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Nootropics Pharmacology. Nootropic preparations of a new generation. According to their chemical composition

Volgograd State Medical University

Department of Pharmacology

according to Pharmacology

Pharmacology and application of nootropic agents

Performed

Higina Olga

group, 3 course

Pharmaceutical Faculty

Volgograd 2011 year

Definition and history of the emergence of nootropic agents

Classification of Nootropov

The mechanism of action and the basic effects of nootropic agents

Application of nootropics in medical practice

Conclusion

List of sources of information

Definition and history of the emergence of nootropic agents

By definition of the World Health Organization, nootropics, they are neurometabolic stimulants - it is medicinal productscapable of rendering direct activating effect on learning processes, improve memory and mental activity, as well as increase the stability of the brain to aggressive impacts. The term "nootropic" is made up of Greek. νους - mind I. τροπή - spoil, prevent, modify. In the chemical structure, most of nootropics are amino acids or their derivatives (including peptides).

The first of nootropov - piracetam was synthesized in Belgium in 1963. Based on the fact that piracetam is a cyclic analogue of the main brake mediator nervous system GABA, it was assumed that it would have an antikinetic property. However, later the study conducted in 1972 was found that piracetam improves cognitive functions and memory, like psychostimulants. However, in contrast to psychostimulants, he did not have the side effects characteristic of them. At the same time, the term "nootropics" was also proposed.

From the opening of Pirachetam (he is currently known as Nootropyl) and the history of nootropic drugs began, which was a fundamentally new stage in the development of psychopharmacotherapy and led to the formation of a nootropic concept. After the successful implementation of Piracetam, other preparations of pyrrolidone series began to appear in the medical practice. It is now synthesized by more than 10 original nootropic drugs of pyrrolidine series, which are in phase III clinical trials or already registered in a number of countries; Among them, oxyzets, aniracets, ethylacets, pramiracets, dupratsteats, rollziracetam, cebracetam, nefiracetams, and feasts, children. These nootropic drugs received the common name "Racetama". There are other groups of nootropics that differ in the action mechanism. Often, some adaptogens are also related to nootrops (substances with a lining effect on the body, increasing resistance to adverse factors), and psychostimulants (stimulate excitability and psychomotor activity, and not just the highest nervous activity). This is due to the fact that all these substances have a stimulating effect on the CNS and often have similar effects.

Classification of Nootropov

There are two main classifications of nootropic drugs:

By mechanism, action:

Nootropic preparations with a dominant meal effect.

1. Pyrrolidone nootropic preparations (racemas), mainly metabolic action (piracetam, oxycetam, aniracetam, etc.)

2. Holinesterase preparations.

2.1. Enhancing synthesis of acetylcholine and its emission (phosphotidyl-serine)

2.2. Holinergic receptor agonists (Oxotremorin, Betanehol)

2.3. Acetylcholinesterase inhibitors (Fizostigmin, Tinner, Amiridine)

2.4. Substances with a mixed mechanism of action (Demanol, Azseglutamate, nerve growth factor, Bifemalan, etc.).

3. Neuropeptides and their analogues (ACTH, ECIRATED, Somatostatin)

4. Substances affecting the excitation system of amino acids (glutamic acid, glycine)

Nootropic mixed action preparations with wide spectrum Effects ("neuroprotectors").

1. Activators of brain metabolism (Actovegin, Instenon, acetyl-L-carnitine)

2. Cerebral vasodilators (Vinpocetin, Oxybral, Nicercoline)

3. Calcium antagonists (namodipine, cinnarizine, fluornarizin, etc.).

4. Antioxidants (mexideol, excipon, tocopherol)

5. Substances affecting the system of GABA (Gammalon, Phoenibut, Phenotropyl, sodium Oxibutirat)

6. Substances from different groups (etonisole, orothic acid, ginseng, ginkgo extract biloba, lemongrass, etc.).

By chemical structure:

Racetama. Pyrrolidine derivatives: piracetam, ethiothetam, aniracetam, etc.

Dimethylaminoethanol derivatives (predecessors of acetylcholine): deanola acegelumat, mecloofenoxate.

Pyridoxine derivatives: pyritinol, biotrier.

The derivatives and the analogues of GABC: GABA (Aminalon), Nicotinyl-GABA (Picigalon), gamma-amino-beta-phenylma acid hydrochloride (phenibut).

Cerebrovascular means: Ginkgo Biloba.

Neuropeptides and their analogues: Noopept, Semax, Selaanka.

Amino acids and substances affecting the system of exciting amino acids: glycine, biotrine.

Derivatives of 2-mercantobenzimidazole: ethylTI-benzimidazole Hydrobromide (chemical).

Vitamin-like funds: Idebanen.

Polypeptides and organic composites: Cortexin, cerebralizin, cerebramine.

Substances of other pharmacological groups with nootropic component:

correctors of brainwater disorders: nichangoline, vinpocetin, xanthinol nicotine, vinkamine, naphthidrofuril, cinnarizin;

common-linking agents and adaptogens: acetylaminantic acid (known as "Amber Acid"), ginseng extract, melatonin, lecithin.

psychostimulators: Sulbutiamine;

antihypoxants and antioxidants: oxymethylpyridine succinate (mexidol);

acephane and its derivatives.

In many ways, these classifications intersect, since the chemical structure determines the effect of matter. But more often the division of nootrops into classes is their chemical formulas.

The mechanism of action and the basic effects of nootropic agents

Since nootropics are an extensive group of compounds, a single action mechanism for them does not exist. It is believed that their effects can determine the following mechanisms of action:

Neurotropic: direct action of nootrops on neurons of mediator brain systems: monoaminergic, cholinergic, gamc-ergic, glutamanthergic, peptidergic.

Microcirculatory: Improving brain blood flow and microcirculation in the body by optimizing the erythrocyte passage through vessels and inhibiting platelet aggregation.

Metabolic: Improving the penetration through the GES and glucose disposal (especially in the cerebral cortex, subcortical ganglia, hypothalamus and cerebellum), improvement nucleic acids, activation of ATP, protein and RNA synthesis.

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 peroxidation oxidation of lipids of cell membranes;

Antihypoxic: reducing the needs of neurons in oxygen under hypoxia;

Neuroprotective: increasing the stability of nerve cells to the effects of adverse factors of various kinds.

These mechanisms determine all the main effects of nootropic drugs:

Nootropic effect (influence on violated higher cortical functions, level of judgment and critical capabilities, improving the cortical control of subcortic activity, thinking, attention, speech).

Raising the level of wakefulness, clarity of consciousness.

Adaptogenic effect (increasing the overall stability of the body to the action of extreme factors).

Anti-asthenic effect (influence on weakness, lethargy, depletion, phenomena of psychic and physical asthenia).

Psychotic effect (effect on apathy, mental inertness, psychomotor inhibition).

Antidepressive action.

Sedative (tranquilizing) action.

Vegetative action (effect on headache, dizziness)

Antikinetic action.

Anti-parkinsonic action.

Anti-epileptic effect, effect on epileptic paroxysmal activity.

Hypoglycemic action.

Energy action (by enhancing glucose consumption by the cells of the body)

SomatotropopyMilling effect (as a result of hypoglycemia)

Anabolic effect.

Lipolytic action (in conditions of glucose shortage, fatty acids are started in the form of energy).

Antitoxic action.

Immunostimulating action.

Application of nootropics in medical practice

Initially, nootropics were used mainly in the treatment of disorders of the brain functions in elderly patients. Now, thanks to the extensive spectrum of effects rendered to the body, nootropics have found much wider use in medicine. They are used at:

dementia of various genes (vascular, seenile, with Alzheimer's disease),

chronic cerebrovascular failure,

psychorganic syndrome,

with the consequences of the brain circulation disorders, the cranopy and brain injury,

intoxication

neuroinfection,

intellectual-meal disorders (violation of memory, concentration of attention, thinking), asthenic, asthenous depressive and depressive syndrome,

neurotic and neurosis-like disorder,

vegeto-vascular dystonia,

chronic alcoholism (encephalopathy, psychoorganic syndrome, abstinence),

to improve mental performance.

