Composition
Active ingredient:
ethylmethylhydroxypyridine succinate 50 mg;
Auxiliary substances:
sodium metabisulfite-0,4 mg,
water d/i-up to 1 ml
Pharmacological action
Pharmacodynamics
Mexidol® has antihypoxic, membrane-protective, nootropic, anticonvulsant, anxiolytic effects, 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, impaired cerebral circulation, intoxication with alcohol and antipsychotic drugs (neuroleptics)).
Mexidol ® improves brain metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membrane structures of blood cells (red blood cells 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 antihypoxant, antioxidant and membrane-protective effects. It inhibits the processes of lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, reduces the viscosity of the membrane, and increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, transport neurotransmitters, and improve synaptic transmission. 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 energy-synthesizing functions of mitochondria, and stabilization of cell membranes.
Mexidol ® normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and improves 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 nitropreparations.
Mexidol ® promotes the preservation of retinal ganglion cells and optic nerve fibers in progressive neuropathy caused by chronic ischemia and hypoxia. Improves the functional activity of the retina and optic nerve, increasing visual acuity.
Pharmacokinetics
Suction
With the introduction of Mexidol® in doses of 400-500 mg, Cmax in plasma is 3.5-4.0 mcg / ml and is reached within 0.45-0.5 hours.
Distribution
After intravenous use, the drug is detected in blood plasma for 4 hours. The average retention time of the drug in the body is 0.7-1.3 hours.
Deduction
It is excreted from the body in the urine mainly in glucuronoconjugated form and in small amounts – in unchanged form.
Indications
- acute cerebrovascular disorders;
- craniocerebral trauma, the consequences of traumatic brain injury;
- encephalopathy;
- the syndrome of vegetative dystonia;
- mild cognitive dysfunction of atherosclerotic;
- anxiety disorders in neurotic and neurosis-like States;
- acute myocardial infarction (from the first day) as part of complex therapy;
- primary open angle glaucoma different stages in the complex therapy;
- the relief of withdrawal syndrome in chronic alcoholism with the prevalence of neurosis and vegetative-vascular disorders;
- acute intoxication with antipsychotic funds;
- acute purulent inflammation of the abdominal cavity (acute necrotic pancreatitis, peritonitis) as part of complex therapy.
Contraindications
- increased individual sensitivity to the drug;
- acute liver and kidney function disorders.
Strictly controlled clinical studies of the safety of Mexidol® in children, during pregnancy and lactation have not been conducted.
Side effects
From the digestive system: Â rarely – nausea, dry mouth.
Other services: Â rarely-allergic reactions.
Interaction
When used together, Mexidol ® enhances the effect of anxiolytics of benzodiazepine derivatives, antiparkinsonian (levodopa) and anticonvulsants (carbamazepine).
Mexidol ® reduces the toxic effect of ethyl alcohol.
How to take, course of use and dosage
IV or IV (jet or drip). With the infusion method of use, the drug should be diluted in 0.9% sodium chloride solution.
Jet Mexidol® is administered slowly for 5-7 minutes, drip – at a rate of 40-60 drops per minute. The maximum daily dose should not exceed 1200 mg.
In acute disorders of cerebral circulation Mexidol® apply in the first 10-14 days-in / in drops of 200-500 mg 2-4 times a day, then in / m 200-250 mg 2-3 times a day for 2 weeks.
For traumatic brain injury and the consequences of traumatic brain injuries Mexidol® apply for 10 – 15 days in / in drops of 200-500 mg 2-4 times a day.
In patients with dyscirculatory encephalopathy in the decompensation phase, Mexidol® should be administered intravenously in a jet or drip at a dose of 200-500 mg 1-2 times a day for 14 days. Then I. m. 100-250 mg / day for the next 2 weeks.
For the course prevention of dyscirculatory encephalopathy, the drug is administered intravenously at a dose of 200-250 mg 2 times a day for 10-14 days.
For mild cognitive impairment in elderly patients and for anxiety disorders, the drug is used intravenously in a daily dose of 100-300 mg / 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, anticoagulants and antiplatelet agents, as well as symptomatic agents according to indications.
In the first 5 days, to achieve maximum effect, the drug should be administered intravenously, in the next 9 days Mexidol® it can be administered intramuscularly.
Intravenous use of the drug is performed by drip infusion, slowly (to avoid side effects) in 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 is possible, lasting at least 5 minutes.
use of the drug (intravenous or intramuscular) is carried out 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg / kg of body weight per day, a single dose is 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose-250 mg.
In open – angle glaucoma of various stages, Mexidol® is administered intramuscularly at 100-300 mg/day,1-3 times a day for 14 days as part of complex therapy.
In patients with alcohol withdrawal syndrome, Mexidol® is administered at a dose of 200-500 mg intravenously or intravenously 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 period. The administered doses depend on the form and severity of the disease, the prevalence of the process, and the clinical course options. Discontinuation of the drug should be carried out gradually only after a sustained positive clinical and laboratory effect.
In acute edematous (interstitial) pancreatitis Mexidol® assign 200-500 mg 3 times a day, IV drip (in 0.9% sodium chloride solution) and IV. Mild severity of necrotizing pancreatitis — 100-200 mg 3 times a day IV drip (in 0.9% sodium chloride solution) and iv. Moderate severity — 200 mg 3 times a day, IV drip (in 0.9% sodium chloride solution). Severe course — in a pulse dosage of 800 mg on the first day, with a double mode of use; then 200-500 mg 2 times a day with a gradual decrease in the daily dose.
Extremely severe course — at an initial dosage of 800 mg / day until persistent relief of manifestations of pancreatogenic shock, after stabilization of the condition,300-500 mg 2 times a day IV drip (in 0.9% sodium chloride solution) with a gradual decrease in the daily dosage.
Overdose
Symptoms: Â drowsiness may develop.
Special instructions
Mexidol can be combined with all medications used to treat somatic diseases.
Use in pediatrics
Strictly controlled clinical studies of the safety of Mexidol® in children have not been conducted.
Influence on the ability to drive motor vehicles and manage mechanisms
During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
In some cases, especially in predisposed patients with bronchial asthma with hypersensitivity to sulfites, severe hypersensitivity reactions may develop.
Form of production
Solution for injection
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C.
Shelf life
2 years
Active ingredient
Ethylmethylhydroxypyridine Succinate
Conditions of release from pharmacies
By prescription
Dosage form
solution for injection and infusion
Purpose
Adults as prescribed by a doctor
Indications
From the consequences of a stroke, From a hangover, From atherosclerosis, Under the influence of adverse factors, From cerebral circulation disorders, From angina pectoris, From vegetative-vascular disorders, Prevention of acute myocardial infarction, From concussion and other traumatic brain injuries
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Side effects of Mexidol, ampoules 5%,2ml, 10pcs.
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