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Dosage form
Tablets, film-coated from white to white with kremovatam white color, round, lenticular.
Composition
etilmetilgidroksipiridina succinate 125 mg
Excipients: lactose monohydrate, povidone, magnesium stearate.
The composition of the shell: Opadry II 33G28435 white (hypromellose, titanium dioxide, lactose monohydrate, polyethylene glycol (macrogol), triacetin)
Pharmacological action
Mexidol® is an inhibitor of free radical processes, membraneelectrode having antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic action. The drug increases organism resistance to influence of various damaging factors (shock, hypoxia and ischemia, cerebrovascular accident, alcohol intoxication and antipsychotic means (neuroleptics)).
The mechanism of action of Mexidol® due to its antioxidant, antihypoxic and membrane-protective action. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the ratio of lipid-protein reduces the viscosity of the membrane increases its fluidity. Mexidol® modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine) that enhances their capability to bind to ligands, contributes to maintaining the structural and functional organization of biological membranes, transport of neurotransmitters and improve synaptic transmission. Mexidol® increases the content in brain dopamine. Causes increased compensatory activation of aerobic glycolysis and reducing the degree of oppression oxidizing processes in the Krebs cycle in hypoxia with an increase in the content of ATP and creatine phosphate, activation energosintezirutuyu functions of mitochondria, stabilization of cell membranes.
The drug improves metabolism and blood supply of the brain, improves microcirculation and blood rheology, reduces platelet aggregation. Stabilizes the membrane structure of red blood cells (erythrocytes and platelets) in the blood. Has hypolipidemic effect, reduces total cholesterol and low density lipoprotein.
Anti-stress effect is to normalize post-stress behavior, SOMATO-vegetative disorders, recovery cycles of sleep-wakefulness, impaired learning and memory, decreasing of dystrophic and morphological changes in different brain structures.
Mexidol® has a strong antitoxic effect in withdrawal syndrome. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication, restores normal behavior, autonomic functions, and is able to remove the cognitive impairment caused by long-term administration of ethanol and its abolition. Under the influence of Mexidol® increases the effect anxiolytic, neuroleptic, antidepressant, tranquilizers and anticonvulsants, which can reduce their dose and reduce side effects. Mexidol® improves the functional state of the ischemic myocardium. In conditions of coronary insufficiency increases collateral blood flow to ischemic myocardium and helps to preserve the integrity of kardiomiotsitov and maintaining their functional activity. Effectively restores the airway diseases in reversible cardiac dysfunction.
Pharmacokinetics
Quickly absorbed by ingestion. The maximum concentration at doses of 400 - 500mg is 3.5 - 4.0 µg/ml is Rapidly distributed to organs and tissues. The average time of retention of the drug in the body the ingestion of 4.9 - 5.2 h. Metabolised in the liver by glukuronirovania. Identified 5 metabolites: 3-hydroxypyridine phosphate is formed in the liver and involvement of alkaline phosphatase breaks down into phosphoric acid and 3-hydroxypyridine; 2-th metabolite is pharmacologically active, it is formed in large quantities and is found in the urine for 1 - 2 hours after the administration; The 3rd is excreted in large quantities in the urine; 4th and 5th - glucuroconjugated. T1/2 the ingestion - 2,0 - 2,6 h is Rapidly excreted in the urine mainly as metabolites and in small amounts in unchanged form. The most intensively excreted during the first 4 h after administration of the drug. Indicators of urine excretion of unchanged drug and metabolites have individual variability
Side effects
From the digestive system: dyspepsia.
Other: allergic reactions.
Special conditions
Effects on ability to drive vehicles and management mechanisms
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.
Testimony
-the consequences of acute stroke, including after transient ischemic attacks in phase subcompensation as prophylactic courses;
-mild traumatic brain injury, consequences of craniocerebral injuries;
-encephalopathy of different Genesis (dyscirculatory, dysmetabolic, posttraumatic, mixed);
syndrome vegetative dystonia;
-mild cognitive disorder atherosclerotic Genesis;
-anxiety disorders with neurotic and neurosis-like States;
-coronary heart disease in the complex therapy;
-relief of withdrawal syndrome in alcoholism with the prevalence of neurosis and vegetative-vascular disorders, post-abstinent disorders;
-conditions after acute intoxication antipsychotic means;
-asthenic conditions, and also to prevent the development of somatic diseases under the influence of extreme factors and loads;
-exposure to extreme (stress) factors.
Contraindications
Acute hepatic and/or renal failure, increased individual sensitivity to the drug.
In connection with the insufficient study of the drug, child age, pregnancy, breast-feeding
Drug interactions
Mexidol® compatible with all drugs used for the treatment of somatic diseases. Increases the effect of benzodiazepine drugs, antidepressants, anxiolytics, anticonvulsants and antiparkinsonian drugs. Reduces the toxic effects of ethanol.