Stimulation of the nervous system. Nervous system stimulants

CNS stimulants are designed to make our black stripes in life less difficult and transfer some of the moral burden. Everyone chooses their own means. Someone drinks a lot of coffee, someone prefers alcohol, and third parties even drink a special sedative. We will try to figure out whether this is correct and whether such stimulants can be called drugs.

CNS stimulants - effect on the body

Stimulants can increase the speed of basic processes in the body. After taking them, a person feels a surge of vivacity, incredible lightness and self-confidence. At such moments, I think “Now I will move mountains!”. After stimulants, difficult annual reports are easily and quickly filled out, lectures are learned in one night, and other actions are performed that require noticeably more time.

But this does not pass without a trace for the body. Interestingly, they were originally sold to people with mental disorders, and later given to suicide bombers before leaving for battle. Therefore, the narcotic properties of such a substance have been mastered for a long time. Their regular intake at the work of the heart and nervous system negatively responds. Today there are many stimulants, both banned and not.

Types of CNS stimulants

The following types of CNS stimulants are not prohibited in the world:

  • Nicotine;
  • Caffeine;
  • Ephedrine;
  • Chafir.

Illicit drugs affect the psyche much more strongly, for example:

  • Amphetamine;
  • methamphetamine;
  • Crack;
  • Cocaine;

Light stimulants

Mild CNS stimulants are widely distributed and used by people all over the world. These include caffeine, ephecrinum, and nicotine. Coffee and cigarettes are regularly advertised on television, in glossy magazines and on the movie screen.

By consuming caffeine in small amounts, you can get rid of fatigue, the desire to sleep and cheer up. Interestingly, this substance is found in much higher concentrations in tea than in coffee. Although it is considered to be the opposite. Caffeine is obtained from coffee beans and leaves.

Caffeine excites the cerebral cortex, due to which such an effect of cheerfulness and extreme lightness turns out. Thanks to this, it is much easier and more productive to work and complete tasks. People with a weak nervous system can become aggressive due to caffeine, they do not sleep well. In such cases, people try to stay away from such a substance.

Cigarettes containing nicotine are the second most popular. Many people feel relaxed during and after smoking, bad thoughts leave them and they stop being aggressive. But smoking has many side effects, including death from lung cancer. Therefore, if you have not started smoking, then it is better not to take up this addiction. Even with a strong desire to quit smoking, it is sometimes very difficult, an anti-nicotine patch, chewing gum, and special literature are used.

Ephedrine is taken by athletes or women who want to lose weight. More recently, it has been used medicinally to treat asthma and allergies.

In our country, it is very difficult to find it due to the fact that other strong drugs can be prepared on the basis of the drug. The effect of the drug is amazing, for a while taking it becomes stronger, does not feel pain and becomes more intelligent. There is vivacity and a surge of strength. All these symptoms disappear when the drug leaves the body.

Heavy CNS stimulants

Heavy CNS stimulants are more dangerous for a person because of their overdose, you can die or end up in intensive care. Cocaine, methamphetamine, and amphetamine cause hallucinations, feelings of euphoria, and a host of other symptoms. However, they cloud the mind of a person and prevent him from performing normal daily tasks.

In addition, it should be noted the huge negative harm that drugs have on the human body. Due to the constant use of drugs, problems with the kidneys, heart, mucous system or lungs can occur. This largely depends on the duration and method of taking the prohibited substance.

Amphetamine, for example, can significantly increase a person's physical strength, but at the same time makes him aggressive and dangerous to those around him.

Cocaine tends to be expensive, which is why non-wealthy people prefer the cheaper alternative in the form of crack. It is less pure and may contain impurities, but the effect of the drug is very similar to that of cocaine.

Trying these substances is highly discouraged as they are highly addictive, and the treatment of psychological and physical attachment from illicit substances can be time-consuming and difficult. In addition, drugs have destructive action on the body and its key systems.

Consequences of admission

The consequences of taking stimulants of the unequal system can be different depending on how often and in what doses a person allows himself such weakness. This will negatively affect the work of the kidneys, heart and gastrointestinal tract. If we mention energy drinks, which contain caffeine and other stimulants, it has been proven that their use led to heart problems in a young man and death because of this.

Abuse of any stimulants is fraught with negative consequences, so you should find an alternative to them and try meditation, reading or walking in the fresh air in order to be distracted and insist on a positive note.

Intentional impact on the body, deprivation of sleep, normal daily routine, proper nutrition and other necessary norms can also be negatively affected, so reconsider your views on this and try to limit yourself in such substances that affect the heart, brain and other key organs.

By doing this, you will not spoil your health and live a long, happy life, not burdened with the need to visit doctors, treat your heart, do ECGs, and recover from such stimulation.

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They are divided into the following groups.

1. Psychostimulants that have a stimulating effect on the functions of the brain and activate the mental and physical activity of the body and are divided into two subgroups.

The first includes caffeine, phenamine, sydnocarb and sydnofen, which have a fast-acting stimulating effect. In drugs of the second subgroup, the action develops gradually. These are nootropic drugs: piracetam, aminalon, sodium oxybutyrate, phenibut, pantogam, encephabol, acephene.

2. Analeptics excite primarily the centers of the medulla oblongata - vascular and respiratory; in large doses, they also stimulate the motor areas of the brain and cause convulsions. These are corazol, cordiamine, camphor. From the group of analeptics, a group of respiratory analeptics (cytiton, lobelin) is distinguished, they are characterized by a stimulating effect on the respiratory center.

3. Means that act primarily on the spinal cord. The main representative of this group is strychnine. There is another group of different herbal remedies that have a stimulating effect on the central nervous system. These are lemongrass fruits, ginseng root, pantocrine, etc.

psychomotor stimulants.

Caffeine(coffinum).

Strengthens and regulates the processes of excitation in the cerebral cortex, leading to an increase in mental and physical performance.

Application: drug poisoning, insufficiency of the cardiovascular system, spasms of cerebral vessels, increased mental and physical performance. Taken orally, the average dose of caffeine for adults is 0.05-0.1 g 2-3 times a day. V. R. D. - 0.3; V. S. D. - 1 year

Side effects: with prolonged use, a decrease in action occurs, and with a sudden cessation of administration, an increase in inhibition with symptoms of fatigue, drowsiness, depression; lowering blood pressure.

Contraindications: irritability, insomnia, severe hypertension, atherosclerosis, organic diseases of the cardiovascular system, old age, glaucoma.

Release form: tablets number 10.

Caffeine-sodium benzoate(Coffeinum-natrii benzoas).

Similar to caffeine, but more soluble in water.

Release form: tablets 0.1 and 0.2 No. 5; in the form of a 10 and 20% solution in 1–2 ml ampoules.

Stimulants are conditionally divided into 4 large groups:

1. PSYCHOSTIMULATORS

a) psychomotor:

Phenamine;

Sidnocarb.

b) psychometabolic (nootropics):

Nootropil (piracetam);

Cerebrolysin;

Hamalon and others.

2. Analeptics

a) direct action:

Bemegrid;

Etimizol and others.

b) reflex action:

Cytiton and others.

c) mixed action:

Cordiamin and others.

3. SPINAL CORD STIMULANTS

Strychnine;

Securenin and others.

4. GENERAL TONING AGENTS (ADAPTOGENS)

a) vegetable origin:

Preparations of ginseng, eleutherococcus, aralia, golden root, maral root, Bittner's balm, etc.

b) animal origin:

Pantokrin etc.

PSYCHOSTIMULATORS and NOOTROPICS

Psychostimulants (or psychotonics, psychoanaleptics, psychomotor stimulants) increase mood, the ability to perceive external stimuli, and psychomotor activity. They reduce the feeling of fatigue, increase physical and mental performance (especially when tired), temporarily reduce the need for sleep (drugs that invigorate a tired body are called "doping" - from the English to dope - to give drugs).

Unlike drugs that depress the central nervous system, stimulants are of less importance, since they are devoid of selectivity of action.

In addition, stimulation of the central nervous system is accompanied by its subsequent oppression.

CLASSIFICATION OF PSYCHOSTIMULANTS

1) Means acting directly on the central nervous system:

a) stimulating mainly the cerebral cortex (xanthine alkaloids, phenamine, sydnocarb, methylphenamine, meridol, etc.);

b) stimulating predominantly the medulla oblongata (corazol, cordiamine, bemegrid, camphor, carbon dioxide);

c) stimulating predominantly the spinal cord (strychnine).

2) Means acting on the central nervous system reflexively (lobelin, veratrum, nicotine).

It should be remembered that such a division is conditional and, when used in large doses, they can stimulate the central nervous system as a whole.

A typical representative of psychostimulants is PHENAMIN (amphetamine sulfate; tab. 0.005; drops in the nose, in the eye 1% solution).

Chemically, it is a phenylalkylamine, that is, it is similar in structure to adrenaline and norepinephrine.

THE MECHANISM OF ACTION is associated with the ability to release NORADRENALIN and DOPAMINE from presynaptic endings. In addition, phenamine reduces the reuptake of norepinephrine and dopamine. Phenamine stimulates the ascending activating reticular formation of the brainstem.

PHARMACOLOGICAL EFFECTS CNS EFFECT Powerful CNS stimulant. It improves mental and physical performance, improves mood, causes euphoria, insomnia, tremors, anxiety. In therapeutic doses, it has an awakening effect, eliminates fatigue, and increases physical capabilities. Stimulates the respiratory center and in this regard acts as an analeptic.


EFFECT ON THE CARDIOVASCULAR SYSTEM Increases both systolic and diastolic blood pressure. In relation to the hypertensive effect of phenamine, tachyphylaxis is known.

SMOOTH MUSCLE Phenamine increases the tone of the sphincter of the bladder and relaxes the muscles of the bronchi, but only at high doses. Phenamine reduces appetite (on the hypothalamus), has some anticonvulsant effect (for Petit mal).

