Elfynat

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ELFUNAT (ELFUNAT)

Composition:

Active substance: ethylmethylhydroxypyridine succinate;

1 ml of solution contains ethylmethylhydroxypyridine succinate 50 mg;

Excipient: water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear colorless or slightly yellow solution.

Pharmacotherapeutic group.
Agents affecting the nervous system. ATC code N07X X.

Pharmacological Properties.

Pharmacodynamics.

Ethylmethylhydroxypyridine succinate is an inhibitor of free radical processes, exerting membrane-protective, anti-hypoxic, stress-protective, nootropic, anticonvulsant, and anxiolytic effects. It increases the organism's resistance to various damaging factors and to oxygen-dependent pathological conditions (shock, hypoxia, ischemia, cerebral circulation disorders, alcohol intoxication, and intoxication with antipsychotic agents (neuroleptics)).

The medicinal product Elfunat improves cerebral metabolism and cerebral blood supply, microcirculation, and rheological properties of blood, and reduces platelet aggregation. It stabilizes blood cell membrane structures (erythrocytes and platelets) during hemolysis. It exerts a hypolipidemic effect, reducing total cholesterol and low-density lipoprotein (LDL) levels. It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of Elfunat is due to its anti-hypoxic, antioxidant, and membrane-protective effects. It inhibits lipid peroxidation, increases superoxide dismutase activity, improves the lipid–protein ratio, reduces membrane viscosity, and increases membrane fluidity. It modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, gamma-aminobutyric acid (GABA), acetylcholine), thereby enhancing their ability to bind ligands, promoting preservation of the structural and functional organization of biomembranes, neurotransmitter transport, and improvement of synaptic transmission. It increases dopamine levels in the brain. It enhances compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions, resulting in increased adenosine triphosphate (ATP) and creatine phosphate levels, activation of mitochondrial energy-synthesizing functions, and stabilization of cellular membranes.

Elfunat normalizes metabolic processes in ischemic myocardium, reduces the necrotic area, restores and improves myocardial electrical activity and contractility, increases coronary blood flow in the ischemic zone, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency. It enhances the antianginal activity of nitro-compounds. It promotes preservation of retinal ganglion cells and optic nerve fibers in progressive neuropathy caused by chronic ischemia and hypoxia. It improves functional activity of the retina and optic nerve, increasing visual acuity.

Pharmacokinetics.

After intramuscular administration, the medicinal product Elfunat is detectable in blood plasma for up to 4 hours after administration. The time to reach maximum concentration is 0.45–0.5 hours. Maximum concentration at doses of 400–500 mg is 3.5–4.0 µg/mL. It rapidly distributes from the bloodstream into organs and tissues and is rapidly eliminated from the body. It is excreted primarily in urine, mainly as glucuronide conjugates, and to a minor extent unchanged.

Clinical characteristics.

Indications.

• Acute cerebrovascular disorders;
• Traumatic brain injury, consequences of traumatic brain injury;
• Dyscirculatory encephalopathy;
• Neurocirculatory dystonia;
• Mild cognitive impairments of atherosclerotic origin;
• Anxiety disorders in neurotic and neurosis-like conditions;
• Acute myocardial infarction (from the first day), as part of complex therapy;
• Primary open-angle glaucoma at various stages, as part of complex therapy;
• Management of alcohol withdrawal syndrome with predominant neurosis-like and neurocirculatory disturbances;
• Acute intoxication with antipsychotic agents;
• Acute purulent-inflammatory processes in the abdominal cavity (acute necrotic pancreatitis, peritonitis), as part of complex therapy.

Contraindications.

• Hypersensitivity to the active substance and/or to excipients of the medicinal product Elfunat.
• Acute hepatic or renal failure.
• Pregnancy.
• Breast-feeding period.
• Childhood.

Interaction with other medicinal products and other forms of interactions.

When used concomitantly, the medicinal product enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), anti-Parkinson agents (levodopa), and reduces the toxic effect of ethanol.

Special precautions for use.

The extent of restrictions is determined by individual intolerance to the medicinal product Elfunat.

Use during pregnancy or breastfeeding.

Controlled clinical safety studies have not been conducted; therefore, the medicinal product Elfunat is contraindicated during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

The medicinal product Elfunat should be used with caution when driving or operating machinery, taking into account the possibility of adverse reactions that may affect reaction speed and the ability to concentrate.

Method of Administration and Dosage

Method of Administration

The medicinal product Elfunat is intended for intramuscular or intravenous (bolus, infusion) administration.

When administered by infusion, the medicinal product Elfunat should be diluted in 0.9% sodium chloride solution.

The bolus injection of Elfunat should be administered slowly over 5–7 minutes; for infusion, the rate should be 40–60 drops per minute.

The maximum daily dose must not exceed 1200 mg.

Dosage

Acute Cerebrovascular Disorders

Elfunat should be administered intravenously by infusion at a dose of 200–500 mg 2–4 times daily for the first 10–14 days, followed by intramuscular administration at a dose of 200–250 mg 2–3 times daily for the subsequent 14 days.

Traumatic Brain Injury, Consequences of Traumatic Brain Injury

Elfunat should be administered intravenously by infusion at a dose of 200–500 mg 2–4 times daily for 10–15 days.

Disirculatory Encephalopathy

Decompensation phase – Elfunat should be administered intravenously either as a bolus or by infusion at a dose of 200–500 mg 1–2 times daily for the first 14 days, followed by intramuscular administration at a dose of 100–250 mg daily for the next 14 days.

Course prophylaxis – Elfunat should be administered intramuscularly at a dose of 200–250 mg twice daily for 10–14 days.

