Does Mexidol increase or decrease blood pressure, when should you take it?


Active ingredients in Mexidol

The main active ingredient of the drug is ethylhydropyridine succinate.

In addition to this component, there are additional elements:

  • sodium metabisilfit;
  • lactose monohydrate;
  • Carmellose;
  • talc;
  • titanium oxide.

The drug is available in the form of tablets of 10 pieces per package and in ampoules of 2 and 5 ml. The solution contains purified water. The amount of active substance per tablet is 125 mg, solution concentration is 5%.

The drug belongs to the category of nootropic drugs, the action of which is aimed at normalizing metabolism in cells.

Taking the drug can protect the body from the toxic effects of harmful substances, so it is often prescribed for the treatment of alcohol and drug addiction.

Indications for the use of Mexidol

Instructions for use classify Mexidol as a universal drug. This drug is currently used in neurology, surgery and psychiatry. It can quickly eliminate headaches and dizziness, improve well-being and stabilize high blood pressure. The drug is capable of providing a rapid therapeutic effect in the event of seizures provoked by external factors in the form of medication.

The manufacturer offers a choice of solution or tablets for treatment.

This function allows you to use the following options for entering the active substance into the body:

  • orally;
  • intramuscularly;
  • intravenously.

The drug allows you to treat the following diseases:

  • disruption of the normal circulatory process;
  • vegetative dystonia;
  • myocardial infarction;
  • purulent inflammatory processes occurring in the abdominal cavity;
  • atherosclerosis;
  • alcohol abuse withdrawal syndrome;
  • peritonitis;
  • pancreatitis in acute forms;
  • overdose of neutroleptics.

The above list is not complete, since Mexidol is now actively used in the treatment of a fairly wide range of diseases. The drug is used as an addition to the complex treatment of diseases resulting from insufficient blood supply and nutrition to the tissues of internal organs.

The active substance has a beneficial effect on brain function, improving memory and the ability to concentrate. The drug is prescribed for ischemia and frequent surges in blood pressure. In the prevention and treatment of arterial hypertension, the drug is used only as a complex remedy in addition to conservative treatment.

The effect of Mexidol on blood pressure

The drug is often prescribed to normalize blood pressure. It is often used for hypotension and hypertension.

The positive effect on low and high blood pressure is due to the following effects:

  • changes the composition of the blood and improves its blood flow, which helps accelerate blood circulation;
  • has a strong antioxidant and anxiolytic effect;
  • reduces the level of intoxication;
  • cell membranes have a positive effect, functional performance is restored;
  • Oxidative processes slow down;
  • Reduces the content of “bad” cholesterol;
  • Helps with neuroses.

Taking the drug improves the activity of neurotransmitters, which are responsible in the body for the quality of transmission of nerve impulses to brain cells. As a result of taking the drug, a person with hypertension experiences a general improvement in well-being, which is ensured by the resumption of metabolic processes and improved nutrition of internal organs. Stress is a common cause of high blood pressure. The effect of the drug reduces anxiety and relieves emotional discomfort, thereby normalizing blood pressure.

The ability to improve sleep quality and reduce psychomotor agitation also has a beneficial effect on blood pressure.

The properties of Mexidol make it possible to influence the mechanisms of formation of various types of diseases, leading to their inhibition and initiating the resumption of the body's defense reactions at the biochemical level. At the same time, the drug has a minimal number of side effects compared to drug analogues.

Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) is a domestic original antioxidant and antihypoxant, created at the Research Institute of Pharmacology of the Russian Academy of Medical Sciences in the mid-80s.

Mexidol consists of two related and functionally significant compounds: 2-ethyl-6-methyl-3-hydroxypyridine and succinic acid. The presence of 3-hydroxypyridine in the structure of Mexidol provides a complex of its antioxidant and membranotropic effects, the ability to reduce glutamate excitotoxicity, and modulate the functioning of receptors, which fundamentally distinguishes Mexidol from other drugs containing succinic acid. The presence of succinate in the structure of Mexidol distinguishes it from emoxipine and other 3-hydroxypyridine derivatives, since succinate is functionally significant for many processes occurring in the body and, in particular, is a substrate for increasing energy metabolism in the cell.

The combination of two compounds with the necessary properties in the structure of Mexidol ensures its good permeability through the blood-brain barrier (BBB), high bioavailability and action on various targets, resulting in a wide range of effects of the drug and high therapeutic potential.

Mexidol is a drug with a multicomponent, multi-target mechanism of action. In this case, its main mechanisms are: antioxidant and membranotropic effects, the ability to reduce glutamate excitotoxicity, modulate the functioning of receptors and membrane-bound enzymes, restore neurotransmitter balance, and increase the energy status of the cell [13, 15, 18, 22, 27, 38]. Through these mechanisms, influencing a set of chemical and physical processes and ensuring the necessary coupling of its main elements (receptors, ion channels, enzymes, etc.), Mexidol is able to influence the functioning of cellular structures associated with the transmission of information and the development of various pathological conditions. An important component of the mechanism of action of Mexidol is also its ability to influence free radical processes, which are one of the basic processes involved in the modifying/damaging effect on the cellular structures of the central nervous system and other organs and tissues.

Among the known antioxidants, Mexidol occupies a special position, since it affects various parts of free radical processes in biomembranes and inside the cell and does not have a pro-oxidant effect, which under certain conditions is characteristic of many other antioxidants [38].

On the one hand, Mexidol inhibits the processes of lipid peroxidation (LPO) and actively reacts with primary and hydroxyl radicals of peptides; reduces the level of NO in the brain increased in pathology, and on the other hand, increases the activity of antioxidant enzymes, in particular superoxide dismutase (SOD) and glutathione peroxidase, responsible for the formation and consumption of lipid peroxides, as well as reactive oxygen species [7, 13, 15, 22, 24 , 25, 30, 35, 36, 42, 46].

In its antioxidant activity, Mexidol is superior to emoxipin and proxipin [30, 36].

Foreign enzymatic antioxidants created on the basis of SOD isolated from natural material (ontosein, oxodrol, peroxinorm) have significant disadvantages: they are unstable, quickly inactivated and have many side effects. Mexidol, which causes activation of endogenous SOD, is free of these disadvantages and, thus, has significant advantages over enzymatic antioxidants of natural origin.

Thus, Mexidol is a universal means of antioxidant pharmacotherapy, since it affects various parts of oxidative stress: it inhibits free radical oxidation of lipids in biomembranes, actively reacts with lipid peroxide radicals, primary and hydroxyl radicals of peptides, reduces the level of NO, increases the activity of SOD and other antioxidant enzymes.

Due to its mechanism of action, Mexidol has a wide range of pharmacological effects, realized at least at two levels - neuronal and vascular. It has neuroprotective, antihypoxic, antiischemic, nootropic, vegetotropic, antistress, anxiolytic, anticonvulsant and other effects. Under the influence of Mexidol, an improvement in cerebral circulation and microcirculation is observed.