ADVERSE REACTIONS An undesirable effect is stimulation of the sympathetic nervous system (tachycardia, anxiety, headache, tremor, agitation, confusion, paranoid psychosis, angina attacks).

The drug causes drug dependence, mainly mental, cumulates. Tolerance may develop.

INDICATIONS FOR USE:

1) neurotic subdepressions;

2) with narcolepsy, with catalepsy, to prevent pathological drowsiness (narcolepsy);

3) obesity;

4) as an analeptic in case of poisoning with narcotic analgesics.

Pyridrol and meridol are similar to phenamine in terms of their effect on the central nervous system. They do not have undesirable peripheral adrenomimetic effects.

In addition to phenamine, the active psychostimulant sydnocarb (mesocarb) also belongs to the group of phenylalkylsindnonimines.

This is an original domestic drug, slightly different in chemical structure from phenamine. In Russian clinics, sidnocarb is currently the main psychostimulant. Compared with phenamine, it is much less toxic and does not show a pronounced peripheral sympathomimetic effect. The psychostimulating effect develops gradually, but it is longer, not accompanied by euphoria and motor excitement. As a rule, there are no tachycardia and a sharp increase in blood pressure. After the action of the drug, the patient does not experience general weakness and drowsiness.

The drug is used for different types asthenia occurring with lethargy and lethargy, with apathy, decreased performance, hypochondria, increased drowsiness.

The drug is used as a psychostimulant for asthenic and neurasthenic disorders in patients who have undergone intoxication, infection and brain injury, in some forms of psychosis.

In addition, sydnocarb is used to relieve asthenic manifestations after the use of neuroleptics, tranquilizers, as well as in the treatment of patients with alcoholism (stopping of asthenoneurotic reactions during the period of "alcohol withdrawal", to reduce the withdrawal phenomenon).

Sidnokarb is also used in the treatment of children with oligophrenia, accompanied by adynamia, aspontaneity, lethargy, lethargy, asthenia.

Side effects. In case of an overdose, increased irritability, anxiety, loss of appetite are possible. In patients with psychosis, delusions and hallucinations may increase. Sometimes there is a moderate rise in blood pressure.

The drug is available in tablets of 0.005; 0.01; 0.025.

The industry also produces a combined preparation Sidnogluton containing 0.025 sidnocarb and 0.1 glutamic acid. The latter potentiates the psychostimulating effect of sidnocarb.

Xanthine ALKALOIDS (purine derivatives; metalxanthines), a typical representative of which is CAFFEINE, also belong to the drugs that stimulate mainly the cerebral cortex.

Xanthine alkaloids have been found in several plants throughout the world. Three natural xanthine alkaloids were found in these plants: caffeine, theobromine, theophylline, which are purine bases. When heated with nitric acid, they form a yellow precipitate, hence the term xanthines (Greek - xanthos - yellow). Caffeine is found in tea leaves (Thea sinensis - 2%), coffee seeds (Coffea arabica - 1-2%), cocoa seeds (Theobroma acuminata), etc.

PHARMACOLOGICAL EFFECTS Caffeine has the most pronounced effect on the central nervous system, followed by theophylline and theobromine. The effect of caffeine on higher nervous activity depends on the dose and type of nervous system. In small doses, caffeine increases the activity of the cortex, in large doses it depresses it. In small doses, it helps to speed up the process of thinking and makes it clearer, brings clarity to the train of thought, reduces drowsiness, fatigue and gives the ability to perform intellectually complex tasks. It reduces reaction time, increases motor activity and strengthens conditioned reflexes. These effects can be observed after 1-2 cups of coffee. One cup contains about 1500 mg of caffeine.

Higher doses cause increased excitability, confusion, insomnia, headache, tremor. Theophylline in large doses can even cause convulsions.

medulla oblongata High doses directly stimulate the respiratory, vasomotor and vagus nerve centers. This leads to increased breathing (increase and deepening), increased blood pressure, tachycardia. True, in large doses, tachycardia and arrhythmias occur, that is, its peripheral effect predominates (cardiac output increases).

SPINAL CORD Very large doses increase the reflex excitability of the spinal cord and may lead to clonic convulsions.

BLOOD VESSELS Xanthines have a myotropic effect on the blood vessels, but this vasodilating effect is short-lived. It cannot be used to treat peripheral vascular disease.

Xanthines have an ambiguous effect on different vascular regions. The latter helps with migraines. Caffeine has a weak myotropic antispasmodic effect on smooth muscle organs (bronchi, biliary tract). This is of great importance for the clinic. It has long been known that theophylline eliminates bronchospasm in anaphylactic shock, stimulates skeletal muscles, increases their metabolism, eliminates their fatigue.

Caffeine increases BMR. Increases glycogenolysis, causing hyperglycemia. Increases lipolysis, releases adrenaline from the adrenal medulla.

DIURESIS Xanthines increase diuresis. Theophylline is the strongest in this regard, followed by theobromine and caffeine.

Xanthines increase the volume, acidity and pepsin content in gastric juice.

THE MECHANISM OF ACTION is connected with two directions:

1) xanthines inhibit cyclic nucleotide phosphodiesterase and prevent the transition of cAMP to 5-AMP;

2) cause changes in the distribution of calcium at the level of intracellular processes.

ADVERSE REACTIONS

1) Confusion, tremor, headache, insomnia.

Ringing in the ears, headache, tachycardia, shortness of breath, arrhythmias. With these reactions, sedatives should be prescribed.

2) Xpintins are contraindicated in patients with peptic ulcer and gastritis.

3) Xanthines develop addiction, to a greater extent, mental dependence, which, however, is not dangerous.

INDICATIONS FOR USE To stimulate mental activity. With fatigue, in the presence of symptoms of asthenia, with migraine, hypotension. With absent-mindedness, impaired attention, exhaustion.

Caffeine is a part of many combined preparations with non-narcotic and narcotic analgesics: citramon, panadol extra, solpadeine, as well as with ergot alkaloids - the drug caffeamine.

NOOTROPS, NOOTROPIC MEDICINES

The term is derived from the Greek - noos - thinking, tropos aspiration, affinity. Means that have a special effect on the higher integrative functions of the brain, stimulate memory, learning, improve mental activity.

Improving mental, mental activity is the main effect of this group of funds. This is manifested in mental insufficiency associated with organic lesions of the brain.

Mechanisms of action of nootropic drugs at the neurophysiological level: influence on transchannel and other types of polysynaptically evoked potentials recorded on the EEG.

The direction of action of nootropic drugs indicates their pronounced effect on the integrative activity of the brain and the processes of information transmission in the brain. Probably, under the influence of nootropics, various brain formations and information transfer processes in the brain are adjusted to the theta rhythm. The ability of nootropics to improve learning and memory processes is based on the process of increasing the level of spatial synchronization of brain biopotentials.

It should be noted that the highest nervous system healthy animals and the psyche of a healthy person, these drugs do not affect. They normally do not change many behavioral reactions, conditioned reflexes, bioelectrical activity of the brain, motor activity.

The basis of the pharmacotherapeutic action of nootropics on molecular level in conditions of pathology, there is a beneficial effect on neurometabolism and brain energy. Therefore, this group of drugs is also called psychometabolic stimulants. The main nootropics used in practice mimic the metabolic effects of α-aminobutyric acid (GABA).

The first drug synthesized abroad in the late 60s in the research laboratory of UCB (Belgium) was named NOOTROPIL. In our country, there is an analogue - PIRACETAM (Piracetamum; in the table, 0.2; in amp. 20% solution, 5 ml; capsules - 0.4).

It is a classic nootropic agent, therefore it is most often used by doctors of various specialties.

PHARMACOLOGICAL EFFECTS Piracetam (nootropil) is a cyclic derivative of GABA.

Nootropics improve the metabolism of brain cells and, above all, the metabolism of glucose and oxygen in them, increase the resistance of cells to hypoxia, improve blood supply to the brain, and communication between the hemispheres. Nootropics increase memory, reduce fatigue. But the effects appear gradually, not immediately after ingestion. Piracetam has anticonvulsant activity, and in last years its immunomodulating effects, immunopotentiating influence are also described.

INDICATIONS FOR USE:

In conditions after a concussion;

In mentally retarded children, with varying degrees of mental retardation; in children with impaired memory, attention, speech;

The elderly, the elderly, in geriatrics to improve memory, mood;

In chronic treatment of drug addicts, alcoholics;

In patients after a stroke;

Nootropics are indicated for enuresis in young children.

In addition, they are prescribed to potentiate the effects of immunostimulants.

AMINALON is a GABA drug. Obtained synthetically. GABA

An inhibitory mediator that plays an important role in the metabolic processes of the nervous tissue. The drug stimulates tissue respiration, activates the enzymes of the Krebs cycle, improves the utilization of glucose by neurons.

Indications for use: vascular diseases of the brain, mental retardation in children.

Side effects of nootropics: brain stimulation can lead to irritability, sleep disturbance, moodiness, anxiety in children, increased blood pressure, sexual excitability. Therefore, they are used in courses (for 2-3 weeks).

In recent years, the group of nootropics has expanded significantly. This is the Hungarian drug Cavinton (Gedeon Rihter), cerebrolysin, etc.

CAVINTON (table. 0.005; amp. 0.5% solution, 2 ml). Ethyl ester of apovinkaminic acid (vinca minor alkaloid preparation).

Cavinton has the following effects:

1) dilates the vessels of the brain;

2) enhances cerebral blood flow, improves blood supply to the brain with oxygen;

3) improves the utilization of glucose by neurons, promotes the accumulation of cAMP, ATP;

4) reduces platelet aggregation;

5) increases the content of catecholamines in the central nervous system.

