мексифин

Overdose

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Symptoms: possible development of drowsiness.

Due to the low toxicity of the drug, an overdose is unlikely.

Symptoms: sleep disturbance (insomnia), in rare cases — a slight and short–term (up to 1.5-2 hours) increase in blood pressure.

Treatment: the development of symptoms of overdose, as a rule, does not require the use of relieving agents, these symptoms of sleep disorders disappear independently within a day. In particularly severe cases, it is recommended to use one of the hypnotics and anxiolytics for oral administration (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg). With an excessive increase in blood pressure-the appointment of antihypertensive drugs (under the control of blood pressure).

Symptoms: in case of overdose, sleep disorders are possible (insomnia, in some cases — drowsiness).

Treatment: as a rule, it is not required — the symptoms disappear on their own within a day. In severe cases of insomnia-the appointment of nitrazepam at a dose of 10 mg, oxazepam-10 mg or diazepam-5 mg. With an excessive increase in blood pressure-the appointment of antihypertensive drugs under the control of blood pressure.

Contraindications

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increased individual sensitivity to the drug,

acute renal failure,

acute liver failure.

Due to the lack of knowledge of the drug's action — childhood, pregnancy, breastfeeding.

hypersensitivity to the drug,

acute disorders of liver and kidney function,

pregnancy,

breastfeeding period,

age under 18 (efficacy and safety not established).

hypersensitivity to the drug,

acute liver failure,

acute renal failure,

lactose intolerance, lactase deficiency, and glucose-galactose malabsorption syndrome,

children's age.

hypersensitivity or intolerance to the drug,

acute disorders of the liver and kidneys.

Incompatibilities

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Mexifin® it is combined with all drugs used for the treatment of somatic diseases.

Increases the effect of benzodiazepine drugs, antidepressants, anxiolytics, anticonvulsants, antiparkinsonian agents. Reduces the toxic effects of ethyl alcohol.

Increases the effect of anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa) and benzodiazepine anxiolytics.

Increases the antianginal activity of nitropreparations.

With the combined use of Mexifin® increases the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. Mexifin® reduces the toxic effect of ethanol.

Undesirable effects

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There may be individual adverse reactions of a dyspeptic or dyspeptic nature, allergic reactions.

With an intravenous injection, especially a jet, there may be a dry mouth and a metallic taste, a feeling of spreading warmth throughout the body, a tickling in the throat and a feeling of discomfort in the chest, a feeling of lack of air. As a rule, these phenomena are associated with an excessively fast rate of administration of the drug and are transient in nature.

Against the background of prolonged administration of the drug, the following side effects may occur:

From the gastrointestinal tract: nausea, flatulence.

From the central nervous system: sleep disorders (drowsiness or sleep disturbance).

From the digestive system: nausea, dryness of the oral mucosa, diarrhea.

Other: allergic reactions, drowsiness.

Nausea and dry mouth may occur.

Therapeutic indications

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consequences of acute cerebral circulatory disorders, including after transient ischemic attacks, in the subcompensation phase as preventive courses,

mild traumatic brain injury, the consequences of traumatic brain injuries,

encephalopathies of various origins (dyscirculatory, dysmetabolic, post-traumatic, mixed),

vegetative dystonia syndrome,

mild cognitive disorders of atherosclerotic origin,

anxiety disorders in neurotic and neurosis-like conditions,

ischemic heart disease (as part of complex therapy),

treatment of withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, post-abstinence disorders,

conditions after acute intoxication with antipsychotic drugs,

asthenic conditions,

prevention of the development of somatic diseases under the influence of extreme factors and loads,

the impact of extreme (stressful) factors.

acute myocardial infarction-as part of complex therapy (from the first day of the disease),

ischemic stroke (as part of complex therapy),

dyscirculatory encephalopathy (including atherosclerotic origin),

mild and moderate cognitive disorders of various origins.

anxiety states in neurotic and neurosis-like states,

vegetative-vascular dystonia,

dyscirculatory encephalopathy,

mild cognitive disorders of atherosclerotic origin,

acute disorders of cerebral circulation (as part of combination therapy),

withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders,

acute intoxication with antipsychotic drugs (as part of complex therapy).

acute disorders of cerebral circulation,

dyscirculatory encephalopathy,

vegetative-vascular dystonia,

atherosclerotic disorders of the brain,

neurotic and neurosis-like disorders with the manifestation of anxiety,

relief of withdrawal syndrome in alcoholism with the presence of neurosis-like and vegetative-vascular disorders in the clinical picture, as well as acute intoxication with neuroleptics,

in the complex treatment of acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis).

