Neurox^® (Tablets, Solution) Instructions for Use

ATC Code

N07XX (Other drugs for the treatment of nervous system diseases)

Active Substance

Ethylmethylhydroxypyridine succinate

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

Mechanism of action, pharmacodynamic effects

It has antihypoxic, membrane-protective, nootropic, anticonvulsant, and anxiolytic effects, and increases the body’s resistance to stress.

The drug increases the body’s resistance to the effects of major damaging factors and to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular accident, intoxication with alcohol and antipsychotic drugs).

Neurox^® improves cerebral metabolism and blood supply to the brain, improves microcirculation and the rheological properties of blood, and reduces platelet aggregation.

It stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis. It has a hypolipidemic effect, reducing the level of total cholesterol and LDL.

It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of Neurox^® is due to its antihypoxant, antioxidant, and membrane-protective effects.

It inhibits lipid peroxidation processes, increases superoxide dismutase activity, increases the lipid-protein ratio, reduces membrane viscosity, and increases its fluidity.

It modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, neurotransmitter transport, and improves synaptic transmission.

Neurox^® increases the dopamine content in the brain.

It causes an increase in the compensatory activity of aerobic glycolysis and a reduction in the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in the content of ATP, creatine phosphate and activation of the energy-synthesizing functions of mitochondria, and stabilization of cell membranes.

Neurox^® normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemia zone, reducing the consequences of reperfusion syndrome in acute coronary insufficiency.

It increases the antianginal activity of nitro drugs.

Neurox^® helps preserve retinal ganglion cells and optic nerve fibers in progressive neuropathy, the causes of which are chronic ischemia and hypoxia.

It improves the functional activity of the retina and optic nerve, increasing visual acuity.

Pharmacokinetics

Absorption and Distribution

After intramuscular administration, the drug is detected in blood plasma for 4 hours after administration. T_max is 0.45-0.5 hours. When administered at a dose of 400-500 mg, C_max is 3.5-4 µg/ml.

Ethylmethylhydroxypyridine succinate quickly passes from the bloodstream into organs and tissues and is rapidly eliminated from the body. The mean residence time (MRT) of the drug is 0.7-1.3 hours.

Metabolism and Excretion

The drug is excreted mainly in the urine, primarily in glucuronoconjugated form and in small amounts unchanged.

Indications

• Acute cerebrovascular accidents (as part of combination therapy);
• Traumatic brain injury, consequences of traumatic brain injuries;
• Dyscirculatory encephalopathy;
• Autonomic (neurocirculatory) dystonia syndrome;
• Mild cognitive disorders of atherosclerotic origin;
• Anxiety disorders in neurotic and neurosis-like states;
• Acute myocardial infarction (from the first days) (as part of combination therapy);
• Primary open-angle glaucoma of various stages (as part of combination therapy);
• Relief of withdrawal syndrome in alcoholism with a predominance of neurosis-like and autonomic-vascular disorders;
• Acute intoxication with antipsychotic drugs;
• Acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) as part of combination therapy.

ICD codes

Dosage Regimen

Tablets

Administered orally, 125-250 mg 3 times/day.

Initial dose – 125-250 mg (1-2 tablets) 1-2 times/day with a gradual increase until a therapeutic effect is achieved; maximum daily dose – 800 mg.

Duration of treatment – 2-6 weeks; for relief of alcohol withdrawal – 5-7 days. Treatment is discontinued gradually, reducing the dose over 2-3 days.

The duration of the course of therapy in patients with coronary artery disease is at least 1.5-2 months. Repeated courses (as recommended by a doctor) are preferably carried out in the spring and autumn periods.

Solution

Intramuscularly or intravenously (bolus or drip).

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

Neurox^® is administered by slow bolus injection over 5-7 minutes, by drip – at a rate of 40-60 drops/min.

The maximum daily dose should not exceed 1200 mg.

For acute cerebrovascular accidents, Neurox^® is used in combination therapy in the first 10-14 days – IV drip, 200-500 mg 2-4 times/day, then – IM, 200-250 mg 2-3 times/day for 2 weeks.

For traumatic brain injury and consequences of traumatic brain injuries, Neurox^® is used for 10-15 days IV drip, 200-500 mg 2-4 times/day.

For dyscirculatory encephalopathy in the decompensation phase, Neurox^® should be prescribed IV bolus or drip at a dose of 200-500 mg 1-2 times/day for 14 days. Then – IM, 100-250 mg/day for the next 2 weeks.

For course prevention of dyscirculatory encephalopathy, Neurox^® is administered IM at a dose of 200-250 mg 2 times/day for 10-14 days.

For neurocirculatory dystonia, neurotic and neurosis-like states, the drug is administered IM at 50-400 mg/day for 14 days.

