Dicynone (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 pathologically altered bleeding time.

It does not affect the normal parameters of the hemostatic 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 blood cells. C_max 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. C_max 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. T_1/2 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 stopping 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, otorhinolaryngological 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

Dosage Regimen

Administer orally, intramuscularly, intravenously, topically, subconjunctivally, or retrobulbarly. Set the dosage regimen individually based on indication, clinical situation, patient age, and dosage form.

For adults, the typical oral dose is 250-500 mg ( 1-2 tablets) three to four times daily. For parenteral administration, administer 250-500 mg ( 2-4 mL of solution) intramuscularly or intravenously two to three times daily.

For severe bleeding, use an initial intravenous dose of 500 mg, followed by 250-500 mg every 6 hours. Switch to oral administration when clinically appropriate.

For prevention of bleeding during surgery, administer 250-500 mg parenterally before the procedure. Postoperatively, continue with 250-500 mg every 6 hours, orally or parenterally, for several days.

In ophthalmology, for diabetic retinopathy, administer 250-500 mg orally two to three times daily for several months. For subconjunctival or retrobulbar use, administer 125-250 mg ( 1-2 mL) daily.

For children, calculate the oral dose at 10-15 mg/kg/day, divided into three to four doses. For parenteral administration, use 5-10 mg/kg intramuscularly or intravenously two to three times daily.

For premature newborns with intracranial hemorrhage, administer 6.25 mg/kg ( 0.5 mL/kg) intravenously or intramuscularly every 6 hours.

Adjust the dose and duration of therapy based on clinical response and hemostatic effect. Do not exceed the maximum daily dose.

For topical use in epistaxis, apply a cotton swab soaked in the solution to the bleeding site. In dental practice, apply topically after tooth extraction.

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 overdose of anticoagulants; 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 according to 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.

In case of 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 parameters is possible, but it should be supplemented by the administration of drugs that eliminate the identified deficiency or defect in the coagulation system 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 antiaggregant effect; 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.