Mexidol tablets and injections: instructions for use

The medication is a drug that affects the central nervous system. Mexidol has a membrane-stabilizing, antihypoxic effect. The medicine increases the body's resistance to stress, improves memory, prevents and suppresses seizures, and reduces the amount of individual lipid fractions in tissues. Acts as a nootropic and antioxidant.

Release form and composition

The drug is available in several forms. Among them:

1. Pills
   The dosage and form of the drug are selected individually by the attending physician. Mexidol tablets are available in a dosage of 125 mg. Indicated for oral administration. They have a round shape, the color of the shell can vary from white to cream. Available in packs of 30 and 50 pieces.

   Active ingredient Mexidol: ethylmethylhydroxypyridine succinate 125 mg

   Excipients: lactose monohydrate, sodium carmellose, magnesium stearate, talc, titanium dioxide, polyvinyl alcohol, macrogol polyethylene glycol.

2. Injection
   The solution for injection is contained in ampoules of 2 and 5 ml. The package contains 5 pieces. The solution is odorless and colorless. A yellowish tint is allowed. The composition of Mexidol depends on the form of release.

   Mexidol 50 mg/2ml

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   Active ingredient Mexidol: ethylmethylhydroxypyridine succinate 50 mg/2 ml. Excipients: sodium metabisulfite.

   Mexidol 50 mg/5 ml

   Active ingredient Mexidol: ethylmethylhydroxypyridine succinate 50 mg/5 ml. Excipients: sodium metabisulfite.

3. Toothpaste
   Mexidol toothpaste is available in a 65 g tube. The color of the drug depends on the type of paste. It can be pink, transparent, light green, white. The entire line of Mexidol toothpaste has a mint flavor. Active ingredient of Mexidol: ethylmethylhydroxypyridine succinate 65 mg. Excipients: sorbitol, polyethylene glycol, titanium dioxide, silicon dioxide, demineralized water, xanthan gum, sodium lauryl sulfate.

History of creation

Mexidol is an original domestic drug that has proven its effectiveness and safety in numerous clinical studies and successful twenty-year use in real clinical practice [1, 2].
Mexidol interrupts the ischemic cascade, affecting its most important stages: energy synthesis disorder, glutamate excitotoxicity and oxidative stress. Thanks to the universal mechanism of action, the drug can be used for all nosologies accompanied by ischemia and hypoxia, but primarily for ischemia of the most energy-consuming organs and systems of the body - nervous and cardiovascular [1]. Mexidol was synthesized in the early 1980s. at the State Institution "Research Institute of Pharmacology" RAMS L.D. Smirnov and V.I. Kuzmin. Under the leadership of Academician of the Russian Academy of Medical Sciences A.V. Waldman conducted its preclinical studies, established its pharmacological action and safety (B.I. Lyubimov) and studied the pharmacokinetics of the drug (A.K. Sariev, V.P. Zherdev) [1]. Having successfully completed clinical trials (G.G. Neznamov, E.S. Teleshova, S.A. Syunyakov, A.I. Fedin, Z.A. Suslina), on December 31, 1996 Mexidol was registered in the Russian Federation [3]. Thus, 2021 marks 20 years of successful use of Mexidol in clinical practice. For the study of the properties and introduction of Mexidol into clinical practice to a group of scientists (K.M. Dyumaev, E.B. Burlakova, L.D. Smirnov, T.A. Voronina, T.L. Garibova, V.P. Zhestkov, L. N. Sernov, N.V. Vereshchagin, Z.A. Suslina, N.V. Mironov, V.I. Shmyrev, A.I. Fedin, B.A. Knyazev, E.A. Avakyan, E.Yu. Lopatukhin) in 2003 was awarded the Russian Government Prize in the field of science and technology “For the creation and introduction into medical practice of antioxidant drugs for the treatment and prevention of cerebrovascular diseases” [4].

Modern ideas about pharmacokinetics

The pharmacokinetics of Mexidol have been studied in detail in experimental studies. It was shown in Chinchilla rabbits that when administered intragastrically at a dose of 100 mg/kg, Mexidol is rapidly absorbed from the gastrointestinal tract. The maximum concentration of the drug is achieved on average 30 minutes after oral administration, the half-life is 2.3 hours, and the average retention time is 3.2 hours. 5 hours after oral administration, Mexidol is not detected in the blood plasma of experimental animals [5]. Similar results were obtained when studying the pharmacokinetics of Mexidol in Wistar rats with intragastric administration at a dose of 200 mg/kg: the time to reach Cmax is on average 1 hour, and 5 hours after administration the drug concentration is below the detection limit [6].

When Mexidol is administered intramuscularly at a dose of 400–500 mg, its Cmax in human blood plasma is reached on average after 0.58 hours and amounts to 3.5–4.0 mcg/ml. The average retention time of the drug is 0.7–1.3 hours, and already 4 hours after intramuscular administration, Mexidol is practically not recorded in the blood plasma of volunteers. Taking into account the rapid elimination of the drug (when administered both in injection and tablet dosage forms) from the body of humans and animals, in order to achieve an optimal therapeutic effect, it is necessary to prescribe the drug at least 3 times a day. An alternative to this approach is the creation of new retarded dosage forms of Mexidol, which ensure a stable concentration of the drug in the blood plasma for 24 hours.

