Clinical and pharmacological characteristics of nootropic drugs. Clinical pharmacology of nootropic drugs. according to their chemical composition

For quotation: Kotova O.V. Nootropic drugs in modern medicine // RMJ. 2011. No. 29. S. 1816

Nootropics are substances that have a specific effect on the higher integrative functions of the brain, improving memory, facilitating the learning process, stimulating intellectual activity, and increasing the brain’s resistance to damaging factors.

Nootropic drugs can improve cognitive (cognitive) functions both in people suffering from various brain diseases and in healthy people. At the same time, they do not cause psychomotor agitation, depletion of the body’s functional capabilities, or addiction.
The term “nootropics” (from the Greek words “noos” - thinking and “tropos” - striving) was adopted in 1972, two years after the appearance of the drug piracetam on the world market. Although there is no generally accepted classification of nootropics yet, these drugs include:
piracetam, its homologues and analogues (aniracetam, oxiracetam, pramiracetam, nefiracetam, etc.);
dimethylaminoethanol derivatives: deanol aceglumate, meclofenoxate, centrophenoxine;
neuroamino acid preparations: gamma-aminobutyric acid (GABA), gamma-aminobutyric acid derivatives (phenibut, nicotinoyl-gamma-aminobutyric acid (picamilon), hopantenic acid (pantogam), glycine, glutamic acid;
pyridoxine derivatives: pyritinol (pyriditol, enerbol, encephabol);
centrally acting cholinomimetic: choline alfoscerate;
Ginkgo biloba preparations: bilobil, memoplant, tanakan, etc.;
compounds of a different chemical structure, belonging to different classes and groups of chemical substances, similar in their mechanism of action to piracetam and having the ability to facilitate learning processes and improve memory.
Along with true nootropic drugs (with a dominant effect on mnestic functions), various authors classify drugs with a wide range of effects as nootropic drugs:
drugs that enhance cerebral circulation, microcirculation and metabolism: vinpocetine, vincamine, vinconate, nicergoline, cinnarizine, flunarizine, nimodipine, xanthine derivatives of pentoxifylline, carnitine, phosphatidylserine, sodium oxybate; vitamins and their derivatives: pantothenic acid, folic acid, vitamin E;
intermediate products of cell metabolism: orotic and succinic acids;
combination drugs: instenon, omarone.
Piracetam became the founder of the class of nootropic drugs. It was synthesized in 1963 by UCB as an antikinetic agent. Studying the effects of piracetam allowed the chief researcher of UCB K. Giurgea already in 1972 to formulate the basic properties of a new class of drugs - nootropics.
The pharmacological effects of nootropics consist of metabolic and neurotrophic effects, which, in turn, determine the processes of improving redox reactions, reducing the aggressive effect of lipid peroxidation (LPO) products, and a positive effect on neurotransmission. In addition, these drugs have a vasoactive and mild antiplatelet effect.
The main mechanisms of action of nootropic drugs include:
accelerating the penetration of glucose through the blood-brain barrier and increasing its absorption by brain cells, especially in the cerebral cortex;
increased conduction of cholinergic impulses in the central nervous system (CNS);
stabilization of cell membranes (increased synthesis of phospholipids and proteins in neurons and red blood cells);
inhibition of lysosomal enzymes;
activation of cerebral microcirculation by improving the deformability of erythrocytes and preventing platelet aggregation;
improvement of cortical-subcortical interaction;
normalization of neurotransmitter disorders;
activating effect on higher mental functions (memory, learning ability, etc.);
improvement of reparative processes in case of brain damage of various origins.
Piracetam has a chemical structure similar to GABA and is sometimes considered a derivative of this amino acid, but it is not converted into GABA in the body and its content in the brain does not increase after using piracetam.
Despite 50 years of use in clinical practice, the exact mechanism of action of piracetam and nootropics in general has not yet been established. Most researchers suggest that piracetam exerts its main action through ion channels or ion transport subunits, resulting in a nonspecific increase in neuronal excitability. At the same time, the lack of agonistic or inhibitory effects on most neurotransmitters explains the low toxicity of piracetam.
One theory that explains many of the effects of piracetam is the membrane theory. Several studies have demonstrated that membrane fluidity decreases with age. This entails a deterioration in membrane-related processes: the interaction of enzymes, receptors and functions. Piracetam can restore this process. On the other hand, there is a positive effect of piracetam on glucose utilization, as well as ATP production.
Piracetam has a beneficial effect in situations related to impaired brain function in conditions such as aging, hypoxia, trauma, and neurodegenerative processes. In all these situations, mitochondrial dysfunction is detected. Impaired mitochondrial function and decreased respiratory chain activity lead to decreased ATP levels, glucose consumption, and ultimately neuronal dysfunction and cell apoptosis. It has been shown that piracetam can improve mitochondrial function and stabilize the mitochondrial membrane in situations of increased risk of damage. This is supported by studies using specific fluorescent dyes to monitor mitochondrial membrane potential.
Thus, protection against mitochondrial dysfunction, increased ATP production, and prevention of apoptosis may be important effects of piracetam on aging and neurodegeneration (since mitochondrial dysfunction and decreased energy metabolism are early processes in Alzheimer's disease).
Piracetam has neuroprotective, antithrombotic and rheological positive effects. The interaction of its molecule with phospholipids of membranes and restoration of the fluidity of cell membranes explains the effectiveness of piracetam in an extremely wide range of diseases.
Piracetam is used in many countries to treat cognitive decline in aging, brain injury, and dementia. Although its clinical effectiveness is still a matter of debate, a meta-analysis of clinical trials using piracetam provides compelling evidence of the drug's effectiveness in older patients with cognitive impairment.
A distinctive feature of piracetam is its low toxicity.
In clinical practice, piracetam is often combined with various drugs. Many clinical studies demonstrate its synergistic effect with anticonvulsants, especially carbamazepine. This combination can enhance the antiepileptic effect and neutralize the deterioration of cognitive functions induced by anticonvulsants. Combination with various vitamin complexes helps enhance the metabolic effect of piracetam. Finally, practical neurologists often combine piracetam with vasoactive drugs, thereby enhancing both nootropic and vascular effects.
The most successful is the combination of piracetam with cinnarizine. Cinnarizine is an antihistamine first synthesized in 1955 as a treatment for motion sickness and Meniere's disease. Further research has shown that cinnarizine can also be considered as a nootropic agent, since its vasoactive effect (due to calcium channel blockade) is mainly realized in the brain. Cinnarizine, by disrupting the flow of calcium ions into vascular smooth muscle cells, reduces the tone of the smooth muscles of arterioles and increases tissue resistance to hypoxia. The vasodilatory effect of cinnarizine is not accompanied by a significant effect on systemic blood pressure.
In addition to the vasodilating effect, cinnarizine reduces blood viscosity by increasing the elasticity of red blood cell membranes and their ability to deform. The spectrum of side effects of cinnarizine includes gastrointestinal symptoms (diarrhea, constipation, nausea, vomiting, abdominal pain), headache, dry mouth, sweating. The severity of side effects is moderate, they are transient and, as a rule, do not require discontinuation of the drug. With long-term use of cinnarizine, disorders of the extrapyramidal system can very rarely occur. Epidemiological studies show that the risk of extrapyramidal side effects becomes significant with continuous use of cinnarizine for more than 4–6 months. at a dose of over 75 mg/day. in persons over 70 years of age. If movement disorders occur, the drug containing cinnarizine must be immediately discontinued. Cinnarizine in its pure form and as part of combination drugs should not be prescribed to patients suffering from Parkinson's disease or having parkinsonism syndrome.
The combination of piracetam with cinnarizine increases the supply of oxygen to the brain. Currently, there are official drugs containing piracetam and cinnarizine in one tablet. One of these drugs is Omaron®, containing 400 mg of piracetam and 25 mg of cinnarizine. The range of indications for Omaron® includes primarily cerebrovascular diseases, including vascular dementia, as well as encephalopathies of various origins, diseases of the central nervous system, accompanied by a decrease in intellectual and mental functions. In case of cerebrovascular disease (dyscirculatory encephalopathy), Omaron® acts on two main links in pathogenesis: improves cerebral perfusion and has a beneficial effect on cerebral metabolism. The mechanism of action of the component cinnarizine included in Omaron® allows the drug to be used for the prevention of migraine attacks. Calcium channel blockers have long been used to prevent migraines.
Omaron® has been shown to be highly effective in treating chronic and acute ischemic brain lesions. Thus, in a controlled study (comparison drug - vinpocetine), which included patients with dyscirculatory encephalopathy, a decrease in the frequency of complaints of memory impairment, headache, dizziness, and decreased performance after 14 days of therapy with Omaron® was demonstrated by an average of 40%, and after 28 days - on average by 70%. This particularly affected dyssomnic disorders, which may be associated with the sedative effect of cinnarizine. The results were comparable to those in patients in the control group, and were superior in some respects (headaches, dizziness, staggering when walking). Positive dynamics were noted according to ultrasound data of the main arteries of the head and neck, and an electroencephalographic study of the bioelectrical activity of the brain.
The use of Omaron® in complex therapy of ischemic stroke can significantly reduce neurological deficit (according to the Lyons scale) by 46% in the main group. In the comparison group, whose patients did not receive nootropic drugs, the same figure decreased by 27%. Significant differences were also recorded in the assessment of cognitive function (MMSE), emotional-volitional sphere (HADS scale) compared with the initial data and indicators of the control group.
In a controlled study assessing the effectiveness of Omaron® in patients with post-stroke cognitive impairment during repeated examinations in the main group and in the comparison group, a significant (p)<0,05) улучшение показателей когнитивных функций по данным нейропсихологического исследования. Это улучшение отмечено уже через 1 мес. лечения, но было более значительным через 2 мес. Через 1 и 2 мес. лечения достоверно (р<0,05) установлены более высокие показатели когнитивных функций по некоторым нейропсихологическим тестам. В частности, результаты теста запоминания 5 слов в основной группе выросли с 8,20±1,53 балла до лечения до 8,89±1,3 балла после 1 мес. лечения и до 9,31±0,97 балла после 2 мес. лечения. По краткой шкале оценки психического статуса (MMSE) и по шкале выявления лобной дисфункции (FAB) также получено достоверное улучшение в группе лечения Омароном®. За 2 мес. наблюдения в обеих группах пациентов отмечены достоверное улучшение показателей неврологического статуса и уменьшение степени инвалидизации (по шкалам Рэнкина, Бартель, NIH–NINDS). В основной группе отмечена тенденция (р>0.05) to a more significant restoration of neurological functions and a decrease in the degree of disability compared to the control group.
Omaron® dosage regimen: 1-2 tablets 3 times a day. within 6–12 weeks. The drug is well tolerated, and the safety of its components has been tested for a long time.
Thus, Omaron® is a successful combination of drugs with different mechanisms of action, allowing the practitioner to effectively and safely help his patients.

