Emsibel (Solution, Drops) Instructions for Use

ATC Code

C05CX (Drugs reducing capillary permeability, other)

Active Substance

Methylethylpiridinol (Grouping Name)

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

Methylethylpiridinol inhibits platelet aggregation, reduces the overall coagulation index, and prolongs blood clotting time. It enhances the process of fibrinolysis. It reduces blood viscosity and decreases the permeability of the vascular wall. It stabilizes the membranes of blood vessel cells and erythrocytes, increases the resistance of erythrocytes to mechanical trauma and hemolysis. It has angioprotective properties. It improves microcirculation.

It effectively inhibits free-radical lipid peroxidation of biomembranes and increases the activity of antioxidant enzymes. It stabilizes cytochrome P450 and has a detoxifying effect. In extreme situations accompanied by increased lipid peroxidation and hypoxia, it optimizes bioenergetic processes.

It increases the brain’s resistance to hypoxia and ischemia. In cases of cerebrovascular accidents (ischemic and hemorrhagic), it helps correct disorders of the peripheral nervous system function, facilitates the restoration of the brain’s integrative activity, and improves memory functions.

It dilates coronary vessels and reduces ischemic damage to the myocardium. In myocardial infarction, it limits the size of the necrosis focus, accelerates reparative processes, and promotes normalization of myocardial metabolism. It has a beneficial effect on the clinical course of myocardial infarction by reducing the incidence of acute heart failure. It promotes the regulation of the redox system in circulatory insufficiency.

It has retinoprotective properties, protects the retina from the damaging effects of high-intensity light, promotes the resorption of intraocular hemorrhages, and improves eye microcirculation.

Pharmacokinetics

After IV administration at a dose of 10 mg/kg, the T_1/2 is 18 min; total clearance is 0.2 L/min; V_d is 5.2 L. It quickly penetrates organs and tissues, where it is deposited and metabolized. Five metabolites of methylethylpiridinol have been identified, represented by dealkylated and conjugated products of its transformation. The metabolites of methylethylpiridinol are excreted by the kidneys. Significant amounts of 2-ethyl-6-methyl-3-hydroxypyridine phosphate are found in the liver.

After retrobulbar administration, Methylethylpiridinol appears in the blood almost instantly; its concentration decreases sharply during the first two hours, and after 24 hours, the active substance is absent from the blood. The concentration of methylethylpiridinol in eye tissues is higher than in blood serum.

Indications

Used as part of complex therapy.

For IM and IV administration: acute pancreatitis (during minimally invasive interventions under ultrasound control and laparoscopy); hemorrhagic stroke; ischemic stroke in the internal carotid artery basin and in the vertebrobasilar system; transient cerebrovascular accidents; chronic cerebrovascular insufficiency; traumatic brain injury accompanied by brain contusions; postoperative period in patients with traumatic brain injury operated on for epi-, subdural, and intracerebral hematomas combined with brain contusions; pre- and postoperative period in patients with arterial aneurysms and arteriovenous malformations of cerebral vessels; acute myocardial infarction, prevention of “reperfusion syndrome”; unstable angina.

For subconjunctival, parabulbar, or retrobulbar administration: subconjunctival and intraocular hemorrhage of various origins; retinopathy (including diabetic retinopathy); central and peripheral chorioretinal dystrophy; thrombosis of the central retinal vein and its branches; complications of myopia; angiosclerotic maculodystrophy (dry form); eye surgeries, condition after surgery for glaucoma with choroidal detachment; dystrophic diseases of the cornea; trauma, inflammation, and burn of the cornea; protection of the cornea (when wearing contact lenses) and retina from the effects of high-intensity light (laser and solar burns, during laser coagulation).

ICD codes

Dosage Regimen

Solution

Subconjunctivally, parabulbarly. If necessary, retrobulbar administration is possible.

Subconjunctivally, 0.2-0.5 ml (2-5 mg) is administered; parabulbarly, 0.5-1 ml (5-10 mg) of a 1% solution. The drug is used for 10-30 days once a day or every other day. If necessary, treatment can be repeated 2-3 times a year.

Retrobulbarly, 0.5-1 ml of the drug is administered for 10-15 days once a day.

To protect the retina during laser coagulation (especially laser coagulation that limits or destroys a tumor), 0.5-1.0 ml of Emsibel is administered parabulbarly or retrobulbarly 24 hours and 1 hour before the procedure and then for 2-10 days once a day.

Drops

Doses and duration of the treatment course are determined individually.

Instill 1-2 drops into the conjunctival sac 2-3 times a day. The duration of treatment is 3-30 days. If necessary and well tolerated, the course of treatment can be continued for up to 6 months or repeated 2-3 times a year.

Adverse Reactions

Possible agitation, drowsiness, increased blood pressure, reaction at the injection site (burning sensation along the vein, pain, itching).

Rarely headache, pain in the heart area; in persons with chronic pathology of the digestive organs – nausea, discomfort in the epigastric region; in case of predisposition to allergic reactions, the appearance of itching and redness of the skin is observed.

Local reactions: possible induration of paraorbital tissues.

Contraindications

Hypersensitivity; pregnancy, breastfeeding period; children and adolescents under 18 years of age.

With caution

For IV infusion: hemostasis disorders, during surgical operations, patients with symptoms of severe bleeding.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in elderly patients to avoid the risk of exacerbation of chronic diseases.

Special Precautions

During treatment, it is necessary to constantly monitor blood pressure and blood coagulability.

Effect on ability to drive vehicles and operate machinery

If drowsiness or changes in blood pressure occur after the use of methylethylpiridinol, patients should refrain from driving a car and other potentially hazardous activities. Should not be used while working by drivers of vehicles.

Drug Interactions

α-Tocopherol acetate potentiates the antioxidant effect of methylethylpiridinol.

Methylethylpiridinol is not recommended to be mixed with other injectable agents in the same syringe.

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.