Mexidol, 50 mg/ml 2 ml 10 pcs

Pharmacodynamics

Mexidol® has antihypoxic, membranoprotective, nootropic, anticonvulsant, anxiolytic effect, increases resistance to stress. The preparation increases resistance to the main damaging factors, to oxygen-dependent pathological states (shock, hypoxia and ischemia, cerebral circulation disorders, intoxication by 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.

The mechanism of action of Mexidol® is due to its antihypoxant, antioxidant and membranoprotective actions. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the 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. 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 ischemic myocardium, reduces the zone of necrosis, restores and improves myocardial electrical activity and contractility as well as increases coronary blood flow in ischemic area and reduces consequences of reperfusion syndrome in acute coronary failure. Increases antianginal activity of nitropreparations.

Mexidol® promotes the preservation of retinal ganglion cells and optic nerve fibers at progressive neuropathy caused by chronic ischemia and hypoxia. It improves the functional activity of the retina and the optic nerve, increasing visual acuity.

Pharmacokinetics

Intake

When Mexidol® is administered in doses of 400-500 mg, the Cmax in plasma is 3.5-4.0 µg/mL and is reached within 0.45-0.5 h.

Distribution

The drug is detectable in plasma for 4 hours after IV/m administration. Average retention time of the drug in the body is 0.7-1.3 h.

Elimination

Extracted from the body with urine mainly in glucuron-conjugated form and in small amounts unchanged.

Indications

Active ingredient

Composition

Active substance:

Ethylmethylhydroxypyridine succinate 50 mg;

Auxiliary substances:

Sodium metabisulfite – 0.4 mg,

water d/i – up to 1 ml.

How to take, the dosage

I/m or intravenously (by jet or drip). When administering by infusion the drug should be diluted in 0.9% sodium chloride solution.

Inject Mexidol® by jetting slowly over 5 to 7 minutes, by drip at a rate of 40 to 60 drops per minute. The maximum daily dose should not exceed 1200 mg.

In case of acute disturbances of cerebral circulation Mexidol® is used in the first 10-14 days – by IV drops 200-500 mg 2-4 times a day, then by IV drops 200-250 mg 2-3 times a day for 2 weeks.

In case of craniocerebral trauma and craniocerebral injury sequelae Mexidol® is used for 10 to 15 days with 200 to 500 mg by IV drip 2 to 4 times daily.

In patients with dyscirculatory encephalopathy in the decompensation phase Mexidol® should be administered by IV streams or by drop infusion at a dose of 200-500 mg 1 to 2 times daily during 14 days. Then 100 to 250 mg/day in a v/m dose 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 for 10 to 14 days.

In mild cognitive impairment in elderly patients and in patients with anxiety disorders the drug is used in a daily dosage of 100 to 300 mg/day in a daily dose for 14 to 30 days.

. In acute myocardial infarction within complex therapy Mexidol® is administered intravenously or intramuscularly during 14 days against the background of traditional therapy of myocardial infarction including nitrates, beta-adrenoblockers, angiotensin-converting enzyme inhibitors (ACE), thrombolytics, anticoagulant and antiaggregant agents and symptomatic agents by indications.

In the first 5 days, for maximum effect the drug should be administered intravenously; in the next 9 days Mexidol® can be given intramuscularly.

Intravenous administration of the drug is carried out by drop infusion slowly (in order to avoid side effects) with 0.9% sodium chloride solution or 5% dextrose (glucose) solution in the volume of 100-150 ml during 30-90 minutes. If necessary, slow trickle administration of the drug, lasting at least 5 minutes, is possible.

Injection 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 daily for 14 days as part of complex therapy.

In patients with alcohol withdrawal syndrome Mexidol® is administered in a dose of 200 – 500 mg intravenously by IV drip or intramuscularly 2 – 3 times daily for 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 the abdominal cavity (acute necrotizing pancreatitis, peritonitis) the drug is prescribed in the first day both in the preoperative and in the postoperative period. Administered doses depend on the form and severity of the disease, process prevalence, variants of the clinical course. Withdrawal of the drug should be carried out gradually only after sustained positive clinical and laboratory effect.

In acute edematous (interstitial) pancreatitis Mexidol® is prescribed in 200 -500 mg 3 times a day, by infusion (in 0.9% sodium chloride solution) and intravenous drip. 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). Severe course – in a pulse dosage of 800 mg in the first day, with twice-daily mode of administration; further 200 – 500 mg 2 times a day with gradual reduction of the daily dose.

Extremely severe course – in initial dosage of 800 mg/day till firm relief of pancreatogenic shock; after stabilization of condition – 300 – 500 mg 2 times a day by IV drop (in 0.9 % sodium chloride solution) with gradual decrease of daily dose.

Interaction

When used together, Mexidol® increases the effect of anxiolytics of benzodiazepine derivatives, antiparkinsonics (levodopa) and anticonvulsants (carbamazepine).

Mexidol® reduces the toxic effects of ethyl alcohol.

Special Instructions

Mexidol can be combined with all drugs used for the treatment of somatic diseases.

Pediatric use

Strictly controlled clinical safety studies of Mexidol® in children have not been conducted.

Impact on driving and operating machinery

When using the drug, caution must be exercised while driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

In individual cases, especially in predisposed patients with bronchial asthma with hypersensitivity to sulfites, severe hypersensitivity reactions may develop.

Contraindications

Strictly controlled clinical studies of safety of Mexidol® usage in children and during pregnancy and lactation have not been conducted.

Side effects

Digestive system: rarely – nausea, dry mouth.

Others: rare – allergic reactions.

Overdose

Symptoms: possible development of drowsiness.

Similarities