Literature
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4. Putilina M.V. Modern ideas about nootropic drugs. Attending Physician: Journal for the Practitioner, 2006, No. 5, pp. 10–14.
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The list of drugs in this group contains substances that help protect the brain from damage and stimulate nerve cells to restore them to the level of healthy people.

Nootropic drug, what is it?

The concept of “nootropic drug” was first introduced in the last century by Belgian pharmacologists.

Nootropics are neurometabolic stimulants that activate metabolic processes in the brain, increasing its overall resistance to extreme situations and influences.

A distinctive factor from psychostimulants is that nootropics are antihypoxants (resist oxygen starvation of the brain), but do not negatively affect the human body, do not lead to disruptions in the functioning of the brain, and do not impair coordination of movements.

Medicines in this group are often of interest to students and people who experience severe intellectual or stress loads, since the instructions indicate that the drugs promote better assimilation of information, quick thinking, improvements in studies and smooth out the effect on the brain under stress and mental stress.

In pharmacology, there is one division of nootropics into two groups:

Which pharmacological group do they belong to?

The nootropic group includes drugs with nootropic action, and they are classified in pharmacology under the code (ATC code: N06ВХ).

The first drug in the group of nootropic drugs is Piracetam.

It was opened back in 1963, and gave rise to their development. The nootropic became the main competitor of psychostimulants, since the side effects from it were not so serious.

Nootropic therapy does not cause addiction, toxic damage, agitation and exhaustion of the body, which are inherent in psychostimulants. In the initial stages of the drug's development, it was used to treat brain dysfunction in older people.

Fact! In modern pharmacology, Piracetam is listed under the name Nootropil.

The table shows a list of drugs that are most often prescribed in nootropic treatment.

Mechanism of action of nootropics

Most drugs in the nootropic group affect neurotransmitters (substances that promote the interaction of nerve cells with each other).

Nootropic therapy affects acetylcholine (which carries out neuromuscular transmission), serotonin (the hormone of happiness), dopamine (the precursor of norepinephrine, which is a necessary part of the “reward system” of the brain, as it induces a feeling of pleasure, which affects the processes of motivation and learning) and norepinephrine ( one of the most important “mediators of wakefulness”).

The effect of a nootropic can prolong life and rejuvenate the body.

Also, these drugs protect nerve cells from deformation and eliminate oxygen starvation, stimulate metabolic processes and simply improve blood circulation in brain tissue.

Different drugs from the nootropic group can have different effects on the body, it all depends on the group to which the drug belongs.

Among them:

Fact! To stimulate biochemical processes in the brain, it may take from a couple of days to a couple of weeks, depending on the drug used. This explains why nootropics are used in courses. There is no point in taking pills immediately before exercising your brain; you should start using them about a month in advance.

What effect do nootropics have?

The impact on the above mechanisms in the brain makes it possible to conclude that the following positive effects have on the body and its systems:

• Vasovegetative action characterized by acceleration of blood circulation and elimination of the main signs of neurocircular dystonia;
• Antihypoxic effect due to the formation of increased resistance of brain cells to oxygen starvation;
• Antidepressant effect. Certain nootropics are prescribed for depression and are aimed at counteracting it;
• Psychostimulating effect caused by stimulation of brain functioning in people with mental disorders suffering from apathy and motor retardation;
• Antiepileptic effect characterized by the fact that it prevents convulsions, confusion and complete loss of consciousness, as well as the prevention of behavioral and autonomic system disorders;
• Sedative effect characterized by a calming effect;
• Nootropic effect is aimed at stimulating cognitive activity;
• Antitoxic action e - this is neutralization, or removal of toxins from the human body;
• Adaptogenic effect due to the development of the body’s resistance to the influence of negative factors;
• Immunostimulating effect characterized by strengthening the immune system and increasing the body’s overall resistance;
• Lipolytic action due to the use of fatty acids as a source of energy.

Note! Nootropics, in most cases, are prescribed for the elderly and children. This is explained by the fact that in old age it is necessary to correct deviations in the functionality of intellectual activity (memory, attention). Prescription in childhood occurs in the fight against intellectual development disorders of the child.

Is it dangerous to be treated with nootropics and are they harmful?

The consequences of using nootropics can range from headaches and dizziness to overexcitation of the nervous system.

But since they are not pathologically dangerous, the catalog of drugs can be prescribed to almost any patient.

The most serious and common side effect is withdrawal symptoms.

It can occur when the use of medications is abruptly stopped, which leads to suffering in the body.

Its most common manifestations can be headaches, lethargy, aggressiveness, loss of sleep, dizziness, etc. That is why the cessation of the course of treatment occurs with a gradual reduction in the drugs used.

The main side effects reported with nootropics are listed below:

Indications for the use of nootropics

The main indications for nootropics and their therapy are the following:

Contraindications to the use of nootropics are:

• Hemorrhagic stroke;
• Severe kidney pathologies;
• The period of bearing and feeding a child;
• Kidney or liver failure;
• Clearly manifested psychomotor agitation;
• Sensitivity to the active ingredients of the drug.

Most Common Nootropics

Nootropic therapy medications are divided into groups of new and old generation. The latter include medications that were discovered a long time ago, even at the start of neurostimulants. These are the production forms of Piracetam.

Such drugs are:

• Pramiracetam;
• Aniracetam;
• Oxiracetam;
• Isacetam;
• Etiracetam;
• Detiracetam;
• Nefiracetam.

After the nineties of the twentieth century, a new round took place in the history of the development of nootropics. New drugs have a selective effect on individual body functions.

The most commonly prescribed new generation drugs are:

• Pantogam– the most effective nootropic drug, often used for treatment in childhood. The main active ingredient is vitamin B15, which is found in almost all plant substances;
• Phenibut is prescribed for a state of general weakness, neuroses, sleep disorders and deviations in the normal functioning of the vestibular apparatus. The interaction of Phenibut helps children overcome stuttering and various tics. This drug normalizes metabolism, stimulates mental processes (memory, attention, etc.), and also has an antioxidant effect. This drug contains practically no toxins and does not cause allergies;
• Fezam is a nootropic prescribed in combination with other drugs for problems with blood circulation in the brain cavity. This drug eliminates the effects of oxygen starvation, helps against headaches, migraines, dizziness and memory loss. Long courses of treatment are prescribed for stroke, traumatic brain injury and inflammation of the membranes and tissues of the brain;
• Piracetam is a classic remedy prescribed to improve metabolic processes in the brain. Effectively treats dizziness, improves memory, and treats encephalopathy in childhood. The drug quickly relieves the negative effects of excessive consumption of alcoholic beverages. It is used for viral neuroinfections and as one of the drugs for restoration after death of heart muscle tissue. The drug is sold both in tablets and in ampoules, solutions, syrups and capsules, which helps to choose the most convenient form of use;
• Cinnarazine– a drug from the nootropic group that helps expand the walls of brain vessels and helps increase their size without affecting blood pressure. Nootropil cinnarizine is an effective drug against motion sickness, as well as suppressing nystagmus. The drug helps relieve high blood pressure, tinnitus, general weakness, headaches, restores normal sleep, removes aggressiveness, etc.;
• Actovegin– a drug from the group of nootropics, aimed at combating oxygen starvation of the brain, restoring metabolic processes, and promoting rapid healing of wounds. The drug is available in tablets and as an ointment or cream;
• Cerebrolysin is a nootropic used in combination with other medications. This drug has passed all tests and confirmed its safety and effectiveness. Stimulates mental activity and improves mood. Long-term use of the drug improves memory processes, increases concentration and the ability to learn.

