Composition and release form
Active ingredient: ethylmethylhydroxypyridine succinate – 50 mg. Excipients: sodium metabisulfite – 0.4 mg; water for injections up to 1 ml. Solution for intravenous and intramuscular administration 50 mg/ml in colorless or light-protective glass ampoules with a blue break point or a white break point and three marking rings (top - yellow, middle - white, bottom - red) 2 ml or 5 ml . 5 ampoules in a blister pack. 1 or 2 blister packs along with instructions for medical use in a cardboard pack. 4, 10 or 20 blister packs along with instructions for medical use in a box of cardboard (for hospitals).
pharmachologic effect
Antioxidant agent. Means for the correction of disorders in alcoholism, toxic and drug addiction.
Pharmacokinetics
With intramuscular administration, it is determined in the blood plasma for 4 hours after administration. The time to reach the maximum concentration Tmax is 0.45-0.5 hours. Cmax when administering a dose of 400-500 mg is 3.5-4.0 μg/ml. Mexidol quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. The drug retention time (MRT) is 0.7-1.3 hours. The drug is excreted mainly in the urine, mainly in glucurone-conjugated form and in small quantities unchanged.
Pharmacodynamics
It has antihypoxic, membrane-protective, nootropic, anticonvulsant, anxiolytic effects, and increases the body's resistance to stress.
The drug increases the body's resistance to the effects of major damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular accident, intoxication with alcohol and antipsychotic drugs (neuroleptics)). Mexidol improves cerebral metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, and reduces platelet aggregation. Stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis. The mechanism of action of Mexidol is due to its antihypoxic, antioxidant and membrane protective effects. It inhibits the processes of lipid peroxidation, increases the activity of superoxide dismutase, increases the 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 enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, transport of neurotransmitters and improve synaptic transmission.
Mexidol increases dopamine levels in the brain. Causes an increase in the compensatory activity 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, creatine phosphate and activation of the energy-synthesizing functions of mitochondria, stabilization of cell membranes. Mexidol normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Increases the antianginal activity of nitro drugs. Mexidol promotes the preservation of retinal ganglion cells and optic nerve fibers during progressive neuropathy, the causes of which are chronic ischemia and hypoxia. Improves the functional activity of the retina and optic nerve, increasing visual acuity.
Buy Mexifin solution intravenously and intramuscularly 50 mg/ml 2 ml No. 10 in pharmacies
Instructions for use Meksifin Buy Meksifin solution IV and IM 50 mg/ml 2 ml No. 10 Dosage forms solution for injection 50 mg/ml 2 ml Synonyms Medomexi Mexidant Mexidol Mexicor Mexiprim Neurox Cerecard Group Antioxidants International nonproprietary name Ethylmethylhydroxypyridine succinate Manufacturers Pharmaceutical protection SPC FMBA (Russia)
Composition 1 ml 1 amp. 2 ethyl-6-methyl-3-hydroxypyridine succinate 50 mg 100 mg Excipients: water d/i.
1 ml 1 amp. 2 ethyl-6-methyl-3-hydroxypyridine succinate 50 mg 250 mg Excipients: water d/i.
Pharmacological action An inhibitor of free radical processes is a membrane protector, which also has antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic effects. Belongs to the class of 3-hydroxypyridines.
The mechanism of action is due to antioxidant and membrane protective properties. Suppresses lipid peroxidation, increases superoxide oxidase activity, increases the lipid-protein ratio, improves the structure and function of the cell membrane.
Modulates the activity of membrane-bound enzymes (Ca2+-independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which promotes their binding to ligands, preservation of the structural and functional organization of biomembranes, transport of neurotransmitters and improvement of synaptic transmission. Increases the concentration of dopamine in the brain.
It enhances the compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in ATP and creatine phosphate, and activates the energy-synthesizing function of mitochondria.
Increases the body's resistance to the effects of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebrovascular accidents, intoxication with ethanol and antipsychotic drugs).