It is used primarily in neurology for:

1) neurological and mental disorders associated with disorders of cerebral circulation (stroke, trauma, sclerosis);

2) memory disorders;

3) dizziness;

4) aphasia;

5) hypertensive encephalopathy;

6) atherosclerosis of retinal vessels, i.e. in ophthalmology, etc.;

7) hearing loss of toxic genesis.

ANALEPTICLES (ANALEPTICS)

Analeptics (from the Greek analeptikos - regenerating, strengthening) mean a group of drugs that primarily stimulate the vital centers of the medulla oblongata - vascular and respiratory. In high doses, these drugs can excite the motor areas of the brain and cause convulsions.

In therapeutic doses, analeptics are used for weakening vascular tone, for respiratory depression, for infectious diseases, in the postoperative period, etc.

Currently, the group of analeptics according to the localization of action can be divided into three subgroups:

1) Preparations directly, directly activating (revitalizing) the respiratory center:

Bemegrid;

Etimizol.

2) Means that reflexively stimulate the respiratory center:

Cititon;

Lobelin.

3) Means of mixed type of action, having both direct and reflex action:

Cordiamin;

Camphor;

Corazol;

Carbon dioxide.

Bemegrid (Bemegridum; in amp. 10 ml of 0.5% solution) is a specific barbiturate antagonist and has a "revitalizing" effect in case of intoxication caused by drugs of this group.

The drug reduces the toxicity of barbiturates, relieves respiratory and circulatory depression. The drug also stimulates the central nervous system, so it is effective not only for barbiturate poisoning.

Bemegrid is used for acute poisoning with barbiturates, to restore breathing at the exit from anesthesia (ether, halothane, etc.), to remove the patient from a severe hypoxic state. Enter the drug intravenously, slowly until the restoration of breathing, blood pressure, pulse.

Side effects: nausea, vomiting, convulsions.

Etimizol occupies a special place among direct-acting analeptics.

Etimizole (Aethimizolum; in the table at 0.1; in amps of 3 and 5 ml of a 1% solution). The drug activates the reticular formation of the brain stem, increases the activity of the neurons of the respiratory center, enhances the adrenocorticotropic function of the pituitary gland. The latter leads to the release of additional portions of glucocorticoids. At the same time, the drug differs from bemegrid by a slight inhibitory effect on the cerebral cortex (sedation), improves short-term memory, and promotes mental work. Due to the fact that the drug promotes the release of glucocorticoid hormones, it has a secondary anti-inflammatory effect.

Indications for use. Etimizol is used as an analeptic, a respiratory stimulant in case of poisoning with morphine, non-narcotic analgesics, in the recovery period after anesthesia, with lung atelectasis. In psychiatry, its sedative effect is used in states of anxiety. Given its anti-inflammatory effect, it is prescribed for the treatment of patients with polyarthritis and bronchial asthma, as well as an anti-allergic agent.

Side effects: nausea, dyspepsia.

Reflex acting stimulants are N-cholinomimetics. These drugs are cytiton and lobelin. They excite H-cholinergic receptors in the carotid sinus zone, from where afferent impulses enter the medulla oblongata, thereby increasing the activity of the neurons of the respiratory center. These funds act for a short time, within a few minutes. Clinically, there is an increase and deepening of breathing, an increase in blood pressure. The drugs are administered only intravenously.

It is used for the only indication - for carbon monoxide poisoning.

In mixed-type agents, the central effect (direct excitation of the respiratory center) is supplemented by a stimulating effect on the chemoreceptors of the carotid glomerulus (reflex component). These are, as stated above, cordiamine and carbonic acid. In medical practice, carbogen is used: a mixture of gases - carbon dioxide (5-7%) and oxygen (93-95%). Assign in the form of inhalations, which increase the volume of breathing by 5-8 times.

Carbogen is used for overdose of general anesthetics, carbon monoxide poisoning, and neonatal asphyxia.

Cordiamin, a neogalenic drug, is used as a respiratory stimulant (it is prescribed as an official one, but it is a 25% solution of nicotinic acid diethylamide).

The action of the drug is realized by stimulation of the respiratory and vasomotor centers.

Assign for heart failure, shock, asphyxia, intoxication.

DRUGS THAT STIMULATE PRIMARY FUNCTIONS OF THE SPINAL CORD

In this group, essentially two drugs are used: strychnine and securinine.

Strychnine (Strichninum; powder; in 1 ml amp. 0.1% solution) is the main alkaloid of chilibukha seeds (vomit). In medical practice, nitrate salt - strychnine nitrate is used.

Strychnine and other preparations of chilibukha excite the central nervous system and, first of all, increase reflex excitability. The reflex reactions of the patient become more generalized. Strychnine improves the activity of the sense organs (vision, taste, hearing, tactile sensation), excites the vasomotor and respiratory centers, tones the skeletal muscles, myocardium.

Strychnine preparations are used as tonics with a general decrease in metabolic processes, rapid fatigue, and hypotension. weakening of cardiac activity due to intoxication and infections, with some functional disorders of the visual apparatus, with paresis and paralysis (of diphtheria origin, for example), with atony of the stomach.

Side effects occur with an overdose and are manifested by tension in muscle groups (facial, occipital), difficulty breathing, convulsions.

The drug securinin, obtained from the herb securenegi, is similar in nature to strychnine, but less active (10 times).

Used for asthenic conditions, paresis and paralysis, with hypo- and asthenic form of neurasthenia, with impotence due to functional disorders.

GENERAL TONING AGENTS (ADAPTOGENS)

Preparations of this group by origin can be divided into means of plant and animal nature. Herbal remedies are more commonly used, namely various herbal preparations of plants (ginseng root extracts, extracts of leuzea, Rhodiola rosea or golden root, eleutherococcus, tincture of zamaniha, lemongrass, Transbaikal skullcap, aralia). Of the means of animal origin, we can name the drug pantocrine, obtained from reindeer antlers, and produced as a neogalenic drug for oral (in drops) and parenteral administration.

The pharmacological action of these drugs is due to the content of salonin glycosides-ginsenoids, essential oils, sterols, peptides and minerals in them. These biologically active substances bring a stimulating effect on the central nervous system, increase efficiency, regulate the functioning of the endocrine glands, moderately lower blood pressure, the level of atherogenic lipids (cholesterol) and glucose in the blood, activate the activity of the adrenal glands. the patient to viral and other infections, improve well-being and appetite.

These drugs are indicated for mental and physical overstrain during the period of convalescence after long and serious illnesses, in particular, of an infectious nature (dysentery, typhoid and viral infections, etc.). The drugs are also prescribed to cancer patients in the rehabilitation period, after courses of chemotherapy and radiation exposure.

As a rule, drugs are prescribed for a long time, for 1-2 months. Acceptance of adaptogens is advisable in the morning, after breakfast.

The appointment of these funds in the afternoon is not shown, because. possible sleep disturbance in the form of difficulty falling asleep. Individuals may experience hypersensitivity to certain drugs.

PSYCHOTROPIC DRUGS

These are means that can affect the mental functions of a person (memory, behavior, emotions, etc.), and therefore they are used for mental disorders, neurotic and neurosis-like disorders, states of internal tension, fear, anxiety, restlessness.

CLASSIFICATION OF PSYCHOTROPIC DRUGS

1) Sedatives.

2) Tranquilizers.

3) Antipsychotics.

4) Anti-manic.

5) Antidepressants.

Let's start the analysis of this group of drugs with sedatives. Sedatives are sedatives. Sedative (sedative) drugs include:

1) small doses of barbiturates,

2) salts of bromine and magnesium,

3) preparations of plant origin (valerian, motherwort, passionflower herbs, etc.).

All of them, causing a moderately calming effect, have an indiscriminate, slightest, depressing effect on the cerebral cortex. In other words, sedatives enhance inhibitory processes in the neurons of the cerebral cortex.

Of the bromine salts, SODIUM BROMIDE and POTASSIUM BROMIDE are most commonly used. Valerian preparations are widely used in the form of infusions, tinctures, extracts.

Motherwort herb preparations are also sedatives. Use infusion and tincture of motherwort. Passiflora preparation - Novopassit. Common hop infusions, Quater's mixture (valerian, bromides, menthol, etc.), magnesium ions (magnesium sulphate).

Indications for use: sedatives are used for neurasthenia, hysteria, mild forms of neuroses, increased irritability, insomnia associated with this.

The second group of drugs from psychotropic drugs is a group of tranquilizers. Tranquilizers are modern sedatives with a selective effect on the emotional sphere of a person. The term tranquilizers comes from the Latin tranquillium - tranquility, peace. The psychotropic effect of tranquilizers is mainly associated with their effect on the libetic system of the brain. In particular, tranquilizers reduce the spontaneous activity of hippocampal neurons. At the same time, they have a depressing effect on the hypothalamus and the activating reticular formation of the brain stem. Acting in this way, tranquilizers are able to reduce the state of internal tension, anxiety, fear, fear.

Based on this, this group of drugs is also called anxiolytics. The fact is that the Latin term anxius- or English "anxious" is translated as "anxious, full of fear, fear", and the Greek lysis - dissolution.

Therefore, in the literature, the term anxiolytics is used as a synonym for the concept of tranquilizers, that is, means that can reduce the state of internal stress.

Due to the fact that these funds are mainly used to treat patients with neurosis, they have their third main name, namely, anti-neurotic drugs.

Thus, we have three equivalent terms: tranquilizers, anxiolytics, anti-neurotic agents, which we can use as synonyms. You can also find synonyms in the literature: small tranquilizers, psychosedatives, ataractics.

Of the tranquilizers used in medical practice, benzodiazepine derivatives are the most widely used, since they have a wide range of therapeutic effects and are relatively safe.

