Mexidol mnn name. Release form, composition and packaging. Chemical rational name
Mexidol belongs to the group of nootropics and improves metabolism in the brain. It acts directly on brain cells, protects them from oxygen starvation and from death as a result of ischemia.
The drug also delivers more oxygen from the blood to neurons, increasing the threshold for the generation of convulsive impulses in the brain. In the process of using Mexidol, a person quickly recovers memory and skills lost as a result of a stroke or transient ischemic attack, improves memory, reproduction, speech, as well as resistance to various stressful situations and intoxications.
Mexidol: Instructions for use
| Tradename | Mexidol(Mexidolum) |
| International name | Methylethylpyridinol succinate(Methylethylpyridinol succinate) |
| Active substance | ethylmethylhydroxypyridine succinate |
| Conditions for dispensing from pharmacies | By doctor's prescription |
| Best before date | 3 years |
| Storage conditions | List B. The drug should be stored in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C. |
| Pharmacological group | Antioxidant agent. Drugs for the treatment of diseases nervous system others (Other Nervous System Drugs). |
| pharmachologic effect |
|
Release forms
Mexidol tablets
Film-coated tablets from white to off-white with a creamy tint, biconvex, 30 or 50 tablets per package. On a cross section, 2 layers are visible: the inner (core) gray or gray with a creamy tint and the outer white or white with a creamy tint.
1 tablet contains:
active substance:
ethylmethylhydroxypyridine succinate 125 mg.
Excipients: lactose monohydrate 97.5 mg; povidone 25 mg; magnesium stearate 2.5 mg
film shell: Opadry II white - 7.5 mg (hypromellose - 3 mg, titanium dioxide - 1.875 mg, lactose monohydrate - 1.575 mg, polyethylene glycol (macrogol) - 0.6 mg, triacetin - 0.45 mg).
Packaging: Tablets 0.125 g in blister packaging, cardboard pack.
Injection
Mexidol in ampoules of 2 or 5 ml. - the solution is colorless or slightly yellowish, transparent. Solution for intravenous and intramuscular administration, 50 mg/ml.
1 ml. solution contains: active substance- ethylmethylhydroxypyridine succinate 50 mg., excipient - water for injection.
Package: 1 or 2 blister packs are placed in a cardboard pack; 4, 10 or 20 blister packs are placed in a pack of cardboard boxes.
Indications for use
Mexidol is proposed for the treatment of acute cerebrovascular accidents, dyscirculatory encephalopathy (a brain disease caused by chronic disorder cerebral circulation), vegetative-vascular dystonia (impaired vascular tone due to dysfunction of the autonomic nervous system), atherosclerotic disorders of brain function, to relieve withdrawal syndrome (to relieve the condition resulting from the sudden cessation of taking drugs or alcohol) in alcoholism and drug addiction, in others conditions accompanied by tissue hypoxia.
- acute cerebrovascular accident;
- encephalopathy;
- cardiopsychoneurosis;
- mild cognitive disorders of atherosclerotic origin;
- neurotic and neurosis-like conditions with anxiety syndrome;
- relief of withdrawal syndrome in alcoholism with the presence of clinical picture neurotic and vegetative-vascular disorders;
- acute intoxication antipsychotics(neuroleptics);
- acute purulent inflammatory processes abdominal cavity (acute pancreatitis, peritonitis) as part of complex therapy.
Pharmacodynamics
The drug has antihypoxic, membrane protective, nootropic, anticonvulsant, anxiolytic effects, and increases the body's resistance to stress. Mexidol increases the body's resistance to various damaging factors, oxygen-dependent pathological conditions(shock, hypoxia and ischemia, cerebrovascular accidents, intoxication with alcohol and antipsychotic drugs).
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 lipid-lowering effect, reduces the level of total cholesterol and LDL. Reduces enzymatic toxemia and endogenous intoxication during 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 oxidase, 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, neurotransmitter transport and improve synaptic transmission.
Mexidol increases dopamine levels in the brain. Causes an increase in 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, stabilization of cell membranes.
Pharmacokinetics
Rapidly absorbed when taken orally. When taken orally in doses of 400-500 mg Cmax is 3.5-4 µg/ml. Quickly distributed in organs and tissues. The average retention time of the drug in the body when taken orally is 4.9-5.2 hours.
Metabolized in the liver by glucuron conjugation. 5 metabolites have been identified: 3-hydroxypyridine phosphate - formed in the liver and with the participation ALP breaks down into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, formed in large quantities and is found in urine on the 1st-2nd days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates.
T1/2 when taken orally - 2-2.6 hours. It is quickly excreted in the urine, mainly in the form of metabolites and in small quantities unchanged. The most intensive elimination occurs during the first 4 hours after taking the drug. Rates of urinary excretion of unchanged drug and metabolites have individual variability.
Dosage regimen
Mexidol tablets
Orally, 125-250 mg 3 times a day; the maximum daily dose is 800 mg (6 tablets).
Duration of treatment - 2-6 week; for cupping alcohol withdrawal- 5-7 days. Treatment is stopped gradually, reducing the dose over 2-3 days.
Initial dose - 125-250 mg (1-2 tablets) 1-2 times a day with a gradual increase until therapeutic effect; the maximum daily dose is 800 mg (6 tablets).
Duration of therapy in patients IHD - at least 1.5-2 months. Repeated courses (on the recommendation of a doctor) are preferably carried out in the spring and autumn.
Injection
Mexidol is prescribed intramuscularly or intravenously (stream or drip). When administered by infusion, the drug should be diluted in an isotonic sodium chloride solution. Doses are selected individually. The recommended dose is 5-10 mg/kg per day depending on the condition. Mexidol is administered in a stream slowly over 5-7 minutes, drip-wise at a rate of 40-60 drops/min.
During treatment acute cerebrovascular accident Mexidol is used as part of complex therapy IV drip at a dose of 200-300 mg 2 times a day in the first 5-7 days, then IM 200-300 mg 2 times a day. The duration of treatment is 10-14 days.
At dyscirculatory encephalopathy in the decompensation phase Mexidol should be prescribed intravenously in a stream or drip at a dose of 200 mg 2-3 times a day for 14 days. Then the drug is administered intramuscularly at 200-300 mg/day over the next 2 weeks.
For course prevention of dyscirculatory encephalopathy the drug is administered intramuscularly (injections) at a dose of 200 mg 1-2 times a day for 10-14 days.
At mild cognitive impairment of atherosclerotic origin in elderly patients and with neurotic disorders with anxiety syndrome Mexidol is prescribed intramuscularly (injections) at a dose of 100-300 mg/day for 14-30 days.
At alcohol withdrawal syndrome Mexidol is administered in a dose of 200-300 mg IM (injections) 2 times a day or IV drip 1-2 times a day for 5-7 days.
At acute intoxication with antipsychotic drugs the drug is administered intravenously at a dose of 200-600 mg/day (up to 800 mg) for 7-14 days.
At acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) Mexidol is prescribed on the first day both in the preoperative and postoperative periods. The dose of the drug depends on the form and severity of the disease, the prevalence of the process, options clinical course. Discontinuation of the drug should be carried out gradually, only after a stable positive clinical and laboratory effect.
- At acute edematous (interstitial) pancreatitis Mexidol is prescribed 200-600 mg 2-3 times a day intravenously and intramuscularly.
- At necrotizing pancreatitis mild degree gravity the drug is prescribed 200-400 mg 2-3 times/day intravenously and intramuscularly;
- at necrotizing pancreatitis medium degree gravity- 200-600 mg 2-3 times/day intravenously;
- in case of severe process- on the first day, a pulse dose of 800 mg is prescribed, divided into two injections, then 300 mg 2 times a day with a gradual decrease daily dose;
- with extremely severe necrotizing pancreatitis- the initial dose is 800 mg/day until the manifestations of pancreatogenic shock are persistently relieved, when the condition stabilizes - 300-400 mg 2 times/day intravenously, with a gradual reduction in the daily dose.
Mexidol for children
The use of Mexidol in pediatrics is indicated for the treatment of purulent neuroinfections, traumatic brain injuries, as well as for emergency care in cases of childhood traumatic brain injuries (100 mg once).
For children, the drug should be prescribed by a doctor who will monitor the child throughout its use. There are no statistically reliable studies of the use of the drug in children. Local application in dental practice occurs without complications.
Side effect
From the outside digestive system:
rarely - nausea, dry mouth.
Rarely- allergic reactions.
Contraindications
- acute liver dysfunction;
- acute renal dysfunction;
- hypersensitivity to the drug.
Pregnancy and lactation
Mexidol is contraindicated during pregnancy and lactation ( breastfeeding) due to insufficient knowledge of the drug's effect.
special instructions
Patients with blood pressure more than 180/100 mmHg, a crisis course of arterial hypertension and severe affective instability require careful monitoring of blood pressure during Mexidol therapy.
The inclusion of Mexidol in complex therapy in patients who suffered acute cerebrovascular accident contributed to an increase in resistance to hypoxia and a decrease in the severity of clinical stroke syndromes.
The use of Mexidol in the complex treatment of acute pancreatitis significantly reduces the level of enzymatic toxemia and endogenous intoxication.
Mexidol has been shown to be highly effective using a combined route of administration for monotherapy of reactive arthritis.
Overdose
Due to the low toxicity of Mexidol, overdose is unlikely, and to date such cases have not been reported.
Drowsiness may develop.
Drug interactions
With simultaneous use, Mexidol enhances the effect of anxiolytics, benzodiazepine derivatives, antiparkinsonian and anticonvulsants.
Mexidol reduces the toxic effects of ethyl alcohol.
Mexidol price
Prices are indicated approximately as of November 2017, because differ in different pharmacies and cities.
Mexidol reviews
I drank Mexidol, and the effect was simply wonderful, right before my eyes I came out of a state of hysteria. I took pills and injections. Moreover, I am also picky, not every drug worked for me, and sometimes even had a paradoxical effect, but Maxidol had no side effects and was very effective.
I was injected with Mexidol. The reason was cerebrovascular insufficiency. The effect was amazing. My eyes immediately brightened, I began to hear better, my head became clearer, and my mood, however, somehow strangely lifted. But I clearly remember that this drug was sold on a separate special prescription with a special seal. So, it is better to give it as the doctor prescribed, so that the effect is not too strong.
Excellent pills for a stressed nervous system. From tablets are the best whatever came from dystonia. Does it help? Definitely! All the symptoms of VSD for me personally subsided. But, after the course of treatment most of symptoms will return. They praised both the cardiologist and the neurologist, i.e. The tablets are quite versatile. They are officially sold with a prescription, but almost everywhere they sell without it. I took the pills, I think the injections will be much better.
I understood from the reviews that Mexidol will help with impaired vegetative function, but does it help fight obsessive thoughts and conditions, or is that something completely different? It didn’t help me, but I only took 1 tablet a day. If you follow the recommended dosage, it may help. But in general intrusive thoughts, as I understand, this is again my “favorite” anxiety. Afobazole helps with it, 2 tablets a day are enough for me.
Instructions for medical use of the drug
MEXIDOL ®
Tradename
Mexidol ®
International nonproprietary name
Medicinalform
Solution for intravenous and intramuscular administration 50 mg/ml, 2 ml or 5 ml
Compound
1 ml of solution contains
active substance - ethylmethylhydroxypyridine succinate - 50 mg,
Excipients: sodium metabisulfite, water for injection
Description
Transparent colorless or slightly yellowish liquid
Pharmacotherapeutic group
Other drugs for the treatment of diseases of the nervous system.
ATX code N07XX
Pharmacological properties
Pharmacokinetics
When administered intramuscularly, the drug is detected in the blood plasma for 4 hours after administration. Time to reach maximum concentration is 0.45 - 0.50 hours. The maximum concentration at doses of 400 - 500 mg is 3.5 - 4.0 mcg/ml. Mexidol ® quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. The retention time (MRT) of the drug in the body is 0.7 - 1.3 hours. The drug is excreted from the body 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. Mexidol ® 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 lipid-lowering effect, reduces the level of total cholesterol and low-density lipoproteins (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, gamma-aminobutyric acid (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 transfers. Mexidol ® increases the content of dopamine 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 adenosine triphosphate (ATP), creatine phosphate and activation of the energy-synthesizing functions of mitochondria, stabilization of cell membranes.
Mexidol ® normalizes metabolic processes in ischemic myocardium, reduces the area of necrosis, restores and improves electrical activity and myocardial contractility, 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 fibers optic nerve with progressive neuropathy, the causes of which are chronic ischemia and hypoxia. Improves the functional activity of the retina and optic nerve, increasing visual acuity.
Indications for use
acute cerebrovascular accidents
traumatic brain injury, consequences of traumatic brain injury
encephalopathy
vegetative-vascular dystonia
mild cognitive impairment of atherosclerotic origin
anxiety disorders in neurotic and neurosis-like conditions
acute heart attack myocardium (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
Directions for use and doses
Intramuscularly or intravenously (stream or drip). When administered by infusion, Mexidol ® should be diluted in 0.9% sodium chloride solution. Mexidol ® is injected slowly over 5 - 7 minutes, drip - at a rate of 40 - 60 drops per minute. The maximum daily dose should not exceed 1200 mg.
At acute disorders cerebral circulation Mexidol ® is used in the first 10 - 14 days - intravenously drip 200 - 500 mg 2 - 4 times a day, then intramuscularly 200 - 250 mg 2 - 3 times a day for 2 weeks.
For traumatic brain injury and consequences of traumatic brain injury Mexidol ® is used intravenously for 10 - 15 days, 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 intramuscularly 100 - 250 mg per day over the next 2 weeks.