In children's practice, testimony for novotropov is:

mental and speech development delay,

mental retardation,

consequences of perinatal damage to the central nervous

cerebral palsy,

attention deficit syndrome.

Nootropics also play a significant role in comprehensive therapy. various diseases: neuroleptic syndrome, stuttering, hyperkinesis, sleep disorders, urination disorders, dizziness of various types, for the prevention of dummy.

The rate of the onset of the effects of nootropov differs in the therapy of the urgent states and in the treatment of chronic diseases. With acute states, nootropics give a rapid positive effect (for example, output from the state of disturbed consciousness). In a situation of chronic disorders, a long-term reception of nootropic drugs is required. Usually they are prescribed by courses up to 3-4 months. The effectiveness of the drug can be judged only at the end of the full course.

In clinical practice, nootropics extremely rarely cause any side effects. However, with overdose, despite their low toxicity, such symptoms can manifest themselves such as sleeping, hesitation of blood pressure, irritability, anxiety, headache, nausea, the revival of psychopathological symptoms. These manifestations quickly disappear when the dosage decreases. Also, when side effects appear, it is proposed to change this preparation on the nootrope of another class. With insufficient effectiveness of the drug, but its good tolerance is possible to use a combination of two nootropic agents with different mechanisms of action.

When prescribing the drug, preference is given to average dosages, with nootropics with a psychostimulating effect (piracetam, pyritinol, mecloofenoxate, etc.) it is desirable to appoint in the morning.

It should also be noted that the effectiveness of therapy depends on the age of the patient: what he is younger, the better the answer to treatment.

Conclusion

The extreme importance of drugs with nootropic effects is evidenced by the data on the widespread use of their application: according to WHO statistics, a third of the adult population of Europe and Japan takes nootropics. A wide range of nootropic drugs and a proven positive clinical effect of their application suggests that these funds are a necessary component of modern pathogenetic drug therapy of a wide variety of states. In addition, nootropics are characterized by good combination with the preparations of other pharmacological groups and rarely give side effects (which, as a rule, do not constitute a serious danger). Thanks to all this, nootropics with confidence can be attributed to vitality for the modern world drugs. But, despite the fact that there are already a large number of nootropic drugs, the search and introduction into the practice of new highly efficient drugs of this class is an important and urgent task, since the need for them is constantly growing.

List of sources of information

nootropic medicine

D. A. Kharkevich. Pharmacology. Textbook for universities. Moscow, "Gootar-Honey", 2002

Lectures on pharmacology for students of 3 courses of the pharmaceutical faculty

The mechanism of action is based on the change in bioenergy processes in the nervous cell:

    the consumption of glucose and oxygen by neurons increases;

    glucose disposal increases;

    activation of adenylate cyclase;

    strengthening of the ATP circuit;

    stimulation of RNA and protein synthesis;

    intensification in the brain tissue of phosphatidyl ethanolmine and phosphatidylcholine.

Nootropic agents also affect the exchange of mediators: they are inherent in the N-methyldeasparty potentiary activity, as well as the ability to activate glutamanthergic and GAB-Ergic processes.

Thus, nootropic agents called neurometabolic cerebroprotectors have both a neuromediator effect and metabolic, which is implemented by stimulating the speed and activity of neuronal energy supply processes.

Pharmacodynamics Nootropov.

    Nootropic effect - affect the delay in the development or violation of higher cortical functions, increase the level of judgments and critical capabilities of the brain;

    psychostimulating action - apathy and mental rations are eliminated;

    sedative effect - irritability and emotional excitability reduced;

    atiasthenic effect;

    mnemotropic action (contribute to the improvement of memorization).

    antidepressive action;

    adaptogenic action (increase the stability of the brain to the effects of adverse environmental factors);

    anti-epileptic effect - prevent degradation of personality when using anti-epileptic agents;

    antio-accountinsonic effect;

    immunocorreggling effect;

    improving the level of wakefulness of consciousness.

    expose antihypoxic effect.

Indications for use.

    Oligophrenia: oligophrenia treatment with nootrops is carried out in order to increase the intellectual ability of the brain, as well as stimulation of trainee.

    In gerontological practice for the treatment of senile dementia, including with Alzheimer's disease. The use of nootropov allows you to preserve the intellectual abilities of the elderly for a longer period.

    The treatment of alcoholic dementia.

    Various cerebrovascular disorders (consequences of crank-brain injuries, strokes) to accelerate and expand the processes of functional rehabilitation.

    Comprehensive depression therapy.

    Epilepsy - in complex therapy with antiepileptic drugs.

    IHD and other diseases accompanied by ischemia.

Side phenomena.

    Dyspeptic disorders;

    exciting action (piracetam);

    drowsiness (phenibut and sodium oxybutyrate);

    reduced blood pressure and bradycardia (Aminalon and Cavinton).

Adaptogens.

Adaptogens this is a group of drugs that increase the nonspecific resistance of the body and increase its resistance to the effects of adverse factors of the external environment.

Classification of adaptogens.

      Preparations of plant origin.

    tincture of Zhen-Shen;

    eleutherococcus extract;

    chinese lemongrass;

    preparations of Echinacea (tincture of Echinacea, Imsental).

      Preparations of animal origin.

    ranaryar;

    pantokrin.

The mechanism of action of adaptogen.

Activates the adaptive synthesis of RNA and proteins due to the membrane protector and regulation of the selective permeability of membranes. An antioxidant action that is implemented by increasing endogenous antioxidants in the body. Weaken biochemical and functional shifts during stress reactions.

Pharmacodynamics.

    Adaptogenic effect - increase the stability of the body to the effects of extreme factors;

    toning action - improve the functions of the central nervous system, without causing euphoria and non-breaking daily rhythms;

    actoprotective action;

    increase the resistance of the body to infectious agents;

    an antioxidant effect, which is implemented by increasing endogenous antioxidants in the body;

    protective effect with xenobiotics intoxication.

Indications for use:

    Neurosis and borderline states.

    Asthenic states.

    The overall weakening of the functions of the body after the diseases suffered.

    Chronic fatigue syndrome (SHU).

    For the prevention of stress reactions.

Adaptogens reception rules.

    Course duration of about 3 months.

    Taking time: autumn, winter.

    Reception mode: Tinstures take on an empty stomach 30 minutes before meals for 15-20 drops.

    Power Mode: Exclusion from the diet of fatty and spicy dishes, alcohol.

Side phenomena:

    Excitation of the CNS;

    increased blood pressure (rarely).

Actoprotectors.

Actoprotectors this is a group of drugs that increase physical and mental performance in extreme conditions. These include the following drugs:

Mechanism of action.

Improve the metabolism of organism cells. Bhemitilo stimulates the activity of gluconeogenesis enzymes, which stimulates aerobic glucose degradation paths.

Indications for use: (See Adaptogens).

Side phenomena:

    Hyperglycemia;

    disps disappointments.

Lecture №11.

Means used in coronary failure (anti-inaniginal means).

Ischemic heart disease (IBS)- This is an acute or chronic disease, which arises as a result of the reduction or termination of the blood supply to myocardium due to the damage to the coronary vessels.

IHD is a collective concept and includes anginapactoris and myocardial infarction (im).

The key link of Pathogenesis of IBS is the inconsistency between the need of myocardium in oxygen (blood) and its delivery.

Ethiopathogenesis IBS.

    The reasons that cause a decrease in the delivery of oxygen to the heart:

    atherosclerosis of the coronary arteries;

    coronary arterial thrombosis;

    spasm coronary arteries;

    violation of microcirculation in myocardium by strengthening platelet aggregation and reducing fibrinolysis;

    hypotension and bradycardia;

    heart failure.

    Causes that cause an increase in the need of myocardium in oxygen (blood):

    psycho-emotional stress;

    severe physical overvoltage;

    myocardial hypertrophy (athletes);

    thyrotoxicosis;

    hypertension and tachycardia;

    infectious myocarditis.