SIBAZON (Sibazonum; in the table at 0.005; in amp. 0.5% solution of 2 ml); synonyms - diazepam, seduxen, relanium, valium. Preparations of the same group: chlozepid (elenium), phenazepam, nozepam, mezapam (rudotel).

The mechanism of action of benzodiazepine tranquilizers: in the body, on the territory of the above CNS zones, benzodiazepines interact with the so-called benzodiazepine receptors, which are closely associated with GABA receptors (GABA - gamma-aminobutyric acid - inhibitory CNS mediator, inhibitory; glycine is also a CNS inhibitory mediator; L-glutamic acid is an excitatory neurotransmitter). Upon stimulation of benzodiazepine receptors, activation of GABA receptors is observed. Therefore, the interaction of benzodiazepines with the same receptors manifests itself in the form of a GABA-mimetic effect.

All benzodiazepines that eliminate the feeling of emotional tension have similar properties, but differ in pharmacokinetics. More often than other drugs, diazepam or sibazon is used.

PHARMACOLOGICAL EFFECTS OF TRANQUILIZERS (on the example of sibazon)

1) The main one is their tranquilizing or anxiolytic effect, which manifests itself in the ability to reduce the state of internal tension, anxiety, mild fear. They reduce aggression and induce a state of calm. At the same time, they eliminate both situational (associated with any event, specific action) and non-situational reactions. In addition, they have a pronounced sedative effect.

2) The next effect is their muscle relaxant effect, although the muscle relaxant effect of tranquilizers is weak. This effect is realized mainly due to the central action, but they also cause inhibition of spinal polysynaptic reflexes.

3) By increasing the threshold of convulsive reaction, tranquilizers have anticonvulsant activity. It is believed that the anticonvulsant and muscle relaxant activity of tranquilizers is associated with GABAergic action.

4) All benzodiazepine tranquilizers have a mild hypnotic effect, and the benzodiazepine tranquilizer NITRAZEPAM has such a powerful hypnotic effect that it rightfully belongs to the group of hypnotics on this basis.

5) Potentiating effect (enhance the effect of drugs that depress the central nervous system and analgesics). Benzodiazepines reduce blood pressure, reduce respiratory rate, stimulate appetite.

INDICATIONS FOR USE:

1) as a remedy for the treatment of patients with primary neuroses (antineurotic agents);

2) with neurosis on the basis of somatic diseases (myocardial infarction, peptic ulcer);

3) for premedication in anesthesiology, as well as in the postoperative period; in dentistry;

4) with local spasms of skeletal muscles ("tic");

5) sibazon in injections (in / in, in / m); with convulsions as an anticonvulsant of various origins and with status epilepticus, muscle hypertonicity;

6) as a mild sleeping pill for some forms of insomnia;

7) with alcohol withdrawal syndrome in persons suffering from chronic alcoholism.

SIDE EFFECTS

1) Benzodiazepines cause drowsiness during the day, lethargy, adynamia, slight lethargy, decreased attention, absent-mindedness. Therefore, they cannot be assigned to transport drivers, operators, pilots, students. Tranquilizers are best taken at night (in any case, 2/3 of the daily dose at night, and 1/3 of the dose for the day).

2) Benzodiazepine tranquilizers can cause

muscle weakness, ataxia.

3) Tolerance and physical dependence may develop.

4) A withdrawal syndrome may develop, characterized by insomnia, agitation, depression.

5) Drugs can cause allergies, photosensitivity, dizziness, headache, sexual dysfunction, menstrual cycle, accommodation.

6) Tranquilizers have a cumulative ability.

Habituation and development of addiction is a reason for the abuse of tranquilizers. This is their main shortcoming and a big misfortune.

In view of the above undesirable effects, the so-called "daytime tranquilizers" have now been created, which have a much less pronounced muscle relaxant and general depressant effect. These include MEZAPAM (rudotel, Germany). They act weaker in their tranquilizing effect, but most importantly, they cause side effects to a lesser extent. They have a sedative, anticonvulsant, muscle relaxant effect. Used to treat patients with neurosis, alcoholism. Therefore, they are considered as "daytime" tranquilizers, less disturbing performance during the day (Table 0.01).

Another drug - PHENAZEPAM (tab. 2.5 mg, 0.0005, 0.001) is a very strong drug, as an anxiolytic, as a tranquilizer it is superior to other drugs. In terms of duration of action, it ranks 1st among the above benzodiazepines, in terms of action it is close even to neuroleptics. For phenazepam, it has been shown that its decrease in blood plasma by 50% occurs after 24-72 hours (1-3 days). It is prescribed for very severe neurosis, which brings it closer to neuroleptics.

It is indicated for neurosis-like, psychopathic and psychopathic conditions, accompanied by anxiety, fear, emotional lability. It is indicated for obsessions, phobias, hypochondriacal syndromes. Used to stop alcohol withdrawal.

Propanediol derivatives, MEPROBAMAT or MEPROTAN, have similar properties to benzodiazepines. Inferior to the tranquilizer phenazepam. It has a sedative, muscle relaxant and anticonvulsant effect. Enhances the inhibitory effect of anesthetics, sleeping pills, ethyl alcohol, narcotic analgesics. Well absorbed from the gastrointestinal tract. It inhibits fast-wave sleep, causes a strong aftereffect, is toxic, depresses the respiratory center, disrupts coordination. Affects the blood, causes allergies.

The third group of psychotropic drugs are NEUROLEPTICS or ANTIPSYCHOTIC DRUGS (neuron - nerve, leptos - tender, thin - Greek). Synonyms: major tranquilizers, neuroplegics. These are drugs for the treatment of patients with psychosis.

PSYCHOSIS - a state characterized by a distortion of reality (that is, delusions, hallucinations, aggressiveness, hostility, affective disorders). In general, this fits into the concept of productive symptoms.

Psychoses can be ORGANIC or ENDOGENIC (schizophrenia, manic-depressive psychosis) and REACTIVE, that is, they are not independent diseases, but a condition that has arisen in response to a shock. For example, during an earthquake in Armenia - mass psychosis. At the heart of psychosis, a sharp increase in sympathetic tone in the central nervous system, that is, an excess of catecholamines (norepinephrine, dopamine or dopamine), is of great importance.

The discovery and introduction into practice in the middle of the century of active psychotropic drugs of the neuroleptic group is one of the greatest achievements of medicine. This fundamentally changed the strategy and tactics of treating many mental illnesses. Prior to the advent of these drugs, the treatment of patients with psychosis was very limited (electroshock or insulin coma). In addition, antipsychotics are currently used not only in psychiatry, but also in the border areas of medicine - neurology, therapy, anesthesiology, surgery. The introduction of these tools contributed to the development of fundamental research in the field of psychopharmacology, physiology, biochemistry, pathophysiology in order to understand the mechanisms of various manifestations of mental disorders.

The mechanism of the antipsychotic action of neuroleptics has not been sufficiently elucidated. It is believed that the antipsychotic effect of neuroleptics is due to the inhibition of dopamine receptors (D-receptors) of the limbic system (hippocampus, lumbar gyrus, hypothalamus).

The blocking effect on dopamine receptors is manifested by antagonism with dopamine and dopaminomimetics (apomorphine, phenamine) both in behavioral reactions and at the level of individual neurons.

On preparations of neuronal membranes, it was found that antipsychotics inhibit the binding of dopamine by its receptors.

In addition to blocking receptors sensitive to dopamine and norepinephrine, antipsychotics reduce the permeability of presynaptic membranes, disrupting the release of these biogenic amines and their reuptake (D-2 receptors). For some antipsychotics (phenothiazine derivatives) in the development of psychotropic effects, their blocking effect on serotonin receptors and M-cholinergic receptors of the brain may be important. Thus, the main mechanism of action of neuroleptics is the blockade of D-receptors.

According to the chemical structure, neuroleptics belong to the following groups:

1) phenothiazine derivatives - chlorpromazine, etaperazine, triftazine, fluorophenazine, thioproperazine or nasheptil, etc.;

2) derivatives of butyrophenone - haloperidol, droperidol;

3) derivatives of dibenzodiazepine - clozapine (leponex);

4) thioxanthene derivatives - chlorprothixene (truxal);

5) indole derivatives - carbidine;

6) rauwolfia alkaloids - reserpine.

Phenothiazine derivatives are the most widely used agents in the treatment of major psychoses.

The most typical representative of phenothiazine derivatives is AMINAZINE or largactyl (international name: chlorpromazine). Aminazinum (dragee 0.025; 0.05; 0.1; amp. 1, 2, 5 and 10 ml - 25% solution).

Aminazine was the first drug of this group, synthesized in 1950. In 1952, it was introduced into clinical practice (Delay and Deniker), which marked the beginning of modern psychopharmacology. Phenothiazines have a three-ring structure in which 2 benzene rings are connected by sulfur and nitrogen atoms.

Since other antipsychotics of the phenothiazine group differ from chlorpromazine only in the strength of action and some features of the psychotropic effect, chlorpromazine should be discussed in detail.

MAIN PHARMACOLOGICAL EFFECTS OF AMINAZINE

1) Pronounced effect on the central nervous system. First of all, it is a neuroleptic effect, which can be characterized as the deepest sedative effect (super-sedative) or an over-expressed tranquilizing effect. In this regard, it is understandable why earlier this group of drugs was called "big tranquilizers."

In patients with major psychosis and arousal, aminosine causes a decrease in psychomotor activity, a decrease in motor-defensive reflexes, emotional calm, a decrease in initiative and arousal, without exerting a hypnotic effect (neuroleptic syndrome). The patient sits silently, he is indifferent to the environment and the events taking place around him, minimally reacting to external stimuli. Emotional dullness. Consciousness during this period is preserved.

This effect develops quickly, for example, with parenteral administration (in / in, in / m) after 5-10 minutes and lasts 6 hours. It is explained by the blockade of adrenoreceptors and dopamine receptors in the brain.