Mexidol is quickly distributed into organs and tissues, incl. and into the brain, penetrating the blood-brain barrier. With intragastric administration of Mexidol to Wistar rats at a dose of 200 mg/kg body weight, the peak of its concentration in the homogenate of the cerebral cortex and medulla oblongata of rats is observed 1.0–1.5 hours after oral administration of the drug, and then gradually decreases by the 4th hour. The highest level of Mexidol in the homogenate of the cerebellum and thalamus of rats is recorded 30 minutes after oral administration of the drug, and subsequently its content gradually decreases. Moreover, its maximum concentration is determined in the homogenate of the cerebral cortex [6].

When studying the correlation between the concentration of Mexidol in homogenates of different parts of the rat brain and its content in the blood plasma, a significant directly proportional relationship was revealed [6]. It has also been shown that Mexidol is not a substrate of the protein transporter glycoprotein-P, which regulates the penetration of a number of drugs through the blood-brain barrier [7]. Taken together, these facts suggest that penetration of the drug into the brain through the blood-brain barrier is most likely simple diffusion.

It has also been shown that Mexidol is able to penetrate into mitochondria, where its antihypoxic effect is realized, with a maximum concentration 1.5 hours after oral administration of the drug [6]. When studying the metabolism of Mexidol in rats, 5 metabolites were identified. The first is 3-hydroxypyridine phosphate (found only in animal liver). The second, 2-methyl-6-methyl-3-hydroxypyridine, formed in large quantities, has a spectrum of psychotropic activity close to Mexidol. The third metabolite was identified as 6-methyl-3-hydroxypyridine. The fourth metabolite is a glucuronic conjugate with 2-ethyl-6-methyl-3-hydroxypyridine. The fifth metabolite is a glucuronic conjugate with 2-ethyl-6-methyl-3-hydroxypyridine phosphate [8].

Mexidol is excreted primarily by the kidneys in the form of a glucuronic conjugate. On average, 12 hours after oral administration of the drug in humans, 0.31 ± 0.03% of the unchanged drug and 49.6 ± 4.65% of its glucuronoconjugate are excreted in the urine. In this case, excretion is most intense during the first 4 hours [9].

Since Mexidol is metabolized in the liver and excreted mainly by the kidneys, acute renal and liver failure are contraindications to the use of this drug. Mexidol has been shown to be an inducer of cytochrome P450 isoform 3A4 [10] and an inhibitor of the drug transporter protein glycoprotein-P [7]. This information must be taken into account when predicting the development of drug-drug interactions involving Mexidol. For example, since this drug is a P-glycoprotein inhibitor, it is better to combine it with rivaroxaban (an oral anticoagulant, a factor Xa inhibitor) rather than with dabigatran ethoxylate (an oral anticoagulant, a direct inhibitor of coagulation factor II). Dabigatran ethoxylate is a substrate of glycoprotein-P, so its combination with Mexidol can lead to the accumulation of an anticoagulant in the body, and accordingly, increase the risk of bleeding.

Modern ideas about the pharmacodynamics of the drug

The Mexidol molecule consists of two components: 2-ethyl-6-methyl-3-hydroxypyridine and a succinic acid residue. When creating its molecule, the researchers assumed that the drug would have antioxidant (due to the presence of 2-ethyl-6-methyl-3-hydroxypyridine) and antihypoxic (due to the succinic acid residue) activity, which was later confirmed in numerous experimental studies [ 12].

The direct antioxidant activity of 2-ethyl-6-methyl-3-hydroxypyridine is due to the presence in its molecule of a mobile hydrogen atom bound to oxygen, i.e. According to its mechanism of action, it is a proton donor. 2-ethyl-6-methyl-3-hydroxypyridine interacts with peroxy- (ROO•) and alkoxy-radicals (RO•) formed during lipid peroxidation processes according to the following mechanism [11]: AH + X*→A* + XH , where AN is Mexidol with a mobile hydrogen atom, X* is a radical initiator or intermediate radical product of free radical oxidation.

The antihypoxic activity of succinate (a succinic acid residue) is associated with the maintenance of the activity of the succinate oxidase unit under hypoxic conditions. This is a FAD-dependent link of the Krebs cycle, which under hypoxic conditions is inhibited later than NAD-dependent oxidases, which makes it possible to maintain energy production in the cell for a certain time, provided that the oxidation substrate in this link, succinate (succinic acid), is present in the mitochondria.

In recent years, it has been established that succinic acid can realize its effects, as well as the ligand of the orphan receptor GPR91 (encoded by the SUCNR1 gene), located on the cytoplasmic membrane of cells and coupled with G-proteins. This receptor is found in the kidneys (epithelium of the proximal tubules, cells of the juxtaglomerular apparatus), as well as in the liver, spleen, and blood vessels. Activation of the receptor by succinate present in the vascular bed increases the reabsorption of phosphate and glucose, stimulates gluconeogenesis, and can increase blood pressure (through an indirect increase in renin formation) [12, 13].

Subsequently, it was found that Mexidol is also capable of modulating receptor complexes of brain membranes, in particular benzodiazepine, GABA, and acetylcholine, enhancing their ability to bind to specific ligands [14].