The therapeutic effect of Mexidol is dose-dependent. As the dose is increased to a certain level, an increase in effect is usually observed. The range of therapeutic doses of Mexidol is quite wide and in experiments ranges from 10 to 300 mg/kg. With an increase in the dose of Mexidol, the latent period of onset decreases and the severity and duration of the effect increases.

Mexidol has the most pronounced effect in the treatment of vascular and neurodegenerative diseases, primarily acute and chronic cerebrovascular accidents, including strokes. It can be distinguished as one of the most effective drugs used in the treatment of these forms of pathology. Thanks to its mechanism of action, Mexidol influences the key basic links in the pathogenesis and other diseases associated with neurodegeneration processes, such as Alzheimer’s and Parkinson’s diseases, brain injuries, convulsions, stress, etc. [47].

Mexidol has a clear therapeutic effect in cerebral ischemia, which occurs when systemic hemodynamics is disrupted, with changes in blood vessels leading to metabolic reactions, when in the ischemic zone the concentration of LPO substrates and the generation of reactive oxygen species increase, pro-oxidants (LPO stimulants) accumulate, and activity decreases antioxidant enzymes. The drug enters ischemic cells, and under its influence, a decrease in the area of ​​brain damage during a stroke is observed (morphological studies), the percentage of animals surviving after a stroke sharply increases, the functional activity of the brain is restored, which is expressed in the improvement of cognitive functions, indicators of neurological deficit and psycho-emotional state [12 , 19, 33, 35, 41]. It is Mexidol's powerful antioxidant effect that makes it preferable to drugs containing succinic acid and not having antioxidant properties.

It was found [14, 33] that Mexidol has the ability to increase life expectancy and the number of surviving animals under various hypoxic conditions: hypobaric hypoxia, hypoxia with hypercapnia in a hermetic volume and hemic hypoxia. For example, in conditions of acute hypobaric hypoxia, when animals rise to a height of 11,000 meters, Mexidol after its injection increases their life expectancy by 2 times, and the number of surviving animals by 2.4 times. In terms of antihypoxic activity, Mexidol is significantly superior to pyritinol and piracetam, which have weak antihypoxic activity under conditions of acute hypobaric hypoxia and hypoxia with hypercapnia.

The mechanism of the antihypoxic action of Mexidol is also associated with its specific effect on energy metabolism, which is due to the succinate succinate included in its composition, which, under hypoxic conditions, entering the intracellular space, is capable of being oxidized by the respiratory chain. Succinic acid provides increased compensatory activation of aerobic glycolysis and decreased inhibition of oxidative processes in the Krebs cycle, which leads, under hypoxic conditions, to an increase in the content of ATP and creatine phosphate, activation of the energy-synthesizing functions of mitochondria, and stabilization of cell membranes. Mexidol is an antihypoxant with a direct energizing effect, the effect of which is associated with the influence on the endogenous respiration of mitochondria, activation of the energy-synthesizing function of mitochondria with the activation of compensatory metabolic flows that supply energy substrates to the respiratory chain, in this case succinate, and acting as an urgent adaptation mechanism during hypoxia [26, 27, 39].

It is known that with traumatic brain injury there is an intensification of lipid peroxidation processes both in the blood and in brain tissue, and there is a decrease in the oxidative and phosphorylating function of mitochondria. In this case, Mexidol, eliminating the excessive activity of free radical oxidation processes in the dynamics of the post-traumatic period, has a protective effect on bioenergetic processes in the brain during traumatic brain injury by changing the functional state of the mitochondrial respiratory chain [30].

It has been established that Mexidol has a pronounced and optimal antioxidant, hypolipidemic, hypoglycemic, hepatoprotective effect compared to Actovegin and Infezol in conditions of alloxan hyperglycemia, cholesterol dyslipidemia and alloxan-cholesterol dyslipidemia [36, 37]. It has a pronounced preventive effect on the dynamics of metabolic parameters in conditions of a combination of lipid and carbohydrate metabolism disorders in the experiment and is superior in this effect to emoxypine, dimephosphone and alpha-tocopherol, providing a hypoglycemic, hypolipidemic effect. Mexidol prevents disturbances in protein metabolism and the development of cytolytic syndrome, providing an antioxidant effect recorded in blood serum, and reducing the growth of markers of electrical instability of the myocardium, restoring the level of malondialdehyde and catalase activity to intact values ​​in the myocardium, liver and kidneys of experimental animals [36].

The most important link in the mechanism leading to cell death is the occurrence of glutamate excitotoxicity, which is observed in various forms of neurodegeneration and is characterized by increased release of glutamate from neuron terminals into the intercellular space. In particular, during a stroke, this release occurs in the lesion and is then observed to diffuse into the ischemic penumbra zone. Glutamate excitotoxicity leads to cell death, which is called “death by overexcitation.” Excessive accumulation of glutamate activates the ionotropic NMDA and AMPA subtypes of glutamate receptors, causing a massive influx and shock increase in Ca2+ ions in the postsynaptic neuron cell. Calcium in the cell triggers activation of the mitochondrial respiratory chain with increased leakage of superoxide anion radical and hydroxyl radical; activation of NADPH2 oxidase, resulting in an increase in the content of superoxide anion radical; activation of NO synthase (NOS) occurs, which leads to the accumulation of NO; activation of heme oxygenase, which converts Fe3+ to Fe2+. All of the above processes intensify LPO, and in response, the cell’s AOS defense system is activated. With prolonged hypoxia, its depletion is observed, which leads to the development of oxidative stress and death of nerve cells through apoptosis or necrosis, depending on the degree of their damage [4, 20]. in vitro studies

on transverse experiencing sections of the hippocampus, it was established that Mexidol at a concentration of 4 mM suppresses orthodromic population responses in the CA1 field, and the non-competitive antagonist of the glutamate NMDA receptor MK-801 weakens the inhibitory effect of Mexidol, while a specific blocker of glutamate AMPA receptors does not affect the effects of Mexidol [28].

Using the methods of microiontophoresis and pneumomicroinjection when Mexidol is applied to individual neurons, it was found that it has a direct effect on the majority of neurons in the sensorimotor cortex of the brain of awake animals, causing both inhibitory and excitatory reactions [28]. Mexidol has a pronounced ability to improve learning and memory processes, has a clear anti-amnestic effect, eliminating memory impairment caused by various influences [9, 13, 22, 46, 47]. The experiment showed that Mexidol effectively eliminates amnesia of the conditioned passive avoidance reflex in rats caused by such harsh influences as administering a maximum electric shock immediately after training, administering the anticholinergic scopolamine or after deprivation of the paradoxical sleep phase. In terms of anti-amnestic action, Mexidol is not inferior, and in some cases superior in activity and depth of effect, to such nootropic drugs as piracetam, pyritinol, meclofenoxate, cleregil, pantogam, picamilon, sodium hydroxybutyrate [8, 22, 46].

