Neurox, 125 mg 50 pcs.

Pharmacotherapeutic group: antioxidant.
ATX code: N07XX
Pharmacological properties

Pharmacodynamics

Ethylmethylhydroxypyridine succinate is an inhibitor of free radical processes, membranoprotector with antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic action. Ethylmethylhydroxypyridine succinate increases resistance of the body to various damaging factors (shock, hypoxia and ischemia, disorders of cerebral circulation, intoxication by alcohol and antipsychotic drugs (neuroleptics)).

The mechanism of action of ethylmethylhydroxypyridine succinate is due to its antioxidant, antihypoxant and membrane-protective action. It inhibits lipid peroxidation, increases superoxide dismutase activity, increases the lipid-protein ratio, reduces membrane viscosity, increases its

fluidity. Ethylmethylhydroxypyridine succinate modulates the activity of membrane-bound enzymes (calcium independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, gamma-aminobutyric acid, acetylcholine), which increases their binding ability to ligands, helps to maintain the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission.

Ethylmethylhydroxypyridine succinate increases the content of dopamine in the brain. It causes enhancement of compensatory activation of aerobic glycolysis and reduction of the degree of inhibition of oxidative processes in the Krebs cycle under hypoxia with increase of adenosine triphosphate and creatine phosphate, activation of energy-synthesizing functions of mitochondria and stabilization of cell membranes.

It improves metabolism and blood supply of the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes membrane structures of blood cells (erythrocytes and platelets) in hemolysis. It has hypolipidemic effect, reduces the content of total cholesterol and low-density lipoproteins.

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

Ethylmethylhydroxypyridine succinate has a pronounced anti-toxic effect in withdrawal syndrome. It eliminates neurological and neurotoxic symptoms of acute alcohol intoxication, restores behavioral disorders, vegetative functions and is also able to relieve cognitive disorders caused by prolonged use of ethanol and its withdrawal. Under the influence of ethylmethylhydroxypyridine succinate the effect of tranquilizing, neuroleptic, antidepressant, hypnotic and anticonvulsant drugs is increased, which allows reducing their doses and side effects.

Ethylmethylhydroxypyridine succinate improves functional state of ischemic myocardium. In conditions of coronary insufficiency it increases collateral blood supply of ischemic myocardium, promotes preservation of integrity of cardiomyocytes and maintenance of their functional activity. Effectively restores myocardial contractility in reversible cardiac dysfunction.

Pharmacokinetics

It is rapidly absorbed when taken orally. Maximum concentration at doses of 400-500 mg is 3.5-4.0 µg/ml. It is rapidly distributed in the organs and tissues. Average retention time of the drug in the body when administered orally is 4.9-5.2 h. It is metabolized in the liver through glucuron conjugation.

Five metabolites have been identified: 3-oxypyridine phosphate – is formed in the liver and with the participation of alkaline phosphatase breaks down into phosphoric acid and 3-oxypyridine; the 2nd metabolite – pharmacologically active, is formed in large amounts and is found in the urine 1-2 days after administration; the 3rd is excreted in large amounts with the urine; the 4th and 5th are glucuronconjugates. T1/2 when administered orally is 2.0-2.6 h.

It is rapidly excreted in the urine mainly as metabolites and in insignificant amounts unchanged. It is excreted most intensively during the first 4 hours after drug administration. Indices of urinary excretion of unchanged drug and metabolites have individual variability.

Indications

• After-effects of acute cerebral circulation disorders, including after transient ischemic attacks, in the phase of subcompensation as a preventive course;
• light craniocerebral trauma, consequences of craniocerebral injuries;
• .encephalopathies of various genesis (discirculatory, dysmetabolic, post-traumatic, mixed);
• dietary dystonia syndrome;
• mild cognitive disorders of atherosclerotic genesis;
• anxiety disorders in neurotic and neurosis-like states;
• ischemic heart disease as a part of complex therapy;
• curing withdrawal syndrome in alcoholism with the prevalence of neurotic and vegetative-vascular disorders, postabstinence disorders;
• during withdrawal from alcoholismconditions after acute intoxication with antipsychotic agents;
• asthenic conditions and for the prevention of the development of somatic diseases under the influence of extreme factors and loads;
• impact of extreme (stress) factors.

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Active ingredient

Ethylmethylhydroxypyridine succinate

Composition

Active ingredient: Ethylmethylhydroxypyridine succinate – 125 mg.

Auxiliary substances: lactose monohydrate, microcrystalline cellulose 102, potato starch, povidone-K90, croscarmellose sodium, magnesium stearate.

Film coating: Opadray II white 85F48105 (polyvinyl alcohol, macrogol, talc, titanium dioxide).