It has been revealed that Mexidol increases the content of polar lipid fractions (phosphatidylserine and phosphatidylinositol) and reduces the cholesterol/phospholipid ratio in biomembranes, reduces their viscosity and increases fluidity, which indicates its lipid-regulating properties [15]. It has been shown that the drug can modulate the activity of membrane-bound enzymes: calcium-independent phosphodiesterase, adenylate cyclase, aldoreductase, acetylcholinesterase [16].

In vitro studies have established that Mexidol reliably suppresses both ascorbate-dependent (non-enzymatic) and NADPH2-dependent (enzymatic) iron-induced lipid peroxidation in brain homogenates, does not affect the activity of the 1-isoenzyme glutathione-S-transferase and catalase, but significantly increases activity of Se-dependent glutathione peroxidase. When studying the effect of Mexidol on the activity of NO synthases, it was revealed that the drug under study does not affect the neuronal activity, but moderately suppresses the activity of the inducible isoform [17].

Biochemical rationale for the use of Mexidol for cerebral hypoxia

The main source of energy in neurons is normally (85–90%) glucose, and the main process during which adenosine triphosphate (ATP) molecules are formed is oxidative phosphorylation, which occurs in the mitochondrial respiratory chain.

When one glucose molecule is oxidized under aerobic conditions, 38 ATP molecules are formed: 10 molecules as a result of aerobic glycolysis (4 molecules as a result of substrate phosphorylation reactions, 6 molecules in the mitochondrial electron transport chain as a result of oxidative phosphorylation during the transfer of protons and electrons from 2 molecules NADH2, formed during glycolysis); 6 ATP molecules - as a result of oxidative decarboxylation of pyruvate in the pyruvate dehydrogenase complex (ATP molecules are synthesized in the mitochondrial electron transport chain as a result of oxidative phosphorylation during the transfer of protons and electrons from 2 NADH2 molecules); 24 ATP molecules - as a result of the citrate cycle (Krebs cycle, tricarboxylic acids) (2 ATP molecules are formed from 2 glutamine triphosphate molecules, which in turn arise during the reaction of converting succinyl-CoA into succinate, 22 ATP molecules are synthesized in the mitochondrial electron transport chain as a result oxidative phosphorylation during the transfer of protons and electrons from 6 molecules of NADH2, 2 molecules of FADH2); in this case, 2 ATP molecules are spent on the phosphorylation of glucose and fructose-1-phosphate during glycolysis reactions [18].

Under normoxic conditions, the functioning of the respiratory chain, as a rule, depends on the oxidation of NAD-dependent substrates, the main supplier of reducing equivalents for the respiratory chain through the first mitochondrial enzyme complex. The contribution of this pathway in intact cells, assessed by oxygen consumption, can be up to 55–65%. However, 25–30% of mitochondrial respiration under these conditions is associated with mitochondrial enzyme complex II and succinate oxidation.

Under hypoxic conditions, there is a reversible suppression of the electron transport function of mitochondrial enzyme complex I and compensatory activation of mitochondrial enzyme complex II. At the same time, the content of succinate in the blood and tissues and the contribution of succinate oxidase to overall respiration sharply increase. The latter can reach 70–80% [13].

The binding of succinate to its specific receptors (GPR91) can trigger a cascade of biochemical reactions that also increase the body’s resistance to oxygen deficiency [13]. Increased amounts of succinate can be formed during a number of chemical reactions. For example, the aminobutyrate shunt (Roberts cycle) is activated in the brain, during which succinic acid is formed from glutamate [19]. In addition, the possibility of the formation of succinate from fumarate as a result of a reversible reaction of the Krebs cycle has been described [20], however, since this reaction consumes the FADH2 molecule, apparently, the significance of this reaction as a source of succinate under hypoxic conditions is small. It is assumed that to maintain energy processes in cells under anoxia and hypoxia, it is advisable to use substrates that can participate in the anaerobic formation of succinate, whereas under hypoxic conditions it is preferable to use succinate itself [21].

With the development of severe and prolonged hypoxia, the rate of endogenous succinate formation, apparently, may be insufficient to optimally compensate for the energy deficit. Therefore, the use of Mexidol, the molecule of which includes a succinic acid residue, to increase cell resistance to oxygen deficiency is biochemically justified, and the binding of succinic acid with 2-ethyl-6-methyl-3-hydroxypyridine increases its penetration into mitochondria [2].

As hypoxia increases, the functioning of the respiratory chain is suppressed and the main source of ATP synthesis becomes anaerobic glycolysis, the energy value of which is 2 ATP molecules [18]. Under physiological conditions, mitochondria are the main producers of reactive oxygen species. Potentially, any component of the respiratory chain under aerobic conditions, as a result of side chemical reactions, can be a donor of one-electron oxygen reduction. However, it is believed that the main sites for the generation of superoxide anion radical in the electron transport chain of mitochondria are flavoprotein, cytochrome B566 and semiubiquinone, and the most significant part of mitochondrial H2O2 is produced during O2 dismutation [22]. In this case, the number of free radicals formed is limited by the endogenous antioxidant system and is maintained at a stationary level.

Under conditions of oxygen deficiency, with an increase in the degree of reduction of respiratory chain transporters, the generation of superoxide anion radical and hydrogen peroxide increases with the participation of flavoproteins and in the ubiquinone–cytochrome C section of the electron transport chain.