What actions will help you recover faster and keep your body normal?

Preventive actions to prevent the use of nootropics are:

• Maintaining a daily routine with proper rest and sleep (at least 8 hours);
• Proper nutrition should be balanced and varied, with plenty of vitamins and nutrients;
• Maintaining water balance (at least 1.5 liters of clean water per day) will help the blood not to thicken and circulate normally;
• Avoid stressful situations, psycho-emotional and intellectual excessive stress;
• Stop smoking, alcohol and drugs;
• Get a full examination once a year.

Conclusion

Nootropic drugs are effective means used to improve the functioning of brain processes.

It is especially effective to take them in courses, in advance of intellectual or psycho-emotional stress.

A wide range of drugs and a low chance of side effects make the drugs accessible and effective. To prevent complications, it is better to consult a qualified doctor.

ISPiP named after Raoul Wallenberg

Abstract on the topic:

"Nootropic drugs"

Completed by a student of group 05/14

"Clinical psychology"

Kulaeva Ya.E.

Nootropics……………………………………………………..3

Mechanisms of action……………………………………….....4

Effect……………………………………………………..6

Classification of nootropics…………………………………..7

4.1 according to their chemical composition…………………………….7

4.2 according to T. A. Voronina, S. B. Seredenin………………...9

4.3 Mixed classification……………………………10

General indications for the use of nootropics……………..12

Side effects……………………………………………………………..14

Complex preparations……………………………………………………….14

Known nootropics……………………………………………………14

Forms of release of drugs…………………………….15

Pharmacokinetics of nootropic drugs………………….16

Literature……………………………………………………..20

Nootropics (neurometabolic stimulants, neurodynamic, neuroregulatory, neurometabolic, eutotrophic, metabolite cerebroprotectors) are drugs intended to provide a specific effect on the higher integrative functions of the brain, stimulating learning and memory, improving mental activity, increasing the brain’s resistance to damaging factors, improving cortical subcortical connections. Recently, within the group of nootropics, a subgroup of neuroprotectors has been identified that have a protective, stabilizing effect on nervous tissue cells under unfavorable conditions.

Nootropics do not have a pronounced psychostimulating or sedative effect and do not cause specific changes in the bioelectrical activity of the brain. At the same time, they, to one degree or another, stimulate the transmission of excitation in central neurons, facilitate the transfer of information between the hemispheres of the brain, improve energy processes and blood supply to the brain, and increase its resistance to hypoxia. The most important manifestation of their action is the activation of intellectual and mnestic functions, antihypoxic activity. To increase physical performance, nootropics are effective only in combination with actoprotectors and psychostimulants or in weakened and asthenic individuals.

Nootropics do not have an independent class in the classification of drugs and are combined with psychostimulants into a separate pharmacotherapeutic group with the ATC code: N06BX.

The term "nootropics"(from the Greek words “noos” - thinking, reason and “tropos” - desire, affinity) was adopted in 1972. This happened after the appearance on the world market of the drug piracetam, synthesized in 1963 by Belgian pharmacologists K. Giurgea and V. Skondia, which was initially studied as an antikinetic agent. developed by the Belgian company UCB. In 1972, K. Giurgea found that after taking piracetam, learning processes, attention, and memory improve are facilitated. Nootropics have a characteristic stimulating effect on the evoked transcallosal potential and have additional antihypoxic activity and, unlike psychostimulants, do not have a negative effect on the body.

Unlike psychostimulants, stimulation of nerve cells with nootropics leads to increased activity and performance, which are not qualitative, but quantitative. The effect of most nootropics does not appear immediately after the first dose, as is observed with psychostimulants, but during long-term treatment.

Later, similar effects were noticed in other substances or complexes of substances. Nootropics are believed to increase the brain's resistance to a variety of harmful influences, such as excessive exercise or hypoxia.

Currently, more than 10 original nootropic drugs of the pyrrolidine series have been synthesized, which are in phase III clinical trials or have already been registered in a number of countries; among them are oxiracetam, aniracetam, etiracetam, pramiracetam, dupracetam, rolisiracetam, cebracetam, nefiracetam, isacetam, detiracetam. These nootropic drugs are collectively called racetams.

In addition, other families of nootropic drugs have been synthesized, including cholinergic, GABAergic, glutamatergic, and peptidergic. The nootropic component of action is also present in other classes of drugs that have different chemical origins.

Mechanisms of action

The mechanisms of action of nootropic drugs are considered to be the influence on metabolic and bioenergetic processes in the nerve cell and interaction with the neurotransmitter systems of the brain. It has been proven that nootropics activate adenylate cyclase and increase its concentration in the neuron. And an increased level of cyclic AMP leads, through a change in the flow of intracellular K+ and Ca2+ ions, to an accelerated release of serotonin from the sensory neuron. In addition, activated adenylate cyclase maintains the stability of ATP production in the cell without the participation of oxygen, and under hypoxic conditions it transfers brain metabolism to an optimally maintained mode. Manufacturers of neurometabolic stimulants claim that their drugs penetrate the BBB well, increase the rate of glucose utilization (especially in the cerebral cortex, subcortical ganglia, hypothalamus and cerebellum), improve the metabolism of nucleic acids, and activate the synthesis of ATP, protein and RNA.

The effect of a number of nootropics is mediated through neurotransmitter systems brain, among which the most important are:

- monoaminergic;

- cholinergic - phenotropil;

- glutamatergic(memantine and glycine act through NMDA receptors).

Nootropics, according to the companies that produce them, also have other effects, including:

- membrane-stabilizing: regulation of the synthesis of phospholipids and proteins in nerve cells, stabilization and normalization of the structure of cell membranes;

- antioxidant: inhibition of the formation of free radicals and lipid peroxidation of cell membranes;

- antihypoxic: decreased oxygen demand of neurons under hypoxic conditions;

- neuroprotective: increasing the resistance of nerve cells to the effects of adverse factors of various kinds.

A significant role is played by improving microcirculation in the brain by optimizing the passage of red blood cells through the microvasculature and inhibiting platelet aggregation. Nootropic effects can be caused by something else.

The complex effect of nootropic drugs improves the bioelectrical activity and integrative activity of the brain, which is manifested by facilitating the passage of information between the hemispheres, increasing the level of wakefulness, increasing the absolute and relative power of the EEG spectrum of the cortex and hippocampus, and increasing the dominant peak.

The declared increase in cortico-subcortical control, improvement of information exchange in the brain, positive impact on the formation and reproduction of a memory trace allow us to assert that these “medicines” lead to improved memory, perception, attention, thinking, increased learning ability, and activation of intellectual functions. The claimed, but unconfirmed, ability to improve cognitive functions has given rise to calling nootropic drugs “cognitive stimulants.”

Several mechanisms underlie the therapeutic action of nootropics:

Improving the energy state of neurons (increased ATP synthesis, antihypoxic and antioxidant effects);

Activation of plastic processes in the central nervous system due to increased synthesis of RNA and proteins;

Strengthening the processes of synaptic transmission in the central nervous system;

Strengthening the conduction of cholinergic impulses in the central nervous system (CNS);

Improved glucose utilization; accelerating the penetration of glucose through the blood-brain barrier and increasing its absorption by brain cells, especially in the cerebral cortex

Membrane stabilizing effect, stabilization of cell membranes (increased synthesis of phospholipids and proteins in neurons and red blood cells);

Inhibition of lysosomal enzymes;

Activation of cerebral microcirculation by improving the deformability of erythrocytes and preventing platelet aggregation;

Improvement of cortical-subcortical interaction;

Normalization of neurotransmitter disorders;

Activating effect on higher mental functions (memory, learning ability, etc.);

Improving reparative processes in case of brain damage of various origins.

Effect

Drugs are isolated from stimulating(piracetam, phenotropil, aminalon, pyriditol, etc.) and oppressive(phenibut, sodium hydroxybutyrate) type of action.

In the spectrum of clinical activity of nootropics, the following claimed main effects are distinguished:

Nootropic effect(impact on impaired higher cortical functions, level of judgment and critical capabilities, improvement of cortical control of subcortical activity, thinking, attention, speech).

Mnemotropic action(effect on memory, learning ability).

Increased level of wakefulness and clarity of consciousness(influence on the state of depressed and darkened consciousness).

Adaptogenic effect(impact on tolerance to various exogenous factors, including medications, increasing the body’s overall resistance to extreme factors).

Antiasthenic effect(effect on weakness, lethargy, exhaustion, mental and physical asthenia).

Psychostimulating effect(influence on apathy, hypobulia, spontaneity, poverty of motives, mental inertia, psychomotor retardation).

Antidepressant effect.

Sedative(tranquilizing) effect, reducing irritability and emotional excitability.

Vegetative action(effect on headache, dizziness, cerebrasthenic syndrome).

Antikinetic effect.

Antiparkinsonian action.

Antiepileptic effect, influence on epileptic paroxysmal activity.

Hypoglycemic effect(reduce the concentration of glucose in the blood).

Energy effect(by increasing the consumption of glucose by the body's cells), which is why it is effective in sports at various stages of recovery after training.

Somatotropin-stimulating effect(as a result of hypoglycemia, growth hormone is released).

Anabolic effect(insofar as they are amino acids, and anabolic and other hormones consist precisely of amino acid residues).