Most of the population of our planet, especially the inhabitants of large cities, are forced to be in conditions of permanent environmental and psycho-emotional stress. It has been proven that stress is not harmless to the human body, it is a risk factor of many, and also has a negative impact on the nervous system, as a result of which a person becomes irritable, it decreases working capacity, the memory and processes of thinking deteriorate. In this regard, scientists are continuously engaged in searching for the paths of prevention and correction of the negative impact of stress on the nervous system. About 50 years ago, the concept of nootropic drugs emerged, was synthesized and tested piracetam. This gave a powerful impetus to the search and creating other substances with such a principle of action, these studies continue to this day.

From this article, the reader will receive an idea of \u200b\u200bwhat nootropics and what effects they possess, get acquainted with testimony, contraindications, side effects of these drugs in general, and also learns the features of individual representatives of the drugs in this group, in particular new generation nootropics. Let's start.

What is nootropics

According to the definition of the World Health Organization, nootropic drugs are funds that have activating the impact on training that improve mental activities and memory, increasing the resistance (stability) of the brain to such aggressive impacts, as injuries, intoxication, hypoxia.

The first in the history of Nootrop is piracetam, which was synthesized and applied in the clinic of Belgian pharmacologists in the distance in 1963. In the process of research, scientists found out that this medicinal substance significantly increases mental performance, improves memory and promotes trainee. In the future, other drugs with similar effects were synthesized, which we will talk below.

Effects and mechanisms of action of nootropic drugs

The main effects of drugs of this group are:

  • psychostimulating;
  • sedative;
  • anti-asthenic (reducing the feeling of weakness, lethargy, phenomena of mental and physical asthenia);
  • antidepressive;
  • anti-epileptic;
  • actually nootropic (impact on the violated higher cortical functions, which is manifested by improving thinking, speech, attention, and so on);
  • mnemotropic (influence on learning and memory);
  • adaptogenic (increase in the body's ability to withstand harmful environmental impacts);
  • vasegeptive (improving the blood supply to the brain, which is manifested by a decrease and, as well as the elimination of other vegetative disorders);
  • antidiskinetic;
  • improving the clarity of consciousness and level of wakefulness.

These drugs do not cause pharmacological dependence and psychomotor arousal, the reception does not determine the exhaustion of the physical capabilities of the body.

At the heart of drugs of this group, such processes are:

  • activation of plastic processes in the central nervous system by enhancing protein and RNA synthesis;
  • activation of energy processes in neurons;
  • activation of the transmission of nerve impulses in the central nervous system;
  • optimization of polysaccharide utilization processes, in particular glucose;
  • depression of formation in cells of free radicals;
  • reducing the need of nerve cells in oxygen under hypoxia;
  • the membrane-stabilizing effect (adjust the synthesis of proteins and phospholipids in nerve cells, stabilize the structure of cell membranes).

Nootropic drugs activate adenylate cyclase enzyme, increasing its concentration in nerve cells. This substance is necessary to maintain the stability of the production of the main energy source for the implementation of biochemical and physiological processes - adenosine trifosphoric acid, or ATP, which, besides, under hypoxia, translates the metabolism in the brain to the optimally saved mode.

In addition, nootropics affect the neurotiator brain systems, in particular, on:

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

As a result of all the effects described above, the patient improves memory, attention, thought processes and processes of perception, increases its ability to learning, intelligent functions are activated.

Classification of Nootropov

The class of nootropic drugs includes substances of various pharmacological groups that provide positive influence To the work of nerve cells and improving their structure.

  1. Substances stimulating metabolic processes in nerve cells:
  • pyrrolidone derivatives: piracetam, pramiracetam, phenylpiracetam and others;
  • derivatives of gamma-amine oil acid (gamc): aminal, peyonal, gopanene acid, phenibut;
  • pantothenic acid derivatives: pantogam;
  • vitamin B6 derivatives - Pyridoxine: pyritinol;
  • means containing dimethylaminoethanol: acephane, centrophenoxin;
  • preparations containing neuroaminoxylotes and peptides: glycine, cerebrolysin, actovegin;
  • antihypoxants: oxymethylpyridine succinate;
  • vitamins, vitamin-like, generalonizing agents: vitamin B15, vitamin E, folic acid, succinic acid, ginseng extract and others.
  1. Preparations that have a positive effect on the vessels, or vasotropic drugs:
  • Xanthinola nicotinate;
  • Vinpocetin;
  • Pentoxifillin;
  • Zinnarizin;
  • Instenon.
  1. Preparations, stimulating memory and learning processes:
  • holinomimetics and anticholinesterase: Galanamin, Holin, Amiridine and others;
  • hormones: Corticotropin, adrenocorticotropic hormone;
  • endorphins, Enkephalins.

Indications for the use of nootropics

Nodules of class Nootropov are used to treat the following diseases:

  • of different nature (vascular, senile);
  • chronic insufficiency of brain vessels;
  • consequences of brain circulation;
  • neuroinfection;
  • intoxication;
  • psychoorganic syndrome with phenomena of memory violations, reduce the concentration of attention and general activity;
  • cortical myoclonia;
  • dizziness, with the exception of dizziness of vasomotor and mental origin;
  • chronic alcoholism (in order to treat encephalopathy, abstineent and psychoorganic syndromes);
  • reduced mental performance;
  • astheno-depressive, depressive, astheno-neurotic syndromes;
  • neurosis-like disorders;
  • card and brain injury;
  • hypercines;
  • sleep disorders;
  • migraine;
  • in complex treatment Open-finished glaucoma, vascular diseases of the retina, diabetic retinopathy, as well as the elder degeneration of yellow stains.

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

  • mental retardation;
  • mental Delay and Speech Development;
  • cerebral palsy;
  • the consequences of the lesion of the central nervous system in childbirth;
  • attention deficit syndrome.

Contraindications for receiving nootrops

Drugs this group cannot be taken in the following cases:

  • with the individual hypersensitivity of the organism of the patient to the active substance or other components of the drug;
  • in case of acute period hemorrhagic stroke (hemorrhages in brain tissue);
  • with hater hateringitton;
  • in the event of a severe renal function (if creatinine clearance is less than 20 ml / min);
  • during pregnancy and lactation.


Side effects of Nootropov

The drugs of this group rarely cause any side effects, however, a number of patients on the background of receiving them may be marked by the following undesirable reactions:

  • headache, irritability, anxiety, sleep disorders, drowsiness;
  • rarely, in sick elderly, the strengthening of symptoms of coronary failure;
  • nausea, discomfort in the area of \u200b\u200bthe stomach, or;
  • strengthening psychopathological symptoms;

Brief description of drugs

Since drugs belonging to the class described by us are actually quite a lot, we will not be able to consider them, but let's talk only about those who have gained the wider distribution in medical practice today.

Piracetam (piracetam, lusteam, biotropyl, nootropyl)

Available in the form of tablets for intakes and a solution for injection and infusion.

The drug has a positive effect on blood circulation and metabolic processes in the brain, as a result of which the stability of the brain tissues towards hypoxia and the effects of toxic substances increases, and the memory, the integrative brain activity improves, increases the ability to learn.

When taking inside, it is well absorbed in the gastrointestinal tract, the maximum concentration in the blood is determined after 1 hour. Penetrates many organs and fabrics, including through the hematorecephalic and placental barriers. The half-life is 4 hours. Excreted by the kidneys.

The path of administration of the drug: inside or parenterally (intramuscularly or intravenously). Tablets are recommended to accept food. Dosage and duration of treatment are determined individually, depending on the disease and features of its clinical flow.

In the treatment of patients suffering, care should be taken and adjust the dose depending on the level of creatinine clearance.

Side effects The drug is standard, and they, as a rule, occur in patients of elderly and senile age, provided they receive the dosage more than 2.4 g of piracetam per day.

It affects the aggregation of platelets, therefore, with caution, it is used in individuals suffering from hemostasis disorders and a tendency to hemorrhage.

During pregnancy and lactation, contraindicated.

In the case of the development of sleep violations against the background of taking Piracetam, the evening reception should be canceled and add this dose to the daytime.

Pramiracetam (Pramistar)

Chemical formula Pramirazetama

Release form - tablets.

It has a high degree of affinity for choline. Improves learning ability, memorization and mental activity as a whole. Does not have a sedative effect, does not affect the vegetative nervous system.