For course prophylaxis of dyscirculatory encephalopathy Mexidol ® 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 Mexidol ® is used intramuscularly in a daily dose of 100 - 300 mg per day for 14 - 30 days.
In 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 agents according to indications. In the first 5 days, to achieve maximum effect It is advisable to administer Mexidol ® intravenously; for the next 9 days, Mexidol ® can be administered intramuscularly. Intravenous administration of Mexidol ® is carried out by drip infusion, slowly (to avoid side effects) in a 0.9% sodium chloride solution or a 5% dextrose (glucose) solution in a volume of 100 - 150 ml for 30 - 90 minutes. If necessary, a slow stream injection of Mexidol ® is possible, lasting at least 5 minutes.
Administration of Mexidol ® (intravenous or intramuscular) is carried out 3 times a day, every 8 hours. The daily therapeutic dose is 6 - 9 mg per kg of body weight per day, a single dose is 2 - 3 mg per kg of 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 per 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 Mexidol ® is administered intravenously at a dose of 200 - 500 mg per day for 7 - 14 days.
In acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) Mexidol ® 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. Mexidol ® should be discontinued gradually only after a sustained 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 degree gravity 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 two-time administration 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 per day until persistent relief of the manifestations of pancreatogenic shock, upon 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.
Side effects
Nausea and dry mouth, metallic taste in the mouth
Drowsiness
Allergic reactions
Unpleasant odor, sore throat and chest discomfort.
Contraindications
Increased individual sensitivity to the drug
Acute liver and kidney dysfunction
Children's and adolescence up to 18 years old
Pregnancy, lactation period
Drug interactions
Enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa), nitrates. Reduces the toxic effects of ethyl alcohol.
special instructions
In some cases, especially in predisposed patients with bronchial asthma with increased sensitivity to sulfites, severe hypersensitivity reactions may develop.
Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms
Care should be taken when driving vehicles and potentially dangerous machinery.
Overdose
Symptoms: increased side effects.
Treatment: the drug is temporarily discontinued. Symptomatic treatment.
Release form and packaging
Solution 50 mg/ml in ampoules of 2 ml or 5 ml, clear or light-protective glass with a break point of blue color or with a white break point and three marking rings (top - yellow, middle - white, bottom - red). 5 ampoules each in a blister pack made of polyvinyl chloride film without aluminum foil coating. 1 (for ampoules of 5 ml) or 2 (for ampoules of 2 ml) blister packs together with instructions for medical use in the state and Russian languages are placed in a cardboard pack.
Mexidol ® , Ethylmethylhydroxypyridine succinate, Mexifin ® , Mexidant ® , Mexicor ® , Mexiprim ®
Dosage form
Chemical name
2-ethyl-6-methyl-3-hydroxypyridine succinate
pharmachologic effect
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 (Ca 2+ -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 functional state ischemic myocardium during myocardial infarction, 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 conditions of hypoxia, increases ATP synthesis 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 left ventricular 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
Rapidly absorbed when taken orally (half-absorption period - 0.08-1 hour). TCmax when administered intramuscularly - 0.3-0.58 hours, when administered orally - 0.46-0.5 hours. Cmax when administered intramuscularly at a dose of 400-500 mg - 2.5-4 μg/ml, when administered orally - 50-100 ng/ml. 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. 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. 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.
Indications
Mexidol, Mexifin, Mexidant: anxiety states for neurotic and neurosis-like conditions, VSD, discirculatory encephalopathy, acute cerebrovascular accidents (as part of combination therapy), mild cognitive disorders of atherosclerotic origin, withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, acute intoxication with antipsychotic drugs. Mexidol (parenteral): acute purulent-inflammatory processes in the abdominal cavity, incl. acute necrotizing pancreatitis, peritonitis (as part of complex therapy). Mexicor: acute myocardial infarction from the first day (parenteral); IHD (oral) - as part of complex therapy.
Contraindications
Hypersensitivity; acute liver and/or renal failure; pregnancy, lactation, childhood.
With caution
Dosage regimen
Mexidol, Mexidant: orally, 0.25-0.5 g/day in 2-3 doses; maximum daily dose - 0.6-0.8 g. Duration of treatment - 2-6 weeks; to relieve alcohol withdrawal - 5-7 days. Treatment is stopped gradually, reducing the dose over 2-3 days. Intramuscularly, intravenously (stream, for 5-7 minutes or drip, at a speed of 60 drops/min). For infusion administration, dilute in 200 ml of 0.9% NaCl 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 once a day in the first 2-4 days, then intramuscularly, 0.1 g 3 times a 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 - intramuscularly, 100-200 mg 2-3 times a day or intravenously, 1-2 times a day for 5-7 days. For acute intoxication with antipsychotic drugs - intravenously, 0.05-0.3 g/day for 7-14 days. Mild cognitive disorders - intramuscularly at 0.1-0.3 g/day for 14-30 days. Mexidol (additionally): 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 - 0.3-0.4 g 2 times a day with a gradual decrease in the daily dose. Meskicor: 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, a single dose - 250 mg. Administer intravenously by infusion over 30-90 minutes in 100-150 ml of 0.9% NaCl solution or 5% dextrose solution or by stream for at least 5 minutes. IHD: 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
Overdose
Symptoms
Sleep disorders (insomnia, in some cases drowsiness); with intravenous administration - a slight and short-term (up to 1.5-2 hours) increase in blood pressure.
Treatment
As a rule, it is not required - the symptoms disappear on their own within 24 hours. IN severe cases for insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. If the increase is excessive blood pressure- antihypertensive drugs under the control of blood pressure and/or complement therapy with nitro drugs.
special instructions
During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous species activities that require increased concentration and speed of psychomotor reactions.
Interaction
Enhances the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. Reduces toxic effects
Registration number: LSR-002063/07 dated 08/09/2007
Trade name of the drug: Mexidol
INN or group name: Ethylmethylhydroxypyridine succinate.
Chemical rational name: 2-ethyl-6-methyl-3-hydroxypyridine succinate.
Dosage form: film-coated tablets
Compound:
- active substance: ethylmethylhydroxypyridine succinate – 125 mg
- Excipients: lactose monohydrate, sodium carboxymethylcellulose (carmellose sodium), magnesium stearate, shell: opadry II white (macrogol (polyethylene glycol), polyvinyl alcohol, talc, titanium dioxide).
Description:
The tablets are round, biconvex, film-coated, white to off-white in color.
Pharmacotherapeutic group: antioxidant agent.
ATX Code: N07XX
Pharmacological properties:
Pharmacodynamics
Mexidol is an inhibitor of free radical processes, a 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 accidents, intoxication with alcohol and antipsychotics (neuroleptics)).
The mechanism of action of Mexidol is due to its antioxidant, antihypoxic and membrane protective effects. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, reduces membrane viscosity, and increases its fluidity. Mexidol 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, neurotransmitter transport and improve synaptic transmission.