During the autoxidation of coenzyme Q and the interaction of its radical with polyunsaturated fatty acids, lipid peroxidation is also activated [23]. The endogenous antioxidant system cannot cope with the increased amount of free radicals generated, which leads to the development of oxidative stress and damage to lipids, proteins, and nucleic acids.

Penetrating into mitochondria, Mexidol is able to directly bind the resulting reactive oxygen species, thus preventing the development of oxidative stress. An important role in the pathogenesis of most neurological diseases, incl. accompanied by the development of hypoxia, plays a role in the dysfunction of neurotransmitter and neuromodulatory systems, in particular the release of the excitatory mediator glutamate, which underlies the so-called. death from overexcitation or the phenomenon of excitotoxicity. When nerve cells are hypoxic, glutamate is released from the endings of neurons into the intercellular space. Its excessive accumulation activates the ionotropic NMDA and AMPA receptor subtypes, causing a massive influx of Ca2+ ions into the cytoplasm of the postsynaptic neuron. Calcium, in turn, triggers a number of processes: 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), which leads to the accumulation of NO; activation of heme oxygenase, which converts Fe3+ to Fe2+. All of these processes intensify lipid peroxidation, and in response, the cell’s antioxidant defense system is activated. With prolonged hypoxia, its depletion is observed, which contributes to the development of oxidative stress and death of nerve cells through apoptosis or necrosis, depending on the degree of their damage [24].

In vitro studies showed that Mexidol at a final concentration in a solution of 10 to 0.1 mM reduced the level of MDA in brain homogenates exposed to L-glutamate. Since free radical reactions play a leading role in the pathogenesis of glutamate neurotoxicity, this effect can be considered as the drug’s ability to suppress glutamate excitotoxicity [17].

Generics Mexidol

Recently, the domestic pharmaceutical market has seen a significant increase in the number of generic drugs. According to statistics, their share is 77% and only 23% are original medicines. At the same time, in the USA the share of generics is only 12%, in Japan – 30%, in Germany – 35% [25]. Mexidol, according to the State Register of Medicines (https://grls.rosminzdrav.ru) for 2021, has 11 generics registered in Russia.

In a study on 14 mature male chinchilla rabbits, we studied the pharmacokinetic parameters of Mexidol and its generic mexiprim (“STADA CIS”) after their oral administration at a dose of 100 mg/kg (3 tablets/rabbit, without compromising the integrity of the tablet shell) [ 5]. It was shown that Mexidol, compared to Mexiprim, is absorbed more completely and quickly from the gastrointestinal tract, which is manifested by a significantly higher (26.1%) maximum concentration of ethylmethylhydroxypyridine succinate and a 50% shorter time to reach it (Mexidol - 30 minutes, mexiprim – 1 hour). The total clearance, half-life and average retention time of ethylmethylhydroxypyridine succinate did not differ significantly after administration of Mexidol and Mexiprim, which indicates similar elimination of the studied drugs from the body of animals.

The results obtained are consistent with the information specified in the instructions for the drugs Mexidol and Mexiprim. Thus, the maximum concentration of ethylmethylhydroxypyridine succinate in blood plasma when taking Mexidol orally in doses of 400-500 mg is 3.5-4.0 μg/ml, and when taking Mexiprim - 50-100 ng/ml.

The identified differences may be associated with differences in the production technology of the drugs (degree of grinding, level of compression pressure when pressing tablets), as well as with the presence of different excipients both in the composition of the tablet core and in their shell.

The film shell of Mexiprim tablets contains most of the components of the Mexidol shell, but it does not contain a water-soluble film-forming polymer with high adhesive and emulsifying properties - polyvinyl alcohol. This may probably be one of the reasons for the lower bioavailability of Mexiprim compared to Mexidol.

A significant difference is observed in the composition of the tablet cores of the studied drugs. For example, the core of Mexiprim tablets includes a water-insoluble filler, kaolin, which can reduce the bioavailability of the active substance due to its physical adsorption or ion exchange [26]. In the injection dosage form of Mexidol, sodium metabisulfite (sodium pyrosulfite, sodium pyrosulphite, Na2S2O5) is used as an excipient - one of the most effective and safe stabilizers [27].

Safety

Currently available clinical and preclinical data indicate a favorable tolerability and safety profile of the drug and allow Mexidol to be classified as a non-toxic or low-toxic drug. Thus, interim data from a multicenter, randomized, double-blind, placebo-controlled study of the effectiveness and safety of Mexidol (solution for intravenous and intramuscular administration/coated tablets) in parallel groups during long-term sequential therapy of patients with hemispheric ischemic stroke in the acute and early recovery periods (EPICA) indicate a favorable safety profile and good tolerability of the drug, comparable to placebo.

Data obtained during the entire period of post-registration observation confirm that the drug Mexidol - film-coated tablets and solution for intravenous and intramuscular administration, is well tolerated and safe, and when used correctly, a favorable balance between benefit and risk is maintained.

pharmachologic effect

The pharmacological effect of Mexidol is due to its antioxidant properties. The drug eliminates oxygen starvation of tissues, normalizes thinking and memory processes. The drug has a positive effect on the condition of blood vessels susceptible to atherosclerotic changes.