It is absorbed in 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 o'clock. Excreted by the kidneys.

During periods of pregnancy and lactation, the reception of Pramistar is contraindicated.

In the treatment of patients with impaired kidney function, it is necessary to closely monitor the development of the side effects of the drug - this will be a sign of an excess of the active substance in the body and require a reduction in the dose.

Vinpocetin (Cavinton, Neurovin, Vinpocetin, Vizobrol)

Produced in the form of tablets and a solution for infusions.

Improves microcirculation in the brain, reinforces brain blood flow, does not cause the phenomenon of "trusting".

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

It is used both in neurology (with chronic violations of the cerebral circulation and other diseases described in the general part of the article) and in ophthalmology (in order to treat chronic diseases of the retinal vessels) and in othiatria (to restore hearing acuity).

In the event of the beginning of therapy in a sharp period of the disease, Vinpocetin parenterally should be introduced, and then continue orally at a dose of 1-2 tablets three times a day after meals.


Phenibut (Bifren, Noofen, Nobut, Phoenibut)

Release form - tablets, capsules, powder for cooking oral solution.

Dominant effects of this medicinal substance are antihypoxic and anti-themselves. The drug improves memory, increases mental and physical performance, stimulates learning processes. In addition, eliminates anxiety, fear, psycho-emotional tension, improves sleep. Enhances and lengthens the effect of sleeping pills, anticonvulsants and neuroleptics. Reduces the manifestation of asthenia.

After taking inside, it is well absorbed and penetrated into all organs and tissues of the body, in particular, through the blood-brain barrier.

It is used in reducing emotional and intellectual activity, concentration of attention, memory disorders, asthenic, disturbing-neurotic and neurosis-like states, insomnia, Meniere disease, as well as in order to prevent the pecification. In comprehensive therapy of preyrium and delicious alcohol states, osteochondrosis of the cervical spine, climacteric disorders.

It is recommended to take inside, before taking food, 250-500 mg three times a day. The maximum daily dose is 2.5 g, the maximum one-time is 750 mg. The duration of therapy is from 4 to 6 weeks.
In various clinical situations, the dosing mode may vary.

It has an irritant action, so caution is used in persons suffering.

Hopantic acid (Pantogam)

Produced in the form of tablets.

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

Quickly absorbed in the gastrointestinal tract. The maximum concentration of the active substance in the blood is determined 60 minutes after the reception. Creates high concentrations in the kidneys, liver, stomach and skin wall. Penetrates the hematorencephalic barrier. It is excreted from the body in 2 days.

Standard readings.

Take the drug inside, after half an hour after eating. Motherwise dose For adults is 250-1000 mg. Daily dose - 1.5-3 g. The course of treatment is 1-6 months. After 3-6 months, you can repeat the course. In the treatment of various doses of the drug may vary.

Contraindications and side effects are described above.

Pyritinol (encephabol)

Produced in the form of tablets and suspension for oral administration (this dosage form Designed for children).

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

When complying with the dosing regime, the development of side effects is unlikely.

Glycine (Glycine, Glycide)

Release form - tablets.

Improves metabolism in muscles and brain tissues. It has a sedative effect.

Apply sublingual (resolving under the tongue).

For the treatment of depression, anxiety and irritability take glycine at 0.1 g 2-4 times a day. In chronic alcoholism is prescribed according to the recommended treatment schemes.

Contraindications - increased sensitivity To glycine. Side effects are not described.

Cerebricsin

The release form is a solution for injections.

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

Penetrates the hematorencephalic barrier.

It is used in metabolic, organic and neurodegenerative diseases of the brain, in particular, when, is also used in the complex therapy of strokes, traumatic brain damage.

Daily doses of the drug are widely vary depending on the pathology and range from 5 to 50 ml. The route of administration is intramuscularly and intravenously.

Use with caution to treat patients with allergic diathesis.

Aktovegin

Release form - tablets, injection and infusion mortar.

Contains exclusively physiological substances. Increases the stability of the brain to hypoxia, accelerates glucose disposal processes.

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

As a rule, it is moved well. In some cases, the reactions described at the beginning of the article are developing.

Allowed to use during pregnancy and breastfeeding periods.

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

It contains sucrose, so patients with hereditary impaired carbohydrate exchange are not applicable.

Hexobendine (Instenon)

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

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

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

Contraindicated in individual sensitivity to the components of the drug, elevated intracranial pressure, epileptiform syndromes. During pregnancy and during lactation, it is applied solely by testimony.

Inside it is recommended to take during or after eating, not chewing, drinking with plenty of water. The dosage is 1-2 tablets three times a day. Maximum daily dose - 5 tablets. The duration of treatment is at least 6 weeks.

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

During the treatment period, this drug cannot be consumed tea and coffee in large quantities. If the drug is injected intravenously drip, only slow infusion is allowed, and intravenous injection should continue at least 3 minutes. Fast administration of the drug can lead to a sharp decrease in blood pressure.

Combined drugs

There are many drugs that have 2 or more components similar to each other or mutually reinforcing each other effects. The main are:

  • Gamalate B6 (contains pyridoxine hydrochloride, gamc, gamma-amino-beta-hydroxyma saline, magnesium glutamate hydrobromide; pressed in complex treatment of functional asthenia; it is recommended to take 2 tablets 2-3 times a day for 2-18 months);
  • Neuro-norms (contains piracetam and zinnarizin; the testimony is standard for nootrops; dosage - 1 capsule three times a day for 1-3 months; take the tablet after eating, not chew, it is possible to abundantly drink water);
  • Noah, Oaron, Fesame, Cinatropyl, Evriza: drugs similar to chemical composition and other indicators with neuro-norms;
  • Olaatropyl (contains a gamke and piracetam; recommended for reception before meal, 1 capsule 3-4, maximum - 6 times a day for 1-2 months; if necessary, after 1.5-2 months, the course can be repeated);
  • Tiocetam (includes piracetam and tiotriazoline; tablets It is recommended to take 1-2 pieces per day; the course of treatment is up to 30 days; in some cases, in the form of a solution for injections: administered intravenously drip at 20-30 ml of the drug in 100- 150 ml of saline or intramuscularly 5 ml 1 time per day for 2 weeks).

So, above you got acquainted with the most sought-after drugs of the group of nootropics. Some of them are the first drugs of this class, but many are developed much later and acting much more efficiently, so they can safely wear the name of new generation nootrops. We draw your attention to the fact that the information provided in the article is not guidance to action: if you have any unpleasant symptoms You should not engage in self-medication, and you need to seek help from a specialist.

Raul Wallenberg

Abstract on the topic:

"Nootropic drugs"

Perched student group 05/14

"Clinical psychology"

Kulaeva Ya.E.

    Nootropics ............................................................ ..3.

    Mechanisms of Daish ............................................. ..... 4

    Effect ............................................................................. ..6

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

4.1 According to their chemical composition ..................................7

4.2 T. A. Voronina, S. B. Sedenin .................. ... 9

4.3 Mixed classification .................................... 10

    General indications for the use of nootrops .................12

    Side Effects ................................................ ..14

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

    Famous nootropics ................................................ 14

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

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

    Literature ............................................................ ..20

    Nootropics (neurometabolic stimulants, neurodynamic, neuroregulatory, neurometabolic, indoor, metabolic cerebroprotectors) - drugs intended for the provision of specific impact on higher integrative brain functionsStimulating learning and memory that improve mental activities that increase the stability of the brain to damaging factors that improve the cortical subcorcant links. Recently, in a group of nootropics, a subgroup of neuroprotectors that have a protective, stabilizing effect on cells nervous tissue Under adverse conditions.

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

Nootropics do not have an independent class in the classification of drugs and are combined with psychostimulants into a highlighted pharmacotherapeutic group with ATX code: N06VX.

The term "nootropics" (from the Greek words "Noos" - thinking, mind and "tropos" - desire, affinity) was adopted in 1972. This happened after the appearance of piracetam drugs on the global market, synthesized in 1963 by Belgian pharmacologists K. Giurgea and V. Skondia, which was at first as an anti-necnetic agent. Developed by the Belgian company UCB. In 1972, K. Giurgea found that after taking Piracetam, learning processes, attention, the memory improves. Nootropics have a characteristic stimulating effect on the resulting transcallozal potential and have additional anti-cellistic activity and do not, in contrast to psychostimulants, negative influence on the body.