Pharmacotherapeutic group

  • Nootropics
  • Antihypoxants and antioxidants
  • Anxiolytics
  • Remedies for the correction of disorders in alcoholism, substance abuse and drug addiction

Pharmacodynamic properties

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Mexifin® it 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 the effects of various damaging factors (shock, hypoxia and ischemia, disorders of cerebral circulation, intoxication with alcohol and antipsychotic drugs (neuroleptics).

Mechanism of action of the drug Mexifin® due to 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, increases its fluidity.

Mexifin® modulates the activity of membrane-bound enzymes (calcium-independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structural and functional organization of biomembranes, the transport of neurotransmitters and the improvement of synaptic transmission.

Mexifin® increases the content of dopamine in the brain. It causes an increase in the 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 the energy-synthesizing functions of mitochondria, and stabilization of cell membranes.

The drug improves the metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation.

It 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 LDL.

The antistress 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.

Mexifin® it has a pronounced antitoxic effect in withdrawal symptoms. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, autonomic functions, and is also able to remove cognitive disorders caused by prolonged use of ethanol and its withdrawal.

Under the influence of the drug Mexifin® the effect of tranquilizing, neuroleptic, antidepressant, hypnotic and anticonvulsant drugs increases, which allows you to reduce their doses and reduce side effects.

Mexifin® improves the functional state of the ischemic myocardium. In conditions of coronary insufficiency, it increases the collateral blood supply to the ischemic myocardium, contributes to the preservation of the integrity of cardiocytes and the maintenance of their functional activity. Effectively restores the contractility of the myocardium in reversible cardiac dysfunction.

Mexifin® improves the functional state of the ischemic myocardium in myocardial infarction, improves the contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle. The action of the drug is based on its antioxidant activity, the ability to inhibit free radical processes (pronounced intensification of which is observed in ischemia and myocardial necrosis, especially during reperfusion) and reduce the damaging effect of free radicals on cardiomyocytes. In conditions of a critical decrease in coronary blood flow Mexifin® promotes the preservation of the structural and functional organization of the membranes of cardiomyocytes, stimulates the activity of membrane enzymes — PDE, adenylate cyclase, acetylcholinesterase. The drug supports the activation of aerobic glycolysis that develops in acute ischemia and promotes the restoration of mitochondrial redox processes in hypoxia, increases the synthesis of ATP and creatine phosphate. These mechanisms ensure the integrity of the morphological structures and physiological functions of the ischemic myocardium.

Mexifin® improves the clinical course of myocardial infarction, increases the effectiveness of therapy, accelerates the restoration of the functional activity of the left ventricular myocardium, reduces the frequency of arrhythmic complications and disorders of intracardiac conduction. The drug normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and / or improves the electrical activity and contractility of the myocardium, as well as increases coronary blood flow in the ischemic zone, increases the antianginal activity of nitropreparations, improves the rheological properties of blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency

Mexifin® it has a neuroprotective effect, increases the stability of blood circulation of the brain in hypoperfusion, prevents a decrease in blood flow of the brain in the reperfusion period after ischemia. The drug helps to adapt to the damaging effect of ischemia, inhibiting the depletion of carbohydrate reserves, blocking the postischemic drop in the utilization of glucose and oxygen by the brain and preventing the progressive accumulation of lactate.

Mexifin® improves and stabilizes brain metabolism and blood supply to the brain, improves the rheological properties of blood and microcirculation. The drug supports the functional activity of the brain, both during ischemia and in the post-ischemic period. Mexifin® it has a selective, not accompanied by sedation and muscle relaxation, anxiolytic effect, eliminates anxiety, fear, tension, anxiety.

Mexifin® it has nootropic properties, prevents and reduces learning and memory disorders that occur in vascular diseases of the brain (ischemic stroke, dyscirculatory encephalopathy), in mild and moderate cognitive disorders, has an antihypoxic effect, increases concentration and performance.

Inclusion of the drug Mexifin® in complex therapy of patients with acute circulatory disorders of the brain, it reduces the severity of clinical manifestations of stroke and improves the course of the rehabilitation period.

Mexifin® it is an inhibitor of free radical processes, a membrane protector. It also has antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic effects. It belongs to the class of 3-oxypyridines.

Mechanism of action of Mexifin® due to its antioxidant and membrane-protective effect. The drug inhibits lipid peroxidation, increases the activity of superoxidase, increases the lipid-protein ratio, improves the structure and function of the cell membrane.

Mexifin® modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structural and functional organization of biomembranes, the transport of neurotransmitters and the improvement of synaptic transmission. Mexifin® increases the content of dopamine in the brain. It causes an increase in the 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 the energy-synthesizing functions of mitochondria.

Increases the body's resistance to the effects of various damaging factors in pathological conditions (hypoxia and ischemia, disorders of cerebral circulation, intoxication with ethanol and antipsychotic drugs).