Pharmacodynamics

The drug has antihypoxic, nootropic, anticonvulsant, anxiolytic and stress-protective effects. Mexidol increases the body's resistance to damaging factors, including shock, oxygen starvation of tissues, alcohol intoxication, and cerebrovascular accident due to ischemia.

The drug helps improve blood circulation in the brain area, prevents blood thickening and thrombus formation.

Has antihypercholesterol effect. Reduces the concentration of total cholesterol and low-density lipoproteins.

Mexidol normalizes sleep processes, increases attention, and improves thought processes.

Taking the drug against the background of withdrawal syndrome helps reduce the manifestations of alcohol and neurotoxic intoxication, normalizes autonomic functions, and eliminates cognitive impairment.

The combined use of the drug Mexidol with tranquilizers, sleeping pills, antidepressants and anticonvulsants enhances the effect of the latter. This allows you to reduce the dosage of prescribed medications.

Pharmacokinetics

The drug is quickly absorbed. The maximum concentration is reached 45-50 minutes after administration. After entering the bloodstream, Mexidol is quickly distributed in organs and tissues. The drug stays in the body for about 4-5.5 hours, depending on the method of administration.

Metabolism of the drug occurs in the liver. Mexidol forms several metabolites and breaks down into components.

Excretion from the body is carried out with urine. Most of it is excreted in the form of metabolites, the rest unchanged. The half-life is approximately 2-3 hours.

conclusions

Mexidol is a drug from the group of antioxidant nootropic drugs, which is widely used in medical practice for the complex treatment of acute and chronic disorders. A competent approach to prescribing and checking for compatibility with other medications is the key to the effectiveness of treatment. There is no evidence base for monotherapy with Mexidol, so independent use of the drug for diagnosed neurological diseases is accompanied by the risk of progression of the pathology and a worsening prognosis for the patient’s life.

Indications for use

The following indications for use of Mexidol in the form of a solution are distinguished:

• acute cerebrovascular accidents;
• traumatic brain injuries;
• manifestations of vegetative dystonia;
• open-angle glaucoma;
• anxiety and neurosis-like conditions;
• withdrawal syndrome due to alcohol abuse;
• drug intoxication;
• hypertonic disease;
• migraine-type headache;
• myocardial infarction in the acute phase.

Mexidol is prescribed as part of complex therapy for acute purulent lesions of the abdominal cavity requiring surgical intervention. This is, for example, acute pancreatic necrosis, peritonitis.

Indications for the tablet form of the drug are:

• consequences of cerebrovascular accidents;
• mild form of traumatic brain injury, as well as consequences;
• encephalopathy of various origins;
• as part of complex therapy of diseases of the cardiovascular system;
• asthenia;
• long-term exposure to psycho-emotional factors.

Mexidol for VSD

The indication for the use of Mexidol injections is vegetative-vascular dystonia. The drug helps improve blood circulation. As a result, headaches and dizziness are relieved. The dosage is selected individually depending on the severity of symptoms.

Mexidol for hypertension

The drug is part of the complex therapy of arterial hypertension. Mexidol normalizes metabolic processes that take part in the functioning of the cardiovascular system. The drug improves blood circulation, helping to stabilize blood pressure.

Mexidol for panic attacks

The drug has antihypoxic, nootropic and stress-protective effects. As a result, brain activity normalizes and the severity of anxiety symptoms decreases.

Mexidol for epilepsy

The anticonvulsant effect of the drug allows its use in the complex treatment of epilepsy. Mexidol normalizes cerebral circulation, improves thinking and memory processes. The dosage is determined by the attending physician depending on the severity of the condition.

Mexidol for oncology

Mexidol is included in the complex therapy of oncopathologies due to its antioxidant effect. The decision about the need to prescribe the drug is made by the attending physician. Some tumor formations exclude the possibility of taking Mexidol.

Mexidol for migraines

The disease tends to periodically worsen. Mexidol is used to prevent migraine-type headaches. The drug improves blood microcirculation processes in the brain area.

Mexidol for stroke

Cerebrovascular accidents and their consequences are included in the list of indications for taking the drug. Mexidol is used both in the acute period and as a prevention of relapse. Indications for the use of the drug in tablets are preliminary injection therapy.

Mexidol for multiple sclerosis

Used as part of complex therapy. Improves cerebral circulation, helps normalize cognitive functions.

The use of Mexidol for parkinsonism

Parkinsonism (Parkinson's disease) is a neurological pathology that is characterized by a progressive decrease in the amplitude and accuracy of movements, against the background of which tremor (shaking) of the limbs develops. Most often, the disease is diagnosed in older people (over 55 years old).

The morphological basis of the disease is associated with a violation of the synthesis of dopamine, a mediator of nerve impulses, in the substantia nigra of the brain. Standard treatment for pathology involves the use of replacement therapy with active precursors of the substance.

Long-term use of such drugs contributes to metabolic disorders in neurons, which is manifested by the synthesis of free radicals and damage to the cell membrane. An integrated approach using antihypoxic agents additionally affects peripheral structures and improves metabolism in the brain.

Clinical studies using Mexidol in the treatment of Parkinson's disease noted:

• increasing the speed of impulse transmission along the nerve (during a study on an electroneuromyograph);
• reducing the manifestations of tremor (oscillations) and increasing the amplitude of movements;
• increased efficiency and the possibility of reducing the dose of basic antiparkinsonian drugs (illustrated using the example of Cyclodol);
• reduction in the severity of symptoms (unsteadiness of gait, tremors in the hands, stiffness of movements) according to the Hen-Yahru scale;
• an increase in the concentration of dopamine metabolic products in the blood (results of an experimental study at the Center for Extrapyramidal Diseases).

