Methostabil - instructions for use, doses, side effects, contraindications

Ethylmethylhydroxypyridine succinate belongs to the class of 3-hydroxypyridines, is an inhibitor of free radical processes, membrane protection. It also has an antihypoxic effect, increases the resistance of the body to stress.

The mechanism of action of ethylmethylhydroxypyridine succinate is due to its antioxidant and membrane-protective action. The drug inhibits lipid peroxidation, increases the activity of superoxide oxidase, increases the ratio of lipid-protein, improves the structure and function of the cell membrane.

Ethyl methyl mercaptopyridine succinate modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands,contributes to the preservation of the structural and functional organization of biomembranes, the transport of neurotransmitters and the improvement of synaptic transmission. Ethyl methylhydroxypyridine succinate 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 ATP and creatine phosphate, activation of the energy-synthesizing functions of the mitochondria.

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

AT the conditions of a critical decrease in coronary blood flow contribute to the preservation of the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes - phosphodiesterase, adenylate cyclase, acetylcholinesterase. Supports the activation of acute ischemia activation of aerobic glycolysis and contributes in the conditions of hypoxia to the restoration of mitochondrial oxidation-reduction processes,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.

Promotes the preservation of retinal ganglion cells and optic nerve fibers with progressive neuropathy, the causes of which are chronic ischemia and hypoxia. It improves the functional activity of the retina and optic nerve, increasing visual acuity.

Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

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 a hypolipidemic effect, due to ant reductionthe total cholesterol and low-density lipoproteins.

Pharmacokinetics:

Suction and distribution

With a single and course admission, the maximum concentration (C_mOh) in the blood plasma is achieved after 0.58 hours When administered at a dose of 400-500 mg C_mOhin blood plasma - 3.5-4 μg / ml. Quickly distributed in organs and tissues. The average retention time of ethylmethylhydroxypyridine succinate in the body is 0.7-1.3 hours.

Metabolism

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; 2metabolite - pharmacologically active, is formed in large quantities and is found in the urine on 1-2 day. after administration; 3rd - is excreted in large quantities with urine; 4-th and 5-th - glucuronconjugates.

Excretion

It is excreted from the blood plasma quickly and practically is not detected after 4 hours in it. It is quickly 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 indices of urinary excretion of unchanged drug and metabolites have individual variability.

Indications:

As part of complex therapy:

- anxiety states with neurotic and neurosis-like disorders;

- syndrome of vegetative dystonia;

- chronic ischemia of the brain;

- light cognitive disorders of atherosclerotic origin;

- acute disorders of cerebral circulation (as part of combination therapy);

- withdrawal syndrome with alcoholism with a predominance of neurosis-like and vegetative-vascular disorders (as part of combination therapy);

- in the treatment of acute intoxication with antipsychotic drugs;

- craniocerebral trauma, consequences of craniocerebral injuries;

- primary open-angle glaucoma of various stages, as part of complex therapy;

- in the complex therapy of acute myocardial infarction.

Contraindications:

- Hypersensitivity to the drug;

- acute liver failure;

- acute renal insufficiency;

- childhood.

Carefully:Aa history of allergic diseases.

Pregnancy and lactation:

In experimental studies, there was no teratogenic, mutagenic embryotoxic effect. Adequate and strictly controlled clinical studies during pregnancy and lactation were not conducted.The drug is contraindicated in pregnancy and during breastfeeding due to the lack of data on the effectiveness and safety of the drug in these periods.

Dosing and Administration:

The drug is administered intravenously (jet or drip) or intramuscularly. When infusion is diluted in 0.9% solution of sodium chloride.

Jet inject slowly for 5-7 minutes, drip at a speed of 40-60 drops per minute. The maximum daily dose should not exceed 1200 mg.

In acute disorders of cerebral circulation in the first 10-14 days - intravenously drip 200-500 mg 2-4 times a day, then intramuscularly 200-250 mg 2-3 times a day for 2 weeks.

With traumatic brain injury and the consequences of injuries for 10-15 days intravenously drip on 200-500 mg 2-4 times a day.

With chronic cerebral ischemia in the stage of decompensation intravenously struino or drip in a dose of 200-500 mg 1-2 times a day for 14 days. Then intramuscularly at 100-250 mg / day for 14 days.

With chronic ischemia intramuscularly at 200-250 mg twice a day for 10-14 days.

With mild cognitive impairment in elderly patients and with anxiety disorders intramuscularly in a daily dose of 100-300 mg for 14-30 days.

In the syndrome of autonomic dystonia intramuscularly at 50-400 mg per day for 14 days.

In complex therapy in the treatment of withdrawal symptoms intravenously drip or intramuscularly 200-500 mg 2-3 times a day for 5-7 days. Treatment is stopped gradually, reducing the dose within 2-3 days.

When acute intoxication with antipsychotic agents intravenously at a dose of 200-500 mg per day for 7-14 days.

With acute myocardial infarction intravenously or intramuscularly for 14 days against standard therapy of myocardial infarction. In the first five days to achieve maximum effect, the drug is preferably administered intravenously, and for the next 9 days intramuscularly. Intravenous administration is carried out by dropwise infusion, slowly (to avoid side effects) on a 0.9% solution of sodium chloride or 5% solution of dextrose in a volume of 100-150 ml for 30-60 minutes. If necessary, a slow jet injection of the drug, which lasts at least 5 minutes, is possible. The drug is administered 3 times a day every 8 hours. The daily therapeutic dose is 6-9 mg / kg body weight per day, single-dose 2-3 mg / kg. The maximum daily dose should not exceed 800 mg, single 250 mg.

With glaucoma intramuscularly at 100-300 mg / day for 14 days.

Side effects:

From the digestive system: nausea, dryness of the oral mucosa or metallic taste in the mouth, flatulence, diarrhea.

From the nervous system: drowsiness, falling asleep.

From the respiratory system: sore throat, chest discomfort, a sense of lack of air (usually associated with an excessively high rate of administration and is of a short duration).

From the cardiovascular system: short-term increase in blood pressure.

Other: allergic reactions, a sensation of "spilling heat" throughout the body, an unpleasant smell.

Overdose:

Due to low toxicity, an overdose is unlikely. In case of an accidental overdose, drowsiness and sedation may occur. With intravenous administration, it is possible to increase blood pressure (BP).

Treatment, as a rule, is not required - the symptoms disappear on their own within a day. With excessive increase in blood pressure - antihypertensive drugs under the control of blood pressure.

In severe cases with insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.

Interaction:

Enhances the action of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) of medicinal products.

Reduces the toxic effect of ethanol.

Special instructions:

Pediatric Use

The drug is not prescribed for children under 18 years due to insufficient knowledge of the effect of the drug.

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

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

Form release / dosage:Solution for intravenous and intramuscular injection, 50 mg / ml.

Packaging:

By 2 ml or 5 ml in ampoules of light-protective neutral glass type I with a colored break ring or with a colored dot and a notch or without a break ring, a colored dot and notches. One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding can additionally be applied to the ampoules.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film. Or 5 The ampoule is placed in a preformed form (tray) made of cardboard with cells for stacking of ampoules.

1 or 2 contour squares or cardboard tracks together with the application and scarifier ampoule or a knife ampoule, or without a scarifier ampoule and a knife ampullum placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004106

Date of registration:30.01.2017

Expiration Date:30.01.2022

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp22.02.2017

Illustrated instructions

Instructions

Metostabil (Metostabil)