In conditions of a critical decrease in coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes-phosphodiesterase, adenylate cyclase, acetylcholinesterase. Supports the activation of aerobic glycolysis that develops in acute ischemia and promotes the restoration of mitochondrial redox processes in hypoxia, increases the synthesis of ATP and creatine phosphate. Ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium. Improves the clinical course of myocardial infarction, increases the effectiveness of therapy, reduces the frequency of arrhythmias and disorders of intracardiac conduction. Normalizes metabolic processes in the ischemic myocardium, increases the antianginal activity of nitrates, improves the rheological properties of blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency

Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Improves the metabolism and blood supply to the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. It stabilizes the membranes of blood cells (red blood cells and platelets), reducing the likelihood of hemolysis.

It has a hypolipidemic effect, reduces the content of total cholesterol and LDL.

Mexidol is an antioxidant - inhibitor of free radical processes, which has antihypoxic, stress-protective, antiamnestic, and anxiolytic effects. The drug increases the body's resistance to the effects of extreme factors and oxygen-dependent pathological conditions (shock, hypoxia, disorders of cerebral circulation), prevents and reduces the toxic effects of ethyl alcohol.

Pharmacokinetic properties

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It is rapidly absorbed when taken orally. When taken orally in doses of 400-500 mg Cmax it is 3.5-4 mcg/ml. 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 with the participation of alkaline phosphatase breaks down into phosphoric acid and 3-oxypyridine, the 2nd metabolite-pharmacologically active, is formed in large quantities and is detected in the urine on day 1-2 after administration, the 3rd — is excreted in large quantities in the urine, the 4th and 5th-glucuronconjugates.

T1/2 when taken orally-2-2. 6 hours. 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. Indicators of urinary excretion of unchanged drug and metabolites have individual variability.

With intravenous administration, the drug quickly (within 0.5–1.5 hours) passes from the bloodstream to organs and tissues, and therefore its concentration in unchanged form quickly decreases. With intravenous administration in therapeutic doses Cmax the drug in the blood plasma is reached in 30-40 minutes and is 2.5-3 mcg/ml, while its metabolites are determined in the blood plasma for 7-9 hours.

The drug is excreted from the body in the urine in glucuronoconjugated form, as well as in small amounts in unchanged form.

Suction and distribution. It is rapidly absorbed when taken orally (the half-absorption period is about 1 h). Tmax when taken orally-0.5 h. Cmax when taken orally-50-100 ng / ml. It is rapidly distributed in organs and tissues. The average retention time of ethylmethylhydroxypyridine succinate in the body when taken orally is about 5 hours.

Metabolism. It is metabolized in the liver by glucuronidation. 5 metabolites were identified: 3-oxypyridine phosphate-is formed in the liver and with the participation of alkaline phosphatase breaks down into phosphoric acid and 3-oxypyridine, the 2nd metabolite-pharmacologically active, is formed in large quantities and is detected in the urine on day 1-2 after administration, the 3rd — is excreted in large quantities in the urine, the 4th and 5th-glucuronconjugates.

Output. T1/2 when taken orally-4-5 hours. It is rapidly excreted in the urine mainly in the form of metabolites (50% in 12 hours) and in a small amount (0.3% in 12 hours) - in an unchanged form. It is most intensively excreted during the first 4 hours after taking the drug. Indicators of urinary excretion of unchanged drug and metabolites have individual variability.

Name of the medicinal product

Mexifin

Qualitative and quantitative composition

Ethylmethylhydroxypyridine Succinate

Dosage (Posology) and method of administration

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Inside, 125-250 mg 3 times a day, the maximum daily dose is 800 mg (6 tables).

The duration of treatment is 2-6 weeks, for the relief of 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 at least 1.5-2 months. Repeated courses (on the recommendation of a doctor), it is desirable to conduct in the spring and autumn periods.

V / m or v / v (jet or drip).

In the treatment of acute myocardial infarction, I/v or I/m is administered for 14 days, against the background of traditional therapy for myocardial infarction, including nitrates, beta-blockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic agents as indicated.

In the first 5 days, to achieve maximum effect, the drug should be administered intravenously, in the next 9 days-intravenously.

Intravenous administration of the drug is performed by drip infusion, slowly (to avoid side effects), on a saline solution or 5% dextrose (glucose) solution in a volume of 100-150 ml for 30-90 minutes. If necessary, a slow jet injection of the drug is possible, lasting at least 5 minutes.

Administration of the drug (intravenous or intravenous) is carried out 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg/kg / day, a single one-2-3 mg/kg. The maximum daily dose should not exceed 800 mg, a single dose-250 mg.

