Composition
Active ingredient:
ethylmethylhydroxypyridine succinate (2-ethyl-6-methyl-3-hydroxypyridine succinate) – 125.0 mg
Auxiliary substances:
lactose monohydrate-97.5 mg,
povidone-25.0 mg,
magnesium stearate-2.50 mg
Film shell:
opadray II white 33G28435 – 7.5 mg (hypromellose-3.0 mg, titanium dioxide-1.875 mg, lactose monohydrate-1.575 mg, polyethylene glycol (macrogol) – 0.6 mg, triacetin-0.45 mg)
Pharmacological action
Mexidol® is an inhibitor of free radical processes, a membrane protector with antihypoxic, stress-protective, nootropic, anticonvulsant and anxiolytic effects. The drug increases the body’s resistance to various damaging factors (shock, hypoxia and ischemia, cerebral circulation disorders, alcohol intoxication and antipsychotic drugs (neuroleptics)).
Mechanism of action of Mexidol® It is caused by its antioxidant, antihypoxant and membrane-protective effects. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, reduces the viscosity of the membrane, and increases its fluidity. Mexidol® modulates the activity of membrane-bound enzymes (calcium 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 the level of dopamine in the brain. It causes an increase in compensatory activation 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 and creatine phosphate, activation of energy-synthesizing functions of mitochondria, and stabilization of cell membranes.
The drug improves 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 content of total cholesterol and low-density lipoproteins.
The anti-stress effect is manifested in the normalization of post-stress behavior, somatovegetative disorders, restoration of sleep-wake cycles, impaired learning and memory processes, and reduction of dystrophic and morphological changes in various brain structures.
Mexidol® it has a pronounced antitoxic effect in withdrawal symptoms. It eliminates neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, autonomic functions, and is also able to relieve cognitive disorders caused by prolonged use of ethanol and its withdrawal. Under the influence of Mexidol®, the effect of tranquilizing, antipsychotic, antidepressant, hypnotic and anticonvulsants increases, which allows them to reduce their doses and reduce side effects. Mexidol ® improves the functional state of the ischemic myocardium. In conditions of coronary insufficiency, it increases the collateral blood supply to the ischemic myocardium, helps preserve the integrity of cardimiocytes and maintain their functional activity. Effectively restores myocardial contractility in patients with reversible cardiac dysfunction.
Pharmacokinetics
Suction
It is rapidly absorbed when taken orally. The maximum concentration at doses of 400-500 mg is 3.5-4.0 mcg / ml.
Distribution
It is rapidly distributed in organs and tissues. The average retention time of the drug in the body when taken orally is 4.9-5.2 hours. It is metabolized in the liver by glucuronconjugation. 5 metabolites were identified: 3-oxypyridine phosphate-is formed in the liver and breaks down into phosphoric acid and 3-oxypyridine with the participation of alkaline phosphatase; the 2nd metabolite is pharmacologically active, is formed in large quantities and is detected in the urine on the 1st-2nd day after use; the 3rd – is excreted in large quantities in the urine; the 4th and 5th – glucuronconjugates. T 1/2 when taken orally – 2.0 – 2.6 hours.
Deduction
It is rapidly excreted in the urine mainly in the form of metabolites and in a small amount – in unchanged form. It is most intensively excreted during the first 4 hours after taking the drug. Urinary excretion rates of unchanged drug and metabolites have individual variability.
Indications
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of effects of acute disorders of cerebral circulation, including after transient ischemic attacks, in the phase of decompensation as a preventive courses;
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easy traumatic brain injury, the consequences of traumatic brain injury;
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encephalopathy different Genesis (dyscirculatory, dysmetabolic, post-traumatic, mixed);
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the syndrome of vegetative dystonia;
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mild cognitive dysfunction of atherosclerotic;
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anxiety disorders in neurotic and neurosis-like States;
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condition after acute intoxication with antipsychotic funds;
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asthenic conditions, and to prevent the development of somatic diseases under the influence of extreme factors and stress;
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the impact of extreme (stress) factors.
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ischemic heart disease as part of complex therapy;
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relief of withdrawal symptoms in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, post-withdrawal disorders
Use during pregnancy and lactation
Strictly controlled clinical studies on the safety of Mexidol® during pregnancy and lactation have not been conducted.
Contraindications
Contraindication to the use of Mexidol is:
- acute liver failure;
- acute renal failure;
- hypersensitivity to the drug.
Due to insufficient knowledge of the drug’s action:
- children’s age;
- pregnancy;
- lactation (breast-feeding).
Side effects
When using the drug, you may: :
From the digestive system: individual adverse reactions of a dyspeptic or dyspeptic nature may occur.
Other: possible allergic reactions.
Interaction
Mexidol® is combined with all medications used for the treatment of somatic diseases.
When used together, Mexidol ® enhances the effect of benzodiazepine derivatives, antidepressants, anxiolytics, antiparkinsonian and anticonvulsants.
Mexidol ® reduces the toxic effect of ethanol.
How to take, course of use and dosage
Method of use and dosage regimen depending on the symptoms
Inside 125-250 mg 3 times a day; the maximum daily dose is 800 mg (6 tablets). Duration of treatment-2-6 weeks; for stopping alcohol withdrawal – 5-7 days. Treatment is stopped gradually, reducing the dose for 2-3 days.
The initial dose is 125-250 mg (1-2 tablets) 1-2 times a day with a gradual increase until a therapeutic effect is obtained; the maximum daily dose is 800 mg (6 tablets).
The duration of the course of therapy in patients with CHD is not less than 1.5-2 months. Repeated courses (on the recommendation of a doctor) should preferably be carried out in the spring and autumn periods.
Overdose
In case of overdose, drowsiness may develop.
Special instructions
Precautions when taking the drug
Mexidol® can be combined with all medications used for the treatment of somatic diseases.
Use in pediatrics
Mexidol® is not prescribed to children due to insufficient knowledge of the drug’s action.
Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention
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.
Interaction with alcohol
Mexidol ® reduces the toxic effect of ethanol.
Conditions of release from pharmacies
The drug is available on prescription.
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C
Shelf life
3 years
Active ingredient
Ethylmethylhydroxypyridine Succinate
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as directed by your doctor
Indications
Concussion and other traumatic brain injuries, Cerebral circulation disorders, Atherosclerosis, Stroke effects, Hangover, Vegetative-vascular disorders, Neurosis, Asthenia, Stress, Exposure to adverse factors
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