Mexidol increases the content of dopamine in the brain. Causes an increase in 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, stabilization of cell membranes. The drug improves 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 lipid-lowering effect, reduces the content of total cholesterol and low-density lipoproteins. The anti-stress effect is manifested in the normalization of post-stress behavior, somatovegetative disorders, restoration of sleep-wake cycles, impaired learning and memory processes, reduction of dystrophic and morphological changes in various structures of the brain.
Mexidol has a pronounced antitoxic effect in withdrawal symptoms. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, autonomic functions, and is also able to relieve cognitive impairment caused by long-term use ethanol and its withdrawal. Under the influence of Mexidol, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects.
Pharmacokinetics:
Rapidly absorbed when taken orally. The maximum concentration at doses of 400 - 500 mg is 3.5 - 4.0 mcg/ml. Quickly distributed in organs and tissues. The average retention time of the drug in the body when taken orally is 4.9 - 5.2 hours. Metabolized in the liver by glucuron conjugation. 5 metabolites have been identified: 3-hydroxypyridine phosphate - formed in the liver and with the participation alkaline phosphatase decomposes into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, is formed in large quantities and is found in the urine 1 - 2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates. Tx/2 when taken orally - 2.0 - 2.6 hours. It is quickly excreted in the urine, mainly in the form of metabolites and in small quantities - unchanged. The most intensive elimination occurs during the first 4 hours after taking the drug. Rates of urinary excretion of unchanged drug and metabolites have individual variability.
Indications for use:
- Consequences of acute cerebrovascular accidents, including after transient ischemic attacks, in the subcompensation phase as preventive courses;
- Mild traumatic brain injury, consequences;
- of various origins(dyscirculatory, ismetabolic, post-traumatic, mixed);
- Syndrome;
- Mild cognitive disorders of atherosclerotic origin;
- Anxiety disorders in neurotic and neurosis-like conditions;
- Relief of withdrawal syndrome with a predominance of neurosis-like and vegetative-vascular disorders, post-withdrawal disorders;
- Conditions after acute intoxication with antipsychotic drugs;
- Asthenic conditions, as well as for the prevention of development somatic diseases under the influence of extreme factors and loads;
- Impact of extreme (stress) factors.
Contraindications:
Directions for use and dosage:
Orally, 125 - 250 mg 3 times a day; the maximum daily dose is 800 mg (6 tablets). Duration of treatment - 2 - 6 weeks; to relieve alcohol withdrawal - 5-7 days. Treatment is stopped gradually, reducing the dose over 2 to 3 days. The initial dose is 125 - 250 mg (1 - 2 tablets) 1 - 2 times a day with a gradual increase until a therapeutic effect is obtained. The maximum daily dose is 800 mg (6 tablets).
Side effect:
It is possible that individual adverse reactions: dyspeptic or dyspeptic nature, allergic reactions.
Interaction with other drugs:
Mexidol is combined with all drugs used to treat somatic diseases. Enhances the effect of benzodiazepine drugs, antidepressants, anxiolytics, anticonvulsants and antiparkinsonian drugs. Reduces the toxic effects of ethyl alcohol.
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.
Overdose:
In case of overdose, drowsiness may develop.
Release form:
Film-coated tablets 125 mg. 10 tablets in a blister pack made of PVC film and aluminum foil or 90 tablets in a food-grade plastic jar. 1,2,3,5 blister packs of 10 tablets each or 1 plastic jar of 90 tablets each along with instructions for use per pack. For hospital use Film-coated tablets 125 mg. 450 and 900 tablets in a plastic jar made of food grade plastic along with instructions for use in corrugated cardboard boxes.
Storage conditions:
List B. Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.
Best before date:
3 years. Do not use after the expiration date indicated on the pack.
Vacation conditions:
On prescription
Manufacturer:
A: ZiO-Zdorovye CJSC, 142103, Moscow region, Podolsk, st. Zheleznodorozhnaya 2
B: CJSC ALSI-Pharma, CJSC ALSI Pharma, 129272, Moscow, Trifonovsky deadlock, 3
Price for Mekidol
- from 200 to 400 rubles depending on the number of tablets in the package and mark-ups in retail pharmacies
Original domestic antihypoxant and antioxidant direct action, optimizing the energy supply of cells and increasing the body's reserve capabilities
Mexidol: Features and benefits
Main Applications
Neurology: acute cerebrovascular accidents, atherosclerotic damage to the blood vessels of the heart and brain; traumatic brain injury, epilepsy; dyscirculatory, post-traumatic, dismetabolic and posthypoxic encephalopathy; neurodegenerative diseases of the nervous system: Alzheimer's disease, Parkinson's disease, Gilles de la Tourette's disease, Huntinton's chorea; peripheral neuropathies (diabetic, toxic, post-traumatic, compression-ischemic, radiculoischemic), syndrome autonomic dysfunction, parasomnic disorders, cerebroasthenic syndrome. Surgery: acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis). Psychiatry: relief of withdrawal syndrome with the presence of neurosis-like and vegetative-vascular disorders in the clinical picture, acute intoxication with neuroleptics.
MEXIDOL- patented medicine.
The copyright holder - Pharmasoft LLC organizes the production and sale of the drug.
annotation
Recently, more and more attention has been paid to the processes of free radical oxidation in health and disease. Their participation in the development of diseases such as atherosclerotic lesions of the heart and brain vessels, hypertension, cancer, neurodegenerative diseases, is most widely publicized. convulsive states, stress, neurosis, pain syndromes, osteoarthritis, amyloidosis, cholecystitis, pancreatitis, inflammatory processes, diseases of the blood, eyes (cataracts, etc.), skin, diabetes mellitus, kidney, liver and lung diseases, allergic and immunodeficiency conditions, etc. Main pathogenetic process accompanying natural aging the body is also free radical oxidation.
This was dictated by one of the most promising directions in maintaining adequate activity of the endogenous antioxidant system - the search for rational antioxidant therapy.
The creation of synthetic antioxidants is an undoubted achievement of the domestic pharmacoindustry. Special place among similar drugs occupied by the drug Mexidol.
The drug was developed by leading scientific institutions(Institute of Biochemical Physics named after N.M. Emmanuel RAS, Research Institute of Pharmacology of the Russian Academy of Medical Sciences and VSC BAV) and has no analogues in Russia and abroad. The first industrial batch of the drug, released in 1999, Pharmasoft LLC went through additional clinical trials at 24 medical institutions countries. Experts highly appreciated the clinical effect of Mexidol, which allowed the Moscow Health Committee, by its order No. 301 dated July 13, 2000, to include the drug in the “List of medicines and medical products dispensed by prescription free of charge or at a discount in Moscow,” as well as recommend it to hospitals for purchases (order of the Moscow Health Committee dated February 16, 2001 No. 79). Mexidol is also included in the "List of necessary and essential medicines for use in institutions Medical center Administration of the President of the Russian Federation."