Improves metabolism and blood supply to 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.
It has a lipid-lowering effect, reduces the content of total cholesterol and LDL.
Improves the functional state of ischemic myocardium during myocardial infarction, the contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle.
In conditions of a critical decrease in coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes - PDE, adenylate cyclase, acetylcholinesterase. Supports the activation of aerobic glycolysis that develops during acute ischemia and promotes the restoration of mitochondrial redox processes under hypoxic conditions, increases the synthesis of ATP and creatine phosphate. Ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium.
Improves the clinical course of myocardial infarction, increases the effectiveness of therapy, accelerates the restoration of functional activity of the LV myocardium, reduces the incidence of arrhythmias and intracardiac conduction disorders. Normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and/or improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, increases the antianginal activity of nitro drugs, improves the rheological properties of blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency.
Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
Pharmacokinetics
Suction
Rapidly absorbed when taken orally (half-absorption period - 0.08-1 hour). TCmax with intramuscular administration - 0.3-0.58 hours, with oral administration - 0.46-0.5 hours. Cmax with intramuscular administration at a dose of 400-500 mg - 2.5-4 mcg/ml, with oral administration - 50-100 ng/ ml.
Distribution
Quickly distributed in organs and tissues. The average retention time of the drug in the body when administered intramuscularly is 0.7-1.3 hours, when taken orally - 4.9-5.2 hours.
Metabolism
Metabolized in the liver by glucuronidation. 5 metabolites have been identified: 3-hydroxypyridine phosphate - formed in the liver and, with the participation of alkaline phosphate, breaks down into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, formed in large quantities and found in urine 1-2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates.
Removal
T1/2 when taken orally - 4.7-5 hours. It is quickly excreted in the urine, mainly in the form of metabolites (50% in 12 hours) and in small quantities - unchanged (0.3% in 12 hours). The most intensive elimination occurs during the first 4 hours after taking the drug. Urinary excretion rates of unchanged drug and metabolites have significant individual variability.
Meksifin, indications for use: anxiety states in neurotic and neurosis-like conditions; vegetative-vascular dystonia; encephalopathy; mild cognitive disorders of atherosclerotic origin; acute cerebrovascular accidents (as part of combination therapy); withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders; acute intoxication with antipsychotic drugs; acute purulent-inflammatory processes in the abdominal cavity (including acute necrotizing pancreatitis, peritonitis (as part of complex therapy)); acute myocardial infarction from the first day (parenteral); IHD; complex therapy of ischemic stroke (orally) - as part of complex therapy. Contraindications: hypersensitivity; acute liver and/or kidney failure; pregnancy; lactation period; childhood. With caution: if you have a history of allergic diseases (for parenteral administration).
Use during pregnancy and lactation Contraindicated during pregnancy and lactation.
Method of administration and dose IM, IV (stream, for 5-7 minutes or drip, at a speed of 60 drops/min).
For infusion administration, dilute in 200 ml of 0.9% sodium chloride solution. The initial dose is 0.05-0.1 g 1-3 times a day with a gradual increase until a therapeutic effect is obtained. The maximum daily dose is 0.8 g.
In case of acute cerebrovascular accident - intravenous drip, 0.2-0.3 g 1 time / day in the first 2-4 days, then intramuscularly, 0.1 g 3 times / day.
For discirculatory encephalopathy (decompensation phase) - intravenously in a stream or drip, 0.1 g 2-3 times a day for 14 days, and then intramuscularly, 0.1 g for 14 days. For course prophylaxis of discirculatory encephalopathy - intramuscularly, 0.1 g 2 times a day for 10-14 days.
VSD, neurotic and neurosis-like conditions - intramuscularly, 0.05-0.4 g/day for 14 days.
For withdrawal syndrome - IM, 100-200 mg 2-3 times a day or IV drip, 1-2 times a day for 5-7 days.
For acute intoxication with antipsychotic drugs - 0.05-0.3 g/day intravenously for 7-14 days.
