Neurox, 50 mg / ml 2 ml, 10 pcs.

Active substance :

 ethylmethylhydroxypyridine succinate 50 mg;

Excipients:

 sodium disulfite - 1 mg;

water for injection - up to 1 ml;

Ethylmethylhydroxypyridine succinate (EMHPS) is an inhibitor of free radical processes, a membrane protector that has antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic effects. Belongs to the class of 3-hydroxypyridines. The mechanism of action is due to antioxidant and membrane-protective properties. Suppresses lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, improves the structure and function of the cell membrane.

Modulates the activity of membrane-bound enzymes, receptor complexes, which contributes to their binding to ligands, preservation of the structural and functional organization of biomembranes and transport of neurotransmitters, and improvement of synaptic transmission. Increases the concentration of dopamine in the brain. It enhances the compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in the level of ADP and creatine phosphate, activates the energy-synthesizing function of mitochondria.

Increases the body's resistance to the effects of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebrovascular accident, intoxication with ethanol and antipsychotic drugs). Improves metabolism and blood supply to the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membranes of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis. It has a hypolipidemic effect, reduces the content of total cholesterol and LDL.

It normalizes metabolic processes in the ischemic myocardium, reduces the area of ​​necrosis, restores and / or improves the electrical activity and contractility of the myocardium, and also increases the coronary blood flow in the ischemic area, increases the antianginal activity of nitro drugs, reduces the consequences of reperfusion syndrome in acute coronary insufficiency.

The stress-protective effect is manifested in the normalization of post-stress behavior, somatovegetative disorders, restoration of sleep-wakefulness cycles, impaired learning and memory processes, and a decrease in dystrophic changes in various structures of the brain.

EMHPS has a pronounced antitoxic effect in withdrawal symptoms, eliminates neurological and neurotoxic manifestations of acute alcohol intoxication, corrects behavioral and cognitive impairments. Under the influence of EMHPS, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects.

Pharmacokinetics

When administered intramuscularly, the drug is determined in blood plasma for 4 hours after administration. T _max with i / m administration - 0.3-0.58 h. C _max  with i / m administration at a dose of 400-500 mg - 2.5-4 μg / ml. EMHPS quickly passes from the bloodstream to organs and tissues and is quickly eliminated from the body. The average retention time of the drug in the body with intramuscular injection is 0.7-1.3 hours. It is metabolized in the liver by glucuronidation. It is quickly excreted in the urine, mainly in the form of 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 taking the drug. The rates of excretion in the urine of unchanged drug and metabolites have significant individual variability.

• acute disorders of cerebral circulation (as part of complex therapy);
• traumatic brain injury, the consequences of traumatic brain injury;
• encephalopathy;
• autonomic (neurocirculatory) dystonia syndrome;
• mild cognitive disorders of atherosclerotic genesis;
• anxiety disorders in neurotic and neurosis-like states;
• acute myocardial infarction (from the first day) as part of complex therapy;
• primary open-angle glaucoma of various stages, as part of complex therapy;
• relief of withdrawal symptoms in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;
• acute intoxication with antipsychotic drugs.

• increased individual sensitivity to the drug;
• acute renal failure;
• acute liver failure;
• pregnancy;
• breast-feeding;
• childhood.

With caution: history of allergic diseases and reactions, incl. hypersensitivity to sulfites.

With parenteral administration (especially intravenous jet): dryness, a metallic taste in the mouth, a feeling of spreading warmth throughout the body, sore throat and discomfort in the chest, a feeling of lack of air (as a rule, associated with an excessively high injection rate and are short-term character).

With prolonged use - nausea, flatulence, sleep disturbance (drowsiness or disturbed sleep).

Allergic reactions.

Strengthens the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. Reduces the toxic effects of ethanol.

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

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

In acute disorders of cerebral circulation, Neurox is used in complex therapy in the first 10-14 days - intravenous drip of 200-500 mg 2-4 times a day, then - 200-250 mg i / m 2-3 times a day within 2 weeks.

For TBI and the consequences of TBI, Neurox is used for 10-15 days intravenous drip, 200-500 mg 2-4 times a day.

In case of discirculatory encephalopathy in the decompensation phase, Neurox should be administered intravenously or by infusion at a dose of 200-500 mg 1-2 times a day for 14 days. Then - in / m at 100-250 mg / day for the next 2 weeks.

For course prevention of discirculatory encephalopathy, Neurox is administered intramuscularly at a dose of 200–250 mg 2 times a day for 10–14 days.

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

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

In acute myocardial infarction, as part of complex therapy, Neurox is administered intravenously or intramuscularly for 14 days, against the background of traditional therapy of myocardial infarction (including nitrates, β-blockers, ACE inhibitors, thrombolytics, anticoagulant and antiplatelet drugs, as well as symptomatic agents according to indications). In the first 5 days, Neurox is administered intravenously, in the next 9 days, the drug can be administered intramuscularly. Intravenous administration of the drug is performed by drip infusion (slowly) for 30–90 minutes (in 100–150 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution, if necessary, a slow jet intravenous administration of the drug is possible , lasting at least 5 minutes The introduction of the drug (i / v or i / m) is carried out 3 times a day, every 8 hours The daily dose is 6-9 mg / kg, a single dose - 2-3 mg / kg.

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

In case of alcohol withdrawal syndrome, Neurox is administered intramuscularly or intravenously at a dose of 200-500 mg 2-3 times a day for 5-7 days.

In case of acute intoxication with antipsychotic drugs, the drug is administered intravenously at a dose of 200–500 mg / day for 7–14 days.

Symptoms: sleep disturbance (insomnia, in some cases drowsiness); with the on / in the introduction - a slight and short-term (up to 1.5-2 hours) increase in blood pressure.

Treatment: As a rule, not required - symptoms disappear on their own within 24 hours. In severe cases of insomnia, nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. With an excessive increase in blood pressure - antihypertensive drugs under the control of blood pressure.

Solution for intravenous and intramuscular administration