For mild cognitive impairments in elderly patients and for anxiety disorders, the drug is used IM at a dose of 100-300 mg/day for 14-30 days.

For acute myocardial infarction as part of combination therapy, Neurox^® is administered IV or IM for 14 days, against the background of traditional therapy for myocardial infarction (including nitrates, beta-blockers, ACE inhibitors, thrombolytics, anticoagulant and antiplatelet drugs, as well as symptomatic agents as indicated). In the first 5 days, Neurox^® is administered IV; in the subsequent 9 days, the drug can be administered IM.

IV administration of the drug is performed by drip infusion, slowly (to avoid side effects), over 30-90 minutes (in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution), if necessary, slow IV bolus administration of the drug is possible, lasting at least 5 minutes.

Administration of the drug (IV or IM) is carried out 3 times/day, every 8 hours. The daily dose is 6-9 mg/kg of body weight, a single dose is 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose – 250 mg.

For open-angle glaucoma of various stages as part of combination therapy, Neurox^® is administered IM at 100-300 mg/day, 1-3 times/day for 14 days.

For alcohol withdrawal syndrome, Neurox^® is administered IM or IV drip at a dose of 200-500 mg 2-3 times/day for 5-7 days.

For acute intoxication with antipsychotic drugs, the drug is administered IV at a dose of 200-500 mg/day for 7-14 days.

For acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis), Neurox^® is prescribed on the first day, both in the pre-operative and post-operative periods. The administered doses depend on the form and severity of the disease, the prevalence of the process, and the variants of the clinical course. Discontinuation of the drug should be gradual only after a stable positive clinical and laboratory effect.

For acute edematous (interstitial) pancreatitis, Neurox^® is prescribed at 200-500 mg 3 times/day, IV drip (in 0.9% sodium chloride solution) and IM. Mild severity of necrotizing pancreatitis – 100-200 mg 3 times/day drip (in 0.9% sodium chloride solution) and IM. Moderate severity – 200 mg 3 times/day, IV drip (in 0.9% sodium chloride solution). Severe course – in a pulse dose of 800 mg on the first day, with a twice-daily administration regimen; then 200-500 mg 2 times/day with a gradual reduction in the daily dose. Extremely severe course – at an initial dose of 800 mg/day until persistent relief of manifestations of pancreatogenic shock, after stabilization of the condition – 300-500 mg 2 times/day IV drip (in 0.9% sodium chloride solution) with a gradual reduction in the daily dose.

Adverse Reactions

To avoid the occurrence of side effects, it is recommended to follow the dosing regimen and the rate of administration of the drug.

The frequency of adverse effects was determined in accordance with the WHO classification: very common (≥10%); common (≥1%, but <10%); uncommon (≥0.1%, but <1%); rare (≥0.01%, but <0.1%); very rare (<0.01%); frequency not known (frequency 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 (may be associated with an excessively high rate of administration and is short-term).

Vascular disorders very rare – decreased blood pressure, increased blood pressure (may be associated with an excessively high rate of administration and is short-term).

Respiratory, thoracic and mediastinal disorders very rare – dry cough, sore throat, chest discomfort, difficulty breathing (may be associated with an excessively high rate of administration and is short-term).

Gastrointestinal disorders very rare – dry mouth, nausea, unpleasant smell sensation, metallic taste in the mouth.

Skin and subcutaneous tissue disorders very rare – itching, rash, hyperemia.

General disorders and administration site conditions very rare – feeling of warmth.

Contraindications

• Hypersensitivity to ethylmethylhydroxypyridine succinate or to any of the excipients;
• Acute renal failure;
• Acute hepatic failure;
• Pregnancy;
• Breastfeeding period;
• Childhood (due to insufficient study of the drug’s action).

With caution

In some cases, especially in predisposed patients with bronchial asthma with increased sensitivity to sulfites, the development of severe hypersensitivity reactions and bronchospasm is possible.

Use in Pregnancy and Lactation

The use of the drug during pregnancy and breastfeeding is contraindicated.

Use in Hepatic Impairment

Contraindicated in acute hepatic failure.

Use in Renal Impairment

Contraindicated in acute renal failure.

Pediatric Use

Contraindicated in children.

Special Precautions

Effect on ability to drive vehicles and operate machinery

During the drug intake, patients should exercise caution when engaging in activities requiring rapid psychophysical reactions (including driving vehicles, operating machinery).

Overdose

Due to low toxicity, overdose is unlikely.

Symptoms drowsiness, insomnia.

Treatment as a rule, not required, symptoms disappear on their own within 24 hours. In case of pronounced manifestations, supportive symptomatic treatment is carried out.

Drug Interactions

Enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), and antiparkinsonian (levodopa) drugs.

Reduces the toxic effects of ethanol.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 5 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

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.