2) The antipsychotic effect is realized by a decrease in productive symptoms and an impact on the emotional sphere of the patient: a decrease in delirium, hallucinations, and a decrease in productive symptoms. The antipsychotic effect does not appear immediately, but gradually, after many days, mainly 1-2-3 weeks after daily intake. It is believed that this effect is caused by the blockade of D-2 receptors (dopamine presynaptic).

3) Aminazine, like all phenathiazine derivatives, has a distinct antiemetic effect associated with blocking the chemoreceptors of the trigger zone (trigger zone) located at the bottom of the IY ventricle. But it is not effective for vomiting caused by irritation of the vestibular apparatus or the gastrointestinal tract. It reverses the effect of apomorphine (a dopamine receptor stimulant) on the trigger zone in the medulla oblongata.

4) Aminazin depresses the center of thermoregulation. In this case, the final effect depends on the temperature. environment. Most often, due to the increase in heat transfer, slight hypothermia is observed.

5) Typical for chlorpromazine is a decrease in motor activity (muscle relaxant effect). At sufficiently high doses, a state of catalepsy develops, when the body and limbs remain for a long time in the position that they were given. This condition is due to the inhibition of the descending facilitating influences of the reticular formation on the spinal reflexes.

6) One of the manifestations of the effect of chlorpromazine on the central nervous system is its ability to potentiate the action of analgesics, anesthetics, hypnotics. This effect is partly due to the inhibition of biotransformation processes of these drugs by chlorpromazine.

7) In large doses, chlorpromazine has a hypnotic effect (light, superficial sleep).

Aminazine, like all phenothiazines, also affects peripheral innervation.

1) First of all, chlorpromazine has pronounced alpha-blocker properties, as a result of which it eliminates some of the effects of adrenaline and norepinephrine. Against the background of chlorpromazine, the pressor reaction to adrenaline sharply decreases or a "perversion" of the effect of adrenaline sets in and blood pressure falls.

2) In addition, chlorpromazine has some M-anticholinergic (that is, atropine-like) properties. This is manifested by a slight decrease in the secretion of the salivary, bronchial and digestive glands.

Aminazine affects not only efferent, but also afferent innervation. With local action, it has a pronounced local anesthetic activity. In addition, it has a distinct antihistamine activity (blocks histamine H-1 receptors), which leads to a decrease in vascular permeability, and is also a myotropic antispasmodic.

Characteristic for chlorpromazine is the effect on the cardiovascular system. First of all, this is manifested by a decrease in blood pressure (both systolic and diastolic), mainly due to alpha-adrenergic blocking action. Marked cardiodepressive effects, antiarrhythmic effect.

Aminazine, in addition to its above-mentioned effect on the nervous system and executive organs, has pronounced pharmacological effects on metabolism.

First of all, it affects the endocrine system. In women, it causes amenorrhea and lactation. Reduces libido in men (blocking D-receptors in the hypothalamus and pituitary gland). Aminazine blocks the release of growth hormone.

Enter chlorpromazine enterally and parenterally. With a single injection, the duration of action is 6 hours.

INDICATIONS FOR USE

1) Used as an ambulance for acute psychoses. For this indication, it is administered parenterally. Aminazine and its analogues are most effective in agitating the patient, excitement, tension and other productive psychotic symptoms (hallucinations, aggression, delirium).

2) Previously used in the treatment of patients with chronic psychoses. There are currently more modern facilities, in the absence of which it can be used.

3) As an antiemetic for vomiting of central origin (during irradiation, for example, with vomiting of pregnant women). Also with persistent hiccups, in the treatment of anticancer drugs.

4) In connection with the alpha-adrenergic blocking effect, it is used in the relief of a hypertensive crisis. In neurology: in conditions with increased muscle tone (after a cerebral stroke), sometimes in status epilepticus.

5) In the treatment of drug dependence in relation to narcotic analgesics and ethyl alcohol.

6) In the treatment of patients with manic states.

7) During operations on the heart and brain (hypothermic effect), during premedication, the same effect is used to eliminate hyperthermia in children.

SIDE EFFECTS

1) First of all, it should be noted that with prolonged use of chlorpromazine, patients develop deep lethargy. This effect is so overpoweringly pronounced that as it grows, the patient eventually turns into an emotionally "stupid" person. Aminazine can change behavioral reactions, accompanied by drowsiness, impaired psychomotor functions. Lethargy, apathy develops.

2) Almost 10-14% of patients receiving chlorpromazine develop extrapyramidal disorders, extrapyramidal symptoms of parkinsonism: tremor (shaking paralysis), muscle rigidity. The development of these symptoms is due to a dopamine deficiency in the black nuclei of the brain, which occurs under the influence of a neuroleptic.

3) Frequent adverse reactions to chlorpromazine are nasal congestion, dry mouth, palpitations. Due to the anticholinergic action, phenothiazines (chlorpromazine, etc.) cause blurred visual perceptions, tachycardia, constipation, suppression of ejaculation.

4) Hypotensive crises may develop, especially in the elderly. With intravenous administration, even death can occur.

5) 0.5% of patients develop blood disorders: agranulocytosis, thrombocytopenia, aplastic anemia. A number of patients (up to 2%) have cholestatic jaundice, various hormonal disorders (gynecomastia, lactation, menstrual disorders), aggravation of diabetes, impotence.

6) Phenothiazines can cause either an increase or decrease in body temperature.

7) In psychiatric practice, one can meet the development of tolerance, especially to sedative and antihypertensive effects. The antipsychotic effect persists.

As already mentioned, chlorpromazine refers to phenothiazine derivatives. He was the first drug of this series. Subsequently, a number of compounds of this class and series were synthesized (meterazine, etaperazine, triftazil, thioproperazine or mazheptil, fluorophenazine, etc.). In general, they are similar to chlorpromazine and differ from it only in the severity of individual properties, less toxicity and fewer side effects. Therefore, chlorpromazine is gradually being replaced from clinical practice by the above-mentioned drugs.

In the last 10 years, the drug THIORIDAZINE (sonapax) has been widely used. In antipsychotic activity inferior to chlorpromazine. The drug has an antipsychotic effect combined with a calming effect without pronounced lethargy, lethargy, emotional indifference. Very rarely causes extrapyramidal disorders. Indicated: for mental and emotional disorders, fear, tension, excitement.

Butyrophenone derivatives are of great interest as antipsychotics. Of this series of compounds, GA is mainly used to treat patients with mental illness.

Loperidol (halofen).

Haloperidolum (table. 0.0015, 0.005; vials of 10 ml of 0.2% - internal; amp. - 1 ml - 0.5% solution). Its action sets in relatively quickly. With the introduction of the drug inside, the maximum concentration in the blood occurs after 2-6 hours and remains at a high level for 3 days.

It has a less pronounced sedative effect and an effect on the autonomic nervous system (alpha-adrenergic blocking, atropine-like and ganglion-blocking action is less). At the same time, it is stronger in antipsychotic activity than chlorpromazine, therefore it is of interest in patients with very strong arousal and mania.

The frequency of extrapyramidal reactions in the treatment of this drug is very high, so it does not have significant advantages over phenothiazines in the treatment of schizophrenia. Used in the treatment of patients with acute mental illness with symptoms of hallucinations, delusions, aggression; with irrepressible vomiting of any origin or with resistance to other antipsychotics, as well as with hypnotics, analgesics as a premedicating agent.

DROPERIDOL belongs to the same group of drugs.

Droperidolum (amp. 5 and 10 ml 0.25% solution, Hungary). It differs from haloperidol in its short-term (10-20 minutes) strong action. Possesses antishock and antiemetic action.

Reduces blood pressure, has an antiarrhythmic effect. Droperidol is used mainly in anesthesiology for neuroleptanalgesia. In combination with the synthetic anesthetic fentanyl, it is part of the thalamonal preparation, which exhibits a rapid neuroleptic and analgesic effect, leads to muscle relaxation, and drowsiness. Used in psychiatry for the relief of reactive conditions. In anesthesiology: premedication during and after surgery. With endotracheal anesthesia. Contraindications: parkinsonism, hypotension, in the appointment of antihypertensive drugs.

Currently, new antipsychotics have been created that practically do not cause extrapyramidal disorders. In this regard, one of the most recent drugs, clozapine (or leponex), is of interest. It has a strong antipsychotic effect with a sedative component in the absence of symptoms of parkinsonism. When using the drug, there is no such sharp general oppression as that of chlorpromazine. Sedation that develops at the beginning of treatment, which then disappears. Clozapine is a dibenzodiazepine derivative. It has a high antipsychotic activity. Used in psychiatry for the treatment of patients with manic-depressive psychosis and schizophrenia, with psychopathy.

It is believed that clozapine and classical antipsychotics (phenothiazines and butyrophenones) interact with different types D-receptors. In addition, clozapine has a pronounced blocking activity against M-cholinergic receptors in the brain.

Clozapine is well tolerated, but it is necessary to monitor the blood because. there is a danger of developing agranulocytosis, possibly developing tachycardia, collapse. It should be used with caution for drivers, pilots and other categories of persons.

SULPIRIDE (eglonil) is a moderate neuroleptic. It has an antiemetic, moderate antiserotonin effect, no squeezing effect, no anticonvulsant activity, has an antidepressant effect, some stimulating effect. It is used in psychiatry (lethargy, lethargy, anergy), in therapy in the treatment of peptic ulcer, migraine, dizziness.

ANTIMANIC MEANS.

MANIA - a painfully elevated excited state, usually accompanied by an increase in mood, a desire to make speeches, etc.

From the Greek - mania - madness.

Mania is usually observed as one of the phases of manic-depressive syndrome (MDS).

