Ethylmethylhydroxypyridine Succinate: instructions for use, price and reviews

Pharmacodynamics and pharmacokinetics

The mechanism of action of the drug is due to its membrane protective and antioxidant properties. The substance can increase the activity of the enzyme superoxide oxidase , stabilize and improve the functional activity of cell membranes. Ethylmethylhydroxypyridine succinate stimulates the functioning of membrane-binding enzymes, calcium-independent phosphodiesterase , acetylcholinesterase , cyclase , benzodiazepine receptor complex gamma-aminobutyric acid receptors , acetylcholine complex . This property helps preserve the structural and functional organization of biomembranes , stabilize the work of synapses , and enhance the transport of neurotransmitters . When taking the drug systematically, the concentration of dopamine in the brain increases.

Under conditions of insufficient oxygen supply to cells, the substance enhances the process of aerobic glycolysis through a compensatory mechanism, increases the production of ATP and creatine phosphate , and activates mitochondria .

The body becomes more resistant to the effects of adverse environmental factors, to shock , ischemia and hypoxia , various intoxications , including ethanol , and circulatory disorders in the brain.

Preparations based on ethylmethylhydroxypyridine succinate inhibit platelet , stimulate metabolism, and improve microcirculation in the brain. The drug also reduces the level of cholesterol in the blood and lipoproteins , improves heart function after myocardial infarction and stroke , the functions of the left ventricle are restored faster, normal cerebral circulation normalizes faster, and a minimum number of cells (necrotic tissue) dies. Under hypoxic , the substance prevents a decrease in the intensity of ATP , ORR , and electrical activity.

Ethylmethylhydroxypyridine succinate also increases the activity of other drugs used as part of the complex treatment of ischemia, heart attacks and strokes , for example, nitro drugs . The drug can reduce intoxication in acute pancreatitis .

After oral administration, it is quickly absorbed in the gastrointestinal tract, in about 60 minutes. When administered intramuscularly, the maximum concentration is maintained for 4 hours. After intramuscular administration, the substance reaches its maximum in the blood within 25-50 minutes. The drug is quickly distributed to organs and tissues and undergoes metabolic reactions in the liver ( glucuronidation ). There are 5 metabolites of Ethylmethylhydroxypyridine succinate: inactive 3-hydroxypyridine phosphate , glucuroconjugants , 2 more active metabolites.

The half-life after oral administration is up to 5 hours. The drug is excreted in the form of inactive metabolites or in its original form through the kidneys within 12 hours. The most active process occurs in the first 4 hours.

Mexican caps. 100 mg 60 pcs

Pharmacological group:

antioxidant agent
Pharmacodynamics:
Ethylmethylhydroxypyridine succinate has antioxidant, antihypoxic, anti-ischemic, membrane-protective, nootropic, stress-protective, anticonvulsant, anxiolytic effects.

The drug helps to increase the body's resistance to the effects of various damaging factors in oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular accidents, coronary heart disease, ethanol intoxication and the state after intoxication with antipsychotic drugs). The drug reduces the manifestations of oxidative stress, inhibits free radical processes of lipid peroxidation, and increases the activity of superoxide dismutase. Modulates the activity of membrane-bound enzymes - calcium independent phosphodiesterase, adenylate cyclase, acetylcholinesterase, receptor complexes (benzodiazepine, gamma-aminobutyric, acetylcholine), which enhances their ability to bind to ligands, helps preserve the structural and functional organization of biological membranes, improves the transport of neurotransmitters and synaptic transmission. Increases dopamine levels in the brain.

The drug causes an increase in the compensatory activity of aerobic glycolysis and helps reduce the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in the content of adenosine triphosphate, creatine phosphate and activation of the energy-synthesizing functions of mitochondria, stabilization of cell membranes.

The energy-synthesizing effect of the drug is associated with an increase in the delivery and consumption of succinate by cells, the implementation of the phenomenon of rapid oxidation of succinic acid by succinate dehydrogenase, as well as with the activation of the mitochondrial respiratory chain. When ethylmethylhydroxypyridine succinate dissociates in a cell into succinate and a 3-hydroxypyridine derivative (base), the base exhibits an antioxidant effect that stabilizes cell membranes and restores the functional activity of cells.

The drug improves the functional state of ischemic myocardium during myocardial infarction, improves the contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle. Normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores the electrical activity and contractility of the myocardium, and also increases its collateral blood supply, activating energy-synthesizing processes in the ischemic zone and helping to preserve the integrity of cardiomyocytes and maintain their functional activity. Effectively restores myocardial contractility in case of reversible cardiac dysfunction, which represents a significant reserve for increasing cardiac contractility in patients with coronary heart disease.