MEXIDOL (Mexidolum)
International nonproprietary name- hydroxymethylethylpyridine succinate.
Chemical rational name- 3-Hydroxy-6-methyl-2-ethylpyridine succinate.
Dosage form:
Pharmacological group- "antioxidant"
Description:
Pharmacological properties:
Pharmacodynamics:
refers to heteroaromatic antioxidants - analogues of compounds of the vitamin B (6) group. It has a wide range of pharmacological activity: it is an inhibitor of free radical processes, a 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, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular accidents, intoxication with alcohol and antipsychotics (neuroleptics)).
The drug 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 lipid-lowering effect, reduces the content of total cholesterol and low-density lipoproteins. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
Mechanism of action of Mexidol
It is determined by its antioxidant and membrane protective action, the key links of which are:
1. Mexidol inhibits free radical oxidation of membrane lipids and freely binds lipid peroxide radicals.
2. Mexidol increases the activity of antioxidant enzymes responsible for the formation and consumption active forms oxygen, in particular superoxide dismutase.
3. Inhibits the synthesis of prostaglandins, prostacyclins, thrombachane A and leukotrienes.
4. It has a hypolipidemic effect, namely it reduces the level of total cholesterol, low-density lipoproteins, reduces the cholesterol/phospholipids ratio, reducing the viscosity of the lipid layer.
5. Improves energy metabolism cells, activates the energy-synthesizing functions of mitochondria, affects the content of biogenic amines and improves synaptic transmission. In addition, succinate, which is part of Mexidol, itself is included in the functioning of the respiratory chain, increasing its efficiency.
6. Mexidol modulates receptor complexes of brain membranes, in particular, benzodiazepine, GABAergic, acetylcholine receptors, enhancing their ability to bind.
7. The drug stabilizes biological membranes, and in particular, the membranes of erythrocytes and platelets.
Thus, due to its mechanism of action and a wide range of pharmacological effects (cerebroprotective, antihypoxic, tranquilizing, antistress, nootropic, vegetotropic, anticonvulsant; improvement and stabilization of cerebral metabolism and blood supply to the brain; correction of disorders in the regulatory and microcirculatory systems; improvement rheological properties blood, suppression of platelet aggregation; activation immune system), Mexidol influences the main links in the pathogenesis of various diseases associated with free radical oxidation processes. In addition, this mechanism of action explains its extremely low side effects and the ability to potentiate the action of other centrally active substances.
Mexidol realizes its pharmacological effects by at least, at two levels - neuronal and vascular. The therapeutic effects of Mexidol are detected in the range from 10 to 300 mg/kg.
increases the body's resistance to the action of various extreme damaging factors, such as sleep disturbance, conflict situations, stress, brain injury, electric shock, physical exercise, hypoxia, ischemia, various intoxications, including ethanol.Mexidol has a pronounced tranquilizing and anti-stress effects, the ability to eliminate anxiety, fear, tension, restlessness, particularly in conflict situations. When administered parenterally, it has a similar depth of effect to diazepam (Seduxen) and alprazolam (Xanax). The anti-stress effect of Mexidol is expressed in the normalization of post-stress behavior, somato-vegetative indicators, restoration of sleep-wake cycles and impaired learning and memory processes, reduction of stomach ulcers, reduction of dystrophic, morphological changes that occur after stress in various structures of the brain and in the myocardium.
Mexidol has a distinct anticonvulsant effect, influencing both primary generalized seizures, caused primarily by the administration of GABAergic substances, and the epileptiform activity of the brain with a chronic epileptogenic focus.
Nootropic properties Mexidol are expressed in the ability to improve learning and memory, contribute to the preservation of a memorable trace and counteract the process of extinction of instilled skills and reflexes. Mexidol has a pronounced anti-amnestic effect, eliminating memory impairment caused by various influences (electric shock, brain injury, sleep deprivation, administration of scopolamine, ethanol, benzodiazepines, etc.).
Mexidol has a distinct effect antihypoxic and anti-ischemic effects. In terms of antihypoxic activity, Mexidol is significantly superior to pyritinol and piracetam. In addition, the drug has a pronounced antihypoxic effect on the myocardium. According to the mechanism by which these effects are realized, Mexidol is an antihypoxant with a direct energizing effect, the effect of which is associated with the influence on the endogenous respiration of mitochondria, with the activation of the energy-synthesizing function of mitochondria. The antihypoxic effect of Mexidol is due not only to its own properties, but also to its constituent succinate, which, under hypoxic conditions, entering the intracellular space, can be oxidized by the respiratory chain.
Mexidol has a pronounced anti-alcohol effect. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication caused by a single injection of high doses of ethanol, and also restores behavioral disorders, vegetative and emotional status, deterioration of cognitive functions, learning and memory processes caused by long-term (5 months) administration of ethanol and its withdrawal, and prevents the accumulation of lipofuscin in brain tissue.
Mexidol has a pronounced geroprotective action, has a clear corrective effect on learning and memory processes impaired during aging, improving the process of fixation, storage and reproduction of information, helps restore emotional and vegetative status, reduces manifestations of neurological deficits, reduces the level of aging markers in the brain and blood - lipofuscin, malonaldehyde, cholesterol. The mechanism of the geroprotective effect of Mexidol is associated with its antioxidant properties, the ability to inhibit lipid peroxidation processes, its direct membranotropic effect, the ability to restore ultrastructural changes in the granular endoplasmic reticulum and mitochondria, and modulate the functioning of receptor complexes.
Mexidol has antiatherogenic action. The drug inhibits the humoral manifestations of atheroarteriosclerosis: reduces hyperlipidemia, prevents the activation of lipid peroxidation, increases the activity of the antioxidant system and has a protective effect on local vascular mechanisms atherogenesis, prevents the development pathological changes in the vascular wall and reduces the degree of damage to the aorta.
Mexidol reduces the content of atherogenic lipoproteins and triglycerides, increases the level of lipoproteins high density in blood serum, prevents deficiency of highly unsaturated phospholipids.
Mexidol not only causes regression of atherosclerotic changes in the main arteries and restores lipid homeostasis, but also corrects disturbances in the regulatory and microcirculatory systems, which is expressed in the fact that there is no constriction of arterioles and precapillaries, and their diameter differs little from the control, only focal aggregates are noted in the venules, and a complete elimination of spasm of the afferent microvessels is observed.
In addition, 2-ethyl-6-methyl-3-hydroxypyridine derivatives, which include Mexidol, suppress platelet aggregation caused by collagen, thrombin, ADP and arachidonic acid, inhibit platelet cyclic nucleotide phosphodiesterase, and also protect blood cells during mechanical injury. In particular, stabilizing resistance of erythrocyte membranes to hemolysis is observed and the process of hematopoiesis (restoration of the number of erythrocytes) after acute blood loss or chemical hemolysis is accelerated.
The hepatoprotective effect of Mexidol was established in three models of acute toxic liver damage, in which hepatocyte cytolysis syndrome was caused by various hepatotoxins.
