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General characteristics. Structure:

Active agent of ethylmethylhydroxypyridine succinate – 100 mg;
1 ampoule (5 ml) contains in quality of active agent of ethylmethylhydroxypyridine succinate – 250 mg;
1 ampoule (10 ml) contains in quality of active agent of ethylmethylhydroxypyridine succinate – 500 mg;
1 ampoule (20 ml) contains in quality of active agent of ethylmethylhydroxypyridine succinate – 1000 mg;
excipients: sodium disulphite, water for injections.

Description: colourless or slightly yellowish transparent liquid.

Pharmacological properties:

Pharmakodinanika. Etilmetilgidroksipiridina succinate (EMGPS) is the inhibitor of free radical processes, a membranoprotektor possessing anti-hypoxemic, stressprotektivny, nootropic, anticonvulsant and anxiolytic action. Belongs to the class 3 of oxypyridines. The mechanism of action is caused antioxidant and membranoprotektorny by properties. Suppresses peroxide oxidation of lipids, increases activity of a superoksidoksidaza, the lipid protein raises a ratio, improves structure and function of a membrane of cells. Modulates activity of membrane-bound enzymes, receptor complexes that promotes their linkng with ligands, preservation of the structurally functional organization of biomembranes, transport of neurotransmitters and improvement of synoptic transfer. Increases concentration in a dopamine brain. Strengthens compensatory activation of aerobic glycolysis and reduces extent of oppression of oxidizing processes in a tricarbonic acid cycle in the conditions of a hypoxia with increase in adenosine triphosphoric acid and creatine phosphate, activates the power synthesizing function of mitochondrions. Increases resistance of an organism to influence of various disturbing factors at morbid conditions (shock, a hypoxia and ischemia, disturbances of cerebral circulation, intoxication ethanol and antipsychotic medicines). Improves metabolism and blood supply of a brain, microcirculation and rheological properties of blood, reduces aggregation of thrombocytes. Stabilizes membranes of blood cells (erythrocytes and thrombocytes), reducing probability of development of hemolysis. Possesses hypolipidemic action, reduces the content of the general cholesterol and lipoproteins of low density.

Normalizes metabolic processes in an ischemic myocardium, reduces a necrosis zone, recovers and/or improves electric activity and contractility of a myocardium, and also increases a coronary blood stream in an ischemia zone, increases anti-anginal activity of nitrodrugs, reduces effects of a reperfusion syndrome at acute coronary insufficiency.

Stressoprotektorny action is shown in normalization of post-stressful behavior, somatovegetativny disturbances, recovery of the cycles "dream wakefulness", the broken processes of training and memory, decrease in dystrophic changes in various structures of a brain.

Etilmetilgidroksipiridina succinate possesses the expressed anti-toxic action at an abstinence syndrome, eliminates neurologic and neurotoxic manifestations of an acute drunkenness, adjusts behavioural and cognitive disturbances. Under the influence of ethylmethylhydroxypyridine of succinate action tranquilizing, antipsychotic, antidepressive, somnolent and anticonvulsants amplifies that allows to lower their doses and to reduce side effects.

Pharmacokinetics. At intramuscular introduction drug is defined in a blood plasma for 4 h after introduction. Time of achievement of the maximum concentration at intramuscular introduction – 0,3-0,58 h. The maximum concentration at intramuscular introduction in a dose of 400-500 mg – 2,5-4 mkg/ml. Etilmetilgidroksipiridina quickly passes succinate from a circulatory bed into bodies and fabrics and is quickly brought from an organism. The average time of deduction of drug in an organism at intramuscular introduction – 0,7-1,3 h. It is metabolized in a liver by a glyukuronirovaniye. It is quickly removed with urine generally in the form of metabolites (50% for 12 h) and in insignificant quantity - in not changed look (0,3% for 12 h). It is most intensively removed during the first 4 h after administration of drug. Removal indicators with urine of not changed drug and metabolites have considerable individual variability.

It is metabolized in a liver by a glyukuronirovaniye. It is quickly removed with urine generally in the form of metabolites (50% for 12 h) and in insignificant quantity - in an invariable look (0,3% for 12 h). It is most intensively removed during the first 4 h after administration of drug. Removal indicators with urine of invariable drug and metabolites have considerable individual variability.

Indications to use:

- Acute disorders of cerebral circulation (as a part of complex therapy);
- distsirkulyatorny encephalopathy;
- neurocirculatory dystonia;
- easy cognitive disorders of atherosclerotic genesis;
- alarming states at neurotic and neurosis-like states;
- an abstinence syndrome at alcoholism with dominance of neurosis-like and vegetovascular frustration;
- acute intoxication antipsychotic medicines.

