MEDICAL INSTRUCTIONS FOR USE
Trade name of the drug: Sevacitol®
Active substance (INN): Ethylmethylhydroxypyridine succinate
Pharmaceutical form: solution for injection
Contents per 1 ml:
Active substance: Ethylmethylhydroxypyridine succinate-50 mg
Excipients: sodium metabisulfite, water for injection.
Description: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group: Antioxidant agent.
ATX code: N07XX
It has antihypoxic, membranoprotective, nootropic, anticonvulsant, anxiolytic effect, increases resistance to stress. The drug increases the body’s resistance to the effects of major damaging factors, to oxygen-dependent pathological states (shock, hypoxia and ischemia, cerebral circulation disorders, intoxication with alcohol and antipsychotic drugs (neuroleptics).
The drug improves cerebral metabolism and blood supply to the brain, improves microcirculation and blood rheological properties, reduces platelet aggregation. Stabilizes membrane structures of blood cells (erythrocytes and platelets) in hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL. It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
The mechanism of action of the drug is due to its antihypoxant, antioxidant and membrane-protective effects. It inhibits lipid peroxidation processes, increases superoxide dismutase activity, increases lipid-protein ratio, reduces membrane viscosity and increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which increases their ability to bind to ligands, helps maintain the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission. The drug increases dopamine content in the brain. Causes enhancement of compensatory activity of aerobic glycolysis and reduction of the degree of inhibition of oxidative processes in the Krebs cycle under hypoxia, with an increase in ATP, creatine phosphate and activation of energy-synthesizing functions of mitochondria, stabilization of cell membranes. The drug normalizes metabolic processes in ischemic myocardium, reduces the zone of necrosis, restores and improves myocardial electrical activity and contractility, as well as increases coronary blood flow in the ischemic area, reduces the effects of reperfusion syndrome in acute coronary failure.
Time to reach maximum concentration (Tmax) – 0.45-0.5 h. Cmax when 400-500 mg dose is administered is 3.5-4.0 mcg/ml.
When administered intravenously, it is determined in plasma for 4 hours after injection. The drug rapidly passes from the bloodstream to organs and tissues and is rapidly eliminated from the body. Time retention time (MRT) is 0.7-1.3 hours.
The drug is eliminated mainly with urine, mainly in glucuron conjugated form and in small amounts unchanged.
Indications for use
- Acute disorders of cerebral circulation;
- craniocerebral trauma, consequences of craniocerebral injuries;
- discirculatory encephalopathy;
- vegetative dystonia syndrome;
- Mild cognitive disorders of atherosclerotic genesis;
- Anxiety disorders in neurotic and neurosis-like conditions;
- Acute myocardial infarction (from the first day) as part of the treatment;
- Primary open-angle glaucoma of different stages, as part of complex therapy;
- acute intoxication with antipsychotic drugs;
- acute pyo-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) as part of the treatment.
Methods of administration and dosage
The drug is administered v/m or intravenously (by stream or dropwise). When administering by infusion the drug should be diluted in 0.9% sodium chloride solution. The drug shall be administered by jetting slowly for 5-7 minutes, by drip infusion at a rate of 40-60 drops/min. The maximum daily dose should not exceed 1200 mg.
In acute cerebral circulation disorders the drug is administered in the first 10-14 days by IV drops 200-500 mg 2-4 times daily, then by IV drops 200-250 mg 2-3 times daily for 2 weeks. In case of craniocerebral trauma and craniocerebral injuries sequelae the drug is used for 10-15 days by IV drip 200-500 mg 2-4 times per day.
In decompensated dyscirculatory encephalopathy the drug should be administered by IV streaming or dropwise in a dose of 200-500 mg 1-2 times per day for 14 days, then by IM 100-250 mg per day during next 2 weeks.
For course prophylaxis of discirculatory encephalopathy the drug is administered in a monthly dose of 200-250 mg 2 times per day for 10-14 days.
In mild cognitive impairment in elderly patients and in cases of anxiety disorders the drug is administered in a daily dose of 100-300 mg/m for 14-30 days.
In acute myocardial infarction, as part of complex therapy, the drug is administered v/v or intravenously for 14 days against the background of traditional therapy of myocardial infarction, including nitrates, beta-adrenoblockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic drugs according to indications.
In the first 5 days, to achieve maximum effect, the drug should be administered v/v, in the next 9 days the drug may be administered v/m.
The preparation is administered intravenously by drop infusion, slowly (in order to avoid side effects) using 0.9% sodium chloride solution or 5% dextrose (glucose) solution in the amount of 100-150 ml in 30-90 minutes. If necessary, slow trickle administration of the drug for at least 5 min is possible.
The drug is administered (intravenously or intramuscularly) 3 times/day every 8 hours. The daily therapeutic dose is 6-9 mg/kg of body weight/day, single dose – 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose – 250 mg.
In open angle glaucoma of various stages the drug is administered as part of complex therapy intravenously in 100-300 mg/day 1-3 times/day for 14 days.
In acute intoxication with antipsychotic drugs the drug is administered in an IV dose of 200-500 mg/day for 7-14 days.
In acute pyo-inflammatory processes of abdominal cavity (acute necrotizing pancreatitis, peritonitis) the drug is prescribed in the first day, both in preoperative and in postoperative period. Administered doses depend on the form and severity of the disease, process prevalence, variants of the clinical course. Withdrawal of the drug should be carried out gradually.
In acute edematous (interstitial) pancreatitis drug is prescribed 200-500 mg 3 times per day by IV drops (in 0.9% sodium chloride solution) and intravenously.
Mild degree of necrotic pancreatitis severity – 100-200 mg 3 times per day by IV drops (in 0.9% sodium chloride solution) and intravenously.
Moderate severity of necrotic pancreatitis – 200 mg 3 times/day by IV drip (in 0.9% sodium chloride solution).
A severe course of necrotic pancreatitis – in pulse dosage of 800 mg during the first day, twice daily, further – 200-500 mg 2 times per day with gradual decrease of daily dose.
Extremely severe necrotic pancreatitis – initial dose is 800 mg per day until symptoms of pancreatogenic shock are relieved; after stabilization, the daily dose is reduced gradually by 300-500 mg twice a day by IV drip (in 0.9% sodium chloride solution).
Nausea and dry mouth, drowsiness and allergic reactions are possible.
- Acute liver dysfunction;
- acute renal dysfunction;
- Individual hypersensitivity to the drug.
Strictly controlled clinical studies on the safety of the drug in children and during pregnancy and lactation have not been conducted.
Increases the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa). Reduces the toxic effects of ethyl alcohol.
In individual cases, especially in predisposed patients with bronchial asthma with hypersensitivity to sulfites, severe hypersensitivity reactions may develop.
In case of overdose, drowsiness may develop.
Form of production
Solution for injection 50 mg/ml 2 ml, 5 ml, #5 #10(2×5,1×10) (ampoules).
Store in a dry, dark place at temperatures under 25°C. Keep out of the reach of children!
2 years. Do not use after the expiration date.
Conditions for dispensing from pharmacies
Released by a doctor’s prescription.