Along with the anti-amnestic effect, Mexidol promotes the preservation of a memory trace and counteracts the process of extinction of acquired/acquired skills and reflexes.

Mexidol has a positive restorative effect on impaired cognitive functions that occur during natural aging and in experimental models of Alzheimer's and Parkinson's diseases [8, 11, 25, 43, 45, 47]. Along with improving learning and memory processes in old animals, under the influence of Mexidol, some manifestations of neurological deficits are eliminated, emotional status is restored, and the level of cholesterol, low-density lipoproteins, triglycerides, and lipofuscin is reduced to normal. The mechanism of Mexidol's positive effect on cognitive functions is also associated with its membrane-protective and antioxidant effects. According to the synapse-membrane organization of memory, the decisive role in consolidating information in the central nervous system belongs to conformational shifts of protein macromolecules in the synapse area. Mexidol, having a pronounced effect on the physicochemical properties of the membrane and causing its structural and functional rearrangements, increases the functional activity of the biological membrane and, thus, promotes the formation of stable conformational changes in protein macromolecules of synaptic membranes, the formation of interconnected systems of membrane complexes of neurons, resulting in activation synaptic processes and improvement of cognitive functions. Also important is the ability of Mexidol to change the phospholipid composition of the outer membrane of brain synaptosomes; For memory processes, it seems especially important to increase the content of phosphatidylserine, which affects the activity of potassium and calcium ATPase and phosphotidylinositol, which increases the affinity of the acetylcholine receptor for acetylcholine. In addition, Mexidol has been shown to prevent the development of atheroarteriosclerosis [21].

Mexidol also has a pronounced anxiolytic effect, i.e. the ability to eliminate fear, anxiety, tension, restlessness. In an experiment using the conflict situation technique in rats, it was shown that Mexidol has pronounced anxiolytic activity, increasing the number of punishable water intakes. It has similar activity to diazepam, however, unlike diazepam, after Mexidol the adequacy of the response to provoking test stimuli on the Brodie-Nauth scale is not impaired and no side effects in the form of sedation and muscle relaxation are observed. Mexidol has an effect on various types of stressful situations, for example, stress due to the novelty of the situation, anxiety and fear caused by negative influences previously received in these conditions, stress in anticipation of pain, and in situations of mismatch between what is desired and what is actually done [6, 16]. Analysis of the mechanism of implementation of the anxiolytic effect of Mexidol showed that Mexidol does not have the ability to bind to benzodiazepine and GABA receptors, however, it has the ability to enhance the binding of labeled diazepam to benzodiazepine receptors. Thus, without having direct affinity for benzodiazepine and GABA receptors, Mexidol has a modifying effect on them, enhancing their ability to bind [32, 44].

In the light of modern ideas about substances of a new type that are not related to direct receptor agonists, the effect of Mexidol can be represented as the effect of a modulator, allosterically potentiating the ligand receptor, and an activator of ion channels through the mechanism of membrane-receptor interaction.

The anti-stress, anxiolytic effect is complemented by Mexidol’s unique ability to increase the body’s resistance to various extreme factors, such as stress, conflict situations, electric shock, physical activity, hypoxia, sleep deprivation, and various intoxications [17, 40]. Along with this, Mexidol eliminates disorders that arise from alcoholism and drug addiction [11][], [].

Mexidol has a wide range of anticonvulsant effects [2, 10, 29, 34]. In animal experiments, Mexidol weakens convulsions caused by various influences: corazol, maximum electric shock, strychnine, thiosemicarbazide, bicuculline, picrotoxin, 5-hydroxytryptophan. Mexidol reduces the duration and number of discharges of primary and secondary generalized tonic-clonic seizures in a model of cobalt epilepsy. The mechanism of the anticonvulsant action of Mexidol is determined by its influence on the processes of free radical metabolism, cellular hypoxia and increased action of GABA.

One of the important properties of Mexidol is its ability to improve and potentiate the specific effect of known drugs [7]. It has been shown that when combining Mexidol and phenazepam in doses of a low therapeutic level, an anxiolytic effect of the same severity is achieved as when the dose of phenazepam is increased by 10 times. The potentiating effect of Mexidol was also revealed by its anticonvulsant effect when combined with phenytoin, phenobarbital, valproate and carbamazepine. It has been shown that, by enhancing the main therapeutic effect of drugs, Mexidol reduces their side effects. The combined use of Mexidol with anticonvulsants in the epilepsy clinic made it possible to significantly reduce the doses of basic anticonvulsants and reduce their side effects [1, 3, 34]. The combined use of Mexidol with antihypertensive drugs, in particular with bisogamma, promotes more effective correction of blood pressure and a reduction in the dose of beta-blocker in young patients [5].

Due to the combination of a pyridine base and succinic acid in its structure, Mexidol has a high ability to pass the BBB and bioavailability. It has been established that when administered enterally and parenterally, Mexidol is quickly absorbed and quickly eliminated from the body [23, 31]. A targeted study of the pharmacokinetics of Mexidol was carried out on patients with neurotic disorders undergoing treatment in a hospital (Mexidol was prescribed intramuscularly at 200-250 mg 2 times a day) [23, 31]. Analysis of the parameters of Mexidol, both with a single and course use, showed that its concentration in the blood increases quite quickly, reaching a maximum after an average of 0.58 hours.

At the same time, Mexidol is quickly eliminated from the blood and after 4 hours it is practically not registered, therefore, to maintain a therapeutic concentration, at least 2-fold administration is necessary during the day. The pharmacokinetic profile of the drug with both single and long-term administration does not differ significantly. A study of Mexidol excretion in urine showed that it is excreted both unchanged and in the form of a glucuronoconjugate, which constitutes a significant amount. A correlation analysis of the relationship between the psychopharmacological effect and the kinetic characteristics of Mexidol showed that with an increase in the maximum concentration of Mexidol, the anxiolytic effect of the drug increases [23, 31].

A significant advantage of Mexidol is that it is a low-toxic drug with a large therapeutic breadth, has virtually no side effects of traditional neuropsychotropic drugs, in particular, does not have a sedative, muscle relaxant, stimulating, euphoric effect, and also does not have the side effects characteristic of neuroprotective drugs.

Thus, the high clinical effectiveness of Mexidol in the treatment of vascular and neurodegenerative diseases is determined by its complex mechanism, primarily antioxidant (inhibition of both enzymatic and non-enzymatic lipid peroxidation processes, decreased NO levels, increased activity of antioxidant enzymes) and membrane protective (decreased viscosity and increased membrane fluidity , change in phospholipid composition) effect, as well as its ability to weaken glutamate excitotoxicity and, most importantly, restore the energy balance of the cell.

