Clinical and pharmacological group: & nbsp

Antihypoxants and antioxidants

Means for correcting disorders in alcoholism, toxic and drug addiction

Included in the formulation
  • Mexico 6®
    pills inwards 
  • АТХ:

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

    Pharmacodynamics:

    Combined drug.

    Ethyl methylhydroxypyridine succinate - inhibitor of free radical processes - membranoprotector, which also possesses antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic action. Antioxidant drug, regulating metabolic processes in the myocardium and vascular wall.

    The mechanism of action is due to antioxidant and membrane-protective properties. It suppresses lipid peroxidation, increases the activity of superoxide oxidase, affects the physicochemical properties of the membrane, increases the content of lipid polar fractions (phosphotidylserine and phosphotidylinositum, etc.) in the membrane, reduces the ratio of cholesterol / phospholipids, reduces the viscosity of the lipid layer and increases the fluidity of the membrane, activates energy-synthesizing functions of mitochondria and improves energy metabolism in the cell and, thus, protects the cell apparatus and the structure of their membranes.

    The change in the functional activity of the biological membrane caused by the drug leads to conformational changes in the protein macromolecules of the synaptic membranes, as a result of which it modulates the activity of membrane-bound enzymes, ion channels and receptor complexes, in particular, benzodiazepine, GABA, acetylcholine, enhancing their ability to bind to ligands, increasing the activity of neurotransmitters and activation of synaptic processes.

    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 adenosine triphosphate (ATP) and creatine phosphate, activates the energy-producing function of mitochondria.

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

    It improves the metabolism and blood supply of 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. Has hypolipidemic action, reduces the content of total cholesterol and low density lipoprotein (LDL).

    Improves the functional state of the ischemic myocardium, reducing the manifestations of systolic and diastolic dysfunction of the left ventricle, as well as electrical instability of the myocardium.

    In conditions of a critical decrease in coronary blood flow, it helps maintain the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane phosphodiesterase enzymes, adenylate cyclase, acetylcholinesterase. It supports the activation of aerobic glycolysis in acute ischemia and promotes the reduction of mitochondrial oxidation-reduction processes in hypoxic conditions, increases the synthesis of adenosine triphosphate (ATP), creatine phosphate and other macroerges. Increases the collateral blood supply of the ischemic myocardium and activates the energosynthesizing processes in the ischemic zone, which contributes to maintaining the integrity of the cardiomyocytes and maintaining their functional activity.

    Patients with stable angina increases exercise tolerance nitrates and anti-anginal activity, improves the rheological properties of the blood, reduces the incidence of acute coronary insufficiency.

    Pyridoxine, Entering the organism is phosphorylated, is converted into pyridoxal-5-phosphate, and part of the enzymes carrying out decarboxylation, transamination, and racemization of amino acids and enzymatic conversion of sulfur-containing amino acids and hydroxylated. Participates in the metabolism; is necessary for the normal functioning of the central and peripheral nervous system. Pyridoxine participates in the exchange of tryptophan, methionine, cysteine, glutamic and other amino acids. It plays an important role in the exchange of histamine. Promotes the normalization of lipid metabolism.

    Pharmacokinetics:

    Ethyl methylhydroxypyridine succinate quickly absorbed when taken internally (the period of half-absorption is 0.08-1 h). The time to reach the maximum concentration when ingested - 0.46-0.5 hours. The maximum concentration when administered orally - 50-100 ng / ml.

    Quickly distributed in organs and tissues.The average retention time of ethylmethylhydroxypyridine succinate in the body with oral administration is 4.9-5.2 hours.

    Ethyl methylhydroxypyridine succinate is metabolized in the liver by glucuronation. Five metabolites were identified: 3-hydroxypyridine phosphate - is formed in the liver and, with the participation of alkaline phosphatase, decomposes into phosphoric acid and 3-hydroxypyridine; The second metabolite, pharmacologically active, is formed in large quantities and is found in the urine on the 1-2 day after administration; 3rd - is discharged in large quantities with urine; 4-th and 5-th - glucuronconjugates.

