Ethylmethylhydroxypyridine succinate
Ethylmethylhydroxypyridine succinate: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Ethylmethylhydroxypyridine succinate
ATX code: N07XX
Active ingredient: ethylmethylhydroxypyridine succinate (Ethylmethylhydroxypyridine succinate)
Manufacturer: JSC "Binnopharm" (Russia)
Description and photo update: 2020-29-04
Ethylmethylhydroxypyridine succinate is an antioxidant drug.
Release form and composition
Dosage forms of Ethylmethylhydroxypyridine succinate:
- solution for intravenous (i / v) and intramuscular (i / m) administration: clear colorless or slightly colored liquid (2, 5 or 10 ml each in colorless glass ampoules with a notch, white dot and self-adhesive label; in a blister strip of 5 ampoules, in a pack of cardboard 1 or 2 packs and instructions for medical use of the solution For hospitals, 4, 10 or 20 packs with the corresponding number of instructions for medical use are placed in a corrugated cardboard box);
- film-coated tablets: round, biconvex, tablet shell and core in cross-section from white to white with a yellowish tinge (10 pcs. in blister packs, in a cardboard box 1–5 packs).
Each pack also contains instructions for the use of Ethylmethylhydroxypyridine succinate.
Composition for 1 ml of solution:
- active substance: ethylmethylhydroxypyridine succinate - 50 mg;
- auxiliary component: water for injection.
Composition for 1 tablet:
- active substance: ethylmethylhydroxypyridine succinate - 125 mg;
- auxiliary components: lactose monohydrate, microcrystalline cellulose (MCC 101), croscarmellose sodium, povidone K30, magnesium stearate;
- film casing: Opadray II 33G280000 white (macrogol, titanium dioxide, hypromellose, lactose monohydrate, triacetin).
Pharmacological properties
Pharmacodynamics
Ethylmethylhydroxypyridine succinate belongs to the class of 3-hydroxypyridines, is an inhibitor of free radical processes, membrane protector. It has antihypoxic effect and increases the body's resistance to stress.
The mechanism of its action is due to antioxidant and membrane-protective efficacy. By inhibiting lipid peroxidation of ethylmethylhydroxypyridine, succinate potentiates the activity of superoxide oxidase, improves the ratio of lipids to proteins, modifies the structure and activates the function of the cell membrane. Models the activity of enzymes associated with the membrane (adenylate cyclase, calcium-independent phosphodiesterase, acetylcholinesterase), receptor complexes (acetylcholine, benzodiazepine, GABA-benzodiazepine), increasing their ability to bind to ligands, which contributes to the preservation of the structural and functional organization of biological and transport of neurotransmitters. Increases the content of dopamine in the brain. It causes an increase in the compensatory activation of aerobic glycolysis,a decrease in the Krebs cycle in the degree of inhibition of oxidative processes during hypoxia with an increase in the concentration of ATP (adenosine triphosphoric acid) and creatine phosphate, stimulates the energy-synthesizing functions of mitochondria.
Ethylmethylhydroxypyridine succinate in patients with such pathological conditions as cerebrovascular accident, hypoxia and ischemia, intoxication with antipsychotic drugs, ethanol, increases the body's resistance to the negative effects of various damaging factors.
With a critical decrease in coronary blood flow, it plays a stabilizing role in the structural and functional organization of the cell membranes of cardiomyocytes, stimulates the activity of such membrane enzymes as adenylate cyclase, acetylcholinesterase, phosphodiesterase. Supports the activation of acetylcholinesterase and aerobic glycolysis, which develops during acute ischemia. Promotes the resumption of redox processes in mitochondria under conditions of hypoxia, enhances the synthesis of creatine phosphate and ATP. In the ischemic myocardium, it maintains physiological functions and the integrity of morphological structures, improves the clinical symptoms of myocardial infarction, increases the effectiveness of concomitant treatment, and reduces the incidence of arrhythmias and cardiac arrhythmias. Normalizes metabolic processes in the ischemic myocardium,increases the antianginal effect of nitrates, in the case of acute coronary insufficiency relieves the effects of reperfusion syndrome, improves rheological parameters of blood.
In patients with progressive neuropathy developing as a result of chronic ischemia and hypoxia, the drug helps to preserve the fibers of the optic nerve and retinal ganglion cells, improving their functional activity and enhancing visual acuity.