In acute disorders of cerebral circulation (ischemic stroke) Mexifin® used in complex therapy in the first 2-4 days of IV, drip 200-300 mg 2-3 times a day, then-in / m 100 mg 3 times a day. The duration of treatment is 10-14 days. In the future, the drug is prescribed in capsules of 100 mg 2 times a day for 14 days and 100 mg 3 times a day for the next 7 days. The frequency and duration of repeated courses of therapy is determined by the doctor.

In dyscirculatory encephalopathy in the decompensation phase of Mexifin® it should be prescribed in / in a jet or drip at a dose of 100 mg 2-3 times a day for 14 days. Then the drug is administered in / m at 100 mg per day for the next 2 weeks. In the future, the drug is prescribed in capsules of 100 mg 2-4 times a day (on the recommendation of a doctor), the frequency and duration of therapy courses is determined by the doctor.

For the course prevention of dyscirculatory encephalopathy, the drug is administered in / m at a dose of 100 mg 2 times a day for 10-14 days.

For the treatment of mild to moderate cognitive disorders Mexifin® assign in/m at a dose of 100-300 mg per day for 14 days. If necessary, in the future, the drug is prescribed in capsules of 100 mg 2-4 times a day (on the recommendation of a doctor), the frequency and duration of therapy courses is determined by the doctor.

Inside 125-250 mg 3 times a day. 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 750 mg (6 tablets). The duration of treatment is 2-6 weeks.

Treatment of withdrawal syndrome (complex therapy) - 250-500 mg 3 times a day.

Treatment is stopped gradually, reducing the dose for 2-3 days.

Solution for intravenous and intramuscular administration

V / m, v / v (jet or drip). The doses are selected individually. With the infusion method of administration, the drug should be diluted in a saline solution of sodium chloride. Start treatment with a dose of 50-100 mg 1-3 times a day, gradually increasing the dose until a therapeutic effect is obtained. Jet drug Mexifin® enter slowly for 5-7 minutes, drip-at a rate of 40-60 drops per minute. The maximum daily dose does not exceed 800 mg.

In acute disorders of cerebral circulation (in complex therapy): in the first 2-4 days-in / in drip 200-300 mg/day, then-in / m 100 mg 3 times a day. The duration of treatment is 10-14 days.

In case of dyscirculatory encephalopathy in the decompensation phase: intravenous jet or drip at a dose of 100 mg 2-3 times a day for 14 days. Then the drug is administered in / m at 100 mg/day for the next 2 weeks. For the course prevention of dyscirculatory encephalopathy, the drug is administered in / m at a dose of 100 mg 2 times a day for 10-14 days.

In mild cognitive impairment in elderly patients and in anxiety disorders: the drug is used in / m in a daily dose of 100-300 mg for 14-30 days.

With alcohol withdrawal syndrome: I / m at a dose of 100-200 mg 2-3 times a day or I / v drip 1-2 times a day for 5-7 days.

In acute intoxication with antipsychotic drugs: i / v at a dose of 50-300 mg/day for 7-14 days.

Film-coated tablets

Inside. The therapeutic doses used and the duration of treatment are determined by the sensitivity of patients to the drug. Start treatment with a dose of 0.25-0.5 g, the average daily dose is 0.25-0.5 g, the maximum-0.8 g. The daily dose of the drug is distributed in 2-3 doses during the day.

For the treatment of patients with anxiety disorders, vegetative-vascular dysfunction and cognitive impairment the drug Mexifin® apply for 2-6 weeks.

When relieving alcohol withdrawal syndrome the drug Mexifin® apply for 5-7 days.

Course therapy with Mexifin® finish gradually, reducing the dose for 2-3 days.

In/m or v/v (jet or drip). For intravenous administration, water for injection is used as a solvent. Jet mexidol is administered for 5-7 minutes, drip-at a rate of 60 drops per minute. The doses are selected individually.

Start treatment with a dose of 0.05-0.1 g 1-3 times a day, gradually increasing the dose until a therapeutic effect is obtained. The duration of treatment and the choice of individual dose depends on the severity of the patient's condition and the effectiveness of treatment. The maximum daily dose should not exceed 0.8 g.

For the treatment of atherosclerotic dementia in elderly patients, mexidol is prescribed in / m at a dose of 0.1–0.3 g/day.

In acute intoxication with neuroleptics, the drug is injected into a vein at a dose of 0.5–0.3 g/day.

In the complex treatment of acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis), mexidol is prescribed in a single dose of 200 mg 3 times a day. In severe cases, the drug is diluted in 200 ml of a physiological 0.9% sodium chloride solution and administered at a rate of 40-60 drops per minute. With a lighter course of the disease, mexidol is administered in/m. The course of treatment is 3-10 days.

ATC - Anatomical and therapeutic chemical classification

N07XX Other drugs for the treatment of diseases of the nervous system