For mild cognitive disorders - 0.1-0.3 g/day intramuscularly for 14-30 days.
For purulent-inflammatory processes in the abdominal cavity (acute necrotizing pancreatitis, peritonitis) - on the first day in the preoperative and postoperative period. The dose depends on the form and severity of the disease, the extent of the process, and the clinical course.
The drug is discontinued gradually after stable clinical and laboratory improvement.
For acute edematous (interstitial) pancreatitis of mild severity - 0.1-0.2 g 3 times a day intravenously and intramuscularly; moderate severity - 0.2 g 3 times a day; in severe cases - intravenous drip, 0.8 g on the first day (divided into 2 injections), then - 0.3 g 2 times a day with a gradual decrease in the daily dose; extremely severe course - intravenous drip, 0.8 g/day until persistent relief of symptoms of pancreatogenic shock; after stabilization of the condition - 0.3-0.4 g 2 times a day with a gradual reduction in the daily dose.
For myocardial infarction - intravenously (in the first 5 days) and intramuscularly (the next 9 days) 3 times a day (every 8 hours). Daily dose - 6-9 mg/kg/day, single dose - 2-3 mg/kg. The maximum daily dose should not exceed 800 mg, single dose - 250 mg. IV is administered by infusion over 30-90 minutes in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose solution or by stream for at least 5 minutes.
For ischemic heart disease: orally, 100 mg 3 times a day. Course duration is at least 2 months; If necessary, it is possible to conduct repeated courses.
Side effects Nausea, dry mouth, diarrhea, drowsiness, allergic reactions.
With parenteral administration (especially intravenous jet): dryness, “metallic” taste in the mouth, sensations of “spreading warmth” throughout the body, unpleasant odor, sore throat and discomfort in the chest, feeling of lack of air (usually associated with excessive high speed of administration and are short-term in nature); with long-term use - nausea, flatulence; sleep disorders (drowsiness or difficulty falling asleep).
Special instructions During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Drug interactions Enhances the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates.
Reduces the toxic effects of ethanol.
Overdose Symptoms: sleep disturbances (insomnia, in some cases drowsiness); with intravenous administration - a slight and short-term (up to 1.5-2 hours) increase in blood pressure.
Treatment: usually not required. Symptoms disappear on their own within 24 hours. In severe cases of insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. If blood pressure is excessively increased, use antihypertensive drugs under blood pressure control.
Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Shelf life: 3 years.
Do not use after the expiration date stated on the package.
Indications for use of Mexidol
- acute cerebrovascular accidents;
- traumatic brain injury, consequences of traumatic brain injury;
- iscirculatory encephalopathy;
- autonomic dystonia syndrome;
- mild cognitive disorders of atherosclerotic origin;
- anxiety disorders in neurotic and neurosis-like conditions;
- acute myocardial infarction (from the first day) as part of complex therapy;
- primary open-angle glaucoma of various stages, as part of complex therapy;
- relief of withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;
- acute intoxication with antipsychotic drugs;
- acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) as part of complex therapy.
Mexidol dosage
IM or IV (stream or drip). When administered by infusion, the drug should be diluted in 0.9% sodium chloride solution.
Mexidol® is administered slowly over 5–7 minutes in a stream, and dropwise at a rate of 40–60 drops per minute. The maximum daily dose should not exceed 1200 mg.
For acute cerebrovascular accidents, Mexidol® is used in the first 10–14 days - 200–500 mg IV drip 2–4 times a day, then 200–250 mg IM 2–3 times a day for 2 weeks .
For traumatic brain injury and the consequences of traumatic brain injuries, Mexidol® is used for 10-15 days intravenously at a dose of 200–500 mg 2–4 times a day.
For dyscirculatory encephalopathy in the decompensation phase, Mexidol® should be prescribed intravenously in a stream or drip at a dose of 200–500 mg 1–2 times a day for 14 days. Then IM 100–250 mg/day over the next 2 weeks.