Lipolytic(fat-mobilizing or fat-burning) effect (in conditions of lack of glucose, fatty acids begin to be released as energy). Antiparkinsonian.

Antidiskinetic.

Antitoxic effect(by removing cell waste products from the body and neutralizing various harmful substances).

Immunostimulating effect(see anabolic effect leading to strengthening of the body).

General resultant actions for this group of drugs:

Improving thought processes - cognitive functions or cognitive processes (learning);

Improving the speed of memorization and storage strength of received information (memory);

Improving the reproduction of existing information, increasing intellectual activity, the volume of intellectual capabilities;

deterioration in retrieving from memory (forgetting) information about pain or stressful conditions;

Stimulation of metabolic processes in nervous tissue, especially in case of various disorders - anoxia, intoxication, injury, etc. (bringing the level of metabolism to the level of optimally functioning neurons);

lack of influence on higher nervous activity and the psyche of healthy people;

Improving the impact on higher nervous activity and mental state in case of functional or morphological disorders;

Increasing the resistance of brain thought processes to the effects of unfavorable factors of the external and internal environment (hypoxia, injuries, strokes).

The presence of a pronounced anabolic effect and an indirect positive effect on physical performance determines the advisability of using some drugs from the group of nootropics (piracetam, etiracetam, aminalone, sodium hydroxybutyrate, phenibut) in schemes for pharmacological support of sports activity.

Classification of nootropics

according to their chemical composition.

Pyrrolidone derivatives: piracetam, etiracetam, aniracetam, oxiracetam, pramiracetam, dupracetam, rolisiracetam, etc.

Diaphenylpyrrolidone derivatives: phenotropil.

Pyridoxine derivatives: pyritinol, biotredin.

GABA derivatives and analogues: gamma-aminobutyric acid (aminalone), nicotinoyl-GABA (picamilon), gamma-amino-beta-phenylbutyric acid hydrochloride (phenibut), hopantenic acid, calcium gamma-hydroxybutyrate (sodium hydroxybutyrate).

Cerebrovascular agents: ginkgo biloba.

Neuropeptides and their analogues: Noopept, Semax, Selank.

Amino acids and substances affecting the system of excitatory amino acids: glycine, biotredin.

2-mercantobenzimidazole derivatives: ethylthiobenzimidazole hydrobromide (bemityl).

Vitamin-like products: idebenone.

neuromodulators: phenotropil;

correctors of cerebrovascular disorders: nicergoline, vinpocetine, xanthinol nicotinate, vincamine, naftidrofuryl, cinnarizine;

general tonics and adaptogens: acetylaminosuccinic acid (known as "succinic acid"), ginseng extract, melatonin, lecithin.

psychostimulants: sulbutiamine;

antihypoxants and antioxidants: hydroxymethylethylpyridine succinate (Mexidol);

acephen and its derivatives.

Signs of nootropic activity are present in the pharmacodynamics of glutamic acid, memantine and levocarnitine.

In addition, the experiment showed the nootropic effect of a number of neuropeptides and their synthetic analogues (ACTH and its fragments, somatostatin, vasopressin, oxytocin, thyrotropin-releasing hormone, melanostatin, cholecystokinin, neuropeptide Y, substance P, angiotensin II, cholecystokinin-8, peptide analogues of piracetam, etc. ).

Currently, there are several classifications of nootropic drugs.

The classification of nootropics by chemical structure involves dividing them into the following groups.

Racetams- pyrrolidone derivatives: piracetam, etiracetam, aniracetam, oxiracetam, pramiracetam, dupracetam, rolisiracetam, etc.

Dimethylaminoethanol derivatives(acetylcholine precursors): deanol aceglumate, meclofenoxate.

Pyridoxine derivatives: pyritinol, biotredin.

Derivatives and analogues of GAM K:γ-aminobutyric acid (aminalone), nicotinoyl-GABA (picamilon), γ-amino-P-phenylbutyric acid hydrochloride (phenibut), hopantenic acid, pantogam, calcium γ-hydroxybutyrate (neurobutal).

Cerebrovascular agents: ginkgo biloba.

Neuropeptides and their analogues: semax.

Amino acids and substances affecting the system of excitatory amino acids: glycine, biotredin.

2-mercantobenzimidazole derivatives: ethylthiobenzimidazole hydrobromide (bemityl).

Vitamin-like products: idebenone.

Polypeptides and organic composites: cortexin, cerebrolysin, cerebramin.

Substances of other pharmacological groups with a nootropic component:

correctors of cerebral circulatory disorders - nicergoline, vinpocetine, xanthinol nicotinate, vincamine, naftidrofuryl, cinnarizine;

general tonics and adaptogens- acetylaminosuccinic acid (known as "succinic acid"), ginseng extract, melatonin, lecithin.

psychostimulants - salbutiamine;

antihypoxants and antioxidants- oxymethylethylpyridine succinate (Mexidol);

acephen and its derivatives.

Classification according to T. A. Voronina, S. B. Seredenin, 1998

1. Nootropic drugs with a dominant mnestic effect (cognitive enhancers).

1.1. Pyrrolidone nootropic drugs (racetams), predominantly of metabolite action (piracetam, oxiracetam, aniracetam, pramiracetam, etiracetam, dipracetam, rolisiracetam, nebracetam, isacetam, nefiracetam, detiracetam, etc.).

1.2. Cholinergic substances.

1.2.1. Activators of acetylcholine synthesis and its release (choline chloride, phosphatidyl-serine, lecithin, acetyl-L-carnitine, DUP-986, aminopyridine derivatives, ZK9346-betacarboline, etc.).

1.2.2. Agonists of cholinergic receptors (oxotremorine, bethanechol, pyropiperidines, quinonucleotides, etc.).

1.2.3. Acetylcholinesterase inhibitors (physostigmine, tacrine, amiridine, ertastigmine, galantamine, metrifonate, velnacrine maleate).

1.2.4. Substances with a mixed mechanism (demanol aceglumate, salbutamine, bifemelan, instenon).

1.3. Neuropeptides and their analogs (ACTH 1–10 and its fragments, ebiratide, somatostatin, Semax, vasopressin and its analogs, thyrotropin-releasing hormone and its analogs, neuropeptide Y, substance P, angiotensin-P, cholecystokinin-8, peptide analogs of piracetam (GVS-111 ), prolyl endopeptidase inhibitors).

1.4. Substances that affect the system of excitatory amino acids (glutamic acid, memantine, milacemide, glycerin, D-cycloserine, nooglutyl).

2. Mixed-type nootropic drugs with a wide range of effects

2.1. Activators of brain metabolism (actovegin, acetyl-L-carnitine, carnitine, phosphatidyl, serine, homopantothenic acid esters, xanthine derivatives of pentoxifylline, propentofylline, tetrahydroquinolines).

2.2. Cerebral vasodilators (instenon, vincamine, vinpocetine, oxybral, nicergoline, vinconate, vindebumol).

2.3. Calcium antagonists (niludipine, cinnarizine, flunarizine, etc.).

2.4. Antioxidants (mexidol, exiphon, pyritinol, tirilazad mesilate, meclofenoxate, atherovit (alpha-tocopherol and meclofenoxate), etc.).

2.5. Substances affecting the GABA system (gammalon, pantogam, picamilon, digam, nicotinamide, phenibut, phenotropil, sodium hydroxybutyrate, neurobutal, etc.).

2.6. Substances from different groups (etimizole, orotic acid, methyl glucoorotate, oxymetacyl, beglimin, naftidrofuryl, cerebrocrast, ginseng preparations, schisandra, ginkgo biloba extract, etc.).

More often a mixed classification of nootropic drugs is used, taking into account the origin, clinical effectiveness, breadth and mechanism of action. According to this classification, nootropic drugs are divided into two main groups:

Drugs with dominant or predominant mnestic effects (cognitive enhancers), the main effect is the effect on memory (mnestic)

1. Pyrrolidone derivatives, namely cyclic GAM K (racetams) - piracetam (nootropil), pramiracetam (pramistar), etiracetam, nefiracetam, aniracetam, phenotropil, etc.

2. Cholinergic drugs:

a) cholinesterase inhibitors - galantamine hydrobromide (Nivalin), rivastigmine (Exelon), donepezil, ipidacrine (Neuromidine), aminostigmine;

b) enhancing the synthesis of mediators - choline chloride, choline alphoscerate (gliatilin), lecithin, etc.;

c) M-, N-cholinomimetics - bethanechol;

d) substances with a mixed type of action - deanol aceglutamate.

3. Neuropeptides and their analogues - Semax, Cerebrolysin, Cerebrocurin, Actovegin, Solcoseryl, Thyroliberin.

4. Drugs affecting the excitatory amino acid system- glutamic acid, nooglutil.

5. Preparations of glycine and its derivatives - glycine, noopept .

II. Mixed drugs with a wide spectrum of action (neuroprotectors)

1. Brain metabolism activators - pentoxifylline, acetyl-L-carnitine.

2. Cerebral vasodilators - vinpocetine (Cavinton), oxybral (Vicamine), nicergoline (Sermion), etc.

3. Calcium antagonists- nimodipine, cinnarizine, flunarizine, etc.

4. Substances affecting the GAM K system - aminalon, membraton, pantogam, picamilon, sodium hydroxybutyrate, phenibut (noofen), etc.