The mechanism of action of Mexidol described above explains the minor side effects of the drug, as well as its ability to potentiate the effect of other substances important for the functioning of the central nervous system.

The data presented have allowed Mexidol to occupy an important place in clinical and outpatient practice in the treatment of various diseases, including neurological and mental.

[] 1Smirnov L.D., Voronina T.A., Dyumaev K.M., Rudenko G.M., Morozov G.V. Patent “Anti-alcohol agent”, No. 1777878. 1984.

[] 2Smirnov L.D., Voronina T.A. Patent “Medicine for the treatment of drug addiction”, No. 2159615. 1999.

Mexidol increases or decreases blood pressure

Mexidol indirectly affects blood pressure. The result of using the drug depends on the characteristics of the disease and the patient’s body. Mexidol belongs to a group of drugs that have a complex effect on the body, improving the functioning of all internal organs. It is thanks to this action that normalization of pressure occurs.

The drug is effective with minor deviations from the norm, and the effect can be both downward and upward.

Therefore, treatment with Mexidol begins with small doses, adjusting the amount of the drug depending on the effect obtained.

With an increased level of pressure, negative processes occur in the patient’s body, resulting in significant oxygen starvation. The hypoxic state causes a sharp deterioration in health and malaise. With high blood pressure, Mexidol improves blood flow, which helps stabilize the situation.

In case of arterial hypotension, Mexidol should be taken with caution, as the drug can lower blood pressure. For problems with blood pressure, drug therapy can provide significant improvement, but the length and duration of medication should be determined by the attending physician. It is worth remembering that the drug for low or high blood pressure should complement traditional treatment, and not be a complete replacement for antihypertensive drugs.

pharmachologic effect

Antioxidant agent. Means for the correction of disorders in alcoholism, toxic and drug addiction.

Pharmacokinetics

With intramuscular administration, it is determined in the blood plasma for 4 hours after administration. The time to reach the maximum concentration Tmax is 0.45-0.5 hours. Cmax when administering a dose of 400-500 mg is 3.5-4.0 μg/ml. Mexidol quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. The drug retention time (MRT) is 0.7-1.3 hours. The drug is excreted mainly in the urine, mainly in glucurone-conjugated form and in small quantities unchanged.

Pharmacodynamics

It has antihypoxic, membrane-protective, nootropic, anticonvulsant, anxiolytic effects, and increases the body's resistance to stress.
The drug increases the body's resistance to the effects of major damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular accident, intoxication with alcohol and antipsychotic drugs (neuroleptics)). Mexidol improves cerebral 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 hypolipidemic effect, reduces the level of total cholesterol and LDL. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis. The mechanism of action of Mexidol is due to its antihypoxic, antioxidant and membrane protective effects. It inhibits the processes of lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, reduces membrane viscosity, and increases its fluidity. 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, transport of neurotransmitters and improve synaptic transmission.

Mexidol increases dopamine levels in the brain. Causes an increase in the compensatory activity 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, creatine phosphate and activation of the energy-synthesizing functions of mitochondria, stabilization of cell membranes. Mexidol normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Increases the antianginal activity of nitro drugs. Mexidol promotes the preservation of retinal ganglion cells and optic nerve fibers during progressive neuropathy, the causes of which are chronic ischemia and hypoxia. Improves the functional activity of the retina and optic nerve, increasing visual acuity.

"Mexidol" in the treatment of hypertension

Simply take 1 or 2 tablets orally, monitoring the result in the form of obtaining the desired pressure readings. The therapeutic effect occurs on average within 10 minutes. The maximum daily dose should not exceed 6 tablets, which is 800 mg. Frequency of use: 2 or 3 times a day. Taking the drug in tablet form should be combined with meals.

The substance is retained in the body for 5 hours; it is metabolized in liver cells and excreted by the kidneys.

Mexidol is administered intravenously by drip, at a rate of 40 to 60 drops per minute. The total duration of the procedure is 5-7 minutes. The content of the drug in plasma is measured after 4 hours, excretion occurs by the kidneys.

For injection, the drug is used in capsules with a 5% solution of the active substance in a volume of 2 ml. By injection, the drug is administered slowly, while the liquid from the ampoule is first diluted with saline solution. The course of therapy includes a course of the drug per day of no more than 1200 mg.

The advantage of Mexidol is the possibility of using it with other drugs that have a psychotropic effect.

Taking it together with sedatives and painkillers will enhance their effect. The dosage and duration of therapy is determined by the attending physician depending on the stage of the disease.

Mexidol tachycardia

  • film-coated tablets 125 mg No. 30
    Mexidol - 2-ethyl-6-methyl-3-hydroxypyridine succinate was synthesized at the Institute of Biochemical Physics of the Russian Academy of Sciences; studied and developed at the Research Institute of Pharmacology of the Russian Academy of Medical Sciences and the All-Russian Scientific Center for the safety of biologically active substances.

    Mexidol is approved for wide medical use and is indicated for the treatment of acute cerebrovascular accidents, dyscirculatory encephalopathy, vegetative-vascular dystonia, atherosclerotic disorders of brain function, neurotic and neurosis-like disorders with anxiety, for the relief of withdrawal syndrome in alcoholism, for the treatment of acute intoxication with neuroleptics and a number of other diseases . Mexidol is a new type of drug, both in mechanism and in the spectrum of pharmacological action and has significant advantages over known neuropsychotropic drugs.

    MECHANISM OF ACTION

    Mexidol has an original mechanism of action, the fundamental difference of which from the mechanism of action of traditional neuropsychotropic drugs is its lack of specific binding to known receptors. Mexidol is an inhibitor of free radical processes, lipid peroxidation, it activates superoxide dismutase, affects the physicochemical properties of the membrane, increases the content of polar lipid fractions (phosphotidylserine and phosphotidylinositol, etc.) in the membrane, reduces the cholesterol/phospholipid ratio, reduces the viscosity of lipid layer and increases the fluidity of the membrane, activates the energy-synthesizing functions of mitochondria and improves energy metabolism in the cell and, thus, protects the cell apparatus and the structure of their membranes.

    The change in the functional activity of the biological membrane caused by Mexidol leads to conformational changes in the protein macromolecules of synaptic membranes, as a result of which Mexidol has a modulating effect on the activity of membrane-bound enzymes, ion channels and receptor complexes, in particular, benzodiazepine, GABA, acetylcholine, enhancing their ability to bind to ligands, increasing the activity of neurotransmitters and the activation of synaptic processes.

    Along with this, Mexidol has a pronounced lipid-lowering effect, reduces the level of total cholesterol and low-density lipoproteins and increases high-density lipoproteins.