As part of complex therapy, Mexidol is recommended for patients with Parkinson's disease at a dose of 200-400 mg/day in the form of a dropper (4-8 ml of a 5% solution of the drug per 250-300 ml of saline).

Directions for use and doses

The method of administration and dosage of Mexidol are determined by the attending physician depending on the disease and the severity of the condition.

Mexidol 5

Solution for injection, 5 ml. Before use, the drug must be diluted with isotonic sodium chloride solution. When using the drug as a jet, it is administered within 5-7 minutes. Drip administration requires a speed of 40-60 drops per minute. The daily dose of the drug should not exceed 1200 mg.

Mexidol 10

The solution for injection contains 5 ampoules of 10 ml each. The contents are dissolved using isotonic saline solution. Used when a long course of therapy is necessary. The drug is administered intravenously or intramuscularly, depending on the pathology and severity of the condition. In case of acute cerebral circulation, intravenous administration of the drug is prescribed at a dosage of 200-500 mg 2-4 times a day, followed by intramuscular administration of 200-300 mg 2-3 times a day.

Mexidol 2

5 ampoules per package contain 2 ml of the drug. The solution is used for intramuscular or intravenous administration by stream or drip. The contents of the ampoule are diluted with isotonic saline solution. The dosage depends on the pathology for which the drug is prescribed. The average dose is 200-500 mg 2-3 times a day IV or IM.

Mexidol 125

The use of Mexidol in tablet form is indicated for various conditions. The dosage is 125-250 mg 3 times a day. The maximum permissible daily dose is 800 mg. The duration of the course is determined by the attending physician depending on the disease and severity of the condition. On average it ranges from 14 days to 1.5 months. The course begins with 1-2 tablets per day. The dose is gradually increased until the clinical effect of the drug is achieved. Abrupt discontinuation of the drug is unacceptable. The dosage is gradually reduced until complete withdrawal.

Mexidol tablets

Mexidol is available in tablet form. The dosage of the drug is 125 mg. The tablets are film-coated and are in cell packaging. Indications for the use of the tablet form of the drug Mexidol are the recovery period after an acute cerebrovascular accident, a mild form of traumatic brain injury, encephalopathy of various origins, VSD, and mild cognitive disorders. Mexidol in tablet form is used as a continuation of injection therapy.

Mexidol solution

The solution for injection is available in volumes of 2, 5 and 10 ml. It has no color. A yellowish tint of the solution is allowed. The contents of the ampoules are dissolved using an isotonic sodium chloride solution. The drug is used for the treatment of acute cerebrovascular accident, severe traumatic brain injury and its consequences, cognitive disorders, acute myocardial infarction, and reducing the severity of symptoms of withdrawal syndrome due to alcoholism. Mexidol in the form of a solution is prescribed for acute cerebrovascular accident, severe traumatic brain injury, and acute myocardial infarction.

The drug is used to reduce the severity of withdrawal symptoms due to excessive consumption of alcoholic beverages. The dosage of the drug is selected by the attending physician individually depending on the pathology.

Mexidol in ampoules

The drug is available in glass ampoules of 2 and 5 ml. The package contains from 5 to 10 ampoules. Mexidol is used for intramuscular or intravenous administration. To obtain the finished solution, the contents of the ampoule are diluted with an isotonic sodium chloride solution. Mexidol is administered in a stream or drip. The dosage and route of administration are determined by the attending physician depending on the disease and severity of the condition. The maximum dose of the drug is 1200 mg per day

.

Mexidol injections

The dosage and frequency of use of Mexidol in the form of injections is determined by the disease for which the drug is prescribed. In case of acute cerebrovascular accident, intravenous drip administration of the drug 2-4 times a day is indicated. The dosage is 200-500 mg. The medicine is then administered intramuscularly. A similar method is used to treat traumatic brain injuries.

To relieve cerebrovascular insufficiency, drip administration of 200-500 mg of the drug is used 1-2 times a day. The course is determined by the severity of symptoms.

In the presence of dyscirculatory encephalopathy, Mexidol is administered intramuscularly at a dose of 400-500 mg 2 times a day.

Age-related impairment of cognitive functions is treated by intramuscular administration of the drug in a dosage of 100-300 mg.

How to inject Mexidol

It is recommended to administer the drug intravenously during the first 5 days of therapy. Then the transition to intramuscular use is allowed. To prepare the solution, the contents of the ampoule are dissolved in an isotonic sodium chloride solution. In some cases, the use of a 5% glucose solution is indicated.

Injection of the drug is carried out within 5-7 minutes. The most suitable speed for drip use of the drug is 40-60 drops per minute. The maximum dosage is 1200 mg per day.

Mexidol Dent (toothpaste)

The drug is available in the form of toothpaste. The tube contains 65 g of product. Indications for the use of Mexidol Dent are inflammation and bleeding of the gums. The drug helps accelerate the regeneration of damaged oral mucosa and normalizes blood microcirculation. The toothpaste does not contain preservatives or dyes. Due to its composition, it does not disturb the microflora of the oral cavity. Mexidol Dent is indicated for long-term use. To use, simply apply a small amount of paste to your toothbrush. Use sweeping movements to process the teeth. The gums are gently massaged. The course of use of the drug is not limited.