5. Antioxidants - mexidol, pyritinol, a-tocopherol and etc.

6. Drugs from different groups- naftidrofuryl, etimizol, ginkgo biloba extract (tanakan, memoplant), melatonin, huato boluses, etc.

Although there is no single generally accepted classification of nootropics yet, these drugs include:

Piracetam, its homologues and analogues (aniracetam, oxiracetam, pramiracetam, nefiracetam, etc.);

Dimethylaminoethanol derivatives: deanolaceglumate, meclofenoxate, centrophenoxine;

Neuroamino acid preparations: gamma-aminobutyric acid (GABA), gamma-aminobutyric acid derivatives (phenibut, nicotinoyl-gamma-aminobutyric acid (picamilon), hopantenic acid (pantogam), glycine, glutamic acid;

Pyridoxine derivatives: pyritinol (pyriditol, enerbol, encephabol);

Centrally acting cholinomimetic: choline alfoscerate;

Ginkgo biloba preparations: bilobil, memoplant, tanakan, etc.;

Compounds of a different chemical structure, belonging to various classes and groups of chemical substances, similar in their mechanism of action to piracetam and having the ability to facilitate learning processes and improve memory.

Along with true nootropic drugs (with a dominant effect on mnestic functions), various authors classify drugs with a wide range of effects as nootropic drugs:

Drugs that enhance cerebral circulation, microcirculation and metabolism: vinpocetine, vincamine, vinconate, nicergoline, cinnarizine, flunarizine, nimodipine, xanthine derivatives of pentoxifylline, carnitine, phosphatidylserine, sodium oxybate; vitamins and their derivatives: pantothenic acid, folic acid, vitamin E;

Intermediate products of cell metabolism: orotic and succinic acids;

Combined drugs: instenon, omarone.

5. General indications for the use of nootropics are:

Cerebral ischemia (acute stage and rehabilitation period);

Traumatic brain injury (acute stage and rehabilitation period);

Coma;

Intellectual activity disorders in children suffering from delay

mental development in weak or moderate form;

Learning difficulties in children with attention deficit disorder;

Chronic fatigue syndrome;

Vegetative-vascular dystonia;

Alzheimer's disease;

Vascular dementia.

A feature of the use of nootropic drugs is the possibility of their use equally for both sick and healthy people in extreme situations, during natural aging, overwork, for “cover-up therapy” to relieve severe “withdrawal syndrome”, as well as anti-alcohol drugs that accelerate recovery from a delirious state and improve the course of a post-delirious state.

Prof. G.V. Kovalev (1990) said that “... the nootropic is addressed to the mind, which is extinguished either due to pathological processes or due to stress caused by physical, chemical (including alcohol), biological or social factors, acting on the human body." In foreign literature, the term “cognitive function enhancer” is sometimes used as a synonym for nootropic drugs. Along with the direct effect on mnestic functions, many nootropic drugs are used to reduce the general level of human activity that occurs under various extreme influences and diseases.

Application in sports medicine and sports training practice

For brain injuries;

To increase concentration;

In case of cerebrovascular disorders during or after training sessions, competitions;

For dizziness;

To prevent motion sickness;

For recovery (rehabilitation) treatment, after competitions, training with heavy loads.

Some nootropics are used for:

Correction of neuroleptic syndrome (deanol aceglumate, pyritinol, pantogam, hopantenic acid),

Stuttering (phenibut, pantogam), hyperkinesis (phenibut, hopantenic acid, memantine),

Urinary disorders (nicotinoyl-GABA, pantogam),

Sleep disorders (glycine, phenibut, calcium gamma-hydroxybutyrate),

Migraines (nicotinoyl-GABA, pyritinol, Semax),

Dizziness (piracetam, phenibut, ginkgo biloba)

To prevent motion sickness (phenibut, GABA).

In ophthalmology for open-angle glaucoma, vascular diseases of the retina and macula, age-related macular degeneration, diabetic retinopathy.

Nootropic drugs are used in Russia for the following conditions:

Psychoorganic syndromes (vascular, traumatic, infectious, intoxication, somatic origin);

Acute vascular pathology; chronic alcoholism;

Epilepsy;

Chronic, treatment-resistant depressive conditions;

Neurotic reactive somatogenic states; schizophrenia;

Correction of learning disabilities in children and adults

dementia of various origins (vascular, senile, Alzheimer's disease),

Chronic cerebrovascular insufficiency,

Psychoorganic syndrome,

With the consequences of cerebrovascular accident, traumatic brain injury,

intoxication,

Neuroinfections,

For intellectual-mnestic disorders, asthenic, asthenic-depressive and depressive syndrome,

For neurotic and neurosis-like disorders,

With vegetative-vascular dystonia,

For chronic alcoholism (encephalopathy, psychoorganic syndrome, abstinence),

And also to improve mental performance.

In pediatrics, indications for prescribing nootropics are:

Delayed mental and speech development,

Mental retardation,

Consequences of perinatal CNS damage,

Cerebral palsy,

Attention deficit disorder.

Nootropic (lat. Pose - mind and thropos - kinship) drugs, due to their beneficial effect on the metabolic processes of the brain, improve mental and mental activity, which is impaired in pathological conditions. The term "nootropic drugs" was proposed in 1972 by C. Jurgea, the author of the nootropic drug piracetam. These drugs do not affect a healthy body, do not change conditioned reflexes and behavior, bioelectrical and motor activity. Nootropic drugs are divided into the following groups:

1. Pyrrolidone derivatives (racetams): piracetam, phenotropil, pramiracetam, Thiocetam, etc.

2. GABA derivatives: aminalon, sodium hydroxybutyrate, picamilon, etc.

3. Derivatives of other amino acids: glutamic acid, glycized, etc.

4. Neuropeptides and their analogues: Semaxa, Noopept, etc.

5. Cerebral vasodilators: vinpocetine, nicergoline, vincamine (oxybral), pentoxifylline, etc.

6. Antioxidants of direct and indirect action: Mexidol, Cerebrolysin, Actovegin, Solcoseryl, melatonin, ginkgo biloba, etc.

7. Cholinergic drugs:

7.2. Anticholinesterase: galantamine hydrobromide, etc.

8. calcium antagonists: nimodipine, cinnarizine, etc.

9. Drugs of different groups: xanthinol nicotinate, etc.

Mechanism of action of nootropics:

1. Excitation of glutamic acid receptors, which perceive signals from memory peptides.

2. Increased synthesis, turnover of ATP, phosphatidylcholine.

3. Activation of protein and RNA synthesis.

4. Improved glucose utilization.

5. Stimulation of adenylate cyclase, accumulation of cAMP.

6. Activation of glycolysis and aerobic respiration.

7. Increased activity of phospholipase A, inhibition of Na + K + ATPase.

8. Suppression of free radical processes, lipid peroxidation, membrane stabilization.

9. Increased activity of the cholinergic system.

10. Dilation of cerebral vessels, improvement of cerebral circulation, rheological parameters.

Properties of the drugs:

1) have a mnestic effect, improve memory, learning ability:

2) increase the brain’s resistance to extreme influences;

3) may have a psychostimulant (glutamic acid) or sedative (tranquilizing) effect (glycine)

4) exhibit antiasthenic effect;

5) some drugs may have antidepressant, antiepileptic, antiparkinsonian, vasovegetative, adaptogenic, stress-protective, cardioprotective effects, and improve the rheological properties of blood.

The main representative of nootropic drugs is piracetam (nootropil). According to its chemical structure, it is a cyclic composition of GABA.

Pharmacokinetics. Piracetam is well absorbed, does not bind to blood proteins, and penetrates the blood-brain barrier and the blood-placental membrane barrier. The drug accumulates in the tissues of the cerebral cortex, cerebellum, and basal ganglia. Piracetam is not metabolized in the body, 80-90 % The drug is excreted unchanged by the kidneys by renal filtration.

Pharmacodynamics. The drug improves mental activity, memory, learning ability, etc. Integrative processes caused by piracetam and other nootropics are associated with its effect on glutamate receptors. The antitoxic effect is due primarily to the effect on energy metabolism. Piracetam improves the absorption of glucose, the metabolism of adenosine triphosphate, phosphatidylethanolamine, phosphatidylcholine, increases the activity of adenylate cyclase, phospholipase, tissue resistance to oxygen deficiency, suppresses the activity of nucleoside phosphatase, stimulates RNA synthesis and blood circulation in brain tissue. It has antioxidant and antihypoxic effects. Piracetam is low-toxic, has adaptive properties, anticonvulsant, cardioprotective effects, does not have a sedative effect, and has a significant antidepressant effect.

Indications: decrease in mental function associated with chronic degenerative lesions of the brain (senile age, alcoholism, hemiplegia, stroke, skull injuries, asthenic syndrome), correction of the side effects of tranquilizers in preparation for operations and other manipulations of persons with asthenic syndrome, the elderly, children. Piracetam combines well with cardiovascular and psychotropic drugs, potentiates the effect of antidepressants, it is combined with cinnarizine and orotic acid.

Side effect dyspepsia, irritability, sleep disturbance.

