Metostabil
Metostabil: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Metostabil
ATX code: N07XX
Active ingredient: ethylmethylhydroxypyridine succinate (Ethylmethylhydroxypyridine succinate)
Manufacturer: LLC "Ozon" (Russia)
Description and photo update: 09.10.2019
Metostabil is an antioxidant drug for the treatment of diseases of the nervous system, an inhibitor of oxidative processes.
Release form and composition
- solution for intravenous and intramuscular administration: clear liquid, colorless or slightly yellowish [2 or 5 ml in ampoules of type 1 neutral light-protective glass without / with a colored break ring / colored dot and a notch (additionally, from one to three colored rings, and / or alphanumeric coding, and / or two-dimensional barcode), in blister packs / cardboard trays with cells of 5 ampoules, in a cardboard box 1 or 2 cell packs / cardboard trays without / with an ampoule scarifier / knife and instructions for the use of Metostabil];
- film-coated tablets: biconvex, round, film shell from almost white to white, a core from white with a yellowish tinge to white stands out in cross-section (5, 10, 25 or 30 pcs. in blister strip packaging, in cardboard a pack of 1–6, 8 or 10 packs with instructions for use; 10, 20, 25, 30, 40, 50 or 100 pieces each in polyethylene terephthalate / polypropylene drug cans sealed with high-pressure polyethylene lids with first opening control / polypropylene lids with a “push-turn” system / lids made of low pressure polyethylene with first opening control, in a cardboard box 1 can with instructions for use).
Composition for 1 ml of solution:
- active ingredient: ethylmethylhydroxypyridine succinate - 50 mg;
- auxiliary ingredients: sodium disulfite - 1 mg; water for injection - up to 1 ml.
Composition for one tablet:
- active ingredient: ethylmethylhydroxypyridine succinate - 125 mg;
- auxiliary ingredients: MCC (microcrystalline cellulose) - 191.4 mg; magnesium stearate - 3.5 mg; povidone (plasdone) K-25 - 14 mg; croscarmellose sodium - 14 mg; colloidal silicon dioxide - 2.1 mg;
- film shell: macrogol-4000 - 1.25 mg; hypromellose - 6 mg; titanium dioxide - 2.75 mg.
Pharmacological properties
Pharmacodynamics
The active component of Metostabil is ethylmethylhydroxypyridine (2-ethyl-6-methyl-3-hydroxypyridine) succinate, belonging to the class of 3-hydroxypyridines, is a membrane protector, inhibits the course of free radical processes, has an antihypoxic effect, and enhances the body's stress resistance. The mechanism of action of 2-ethyl-6-methyl-3-hydroxypyridine succinate is determined by its antioxidant and membrane-protective effects. The drug stimulates the growth of superoxide oxidase activity, inhibits lipid peroxidation, increases the ratio of lipids and proteins, improves the structure and function of the plasma membrane.