    Thus, the mechanism of action of Mexidol is determined primarily by its antioxidant properties, the ability to stabilize cell biomembranes, activate the energy-synthesizing functions of mitochondria, modulate the functioning of receptor complexes and the passage of ionic currents, enhance the binding of endogenous substances, improve synaptic transmission and the interconnection of brain structures. Thanks to this mechanism of action, Mexidol influences the key basic links in the pathogenesis of various diseases, has a wide range of effects, extremely few side effects and low toxicity, and has the ability to potentiate the action of other centrally active substances, especially those that act as direct receptor agonists.

    PHARMACODYNAMICS

    Mexidol, unlike well-known drugs, has a wide range of pharmacological effects, realized at least at two levels - neuronal and vascular.

    It has cerebroprotective, anti-alcohol, nootropic, antihypoxic, tranquilizing, anticonvulsant, antiparkinsonian, anti-stress, vegetotropic effects. In addition, it has the ability to improve cerebral circulation, inhibit platelet aggregation, reduce total cholesterol levels, and have an anti-atherosclerotic effect. The therapeutic effects of Mexidol are detected in the dose range from 10 to 300 mg/kg.

    Mexidol increases the body's resistance to various extreme damaging factors, such as sleep disturbance, conflict situations, stress, brain injury, electric shock, physical activity, hypoxia, ischemia, and various intoxications, including ethanol.

    Mexidol has a pronounced tranquilizing and anti-stress effect, the ability to eliminate anxiety, fear, tension, restlessness, in particular in conflict situations. When administered parenterally, it has a similar depth of effect to diazepam (Seduxen) and alprazolam (Xanax). Anti-stress effect

    Mexidol is expressed in the normalization of post-aggressive behavior, somatovegetative indicators, restoration of sleep-wake cycles and impaired learning and memory processes, reduction of stomach ulcers, reduction of dystrophic, morphological changes that occur after stress in various structures of the brain and in the myocardium.

    Mexidol has a distinct anticonvulsant effect, influencing both primary generalized seizures, caused primarily by the administration of GABAergic substances, and the epileptiform activity of the brain with a chronic epileptogenic focus.

    The nootropic properties of Mexidol are expressed in the ability to improve learning and memory, promote the preservation of a memorable trace and counteract the process of extinction of acquired skills and reflexes. Mexidol has a pronounced anti-amnestic effect, eliminating memory impairment caused by various influences (electric shock, brain injury, sleep deprivation, administration of scopolamine, ethanol, benzodiazepines, etc.).

    Mexidol has a clear antihypoxic and antiischemic effect, which is expressed in the ability of the drug to increase life expectancy and the number of surviving animals under various hypoxic conditions: hypobaric hypoxia, hypoxia with hypercapnia in a hermetic volume and hemic hypoxia. In terms of antihypoxic activity, Mexidol is significantly superior to pyritinol and piracetam, which at doses of 300 and even 500 mg/kg have weak antihypoxic activity under conditions of acute hypobaric hypoxia and hypoxia with hypercapnia. In addition, Mexidol has a pronounced antihypoxic effect on the myocardium in experiments on an isolated, perforated, contracting heart. According to the mechanism for the implementation of these effects, Mexidol is an antihypoxant with a direct energizing effect, the effect of which is associated with the influence on the endogenous respiration of mitochondria, with the activation of the energy-synthesizing function of mitochondria. The antihypoxic effect of Mexidol is due not only to its own antioxidant properties, but also to its constituent succinate, which, under hypoxic conditions, entering the intracellular space, can be oxidized by the respiratory chain.

    Mexidol has a pronounced anti-alcohol effect. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication caused by a single injection of high doses of ethanol, and also restores behavioral disorders of the vegetative and emotional status, deterioration of cognitive functions, learning and memory processes caused by long-term (5 months) administration of ethanol and its withdrawal, and prevents accumulation of lipofuscin in the brain of alcoholized animals.

    Mexidol has a pronounced geroprotective effect, has a clear corrective effect on learning and memory processes impaired during aging, improving the process of fixation, storage and reproduction of information, helps restore emotional and vegetative status, reduces manifestations of neurological deficits, reduces the level of aging markers - lipofuscin - in the brain and blood , malonaldehyde, cholesterol. The mechanism of the geroprotective action of Mexidol is associated with its antioxidant properties, the ability to inhibit lipid peroxidation processes, its direct membranotropic effect, the ability to restore ultrastructural changes in the granular endoplasmic reticulum and mitochondria, and modulate the functioning of receptor complexes. Mexidol has an antiatherogenic effect. The drug inhibits the humoral manifestations of atheroarteriosclerosis: reduces hyperlipidemia, prevents the activation of lipid peroxidation, increases the activity of the antioxidant system, prevents the development of pathological changes in the vascular wall and reduces the degree of damage to the aorta.

    Mexidol reduces the content of atherogenic lipoproteins and triglycerides, increases the level of high-density lipoproteins in the blood serum, and prevents deficiency of highly unsaturated phospholipids.

    Mexidol not only causes regression of atherosclerotic changes in the main arteries and restores lipid homeostasis, but also corrects disturbances in the regulatory and microcirculatory systems, which is expressed in the fact that there is no structure of arterioles and precapillaries, and their diameter differs little from the control, only focal ones are determined in venules aggregates, and complete elimination of spasm of afferent microvessels is observed.

    In addition, 2-ethyl-6-methyl-3-hydroxypyridine derivatives, which include Mexidol, suppress platelet aggregation caused by collagen, thrombin, ADP and arachidonic acid, inhibit platelet cyclic nucleotide phosphodiesterase, and also protect blood cells during mechanical injury . In particular, stabilizing resistance of erythrocyte membranes to hemolysis is observed and the process of hematopoiesis (restoration of the number of erythrocytes) after acute blood loss or chemical hemolysis is accelerated.

    The hepatoprotective effect of Mexidol was established in three models of acute toxic liver damage, in which hepatocyte cytolysis syndrome was caused by various hepatotoxins.

    In conditions of liver damage caused by carbon tetrachloride, Mexidol reduces areas of liver tissue necrosis and the volume of fatty degeneration of hepatocytes, normalizes the energy balance of hepatocytes, and has a protective effect on the nuclear and cytoplasmic pool of nucleic acids. In case of alcoholic liver damage, the effect of Mexidol is expressed in a decrease in the number of hepatocytes with lysis of nuclei and chromatin, acceleration of restoration of the total genome of hepatocytes and an increase in the content of nucleic acids in the liver tissue and nuclei of hepatocytes. 3-hydroxypyridine derivatives have a protective effect against the toxic effect on the liver of the strong hepatotropic carcinogen diethylnitrosoamine (DENA), since they form complexes with cytochrome P-450 and thereby prevent its complex formation with DENA.