Pramiracetam (Pramistar) unlike piracetam, it has a high affinity for choline and acts in the cholinergic structures of the brain, does not have a sedative effect, but has a pronounced antidepressant effect.

Fenotropil increases the content of norepinephrine, serotonin, dopamine in brain tissue, does not affect the content of GABA, does not bind to GABA and GABAB receptors, stimulates redox processes, increases energy potential due to the utilization of glucose, increases regional blood flow in ischemic areas of the brain. Phenotropil has a moderate effect on enhancing physical performance and antagonizes the cataleptic effects of neuroleptics. A moderately pronounced psychostimulating effect is combined with anxiolytic activity. The drug improves mood, has an analgesic, adaptogenic, and stress-protective effect. When taking phenotropil, visual acuity increases, the drug improves blood supply to the lower extremities, and exhibits a diuretic effect. The drug promotes the formation of antibodies without developing an allergenic effect.

GABA is γ-aminobutyric acid.

GABA (GABA), unlike previous drugs, does not pass through the blood-brain barrier, but improves energy processes, glucose utilization, oxygen consumption, improves blood circulation, and the dynamics of nervous processes. May cause bradycardia and hypotension.

Pharmacodynamics. GABA improves blood circulation in the brain, has anticonvulsant and antihypoxic properties, and due to the normalization of GABA levels, blood pressure decreases, especially in conditions of arterial hypertension. The drug causes bradycardia, exhibits a mild psychostimulant effect, and in cases of elevated blood glucose levels has a hypoglycemic effect.

Indications: memory loss after injury, stroke, infectious diseases, arterial hypertension, paralysis, complications of cerebral atherosclerosis, cerebrovascular accident, headache, insomnia, dizziness, polyneuritis, mental retardation in children.

Side effect dyspepsia, sleep disorders, feeling of heat, hypotension, bradycardia.

Vinpocetine (Cavinton) - ethyl ester of apovincamine acid is a semi-synthetic derivative compound of the alkaloid devincan, a white vinca alkaloid.

Pharmacodynamics. Dilates cerebral and peripheral vessels, stimulates cerebral circulation, increases oxygenation of brain tissue, and glucose uptake. Reduces platelet aggregation, inhibits phosphodiesterase, increases cAMP levels, modulates ion channels, affects norepinephrine metabolism.

Indications: neurological diseases associated with cerebrovascular accidents, memory impairment, aphasia, menopausal syndrome, eye diseases (atherosclerotic and angiospastic changes in the retina, choroid, secondary glaucoma, degenerative eye diseases), hearing loss of vascular or toxic origin; dizziness.

Side effect slight arterial hypotension, extrasystole.

Nicergoline (sermion)- belongs to the group of α-adrenergic blockers.

Pharmacodynamics. Significantly reduces the tone of cerebral and peripheral vessels, reduces cerebrovascular resistance, increases cerebral circulation, and activates metabolism in brain tissue. Increases the supply of oxygen and glucose to brain tissue, the speed of blood circulation in the vessels of the extremities, and reduces the resistance of pulmonary vessels. Nicergoline causes a gradual decrease in blood pressure in patients with arterial hypertension.

Indications: atherosclerosis of cerebral vessels, thrombosis and embolism of cerebral vessels, transient cerebrovascular accidents, obliterating endarteritis, Raynaud's syndrome, migraine, hypertensive crisis.

Side effect dizziness, drowsiness, insomnia, fever, flushing of the face.

Pentoxifylline (trental) is an antispasmodic.

Pharmacodynamics. Blocks phosphodiesterase, competes with adenosine for receptors and promotes the accumulation of cAMP. Provides brain tissue with oxygen, improves microcirculation and rheological properties of blood, reduces platelet aggregation, increases the elasticity of red blood cells, and blocks the release of cytokines.

Indications: brain diseases, including atherosclerosis of cerebral vessels, coronary heart disease, condition after myocardial infarction, diabetic myopathy, nephroangiopathy; peripheral circulatory disorders, vascular pathology of the eyes (acute and chronic insufficiency of blood supply to the retina and choroid), functional hearing impairment.

Side effect nausea, vomiting, gastralgia, dizziness, facial skin flushing, decreased blood pressure with parenteral administration, itching, urticaria.

Thiocetam, containing thiotriazoline and piracetam, has nootropic, anti-ischemic, antioxidant, membrane-stabilizing properties. The drug oxidizes glucose in aerobic and anaerobic oxidation reactions, normalizes bioenergetic processes, ATP levels, stabilizes other types of metabolism, has an antioxidant effect during ischemia, improves the rheological properties of blood by activating the fibrinolytic system. Thiocetam increases the intensity of the metabolic GABA shunt and the concentration of GABA in ischemic tissues. The drug improves integrative and cognitive activity of the brain, promotes the learning process, eliminates amnesia and the effects of stress.

Indications: disorders of cerebral circulation caused by atherosclerosis of cerebral vessels, metabolic disorders as a result of traumatic brain injury, intoxication, diabetic encephalopathy.

Side effect general weakness, headache, anxiety, dizziness, hallucinations, nausea, vomiting, abdominal pain and weight gain, allergic reactions (rash, fever, anaphylactic shock, angioedema, suffocation).

Fezama (Omaron) contains piracetam and cinnarizine, improves blood circulation, metabolism of neurons of the visual and auditory analyzers, restores their function.

Olatropil- a combination of γ-aminobutyric acid and piracetam, promotes regulation between the processes of excitation and inhibition due to the content of GABA, regulates blood circulation and metabolism.

Noofen (phenibut)- a derivative of GABA and phenylethylamine. The main effects are antihypoxic and anti-anamnestic effects. The drug has a tranquilizing effect, but stimulates memory and the learning process, eliminates psycho-emotional stress, fear, and anxiety.

Picamilon, which is a combination of GABA and nicotinic acid, penetrates the blood-brain barrier. The drug has a significant vasodilating effect, improves cerebral circulation and, thanks to nicotinic acid, has a hypolipidemic effect, which can be useful for cerebral atherosclerosis. However, picamilon is prescribed with caution to persons who are hypersensitive to nicotinic acid.

Tanakan(liquid extract of the Ginkgo biloba plant) - vasodilator, vasoregulator, neuroprotector, antihypoxant, antiplatelet agent.

Indications: encephalopathy, traumatic brain injury, decreased intelligence.

Side effect dyspepsia, headache, allergic reactions.

Actovegin- hemoderivative from the blood of deproteinized calves, containing physiologically active substances with a molecular weight of less than 5000 Da. The drug helps reduce the utilization of oxygen and glucose by brain tissue, activates energy metabolism and therefore increases the resistance of neurons, as well as other tissues, to hypoxia and ischemia.

Indications: metabolic and circulatory disorders of the central nervous system - ischemic stroke, residual effects after hemorrhagic stroke, traumatic brain injury, encephalopathy, peripheral circulatory disorders, I-III degree burns, radiation damage to the skin, mucous membranes, radiation neuropathy.

Side effects: hypersensitivity phenomena (urticaria, flushing, increased body temperature, anaphylactic shock).

Solcoseryl- standardized deproteinization dialysate from the blood of dairy calves. The drug activates tissue metabolism, improves trophism, and accelerates regeneration. Solcoseryl affects aerobic processes and oxidative phosphorylation, activates collagen synthesis, cell proliferation and migration.

Indications: metabolic and circulatory disorders of the brain (ischemic and hemorrhagic stroke, traumatic brain injury). The drug can be prescribed for chronic venous insufficiency with trophic disorders if they last for a long time.

Side effect urticaria, increased body temperature, hyperemia, swelling at the injection site.

Cerebrolysin- proteolytic fraction from pig brain, stimulates differentiation, improves neuronal function, activates metabolic processes, reduces the volume of brain tissue infarction, edema, stabilizes microcirculation, improves cognitive functions.

Indications: organic, metabolic disorders and neurodegenerative diseases of the brain, vascular dementia and Alzheimer's disease, brain injuries, condition after neurosurgical intervention, strokes, complications after stroke, mental retardation.

Side effects action: hypersensitivity phenomena, rarely insomnia, depression, agitation, dizziness, tremor, headache, seizures, blood pressure fluctuations, hypertension, hyperventilation, loss of appetite, dyspepsia, nausea, vomiting.

Cerebrocurin- peptide regulator of the central nervous system, contains amino acids, peptides and low molecular weight products of proteolysis of proteins in the brain of cattle embryos. The drug activates the protein-activating function of nerve cells, increases the functional activity of the synaptic apparatus of neurons, increases the diameter and area of ​​mitochondria, restores myelin sheaths, improves arterial and venous cerebral circulation, has vasoactive, neuroprotective, hepatoprotective, anabolic effects, stabilizes the nootropic effect.

Indications: diseases of the central nervous system, vegetative-vascular dysfunction, chronic, ischemic, discirculatory and post-traumatic encephalopathies, residual effects after a stroke.

Side effect phenomena of hypersensitivity to the components of the drug.

Glycised (glycine)- amino acid, is an inhibitory neurotransmitter, has a sedative effect, improves metabolic processes in brain tissue.

Indications: as part of complex pharmacotherapy for cerebrovascular disorders, decreased tendency to alcohol, depression, increased irritability.

Side effect hypersensitivity phenomena.