Route of administration and doses:

Intramusculary or intravenously (struyno or kapelno). At an infusional way of introduction drug should be dissolved in 0,9% chloride sodium solution.

Doses select individually. Begin treatment with a dose of 50-100 mg 1–3 times a day, gradually raising it to obtaining therapeutic effect.

Struyno Neyroks is entered slowly within 5–7 min., kapelno - with a speed of 40-60 thaws a minute. The maximum daily dose should not exceed 800 mg.

At acute disorders of cerebral circulation of Neyroks apply in complex therapy in the first 2–4 days - intravenously kapelno 200–300 mg of 1 times a day, then - intramusculary on 100 mg 3 times a day. Duration of treatment makes 10-14 days.

At distsirkulyatorny encephalopathy in a phase of a decompensation of Neyroks it is necessary to appoint intravenously struyno or kapelno in a dose of 100 mg 2–3 times a day for 14 days. Then - intramusculary on 100 mg/days for the next 2 weeks.

For course prevention of distsirkulyatorny encephalopathy the drug is administered intramusculary in a dose of 100 mg by 2 times a day for 10–14 days.

At neurocirculatory dystonia, neurotic and neurosis-like states the drug is administered intramusculary on 50-400 mg a day within 14 days.

At an abstinence alcoholic syndrome of Neyroks 2–3 times a day or intravenously kapelno 1–2 times a day within 5–7 days enter intramusculary in a dose 100–200 mg.

At acute intoxication antipsychotic medicines the drug is administered intravenously in a dose of 50-300 mg/days for 7–14 days.

At easy cognitive disturbances at patients of advanced age and at alarming frustration drug is used intramusculary in a daily dose of 100-300 mg/days for 14–30 days.

Features of use:

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding concentration of attention and speed of psychomotor reactions.

Side effects:

At parenteral administration (especially intravenous jet): dryness, "metal" smack in a mouth, feelings of "the spreading heat" in all body, an unpleasant smell, irritation in a throat and discomfort in a thorax, feeling of shortage of air (as a rule, are connected with excessively high rate of administering and have short-term character).

At prolonged use – nausea, a meteorism, sleep disorders (drowsiness or disturbance of backfilling).

Allergic reactions.

Interaction with other medicines:

Strengthens effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), protivoparkinsonichesky (levodopa) medicines, nitrates. Reduces toxic effects of ethanol.

Contraindications:

- The increased individual sensitivity to drug;
- acute renal failure;
- acute liver failure;
- pregnancy;
- breastfeeding;
- children's age.

With care: allergic diseases and reactions in the anamnesis.

Overdose:

Symptoms: sleep disorder (sleeplessness, in certain cases drowsiness); at intravenous administration – insignificant and short-term (to 1,5 – 2 h) increase in arterial pressure.

Treatment: as a rule, it is not required – symptoms disappear independently within a day. In hard cases at sleeplessness – nitrazepam of 10 mg, oxazepam of 10 mg or diazepam of 5 mg. At excessive increase in arterial pressure – hypotensive medicines under control of arterial pressure.

Storage conditions:

List B. In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules of light-protective glass with a color ring of a break or with a color point and a notch. One, two or three color rings and/or a two-dimensional barcode, and/or the alphanumeric coding or without additional color rings, a two-dimensional barcode, the alphanumeric coding in addition apply on ampoules. On 5 ampoules in a blister strip packaging.

On 1, 2, 4 or 10 planimetric packagings together with the application instruction in a pack from a cardboard.

On 5 ml in ampoules of light-protective glass with a color ring of a break or with a color point and a notch. One, two or three color rings and/or a two-dimensional barcode, and/or the alphanumeric coding or without additional color rings, a two-dimensional barcode, the alphanumeric coding in addition apply on ampoules. On 5 ampoules in a blister strip packaging.

On 1, 2, 4 blister strip packagings together with the application instruction in a pack from a cardboard.

On 10 ml or 20 ml in ampoules of light-protective glass with a color ring of a break or with a color point and a notch. One, two or three color rings and/or a two-dimensional barcode, and/or the alphanumeric coding or without additional color rings, a two-dimensional barcode, the alphanumeric coding in addition apply on ampoules. On 1 ampoule in a blister strip packaging. On 1 blister strip packaging together with the application instruction in a pack from a cardboard.