    Mexidol has a pronounced ability to have a potentiating effect on the effects of other neuropsychotropic drugs. 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. In particular, when Mexidol is combined with carbamazepine, the dose of the anticonvulsant can be reduced by 2 times without reducing its therapeutic effect. The combined use of Mexidol with carbamazepine allows for adequate pathogenetic therapy of partial epilepsy, reduces the side effects of carbamazepine with long-term use without reducing its therapeutic effectiveness, and thereby optimizes the treatment of patients with epilepsy.

    Side effects and toxicity

    A significant advantage of Mexidol is that it has minor side effects and low toxicity. When studying the side effects of Mexidol, it was found that even in the upper range of therapeutic doses it has neither a depressing nor a stimulating effect on spontaneous motor activity, does not change the coordination of movements, the exploratory behavior of animals, rectal temperature, corneal and pineal reflexes, and does not cause drowsiness . The drug maintains the adequacy of the animals' response to the stimuli provoking the test, and simple reflexes are not impaired. With an increase in the average therapeutic dose by 4-5.5 times, Mexidol does not have a muscle relaxant effect. Along with this, Mexidol, even in extremely high doses, does not impair memory and does not cause amnesia, but, on the contrary, has an anti-amnestic effect in case of memory impairment.

    Mexidol does not have a negative effect on the liver, but on the contrary, has a hepatoprotective effect. The drug does not change the heart rate, does not change blood pressure, ECG, hemodynamics and breathing rhythm, does not cause changes in the composition of the blood, skin color and mucous membranes, urination, bowel movements and salivation.

    Side effects

    Mexidol is expressed mainly in inhibition of motor activity and impaired coordination of movements and begins to appear in individual animals when doses are increased to 300 mg/kg and higher when administered intraperitoneally and in doses of 400 mg/kg and higher when Mexidol is administered orally.

    Long-term administration

    Mexidol (2-3 months) does not cause a decrease in its therapeutic effect or the appearance of additional undesirable manifestations. After stopping long-term administration of Mexidol, no withdrawal syndrome is observed.

    Acute toxicity

    Mexidol was determined by recording the death of animals 24 hours after administration of the drug.
    The lethal dose of Mexidol, causing the death of 50% of animals (LD50) is 820 (625 - 1025) mg/kg for rats and 475 (365 -617) mg/kg for mice, and when administered orally - more than 3000 mg/kg in rats and 2010 (1608 - 2513) mg/kg in mice. A study of the chronic toxicity
    of Mexidol with long-term oral and parenteral use in experimental animals did not reveal significant changes in the organs and tissues of the body.

    A comparison of effective therapeutic doses of Mexidol with doses that cause side effects (sedation, incoordination, LD50) or toxic, lethal doses (LD50) shows the significant therapeutic breadth of Mexidol. The therapeutic index calculated from the LD50/ED50 ratio is 6.2, and from the LD50/ED50 ratio is 16.4, which indicates the harmlessness and safety of the drug.

    PHARMACOKINETICS AND METABOLISM

    Mexidol has high bioavailability. When administered parenterally to rats, it is rapidly absorbed from the abdominal cavity with a half-absorption period of 0.94 hours and maximum concentrations in plasma are reached after 3 hours, and in the brain and liver of animals - after 2-3 hours. A study of the binding ability of the membranes of the endoplasmic reticulum of the liver and brain of rats with Mexidol showed that the substance is determined in significant quantities in the membranes for 72 hours, which indicates the membranotropic properties of Mexidol. After intravenous administration of Mexidol to rabbits, the substance is eliminated from the blood plasma bioexponentially and can be determined according to theoretical calculations in fairly high concentrations for 6-12 hours. The high lipophilicity of Mexidol, its ability to bind to blood plasma proteins and endoplasmic reticulum membranes suggest the formation of tissue and blood depots of Mexidol in the body of animals.

    An analysis of the pharmacokinetic parameters of Mexidol in patients in the clinic showed that, both with single and course use, the concentration of Mexidol in the blood increases quite quickly, reaching a maximum after an average of 0.58 hours. At the same time, Mexidol is quickly eliminated from the blood and after 4 hours it is practically not registered. The pharmacokinetic profiles of the drug did not differ significantly between single and chronic administration. A study of the excretion of Mexidol in the urine showed that it is excreted both unchanged and in the form of a glucuronoconjugate, which constitutes a significant amount. When studying the metabolism of Mexidol in rats, 5 metabolites were identified.

    Metabolite I is phosphate (at the hydroxy group) of 3-hydroxypyridine, the formation of which occurs in the liver. In the blood, under the influence of alkaline phosphatase, 3-hydroxypyridine phosphate is split into phosphoric acid and 3-hydroxypyridine.

    Metabolite II - 2-methyl-6-methyl-3-hydroxypyridine - is formed in large quantities and is found in the urine on the first and second days after Mexidol administration; this metabolite has a spectrum of pharmacological activity close to Mexidol.

    Metabolite III - 6-methyl-3-hydroxypyridine is contained and excreted in large quantities in the urine.

    Metabolite IV is a glucuronic conjugate with 2-ethyl-6-methyl-3-hydroxypyridine.

    Metabolite V is a glucuronic conjugate with 2-ethyl-6-methyl-3-hydroxypyridine phosphate.

    APPLICATION OF MEXIDOL IN NEUROLOGY AND PSYCHIATRY

    Mexidol is an effective means of anti-ischemic protection of the brain in cerebral strokes. The drug has a pronounced therapeutic effect in patients with acute cerebrovascular accidents, including patients with ischemic and hemorrhagic stroke located in the circulation zone of the internal carotid artery and its branches, as well as in the vertebrobasilar system. Mexidol, as a rule, is administered to patients in the first hours of admission to the clinic intravenously in a stream or intravenously drip and intramuscularly, in doses of 50 mg. up to 400 mg. once, from 50 mg. up to 900 mg. per day with a frequency of administration of 3. The duration of action of the drug is about 4 hours. During the same time, the drug is detected in the blood of patients. One of the most significant manifestations of the effect of Mexidol when included in the complex therapy of cerebral stroke is a significant decrease in the daily mortality of patients in the acute period of stroke, as well as a tendency to an overall decrease in mortality in this disease. In the acute period of cerebral stroke, the mortality rate of patients was -31.5% for those taking Mexidol, and -52.5% without it; The bed days also decreased significantly: 38.2±2.7 with Mexidol and 45.2±4.0 days without Mexidol (B.A. Spasennikov). When using Mexidol in the treatment of cerebral stroke, first of all, a more rapid regression of neurological symptoms, assessed on the Matthew scale, is observed. Thus, in patients who were in serious condition at the time of admission to the clinic, the Matthew index at the end of the acute period (21 days) was 51.5 ± 2.1, and after treatment with Mexidol it significantly increased to 59.7 ± 1.0. When treating patients with Mexidol, the dynamics of improvement in motor functions, revealed when using the ADL index, was also indicative. So, after 21 days this indicator was 76.6±3.1 in patients using Mexidol, and in the group of patients without using Mexidol it was 63.2±4.6 (the difference is significant at P

    Echopulsography of intracranial arteries and veins after intravenous administration of Mexidol showed that already 30 minutes after the injection and for 4-6 hours, there is an increase in the amplitude (on average by 25.5%) of pulse oscillations of the cerebral vessels and the outflow of blood into the cerebral veins is facilitated. Under the influence of Mexidol, an increase in linear and volumetric blood flow is observed in the extracranial sections of the main arteries of the head, which is recorded within 6 hours after administration of the drug.