In contrast to psychostimulants, the stimulation of nerve cells by nootrops leads to an increase in activity and execution that have not qualitative, and quantitative. The action of most nootropics is manifested immediately after the first reception, as is observed in psychostimulants, but with long-term treatment.

Later similar effects were noticed in other substances or complexes of substances. Nootropics are believed that nootropics increase the stability of the brain to a variety of harmful effects, such as excessive loads or hypoxia.

It is now synthesized by more than 10 original nootropic drugs of pyrrolidine series, which are in phase III clinical trials or already registered in a number of countries; Among them, oxyzets, aniracets, ethylacets, pramiracets, dupratsteats, rollziracetam, cebracetam, nefiracetams, and feasts, children. These nootropic drugs received the common name "Racetama".

In addition, other families of nootropic drugs are synthesized, including cholinergic, gamkergic, glutamhergic, peptidegic. Nootropic component of action is also present in other classes of drugs with different chemical origins.

    Mechanisms of action

The mechanisms of action of nootropic agents are the effect on metabolic and bioenergy processes in the nervous cell and interaction with neurotiator brain systems. It is proved that nootropics are activated by adenylate cyclase, increase its concentration in neuron. And the elevated level of cyclic AMP leads through the change in the flow of intracellular ions K + and Ca2 + to the accelerated release of serotonin from the sensory neuron. In addition, the activated adenylate cyclase supports the stability of the production in the ATP cell without the participation of oxygen, and under hypoxia conditions translates the brain metabolism into optimally saved mode. Manufacturers of neurometabolic stimulants state that their drugs penetrate well through the GEB, increase the glucose disposal rate (especially in the cerebral cortex, subcortical ganglia, hypothalamus and cerebellum), improve the exchange of nucleic acids, activate the synthesis of ATP, protein and RNA.

The effect of a number of nootropic agents is mediated through neuromediator systems Brain, including the most important:

- monoaminergic;

- Holieregic - phenotropyl;

- Glutamatergic (Mementine and glycine affect the NMDA receptors).

Nootropics, according to their companies, also have other impacts, including:

- membranetabilizing: Regulation of the synthesis of phospholipids and proteins in nerve cells, stabilization and normalization of the structure of cell membranes;

- antioxidant: inhibiting the formation of free radicals and peroxidation oxidation of lipids of cell membranes;

- antihypoxic: reducing the needs of neurons in oxygen under hypoxia;

- neuroprotective: Increase the stability of nerve cells to the effects of adverse factors of various kinds.

A significant role is played by improving microcirculation in the brain due to the optimization of the passage of erythrocytes through the vessels of the microcirculatory channel and inhibiting platelet aggregation. Nootropic effects can be called something else.

The integrated effect of nootropic drugs improves bioelectric activity and integrative brain activity, which is manifested by facilitating the passage of information between hemispheres, an increase in the level of wakefulness, enhancing the absolute and relative power of the EEG spectrum of the cortex and hippocampus, an increase in the dominant peak.

The declared increase in cortic subcorcant control, improving the information exchange in the brain, the positive impact on the formation and reproduction of a memorable track make it possible to assert that these "medicines" lead to improved memory, perception, attention, thinking, increase the ability to learn, activate intellectual functions. The claimed, but unconfirmed, the ability to improve cognitive (cognitive) functions gave reason to impose drugs of the nootropic series "Stimulants of Cognition".

At the heart of the therapeutic action of nootropov lies several mechanisms:

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

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

Strengthening the synaptic transmission processes in the central nervous system;

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

Improving glucose disposal; Acceleration of glucose penetration through the hematostephalic barrier and the increase in the absorption of its cerebral cells, especially the cortex of large hemispheres

A membrane-stabilizing effect, stabilization of cell membranes (an increase in the 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 the warning of platelet aggregation;

Improvement of cortical subcortical interaction;

Normalization of neurotransmitter disorders;

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

Improving reparative processes during brain damage of various genes.

    Effect

Preparations of CO stimulating (piracetam, phenotropyl, aminal, pyriditol, etc.) and depressing (Phoenibut, sodium oxybutirate) type of action.

In the spectrum of clinical activity of nootropov, the following claimed basic effects are distinguished:

Nootropic action (Impact on the violated higher cortical functions, the level of judgment and critical possibilities, improving the cortical control of subcortic activity, thinking, attention, speech).

Mnemotropic action (influence on memory, learning).

Raising the level of wakefulness, clarity of consciousness (influence on the condition of the oppressed and fastened consciousness).

Adaptogenic action (Effect on tolerance to various exogenous factors, including medicines, increasing the overall sustainability of the body to the action of extreme factors).

Anti-asthenic action (influence on weakness, lethargy, deapt, phenomena of psychic and physical asthenia).

Psychostimulating action (influence on apathy, hystobulia, aspotation, poverty of motivation, mental inertness, psychomotor inhibition).

Antidepressive action.

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

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

Antichinetic action.

Anti-parkinsonic action.

Anti-Epileptic actionEffect on epileptic paroxysmal activity.

Hypoglycemic action (Reduce blood glucose concentration).

Energy action (By enhancing glucose consumption by cells of the body), because of which is effective in sports at various stages of recovery after training.

Somatotropopyimulating action (As a result of hypoglycemia, a growth hormone will be released).

Anabolic action (In addition, since amino acids, and the anabolic and other hormones are precisely from amino acid residues and consist).

Lipolytic (fatobilizing or fat burning) action (under conditions of glucose shortage, fatty acids are started in the form of energy). Anti-Parkinsonic.

Antidiskinetic.

Antitoxic effect (By the withdrawal from the body of the products of the cells of cells and neutralization of various harmful substances).

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

General resulting actions for this group of drugs:

Improvement of mental processes - cognitive functions or cognitive processes (training);

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

Improving the reproduction of available information, increasing intellectual activity, the volume of intellectual possibilities;

deterioration of extraction from memory (oblivion) \u200b\u200bof information about pain or stressful states;

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

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

Improving the impact on the highest nervous activity and mental state with functional or morphological disorders;

Increasing the stability of cerebral mental processes to the effects of adverse factors of the outer and internal environment (hypoxia, injury, strokes).

The presence of a pronounced anabolic effect and indirect positive effect on physical performance determines the feasibility of the use of certain drugs from a group of nootrops (piracetam, ethiyatsetam, aminalon, sodium oxybutirate, phenibuta) in the schemes of pharmacological support of sports activities.

    Classification of Nootropov

    according to their chemical composition.

Pyrrolidone derivatives: piracetam, ethiothetates, aniracets, oxycetam, pramiracetam, dupracetam, rollziracetam, etc.

Diaphenylpyrrolidone derivatives: Phenotropyl.

Pyridoxine derivatives: Pyritinol, biotrine.

Derivatives and analogues of GABS: Gamma-amine-oil acid (Aminalon), nicotinoyl-gamke (peyonal), gamma-amino-beta-phenylmacean acid hydrochloride (phenibut), gopanenic acid, calcium gamma hydroxybutyrate (sodium oxybutirate).

Cerebrovascular tools: ginkgo biloba.

Neuropeptides and their analogues: Noopept, Semax, Selaanka.

Amino acids and substances affecting the system of exciting amino acids: Glycine, biotrine.

Derived 2-mercantobenzimidazole: EthylTIBENZimidazole Hydrobromide (Brhemative).

Vitamin-like funds: Icebenon.

neuromodulators: phenotropyl;

correctors of Brain Circulation Disorders: Nichangolin, Vinpocetin, Xanthing Nicotine, Vinkin, Naphthidrofuril, Cinnarizin;

common Constitutional Means and Adaptogens: Acetylaminationic acid (known as "Amber Acid"), ginseng extract, melatonin, lecithin.

psychostimulators: Sulbutiamine;

antihypoxants and antioxidants: oxymethylpyridine succinate (mexidol);

acephane and its derivatives.