In patients with stable angina pectoris, it increases exercise tolerance and the antianginal activity of nitro drugs, improves the rheological properties of blood, reduces platelet aggregation and the consequences of reperfusion syndrome in acute coronary insufficiency. It has a lipid-lowering effect, reduces the content of total cholesterol and low-density lipoproteins.

Improves blood supply to the brain and cerebral metabolism, improves blood microcirculation, prevents a decrease in cerebral blood flow during the reperfusion period after ischemia. Prevents a post-ischemic drop in the utilization of glucose and oxygen by the brain, and prevents the progressive accumulation of lactate. The drug has a selective anxiolytic effect, not accompanied by sedation and muscle relaxation, eliminates anxiety, fear, tension, restlessness, increases adaptation and emotional status.

The effectiveness of the drug under stressful conditions is manifested in the normalization of post-stress behavior, psycho-vegetative disorders, restoration of sleep-wake cycles, mnestic functions, learning processes, and a decrease in structural changes in the brain substance. The drug is characterized by a pronounced antitoxic effect during withdrawal syndrome. Eliminates the neurological manifestations of acute alcohol intoxication, restores behavioral disorders, autonomic functions, and is also able to reduce cognitive impairment caused by long-term use of ethanol. Under the influence of ethylmethylhydroxypyridine succinate, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects.

Pharmacokinetics:

Absorption Rapidly absorbed when taken orally. The maximum concentration at doses of 400 - 500 mg is 3.5 - 4.0 mcg/ml.

Distribution Quickly distributed in organs and tissues. The average retention time of the drug in the body when taken orally is 4.9 - 5.2 hours.

Metabolism Metabolized in the liver by glucuron conjugation. 5 metabolites have been identified: 3-hydroxypyridine phosphate - formed in the liver and, with the participation of alkaline phosphatase, breaks down into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, is formed in large quantities and is found in the urine 1 - 2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th are glucurone conjugates.

Excretion The half-life of T1/2 when taken orally is 2.0 - 2.6 hours. It is quickly excreted in the urine, mainly in the form of metabolites and in small quantities unchanged. The most intensive elimination occurs during the first 4 hours after taking the drug. Urinary excretion rates of unchanged drug and metabolites have high individual variability.

Indications for use

The active substance has a fairly wide range of applications, depending on its trade name and release form.

So the tablet form ( Mexicor ) is most often prescribed for coronary heart disease, and injection solutions for other diseases.

The drugs Mexifin, Mexifor and Meksidant are used:

for the treatment of anxiety conditions ( neurotic and neurosis-like ), vegetative-vascular dystonia , discirculatory encephalopathy ;
mild degree of atherosclerosis ;
in case of acute intoxication with antipsychotic drugs;
as part of a complex treatment of acute cerebrovascular accidents;
during abstinence in alcoholics with vegetative-vascular and neurosis-like disorders .

Mexidol is administered intramuscularly for peritonitis , acute pancreatitis and other purulent-inflammatory diseases of the abdominal cavity.

Mexicor in the form of a solution is administered during the first day after myocardial infarction .

Mexidol tablet p/o film 125mg 50 pcs

Pharmacological group:

Antioxidant agent.
Pharmacodynamics:
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 the effects of various damaging factors (shock, hypoxia and ischemia, cerebrovascular accidents, intoxication with alcohol and antipsychotics (neuroleptics)).

The mechanism of action of Mexidol is due to its antioxidant, antihypoxic and membrane protective effects. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, 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 enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, neurotransmitter transport and improve synaptic transfers. Mexidol® increases the content of dopamine in the brain. 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 the energy-synthesizing functions of mitochondria, stabilization of cell membranes.

The drug improves metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, and reduces platelet aggregation. Stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis. It has a lipid-lowering 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, reduction of dystrophic and morphological changes in various structures of the brain.

Mexidol® 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 relieve cognitive impairment caused by long-term use of ethanol and its withdrawal. Under the influence of Mexidol, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects. Mexidol® improves the functional state of ischemic myocardium. In conditions of coronary insufficiency, it increases collateral blood supply to the ischemic myocardium, helps maintain the integrity of cardiomyocytes and maintain their functional activity. Effectively restores myocardial contractility in reversible cardiac dysfunction.

