Description
Mexidol Pharmacodynamics
It has antihypoxic, membranoprotective, nootropic, anticonvulsant, anxiolytic effect, increases the body’s resistance to stress. The drug increases resistance to the effects of major damaging factors, oxygen-dependent pathological states (shock, hypoxia and ischemia, impaired cerebral circulation, intoxication with alcohol and antipsychotic drugs (neuroleptics).
Mexidol® improves cerebral metabolism and blood supply of the brain, improves microcirculation and blood rheology, reduces platelet aggregation. It stabilizes membrane structures of blood cells (erythrocytes and platelets) in hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL.
It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
Mechanism of action of Mexidol® is due to its antihypoxant, antioxidant and membrane-protective effects. It inhibits lipid peroxidation processes, increases superoxide dismutase activity, increases lipid-protein ratio, reduces membrane viscosity and increases its fluidity. It modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which increases their ability to bind to ligands, helps maintain the structural and functional organization of biomembranes, neurotransport and improve synaptic transmission. Mexidol® increases dopamine content in the brain. It causes enhancement of compensatory activity of aerobic glycolysis and reduction of the degree of inhibition of oxidative processes in the Krebs cycle under hypoxia, with increase of ATP, creatine phosphate and activation of energy-synthesizing functions of mitochondria, stabilization of cell membranes. Mexidol® normalizes metabolic processes in the ischemic myocardium, reduces the zone of necrosis, restores and improves myocardial electrical activity and contractility, as well as increases coronary blood flow in the ischemic zone, reduces the consequences of reperfusion syndrome in acute coronary failure. Increases antianginal activity of nitropreparations. Mexidol® promotes preservation of retinal ganglion cells and optic nerve fibers at progressive neuropathy caused by chronic ischemia and hypoxia. It improves functional activity of the retina and optic nerve, increasing visual acuity.
Indications
-acute disorders of cerebral circulation;
-cranial trauma, consequences of craniocerebral injuries;
-dyscirculatory encephalopathy;
-vegetative dystonia syndrome;
-Mild cognitive disorders of atherosclerotic genesis;
-anxiety disorders in neurotic and neurosis-like conditions;
-Acute myocardial infarction (from the first day) as part of complex therapy;
Primary open-angle glaucoma of different stages, as part of the complex therapy;
-withdrawal syndrome in alcoholism with a predominance of neurosis and vegetovascular disorders;
-Acute intoxication with antipsychotic agents;
-Acute pyo-inflammatory processes of the abdomen (acute necrotizing pancreatitis, peritonitis) as part of the treatment.
Contraindications .
Acute liver and kidney function abnormalities, hypersensitivity to the drug. Strictly controlled clinical trials of Mexidol usage safety in children and during pregnancy and lactation have not been carried out.
Dosage and administration method
- V/m or intravenously (by jet or drop). When administering by infusion method the drug should be diluted in 0.9% sodium chloride solution.
- Mexidol® is administered by jetting slowly during 5 to 7 minutes, by drip at a rate of 40 to 60 drops per minute. Maximum daily dose should not exceed 1200 mg.
- In acute cases of cerebral circulation disorders Mexidol® is used during the first 10-14 days as intravenous dropwise 200-500 mg 2-4 times daily, afterwards intravenously 200-250 mg 2-3 times daily during 2 weeks.
- In case of craniocerebral trauma and craniocerebral injury sequelae, Mexidol® is used for 10 to 15 days with 200-500 mg drip infusion 2 to 4 times daily.
- In decompensated dyscirculatory encephalopathy Mexidol® should be administered by IV streaming or dropwise at a dose of 200-500 mg 1 to 2 times daily during 14 days.
- Thereafter, 100-250 mg/day i.m. should be administered intravenously for the next 2 weeks.
- For course prophylaxis of discirculatory encephalopathy the drug is administered in a monthly dose of 200-250 mg 2 times a day during 10-14 days.
- In case of light cognitive disorders in elderly patients and in case of anxiety disorders, the drug is administered in a daily dose of 100 to 300 mg/day in a daily dose for 14 to 30 days.
- In acute myocardial infarction, Mexidol® is administered intravenously or intramuscularly during 14 days against conventional therapy of myocardial infarction, including nitrates, beta-adrenoblockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulants and antiaggregants, and symptomatic agents as indicated.
- During the first 5 days, to achieve maximum effect, it is desirable to administer the drug intravenously, in the next 9 days, Mexidol® can be given intramuscularly.
- Intravenous drug administration is carried out by drop infusion, slowly (in order to avoid side effects) using 0.9% sodium chloride solution or 5% dextrose (glucose) solution in 100-150 ml volume during 30-90 minutes. If necessary, slow trickle administration of the drug, lasting at least 5 minutes, is possible.
- Administration 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 different stages, Mexidol® is administered intramuscularly in 100 to 300 mg/day, 1 to 3 times a day for 14 days as part of a complex therapy.
In withdrawal alcohol syndrome Mexidol® is administered in dose of 200-500 mg intravenously by drop or intramuscularly 2 to 3 times daily during 5-7 days. - In acute intoxication with antipsychotic agents the drug is administered by IV in a dose of 200 to 500 mg/day for 7 to 14 days. In acute pyo-inflammatory processes of abdominal cavity (acute necrotizing pancreatitis, peritonitis) the drug is prescribed in the first day both preoperatively and postoperatively. Administered doses depend on the form and severity of the disease, process prevalence, variants of the clinical course. Drug should be withdrawn gradually only after a sustained positive clinical and laboratory effect.
- In acute edematous (interstitial) pancreatitis Mexidol® is prescribed 200 -500 mg 3 times daily, by IV drip (in 0.9 % sodium chloride solution) and intramuscularly. Mild degree of severity of necrotic pancreatitis – 100 – 200 mg 3 times a day by IV dropwise (in 0.9% sodium chloride solution) and intravenously. Moderate degree of severity – 200 mg 3 times a day, IV drops (in 0.9% sodium chloride solution). A severe course – in a pulse dosage of 800 mg during the first day, with twice-daily administration; then 200 to 500 mg twice daily with gradual reduction of the daily dose. Extremely severe course – in initial dosage of 800 mg daily until stable relief of pancreatogenic shock; after stabilization, 300 – 500 mg 2 times daily by IV drip (in 0.9% sodium chloride solution) with gradual lowering of daily dosage.