Signs of nootropic activity are present in the pharmacodynamics of glutamic acid, meamantine and levokarnin.

In addition, the experiment shows the nootropic effect of a number of neuropeptides and their synthetic analogs (ACTH and its fragments, somatostatin, vasopressin, oxytocin, thyroliberin, melanostatin, cholecystokinin, neuropeptide y, substance p, angiotensin II, cholecystokinin-8, peptide analogs of piracetam, etc. ).

Currently, there are several classifications of nootropic drugs.

The classification of nootropics for the chemical structure provides for dividing them into the following groups.

Racetama - Pyrrolidone derivatives: piracetas, ethiothetam, aniracets, oxycetam, pramirazetam, dupratsteats, rollziracetam, etc.

Dimethylaminoethanol derivatives (Predecessors of acetylcholine): deanola Acegelumat, Meclofenoxate.

Pyridoxine derivatives: Pyritinol, biotrine.

Derivatives and analogues of gams to: U-aminobalic acid (aminal), nicotinyl-gamke (peyonal), y-amino-p-phenylma acid hydrochloride (phenibut), gopanenic acid, pantogam, calcium y-hydroxybutyrate (neurobatul).

Cerebrovascular means: Ginkgo Biloba.

Neuropeptides and their analogues: Semax.

Amino acids and substances affecting the system of exciting amino acids: glycine, biotrine.

2-mercantobenzimidazole derivatives: EthylTIBENZimidazole Hydrobromide (Bemical).

Vitamin-like funds: Icebenon.

Polypeptides and organic composites: Cortexin, cerebricsin, cerebramine.

Substances of other pharmacological groups with nootropic component:

correctors of Brain Circulation Disorders - Nichangolin, Vinpocetin, Ksantinol Nicotinate, Winkin, Naphthidrofuril, Cinnarizin;

common Constitutional Tools and Adaptogens - acetylaminantic acid (known as "succinic acid"), ginseng extract, melatonin, lecithin.

psychostimulators - salbutiamine;

antihypoxants and antioxidants - oxymethylpyridine succinate (mexideol);

acephane and its derivatives.

    Classification on T. A. Voronina, S. B. Senenin, 1998

1. Nootropic drugs with the dominant epistemic effect (Cognitive Enhancers).

1.1. Pyrrolidone nootropic preparations (racemas), mainly metabolic action (piracetam, oxycetam, aniracets, pramiracetam, ethiothetam, dipracets, rollziracetam, nebraztam, and female, nefiracetyl, children, etc.).

1.2. Holieregic substances.

1.2.1. Acetylcholine synthesis activators and its emissions (choline chloride, phosphotidyl-serine, lecithin, acetyl-L-carnitine, DUP-986, derivatives of aminopyridine, ZK9346-betaqarboline, etc.).

1.2.2. Cholinergic receptor agonists (oxotremorine, betanehol, pyropyperidines, rinucleotides, etc.).

1.2.3. Acetylcholinesterase inhibitors (Fizostigmin, Torner, Amiridine, Ertastigmine, Galanamin, Metrifonate, Zelnakrin Maleat).

1.2.4. Substances with a mixed mechanism (Demanol Aceseglumat, Salbutamin, Bifemelan, Instenon).

1.3. Neuropeptides and their counterparts (ACTH 1-10 and its fragments, vasopide, somatostatin, semaax, vasopressin and its analogues, thyrolyiberin and its analogues, neuropeptide y, substance P, angiotensin-p, cholecystokinin-8, peptide analogues of Pirachetam (GVS-111 ), Prolandopeptidase inhibitors).

1.4. Substances affecting the system of exciting amino acids (glutamic acid, memannant, milamid, glycerin, d-cycloserine, reductly).

2. Nootropic drugs of mixed type with a wide range of effects

2.1. Activators of brain metabolism (actovegin, acetyl-l-carnitine, carnitine, phosphatidyl, serine, homopantotonic acid esters, xanthine derivatives of pentoxifyillin, propientofillin, tetrahydroquinolines).

2.2. Cerebral Vasodilators (Instenon, Winkin, Vinpocetin, Oxybral, Nicergolin, Winconat, Winbusol).

2.3. Calcium antagonists (niilyudipine, cinnarizine, fluunarized, etc.).

2.4. Antioxidants (mexidol, excipon, pyritinol, thyrilazad mesalalate, mecloofenoxate, atherovit (alpha tocopherol and meclofenoxate), etc.).

2.5. Substances affecting the system of gamke (gammalon, pantogam, peyonal, digam, nicotinamide, phenibut, phenotropyl, sodium oxybutirate, neurobatal, etc.).

2.6. Substances from different groups (etonisole, ocheric acid, methylglucorotatte, oxymetacyl, boiling, naphthidrofuril, cerebroaster, ginseng, lemongrass, ginkgo extract biloba, etc.).

    More often use mixed clusification of nootropic drugs,given the origin, clinical efficacy, latitude and mechanism of action. According to such a classification, nootropic funds are divided into two main groups:

    Preparations with dominant or preferential meal effects (Cognitive Enhancers), the main effect - the effect of memory (mnovic)

1. Pyrrolidone derivatives, namely, cyclic gams to (racetama) -piracetam (nootropyl), pramiracetam (pramistar), ethylacets, nefiracetam, aniracetam, phenotropyl, etc.

2. Holieregic means:

a) Holinesterase inhibitors - Galantamine Hydrobromide (Nivalin), Rivastigmine (Exelon), Donenezil, Ipidakrin (Neuromidin), AmininityGmin;

b) enhancement synthesis of the mediator - choline chloride, choline alfoscerat (glatchin), lecithin et al.;

c) M-, n-cholinomimetics - betanehol;

d) substances with a mixed type of action - deanola acegelutamate.

3. Neuropeptides and their analogues -semax, cerebriculisive, cerebrospyrin, Actovegin, Salcossuril, Tyrolyberin.

4. Preparations affecting the system of exciting amino acids- Glutamic acid, reductly.

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

II. Preparations of mixed type with a wide range of action (neuroprotectors)

1. Metabolism activators of the brain -pentoxifillain, acetyl-L-carnitine.

2. Cerebral Vasodilators -vinpocetin (Cavinton), oxybral (Vikin), Nicergolin (Sermion), etc.

3. Calcium antagonists- namodipine, zinnarizin, flunarized, etc.

4. Substances affecting the gam system to -aminal, Membraton, Pantogam, Picigalon, Sodium Oxibutirate, Phenibut (Noofen), etc.

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

6. Preparations from different groups - Naphthidrofuril, etonisole, Ginkgo Extract Bloba (Tanacanan, Memoplant), Melatonin, Huato Bolus, etc.

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

Piracetas, its homologs and analogs (aniracets, oxycetam, pramiracetam, nefiracetam, etc.);

Dimethylaminoethanol derivatives: deanolaacegeglumate, meclofenoxate, centrophenoxin;

Neuro-amino acid preparations: gamma-amine oil acid (gamc), derivatives of gamma-amine oil acid (phenibut, nicotinylene-gamma-amine oil acid (peyonal), gopanene acid (pantogam), glycine, glutamy acid;

Pyridoxine derivatives: pyritinol (pyriditol, energy, enezephabol);

Holinomimetics of the central action: Holine Alfoscerat;

Preparations of Ginkgo Biloba: Bilobil, Memoplant, Tanakan et al.;

Compounds of another chemical structure relating to various classes and groups of chemicals similar to the mechanism of action with piracetam and have the ability to facilitate learning processes and improve memory.

Along with true nootropic drugs (with a dominant effect on the meal functions), various authors belong to a group of nootropic drugs with a wide range of effects:

Preparations, reinforcing cerebral circulation, microcirculation and metabolism: Vinpocetin, Vinkin, Winconate, Nicergoline, Cinnarizin, fluornarized, nimodipine, xanthine derivatives of pentoxifyillin, carnitine, phosphatidylserin, sodium oxybat; Vitamins and their derivatives: Pantothenic acid, folic acid, vitamin E;

Intermediate cells of cell metabolism: rally and succinic acid;

Combined drugs: Instenon, Oaron.