Ethylmethylhydroxypyridine succinate in acute pancreatitis relieves the symptoms of endogenous intoxication syndrome and enzymatic toxemia.
Improves blood supply to the brain, enhances metabolism, normalizes microcirculation and restores blood rheological parameters, reduces platelet aggregation. It stabilizes the cell membranes of the main blood elements (platelets and erythrocytes), preventing the development of hemolysis.
Due to a decrease in the level of total cholesterol and a decrease in the content of low density lipoproteins, it has a hypolipidemic effect.
Pharmacokinetics
- absorption: ethylmethylhydroxypyridine succinate is absorbed quickly, with oral administration, the half-absorption period is 0.08–1 h. The maximum concentration (C max) with i / m administration of the substance at a dose of 400–500 mg varies from 2.5 to 4 μg / ml, with oral administration reaches 50-100 ng / ml. T Cmax (time required to reach C max) with intramuscular administration is 0.3–0.58 hours, with oral administration - 0.46–0.5 hours;
- distribution: the substance is quickly distributed in organs and tissues. When administered intramuscularly, the average retention time in the body is 0.7–1.3 hours, with oral administration - 4.9–5.2 hours;
- metabolism: ethylmethylhydroxypyridine succinate is biotransformed in the liver through glucuronidation. In total, 5 of its metabolites are known: the first, 3-hydroxypyridine phosphate, under the influence of alkaline phosphatase, is split into 3-hydroxypyridine and phosphoric acid; the second - is formed in large quantities, is pharmacologically active, 1–2 days after application of the drug is found in urine; the third - in large quantities is excreted in the urine; the fourth and fifth metabolites are glucurone conjugates;
- excretion: the half-life (T 1/2) after oral administration is 4.7–5 hours. After intramuscular administration, the substance is rapidly and almost completely excreted from the blood plasma within 4 hours. Eliminated in the urine: in 12 hours as metabolites displayed up to 50%, unchanged - about 0.3%. The level of excretion in the urine of both the unchanged drug and its metabolites is characterized by significant individual variability.
Indications for use
A solution for i / v and i / m administration of Ethylmethylhydroxypyridine succinate is used as part of the complex therapy of the following conditions and diseases:
- traumatic brain injury, consequences of traumatic brain injury;
- acute violation of cerebral circulation;
- neurocirculatory (vegetative-vascular) dystonia;
- encephalopathy;
- mild cognitive impairment of vascular origin;
- acute myocardial infarction (from the first day);
- anxiety disorders as a consequence of neurotic and neurosis-like pathologies;
- primary open-angle glaucoma (at various stages);
- alcohol withdrawal syndrome with a predominance of vegetative-vascular and neurosis-like disorders (for relief);
- acute poisoning with neuroleptics;
- acute purulent-inflammatory lesions of the abdominal cavity, including peritonitis and acute necrotizing pancreatitis.
Indications for use for Ethylmethylhydroxypyridine succinate in the form of film-coated tablets:
- consequences of acute disorders of cerebral circulation, including the period after transient ischemic attacks, preventive therapy in the phase of subcompensation;
- mild traumatic brain injury, consequences of traumatic brain injury;
- neurocirculatory (vegetative-vascular) dystonia;
- encephalopathy of various etiology and pathogenesis (post-traumatic, dysmetabolic, dyscirculatory, mixed);
- mild cognitive impairment of vascular origin;
- anxiety disorders as a consequence of neurotic and neurosis-like pathologies;
- ischemic heart disease (as part of complex treatment);
- alcohol withdrawal syndrome with a predominance of vegetative-vascular and neurosis-like disorders (for relief), post-withdrawal disorders;
- conditions after acute poisoning with neuroleptics;
- asthenia, prevention of the development of somatic diseases under the influence of extreme loads and negative factors;
- the influence of extreme (stress-forming) factors.
Contraindications
Absolute:
- acute hepatic / renal failure;
- children and adolescence;
- pregnancy;
- breast-feeding;
- lactase deficiency, lactose (fructose) intolerance, glucose-galactose malabsorption - for tablets;
- individual hypersensitivity to the main and auxiliary components in the preparation.
With caution, all forms of release of ethylmethylhydroxypyridine succinate are used if there is a history of allergic diseases and reactions, including sulfites.
Ethylmethylhydroxypyridine succinate, instructions for use: method and dosage
The dose, frequency of use and duration of therapy are set in each case individually and depend on the indications and the clinical situation.
