| R04.8 | Bleeding from other parts of the respiratory tract |
| R31 | Unspecified hematuria |
| R58 | Hemorrhage, not elsewhere classified |
| ICD-11 code | Indication |
| 3B12 | Von Willebrand’s disease |
| 3B62.Z | Thrombocytopathy, unspecified |
| 3B64.10 | Immune thrombocytopenic purpura |
| 8B0Z | Intracranial hemorrhage, unspecified |
| 9B3Z | Disorders of the anterior segment of the eyeball, unspecified |
| 9B71.0Z | Diabetic retinopathy, unspecified |
| 9B78.5 | Retinal hemorrhage |
| 9C0Z | Diseases of the posterior segment of the eye, unspecified |
| 9E1Z | Diseases of the visual system, unspecified |
| GA20.Z | Menstrual cycle disorders associated with bleeding, unspecified |
| GA2Z | Abnormal uterine or vaginal bleeding, unspecified |
| KA82.Z | Intracranial nontraumatic hemorrhage of fetus or newborn, unspecified |
| MD20 | Epistaxis |
| MD23 | Bleeding from other parts of the respiratory tract |
| ME24.90 | Acute gastrointestinal hemorrhage, not elsewhere classified |
| ME24.A0 | Gastrointestinal hemorrhage of unspecified site |
| ME24.A2 | Esophageal bleeding |
| ME24.Y | Other specified clinical manifestations related to the digestive system |
| MF50.4Z | Hematuria, unspecified |
| MG27 | Hemorrhage, not elsewhere classified |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Administer orally, intramuscularly, intravenously, topically, subconjunctivally, or retrobulbarly.
Determine the dosage regimen individually based on the indication, clinical situation, patient age, and the specific dosage form used.
For adults, the typical oral dose is 250-500 mg (1-2 tablets) three to four times daily.
For parenteral administration in adults, administer 125-250 mg (1/2-1 ampoule) intramuscularly or intravenously three to four times daily.
For severe or acute bleeding, initiate therapy with a single intravenous dose of 250-500 mg, followed by 250 mg every 6 hours via intramuscular or intravenous injection.
For children aged 3 to 14 years, the oral dose is 125-250 mg (1/2-1 tablet) three times daily.
For parenteral administration in children, the dose is 125 mg (1/2 ampoule) intramuscularly or intravenously three times daily.
For premature newborns and infants, administer a dose of 12.5 mg/kg body weight intravenously every 6 hours.
For ophthalmic surgery, administer a subconjunctival or retrobulbar injection of 125-250 mg (1/2-1 ampoule) preoperatively.
For topical application, apply a solution-soaked gauze pad directly to the bleeding site.
The duration of treatment depends on the hemostatic effect achieved and the underlying condition; continue therapy until bleeding is controlled and for several days thereafter to prevent recurrence.
Do not administer intra-arterially.
For intravenous injection, administer the solution slowly over several minutes to minimize the risk of a pronounced decrease in blood pressure.
Adverse Reactions
From the digestive system often – nausea, diarrhea, heaviness in the epigastric region.
From the skin and subcutaneous tissues often – skin rash; frequency unknown – facial skin redness.
From the nervous system: often – headache; frequency unknown – dizziness, paresthesia of the lower extremities.
From the cardiovascular system very rarely – thromboembolism, pronounced decrease in blood pressure.
From the hematopoietic system very rarely – agranulocytosis, neutropenia, thrombocytopenia.
From the musculoskeletal system: very rarely – arthralgia.
Other often – asthenia; very rarely – allergic reactions, fever.
Contraindications
Hypersensitivity to etamsylate, acute porphyria, hemoblastosis in children, thrombosis, thromboembolism; pregnancy, lactation (breastfeeding); children under 3 years of age (for oral administration).
With caution
History of thrombosis, thromboembolism; bleeding due to anticoagulant overdose; impaired liver and/or kidney function.
Use in Pregnancy and Lactation
Contraindicated for use during pregnancy and breastfeeding.
Use in Hepatic Impairment
Should be used with caution in patients with impaired liver function.
Use in Renal Impairment
Should be used with caution in patients with impaired kidney function.
Pediatric Use
It is possible to use in children according to indications, in doses, regimens and dosage forms recommended for the respective age. It is necessary to strictly follow the instructions in the etamsylate drug leaflets regarding contraindications for the use of specific etamsylate dosage forms in children of different ages.
Geriatric Use
Use with caution in elderly patients to avoid the risk of exacerbation of chronic diseases.
Special Precautions
Before starting treatment, other causes of bleeding should be excluded.
Etamsylate is ineffective in patients with a reduced platelet count.
For hemorrhagic complications associated with anticoagulant overdose, the use of specific antidotes is recommended.