In the treatment of patients with mania use:

1) neuroleptics;

2) lithium salts.

Antipsychotics are effective not only for mania, but also in general for agitated (strong excitement, excitement) states of various origins. Their action is manifested in general depression, the development of apathy and drowsiness.

Lithium salts act more specifically. They have a pharmacotherapeutic effect only in mania, without causing general lethargy.

Lithium salts are used to treat and prevent mania.

The mechanism of action of lithium salts is not well understood. It is believed that they reduce the release of norepinephrine from nerve endings by increasing intracellular oxidative deamination and more active neuronal reuptake of the mediator. In addition, it is believed that lithium, as it were, displaces sodium from cells, and as is known, sodium provides depolarization, that is, excitation of cells (neurons).

With enteral administration of lithium salts, they are well absorbed from the small intestine. Lithium is excreted by the kidneys by filtration.

The rate of lithium elimination can be slightly increased by increasing the sodium chloride content in the diet. With a decrease in the introduction of sodium chloride or its excessive excretion, lithium is retained in the body and this leads to intoxication (salt-free diet, the use of diuretics).

Various lithium salts are used: carbonate, chloride, iodite, acetate, nitrate. Lithium carbonate is the most commonly used.

Lithii carbonatus (tablet in a shell of 0.3). Lithium carbonate has been used in the treatment of mental illness since 1949 (Cade).

Lithium carbonate is administered only enterally.

As noted above, one of the most important indications for the use of lithium salts is the treatment of patients with mania. Lithium salts differ from neuroleptics in:

1) slower development of the effect (after 2-3 weeks), which dictates the use of neuroleptics at the beginning of treatment in severe manic states;

2) the difference between the action of lithium salts and antipsychotics lies in the fact that they have a more selective effect on mania, the absence of a sedative effect (does not cause lethargy, apathy in patients).

Great importance has the effectiveness of lithium salts for the prevention of mania, as well as depression in TIR.

ADVERSE REACTIONS It is necessary to take into account the low therapeutic range of lithium salts. This leads to the fact that the toxicity of these drugs is proportional to their content in serum. In this regard, their use requires regular monitoring of their blood levels (no more than 1.6-2 meq / l).

Moderate toxicity is manifested by diarrhea, dyspeptic disorders, drowsiness, muscle weakness, tremor, ataxia, polyuria, thirst. Lithium carbonate can cause allergic reactions, blurred vision. Non-toxic goiter, hypothyroidism, ECG changes may develop.

Lithium salts are contraindicated in violation of the excretory function of the kidneys, in diseases of the thyroid gland, with caution it is necessary to use the drug for peptic ulcer, cholecystitis.

The fifth group of psychotropic drugs is ANTIDEPRESSANTS. A lot of them. Used for pathologically low mood. Antidepressants with a sedative effect are also called TIMOLEPTICS (from the Greek - thymos - soul, spirit; leptos - gentle, thin), and with a stimulating effect - TIMORETICS (Greek - ereto - to irritate).

Successful correction of depression with the help of medications is one of the most important achievements of psychopharmacology in recent years.

CLASSIFICATION OF ANTIDEPRESSANTS Briefly, it can be represented by two main groups of drugs most commonly used in the clinic.

1) Means that potentiate the action of monoamines (monoamines tyrazine, serotonin). In this group, we will analyze two drugs: imizin, amitriptyline.

2) Inhibitors of monoamine oxidase - nialamide (nuredal). The most widely used are drugs of the first group, which are usually referred to as TRICYCLIC ANTIDEPRESSANTS due to their structure.

IMIZIN (Imizinum; in the table at 0.025; in amp. 1.25% solution of 2 ml) is a typical representative of this group of drugs and is used very often.

Other drugs: desipramine (norpramine), trimipramine, amitriptyline, nortriptyline (sensivan), protriptyline (vivactyl), nitroxazepine, etc.

Imizin has pronounced antidepressant properties, combined with a weak sedative effect. Sometimes, however, imizin can also have a psychostimulating effect (euphoria, agitation, insomnia).

The mechanism of action by which tricyclic antidepressants act in humans is unknown. There are only hypotheses. One of them connects the antidepressant effect of imizin with its ability to inhibit the reuptake of norepinephrine.

This leads to a large accumulation of the specified mediator at the receptors, which enhances the adrenergic effects. Imizin does not affect the activity of monoamine oxidase (MAO). In addition, imizin probably activates serotonergic receptors, which is due to a violation of its neuronal and extraneuronal uptake. Strengthening the inhibitory effect of serotonin on the limbic system (almond-shaped complex) may be one of the important mechanisms of the antidepressant action of imizin.

In addition, the central M-cholinoblocking effect of tricyclic antidepressants also plays an important role.

PHARMACOLOGICAL EFFECTS

1) Tricyclic antidepressants have a pronounced effect on behavior. Imizin has an antidepressant effect.

Improves mood, eliminates melancholy, unmotivated anxiety, suicidal thoughts, increases activity, desire for activity. In addition, it has some sedative effect.

2) Along with the central effects, imizin has some peripheral M-anticholinergic (atropine-like), papaverine-like (myotropic antispasmodic) and distinct antihistamine action.

When using imizin for depression, the therapeutic effect occurs in 2-3 weeks, and when using amitroptyline, it is somewhat faster. Excreted by the kidneys, 90% bound to plasma proteins.

SIDE REACTIONS Most often, side effects are associated with: 1) atropine-like properties (dry mouth, disturbance of accommodation, tachycardia, constipation, delayed diuresis). There may be phenomena: 2) orthostatic hypotension, collapse. In case of overdose - tachycardia, arrhythmias. On the part of the psyche, there may also be undesirable effects: either excessive sedation, or agitation, hallucinations, insomnia.

There may be headache, allergic reactions, tremor, jaundice, leukopenia.

THE DRUG IS CONTRAINDICATED in glaucoma, prostate adenoma.

Do not use together with MAO inhibitors.

AMITRIPTYLIN (Amitriptylinum; in the table at 0.025; in amp. 1% solution of 2 ml) - in pharmacodynamics and pharmacokinetics it is similar to imizin.

Along with high antidepressant activity, amitriptyline has pronounced psychosedative properties. It has no stimulating effect. Surpasses imizin on M-anticholinergic and protivogistaminny action.

Amitriptyline is the most active antidepressant drug.

Its therapeutic effect is revealed after 10-14 days. Side effects: constipation, tremors, muscle rigidity, dry mouth.

The second group of drugs INHIBITORS - MAO (MAOI - nialamid).

Currently, they are used quite rarely due to high hepatotoxicity. Therefore, when choosing, preference is given to tricyclic antidepressants. But sometimes MAOIs are useful.

The mechanism of action of MAOIs is due to the fact that these drugs inhibit the process of oxidative deamination of norepinephrine and serotonin, which leads to the accumulation of the latter in the brain tissue in significant quantities. Most drugs in this group block MAO irreversibly. Therefore, to restore MAO, it must be synthesized anew, which requires a certain time (up to 2 weeks).

Although the maximum effect of MAO inhibition occurs a few hours after the absorption of MAO inhibitors, the antidepressant effect develops only after 7-14 days. It is possible that the influence of MAO inhibitors on the metabolism of aminobutyric acid may play a certain role.

PHARMACOLOGICAL EFFECTS Along with antidepressant activity, MAO inhibitors are characterized by pronounced psychostimulant properties (euphoria, agitation, insomnia).

MAO inhibitors have hypotensive activity, which is associated with inhibition of the release of norepinephrine from the presynaptic endings of adrenergic fibers. They reduce pain in angina pectoris (a block of the central links of the reflex pathways from the heart).

Absorbed from the gastrointestinal tract well, eliminated by the kidneys.

SIDE EFFECTS The drugs are relatively toxic. This is manifested mainly by a hepatotoxic effect (severe hepatitis). In addition, they excite the central nervous system (insomnia, euphoria, convulsions).

Antidepressants found wide application in the treatment of patients with a depressive phase of manic-depressive psychosis, as well as with neurotic and reactive depressions. Used in child psychiatry to correct the behavior of children in case of their mental underdevelopment, as well as for the treatment of enuresis.

There is a possibility of developing orthostatic collapse. It is necessary to carefully use them together with other neurotropic drugs (narcotic analgesics, indirect-acting adrenomimetics, tricyclic antidepressants).

It is necessary to exclude food products containing tyrazine (cheese) from the patient's diet.

A large number of hydrazine derivatives have been synthesized as MAO inhibitors. But at present, few are used, in particular - NIALAMID. This is one of the least effective antidepressants (effect after 12-14 days). But low toxicity, which is its advantage. From non-hydrazine MAOIs - TRANSAMIN (strong MAO inhibitor - effect after 7-9 days). These funds are contraindicated in diseases of the liver, kidneys, cerebrovascular accident, with mental arousal.

ANTIEPILEPTIC DRUGS

"Epilepsy" is a collective term used to refer to a group of chronic convulsive pathologies that are characterized by sudden seizures (fits) with loss or disturbance of consciousness, usually, but not always, accompanied by characteristic movements (convulsions) and sometimes spontaneous hyperreactivity.

Seizures almost always correlate with EEG changes.

There are several convulsive and non-convulsive forms of epileptic seizures, each of which is characterized by a peculiar clinical picture and certain EEG changes (the latter is of great diagnostic value).

Allocate:

1) large convulsive seizures (great epilepsy, grand mal, the attack lasts 10-15 minutes);

2) psychomotor seizures;

3) small seizures of epilepsy (petit mal);

4) myoclonus epilepsy.

From the French - grand - big, mal - disease - generalized tonic-clonic convulsions with loss of consciousness, which after a few minutes are replaced by general depression of the central nervous system. Prolonged seizures or seizures following one after another at short intervals are referred to as status epilepticus.