Solution for intramuscular or intravenous administration
A solution of ethylmethylhydroxypyridine succinate is administered intramuscularly or intravenously (jet or drip).
For the infusion method of administration, the solution is additionally diluted in 0.9% NaCl solution.
Administration time: jet (slow) - 5-7 minutes; drip - 40-60 drops / min.
The maximum daily dose is 1200 mg.
Recommended dosage of ethylmethylhydroxypyridine succinate:
- acute disorders of cerebral circulation: the first 10-14 days - intravenous drip of 200-500 mg 2-4 times / day, then in / m 200-250 mg 2-3 times / day; course - 2 weeks;
- traumatic brain injury, the consequences of traumatic brain injury: intravenous drip, 200-500 mg 2-4 times / day; course - 10-15 days;
- discirculatory encephalopathy in the phase of decompensation: intravenous stream or drip at a dose of 200-500 mg 1-2 times / day for 14 days; then within 2 weeks i / m at 100–250 mg / day;
- discirculatory encephalopathy (course prophylaxis): i / m in a dose of 200–250 mg 2 times / day; course - 10-14 days;
- neurocirculatory dystonia, neurotic and neurosis-like states: intramuscularly, 50-400 mg / day; course - 14 days;
- mild cognitive impairment in anxiety disorders and in elderly patients: intramuscularly at a dose of 100–300 mg / day; course - 14-30 days;
- acute myocardial infarction: against the background of standard treatment, including anticoagulant and antiplatelet agents, β-blockers, nitrates, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, as well as symptomatic drugs according to indications, Ethylmethylhydroxypyridine in / out / in 14 days. The first 5 days, in order to achieve the maximum effect, the solution is injected into a vein, then for 9 days it is allowed to be injected intramuscularly. The IV drug is administered by slow drip infusion to avoid side effects. For infusion administration, the solution is diluted in 100-150 ml of 0.9% NaCl solution or 5% glucose (dextrose) solution and injected for 30-90 minutes. If necessary, a slow jet injection of the solution with a duration of at least 5 minutes is allowed. Injections or infusions are performed 3 times / day, every 8 hours. The daily therapeutic dose is 6-9 mg / kg of body weight, a single dose is 2-3 mg / kg, while the maximum daily dose should not be more than 800 mg, a single dose is 250 mg;
- primary open-angle glaucoma at different stages (as part of a combination treatment): i / m, 100-300 mg / day, respectively 1-3 times / day; course - 14 days;
- alcohol withdrawal syndrome: 200–500 mg intravenously or intramuscularly 2–3 times / day; course - 5-7 days;
- acute intoxication with neuroleptics: 200–500 mg / day iv; course - 7-14 days;
- acute purulent-inflammatory lesions of the abdominal cavity, including peritonitis and acute necrotizing pancreatitis (on the first day in the preoperative and postoperative period, it is prescribed in a dose depending on the form / severity of the pathology, the prevalence of the process, the clinical course of the disease; canceled gradually, after reaching a stable positive clinical -laboratory effect): acute edematous (interstitial) pancreatitis - 200-500 mg 3 times / day intravenously (in 0.9% NaCl solution) and intramuscularly; necrotizing pancreatitis of mild severity - 100-200 mg 3 times / day intravenously (in 0.9% NaCl solution) and intramuscularly; necrotizing pancreatitis of moderate severity - 200 mg 3 times / day IV drip (in 0.9% NaCl solution); severe necrotizing pancreatitis - on the first day, 800 mg, divided into 2 injections;then 200-500 mg 2 times / day with a gradual decrease in the daily dose; extremely severe necrotizing pancreatitis - the initial dose is 800 mg / day until persistent relief of the symptoms of pancreatogenic shock, with stabilization of the condition - 300-500 mg 2 times / day intravenously (in 0.9% NaCl solution) with a gradual decrease in the daily dose …
Film-coated tablets
Ethylmethylhydroxypyridine succinate tablets are taken orally.
Recommended dosage: 125–250 mg (1–2 tablets) 3 times / day. The maximum daily dose should not exceed 800 mg (6 tablets).
The duration of therapy is from 2 to 6 weeks. The duration of treatment for the relief of alcohol withdrawal is 5-7 days.
Treatment should be discontinued gradually, decreasing the dose over 2-3 days.
The initial dose (125-250 mg 1-2 times / day) is gradually increased until a stable therapeutic effect is obtained.