The main pharmacological properties of ethylmethylhydroxypyridine succinate:
- modulation of the activity of membrane-bound enzymes (adenylate cyclase, acetylcholinesterase, calcium-independent phosphodiesterase) and receptor complexes [benzodiazepine, acetylcholine, GABA (gamma-aminobutyric acid)], which leads to an increase in their ability to bind to ligands-functional, allowing to maintain the biomembrane transport neurotransmitters and improved synaptic transmission; increased dopamine content in the brain;
- enhancement of compensatory activation of aerobic glycolysis under conditions of hypoxia and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle with an increase in the level of adenosine triphosphate and creatine phosphoric acids, activation of energy-synthesizing functions of mitochondria;
- an increase in the body's resistance to various damaging factors in such pathological conditions as cerebrovascular accident, hypoxia and ischemia, intoxication with ethanol and neuroleptics;
- preservation of the structural and functional organization of cardiomyocyte membranes in conditions of a critical decrease in coronary blood flow, stimulation of the activity of such membrane enzymes as adenylate cyclase, acetylcholinesterase, phosphodiesterase;
- support for the activation of aerobic glycolysis that develops in acute ischemia and assistance in the restoration of mitochondrial redox processes under hypoxic conditions, increased synthesis of adenosine triphosphate and creatine phosphate; ensuring the integrity of physiological functions and morphological structures of the ischemic myocardium;
- improving the picture of the clinical course of myocardial infarction and the effectiveness of thrombolytic (fibrinolytic) therapy, reducing the incidence of arrhythmias and cardiac conduction disorders;
- normalization of metabolic processes in the ischemic myocardium, an increase in the antianginal activity of nitrates, an improvement in the rheological properties of blood, a decrease in the consequences of reperfusion syndrome in patients with acute coronary insufficiency;
- decrease in patients with acute pancreatitis of the severity of enzymatic toxemia and endogenous intoxication;
- increased metabolism and blood supply to the brain, improved microcirculation and rheological properties of blood, reduced platelet aggregation, stabilized membranes of blood cell elements (erythrocytes and platelets), reduced risk of hemolysis;
- a decrease in the concentration of total cholesterol and low density lipoproteins due to the hypolipidemic effect;
- preservation of retinal ganglion cells and optic nerve fibers in patients with progressive neuropathy developing as a result of chronic ischemia and hypoxia; improving the functional activity of the retina and optic nerve, increasing visual acuity (solution for intravenous and intramuscular administration).
Pharmacokinetics
- absorption and distribution: as a result of parenteral administration of 400–500 mg of Metostabil, the maximum concentration of its active substance (C max) in blood plasma reaches 3.5–4 μg / ml. With both single and course use, the time to reach the maximum concentration (T Cmax) in the blood plasma is 0.58 h. After oral administration, the half-absorption period is 0.08–1 h, C max reaches a level of 50–100 ng / ml, and the T Cmax value varies in the range of 0.46–0.5 hours. The substance is rapidly distributed in tissues and organs. The average time at which 2-ethyl-6-methyl-3-hydroxypyridine succinate is determined in the body for parenteral and oral administration is 0.7-1.3 and 4.9-5.2 hours, respectively;
- metabolism: biotransformation of 2-ethyl-6-methyl-3-hydroxypyridine succinate occurs in the liver through glucuronidation. As a result, 5 identifiable metabolites are formed: 1st - 3-hydroxypyridine phosphate (formed in the liver and with the participation of alkaline phosphatase decomposes into 3-hydroxypyridine and phosphoric acid); 2nd - is pharmacologically active, is formed in large quantities and is determined in urine 1–2 days after the use of Metostabil; 3rd - eliminated in large quantities in the urine; 4th and 5th are glucuron conjugates;
- Elimination: 4 hours after parenteral administration of 2-ethyl-6-methyl-3-hydroxypyridine, succinate is practically not detected in blood plasma. When ingested, it is most intensively excreted during the first 4 hours, T 1/2 (half-life) is from 4.7 to 5 hours. The substance is rapidly eliminated in the urine, mainly in the form of metabolites - up to 50% within 12 hours, an insignificant amount is excreted in the form of an unchanged substance - 0.3% within 12 hours. The quantitative characteristics of the elimination of unchanged drug and its metabolites through the urinary system are characterized by significant individual variability.
Indications for use
Solution for intravenous and intramuscular administration
Metostabil solution for intravenous and intramuscular administration is recommended for use in the complex therapy of the following diseases / conditions:
- anxiety states with neurotic level syndromes (neurotic and neurosis-like);
- HIGM (chronic cerebral ischemia);
- SVD (vegetative dystonia syndrome);
- mild cognitive impairment of atherosclerotic genesis;
- ONMK (acute disorders of cerebral circulation);
- alcohol withdrawal syndrome with a predominance of vegetative-vascular and neurosis-like disorders;
- POAG (primary open-angle glaucoma) of various stages;
- acute intoxication with neuroleptics;
- craniocerebral trauma, consequences of craniocerebral trauma;
- acute myocardial infarction.