    Registration of rheoencephalography after a course of treatment with Mexidol revealed normalization of waveforms in 67% of patients, and improvement in venous outflow in 38%. There is an increase in pulse blood supply in the external carotid artery system and in the vertebrobasilar system, with its initially low level, and normalization of the tone of small arteries and veins in both vascular systems. Mexidol causes normalization of the EEG of patients with DE, which is expressed in an increase in the total power of the spectrum due to the alpha and beta ranges without a significant change in the slow wave part of the spectrum. In patients receiving Mexidol, the increased content of hemoglobin and leukocytes decreases, blood viscosity decreases, cholesterol levels decrease, and the lecithin-cholesterol ratio increases.

    Thus, Mexidol has a pronounced therapeutic effect in patients with dyscirculatory encephalopathy of stages 1, 2 and 3. Under the influence of Mexidol, remission or regression of neurological syndromic deficit is observed. As a result of treatment with Mexidol, 64% of patients showed a marked improvement in their condition, 32% had a moderate improvement, 20% had a slight improvement, and 16% had no effect. A comparison of the clinical effectiveness of Mexidol and known drugs showed that the index of overall effectiveness in the treatment of DE was 2.05 for Mexidol. for Cavinton, Trental and Sermion -2.1, Arsdergin -1.8. Mexidol is effective in patients with vegetative-vascular dystopia with symptoms of autonomic crises of a sympatho-adrenal nature, in whom improvement occurred within 5-14 days after the start of treatment. The intensity and frequency of headaches decreased, vasoactive imbalance and excitability decreased, and sleep improved. In 13% of patients, vegetative crises completely stopped and did not reappear over the next 2-3 months. Mexidol has a positive effect in patients with mental pathology of late age, especially with atherosclerotic dementia, in whom Mexidol was administered intramuscularly (patients received 100 mg for the first 5 days, and 300 mg daily for the remaining days, course - 3 weeks). Mexidol had a positive effect on memory, especially on current events, improved concentration, learning instructions, caused a decrease in headaches and symptoms of anxiety and depression. The degree of dysarthria and tearfulness in patients decreased. In some patients, dizziness completely disappeared, a confident gait appeared, and asthenia decreased. In some patients with initial manifestations of the senile-atrophic process and in patients with atherosclerotic dementia, after treatment with Mexidol, there is an increase in activity and an improvement in mood in the head. Thus, the use of Mexidol improves intellectual-mnestic activity in patients with age-related organic weakening processes, mainly in patients with atherosclerotic dementia, helping to improve concentration, follow instructions, memory for the present, reduce headaches, dizziness, tearfulness, dysarthria, and increase activity .

    Mexidol has a pronounced positive effect in the treatment of chronic neuroleptic syndrome with symptoms of tardive dyskinesia and subacute neuroleptic syndrome. Before treatment with Mexidol, all patients received active therapy for neuroleptic syndrome with the drugs cyclodol, norparkin, midantan, tiapride, cerucal, tremblex, detoxification therapy with intravenous administration of nootropil, vitamins B and C, which was assessed as ineffective.

    Mexidol had a pronounced antiparkinsonian and vegetotropic effect in these patients who were difficult to treat. The effect of Mexidol began to manifest itself already from the 2-3rd day of therapy and consisted of a decrease in the severity of oral-lingual hyperkinesis, which completely disappeared by the 7-14th day of treatment, then, under the influence of the drug, a decrease in limb tremor, stiffness, hypokinesia and hypomimia was noted, it improved, became more confident, free gait of patients, which ceased to be shuffling and mincing. The phenomena of orthogatism and dizziness decreased and disappeared, there was a tendency to normalize blood pressure with drug-induced hypotension, and Mexidol had no effect on normal blood pressure, weakness, lethargy, and dizziness decreased. The antiparkinsonian effect of Mexidol persisted for another 3-5 days after its discontinuation. Mexidol also has the ability to overcome the body's resistance to the effects of psychotropic drugs. Mexidol for this pathology was used at a dose of 300-500 mg per day with a treatment duration of 2-4 weeks. The effect of Mexidol began to appear already on the 3rd day of administration. Patients noted an improvement in the appearance, color and turgor of the skin, appetite, a decrease in lethargy, weakness, dizziness, dry mouth, and they became less lethargic. Against the background of Mexidol, it was possible to increase the doses of antidepressants and antipsychotics by 1.5-2 times without the occurrence of side effects. In a number of cases, the administration of previously ineffective drugs against the background of Mexidol made it possible to overcome the body's resistance and caused a significant decrease in depressive disorders and improvement in condition. In neurotic and neurosis-like conditions, Mexidol has a distinct tranquilizing effect, combined with a vegeto-normalizing effect. The therapeutic effect of Mexidol was most fully manifested in patients with neuroses and organic damage to the central nervous system with asthenic and astheno-vegetative disorders. The drug was effective and well tolerated by elderly patients. In 6 patients with asthenic disorders, the reverse development of anxiety and emotional tension against the background of Mexidol was accompanied by a peculiar activation with an increase in the background mood, a reduction in asthenic symptoms themselves. The tranquilizing effect of Mexidol is comparable in power to the effect of uxepam. Mexidol has a positive effect on sleep, restoring its duration and depth. The effect of Mexidol appears after 3-7 days of therapy. According to its spectrum of action, Mexidol can be classified as a daytime tranquilizer, which is effective both in hospital and outpatient settings, as well as in the elderly.

    Mexidol has shown high effectiveness in the treatment of alcohol withdrawal syndrome with somato-neurological and mental symptoms. The dose of Mexidol was 100-400 mg per day intramuscularly with a course duration of 5-7 days (against the background of conventional detoxification agents). Mexidol is an effective remedy for the rapid relief of alcohol withdrawal syndrome with a wide range of effects, both on its psychopathological components and on vegetative-vascular manifestations.

