Elfynat

INSTRUCTION for medical use of the medicinal product ELPHUNAT (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: transparent, colorless or slightly yellowish 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 enhances the organism's resistance to various damaging factors and to oxygen-dependent pathological conditions (shock, hypoxia, ischemia, cerebrovascular disorders, alcohol intoxication, and intoxication with antipsychotic agents (neuroleptics)).

The medicinal product Elfunat improves cerebral metabolism and cerebral blood supply, microcirculation, and the rheological properties of blood, and reduces platelet aggregation. It stabilizes blood cell membrane structures (erythrocytes and platelets) during hemolysis. Elfunat 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 improving synaptic transmission. It increases dopamine levels in the brain. It enhances compensatory activation of aerobic glycolysis and reduces the degree of suppression of oxidative processes in the Krebs cycle under hypoxic conditions, leading to increased levels of adenosine triphosphate (ATP) and creatine phosphate, 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 nitrate preparations. 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. 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. The drug rapidly transfers from the bloodstream into organs and tissues and is rapidly eliminated from the body. It is excreted in the urine, primarily in glucuronide-conjugated form, and in insignificant amounts in unchanged form.

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 neurasthenia-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 predominance of neurasthenia-like and neurocirculatory disturbances;
• acute intoxication with antipsychotic agents;
• acute suppurative-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.
• Breastfeeding period.
• Childhood.

Interaction with other medicinal products and other forms of interactions.

When used concomitantly, the medicinal product Elfunat enhances the effects 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.

Well-controlled clinical safety studies have not been conducted; therefore, the medicinal product Elfunat is contraindicated during pregnancy and breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

Elfunat should be used with caution when driving or operating machinery, due to the potential for 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 physiological saline (sodium chloride solution).

For bolus administration, Elfunat should be administered slowly over 5–7 minutes; for infusion, at a rate of 40–60 drops per minute.

The maximum daily dose should not exceed 1200 mg.

Dosage

Acute cerebrovascular disorders

Administer Elfunat 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

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

Discirculatory encephalopathy

Decompensation phase – administer Elfunat intravenously either by bolus or 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 – administer Elfunat intramuscularly at a dose of 200–250 mg twice daily for 10–14 days.

Mild cognitive impairment in elderly patients and anxiety states

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

Acute myocardial infarction, as part of combination therapy

Administer Elfunat 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 maximum effect during the first 5 days, intravenous administration is recommended; intramuscular administration may be used during 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 administration over at least 5 minutes may be used.

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 should not exceed 800 mg; the maximum single dose should not exceed 250 mg.

Open-angle glaucoma at various stages, as part of combination therapy

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

Alcohol withdrawal syndrome

Administer Elfunat 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

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

Acute purulent-inflammatory processes in the abdominal cavity (acute necrotic pancreatitis, peritonitis), as part of combination therapy

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

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

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

Moderate severity of necrotic pancreatitis – administer Elfunat intravenously by infusion (in isotonic sodium chloride solution) and intramuscularly at a dose of 200 mg 3 times daily.

Severe course of necrotic pancreatitis – administer Elfunat in 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 necrotic pancreatitis – administer Elfunat intravenously by infusion (in isotonic sodium chloride solution) at an initial dose of 800 mg daily until sustained control of pancreatogenic shock symptoms; after stabilization of the patient’s condition, administer 300–500 mg twice daily.

Children

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:

Due to the low toxicity of the drug, overdose is unlikely. Usually, no treatment is 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 must 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 available data).

Immune system disorders:

very rare – anaphylactic shock, angioneurotic edema, 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, breathing difficulty (which may be related to too rapid administration and is transient).

Gastrointestinal disorders:

very rare – dry mouth, nausea, unpleasant taste 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 of suspected adverse reactions after marketing authorization is very important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions through the national pharmacovigilance system.

Shelf life.

3 years.

Storage conditions.

Store at temperatures not exceeding 25 ºC, in a place inaccessible to children.

Packaging.

2 ml in vials, 10 units (5×2) in blister packs, in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

K.O. Rompharm Company S.R.L., Romania.

S.C. Rompharm Company S.R.L., Romania.

Manufacturer's address and location of operations.

Otopeni city, Eroilor str. № 1A, 075100, jud. Ilfov.

Otopeni сіty, Eroilor str. № 1A, 075100, jud. Ilfov.

Marketing authorization holder.

WORLD MEDICINE LLC, Ukraine.

WORLD MEDICINE LLC.