Film-coated tablets
Indications for the use of Metostabil tablets:
- consequences of stroke, including conditions after transient ischemic attacks, in the phase of subcompensation - for the purpose of prevention;
- minor craniocerebral trauma, the consequences of craniocerebral trauma;
- encephalopathic pathologies of various origins (dysmetabolic, dyscirculatory, post-traumatic, mixed);
- SVD;
- mild cognitive impairment of atherosclerotic genesis;
- anxiety states with neurotic level syndromes (neurotic and neurosis-like);
- IHD (ischemic heart disease) - as part of a combination treatment;
- alcohol withdrawal syndrome with a predominance of vegetative-vascular and neurosis-like disorders - relief of the condition; post-withdrawal disorders;
- acute intoxication with neuroleptics;
- asthenic syndrome; exposure to extreme factors and loads - prevention of the development of somatic diseases;
- exposure to stress factors.
Contraindications
Absolute:
- acute hepatic / renal failure;
- pregnancy and the period of breastfeeding;
- children and adolescents up to 18 years old;
- hypersensitivity to ethylmethylhydroxypyridine succinate and / or the auxiliary components of Metostabil.
The drug should be used with caution if there is data in the patient's history of allergic diseases.
Metostabil, instructions for use: method and dosage
Solution for intravenous and intramuscular administration
Metostabil solution is administered intramuscularly or intravenously (jet or drip).
For infusion administration, the solution must be diluted in 0.9% sodium chloride solution.
The time of the jet injection of a single dose is 5–7 minutes; drip infusion rate - 40-60 drops / min.
Recommended dosage regimen of Metostabil:
- acute disorders of cerebral circulation: the first 10-14 days - 200-500 mg intravenously drip from 2 to 4 times a day, then within 14 days - 200-250 mg intramuscularly from 2 to 3 times a day; general course - 24-28 days;
- craniocerebral trauma, consequences of craniocerebral trauma: 200-500 mg intravenously, 2 to 4 times a day; course - 10-15 days;
- CCI in the stage of decompensation: the first 14 days - 200–500 mg intravenously (jet or drip) 1–2 times a day; then within 14 days - 100–250 mg intramuscularly 1 time per day; general course - 28 days;
- chronic ischemia: 200–250 mg intramuscularly 2 times a day; course 10-14 days;
- mild cognitive impairment in elderly patients, anxiety disorders: 100–300 mg intramuscularly 1 time per day; course 14-30 days;
- SVD: 50-400 mg intramuscularly 1 time per day; course - 14 days;
- withdrawal symptoms: 200-500 mg intravenously / intramuscularly 2-3 times a day; course - 5-7 days (therapy should be stopped gradually, reducing the dose for 2-3 days);
- acute intoxication with neuroleptics: 200–500 mg intravenously 1 time per day; course - 7-14 days;
- acute myocardial infarction: for the first 5 days, in order to achieve maximum clinical effect, the solution is recommended to be administered slowly intravenously (to avoid side reactions) by drip infusion, lasting 30-60 minutes, it should be diluted in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose solution (if necessary, Metostabil can also be injected slowly in a jet for at least 5 minutes); the next 9 days, the solution is administered intramuscularly. Infusion and injections are carried out 3 times a day at regular intervals (1 time in 8 hours); the therapeutic dose is determined from the calculation: daily - 6-9 mg / kg of the patient's body weight; single dose - 2-3 mg / kg, while the maximum single dose should not exceed 250 mg, daily dose - 800 mg; course - 14 days (against the background of standard therapy for myocardial infarction);
- glaucoma: 100–300 mg intramuscularly 1 time per day; course - 14 days.
The maximum daily dose for parenteral administration of Metostabil is 1200 mg.
Film-coated tablets
Metostabil tablets are intended for oral administration.
Recommended dosage regimen: 3 times a day, 1-2 tablets (125-250 mg). The course of therapy is from 2 to 6 weeks.