For a course of prophylaxis of discirculatory encephalopathy, the drug is administered intramuscularly at a dose of 200–250 mg 2 times a day for 10–14 days.
For mild cognitive impairment in elderly patients and anxiety disorders, the drug is used intramuscularly at a daily dose of 100–300 mg/day for 14–30 days.
In case of acute myocardial infarction, as part of complex therapy, Mexidol® is administered intravenously or intramuscularly for 14 days, against the background of traditional therapy for myocardial infarction, including nitrates, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulant and antiplatelet agents, as well as symptomatic means according to indications.
In the first 5 days, to achieve maximum effect, it is advisable to administer the drug intravenously; in the next 9 days, Mexidol® can be administered intramuscularly.
Intravenous administration of the drug is carried out by drip infusion, slowly (to avoid side effects) in a 0.9% sodium chloride solution or 5% dextrose (glucose) solution in a volume of 100–150 ml for 30–90 minutes. If necessary, a slow jet injection of the drug, lasting at least 5 minutes, is possible.
The drug is administered (intravenous or intramuscular) 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg/kg body weight per day, a single dose is 2-3 mg/kg body weight. The maximum daily dose should not exceed 800 mg, single dose - 250 mg.
For open-angle glaucoma of various stages, as part of complex therapy, Mexidol® is administered intramuscularly at 100–300 mg/day, 1–3 times a day for 14 days.
For alcohol withdrawal syndrome, Mexidol® is administered in a dose of 200–500 mg intravenously or intramuscularly 2–3 times a day for 5–7 days.
In case of acute intoxication with antipsychotic drugs, the drug is administered intravenously at a dose of 200-500 mg/day for 7-14 days. In acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis), the drug is prescribed on the first day both in the preoperative and postoperative periods. The administered doses depend on the form and severity of the disease, the prevalence of the process, and variants of the clinical course. The drug should be discontinued gradually only after a stable positive clinical and laboratory effect.
For acute edematous (interstitial) pancreatitis, Mexidol® is prescribed 200–500 mg 3 times a day, intravenously (in 0.9% sodium chloride solution) and intramuscularly. Mild severity of necrotizing pancreatitis - 100-200 mg 3 times a day intravenously (in 0.9% sodium chloride solution) and intramuscularly. Moderate severity - 200 mg 3 times a day intravenously (in 0.9% sodium chloride solution). Severe course - in a pulse dosage of 800 mg on the first day with a double dose regimen; then 200–500 mg 2 times a day with a gradual reduction in the daily dose. Extremely severe course - at an initial dosage of 800 mg/day until the manifestations of pancreatogenic shock are persistently relieved, after stabilization of the condition, 300-500 mg 2 times a day intravenously (in 0.9% sodium chloride solution) with a gradual decrease in the daily dosage.
Meksifin analogues and prices
Pharmacological action Mexifin has antioxidant, anticonvulsant, anxiolytic, antihypoxic, nootropic, stress-protective and membrane-stabilizing effects. The main component of the product is ethylmethylhydroxypyridine succinate (a compound of succinic acid and 3-hydroxypyridine). The drug inhibits the activity of free radicals, slows down the oxidative degradation of lipids and increases the antioxidant properties of enzymes. Under the influence of the drug, the structures of cell membranes are restored, regardless of the factor of damage. The drug restores neurotransmitter and synaptic transmission and increases dopamine levels. Mexifin improves metabolism in brain structures, its blood supply, and prevents constriction of precapillaries and arterioles. During therapy, normal formation of platelets and red blood cells is restored, blood rheology improves, and immunity increases. The use of the drug for atherosclerosis helps reverse atherosclerotic changes, reduce cholesterol and LDL levels. Meksifin increases the body's endurance and resilience in extreme oxygen-dependent conditions (shock, physical, emotional and mental stress, cerebrovascular accident, hypoxia, stress, ischemia), in case of poisoning with psychotropic drugs and alcohol-containing drinks. Indications for use Meksifin is indicated for use in acute cerebral disorders, vegetative-vascular dystonia, poisoning with antipsychotic drugs and discirculatory encephalopathy. The drug is recommended for use in cognitive disorders caused by atherosclerotic changes, generalized anxiety disorders accompanying neuroses and neurotic conditions. Mexifin is effectively used to eliminate symptoms of alcohol withdrawal with vegetative-vascular disorders and neurosis-like symptoms.