In conditions of liver damage caused by carbon tetrachloride, Mexidol reduces areas of liver tissue necrosis and the volume of fatty degeneration of hepatocytes, normalizes the energy balance of hepatocytes, and has a protective effect on the nuclear and cytoplasmic pool nucleic acids. At alcohol impairment In the liver, the effect of Mexidol is expressed in a decrease in the number of hepatocytes with lysis of nuclei and chromatin, acceleration of the restoration of the total genome of hepatocytes and an increase in the content of nucleic acids in the liver tissue and nuclei of hepatocytes.
Mexidol has a pronounced ability to provide potentiating effect on the effects of other neuropsychotropic drugs. Under the influence of Mexidol, the effect of tranquilizing, neuroleptic, antidepressant, hypnotic, anticonvulsant and analgesic drugs is enhanced, which makes it possible to reduce their doses and reduce side effects. In particular, when combining Mexidol with carbamazepine, the dose of the anticonvulsant can be reduced by 2 times without reducing its therapeutic effect. Combined use Mexidol with carbamazepine allows for adequate pathogenetic therapy of partial epilepsy, reduces the side effects of carbamazepine in long-term use without reducing its therapeutic effectiveness and thereby optimizing the treatment of patients with epilepsy.
Pharmacokinetics:
When administered intramuscularly, the drug is detected in the blood plasma for 4 hours after administration. The time to reach maximum concentration is 0.45-0.50 hours. The maximum concentration at doses of 400-500 mg is 3.5-4.0 mcg/ml. Mexidol quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. The retention time (MRT) of the drug in the body is 0.7-1.3 hours. The drug is excreted from the body in the urine mainly in glucurone-conjugated form and in small quantities unchanged.
When administered orally, Mexidol is rapidly absorbed from gastrointestinal tract with an absorption half-life (T1/2 abs) of 0.08-0.10 hours. The time to reach maximum concentration (Tmax) in blood plasma is 0.46-0.50 hours. The maximum concentration of the drug in blood plasma (Cmax) is in the range from 50 to 100 NG/ML. The half-life of Mexidol (T V et) and the mean retention time (MRT) of the drug in the body are 4.7-5.0 hours and 4.9-5.2 hours, respectively.
Mexidol is intensively metabolized in the human body with the formation of its glucuron-conjugated product. On average, over 12 hours, 0.3% of the unchanged drug and 50% of the administered dose are excreted in the urine in the form of glucuronoconjugate. Mexidol and its glucuronoconjugate are excreted most intensively during the first 4 hours after taking the drug. The urinary excretion rates of Mexidol and its conjugated metabolite have significant individual variability.
Indications for use:
1. Acute cerebrovascular accidents, subacute period of stroke, early and late period of post-stroke rehabilitation.
2. Dyscirculatory encephalopathy - both against the background of atherosclerotic lesions of cerebral vessels, and against the background hypertension(in the phase of decompensation, subcompensation and, as planned maintenance therapy, in the compensation phase).
3. Posthypoxic, dysmetabolic and, above all, diabetic encephalopathies.
4. Vertebro-basilar insufficiency due to osteochondrosis of the cervical spine.
5. Acute period of traumatic brain injury, early recovery period after TBI, post-traumatic encephalopathy.
6. Epilepsy, episyndrome.
7. Degenerative-dystrophic lesions of the nervous system (Alzheimer's disease, Parkinson's disease, vascular parkinsonism).
8. Autonomic dysfunction syndrome, neurotic and neurosis-like states.
9. Parasomnic disorders.
10. Polyneuropathies (dysmetabolic, primarily diabetic, compression-ischemic, post-traumatic, toxic, including alcoholic).
11. Exogenous-organic diseases of the brain (as a result of previous neuroinfections, radiation exposure, traumatic brain injury).
12. For memory disorders and intellectual disability in the elderly.
13. Periods of extreme stress, neurotic and neurosis-like disorders.
14. Intoxication with neuroleptics.
15. Acute intoxication ethyl alcohol and relief of alcohol withdrawal syndrome.
16. Complex treatment and rehabilitation of patients with opium (heroin) addiction.
17. Use in complex therapy to prevent post-resuscitation metabolic disorders.
18. Acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis).
19. Complex therapy of liver failure.
20.Use for premedication of patients in dentistry medical practice.
Directions for use and doses
Mexidol is prescribed intravenously (stream or drip), intramuscularly and orally. When administered intravenously, the drug should be diluted with water for injection or in physiological sodium chloride solution. For infusion administration saline NaCL solution should be used.
Mexidol is administered in a stream over 1.5-3.0 minutes, and dropwise at a rate of 80-120 drops per minute. The duration of treatment and the daily dose of the drug depend on the nosology of the disease and the severity of the patient’s condition.
For treatment acute cerebrovascular accident Mexidol is prescribed intravenously drip 400 mg (8 ml) in isotonic sodium chloride solution (100-150 ml) twice a day for the first 15 days, and then:
In the future, it is recommended to administer Mexidol intramuscularly at a dose of 200 mg (4 ml) once a day for 10-15 days. In the subsequent comprehensive drug therapy It is advisable to include a tablet form of the drug, 0.25-0.5 g/day for 4-6 weeks. The daily dose is distributed into 2-3 doses during the day.
For treatment dyscirculatory encephalopathy(both against the background of cerebral atherosclerosis and against the background of hypertension):
- either 400 mg (8 ml) intravenously in drops per 100 ml of isotonic NaCL solution daily for 10-15 days;
- either 200 mg (4 ml) intravenously in 16.0 ml of water for injection or in isotonic sodium chloride solution (16.0 ml) twice a day, for 10-15 days.
Then the drug is administered intravenously in a stream of 100 mg (2 ml) per 10.0 ml of isotonic sodium chloride solution, daily, for a course of 10 days. Or 200 mg (4 ml) intramuscularly, daily for 10 days. Subsequently it is recommended oral administration Mexidol 0.125 g three times a day for 4-6 weeks.
- either 200 mg (4 ml) intravenously in a bolus with 16.0 ml of physiological NaCL solution (or 16.0 ml of water for injection), daily, for 10-15 days;
- either 200 mg (4 ml) intramuscularly, twice a day, for 1015 days.
- either 100 mg (2 ml) intravenously in a bolus per 10.0 ml of physiological NaCL solution, daily for 10 days;
- either 200 mg (4 ml) intramuscularly, daily, for a course of 10 days. Subsequently, it is advisable to take the tablet form of 0.125 g three times a day for 2-6 weeks (in both cases - with both intravenous and intramuscular administration of Mexidol);
- or initially, a course of prophylaxis can be started with the use of a tablet form of 0.125 g three times a day, for at least 4-6 weeks.