For relief of alcohol withdrawal at the beginning of treatment, take 1-2 times a day, 1-2 tablets (125-250 mg), the dose is gradually increased until a stable therapeutic effect is obtained. The course of therapy is 5-7 days. The treatment should be completed by reducing the dose gradually over 2-3 days.
The maximum daily dose for oral administration of Metostabil is 800 mg.
The duration of the course of treatment for patients with coronary artery disease should be at least 1.5–2 months.
On the recommendation of a doctor, it is possible to conduct repeated courses, which should preferably be carried out in the spring-autumn period.
Side effects
With intramuscular or intravenous administration of Metostabil solution, the following negative side reactions from organs and systems are possible:
- digestive system: dryness of the oral mucosa / metallic taste in the mouth, nausea, diarrhea, flatulence;
- nervous system: violation of falling asleep, drowsiness;
- respiratory system: discomfort in the chest, sore throat, feeling of lack of air (it is short-term, most often associated with a too high rate of solution administration);
- cardiovascular system: short-term increase in blood pressure;
- others: hypersensitivity reactions, unpleasant odor, feeling of spreading heat throughout the body.
As a result of taking Metostabil in the form of tablets, dryness of the oral mucosa and / or diarrhea may develop on the part of the digestive system, as well as side effects in the form of hypersensitivity reactions and / or drowsiness.
Overdose
Due to the low toxicity of ethylmethylhydroxypyridine succinate, an overdose of Metostabil is unlikely. Possible reactions in case of accidental overdose are drowsiness and sedation. Intravenous administration of high doses of the drug can cause an increase in blood pressure.
As a rule, the symptoms of an overdose disappear on their own within 1 day and do not require additional therapeutic measures. In case of an excessive increase in blood pressure, it is recommended to use antihypertensive drugs under the control of the patient's condition.
For severe intoxication, accompanied by insomnia, diazepam - 5 mg, nitrazepam - 10 mg, or oxazepam - 10 mg are prescribed.
special instructions
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy with Metostabil, patients should be careful when driving vehicles and performing other potentially dangerous types of work that require increased concentration of attention and high speed of psychomotor reactions.
Application during pregnancy and lactation
In the course of experimental studies of ethylmethylhydroxypyridine succinate, the mutagenic, embryotoxic and teratogenic effects of the substance were not revealed. But adequate and strictly controlled clinical studies of its use during pregnancy and during breastfeeding have not been conducted.
Metostabil is contraindicated in pregnant and breastfeeding women, as there is insufficient data on the effectiveness / safety of therapy during these periods.
Pediatric use
In pediatric practice, Metostabil is contraindicated for the treatment of children and adolescents under 18 years of age due to insufficient knowledge of its effectiveness / safety.
With impaired renal function
Metostabil is contraindicated in acute renal failure.
For violations of liver function
Metostabil is contraindicated in acute liver failure.
Drug interactions
Ethylmethylhydroxypyridine succinate potentiates the effect of the following drugs: antiparkinsonian (levodopa), antiepileptic (carbamazepine) and benzodiazepine anxiolytics.
Metostabil reduces the toxic effect of ethyl alcohol.
Analogs
Metostabil's analogs are Astrox, Medomeksi, Meksidant, Meksidol, Meksikor, Meksilek-Lekpharm, Meksiprim, Meksifin, MetutsinVel, Neurocard, Neuroks, Proinin, Cerecard, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children. Do not freeze the solution and store in a place out of the reach of light.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Metostable
It is extremely rare on specialized forums and sites to find reviews about Metostable. This could be due to a lack of medication in most pharmacies. A situation was described when the drug helped a woman in the postmenopausal period to solve problems with falling asleep, insomnia, nervous breakdowns, which significantly improved the quality of her life.
It is important to take into account that Metostabil acts on each person individually, therefore, reviews written by a specific patient reflect the effect of the drug exclusively on his body.
Price for Metostabil in pharmacies
Approximate price of Metostabil, film-coated tablets, 125 mg, for 30 pcs. in the package can be from 158 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