    The effect of Mexidol is observed within 1-1.5 hours after administration of the drug, and a persistent improvement in the condition occurs after 2-3 days. Patients experience a feeling of enlightenment, clarity in the head, headaches disappear, the process of concentration and comprehension when reading literature improves, anxiety, unaccountable fear, internal tension decrease, relaxation and a comfortable state appear, nightmares disappear, hypnotic hallucinations disappear, dreams become alcohol-free topics, sleep disorders disappear. Patients note the appearance of vigor and activity. Along with this, under the influence of Mexidol, alcohol motivation was significantly suppressed. Side effects. Comparison with cerebroprotective and psychotropic drugs. Mexidol is well tolerated by patients and causes only isolated side effects, which quickly disappear on their own or when the drug is discontinued.

    Of the hundreds of patients treated with Mexidol, side effects occurred in exceptional cases. Two patients with discirculatory encephalopathy experienced nausea and dizziness a few minutes after the intramuscular injection of Mexidol, which went away on their own. Two patients with alcoholism experienced bitterness and dry mouth, dizziness, and weakness, which quickly disappeared when the drug was discontinued. In three patients with resistant depression combined with manifestations of chronic neuroleptic syndrome, after the first two or three injections a slight drowsiness appeared, which then disappeared on its own. One patient with neurosis, at the beginning of therapy, had a pinpoint rash on the skin of the forearms, not accompanied by itching and peeling, which self-reduced within three days with continued therapy. The insignificance of side effects makes Mexidol stand out among the known neuroprotective, nootropic and tranquilizing agents. The arsenal of drugs used in modern medicine that improve cerebral circulation and are used in injection form is quite limited and includes pentoxifylline (Trental), vinpocetine (Cavinton), nicergoline (Sermion), dihydroergotoxin (Redergan). Cinnarizine (stugeron), flunarizine, nimodipine are used in the form of tablets and capsules. A significant drawback of these known drugs, which in many cases limits their use, is the significant number and frequency of side effects. Pentoxifylline (trental) causes headache, dizziness, tachycardia, facial flushing, palpitations, angina pectoris, arterial hypotension, nervousness, drowsiness or insomnia, bleeding from the vessels of the skin and mucous membranes, urticaria, skin rashes, itching, nausea, vomiting, a feeling of heaviness in the epigastrium, increased fragility of nails, changes in body weight, swelling, and in case of an overdose of the drug, convulsions, loss of consciousness, and fever may occur. In this regard, contraindications to the use of trental are acute myocardial infarction, massive bleeding, cerebral hemorrhage, retinal hemorrhage, severe atherosclerotic damage to the blood vessels of the brain and heart, severe heart rhythm disturbances, pregnancy, lactation. Characteristic side effects of vinpocetine (Cavinton) are a decrease in blood pressure and tachycardia, and contraindications to the use of the drug are coronary heart disease and severe forms of arrhythmias. Nicergoline (sermion) causes arterial hypotension, dizziness, a feeling of heat and flushing, drowsiness and sleep disturbance. Side effects of dihydroergotoxin (redergin) are nausea, vomiting, a feeling of heaviness in the stomach, loss of appetite, blurred vision, hyperemia of the nasal mucosa, skin rash, orthostatic hypotension, and contraindications to the use of the drug are severe coronary heart disease, severe bradycardia and arterial hypotension .

    Thus, all drugs currently used to treat cerebrovascular accidents are associated with significant side effects. In conditions of oxygen and energy deficiency that occurs with cerebrovascular lesions of the brain, Mexidol, which has a normalizing effect on cerebral metabolism, on fine neurochemical regulation and has minimal side effects, is of particular value. Cerebroprotective therapy with Mexidol differs from traditional effects on homeostasis and hemodynamics in its safety of use, the possibility of long-term use, and the ability to influence various levels and types of neurological and mental disorders. In contrast to traditional drugs, Mexidol does not cause a decrease in blood pressure, hemodynamic or ECG disturbances, and does not affect the heart rate. The positive effects of Mexidol in comparison with well-known drugs are its therapeutic effect on vasomotor instability, reduction of autonomic dysfunction, reduction of tachycardia, hyperemia, sweating, etc. In addition, Mexidol has a restorative effect on the functions of the motor sphere, improving coordination of movements and reducing psychomotor agitation, improves sleep, eliminates nervousness. Thus, having a high therapeutic effect, Mexidol does not have the side effects characteristic of other neuroprotective drugs. In contrast to sodium hydroxybutyrate and seduxen, Mexidol does not change the rhythm and frequency of breathing, i.e. does not cause the cardiorespiratory depression inherent in these drugs.

    In contrast to noopropic drugs, when using Mexidol, there is no activating effect, sleep disturbances or increased convulsive readiness. In addition, Mexidol is significantly more effective than piracetam (nootropil). In comparison with benzodiazepine tranquilizers (seduxen, elenium, oxazepam, lorazepam, phenazepam, etc.), Mexidol does not have a muscle relaxant effect even in doses exceeding the average therapeutic anxiolytic dose by 4-5.5 times and does not cause such manifestations as impaired coordination movements, decreased muscle tone and muscle strength. Mexidol, in contrast to anxiolytics, does not have a sedative or amnesic effect, but, on the contrary, has a positive effect on memory, especially in conditions of impaired cognitive functions. With long-term administration of Mexidol and cessation of its use, there are no signs of withdrawal syndrome characteristic of benzodiazepine tranquilizers. Thus, Mexidol is a selective tranquilizer of “daytime” action, in which the anxiolytic and anti-stress effects are carried out without the layering of sedative, muscle relaxant and amnesic effects.

    Possessing a high therapeutic effect, Mexidol does not cause side effects characteristic of known neuroprotective, nootropic and tranquilizing drugs, which indicates its safety and significantly expands the possibilities of use.

    Directions for use and doses

    Mexidol is prescribed intravenously (stream or drip), intramuscularly and orally. When administered intravenously, the drug should be diluted with water for injection or in physiological sodium chloride solution. For infusion administration, physiological NaCl solution should be used. Mexidol is administered in a stream over 1.5-3.0 minutes, and dropwise at a rate of 80-120 drops per minute. The duration of treatment and the daily dose of the drug depend on the nosology of the disease and the severity of the patient’s condition. For the treatment of acute cerebrovascular accident, Mexidol is prescribed intravenously by drip of 400 mg (8 ml) in isotonic sodium chloride solution (100-150 ml) twice a day for the first 15 days in intensive care or a specialized neurological department (maximum daily dose 1600 mg) . Then 400 mg (8 ml) 1 time per day intravenously in physiological NaCl solution daily for 15 days.

    In the future, it is recommended to administer Mexidol intramuscularly at a dose of 200 mg (4 ml) once a day for 10-15 days. In subsequent complex drug therapy, it is advisable to include a tablet form of the drug, 0.25-0.5 g/day for 4-6 weeks. The daily dose is distributed into 2-3 doses during the day.

    For the treatment of dyscirculatory encephalopathy (both against the background of cerebral atherosclerosis and against the background of hypertension):

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