Product Overview
Composition
1 ml:
- ethylmethylhydroxypyridine succinate 50 mg
Excipients:
Water for injections.
pharmachologic effect
Mexiprim® is an inhibitor of free radical processes, membrane protector with antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic effects.
The drug increases the body's resistance to the effects of various damaging factors (shock, hypoxia and ischemia, cerebrovascular accident, alcohol intoxication and antipsychotic drugs (neuroleptics).
The mechanism of action of Mexiprim® is due to its antioxidant and membrane-protective action.
It inhibits lipid peroxidation, increases the activity of superoxide oxidase, increases the lipid-protein ratio, reduces the viscosity of the membrane, and increases its fluidity.
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, helps preserve the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission.
Mexiprim® 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 hypoxic conditions with an increase in the content of ATP and creatine phosphate, activation of the energy-synthesizing functions of mitochondria, and stabilization of cell membranes.
The drug improves metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation.
It stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis. It has a hypolipidemic effect, reduces the content of total cholesterol and LDL.
Pharmacokinetics:
When administered intramuscularly, the drug is determined in blood plasma for 4 hours after administration. Tmax is 0.45–0.50 hours. Cmax at doses of 400–500 mg is 3.5–4.0 μg / ml.
Mexiprim® quickly passes from the bloodstream to organs and tissues and is quickly eliminated from the body. The retention time of the drug (MRT) is 0.7-1.3 hours.
Mexiprim® is excreted in the urine, mainly in the glucuronoconjugated form and in small amounts unchanged.
Mexiprim® is rapidly absorbed from the gastrointestinal tract with a half-absorption period of 0.08–0.1 hours. Tmax in blood plasma is 0.46–0.5 hours. The value of Cmax of Mexiprim® in blood plasma is in the range from 50 to 100 ng / ml.
T1 / 2 of Mexiprim® and the average retention time of the drug in the body are 4.7-5 hours and 4.9-5.2 hours, respectively. Mexiprim® in the human body is extensively metabolized to form its glucuronoconjugated product.
On average, for 12 hours, 0.3% of the drug is excreted in the urine - unchanged and 50% - in the form of glucuronoconjugate (of the administered dose).
The most intense Mexiprim® and its glucuronoconjugate are excreted during the first 4 hours after taking the drug.
The indicators of excretion in the urine of Mexiprim® and its conjugated metabolite have significant individual variability.
Indications
- Common to both dosage forms:
vegetative dystonia;
anxiety disorders in neurotic and neurosis-like states;
relief of withdrawal symptoms in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;
- Solution for intravenous and intramuscular administration (optional):
acute violation of cerebral circulation;
encephalopathy;
mild cognitive disorders of atherosclerotic genesis.
- Tablets (optional):
mild cognitive disorders of various origins (with psychoorganic syndrome and asthenic disorders caused by acute and chronic disorders of cerebral circulation, TBI,
neuroinfections and intoxications, senile and atrophic processes);
memory disorders and intellectual disability in the elderly;
exposure to extreme (stress) factors.
Contraindications
Acute hepatic and / or renal failure, increased individual sensitivity to the drug.
Childhood, pregnancy, breastfeeding - due to insufficient knowledge of the effect of the drug in these categories of patients.
Side effects
The appearance of individual side reactions is possible: nausea and dryness of the oral mucosa, drowsiness, allergic reactions.
Interaction
Compatible with psychotropic drugs.
Strengthens the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa), reduces the toxic effect of ethyl alcohol.
How to take, course of administration and dosage
Mexiprim is prescribed intramuscularly or intravenously (jet or drip). Doses are selected individually. When administered by infusion, the drug should be diluted in physiological sodium chloride solution.
Treatment is started with a dose of 50-100 mg 1-3 times a day, gradually increasing the dose until a therapeutic effect is obtained.
Jet Mexiprim is injected slowly over 5-7 minutes, drip - at a rate of 40-60 drops per minute. The maximum daily dose does not exceed 800 mg.
In case of acute disorders of cerebral circulation, Mexiprim is used in complex therapy in the first 2-4 days by intravenous drip of 200-300 mg once a day, then intramuscularly at 100 mg 3 times a day. The duration of treatment is 10-14 days.
In case of discirculatory encephalopathy in the decompensation phase, Mexiprim should be administered intravenously by jet or drip at a dose of 100 mg 2-3 times a day for 14 days.
Then the drug is injected intramuscularly at 100 mg 2-3 times a day for the next 2 weeks. For the course prevention of discirculatory encephalopathy, the drug is administered intramuscularly at a dose of 100 mg 2 times a day for 10-14 days.