Psychomotor seizures (or equivalents) are manifested by attacks of behavioral disorders, unconscious and unmotivated actions that the patient does not remember. Attacks are often accompanied by twilight consciousness and automatisms. There are no convulsions.

Petit - from French - small, small. It is characterized by a very short loss of consciousness. There may be twitching of the muscles of the face and other muscle groups.

Myoclonus epilepsy is manifested by short-term convulsive twitching of muscles without loss of consciousness.

Antiepileptic drugs are used to prevent or reduce the intensity and frequency of seizures or their equivalents, observed in recurrent seizures of various forms of epilepsy.

The mechanism of action of drugs is not entirely clear, since the etiology of epilepsy is not known. These drugs reduce the excitability of neurons of the epileptogenic focus. Primary reactions of antiepileptic drugs occur at the level of neuronal membranes. Under their influence, stabilization of neuronal membranes occurs, which leads to an increase in the refractory period, a decrease in lability, and inhibition of interneuronal excitation transmission.

It is possible that the action of a number of antiepileptic drugs is associated with an increase in the content of gamma-aminobutyric acid (GABA) in the brain.

Treatment of patients with each of these forms of epilepsy is carried out with certain antiepileptic drugs, for a long time, usually for years. Cancellation of drugs is carried out gradually, carefully.

The main drugs of choice for the prevention of grand mal seizures in epilepsy are:

PHENOBARBITAL AND DIFENIN.

These drugs are used for chronic treatment, not for the relief of a seizure. These 2 remedies are the main remedies for major convulsive seizures. In addition to them, you can use:

a) hexamidine;

b) chloracone;

c) sodium valproate;

d) clonazepam;

e) carbamazepine.

Phenobarbital for the treatment of epilepsy is used in a subhypnotic dose (from 60 to 180 mg). It is the best remedy for starting the treatment of any form of epilepsy, with the exception of Petit mal. In its therapeutic effect, an essential role is played by an increase in the sensitivity of GABA receptors to the mediator, as well as CNS depression, typical of the entire group of barbiturates.

The appointment of phenobarbital is accompanied by the occurrence of undesirable effects. In the first days of therapy, drowsiness, lethargy, irritability and hyperactivity often occur.

As a result of the induction of the activity of detoxifying liver enzymes (cytochrome P-450, glucuronidase system), the formation of inactive metabolites of a number of endogenous substances, primarily vitamins D, K, Vs, is accelerated. The latter leads to osteopathy, megaloblastic anemia, hypoproteinemia, hemorrhages.

To prevent these complications, patients receiving phenobarbital for a long time should additionally take vitamins D, K, Vs, as well as calcium salts.

The hydantoin derivative DIFENIN is more selective and most effective in large convulsive seizures.

Dipheninum - can be prescribed as an official drug in tablets of 0.117. Difenin is also effective in psychomotor equivalents. The activity of difenin is approximately the same as that of phenobarbital.

Difenin eliminates the increased permeability of sodium ions (Na) through the cell membrane of neurons of the epileptogenic focus. By this, difenin prevents the occurrence of pathological discharges in them that initiate a seizure.

Difenin is well absorbed from the gastrointestinal tract, but its maximum concentration in blood plasma is reached slowly - from 4-6 to 24 hours after administration. 90% bound to albumin in the blood. It is biotransformed in the liver and excreted by the kidneys. It is an inducer of microsomal liver enzymes. Accelerates the formation of inactive metabolites D, K, Vs. In this regard, vitamins are also prescribed to the patient. Difenin can accumulate, but to a lesser extent than f

According to doctors, the lack of vitamins and minerals in the body is a common problem for people. modern society. Unfortunately, almost all people have a lack of micronutrients due to the fact that simple fast food cannot provide a person with all the necessary substances and microelements.

Preparations (mineral-vitamin complexes), energizing

The only way to make up for their deficiency is the use of dietary supplements., adaptogens, nootropics and other pills for vitality and energy:

Vitus Energy

Pills for vivacity and energy that increase efficiency. They combine a number of substances necessary for the body: taurine, inositol, guarana extract, succinic acid, caffeine, vitamin B1, B6 and cyanocobalamin.

These substances together have a stimulating effect on the human body, filling it with strength. After using the drug, a person feels more energetic and active.

This article will discuss the most effective pills for vivacity and energy.

Vitamins Alphabet Energy

A complex of vitamins designed for people with a depleted body. The composition includes components with a daily dose: vitamins A, B5, B12, D, K, iron, copper, manganese, iodine, chromium. The content of vitamin B1, B2, B6, B9, C, E, PP exceeds the daily norm.

Not everyone is recommended to use this drug due to the threat of hypervitaminosis. It is prescribed in severe cases with severe stress and stress. The package contains 3 plates with tablets of different colors:

  • yellow a pill for vivacity and energy, therefore it is taken for breakfast;
  • orange affects the metabolism and should be consumed at lunch;
  • green acts as a sedative, so you should drink it in the evening.

For 1 day, you need to take 1 tablet from each plate at intervals of 4-5 hours. They cannot be taken together, as each pill contains matching vitamins. Thanks to the 3 single intake of certain vitamins, the possibility of an allergic reaction is excluded. Price — 350 r.

Duovit Energy

Means for raising the tone in the body. Contains ginseng root extract, vitamin A, C, E, B1, B2, B6, B12, D, nicotinamide, pantothenic and folic acids, zinc and copper sulfate.

The drug restores the energy reserves of the body, improves well-being, gives strength for vigorous activity in conditions of increased stress. You need to take vitamins in the morning during a meal, 1 tablet for 1 or 2 months. Price - 380 rubles.

Doppelhertz Energotonic

The creators of the unique formula of the drug are German pharmacists. The composition includes: vitamin B1, B2, B5, B6, B12, P, PP, folic acid, iron ammonium citrate, sodium glycerophosphate, copper sulfate, manganese sulfate, choline citrate.

Pills for vivacity and energy perfectly restore the body after operations, illnesses and the consequences of a monotonous diet.

Also, the drug helps to cope with heavy intellectual and physical stress, increase labor productivity. How to use: 1 tbsp. l. (20 ml) after meals 3 or 4 times a day. Price - 460 rubles.

Vitrum Energy

Multivitamin complex, raising the tone of the body. Contains vitamin A, B1, B2, B6, B12, C, E, K, folic and pantothenic acids, boron, calcium, phosphorus, iron, iodine, copper, magnesium, zinc, selenium, nickel, silicon, tin, ginseng extract .

The drug activates the immune forces of the body, favorably affects the heart and blood vessels, helps to restore nerve cells and helps to withstand severe stress and physical exertion. You need to take the remedy in the morning after meals 1 time per day, 1 pc. up to 2 months. Price (60 tablets) - 1100 rubles.

Dynamizan

General tonic for the body. The composition includes: vitamin A, B1, B2, B3, B5, B6, B8, B12, C, D3, E, glutamine, arginine, calcium, magnesium, phosphorus, selenium, iodine, zinc and ginseng extract.

Pills for vigor and activity are recommended to be taken with malnutrition (diet), reduced libido, smoking addiction, postoperative period, maintaining an exhausted body from mental and physical stress. You need to take the remedy in the morning, 1 pc. 1 per day. Price — 500 r.

Herbal adaptogens

Adaptogens are a group of medicinal plants that help a person maintain his energy level, which allows you to prevent mechanical, physical and psychogenic factors.

Adaptogens are often prescribed in the off-season for up to 2 months to prevent acute respiratory and chronic diseases.

The most common adaptogen experts include such plant products.

Maral root (leuzea)

Due to the large amount of anthocyanins, alkaloids, provitamin A, vitamin C, the plant has a tonic, cardiostimulating effect. It is used to increase efficiency, concentration, endurance, potency.

It should not be used by those who suffer from heart failure and high blood pressure.

Bear Root (Kopechnik or Red Root)

It is anti-inflammatory, antitumor, hemostatic, diuretic. Effective for prostatitis, prostate adenoma, reduced immunity, uterine bleeding, cystitis, nephritis, uterine prolapse, diseases of the mammary glands.

Bear root - herbal remedy for vivacity and energy

Used as a tincture. Its composition: 10 g of root and 100 g of vodka. It is prescribed in courses and applied in drops in small doses. Red root tincture is taken 3-5 ml 3 times a day for up to 1 month. The price depends on the form of release, on average from 70 to 400 rubles.

Rhodiola rosea

This tool allows you to restore the body after prolonged illness, physical overwork. It also has a therapeutic gynecological effect: it increases the possibility of conception in case of infertility and raises the hormonal background. It has antimicrobial and anti-inflammatory properties.


Rhodiola rosea

Helps with any acute chronic diseases. Rhodiola rosea tincture is used during chemotherapy because it allows the body to transfer this process much more easily. The composition of the tincture: vodka and the plant Rhodiola rosea. Affects male power, increasing potency. The dosage of the drug is determined by the doctor. Price - 35 rubles.

Interesting fact! Before people discovered adaptogens, they observed animals that actively used them.

Maral root was used by deer during the mating season. With a minimal amount of food, they expended very little energy. And the bear root was dug out by exhausted bears after hibernation to restore strength.

A growth hormone

Growth hormone or growth hormone is produced by the anterior pituitary gland. Affects all cells of the body, enhances protein synthesis. It affects the cardiovascular system, musculoskeletal system, nervous and hormonal systems.

It has been established that under the action of growth hormone, the condition of the skin, bone and cartilage tissue improves. Reduces the amount of cholesterol in the blood, promotes the breakdown of adipose tissue and muscle building. With age, its content in the body decreases, starting from the age of 25.

Factors affecting the production of growth hormone:

  • dream. The peak of growth hormone occurs in the first hours after falling asleep;
  • physical exercise. Strength training also increases the production of this hormone;
  • starvation. Lack of nutrition for up to a day leads to an increase in growth hormone;
  • nutrition. Products containing growth hormone releasers stimulate its production.