For vertebrobasilar insufficiency against the background of osteochondrosis of the cervical spine, Mexidol is used:
- either 400 mg (8 ml) intravenously, in 100.0 ml of physiological NaCL solution, daily, 10 days;
- either 200 mg (4 ml) intravenously in a bolus per 16.0 ml of isotonic sodium chloride solution, twice a day, for 10 days;
In the future, it is recommended to administer Mexidol 200 mg (4 ml) intramuscularly for 10-15 days. At the end intramuscular injections- switch to oral administration of the drug at 0.125 mg three times a day, for a course of 2-6 weeks.
- either 200 mg (4 ml) of Mexidol is administered intravenously, per 16.0 ml of isotonic sodium chloride solution, for 10 days;
- either 200 mg (4 ml) intramuscularly, twice a day, 10 days.
In the future, it is advisable to prescribe Mexidol in tablet form in the doses described above.
IN acute period of traumatic brain injury the prescription of Mexidol is pathogenetically justified, since, in addition to its cerebroprotective properties, its anticonvulsant activity and potentiation of the action of dehydration agents are of great importance.
Recommended doses of the drug:
- in the acute period - 200 mg (4 ml) intravenously, per 16.0 ml of isotonic sodium chloride solution, twice a day, 10-15 days;
- in the subacute period - 200 mg (4 ml) intravenously in a bolus per 16.0 ml of isotonic sodium chloride solution, daily for 10 days; or 200 mg (4 ml) intramuscularly, twice a day, 10-15 days.
The administration of Mexidol is very effective in the treatment of dismetabolic, and, first of all, diabetic encephalopolyneuropathies. Mexidol, used for diabetes, improves the course of the disease itself, and also improves the uptake of glucose by cells in conditions of insulin resistance. Intravenous administration of the drug is recommended: 200 mg (4 ml) intravenously in a bolus, per 16.0 ml of physiological NaCL solution, twice a day, for 10-15 days. In the future, 100 mg (2 ml) is administered intramuscularly daily for 15-30 days. At the end of parenteral administration, Mexidol is given in tablets - 0.125 g three times a day, for at least 4-6 weeks.
Considering the lack of direct stimulating effect on the cerebral cortex, and having a pronounced anticonvulsant effect, it is advisable to use Mexidol in the treatment of epilepsy. In addition, the drug enhances the effect of anticonvulsants, which allows, when prescribing it, to reduce the doses of anticonvulsants used, as well as reduce their side effects. Mexidol is recommended to be administered 100 mg (2 ml) intravenously in a bolus of 18.0 ml of isotonic sodium chloride solution (or in the same amount of water for injection), twice a day, for 15 days. Then the drug is administered intramuscularly at 100 mg (2 ml) daily for 15 days.
Degenerative-dystrophic lesions of the central nervous system
Mexidol has a pronounced positive effect in the treatment of chronic neuroleptic syndrome with symptoms of tardive dyskinesia and subacute neuroleptic syndrome. The drug reduces the severity of oral-lingual hyperkinesis, reduces limb tremors, stiffness, hypomimia and hypokinesia, and improves the motor functions of patients. In addition, Mexidol potentiates the effect of antiparkinsonian drugs, which makes it possible to reduce the doses of drugs used and reduce their side effects.
For the treatment of degenerative-dystrophic lesions of the central nervous system, it is recommended to use Mexidol 200 mg (4 ml) intravenously in a bolus per 16.0 ml of isotonic sodium chloride solution, twice a day, for 10 days. Then the drug is administered intramuscularly at 200 mg (4 ml), daily, for 15 days. In the next 4-6 weeks, it is advisable to prescribe the tablet form - 0.125 g three times a day.
Autonomic dysfunction syndrome, neurotic and neurosis-like conditions
Mexidol showed its high efficiency with vegetative-vascular dystonia, especially of the paroxysmal type. It has a vegetative-normalizing effect and a distinct tranquilizing effect in neurotic and neurosis-like conditions. Dosage regimen of the drug: 100-200 mg (2-4 ml) of Mexidol is administered intravenously in a stream of 10.0-16.0 ml of isotonic sodium chloride solution, daily for 10 days. It is possible to administer the drug intramuscularly at 200 mg (4 ml), daily, for 15 days. After injections, it is advisable to prescribe a tablet form of Mexidol at 0.25-0.50 g per day. The daily dose is distributed into 2-3 doses. The course of treatment is 2-6 weeks. In this case, a course of Mexidol therapy is completed gradually, reducing the dose of the drug over 2-3 days.
Parasomnic disorders
Mexidol provides positive influence to sleep, restoring its duration and depth, while helping to restore the correct rhythm of sleep. This is combined with the absence of sedation effects when taking the drug in daytime. In this case, the drug is recommended to be administered intramuscularly, 100-200 mg (2-4 ml), daily for 15-20 days. The drug is then given in tablet form, 0.125 g three times a day, for 4-6 weeks. Before discontinuation, the dose of the drug is reduced gradually over 2-3 days.
Memory disorders and intellectual disability in the elderly
Mexidol is effective drug for revitalization of elderly people. The drug has a positive effect on hypomnesia, increased distractibility and difficulty concentrating, improves the ability to concentrate and count, improves short-term memory for current events and long-term memory for the past. Recommended dosage regimen for Mexidol: 100-200 mg (2-4 ml) - depending on the degree of intellectual disability - administered intramuscularly for 10-15 days, then the drug is given orally at 0.125 g, three times a day, for less than 4-6 weeks. Such courses are repeated every 5-6 months.
Periods of extreme stress
Mexidol has a pronounced ability to improve mental and physical performance, especially under conditions of extreme influences. It is advisable to start prescribing Mexidol in such cases with intravenous administration 200 mg (4 ml) intravenously in a stream, per 16.0 ml of isotonic sodium chloride solution, daily for 10-15 days. Then the drug is administered intramuscularly at 200 mg (4 ml) per day for 10 days, followed by a transition to taking the tablet form at 0.25-0.50 g per day; course of treatment - 2-6 weeks. It is possible to switch to the tablet form immediately after intravenous administration of Mexidol.
Exogenous-organic diseases of the brain
The causes of exogenous-organic brain damage are: previous traumatic brain injuries, intoxication (excluding alcohol), neuroinfections, radiation exposure, as well as combinations of these factors.
Patients with exogenous-organic diseases are known to have poor tolerance to a number of drugs. Mexidol, as studies have shown, is not one of them. When used, there is a clear positive effect on existing neurological deficits in this category of patients. Recommended dosage regimen: intravenous bolus of 200 mg (4 ml) of Mexidol per 16.0 ml of isotonic sodium chloride solution, daily, for 10-15 days; then the drug can be administered intramuscularly at 100-200 mg (2-4 ml) per day for 10-15 days, or switch to the tablet form at 0.125 g three times a day for 4-6 weeks.