Neurorubin(B1; B6; 12) - a multivitamin preparation containing B vitamins, regulates protein, lipid, carbohydrate metabolism, supports vital functions.

Indications: toxic reactions due to alcohol poisoning, acute and chronic neuritis, polyneuropathy, toxic lesions of the central nervous system, neurotic pain due to neuritis and polyneuritis, diabetic polyneuropathy.

Side effect hypersensitivity phenomena, angioedema is possible.

Mexidol- a derivative of oxypyridine and succinic acid. It has antioxidant, antihypoxic, membrane-stabilizing, nootropic, anxiolytic effects, has a stress-protective, anticonvulsant, hypolipidemic effect, and prevents learning and memory disorders. The drug stabilizes the membranes of platelets and red blood cells, improves the rheological properties of blood, blood supply to the brain, microcirculation, and activates metabolism. The drug enhances the activation of aerobic glycolysis, oxidative processes in the Krebs cycle during hypoxia, increases the level of ATP, creatine phosphate, the energy function of mitochondria, inhibits lipid peroxidation, modulates the activity of membrane-bound enzymes (adenylate cyclase, etc.), receptor complexes (benzodiazepine, etc.), enhances communication with ligands, improves the transport of mediators, increases the content of dopamine, reduces cholesterol, low-density lipoproteins. Increases the body's resistance to damaging factors (alcohol intoxication, neuroleptics), hypoxia, reduces the manifestations of toxemia, endogenous intoxication in acute pancreatitis.

Indications: acute cerebrovascular accidents, dyscirculatory encephalopathy, vegetative-vascular dysfunction, cognitive disorders of atherosclerotic origin, anxiety disorders in neurotic conditions, withdrawal syndrome in alcoholism, acute intoxication with antipsychotic drugs, acute pancreatitis, peritonitis (in complex therapy).

Side effect nausea, dry mouth, drowsiness.

Naftidrofuryl- a vasodilator, reduces overall peripheral vascular resistance, activates tissue metabolism, tissue oxygen supply, promotes glucose utilization, increases ATP formation.

Indications: ischemic stroke, presenile disorders, recovery period after stroke, trauma, Meniere's disease, ischemic lesions of the retina, disorders of the blood supply to the inner ear, pain in the limbs, paresthesia, diabetic neuropathy, wound healing disorders and the like.

Side effect insomnia, rash, anxiety, dizziness, headache, hypotension, orthostatic collapse, cardiac arrhythmias, hepatitis.

The majority of the population of our planet, especially residents of large cities, are forced to live in conditions of constant environmental and psycho-emotional stress. It has been proven that stress is not harmless to the human body, it is a risk factor for many, and also has a negative effect on the nervous system, as a result of which a person becomes irritable, his performance decreases, his memory and thinking processes deteriorate. In this regard, scientists are continuously searching for ways to prevent and correct the negative effects of stress on the nervous system. About 50 years ago, the concept of nootropic drugs arose, Piracetam was synthesized and tested. This gave a powerful impetus to the search and creation of other substances with a similar principle of action; these studies continue to this day.

From this article, the reader will get an idea of ​​what nootropics are and what effects they have, get acquainted with the indications, contraindications, side effects of these drugs in general, and also learn the characteristics of individual representatives of drugs in this group, in particular new generation nootropics. Let's begin.

What are nootropics

According to the definition of the World Health Organization, nootropic drugs are drugs that have an activating effect on learning, improve mental activity and memory, and increase the resistance (stability) of the brain to such aggressive influences as injury, intoxication, and hypoxia.

The first nootropic in history is Piracetam, which was synthesized and used clinically by Belgian pharmacologists back in 1963. During the study, scientists found that this medicinal substance significantly increases mental performance, improves memory and promotes learning. Subsequently, other drugs with similar effects were synthesized, which we will discuss below.

Effects and mechanisms of action of nootropic drugs

The main effects of drugs in this group are:

• psychostimulant;
• sedative;
• anti-asthenic (reducing feelings of weakness, lethargy, mental and physical asthenia);
• antidepressant;
• antiepileptic;
• actually nootropic (impact on impaired higher cortical functions, which is manifested by improved thinking, speech, attention, and so on);
• mnemotropic (effect on learning and memory);
• adaptogenic (increasing the body’s ability to resist harmful environmental influences);
• vasovegetative (improved blood supply to the brain, which is manifested by a decrease and, as well as the elimination of other autonomic disorders);
• antidiskinetic;
• increasing clarity of consciousness and level of wakefulness.

These drugs do not cause pharmacological dependence and psychomotor agitation; taking them does not deplete the physical capabilities of the body.

The action of drugs in this group is based on the following processes:

• activation of plastic processes in the central nervous system by enhancing the synthesis of proteins and RNA;
• activation of energy processes in neurons;
• activation of the processes of transmission of nerve impulses in the central nervous system;
• optimization of polysaccharide utilization processes, in particular glucose;
• inhibition of the formation of free radicals in cells;
• decreased oxygen demand of nerve cells under hypoxic conditions;
• membrane-stabilizing effect (regulate the synthesis of proteins and phospholipids in nerve cells, stabilize the structure of cell membranes).

Nootropic drugs activate the enzyme adenylate cyclase, increasing its concentration in nerve cells. This substance is necessary to maintain the stability of the cell’s production of the main source of energy for biochemical and physiological processes - adenosine triphosphoric acid, or ATP, which, moreover, under hypoxic conditions, transfers metabolism in the brain to an optimally maintained mode.

In addition, nootropics affect the neurotransmitter systems of the brain, in particular:

• monoaminergic (increase the content of dopamine and norepinephrine, as well as serotonin in the brain);
• cholinergic (increase the content of acetylcholine in nerve endings, necessary for adequate transmission of impulses from cell to cell);
• glutamatergic (also improve signal transmission from neuron to neuron).

As a result of all the effects described above, the patient’s memory, attention, mental processes and perception processes improve, his ability to learn increases, and intellectual functions are activated.

Classification of nootropics

The class of nootropic drugs includes substances of various pharmacological groups that have a positive effect on the functioning of nerve cells and improve their structure.

1. Substances that stimulate metabolic processes in nerve cells:

• pyrrolidone derivatives: Piracetam, Pramiracetam, Phenylpiracetam and others;
• derivatives of gamma-aminobutyric acid (GABA): Aminalon, Picamilon, Hopanthenic acid, Phenibut;
• pantothenic acid derivatives: Pantogam;
• derivatives of vitamin B6 - pyridoxine: Pyritinol;
• products containing dimethylaminoethanol: Acefen, Centrophenoxin;
• preparations containing neuroaminoxylates and peptides: Glycine, Cerebrolysin, Actovegin;
• antihypoxants: Oxymethylethylpyridine succinate;
• vitamins, vitamin-like, general tonic substances: vitamin B15, vitamin E, folic acid, succinic acid, ginseng extract and others.

1. Drugs that have a positive effect on blood vessels, or vasotropic drugs:

• Xanthinol nicotinate;
• Vinpocetine;
• Pentoxifylline;
• Cinnarizine;
• Instenon.

1. Drugs that stimulate memory and learning processes:

• cholinomimetics and anticholinesterases: Galantamine, Choline, Amiridin and others;
• hormones: Corticotropin, adrenocorticotropic hormone;
• endorphins, enkephalins.

Indications for the use of nootropics

Medicines of the nootropic class are used to treat the following diseases:

• of various nature (vascular, senile);
• chronic cerebral vascular insufficiency;
• consequences of cerebrovascular accident;
• neuroinfections;
• intoxication;
• psychoorganic syndrome with symptoms of memory impairment, decreased concentration and general activity;
• cortical myoclonus;
• dizziness, with the exception of dizziness of vasomotor and mental origin;
• chronic alcoholism (for the purpose of treating encephalopathy, withdrawal and psychoorganic syndromes);
• reduced mental performance;
• astheno-depressive, depressive, astheno-neurotic syndromes;
• neurosis-like disorders;
• traumatic brain injury;
• hyperkinesis;
• sleep disorders;
• migraine;
• in the complex treatment of open-angle glaucoma, retinal vascular diseases, diabetic retinopathy, as well as age-related macular degeneration.

In pediatric practice, nootropics are used to treat the following conditions:

• mental retardation;
• delayed mental development and speech development;
• cerebral palsy;
• consequences of damage to the central nervous system during childbirth;
• attention deficit disorder.

Contraindications to taking nootropics

Medicines in this group should not be taken in the following cases:

• in case of individual hypersensitivity of the patient’s body to the active substance or other components of the drug;
• in case of an acute period of hemorrhagic stroke (bleeding in brain tissue);
• with Gettington's chorea;
• in case of severe renal impairment (if creatinine clearance is less than 20 ml/min);
• during pregnancy and lactation.

Side effects of nootropics

Medicines in this group rarely cause any side effects, however, some patients may experience the following undesirable reactions while taking them:

• headache, irritability, anxiety, sleep disturbances, drowsiness;
• rarely, in elderly patients, increased symptoms of coronary insufficiency;
• nausea, stomach discomfort, or;
• increased psychopathological symptoms;

Brief description of drugs

Since there are actually quite a lot of medicines belonging to the class of drugs we are describing, we will not be able to consider all of them, but we will only talk about those that are most widely used in medical practice today.