    Half-life when ingested - 4.7-5 hours. It is rapidly excreted in the urine mainly in the form of metabolites (50% in 12 hours) and in an insignificant amount - unchanged (0.3% per 12 hours). The most intense withdrawal during the first 4 hours after taking ethylmethylhydroxypyridine succinate. The urinary excretion of unchanged ethylmethyl hydroxypyridine succinate and metabolites has a significant individual variability.

    Pyridoxine absorbed rapidly throughout the small intestine.

    Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate).

    Pyridoxal phosphate with plasma proteins binds to 90%. It penetrates well into all tissues; accumulates mainly in the liver, less - in the muscles and central nervous system. Penetrates through the placenta, is secreted with breast milk.

    Half-life - 15-20 days. It is excreted by the kidneys (with intravenous injection - with bile 2%), as well as during hemodialysis.

    Indications:

    In the combination therapy:

    - dyscirculatory encephalopathy;

    - a syndrome of vegetative dystonia;

    - anxiety states in neurotic and neurosis-like states;

    - An abstinence syndrome with alcoholism with prevalence of neurosis-like and vegetative-vascular disorders;

    - ischemic heart disease (prevention of seizures);

    - conditions after acute intoxication by antipsychotic agents;

    - asthenic conditions, as well as for the prevention of the development of somatic diseases under the influence of extreme factors and loads;

    - the impact of extreme (stressor) factors.

    V.F90-F98.F90.0   Violation of activity and attention

    V.F40-F48.F40.0   Agoraphobia

    IX.I60-I69.I69   Effects of cerebrovascular disease

    IX.I60-I69.I67.2   Cerebral atherosclerosis

    IX.I20-I25.I25.8   Other forms of chronic ischemic heart disease

    IX.I20-I25.I25   Chronic ischemic heart disease

    VI.G20-G26.G24   Dystonia

    VI.G90-G99.G93.4   Encephalopathy, unspecified

    Contraindications:
    • Hypersensitivity.
    • Acute hepatic and / or renal failure.
    • Pregnancy.
    • Lactation.
    • Childhood.
    Carefully:

    Stomach ulcer and duodenal ulcer.

    Pregnancy and lactation:

    Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside 1 tablet 3 times a day; the initial dose of 1-2 tablets 1-2 times a day with a gradual increase to obtain a therapeutic effect. The maximum daily dose of 6 tablets per day.

    Duration of treatment is 2-8 weeks. If necessary, it is possible to conduct repeated courses.

    Side effects:

    Nausea, dry mouth, diarrhea, drowsiness, allergic reactions, hypersecretion of hydrochloric acid, numbness, the appearance of a feeling of compression in the extremities - a symptom of "stocking" and "gloves," a decrease in lactation (sometimes it is used as a therapeutic effect).

    Overdose:

    Ethyl methylhydroxypyridine succinate

    Due to low toxicity, an overdose is unlikely.In case of an accidental overdose, drowsiness and sedation may occur. Treatment, as a rule, is not required - the symptoms disappear on their own within a day. In severe cases with insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.

    Pyridoxine

    Taking high doses of pyridoxine for a short period of time (at a dose of more than 1 g per day) can lead to a short-term occurrence of neurotoxic effects.

    When taking pyridoxine in a dose exceeding 150 mg / kg body weight, it is recommended to induce vomiting and take Activated carbon. Provocation of vomiting is most effective during the first 30 minutes after taking the drug. Emergency measures may be required.

    Interaction:

    Ethyl methylhydroxypyridine succinate

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

    Pyridoxine

    Strengthens the action of diuretics; weakens the activity of levodopa, it combines well with cardiac glycosides (pyridoxine promotes an increase in the synthesis of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate (increases resistance to hypoxia).

    Pyridoxine is pharmaceutically incompatible with thiamine and cyanocobalamin. Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine.

    Special instructions:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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