Acute intoxication with ethyl alcohol
Considering the antihypoxic, antioxidant, anxiolytic and hepatoprotective effects of Mexidol, the drug is recommended as part of complex therapy for the relief of acute intoxication with ethyl alcohol. In addition, Mexidol prevents and weakens the toxic effect of alcohol. Dosage regimen: 400 mg (8 ml) intravenously in 150.0 ml of isotonic sodium chloride solution twice a day - 3 days; then 200 mg (4 ml) intravenously in a bolus with 16.0 ml of physiological NaCL solution, twice a day, for 7 days. If necessary, treatment can be continued using the tablet form of the drug - 0.125 g three times a day - 2-6 weeks.
Alcohol withdrawal syndrome
Mexidol is effective as a means for relieving alcohol withdrawal syndrome with somato-neurological and mental symptoms due to its pronounced antioxidant and tranquilizing effects. When comparing the speed of the relief effect of Mexidol in relation to individual symptoms alcohol withdrawal syndrome with the effectiveness of traditional detoxification agents, a significant advantage of this drug was established. Mexidol is effective means for rapid relief of alcohol withdrawal syndrome with a wide range of effects, both on its psychopathological components and on vegetative-vascular manifestations. “Injection” Mexidol, in contrast to the tablet form, turns out to be more effective in relation to affective pathology, eliminating anxiety in a significantly shorter time.
Recommended dosage regimen: 200 mg (4 ml) intravenously in a bolus, per 16.0 ml of isotonic NaCL solution, daily, for 10-15 days, then it is possible to switch to intramuscular administration of the drug at a dose of 200 mg (4 ml), daily, for 10 days, followed by switching to tablet form (0.125 g three times a day, 4-6 weeks).
In some cases, a combination of only intramuscular administration of the drug (in the described dosages) and tablet form is possible.
It is possible to use only the oral form of Mexidol (tablets) at a dose of 500 mg/day - 2 tablets (0.125 g each) twice a day during the entire period of the hangover syndrome.
Treatment and rehabilitation of patients with opium (heroin) addiction
Acute drug withdrawal syndrome:
The inclusion of Mexidol in the complex treatment of acute drug withdrawal syndrome leads to a decrease in the intensity of vegetative disorders, makes it possible to reduce the dosages of a number of medications used to relieve drug withdrawal syndrome, significantly mitigate the side effects of neuroleptic drugs, reduce the phenomena of drug intoxication, and accelerate the restoration of some vital functions ( sleep, appetite), as well as reduce the time required to prepare patients for psychotherapeutic measures. It has been established that intravenous jet administration of the drug to patients with drug addiction at the initial stage of withdrawal syndrome has a pronounced tranquil-sedative effect.
Post-withdrawal period and rehabilitation stage:
Cerebroprotective, anti-amnestic properties, as well as the ability of Mexidol to eliminate the side effects of neuroleptics, determined its prescription for drug addicts in the post-withdrawal period and at the stages of rehabilitation. It has been established that daily administration of the drug prevents or eliminates extrapyramidal disorders when prescribed antipsychotics. The drug is recommended to be prescribed in doses of 200-400 mg/day (4-8 ml) intravenously or intramuscularly, for a course of 10-20 days.
The data obtained on the use of Mexidol at the stages of remission formation showed its positive impact to stabilize the condition of patients with heroin addiction. In the same time long-term treatment Mexidol was limited by the need for parenteral administration. There is reason to believe that the use of Mexidol in tablet form, which is more convenient for prescribing the drug in outpatient setting, may have an even more significant therapeutic effect on the course of the rehabilitation process in patients with heroin addiction. In tablet form, it is recommended to prescribe Mexidol 0.25 g (2 tablets of 0.125 g) twice a day for at least 4-6 weeks.
Complex therapy of acute purulent-inflammatory processes of the abdominal cavity
In acute destructive pancreatitis and peritonitis, Mexidol 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. Discontinuation of the drug should be done gradually, only after a stable positive clinical and laboratory effect.
- For acute edematous (interstitial) pancreatitis, Mexidol is prescribed 100 mg (2 ml) three times a day intravenously, in isotonic sodium chloride solution.
- Mild severity of necrotizing pancreatitis - 100-200 mg (2-4 ml) three times a day intravenously (in isotonic NaCL solution).
- Severe necrotizing pancreatitis - Mexidol is administered in a pulse dosage - 800 mg (16 ml) on the first day, with a double administration regimen; then 300 mg (6 ml) twice a day with a gradual reduction in the daily dose.
- Extremely severe course - at an initial dosage of 800 mg/day (16 ml) until the manifestations of pancreatogenic shock are persistently relieved, upon stabilization of the condition, 300-400 mg (6-8 ml) twice a day intravenously (in isotonic sodium chloride solution) with a gradual reduction in daily dosage.
Use in dental medical practice
The features and mechanism of action of Mexidol clearly reveal its advantages over known drugs and determine the prospects of using it for premedication of patients in dental medical practice. Mexidol has an advantage over both classical tranquilizers and non-narcotic analgesics, which consists in the complexity of the action of this drug, which has both a tranquilizing and analgesic effect without side effects.
For the purpose of premedication of patients on an outpatient basis dental appointment It is recommended to administer 100-200 mg (2-4 ml) of a 5% Mexidol solution per 10.0-16.0 ml of isotonic sodium chloride solution 20-30 minutes before the upcoming dental intervention.
Contraindications
The use of Mexidol is contraindicated in acute disorders of liver and kidney function. Hypersensitivity or intolerance to the drug.
Side effects
When studying the side effects of Mexidol, it was found that even in the upper range of therapeutic doses it:
- does not affect spontaneous motor activity;
- does not change the coordination of movements;
- does not cause drowsiness;
- does not have a muscle relaxant effect;
- does not provide negative impact on the liver, but, on the contrary, has a hepatoprotective effect;
- does not affect blood pressure, heart rate, ECG, breathing rhythm, does not cause changes in the composition of the blood.
May be observed: from the digestive system: rarely - nausea, dry mouth. Caution is required when prescribing Mexidol to patients with high and low blood pressure numbers and a crisis of hypertension.
With intravenous jet administration of Mexidol, a sore throat, a metallic taste in the mouth, and coughing may sometimes occur. This is not a reason to discontinue the drug. Firstly, with subsequent administrations of Mexidol, the severity of the described phenomena decreases; and secondly, with greater dilution of the drug or slower administration, the intensity of the described phenomena decreases.
Interaction with other drugs
The drug is combined with anticoagulants, antiplatelet agents, antihypertensive drugs, and hypoglycemic drugs; all medicines used to treat diseases of the cardiovascular system.
Mexidol potentiates the effect of anticonvulsants, tranquilizers, antiparkinsonian drugs, and analgesics. The drug reduces the toxic effects of ethyl alcohol.
Overdose
Due to low toxicity, overdose is unlikely and no such cases have been reported to date. Theoretically, in case of overdose, drowsiness and sedation may occur.
Storage conditions
List B. The drug should be stored in a place protected from light, out of reach of children.
Best before date
2 years. Do not use after the expiration date indicated on the package.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