For mild cognitive impairments in elderly patients and for anxiety disorders, the drug is used intramuscularly in a daily dose of 100-300 mg per day for 14-30 days.
In case of alcohol withdrawal syndrome, Mexiprim is administered in a dose of 100-200 mg intramuscularly 2-3 times a day or intravenously drip 1-2 times a day for 5-7 days.
In case of acute intoxication with antipsychotic drugs, the drug is administered intravenously at a dose of 50-300 mg per day for 7-14 days.
Overdose
Symptoms:
sleep disturbance (insomnia, in some cases - drowsiness).
Treatment:
usually not required - symptoms disappear on their own within 24 hours.
In severe cases of insomnia, sleeping pills are recommended.
Appointment
Description
Functional features
The maximum plasma concentration of Mexiprim is in the range from 50 to 100 ng / ml.
The half-life of Mexiprim and the average retention time of the drug in the body are 4.7-5.0 hours and 4.9-5.2 hours, respectively.
Mexiprim in the human body is extensively metabolized to form its glucuronoconjugated product.
On average, 0.3% of the unchanged drug and 50% of the administered dose are excreted in the urine over 12 hours.
The most intense Mexiprim and its glucuronoconjugate are excreted during the first 4 hours after taking the drug.
Indicators of excretion in the urine of Mexiprim and its conjugated metabolite have significant individual variability.
Result
Mexiprim® belongs to heteroaromatic antioxidants.
Has a wide range of pharmacological activity: increases the body's resistance to stress, exhibits anxiolytic effect, not accompanied by drowsiness and muscle relaxant effect; possesses
nootropic properties, prevents and reduces learning and memory disorders arising from aging and exposure to various pathogenic factors; has an anticonvulsant effect; exhibits
antioxidant and antihypoxic properties; increases concentration and performance; weakens the toxic effect of alcohol. The drug improves the metabolism of brain tissues and their blood supply, improves microcirculation and rheological properties of blood, reduces platelet aggregation.
It stabilizes the membrane structures of blood cells (erythrocytes and platelets). It has a hypolipidemic effect, reduces the content of total cholesterol and low density lipoproteins.
The mechanism of action of Mexiprim is due to its antioxidant and membrane-protective action.
It inhibits lipid peroxidation, increases the activity of superoxide oxidase, increases the lipid-protein ratio, reduces the viscosity of the membrane, and increases its fluidity.
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, helps preserve the structural and functional organization of biomembranes, transport neurotransmitters and improve synaptic transmission.
Mexiprim 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 hypoxic conditions with an increase in the content of ATP and creatine phosphate, activation of the energy-synthesizing functions of mitochondria, and stabilization of cell membranes.
Equipment
Solution for intravenous and intramuscular administration of 50 mg / ml. Manufactured at FSUE "Moscow Endocrine Plant", Russia 2 ml or 5 ml per ampoule of neutral glass grade NS-3 or imported.
5 ampoules in a blister strip made of polyvinyl chloride film and aluminum foil.
1, 2 or 3 blister packs with instructions for medical use of the drug, with a knife or ampoule scarifier are placed in a carton box.
For hospitals, 6, 12, 20, 50 or 100 blisters with foil with 3, 6, 10, 25 or 50 instructions for medical use of the drug, knives or ampoule scarifiers are placed in a cardboard box or in corrugated cardboard boxes.
When packing ampoules with notches, rings or break points, scarifiers or ampoule knives are not inserted.
During production at OOO NTFF Polisan, Russia 2 ml or 5 ml in ampoules of neutral glass of NS-3 brand or imported, or ampoules of brown glass.
5 ampoules in a blister strip from a polyvinyl chloride film, or from a polyvinyl chloride film and aluminum foil, or a polyvinyl chloride film and a cover film.
1, 2 or 3 blister packs with instructions for medical use of the drug, with a knife or ampoule scarifier are placed in a carton box.
For hospitals, 6, 12, 20, 50 or 100 blisters with foil or cover film, respectively, with 6, 12, 20, 50 or 100 instructions for the medical use of the drug, with knives or ampoule scarifiers are placed in a cardboard box or in boxes made of corrugated cardboard.
When packing ampoules with notches, rings or break points, scarifiers or ampoule knives are not inserted.
Special instructions
The degree of restrictions is determined by the individual tolerance of the drug.
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
Release form
Solution for intravenous and intramuscular use 50 mg / ml.