5. Common testimony for the use of nootropov are:

Cerebral ischemia ( acute Stage and rehabilitation period);

Card-brain injury (acute stage and period of rehabilitation);

Coma;

Intellectual activity disorders in children suffering from delay

mental development in a weak or moderate form;

Difficulties in teaching children with deficiency syndrome concentration of attention;

Chronic fatigue syndrome;

Vegeth-vascular dystonia;

Alzheimer's disease;

Vascular dementia.

A feature of the use of nootropic drugs is the possibility of using them equally both for patients and for healthy people in extreme situations, with natural aging, when overwork, for the "cover therapy" to remove the severe course of "cancellation syndrome", as well as as Anti-alcohol tools that accelerate the exit from the delicious state and improving the course of the post-sideliosis state.

Prof. G. V. Kovalev (1990) said that "... Nootrop is facing a mind that fell either due to pathological processesor in connection with stress due to physical, chemical (including alcoholic), biological or social factors acting on the human body. " In foreign literature, as a synonym for nootropic drugs, the term "amplifier of cognitive functions" is sometimes used. Along with the direct influence on the epistemic functions, many nootropic drugs are used with a decrease in the overall level of human activity arising from various extreme impacts and diseases.

Application in sports medicine and in the practice of sports training

Under injuries of the brain;

To increase the concentration of attention;

Under cerebrovascular disorders during or after training sessions, competitions;

When dull;

In order to prevent the teaching;

For reducing (rehabilitation) treatment, after competitions, workout with large loads.

Some nootropics are used for:

Correction of neuroleptic syndrome (deanola acegelumat, pyritinol, pantogam, gopanene acid),

Stuttering (phenibut, pantogam), hypercines (phenibut, gopanenic acid, meminant),

Urination disorders (nicotinyl-gamke, pantogam),

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

Migraines (nicotinyl-gamke, pyritinol, semaax),

Dizziness (piracetam, phenibut, ginkgo biloba)

For the prevention of the tech (phenibut, gamc).

In ophthalmology with open-angle glaucoma, vascular diseases of the retina and yellow stain, with the elder degeneration of yellow spot, diabetic retinopathy.

Nootropic agents are used in Russia with the following states:

Psycho-organic syndromes (vascular, traumatic, infectious, intoxication, somatic genesis);

Acute vascular pathology; chronic alcoholism;

Epilepsy;

Chronic, therapeutic resistant depressive states;

Neurotic reactive somatogenic states; schizophrenia;

Correction of low training in children and adults

dementia of various genes (vascular, seenile, with Alzheimer's disease),

Chronic cerebrovascular failure,

Psychoorganic syndrome,

With the consequences of the brain circulation disorders, the cranopy and brain injury,

intoxication

Neuroinfection,

With intellectual-meal disorders, asthenic, astheno-depressive and depressive syndrome,

With neurotic and neurosis-like disorder,

With a terretous dystonia,

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

And also to improve mental performance.

In pediatrics, testimony to the appointment of nootrops are:

Mental and speech development delay,

Mental retardation,

Consequences of perinatal damage to the central nervous

Cerebral palsy,

Attention deficit syndrome.

Nootropic tools
Nootropic funds (psychometable stimulants), providing a selective mnemotropic effect (Greek .. Tpet - Memory, Tropos - direction), improve the highest integrative functions of the brain - intellect, attention, short- and long-term memory, create the ability to rapid information reproduction, accelerate training , reduce the number of errors in solving tasks. Nootropic tools weaken the perception of stressful situations, restore interest in life, target plants, sense of confidence, optimism, vital tone, increase the stability of the brain to harmful effects.
The action of nootropic drugs is directed to the bark of large hemispheres. They facilitate the intermetrous transmission of nerve impulses, enhance the controlling effect of the crust on subcortical structures, improve the functions of both neurons and neuroglia.
In memory formation, large hemispheres are involved (especially temporal and frontal lobes), hippocampus, amygdala, thalamus, cerebellum (engine training conditional reflexes). The transition from short-term to long-term memory is the transformation of the process of obtaining information in the process of saving it. Similar transformation provide medial temple share Core, hippocampus (remember memorizing and consolidating memory tracks), reticular formation (regulates attention).
The accumulation and storage of information in memory is due to electrical and chemical processes in the brain, leading to structural rearrangements. The short-term memory is based on trace phenomena - circulation of nerve pulses in the neuron chain after the cessation of irritants.
Long-term memory is associated with chemical coding of information and activation of synapses. When neurons are repeatedly excited and long, the concentration of calcium ions increases in their postsynaptic membrane. These ions activate calcium-dependent proteinase (Callin), splitting membrane protein (Fodrine), followed by demissation and increasing the number of functioning glutamic acid receptors. Sinapses become more sensitive, since their conductivity increases due to the growth in the number of glutamic acid receptors.
The first nootropic remedy for piracetam was created in the 1980s. K. Dzhurja and V. Skondia - Employees of the company UCB (Belgium). They also offered the term "nootropic means."
The most famous drugs of this group are as follows:

