Ethylmethylhydroxypyridine-Acrichin, 125 mg 50 pcs

ATC: N.07.X.X Other drugs for the treatment of diseases of the nervous system

Ethylmethylhydroxypyridine is an inhibitor of free-radical processes, a membranoprotector with antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic effects. It belongs to the class of 3-oxypyridines.

The mechanism of action of ethylmethylhydroxypyridine is due to its antioxidant, antihypoxant and membrane-protective action. It inhibits lipid peroxidation, increases superoxide dismutase activity, increases lipid-protein ratio, improves cell membrane structure and function. The drug modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which increases their ability to bind to ligands, helps maintain the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission.

Ethylmethylhydroxypyridine-Acrichine increases the content of dopamine in the brain. 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 (ATP) and creatine phosphate, activation of energy-synthesizing functions of mitochondria.

Enhances resistance of the body to various damaging factors in pathological conditions (hypoxia and ischemia, disorders of cerebral circulation, intoxication with ethanol and antipsychotic drugs).

In conditions of critical reduction of coronary blood flow promotes the preservation of structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes – phosphodiesterase, adenylate cyclase, acetylcholinesterase. It supports activation of aerobic glycolysis developing in acute ischemia and promotes under hypoxia restoration of mitochondrial redox processes, increases ATP and creatine phosphate synthesis. Ensures the integrity of morphological structures and physiological functions of ischemic myocardium. Improves the clinical course of myocardial infarction, increases the effectiveness of therapy, accelerates the recovery of LV myocardial functional activity, reduces the frequency of arrhythmias and intracardiac conduction disturbances. It normalizes metabolic processes in ischemic myocardium, increases antianginal activity of nitrates, improves rheological properties of blood, reduces consequences of reperfusion syndrome in acute coronary failure.

Limits enzymatic toxemia and endogenous intoxication in acute pancreatitis.

It improves metabolism and blood supply of the brain, improves microcirculation and rheological properties of the blood, reduces platelet aggregation. It stabilizes membrane structures of blood cells (erythrocytes and platelets), reducing the likelihood of 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-Acrichine has a pronounced anti-toxic effect during withdrawal syndrome. It eliminates neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, vegetative functions and is also able to relieve cognitive disorders caused by prolonged ethanol intake and its withdrawal.

The effects of tranquilizers, neuroleptics, antidepressants, hypnotics and anticonvulsants are increased under the influence of the drug, which allows reducing their doses and side effects.

Ethylmethylhydroxypyridine-Acrichine improves the functional state of the 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.

Absorption and distribution

It is rapidly absorbed when ingested (half-absorption period is 0.08-1 h). Time to reach maximum concentration (TSmax) when taken orally is 0.46-0.5 h. Maximum concentration (Cmax) when administered orally is 50-100 ng/ml.

It is rapidly distributed in the organs and tissues. Average retention time of ethylmethylhydroxypyridine succinate in the body when administered orally is 4.9-5.2 hours.

Metabolism

Metabolized in the liver by glucuronidation. Five metabolites were identified: 3-oxypyridine phosphate – is formed in liver, with the help of alkaline phosphatase it splits into phosphoric acid and 3-oxypyridine; the 2nd metabolite – pharmacologically active, is formed in large amounts and is found in urine 1-2 days after administration; the 3rd one is excreted in large amounts with urine; the 4th and the 5th are glucuronconjugates.

The elimination half-life when administered orally (T1/2) is 4.7-5 hours. It is rapidly excreted in the urine, mainly as metabolites (50% in 12 hours) and in a small amount – in unchanged form (0.3% in 12 hours). It is most intensively excreted during the first 4 hours after drug administration. The rates of urinary excretion of unchanged drug and metabolites have individual variability.