The duration of a therapeutic course for ischemic heart disease should be at least 1.5–2 months. On the recommendation of a doctor, it is possible to carry out repeated courses, which are desirable to be carried out in the spring-autumn periods.
Side effects
With parenteral administration of a solution of ethylmethylhydroxypyridine succinate, the following undesirable reactions from systems and organs may develop:
- digestive system: dryness of the oral mucosa or metallic taste in the mouth, nausea, flatulence, diarrhea;
- nervous system: violation of falling asleep, drowsiness;
- respiratory system: chest discomfort, sore throat, feeling of lack of air (associated, as a rule, with a high rate of administration of the solution, is of a short-term nature);
- cardiovascular system: a short increase in blood pressure;
- others: a feeling of spreading heat throughout the body, an unpleasant odor, allergic reactions.
When taking the tablets, gastrointestinal disturbances can develop in the form of dry mouth, nausea, diarrhea, as well as drowsiness and allergic reactions.
Overdose
Due to the low toxicity of ethylmethylhydroxypyridine succinate, overdose is unlikely.
With intoxication, symptoms such as sleep disorders (insomnia or drowsiness) may develop; with intravenous administration - a short-term (1.5-2 hours) slight increase in blood pressure.
Patients, as a rule, do not need therapy, since the symptoms disappear on their own within 24 hours. For severe insomnia, it is recommended that one of the hypnotics and anxiolytics be administered orally, for example, oxazepam - 10 mg, nitrazepam - 10 mg, or diazepam - 5 mg.
An excessive increase in blood pressure with parenteral administration of the solution may require taking antihypertensive drugs and controlling blood pressure.
special instructions
In predisposed patients, especially those with bronchial asthma and hypersensitivity to sulfites, in some cases, severe allergic reactions may develop.
Influence on the ability to drive vehicles and complex mechanisms
Since the use of ethylmethylhydroxypyridine succinate can cause adverse reactions such as drowsiness, it is important to be careful during therapy when driving and engaging in other potentially hazardous activities that require increased concentration and high speed of psychomotor reactions.
Application during pregnancy and lactation
In experimental studies, the teratogenic, mutagenic and embryotoxic effects of ethylmethylhydroxypyridine succinate were not revealed. There have been no strictly controlled clinical studies of the safety of its use during gestation and breastfeeding.
It is contraindicated to use Ethylmethylhydroxypyridine succinate for the treatment of pregnant and breastfeeding women due to insufficient data on the effectiveness and safety of its use during these periods.
Pediatric use
In pediatric practice, the use of ethylmethylhydroxypyridine succinate for the treatment of patients under 18 years of age is contraindicated due to insufficient knowledge of its effect on children and adolescents.
With impaired renal function
It is contraindicated to prescribe ethylmethylhydroxypyridine succinate in patients with acute renal failure.
For violations of liver function
It is contraindicated to prescribe the drug to patients with acute hepatic failure.
Use in the elderly
Elderly patients do not require dosage adjustment.
Drug interactions
Ethylmethylhydroxypyridine succinate enhances the effect of antiepileptic drugs (carbamazepine), benzodiazepine anxiolytics and antiparkinsonian drugs (levodopa).
The drug reduces the toxic effect of ethyl alcohol.
Analogs
The analogues of Ethylmethylhydroxypyridine succinate are MEXellara, Meksiprim, Medomeksi, Meksidant, Meksidol, Meksilek-Lekpharm, Meksidol Forte 250, Meksikor, Meksifin, MetucinVel, Metostabil, Neurox, Neurocard, Ethylmethylhydroxypyridine and dr.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a place protected from light. Keep out of the reach of children.
Shelf life: tablets - 2 years; solution - 0.5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about ethylmethylhydroxypyridine succinate
Since there are no reviews on Ethylmethylhydroxypyridine succinate on specialized sites and forums, there is no way to assess the efficacy and safety of this drug.
Price for ethylmethylhydroxypyridine succinate in pharmacies
Since the drug is not available for sale, the price of Ethylmethylhydroxypyridine succinate is unknown.
The cost of some drugs containing a similar active ingredient: Mexiprim, film-coated tablets, 125 mg, packaging of 60 pcs. - 269–326 rubles; Neurox, solution for intravenous and intramuscular injection, 50 mg / ml, pack of 10 ampoules, 2 ml each - 223-318 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
