Neurox, 50 mg/ml 2 ml 50 pcs

Ethylmethylhydroxypyridine succinate (EMHPS) is an inhibitor of free radical processes, membrane protector with antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic effects. It belongs to the class of 3-oxypyridines. The mechanism of action is due to the antioxidant and membrane-protective properties. It suppresses lipid peroxidation, increases superoxide dismutase activity, increases lipid-protein ratio, improves cell membrane structure and function. It modulates the activity of membrane-bound enzymes and receptor complexes, which promotes their binding to ligands, preserving the structural and functional organization of biomembranes and transport of neurotransmitters and improving synaptic transmission.

Enhances concentration of dopamine in the brain. Increases compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle in hypoxia with increasing levels of ADP and creatine phosphate, activates the energy-synthesizing function of mitochondria. Increases the body’s resistance to various damaging factors in pathological conditions (shock, hypoxia and ischemia, impaired cerebral circulation, intoxication with ethanol and antipsychotic drugs). It improves metabolism and blood supply of the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes blood cell membranes (erythrocytes and platelets), reducing the likelihood of hemolysis. It has hypolipidemic effect, reduces the content of total cholesterol and LDL.

Normalizes metabolic processes in ischemic myocardium, reduces the zone of necrosis, restores and/or improves myocardial electrical activity and contractility as well as increases coronary blood flow in the ischemic zone, increases antianginal activity of nitro preparations, reduces the consequences of reperfusion syndrome in acute coronary failure.

The stress-protective effect is manifested by the normalization of post-stress behavior, somatovegetative disorders, restoration of sleep-wake cycles, disturbed learning and memory processes, decrease of dystrophic changes in different brain structures.

The EMGPS has a pronounced anti-toxic effect in withdrawal syndrome, eliminates neurological and neurotoxic symptoms of acute alcohol intoxication, corrects behavioral and cognitive disorders. Under the influence of EMGPS the effects of tranquilizers, neuroleptics, antidepressants, hypnotics and anticonvulsants are strengthened, which allows to reduce their doses and side effects.

Pharmacokinetics

When administered by injection, the drug is determined in plasma for 4 hours after administration. T_max when administered in the m/m is 0.3-0.58 h. C_max when administered in the m/m dose of 400-500 mg is 2.5-4 µg/mL. EMGPS rapidly passes from the bloodstream to organs and tissues and is rapidly eliminated from the body. Average retention time of the drug in the body when administered by injection is 0.7-1.3 hours. The drug is metabolized in the liver by glucuronidation. It is rapidly excreted in the urine, mainly as metabolites (50% in 12 hours) and in a small amount unchanged (0.3% in 12 hours). It is most intensively excreted during the first 4 hours after drug administration. Indicators of urinary excretion of unchanged drug and metabolites have significant individual variability.

Indications

Active ingredient

Composition

Active substance:

Ethylmethylhydroxypyridine succinate 50 mg;

Auxiliary substances:

sodium disulfite, 1 mg;

water for injection, up to 1 ml;

How to take, the dosage

Intramuscularly or intravenously (by trickle or drip). When administering by infusion, the drug should be diluted in 0.9% sodium chloride solution.

Struly Neurox is administered slowly over 5-7 minutes, dripally at a rate of 40-60 drops per minute. The maximum daily dose should not exceed 1200 mg.

In case of acute impairment of cerebral circulation Neurox is used in combination therapy in the first 10-14 days – by IV drops 200-500 mg 2-4 times a day, then by IV drops 200-250 mg 2-3 times a day for 2 weeks.

In case of ChMT and consequences of ChMT, Neurox is used for 10-15 days by IV drip 200-500 mg 2-4 times daily.

In patients with dyscirculatory encephalopathy in decompensation phase Neurox should be administered by infusion or dropwise in dose 200-500 mg 1-2 times daily during 14 days. Thereafter, 100-250 mg/day v/m for the next 2 weeks.

For course prophylaxis of discirculatory encephalopathy Neurox is administered in a monthly dose of 200-250 mg 2 times a day for 10-14 days.

In cases of neurocirculatory dystonia, neurotic and neurosis-like conditions the drug is administered in 50-400 mg/day in the mum for 14 days.

In mild cognitive disorders in elderly patients and in patients with anxiety disorders the drug is used in/m in a dose of 100-300 mg/day for 14-30 days.

In acute myocardial infarction as part of complex therapy Neurox is administered by IV or IM within 14 days with traditional therapy of myocardial infarction (including nitrates, β-adrenoblockers, ACE inhibitors, thrombolytics, anticoagulant and antiplatelet agents and symptomatic agents as indicated). In the first 5 days Neurox is administered by IV, in the next 9 days the drug may be administered by IV/m. I/V drug administration is carried out by drop infusion (slowly) for 30-90 minutes (in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution, if necessary, slow trickle I/V drug administration of at least 5 minutes is possible. The drug is administered (v/v/m) 3 times a day, every 8 hours. The daily dose is 6-9 mg/kg, the single dose is 2-3 mg/kg. The maximum daily dose should not exceed 800 mg, a single dose 250 mg.

In open-angle glaucoma of various stages, Neurox is administered as part of complex therapy in 100-300 mg/day, 1-3 times a day for 14 days.

In case of withdrawal alcohol syndrome Neurox is administered by injection or intravenous drops in a dose of 200-500 mg 2-3 times a day for 5-7 days.

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

Interaction

It enhances the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), anti-Parkinsonian (levodopa) drugs, nitrates. Reduces the toxic effects of ethanol.

Contraindications

Side effects

When administered parenterally (especially by IV fluids): dryness, metallic taste in the mouth, sensation of heat spreading throughout the body, throat and chest discomfort, feeling of shortness of breath (usually associated with excessive speed of administration and of short duration).

In long-term use, nausea, flatulence, and sleep disturbance (drowsiness or trouble falling asleep).

Allergic reactions.

Overdose

Symptoms: sleep disturbance (insomnia, in some cases somnolence); when injected intravenously, slight and transient (up to 1.5-2 hours) increase in BP.

Treatment: usually not required – symptoms disappear on their own within 24 hours. In severe cases with insomnia – nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. In excessive rise in BP – hypotensive drugs under control of BP.

Similarities