Ethylmethylhydroxypyridine tablets p / o 125mg, No. 50 Akrihin

• Anxiety states with neurotic and neurosis-like states;

• vegetative-vascular dystonia;

• encephalopathy;

• Mild cognitive disorders of atherosclerotic genesis.

• Acute disorders of cerebral circulation (as part of combination therapy).

• Withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;

• Acute intoxication with antipsychotic drugs.

• Acute purulent-inflammatory processes in the abdominal cavity (including acute necrotizing pancreatitis, peritonitis (as part of complex therapy));

• Acute myocardial infarction from the first day (parenteral);

• Ischemic heart disease;

• Complex therapy of ischemic stroke (oral) - as part of complex therapy.

The dose, frequency of use and duration of treatment are set individually depending on the indications and the clinical situation. Inside - 0.25-0.5 g / day in 2-3 doses; the maximum daily dose is 0.6-0.8 g.

ethylmethylhydroxypyridine succinate

Hypersensitivity; acute hepatic and / or renal failure; pregnancy; lactation period; childhood.

pharmachologic effect

An inhibitor of free radical processes is a membrane protector that also has antihypoxic, stress-protective, nootropic, antiepileptic 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 oxidase, increases the lipid-protein ratio, improves the structure and function of the cell membrane. It modulates the activity of membrane-bound enzymes (Ca2 + -independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which contributes to their binding to ligands, preservation of the structural and functional organization of biomembranes, and the transport of neuromediate mediators. 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 conditions of hypoxia with an increase in ATP 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, cerebral circulation disorders, 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.Improves the functional state of ischemic myocardium in myocardial infarction, contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle. In conditions of a critical decrease in coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes - PDE, adenylate cyclase, acetylcholinesterase. Supports the activation of aerobic glycolysis that develops during acute ischemia and promotes the restoration of mitochondrial redox processes under conditions of hypoxia, increases the synthesis of ATP and creatine phosphate. Provides the integrity of the morphological structures and physiological functions of the ischemic myocardium. Improves the clinical course of myocardial infarction, increases the effectiveness of the therapy,accelerates the restoration of functional activity of the left ventricular myocardium, reduces the incidence of arrhythmias and intracardiac conduction disorders. 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 coronary blood flow in the ischemic area, increases the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.reduces the zone of necrosis, restores and / or improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, increases the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.reduces the zone of necrosis, restores and / or improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, increases the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Pharmacokinetics

It is rapidly absorbed when taken orally (half-absorption period - 0.08-1 h). Tmax for i / m administration - 0.3-0.58 h, for oral administration - 0.46-0.5 h. Cmax for i / m administration at a dose of 400-500 mg - 2.5-4 ?g / ml, for oral administration - 50-100 ng / ml. It is quickly distributed in organs and tissues. The average retention time of the drug in the body with intramuscular administration is 0.7-1.3 hours, when taken orally - 4.9-5.2 hours. It is metabolized in the liver by glucuronidation. 5 metabolites have been identified: 3-hydroxypyridine phosphate - formed in the liver and, with the participation of alkaline phosphatase, decomposes into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, is formed in large quantities and is found in urine for 1-2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates. T1 / 2 when taken orally - 4.7-5 hours.It is rapidly 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). The 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.

Side effect

Ingestion: nausea, dry mouth, diarrhea, drowsiness, allergic reactions. With parenteral administration (especially intravenous jet): dryness, a 'metallic' taste in the mouth, sensations of 'spreading warmth' throughout the body, unpleasant odor, sore throat and chest discomfort, feeling of lack of air (usually associated with excessive high speed of introduction and are short-term); with prolonged use - nausea, flatulence; sleep disturbances (drowsiness or trouble falling asleep).

Application during pregnancy and lactation

Use during pregnancy and breastfeeding is contraindicated.

Application for violations of liver function

Contraindication: acute liver failure.

Application for impaired renal function

Contraindication: acute renal failure.

Application in children

The drug is contraindicated for use in children and adolescents under the age of 18 years.

special instructions

Use with caution if there is a history of allergic diseases. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

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