Mexidol, 5%, 5 ml, 20 pcs.

Pharmacological group

Antioxidant drug.

Pharmacological action

It has antihypoxic, membrane protective, nootropic, anticonvulsant and anxiolytic action, increases the body’s resistance to stress. The preparation increases resistance to the effects of major 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) during hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL.

Limits enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of Mexidol® is based on its antihypoxic, antioxidant and membranoprotective actions. The drug inhibits lipid peroxidation processes, increases the activity of superoxide dismutase, increases the ratio “lipid-protein”, 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 increases their ability to bind to ligands, helps maintain the structural and functional organization of biomembranes, transport neurotransmitters 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 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 detected in plasma for 4 hours after IV/Introduction. The 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 insignificant amounts in unchanged form.

Indications

Active ingredient

Composition

The solution for intravenous and intravenous administration is colorless or slightly yellowish, transparent.

1 ml of the solution contains:

Active substances:

ethylmethylhydroxypyridine succinate 50 mg.

Excipients:

Sodium metabisulfite – 1 mg,

water d/i – up to 1 ml.

In an ampoule there are 2 or 5 ml of solution.

There are 5 ampoules in the carton pack.

In a carton pack of 1, 2, 4, 10 or 20 carton packs.

How to take, the dosage

Dosage and administration method

Mexidol® is administered intramuscularly or intravenously (by trickle or drip). For preparation of solution for infusion the drug should be diluted in 0.9% sodium chloride solution.

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

Dosage regimen depending on symptoms

In acute disorders of cerebral circulation Mexidol® is used in the first 10-14 days by IV drip 200-500 mg 2-4 times/day, then by IM 200-250 mg 2-3 times/day for 2 weeks.

In case of craniocerebral trauma and consequences of craniocerebral trauma Mexidol® is used for 10-15 days with 200-500 mg 2-4 times per day in the form of IV drops.

In patients with discirculatory encephalopathy in decompensation phase Mexidol® is used by IV streaming or dropwise in dose 200-500 mg 1-2 times per day during 14 days, then in 100-250 mg/day by injection for the next 2 weeks. For prophylaxis of discirculatory encephalopathy Mexidol® is administered in a monthly dose of 200-250 mg 2 times a day during 10-14 days.

In case of mild cognitive impairment in elderly patients and in case of anxiety disorders Mexidol® is administered in a dosage of 100-300 mg/day in the dosage for 14-30 days.

In acute myocardial infarction, as part of complex therapy, Mexidol® is administered by IV or IM over 14 days with traditional therapy of myocardial infarction including nitrates, beta-adrenoblockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic agents according to indications.

In the first 5 days, for maximum effect the drug should be administered by IV, in the next 9 days Mexidol® can be administered by IV.

Intravenous administration of the drug 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 the volume of 100-150 ml for 30-90 minutes. If necessary, slow trickle administration of the drug for at least 5 minutes is possible.

The drug is administered (intravenously or intramuscularly) 3 times/day every 8 hours. The daily therapeutic dose is 6-9 mg/kg of body weight/day, single dose – 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, the single dose is 250 mg.

In case of various stages of open-angle glaucoma in combination therapy Mexidol® is administered in a monthly dose of 100-300 mg/day 1-3 times/day for 14 days.

In patients with alcohol withdrawal syndrome Mexidol® is administered in a dose of 200-500 mg by IV drops or intravenously 2-3 times per day for 5-7 days.

In acute intoxication with antipsychotic agents Mexidol® is administered in a dose of 200-500 mg/day in 7-14 days.

In acute pyo-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis) Mexidol® is prescribed during the first day, both in the preoperative and in the postoperative period. Doses administered depend on the form and severity of the disease, prevalence of the process, variants of the clinical course. Withdrawal of the drug should be done gradually, only after a sustained positive clinical and laboratory effect.

In acute edematous (interstitial) pancreatitis Mexidol® is prescribed in 200-500 mg 3 times per day by IV drop (in sodium chloride isotonic solution) and intravenously.

In mild necrotizing pancreatitis Mexidol® is prescribed 100-200 mg 3 times per day by IV drip (in sodium chloride isotonic solution) and intravenously.

In moderately severe necrotizing pancreatitis 200 mg 3 times/day by IV drop (in isotonic sodium chloride solution).

In severe necrotizing pancreatitis – in pulse dosage of 800 mg during the first day, twice daily, further 200-500 mg 2 times per day with gradual decrease of daily dose.

In extremely severe form of necrotic pancreatitis initial dose is 800 mg/day till firm relief of pancreatogenic shock; after stabilization of condition – by 300-500 mg 2 times/day by IV drops (in 0.9% sodium chloride solution) with gradual lowering of daily dose.

Interaction

Mexidol® enhances the effects of anxiolytics of benzodiazepine derivatives, anti-Parkinsonian (levodopa) and anticonvulsants (carbamazepine).

Mexidol® reduces the toxic effects of ethanol.

Special Instructions

Precautionary measures when taking the drug

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

Interaction with alcohol

Mexidol® reduces the toxic effects of ethanol.

Prescription conditions

The drug is available with a prescription.

Contraindications

The contraindication to the use of Mexidol is:

Strictly controlled clinical trials of safety of Mexidol® preparation use in children and during pregnancy and lactation have not been conducted.

Side effects

When using the drug it is possible:

In the digestive system: nausea and dry mouth may occur.

Other: allergic reactions, drowsiness.

Overdose

In case of overdose, drowsiness may develop.

Pregnancy use

The use of Mexidol® is not recommended during pregnancy and lactation (breast-feeding) due to insufficient study of the drug action.

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

Similarities