Mild Cognitive Impairment in Elderly Patients and Anxiety States

Elfunat should be administered intramuscularly at a dose of 100–300 mg daily for 14–30 days.

Acute Myocardial Infarction, as part of combination therapy

Elfunat should be administered intravenously or intramuscularly for 14 days, alongside conventional myocardial infarction therapy, including nitrates, beta-adrenoblockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulant and antiplatelet agents, as well as symptomatic treatments as indicated.

For the first 5 days, intravenous administration is recommended to achieve maximum effect; intramuscular administration may be used for the following 9 days. Intravenous administration should be performed as a slow infusion (to avoid adverse reactions) in 0.9% sodium chloride solution or 5% dextrose (glucose) solution, in a volume of 100–150 ml over 30–90 minutes. If necessary, slow bolus injection may be used, administered over no less than 5 minutes.

Elfunat should be administered (intravenously or intramuscularly) 3 times daily, every 8 hours. The daily therapeutic dose is 6–9 mg/kg body weight/day; the single dose is 2–3 mg/kg body weight. The maximum daily dose must not exceed 800 mg; the maximum single dose must not exceed 250 mg.

Open-Angle Glaucoma at Various Stages, as part of combination therapy

Elfunat should be administered intramuscularly at a dose of 100–300 mg 1–3 times daily for 14 days.

Alcohol Withdrawal Syndrome

Elfunat should be administered intravenously by infusion or intramuscularly at a dose of 200–500 mg 2–3 times daily for 5–7 days.

Acute Intoxication with Antipsychotic Agents

Elfunat should be administered intravenously at a dose of 200–500 mg daily for 7–14 days.

Acute Purulent-Inflammatory Processes in the Abdominal Cavity (Acute Necrotizing Pancreatitis, Peritonitis), as part of combination therapy

In acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis), Elfunat should be administered on the first day both preoperatively and postoperatively. Dosage depends on the form and severity of the disease, extent of the process, and clinical course. Discontinuation of Elfunat should be gradual and only after a sustained positive clinical and laboratory response.

Acute edematous (interstitial) pancreatitis – Elfunat should be administered intravenously by infusion (in isotonic sodium chloride solution) and intramuscularly at a dose of 200–500 mg 3 times daily.

Mild course of necrotizing pancreatitis – Elfunat should be administered intravenously by infusion (in isotonic sodium chloride solution) and intramuscularly at a dose of 100–200 mg 3 times daily.

Moderate severity course of necrotizing pancreatitis – Elfunat should be administered intravenously by infusion (in isotonic sodium chloride solution) and intramuscularly at a dose of 200 mg 3 times daily.

Severe course of necrotizing pancreatitis – Elfunat should be administered using pulse dosing: 800 mg on the first day, given in two doses; thereafter, 200–500 mg twice daily, with gradual reduction of the daily dose.

Very severe course of necrotizing pancreatitis – Elfunat should be administered intravenously by infusion (in isotonic sodium chloride solution) at an initial dose of 800 mg daily until sustained resolution of pancreatogenic shock symptoms; after stabilization of the patient's condition, the dose should be reduced to 300–500 mg twice daily.

Children

Well-controlled clinical studies on the safety of Elfunat in children have not been conducted; therefore, Elfunat is contraindicated in this patient population.

Overdose

Symptoms: drowsiness, insomnia.

Treatment of Overdose

Due to the low toxicity of the drug, overdose is unlikely. Treatment is generally not required, and symptoms resolve spontaneously within several days. In cases of pronounced overdose symptoms, symptomatic and supportive therapy should be administered.

Adverse reactions.

To avoid the development of adverse reactions, the dosage regimen and rate of administration of the medicinal product Elfunat should be strictly followed.

Criteria for assessing the frequency of adverse reactions: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1,000 to < 1/100); rare (≥ 1/10,000 to < 1/1,000); very rare (< 1/10,000); not known (cannot be estimated from the available data).

Immune system disorders:

very rare – anaphylactic shock, angioedema, urticaria.

Psychiatric disorders:

very rare – drowsiness.

Nervous system disorders:

very rare – headache, dizziness (which may be related to too rapid administration and is transient).

Vascular disorders:

very rare – decreased blood pressure, increased blood pressure (which may be related to too rapid administration and is transient).

Respiratory, thoracic and mediastinal disorders:

very rare – dry cough, throat irritation, chest discomfort, dyspnea (which may be related to too rapid administration and is transient).

Gastrointestinal disorders:

very rare – dry mouth, nausea, unpleasant odor sensation, metallic taste in the mouth.

Skin and subcutaneous tissue disorders:

very rare – itching, rash, urticaria.

General disorders and administration site conditions:

very rare – sensation of warmth.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after the medicine has been authorized is important. It allows continuous monitoring of the benefit-risk balance of the medicine. Healthcare professionals should report any suspected adverse reactions via the national pharmacovigilance system.

Shelf life.

3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C. Keep out of the reach of children.

Packaging.

5 ampoules (2 ml in each ampoule) in a blist er pack, 2 blisters per cardboard box;

5 ampoules (5 ml in each ampoule) in a blister pack, 1 blister per cardboard box.

Prescription status.

Prescription-only.

Manufacturer.

UORL D MEDICIN E ILAC SAN. VE TIC. A.S.H./

WORLD MEDICINE ILAC SAN. VE TIC. A.S.

Manufacturer's address and location of operations.

COSB G.O.Pasa Mah. 6. Cad. No:30, Cerkezkoy/Tekirdag, Turkey.

Marketing Authorization Holder.

LLC "WORLD MEDICINE", Ukraine/

WORLD MEDICINE, LLC, Ukraine.