Piracetam (Piracetam, Lucetam, Biotropil, Nootropil)

Available in the form of tablets for oral administration and solution for injections and infusions.

The drug has a positive effect on blood circulation and metabolic processes in the brain, resulting in increased resistance of brain tissue to hypoxia and the effects of toxic substances, as well as improved memory, integrative brain activity, and increased learning ability.

When taken orally, it is well absorbed from the gastrointestinal tract, the maximum concentration in the blood is determined after 1 hour. Penetrates into many organs and tissues, including through the blood-brain and placental barriers. The half-life is 4 hours. Excreted by the kidneys.

Routes of drug administration: orally or parenterally (intramuscular or intravenous). It is recommended to take the tablets before meals. The dosage and duration of treatment are determined individually, depending on the disease and the characteristics of its clinical course.

When treating patients suffering from, caution should be exercised and the dose adjusted depending on the level of creatinine clearance.

Side effects of the drug are standard, and they usually occur in elderly and senile patients, provided they receive a dosage of more than 2.4 g of piracetam per day.

It has an effect on platelet aggregation, therefore it is used with caution in persons suffering from hemostasis disorders and a tendency to hemorrhage.

Contraindicated during pregnancy and lactation.

If sleep disturbances develop while taking piracetam, you should stop taking it in the evening and add this dose to the daytime dose.

Pramiracetam (Pramistar)

Release form: tablets.

Has a high degree of affinity for choline. Improves learning ability, memory and mental performance in general. Does not have a sedative effect and does not affect the autonomic nervous system.

Absorbed from the gastrointestinal tract quickly and almost completely, the maximum concentration of the active substance in the blood is determined after 2-3 hours. The half-life is 4-6 hours. Excreted by the kidneys.

During pregnancy and lactation, taking Pramistar is contraindicated.

When treating patients with impaired renal function, you should carefully monitor the development of side effects of the drug in them - this will be a sign of an excess of the active substance in the body and require a dose reduction.

Vinpocetine (Cavinton, Neurovin, Vinpocetine, Vicebrol)

Available in the form of tablets and solution for infusion.

Improves microcirculation in the brain, increases cerebral blood flow, and does not cause the “steal” phenomenon.

When taken orally, it is absorbed by 70% of the digestive tract. The maximum concentration in the blood is determined after 60 minutes. The half-life is almost 5 hours.

It is used both in neurology (for chronic cerebrovascular accidents and other diseases described in the general part of the article), and in ophthalmology (for the treatment of chronic retinal vascular diseases) and in otiatrics (to restore hearing acuity).

If therapy is started in the acute period of the disease, vinpocetine should be administered parenterally, and then continued orally at a dose of 1-2 tablets three times a day after meals.

Phenibut (Bifren, Noofen, Noobut, Phenibut)

Release form: tablets, capsules, powder for the preparation of oral solution.

The dominant effects of this drug are antihypoxic and antiamnestic. The drug improves memory, increases mental and physical performance, and stimulates learning processes. In addition, it eliminates anxiety, fear, psycho-emotional stress, and improves sleep. Strengthens and prolongs the effect of sleeping pills, anticonvulsants and antipsychotics. Reduces manifestations of asthenia.

After oral administration, it is well absorbed and penetrates into all organs and tissues of the body, in particular through the blood-brain barrier.

It is used for decreased emotional and intellectual activity, concentration, memory impairment, asthenic, anxiety-neurotic and neurosis-like conditions, insomnia, Meniere's disease, as well as for the prevention of motion sickness. In the complex treatment of preliriious and delirious alcoholic conditions, osteochondrosis of the cervicothoracic spine, menopausal disorders.

It is recommended to take 250-500 mg orally, before meals, three times a day. The maximum daily dose is 2.5 g, the maximum single dose is 750 mg. Duration of therapy is from 4 to 6 weeks.
In different clinical situations, the dosage regimen may vary.

It has an irritating effect, so it is used with caution in people suffering.

Hopanthenic acid (Pantogam)

Available in tablet form.

Reduces motor excitability, normalizes behavioral reactions, increases performance, and activates mental activity.

Rapidly absorbed from the gastrointestinal tract. The maximum concentration of the active substance in the blood is determined 60 minutes after administration. Creates high concentrations in the kidneys, liver, stomach wall and skin. Penetrates the blood-brain barrier. It is eliminated from the body after 2 days.

Indications are standard.

Take the drug orally, half an hour after eating. A single dose for adults is 250-1000 mg. Daily dose – 1.5-3 g. Course of treatment – ​​1-6 months. After 3-6 months you can repeat the course. When treating different diseases, the dose of the drug may vary.

Contraindications and side effects are described above.

Pyritinol (Encephabol)

Available in the form of tablets and suspension for oral use (this dosage form is intended for children).

It has a pronounced neuroprotective effect, stabilizes neuronal membranes, reduces the number of free radicals, and reduces red blood cell aggregation. Positively affects behavioral and cognitive functions.

If the drug dosage regimen is followed, the development of side effects is unlikely.

Glycine (Glycine, Glycised)

Release form: tablets.

Improves metabolism in muscles and brain tissue. Has a sedative effect.

Use sublingually (dissolving under the tongue).

To treat depression, anxiety and irritability, take glycine 0.1 g 2-4 times a day. For chronic alcoholism, it is prescribed according to recommended treatment regimens.

Contraindications: hypersensitivity to glycine. Side effects are not described.

Cerebrolysin

Release form: solution for injection.

Improves the function of nerve cells, stimulates their differentiation processes, activates protection and recovery mechanisms.

Penetrates the blood-brain barrier.

It is used for metabolic, organic and neurodegenerative diseases of the brain, in particular, and is also used in the complex treatment of strokes and traumatic brain injuries.

Daily doses of the drug vary widely depending on the pathology and range from 5 to 50 ml. Routes of administration: intramuscular and intravenous.

Use with caution to treat patients with allergic diathesis.

Actovegin

Release form: tablets, solution for injections and infusions.

Contains exclusively physiological substances. Increases the brain's resistance to hypoxia and accelerates the processes of glucose utilization.

It is used for ischemic and residual effects of hemorrhagic stroke, traumatic brain injury. Widely used for the treatment of diabetic polyneuropathy, burns, peripheral circulatory disorders, as well as for trophic disorders in order to accelerate wound healing processes.

As a rule, it is well tolerated. In some cases, the reactions described at the beginning of the article develop.

Approved for use during pregnancy and lactation.

Contraindicated in case of individual hypersensitivity to the components of the drug.

Contains sucrose, so it is not used in patients with hereditary disorders of carbohydrate metabolism.

Hexobendine (Instenon)

Available in the form of tablets for oral administration and solution for intramuscular and intravenous administration.

It has a stimulating effect on metabolic processes in the brain and myocardium, improves cerebral and coronary circulation. Antispasmodic.

Indications for the use of this drug are diseases of the brain of an age-related and vascular nature, the consequences of insufficient blood supply to the brain, dizziness.

Contraindicated in case of individual sensitivity to the components of the drug, increased intracranial pressure, epileptiform syndromes. During pregnancy and lactation it is used exclusively according to indications.

It is recommended to take orally during or after meals, without chewing, with plenty of water. The dosage is 1-2 tablets three times a day. The maximum daily dose is 5 tablets. The duration of treatment is at least 6 weeks.

The injection solution is administered intramuscularly, slowly intravenously or by drip. The dosage depends on the characteristics of the clinical course of the disease.

During treatment with this drug, you should not drink tea and coffee in large quantities. If the drug is administered intravenously, only a slow infusion is allowed, and the intravenous injection should last at least 3 minutes. Rapid administration of the drug can lead to a sharp decrease in blood pressure.

Combination drugs

There are many drugs that contain 2 or more components that are similar in action or mutually enhance the effects of each other. The main ones are:

• Gamalate B6 (contains pyridoxine hydrochloride, GABA, gamma-amino-beta-hydroxybutyric acid, magnesium glutamate hydrobromide; prescribed for adults in the complex treatment of functional asthenia; recommended to take 2 tablets 2-3 times a day for 2-18 months);
• Neuro-norm (contains piracetam and cinnarizine; indications are standard for nootropics; dosage – 1 capsule three times a day for 1-3 months; take the tablet after meals, do not chew, drink plenty of water);
• Noozom, Omaron, Fezam, Cinatropil, Evriza: drugs similar in chemical composition and other indicators to Neuro-norm;
• Olatropil (contains GABA and piracetam; recommended for use before meals, 1 capsule 3-4, maximum 6 times a day for 1-2 months; if necessary, the course can be repeated after 1.5-2 months);
• Thiocetam (includes piracetam and thiotriazoline; it is recommended to take 1-2 tablets three times a day; the course of treatment is up to 30 days; in some cases it is used in the form of an injection solution: 20-30 ml of the drug is administered intravenously in 100- 150 ml of saline solution or 5 ml intramuscularly once a day for 2 weeks).

So, above you got acquainted with the most popular nootropic drugs today. Some of them are the first drugs of this class, but many were developed much later and are much more effective, so they can safely be called new generation nootropics. Please note that the information provided in the article is not a guide to action: if you experience any unpleasant symptoms, you should not self-medicate, but rather seek help from a specialist.