Mexidol White (toothpaste)

The release form of the drug allows its use in dental practice. The tube contains 65 g of product. Indications for the use of Mexidol White include the presence of plaque and inflammatory gum diseases. Thanks to the components included in the composition, the drug provides gentle cleaning of teeth and prevents the re-formation of plaque. Mexidol White protects teeth from aggressive agents that cause caries. The active ingredient in toothpaste prevents gum bleeding and reduces the severity of inflammatory diseases. Contraindication for use is individual intolerance to the components of the drug.

How often can the course of treatment be repeated?

Mexidol is a drug that is used to systemically improve cellular metabolic processes. Experts recommend taking the product regularly, in short or medium-duration courses:

• 10-14 days - every 2 months;
• 6 weeks - once every 6-12 months.

It is always prohibited to use Mexidol due to addiction and reduced effectiveness of the drug. For long-term correction of oxidative processes in the body, the use of other means is recommended during the pause.

Interaction

The drug is combined with many drugs used to treat somatic pathologies. Mexidol enhances the effect of antidepressants, anticonvulsants, antiparkinsonian, and benzodiazepine drugs. This allows you to reduce the initial dosage of prescribed medications.

Compatibility of Mexidol and Combilipen

In neurological practice, Mexidol and Combilipen are often prescribed for the treatment of various diseases. The drugs enhance each other’s effects, promoting rapid restoration of affected areas of the nervous system and improving tissue trophism. Combilipen is one of the vitamin-containing medicines. It contains B vitamins. The drug improves nerve conduction and helps normalize blood microcirculation. Vitamins and antioxidants are used to treat strokes, encephalopathies, polyneuropathies and other neurological diseases. The combined use of the drugs Combilipen and Mexidol normalizes emotional states and improves brain activity.

Compatibility of Mildronate and Mexidol

Mildronate has a general tonic effect on the body, eliminates the manifestations of hypoxia and restores damaged cells. The drug increases endurance. Indications for prescribing Mildronate include physical and psycho-emotional stress, the recovery period after surgery, treatment of alcohol dependence, and decreased performance. The simultaneous use of Mildronate and Mexidol is not contraindicated. Medicines are used as part of complex therapy for brain disorders.

Compatibility of Mexidol and Grandaxin

Grandaxin belongs to the group of anxiolytic drugs derived from benzodiazepines. Indicated in the presence of psycho-emotional disorders. For example, neuroses, mental disorders, withdrawal symptoms due to alcohol abuse, depression, menopause. Mexidol enhances the effect of benzodiazepines. Therefore, a dosage adjustment of Grandaxin may be required. This must be taken into account when prescribing these drugs simultaneously.

Compatibility of Mexidol and Eglonil

Eglonil belongs to the group of neuroleptics. Has an antipsychotic effect. The drug blocks dopamine receptors. Indicated in the presence of psychosis and schizophrenia. Taking Mexidol and Eglonil together can enhance the effect of the latter. This may require adjustment of the drug dose.

Analogues and domestic substitutes

The domestic manufacturer offers patients many analogues - products that differ in name and cost: Mexiprim, Neurox, Astrox, Meksifin, Neurocard, Proinin.

Complex therapy in an inpatient clinic for neurological and cardiovascular diseases is accompanied by the use of antioxidants and other agents that improve metabolism.

The drugs most used in clinical practice are:

• nootropics (to improve cognitive abilities, accelerate metabolic processes in the brain): Piracetam, Pantogam, Bifren, Noofen, Cerebrolysin;
• “Actovegin” is a product made from dried calf blood extract, which increases tissue resistance to hypoxia, improves metabolic processes, and accelerates the healing of ulcers and wounds;
• "Mydocalm" is a drug used in neurology for the treatment of diseases with increased muscle tone (multiple sclerosis, parkinsonism), postoperative and traumatic contractures;
• "Meldonium" ("Mildronate") is a universal metabolic agent that is used in cardiology to restore the myocardium after a heart attack;
• vitamin preparations with antioxidant and neuroprotective effects: “Milgamma” (group B complex), “Aevit” (A+E).

Autonomic disorders caused by compression of nerve roots due to osteochondrosis require complex therapy:

• diuretics (“Furosemide”);
• nonsteroidal anti-inflammatory drugs (“Voltaren”, “Diclofenac”);
• muscle relaxants - to relax spastic back muscles (Mydocalm, Baclofen).

To relieve headaches, doctors recommend drugs with proven effectiveness - Spazmalgon, Ibuprofen.

Mexidol and alcohol

Mexidol is used to treat withdrawal symptoms associated with alcohol abuse. The drug helps normalize brain activity, improve blood circulation, and remove toxins from the body. Indications for the use of Mexidol are alcoholic encephalopathy, polyneuropathy, manifestations of withdrawal syndrome, epileptic seizures due to an overdose of alcoholic beverages, intoxication syndrome. Prescribing the drug to dependent people helps speed up the recovery period. Taking alcohol together with Mexidol leads to the fact that the drug does not have time to restore damaged cells. As a result, the effect of the drug is reduced to zero. Further use of the drug is pointless.