Method of administration Meksifin is intended for intravenous or intramuscular administration. When administered by infusion, the drug can be diluted in saline. solution. When using intravenous injection, Mexifin is administered slowly over 5–7 minutes. For each patient, the dose is selected individually, based on the recommended ones. Therapy begins with 1–2 ml 1–3 times/day, and the dose is increased until a lasting therapeutic effect is obtained. Do not exceed the maximum dose of 800 mg/day. For cerebrovascular pathologies, Meksifin is used intravenously at 200–300 mg/day. 2–4 days, then 0.1 g intramuscularly 3 times a day. Therapy is carried out for 10–14 days. For DEP, the drug is used intravenously, 2 ml 2–3 times a day. 14 days and another 2 weeks. IM 2 ml/day. For prophylaxis, Meksifin is administered intramuscularly, 2 ml 2 times a day for 2 weeks. For anxiety and cognitive disorders, the use of the drug intramuscularly at 2–6 ml/day is indicated. 14–30 days. For withdrawal symptoms, Mexifin is used intramuscularly, 2–4 ml 2–3 times/day. 5–7 days. To reduce the symptoms of acute intoxication with neuroleptics, Mexifin is used intravenously at 0.05–0.3 g/day. 1–2 weeks For VSD and neurotic disorders, Meksifin is administered at a dose of 50–400 mg/day for 14 days.
Side effects During therapy with Mexifin, the development of allergic reactions (rash, swelling, angioedema, urticaria) is possible. Infrequently, the administration of the drug causes nausea, dry mouth and drowsiness.
Contraindications Meksifin is prohibited from being administered to patients with allergies to the composition of the drug. The drug is prohibited for use in acute liver dysfunction and renal pathologies. The use of the solution is contraindicated for children.
Pregnancy It is prohibited to use Mexifin for the treatment of pregnant women. If therapy with Mexifin is necessary, breastfeeding should be avoided.
Drug interactions Mexifin prolongs and enhances the effect of benzodiazepines and anticonvulsant antiparkinsonian drugs. When treated with Mexifin, the toxic effects and consequences of consuming ethyl alcohol are reduced.
Overdose Exceeding the dose of Mexifin is manifested by increased side symptoms and increased drowsiness.
Release form Meksifin is available in the form of a medicinal solution of 50 mg of the main component in 1 ml, bottled in ampoules of 2 and 5 ml. The package consists of 5, 10, 20, 25, 40, 50 or 100 ampoules.
Storage conditions: In a dark place, up to +25 degrees Celsius.
The composition of Mexifin consists of ethyl methylhydroxypyridine succinate, supplemented with water for injection.
Pharmacological group Cardiovascular drugs Medicines that improve cerebral circulation
Nosological classification (ICD-10) Mild cognitive impairment (F06.7) Post-concussion syndrome (F07.2) Mental and behavioral disorders caused by alcohol consumption - withdrawal state (F10.3) Anxiety disorder, unspecified (F41.9) Transient transient cerebral ischemic attacks [attacks] and related syndromes (G45) Disorders of the autonomic nervous system (G90) Encephalopathy, unspecified (G93.4) Primary open-angle glaucoma (H40.1) Acute myocardial infarction (I21) Cerebral atherosclerosis (I67.2)
Active ingredient : ethylmethylhydroxypyridine succinate
ATX: N07XX
Manufacturer: Brand Pharma
Additional information about the manufacturer Country of manufacture – Russia.
Additionally, during the period of therapy with Mexifin, you should stop driving.