Pharmacokinetics:

Rapidly absorbed when taken orally. The maximum concentration at doses of 400-500 mg is 3.5-4.0 mcg/ml. Quickly distributed in organs and tissues. The average retention time of the drug in the body when taken orally is 4.9-5.2 hours. Metabolized in the liver by glucuron conjugation. 5 metabolites have been identified: 3-hydroxypyridine phosphate is formed in the liver and, with the participation of alkaline phosphatase, breaks down into phosphoric acid and 3-hydroxypyridine; 2nd metabolite - pharmacologically active, formed in large quantities and found in urine 1-2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates. T1/2 when taken orally - 2.0-2.6 hours. It is rapidly excreted in the urine, mainly in the form of metabolites and in small quantities unchanged. The most intensive elimination occurs during the first 4 hours after taking the drug. Rates of urinary excretion of unchanged drug and metabolites have individual variability.

Side effects

After long-term use of the medicine, the following adverse reactions may occur:

excessive gas formation;
nausea;
disturbances in sleep patterns, insomnia or drowsiness ;
dry mouth;
allergic rashes and other hypersensitivity reactions ;
diarrhea.

Also, with intravenous jet administration, if the rate of drug administration is too high, the following may occur:

metallic taste and dry mouth;
feeling of warmth throughout the body and limbs;
distortion of smell and taste;
a feeling of sore throat, heaviness in the chest, suffocation.

Ethylmethylhydroxypyridine succinate, instructions for use (Method and dosage)

Depending on the disease and its course, various forms of medication are used. facilities.

Instructions for the solution

The substance is administered intravenously or intramuscularly , in a stream or drip, using sodium chloride as a solvent.

The duration of the jet injection should be at least 5-7 minutes. The dropper speed is from 40 to 60 drops per minute.

The daily dosage is selected by the attending physician on an individual basis.

Typically the initial dosage is 50 to 300 mg per day, divided into 1-3 injections. Then the dose can be gradually increased.

The maximum daily dosage of the product is 0.8 grams.

For the treatment of discirculatory encephalopathy in the stage of decompensation, 0.1 g of the drug is prescribed intravenously, 2-3 times a day, for 2 weeks. Next, 0.1 g per day is administered intramuscularly for another 2 weeks.

As a prophylactic agent for dyscirculatory encephalopathy, 0.1 g of the drug is prescribed intramuscularly 2 times a day for 10-14 days.

In cerebral circulatory disorders

as an additional remedy, 0.2-0.3 g per day, drip for the first 4 days;
then switch to intramuscular injections of 0.3 g per day, in 3 injections over 10-14 days.

To treat acute pancreatic necrosis or peritonitis , the substance is administered to the patient before and after surgery. The dosage is selected individually.

Elderly patients with mild cognitive impairment or anxiety disorders are administered intramuscularly at 0.1-0.3 grams per day for 5-7 days.

To relieve acute intoxication with neuroleptics, intravenous injections are used for 10-14 days.

Instructions for Ethylmethylhydroxypyridine succinate tablets

As a rule, 125 mg is prescribed, 2-3 times a day. The course of treatment is at least two months. On the recommendation of the attending physician, the course can be repeated.

ETHYLMETHYLHYDROXYPYRIDINE AKRIKHIN tab. p/o captivity. 125 mg No. 50

Pharmacodynamics

Ethylmethylhydroxypyridine is an inhibitor of free radical processes, a membrane protector with antihypoxic stress-protective nootropic antiepileptic and anxiolytic effects.
Belongs to the class of 3-hydroxypyridines. The mechanism of action of ethylmethylhydroxypyridine is due to its antioxidant, antihypoxic and membrane protective effects. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, improves the structure and function of the cell membrane. The drug modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase adenylate cyclase acetylcholinesterase) receptor complexes (benzodiazepine gamma-aminobutyric acid (GABA) acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structural and functional organization of biomembranes of neurotransmitter transport and improvement of synaptic transmission.

Ethylmethylhydroxypyridine-Akrikhin increases the content of dopamine in the brain. 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 adenosine triphosphate (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, cerebrovascular accident, 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 and stimulates the activity of membrane enzymes - phosphodiesterase adenylate cyclase acetylcholinesterase. It supports the activation of aerobic glycolysis that develops during acute ischemia and promotes the restoration of mitochondrial redox processes under hypoxic conditions; it 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, accelerates the restoration of functional activity of the LV myocardium, reduces the incidence of arrhythmias and intracardiac conduction disorders. Normalizes metabolic processes in 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 metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membrane structures of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis. It has a lipid-lowering effect and reduces the content of total cholesterol and low-density lipoproteins.

The anti-stress effect is manifested in the normalization of post-stress behavior, somato-vegetative disorders, the restoration of sleep-wake cycles, impaired learning and memory processes, and the reduction of dystrophic and morphological changes in various structures of the brain.