Features of application at low pressure

The decrease in blood pressure when taking Mexidol is due to increased synthesis and accumulation of natriuretic peptide, which promotes the removal of sodium salts and water from the body (diuretic effect).

The moderate hypotensive effect of the drug requires careful use in patients with low levels of:

• at values ​​of 110/70-90/60 – it is allowed to take a standard dose of Mexidol;
• less than 90/60 – consultation with a specialist is required about the advisability of prescribing the drug and the need for pressure correction.

For mild hypotension, Mexidol is recommended due to its ability to normalize the autonomic innervation of the vascular wall and increase indicators to optimal values.

Drug interactions: the drug enhances the effect of antihypertensive drugs (beta-blockers, diuretics), therefore it is prescribed with caution to patients with mild hypertension.

Comparison with other drugs

Analogs of Mexidol in terms of their effect include Mexiprim Astrox, Medomexi, Actovegin, Cerakson, Picamilon, Cavinton.

Mexidol or Mexiprim?

Mexiprim is one of the neuroprotectors. Available in tablet form and also as a solution for injection. The drug helps improve blood microcirculation, has a nootropic effect, and helps increase the body's resistance to psycho-emotional overload. Mexiprim is used to treat convulsive and withdrawal symptoms associated with alcohol abuse. Mexidol is the original drug, Mexiprim is a generic. According to research, Mexidol is absorbed more quickly into the gastrointestinal tract; its shell contains no preservatives or insoluble substances. Among the components of Mexiprim there is a preservative, the presence of which increases the possibility of developing individual intolerance to the drug.

Mexidol or Astrox?

Astrox is a generic version of the drug Mexidol. The drugs have the same active ingredient. Accordingly, the medications have identical effects. The difference between drugs lies in the manufacturing technology, excipients, release form and the quality of the purification of raw materials. These factors affect the bioavailability of the drug. Mexidol has a larger number of release forms. This variety allows you to select the required dosage depending on the disease and severity of the condition. The number of side effects of Astrox is significantly greater than that of Mexidol.

Mexidol or Medomexi?

Mexidol and Medomexi belong to the group of nootropic and antioxidant drugs. The action of the drugs is identical. The composition contains one active ingredient. Medomexi is an analogue of Mexidol. The difference between them lies in the total cost of the drug.

Mexidol or Actovegin?

Actovegin improves microcirculation of blood in the brain, accelerates healing processes, and increases the body's endurance in conditions of oxygen starvation. Actovegin is prescribed for cerebrovascular accidents, polyneuropathy, distal angiopathy due to diabetes mellitus. The drug promotes rapid tissue regeneration in wounds, abrasions and burns. Available in tablet form, as a solution for injection and ointments for external use. The differences between Mexidol and Actovegin lie in their mechanism of action. Unlike Mexidol, Actovegin has regenerating properties. Mexidol has a wider range of indications. Actovegin is approved for use during pregnancy and lactation. Often both drugs are prescribed as part of complex therapy for various diseases.

Mexidol or Ceraxon?

Ceraxon is one of the nootropic drugs. Used to treat acute cerebrovascular accident. The drug allows you to slow down the growth of the lesion for several hours. This time is enough to transport the patient to the hospital. Cerakson is prescribed during the rehabilitation period after a stroke, to normalize the condition after traumatic brain injury. Ceraxon and Mexidol are complementary drugs. They are used as part of complex therapy for brain disorders.

Mexidol or Picamilon?

Picamilon is a nootropic drug. Promotes the expansion of blood vessels in the brain. Indications for the use of the drug are cerebrovascular accident, withdrawal syndrome, encephalopathy of various origins, increased anxiety and irritability, severe migraine-type headaches. Unlike Mexidol, Picamilon is approved for use in school-age children. The medicine is used to increase brain activity.

Mexidol and Picamilon are complementary medicines. Their combined use improves the prognosis and speeds up the recovery period.

Mexidol or Cavinton?

Cavinton has antioxidant and antihypoxic effects and reduces the possibility of blood clots. Indicated as part of complex therapy for cerebrovascular accidents, encephalopathy of various origins, increased blood pressure, and pathology of the vestibular apparatus. The simultaneous use of Mexidol and Cavinton is not contraindicated. Medicines are considered complementary, but they should be taken at different times of the day.

Contraindications

Mexidol for low or high blood pressure may be contraindicated in various conditions complicated by other pathologies, otherwise there is a risk of harm to health.

Among the main contraindications:

• severe kidney pathologies up to the onset of acute failure;
• hypersensitivity to any substance in the medication, which may cause an allergic reaction;
• not prescribed for children under 16 years of age;
• should not be used by pregnant women;
• danger to the baby during lactation, as the drug can pass into breast milk.

Where to buy Mexidol: price, reviews

The product can be bought in pharmacies at a price of 250 rubles for a package of 30 tablets or 450 rubles for 10 ampoules with a solution of 50 mg/ml. If you study customer reviews, you can see that the drug is very popular - the drug is recommended by more than 80% of patients.

Among the advantages are efficiency, reasonable price, and completely reliable information in the instructions. Many buyers write that their headaches, dizziness and other unpleasant sensations have gone away. In some cases, they talk about the lack of treatment results and the occurrence of side effects.

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 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.