Active substanceEthyl methylhydroxypyridine succinateEthyl methylhydroxypyridine succinate
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Composition per 1 tablet:

    Active substance:

    Ethyl methylhydroxypyridine succinate in terms of 100% substance - 250.0 mg.

    Excipients: lactose monohydrate, povidone K-30, magnesium stearate.

    Film Sheath: Opaprai II pink 33G240018 (hypromellose, titanium dioxide, lactose monohydrate, macrogol 4000, triacetin, iron oxide red oxide, iron oxide yellow dye).

    Description:

    Round biconvex tablets, covered with a film coat of light pink color. On the cross section, the nucleus is almost white.

    Pharmacotherapeutic group:Antioxidant
    ATX: & nbsp

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

    Pharmacodynamics:

    Mexidol® FORTE 250 is an inhibitor of free radical processes, a membrane protector possessing antihypoxic, stress-protective, nootropic, anti-epileptic and anxiolytic action. It belongs to the class of 3-hydroxypyridines.

    Mechanism of action Mexidol FORTE 250 is due to its antioxidant, antihypoxic and membrane-protective action. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, improves the structure and function of the cell membrane.The drug modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, gamma-aminobutyric acid (GABA), acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structurally functional organization of biomembranes, neurotransmitter transport and improvement synaptic transmission. Meksidol® FORTE 250 increases the content of dopamine in the brain. It causes an increase in the compensatory activation of aerobic glycolysis and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle under conditions of hypoxia with an increase in the content of adenosine triphosphate (ATP) and creatine phosphate, activation of the energy-synthesizing functions of the mitochondria.

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

    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 enzymes - phosphodiesterase, adenylate cyclase, acetylcholinesterase. It supports the activation of aerobic glycolysis in acute ischemia and promotes the restoration of mitochondrial oxidation-reduction processes under conditions of hypoxia, increases the synthesis of ATP and creatine phosphate. Ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium. It improves the clinical course of myocardial infarction, improves the effectiveness of therapy, reduces the incidence of arrhythmias and intracardiac conduction disorders. Normalizes metabolic processes in ischemic myocardium, increases the antianginal activity of nitrates, improves rheological properties of blood, reduces the effects of reperfusion syndrome in acute coronary insufficiency.

    Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

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

    Anti-stress action is manifested in the normalization of post-stress behavior, somatogenetic disorders, restoration of sleep-wake cycles, disrupted learning and memory processes, and reduction of dystrophic and morphological changes in various structures of the brain.

    Mexidol® FORTE 250 has a pronounced antitoxic effect on withdrawal symptoms. It eliminates neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, vegetative functions, and is also capable of removing cognitive impairments caused by prolonged intake of ethanol and its cancellation. Under the influence of the drug, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which helps to reduce their doses and reduce side effects.

    Mexidol® FORTE 250 improves the functional state of the ischemic myocardium.In the context of coronary insufficiency increases collateral blood flow to ischemic myocardium, it helps to preserve the integrity of cardiomyocytes and maintaining their functional activity. Effectively restores myocardial contractility with reversible cardiac dysfunction.

    Pharmacokinetics:

    Quickly absorbed when taken orally. The maximum concentration (CmOh) at doses of 400-500 mg is 3.5-4.0 μg / ml. Quickly distributed in organs and tissues. Average hold time (MRT) preparation in the body when ingested - 4.9-5.2 hours. Metabolized in the liver by glucuronconjugation. Five metabolites were identified: 3-hydroxypyridine phosphate - formed in the liver, with the participation of alkaline phosphatase breaks down into phosphoric acid and 3-hydroxypyridine; The second metabolite, pharmacologically active, is formed in large quantities and is found in the urine for 1-2 days. after administration; 3rd - is excreted in large quantities with urine; 4-th and 5-th - glucuronconjugates. The half-life (T1 / 2) with oral administration is 2.0-2.6 hours. It is quickly excreted in the urine mainly in the form of metabolites and in an insignificant amount in unchanged form.The most intense withdrawal within the first 4 hours after taking the drug. The indices of urinary excretion of unchanged drug and metabolites have individual variability.

    Indications:

    - The consequences of acute disorders of cerebral circulation, including after transient ischemic attacks, in the phase of subcompensation as preventive courses;

    - light craniocerebral injury, the consequences of craniocereberal trauma;

    - encephalopathy of various genesis (dyscirculatory, dismetabolic, posttraumatic, mixed);

    - syndrome of vegetative dystonia;

    - light cognitive disorders of atherosclerotic origin;

    - anxiety disorders in neurotic and neurosis-like states;

    - ischemic heart disease as part of complex therapy;

    - relief of withdrawal syndrome with alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, post-retroviral disorders;

    - state after acute intoxication by antipsychotic drugs;

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

    - influence of extreme (stressor) factors.

    Contraindications:

    Acute violations of liver and kidney function, increased individual sensitivity to the drug. In connection with the insufficient study of the effect of the drug

    - children's age, pregnancy, breast-feeding.

    Pregnancy and lactation:

    The drug Mexidol® FORTE 250 is contraindicated in pregnancy and during breastfeeding.

    Dosing and Administration:

    Inside, 250 mg 3 times a day.

    The initial dose is 250 mg (1 tablet) 1-2 times a day with a gradual increase to a therapeutic effect. The maximum daily dose is 750 mg (3 tablets). Duration of treatment is 2-6 weeks; for relief of alcohol withdrawal - 5-7 days. The duration of therapy in patients with coronary heart disease is at least 1.5-2 months.

    Repeated courses (on the recommendation of a doctor), preferably in the spring-autumn periods.

    Side effects:

    Possible occurrence of individual adverse reactions: dyspeptic or dyspepsia, allergic reactions.

    Overdose:

    Symptoms: drowsiness, insomnia.

    Treatment: due to low toxicity, an overdose is unlikely. Treatment, as a rule, is not required, - the symptoms disappear on their own within 24 hours.In severe manifestations, supportive and symptomatic treatment is performed.

    Interaction:

    Mexidol® FORTE 250 is combined with all drugs used to treat somatic diseases.

    Strengthens the action of benzodiazepines, antidepressants, anxiolytics, antiepileptic drugs (carbamazepine) and antiparkinsonian drugs (levodopa), nitrates. Reduces the toxic effect of ethanol.

    Effect on the ability to drive transp. cf. and fur:

    During the period of taking the drug should be careful when working, requiring rapidity of psychophysical reactions (management of vehicles, mechanisms, etc.).

    Form release / dosage:

    Tablets, film-coated, 250 mg.

    Packaging:

    For 10 tablets, coated with a film sheath, into a contour mesh box made of a polyvinylchloride film and aluminum foil. By 1, 2, 3, 4, 5, 6 contour squares with instructions for use in a cardboard pack.

    Storage conditions:

    Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004831
    Date of registration:26.04.2018
    Expiration Date:26.04.2023
    The owner of the registration certificate:FARMASOFT NPK, LLC FARMASOFT NPK, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp28.05.2018
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