  • Piracetam (nootropyl) - pyrrolidone derivative, cyclic derivative of GABA;
  • Aminalon (gammalon) - gamke in pure form;
  • Phoenibut is a phenyl derivative of GABC;
  • Picigalon - a combination of gamke and nicotine acid molecules;
  • Pyritolol (pyritinol, energy, encephabol) - chemical analogue of pyridoxine
(Two pyridoxine molecules connected by disulfide bridge), but without vitamin B6 properties,
maybe even act as his antagonist.
Mechanism of action
Improved brain bioenergy
Nootropic agents increase the synthesis of ATP and CAMF, the utilization of glucose, intensify glycoliz and aerobic breathing, contribute to the growth of adenylate cyclase activity. As is known, for aging and neuropsychiatric diseases are characterized by energy deficit and decrease in adenylate cyclase activity in neurons.
Nootropic agents having the structure of the GABA have an antihipoxic effect, modifying the biochemical reactions of GABC Shunts.
The gamke-shunt is a workaround between two consecutive metabolites of tricarboxylic acid cycle - A-ketoglutar and succinic acids. Part of a-ketoglutaric acid turns into amber not directly, but undergoing rehabilitative amination in glutamic acid. Then glutamic acid is decarboxylated in GABA,
which reacts with the reasamination with A-Ketoglutar Tom and forms glutamic acid and amber semi-sub-subsidis. The latter is either restored to GOM, or oxidized in amber acid. The GOM system is an amber semi-subsidy in the conditions of oxygen deficiency supplies an additional oxidized fund for the oxidized + required for the oxidation of lactate into pyruvate. This reduces the toxic effect of lactate on cell enzyme systems, prevents ammonia accumulation. The correlation of antihypoxic and mnemotropic action of nootropic means is absent.
Enhance the synthesis and separation of neurotransmitters
Nootropic means activate the synthesis, exemption and turnover of dopamine, norepinerenaline, acetylcholine, inhibit Mao, increase the formation of P-adrenoreceptors, cholinoreceptors and neuronal capture of choline. The mechanism for the release of neurotransmitters is the value of the blockade of potassium channels, which facilitates the membrane depolarization.
Increase the synthesis of protein and membrane phospholipids
Nootropic agents improve the regeneration of neurons, activate their genome and increase the synthesis of information neuropeptides, intensify the exchange of phosphatidylcholine and phosphatidyl ethanolmine.
It is shown that cycloheximide introduced by roouss on the 7th day of postnatal development causes disorders of behavior and tract. Reception of nootropic drugs from the 8th to the 14th day eliminates these violations. Piracetam stimulates the inclusion of leucine into the brain protein, stabilizes the lysosomes of neurons and prevents catabolic processes in the brain when aging.
Improvement of cerebral blood flow and hemorological indicators
Nootropic remedies expand brain vessels, improve blood flow in brain ischemia zones, prevent the development of its edema, block platelet aggregation, thrombosis, improve elasticity of erythrocytes and microcirculation. A nicotinic acid A direct vessels and anti-seaterosclerotic effect is provided in the piciacalon.
Antioxidant action
Nootropic agents, inhibiting free-radical peroxidation, protect against the destruction of phospholipids of neurons membranes, which facilitates fixing the traces of memory. Lipoperoxidation is enhanced in the brain at organic diseases, aging and stress.
Potentiation of mnemotropic memory neuropeptide effects
Pyracetam, the pyrrolidone ring of which is not disclosed to the formation of the linear molecule GABA, is a receptor agonist that perceive signals from the neuropeptides of the memory (fragments of ACTH, vasopressin, substance P). According to the chemical structure, piracetam is similar to the cyclic form of the terminal amino acid of neuropeptides of memory - pyroglutamate and affects receptors as an exogenous ligand. Probably, the greatest value For mnemotropic action of piracetam, the glutamic acid amra receptors are activated.
Application and features of the action of drugs
Indications for the appointment of nootropic funds are as follows:
  • oligophrenia, children's cerebral paralysis, prevention of cerebral violations
newborn children from high-risk groups;
  • atherosclerosis of the brain vessels, discirculatory and hypertensive encephalopathy, brain
stroke and its consequences;
  • mixing disorders with alcoholism, epilepsy, neuroinfection;
  • post-traumatic acute and chronic brain lesions;
  • asthenia and depression in the elderly, senile dementia;
  • neurotic states, severe stress with overwork, impaired mental and
social adaptation;
  • dizziness;
  • comatous states of vascular, toxic or traumatic etiology.
Thus, nootropic agents are treated to the mind, which is fading either due to pathological processes, or as a result of stress caused by physical, chemical, biological and social factors.
Nootropic remedies provide therapeutic effect only with long term applications. The effectiveness of therapy depends on the age of the patient: the younger, the better the answer to treatment.
Piracetam has a stressboard and anti-leaving effect as a ligand activated at fear and alarm of benzodiazepine receptors. The antisole effect enhances emotional reactivity in a conflict situation. Thus, piracetam is a daily tranquilizer. It is considered to be a drug selection during examination stress, when nootropic properties are important. With the introduction of piracetam in Vienna or the muscles, the oppression of the central nervous system decreases in patients in the state of the spin and coma.
Aminal reduces heart rate and blood pressure in patients arterial hypertension, accelerates awakening at a coma, normalizes blood glucose levels with hyperglycemia, has a moderate anticonvulsant action during epilepsy.
Phoenibut has the properties of a weak daytime tranquilizer with an anesthetic, anticonvulsant and mineral activity, potentiates the effects of substances inhibiting CNS. It is a gamKV receptor agonist, inhibits gamke-transaminase and increases the release of the GABA. Phenibut is prescribed to calm excited children and neurotic children, elderly people with anxious fussiness, night anxiety, sleep disorders, before operations and painful diagnostic procedures, for steering therapy, tick, spasticity.
Picicon is characterized by a moderate anti-elevation effect with a stimulating component, significantly improves brain circulation, prevents the progression of atherosclerosis, reduces the content of GABA and the activity of the GAB-transaminase in the brain.
Pyritolol increases the permeability of the hematoencephalic barrier for glucose, fatty acids, acetic acid and amino acids, stimulates their oxidation and production of ATP in neurons, reduces the formation of lactate, creates conditions for the flow of metabolic processes without oxygen needs, and also increases the synthesis of protein and flow of sodium ions in the brain. Under the influence of pyriditol in the brain, the level of acetylcholine, dopamine and serotonin increases, the number and sensitivity of cholinoreceptors and NMDA-receptors of glutamic acid increases, the death of cholinergic neurons decreases. Pyritolol is also an antagonist of benzodiazepine receptors associated with gamke receptors.
Pyritolol occupies an intermediate position between nootropic agents and psychostimulants. It activates the ideological and motor sphere of activity, increases physical endurance, has a neuroprotective effect. Indications for the use of pyriditol - discirculatory encephalopathy, consequences of brain stroke and cranial injuries, shallow depression, asthenic and neurotic disorders of organic origin, alcoholic intoxication. The appointment of this drug in neuro-heroerontological practice is limited to a pronounced psychostimulating effect.

Acephane (mecloofenoxate hydrochloride, centrophenoxine) is split in the body to form N-chlorofenoxaceous acid (synthetic analog of auxine plants) and dimethylaminoethanol (active antioxidant). Acephane has a mnemotropic and moderate psychostimulating effect, activates the transport of glucose through the hematomanecephalic barrier, stabilizes mitochondrial membranes, improves oxidative phosphorylation, the synthesis of ATP in neurons, increases the synaptic transmission of nerve pulses and the number of cholinorceptionors, in the experiment contributes to the disappearance of lipofuscin granules (neurons of old animals differ little from Nervous cells of young animals). Shown in asthenia, impaired intelligence at high age, somatogenic psychosis, injuries and vascular diseases
brain, neurosis of obsessive states, diancephal and lateral amyotrophic syndromes. Dimethylaminoethanol is used as a nootropic agent called Demanola Acegelumat (Demanol).
Pantoga (acid is homopantotonic) - calcium salt of D-homopantotonic acid, in which the fragment of R-Alanine is substituted on GABA. Normally, the content of homopantotonic acid in the brain is 0.5 - 1% of the amount of gamke. It is a backup form of GABA. For Pantogama, pronounced anticonvulsant and anti-leaving effects are characterized, the ability to reduce the reaction to painful irritation. This nootropic agent enhances in the brain
oxidation of fatty acids, oxidative decarboxylation of A-ketoxlot, cycle of tricarboxylic acids, has hypocholesteromemic effect.
Pantogama is recommended for neurotic states, Parkinson's disease, some forms of epilepsy, tremor, stuttering, encephalitis, children's cerebral palsy, oligophrenia, trigeminal nerve neuralgia. It is not effective in medicinal parkinsonism, depression and chronic alcoholism.
Nootropic tools are well transferred to patients. In individual patients receiving piracetam, peyalon, pyritolol or acephane, irritability, anxiety, insomnia, anxiety, dyspeptic disorders, allergic reactions. Piracetam sometimes causes the aggravation of angina in the elderly people. Sick diabetes must take into account the large amount of sugar in the composition of Piracmetam's granules. Reception of the aminalon may be accompanied by vomiting, a feeling of heat, hesitations of hell. Acephane enhances nonsense, hallucinations, anxiety in mental patients, provokes arrhythmia (dimethylaminoethanol acts as a choline antagonist in acetylcholine synthesis). In the treatment of pantogam described syndrome, similar to the Reee syndrome (encephalopathy and fatty dystrophy internal organs). This severe complication is due to violation of carnitine metabolism.
Piracetam is contraindicated in acute renal failure, sugar diabetes (Granules), children up to one year. Picigalon is not prescribed against the background of acute and chronic kidney disease, pyriditol and acephane - with mental excitation, neuroinfection, epilepsy and other convulsive states.
Therapy by nootropic means is inexpedient with a rapid and significant violation of mental activities and intelligence.
Actoprotectors
Actovectors (lat. Actus - movement, ProtectLo - cover) increase physical and mental performance in complicated conditions. The drug of this group is a derivative of mercaptobenzimidazole inboard improves
movements, mental activity and attention, improves brain circulation. It has a strong antihypoxic effect, since it reduces oxygen consumption by tissues, heat product, the spending of energy resources per unit of work performed, increases the conjugacy of oxidative phosphorylation and synthesis of macroeergic phosphates. Activates glyconeogenesis, improves glucose recycling with a brain, heart and skeletal muscles, while the body is purified from lactic acid and ammonia, recycled in glucose-lactate and glucose-alanine cycles. Stimulates the synthesis of RNA, protein and tissue regeneration. The effects of endogenous antioxidant systems - superoxiddismutase and catalases potentiate.
Bhemitili is used for disease therapy accompanied by chronic hypoxia, for example, in psychstore, vestibular disorders, myocardiodestrophs, acute hepatitis, radiation disease. It is prescribed for rapid recovery with intensive physical Loads In sports and industrial medicine. The drug is also used as a stimulator of humoral and cellular immunity.
In some patients, chemicals cause dyspeptic disorders, irritability and insomnia, contraindicated in hypoglycemia.

 


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