The use of etamsylate in patients with impaired blood clotting parameters is possible, but it should be supplemented by the administration of drugs that eliminate the identified deficiency or defect in the clotting factors.
Due to the increased risk of a pronounced decrease in blood pressure with the parenteral method of etamsylate administration, caution should be exercised in patients with unstable blood pressure or a tendency to hypotension.
Drug Interactions
Administration of etamsylate at a dose of 10 mg/kg 1 hour before the administration of dextran solutions with an average molecular weight of 30,000-40,000 prevents their antiaggregatory action; administration of etamsylate after dextran solutions does not have a hemostatic effect.
Combination with aminocaproic acid and menadione sodium bisulfite is possible.
Etamsylate is pharmaceutically incompatible (in the same syringe) with other drugs.
Storage Conditions
Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.
Dispensing Status
Rx Only
Important Safety Information
This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Solution for injection 125 mg/ml: amp. 2 ml 10 pcs.
Marketing Authorization Holder
Alvils, LLC (Russia)
Manufactured By
Ozon, LLC (Russia)
Dosage Form
 |
Etamsylate | Solution for injection 125 mg/ml: amp. 2 ml 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection transparent, colorless or slightly colored.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients : sodium disulfite (metabisulfite) – 2.5 mg, sodium sulfite – 1 mg, disodium edetate dihydrate – 0.5 mg, water for injections – up to 1 ml.
2 ml – ampoules (10) – blisters (1) – cardboard packs.
Solution for injection 125 mg/ml: 2 ml amp. 5 or 10 pcs.
Marketing Authorization Holder
Atoll LLC (Russia)
Manufactured By
Ozon, LLC (Russia)
Dosage Form
|
Etamsylate | Solution for injection 125 mg/ml: 2 ml amp. 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection transparent, colorless or slightly yellowish.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients : sodium disulfite 2.5 mg, sodium sulfite – 1 mg, disodium edetate – 0.5 mg, water for injections up to 1 ml.
2 ml – ampoules made of colorless type I glass (5) – contour cell packs (1) – cardboard packs.
2 ml – ampoules made of colorless type I glass (5) – contour cell packs (2) – cardboard packs.
Solution for injection 125 mg/ml: 2 ml amp. 10 pcs.
Marketing Authorization Holder
Biosintez, PJSC (Russia)
Dosage Form
|
Etamsylate | Solution for injection 125 mg/ml: 2 ml amp. 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection transparent, colorless or slightly colored.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients : sodium disulfite 2.5 mg, anhydrous sodium sulfite 1 mg, sodium edetate dihydrate 0.5 mg, water for injections up to 1 ml.
2 ml – ampoules (5) – contour cell packs made of polyvinyl chloride film (2) – cardboard packs.
2 ml – ampoules (10) – cardboard boxes with partitions.
Tablets 250 mg: 50 pcs.
Marketing Authorization Holder
Lugansk Chemical And Pharmaceutical Plant, PJSC (Ukraine)
Dosage Form
|
Etamsylate | Tablets 250 mg: 50 pcs. |
Dosage Form, Packaging, and Composition
Tablets white or white with a creamy or pinkish tint, with a score and a bevel.
| 1 tab. | |
| Etamsylate | 250 mg |
Excipients : calcium phosphate dihydrate, sodium pyrosulfate (sodium acid pyrosulfate), potato starch, calcium stearate, polyvinylpyrrolidone.
10 pcs. – contour cell packs (5) – cardboard packs.
50 pcs. – contour cell packs (1) – cardboard packs.
50 pcs. – dark glass jars (1) – cardboard packs.
Solution for injection 125 mg/1 ml: amp. 2 ml 5, 10, 20 or 50 pcs.
Marketing Authorization Holder
Novosibkhimpharm, JSC (Russia)
Dosage Form
|
Etamsylate | Solution for injection 125 mg/1 ml: amp. 2 ml 5, 10, 20 or 50 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection in the form of a transparent, colorless or slightly colored liquid.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients : sodium disulfite (sodium pyrosulfite) – 2.5 mg, sodium sulfite (sodium sulfite) – 1 mg, disodium edetate (disodium salt of ethylenediaminetetraacetic acid) [Trilon B] – 0.5 mg, water for injections – 1 ml.
2 ml – glass ampoules (10) – cardboard boxes.
2 ml – glass ampoules (5) – contour cell packs (1) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packs (2) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packs (10) – cardboard packs.
2 ml – glass ampoules (10) – contour cell packs (1) – cardboard packs.
2 ml – glass ampoules (10) – contour cell packs (2) – cardboard packs.
2 ml – glass ampoules (10) – contour cell packs (5) – cardboard packs.