Ethylmethylhydroxypyridine-Akrikhin 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 relieve cognitive impairment caused by long-term use of ethanol and its withdrawal.

Under the influence of the drug, the effect of tranquilizing neuroleptic antidepressant hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects.

Ethylmethylhydroxypyridine-Akrikhin improves the functional state of ischemic myocardium. In conditions of coronary insufficiency, it increases collateral blood supply to the ischemic myocardium, helps to preserve the integrity of cardiomyocytes and maintain their functional activity. Effectively restores myocardial contractility in reversible cardiac dysfunction.

Interaction

This substance enhances the effect of bromodihydrochlorophenylbenzodiazepine , carbamazepine , diazepam , levodopa .

When combining Ethylmethylhydroxypyridine succinate with ethyl alcohol , the toxic effect of alcohol is reduced.

The medicine is often prescribed in conjunction with Piracetam, Cavinton, Actovegin and other drugs. This makes it possible to enhance their effectiveness and reduce the incidence of side effects.

Ethylmethylhydroxypyridine succinate (Aethylmethylhydroxypyridini succinas)

Pharmacological action - antioxidant, membrane stabilizing, nootropic, cerebroprotective, adaptogenic, anxiolytic.

Inhibits lipid peroxidation, increases the activity of the antioxidant system, activates the energy-synthesizing functions of mitochondria, improves energy metabolism in the cell, and helps maintain the level of macroergs, including during stress hypoxia. Activates intracellular synthesis of protein and nucleic acids, enzymatic processes of the Krebs cycle, promotes glucose utilization, synthesis and intracellular accumulation of ATP. Restores the structure and function of membranes, has a modulating effect on membrane-bound enzymes, ion channels, neurotransmitter transport systems, receptor complexes, including GABA-benzodiazepine, acetylcholine, improves synaptic transmission and interconnection of brain structures.

Improves metabolism and blood supply to the brain, rheological properties of blood and microcirculation, functioning of the immune system, suppresses platelet aggregation. It has antihypoxic, cerebroprotective, anxiolytic, antistress, nootropic (improving memory, attention, mental performance), antihypnotic, antialcohol, anticonvulsant, antiparkinsonian and vegetotropic effects. Reduces the level of total cholesterol and LDL and causes regression of atherosclerotic changes in the arteries (hypolipidemic and antiatherogenic effects). It has anti-ischemic properties: improves blood flow, limits the area of ischemic damage and stimulates reparative processes. Increases the body's resistance to the effects of extreme factors and oxygen-dependent pathological conditions, such as shock, stress, sleep deprivation, hypoxia, cerebrovascular accidents, brain injuries, ischemia, electric shock, physical and mental overload, conflict situations, intoxication (ethanol, etc.) . Slows down the aging process. The anti-alcohol effect manifests itself in a sobering effect and weakening of motivation and is used to relieve withdrawal symptoms and treat acute poisoning. Concomitant use with alcohol does not aggravate intoxication, but prevents it. Reduces resistance to psychotropic drugs and enhances their effect, which makes it possible to reduce therapeutic doses and the likelihood of side effects. Radioprotective properties can be used for prophylactic purposes in case of increased radiation levels.

Experimental and clinical placebo-controlled studies have shown the high effectiveness of hydroxymethylethylpyridine succinate in the complex therapy of ischemic stroke (100-1000 mg per day intravenously), manifested by regression of disorders of consciousness and signs of vasomotor instability, and accelerated recovery of motor functions.

In children, the inclusion of the drug (10 mg/kg per day orally) in the treatment regimen for non-paroxysmal supraventricular tachycardia and sick sinus syndrome increased the effectiveness of treatment by an average of 20-27%.

Preparations containing (Ethylmethylhydroxypyridine succinate analogues)

Level 4 ATC code matches:
Trigamma

Riluzole

Huato Boluses

Vitagamma

Vitaxon

Hypoxene

Glycine

Mexiprim

Mexidol

Neurox

Glitsed

Cytoflavin

Trade names of Ethylmethylhydroxypyridine succinate: Metostabil, Mexidol, Cerecard, Mexifin, Mexidant, Mexicor, Mexibel, Medomexi, Solution for injection 3% Mexidol, Mexiprim, Neurox .

Reviews of Ethylmethylhydroxypyridine succinate

As a rule, reviews of drugs containing Ethylmethylhydroxypyridine succinate are good. Most often, medications are used to treat withdrawal symptoms, vegetative-vascular dystonia , after TBI and strokes . The remedy is prescribed even to children and newborns. Adverse reactions occur quite rarely, most often they are allergies , drowsiness, headache or nausea. A week after starting treatment, these symptoms disappear on their own.