Solution for injection 125 mg/ml: syringe 2 ml
Marketing Authorization Holder
Pharmazashchita SPC, FSUE FMBA of Russia (Russia)
Dosage Form
|
Etamsylate | Solution for injection 125 mg/ml: syringe 2 ml |
Dosage Form, Packaging, and Composition
Solution for injection in the form of a colorless or slightly colored, transparent liquid.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients : sodium metabisulfite – 0.42 mg, sodium hydroxide solution 1M – to pH 6.3, water for injections – up to 1 ml.
2 ml – glass syringes (1) – contour cell packs (1) – cardboard packs.
Solution for intravenous and intramuscular administration 250 mg/2 ml: amp. 10 pcs.
Marketing Authorization Holder
Experimental Plant Of The Ssc Ls Of The Ukrmedprom Association, SC (Ukraine)
Dosage Form
|
Etamsylate | Solution for intravenous and intramuscular administration 250 mg/2 ml: amp. 10 pcs. |
Dosage Form, Packaging, and Composition
| Solution for intravenous and intramuscular administration | 1 ml | 1 amp. |
| Etamsylate | 125 mg | 250 mg |
2 ml – ampoules (10) – carton packs.
Solution for intravenous and intramuscular administration 250 mg/2 ml: amp. 5 or 10 pcs.
Marketing Authorization Holder
Promomed Rus LLC (Russia)
Manufactured By
Biokhimik, JSC (Russia)
Dosage Form
|
Etamsylate | Solution for intravenous and intramuscular administration 250 mg/2 ml: amp. 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
| Solution for intravenous and intramuscular administration | 1 ml | 1 amp. |
| Etamsylate | 125 mg | 250 mg |
2 ml – ampoules (10) – carton packs.
2 ml – ampoules (5) – contour plastic packs (1) – carton packs.
2 ml – ampoules (5) – contour plastic packs (2) – carton packs.
Solution for injection 125 mg/ml: 2 ml amp. 1, 2, 5 or 10 pcs.
Marketing Authorization Holder
Ellara, LLC (Russia)
Dosage Form
|
Etamsylate | Solution for injection 125 mg/ml: 2 ml amp. 1, 2, 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection transparent, colorless or with a yellowish tint.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients: sodium disulfite – 2.5 mg, sodium sulfite – 1 mg, disodium edetate – 0.5 mg, water for injection – up to 1 ml.
2 ml – ampoules – carton packs.
2 ml – ampoules (2) – carton packs.
2 ml – ampoules (5) – carton packs.
2 ml – ampoules (10) – carton packs.
2 ml – ampoules (20) – carton packs (for hospitals).
2 ml – ampoules (25) – carton packs (for hospitals).
2 ml – ampoules (50) – carton packs (for hospitals).
2 ml – ampoules (250) – carton boxes (for hospitals).
2 ml – ampoules (500) – carton boxes (for hospitals).
Solution for injection 125 mg/1 ml: amp. 2 ml 5 or 10 pcs.
Marketing Authorization Holder
Bryntsalov-A, JSC (Russia)
Manufactured By
Bryntsalov-A, JSC (Russia)
Or
Ferein, CJSC (Republic Of Belarus)
Dosage Form
|
Etamsylate-Ferein® | Solution for injection 125 mg/1 ml: amp. 2 ml 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for injection transparent, colorless or slightly colored.
| 1 ml | |
| Etamsylate | 125 mg |
Excipients: sodium disulfite – 2.5 mg, sodium sulfite – 1 mg, disodium edetate – 0.5 mg, water for injection – up to 1 ml.
2 ml – glass ampoules (5) – contour cell packs (1) – carton packs.
2 ml – glass ampoules (5) – contour cell packs (2) – carton packs.
Tablets 0.25 g: 10, 20, 30, 40, or 50 pcs.
Marketing Authorization Holder
Bryntsalov-A, JSC (Russia)
Dosage Form
|
Etamsylate-Ferein® | Tablets 0.25 g: 10, 20, 30, 40, or 50 pcs. |
Dosage Form, Packaging, and Composition
Tablets white or white with a creamy or pinkish tint, slightly marbled, flat-cylindrical with a score.
| 1 tab. | |
| Etamsylate | 0.25 g |
Excipients: calcium phosphate dihydrate – 0.161 g, sodium pyrosulfite (sodium metabisulfite) – 0.001 g, potato starch – 0.033 g, povidone – 0.002 g, calcium stearate – 0.002 g.
10 pcs. – contour cell packs (1) – carton packs.
10 pcs. – contour cell packs (2) – carton packs.
30 pcs. – polymer jars (1) – carton packs.
40 pcs. – polymer jars (1) – carton packs.
50 pcs. – polymer jars (1) – carton packs.
![Etamsylate [Tablets, Solution] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Etamsylate [Tablets, Solution] 2")