The releasers include amino acids: arginine, ornithine, glutamine. These substances are found in a large number of foods and affect the production of growth hormone in the same way as medications.

When eating food containing these amino acids, their level in the body begins to rise very slowly.

If you use amino acids in their pure form, then their level will increase dramatically. There are medical products that contain growth hormone itself, for example, jintropin.

It contains somatotropin, mannitol, glycine, sodium dihydrogen phosphate. Has a large number of side effects. Jintropin is available in injections that are administered once a day. Use is allowed only under the supervision of a physician.

Important to remember! Continuous use of growth hormone releasers for 4 weeks leads to addiction, which reduces their effect on the body. You need to take breaks.

Mental health drugs

Piracetam

Piracetam is a psychotropic drug (nootropic) that activates the nervous system, strengthens and calms nerve cells, improving their metabolism. Contains piracetam, povidone, magnesium carbonate, calcium stearate. Available in the form of injections and tablets.

It is used in rehabilitation therapy in psychiatry and neurology. The drug is prescribed in the morning and afternoon until 16:00 because it increases efficiency and activity. The duration of treatment with injections is determined by the doctor, as a rule, their number does not exceed 20. The course of treatment with tablets is up to 4 months.

Deanol aceglumate

Deanol aceglumate is a nootropic, antidepressant drug that restores mental activity, improves concentration and memory. The composition includes deanol aceglumate, N-acetyl-L-glutamic acid. The drug should be used orally 1 g 2 times a day in the morning and afternoon for 2 months. Price - 400 rubles.

Picamilon

Picamilon is a nootropic drug. It is prescribed for people with depression, impaired cerebral circulation, as well as after injuries and strokes. Increases concentration, improves brain activity and memory.

The composition includes gamma-aminobutyric and nicotinic acids. It is not recommended to take more than 2 months. Dosage 20-30 mg 3 times a day. Price - 120 rubles.

Calcium hopantenate

Calcium hopantenate is a nootropic drug that affects concentration, learning, memory and helps overcome psycho-emotional overload.

Used after traumatic brain injury. Contains calcium hopantenate, magnesium carbonate, calcium stearate. Produced in the form of tablets. Method of application: 0.25 - 1 g 3 times a day for 1-4 months. Price - 250 rubles.

Phenotropil

Phenotropil (phenylpiracetam) is a nootropic drug that allows you to cope with stress and increase the efficiency of the body. The drug is so powerful that its effect is 60 times stronger than that of piracetam.

Phenotropil also suppresses the feeling of hunger, so it is prescribed for obesity. The duration of admission is up to 3 months, the nootropic effect occurs after 2 weeks of treatment. The composition includes phenotropil, lactose monohydrate, calcium stearate. Price — 450 r.

Dosage of the drug:

Be careful! Phenotropil is included in the doping list because the effect of the drug is similar to the effect of amphetamine. Tablets for tone and energy increase the production of dopamine, serotonin and norepinephrine.

These neurotransmitters cause cheerfulness and good mood, but with prolonged use, their production depletes the nervous system.

Drugs that increase physical performance

Acetylaminosuccinic acid

Acetylaminosuccinic acid (succinic acid) is an anti-asthenic, general tonic agent with a nootropic effect. It is prescribed for neurosis, depression, increased fatigue.

The drug is a strong antioxidant that rejuvenates the body. Contains acetylaminosuccinic acid. Apply succinic acid 1-3 tablets. Price - 30 rubles.

Pills for vigor and energy are so harmless that they can be taken for a long time without health consequences.

Melatonin

Melatonin is a drug that contains the sleep hormone (melatonin). It boosts immunity, helps to cope with depression and stress. Studies have shown that the drug increases life expectancy by 20%.

Melatonin is an antioxidant that reduces the risk of developing cancerous tumors by blocking the division of malignant cells. Assign to people with impaired melatonin synthesis. As a rule, these are people of an age in whom it is produced in smaller quantities.

Recommended for people with insomnia, the elderly, and people who often change time zones. When changing 2 time zones, you need to take 1 tablet, and when changing 4 time zones - 2 tablets. In other diseases, the dosage of the drug is determined by the doctor.

The composition includes melatonin, calcium phosphate, croscarmellose sodium, magnesium stearate, stearic acid. Price - 800 rubles.

Note! The drug is more effective in capsules. When taking tablets, a certain amount of this substance breaks down under the action of gastric juice. Capsules dissolve only in the intestine in an alkaline environment and melatonin is not destroyed.

Calcium glycerophosphate

Calcium glycerophosphate is a drug that compensates for calcium in the body. Activates efficiency and has a general strengthening effect. Contains calcium glycerophosphate, calcium stearate. Take after meals 2 tablets 2 times a day for up to 4 weeks. Price - 100 rubles.

Pantocrine

Pantocrine is a biologically active agent that is produced on the basis of deer antlers. Contains many amino acids (alanine, histidine, proline, glycine, leucine, threonine, tryptophan, cystine, lysine, valine), lipoids and trace elements.

Pills for vitality and energy stimulate the central and peripheral systems, affect the renewal of the cellular composition of the body. This drug allows the body to increase resistance to various stimuli.

Used for fatigue chronic fatigue, low blood pressure, neurosis, asthenia, anemia. It is also prescribed in the postoperative period. Tincture is taken before meals from 20 to 40 drops per ½ glass of water 2-3 times a day, tablets 1-2 pcs. 2-3 times a day for 4 weeks. Price - 400 rubles.

Alcohol tinctures of ginseng and eleutherococcus

Alcohol tinctures of ginseng and eleutherococcus. Ginseng tincture has an adaptogenic effect, activates the nervous system, metabolism and reduces fatigue. Used 20-25 drops 2-3 times a day for 30 days. Price - 60 rubles.

Eleutherococcus tincture has an adaptogenic effect, stimulates the central nervous system, increases physical and intellectual activity, preventing overwork. Ingredients: Eleutherococcus extract, alcohol. It should be used 20-40 drops 2-3 times a day for a month. Price - 60 rubles.

Pills, tinctures and injections for vigor and energy can help a person improve their general physical condition and cope with many problems. It is important to choose the right drug, given its side effects and the characteristics of your body.

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STIMULATORS OF THE CENTRAL NERVOUS SYSTEM

INTRODUCTION

Stimulants are conditionally divided into 4 large groups:

1. Psychostimulants:

a) psychomotor:

Phenamine;

Sidnocarb.

b) psychometabolic (nootropics):

Nootropil (piracetam);

Cerebrolysin;

Hamalon and others.

2. Analeptics:

a) direct action:

Bemegrid;

Etimizol and others.

b) reflex action:

Cytiton and others.

c) mixed action:

Cordiamin and others.

3. Spinal cord stimulators:

Strychnine;

Securenin and others.

4. General tonic (adaptogens):

a) vegetable origin:

Preparations of ginseng, eleutherococcus, aralia, golden root, maral root, Bittner's balm, etc.

b) animal origin:

Pantokrin etc.

PSYCHOSTIMULATORS AND NOOTROPICS

Psychostimulants. Psychostimulants (or psychotonics, psychoanaleptics, psychomotor stimulants) increase mood, the ability to perceive external stimuli, and psychomotor activity. They reduce the feeling of fatigue, increase physical and mental performance (especially when tired), temporarily reduce the need for sleep (drugs that invigorate a tired body are called "doping" - from the English to dope - to give drugs).

Unlike drugs that depress the central nervous system, stimulants are of less importance, since they are devoid of selectivity of action. In addition, stimulation of the central nervous system is accompanied by its subsequent oppression.

Classification of psychostimulants.

1) Means acting directly on the central nervous system:

a) stimulating mainly the cerebral cortex (xanthine alkaloids, phenamine, sydnocarb, methylphenamine, meridol, etc.);

b) stimulating mainly the medulla oblongata (cortex<зол, кордиамин, бемегрид, камфора, двуокись углерода);

c) stimulating predominantly the spinal cord (strychnine).

2) Means acting on the central nervous system reflexively (lobelin, veratrum, nicotine).

It should be remembered that such a division is conditional and, when used in large doses, they can stimulate the central nervous system as a whole.

A typical representative of psychostimulants is PHENAMIN (amphetamine sulfate; tab. on 0, 005; drops in the nose, in the eye 1% solution). Chemically, it is a phenylalkylamine, that is, it is similar in structure to adrenaline and norepinephrine.

Mechanism of action associated with the ability to release norepinephrine and dopamine from presynaptic endings. In addition, phenamine reduces the reuptake of norepinephrine and dopamine.

Phenamine stimulates the ascending activating reticular formation of the brainstem.

pharmacological effects. Effect on the central nervous system. Powerful CNS stimulant. It increases mental and physical performance, improves mood, causes euphoria, insomnia, tremor, and anxiety. In therapeutic doses, it has an awakening effect, eliminates fatigue, and increases physical capabilities. Stimulates the respiratory center and in this regard acts as an analeptic.

Influence on the cardiovascular system. Increases both systolic and diastolic blood pressure. In relation to the hypertensive effect of phenamine, tachyphylaxis is known.

smooth muscle. Phenamine increases the tone of the sphincter of the bladder and relaxes the muscles of the bronchi, but only at high doses. Phenamine reduces appetite (on the hypothalamus), has some anticonvulsant effect (for Petit mal).

Adverse reactions. An undesirable effect is stimulation of the sympathetic nervous system (tachycardia, anxiety, headache, tremor, agitation, confusion, paranoid psychosis, angina attacks).

The drug causes drug dependence, mainly mental, cumulates. Tolerance may develop.

Indications for use:

1) neurotic subdepressions;

2) with narcolepsy, with catalepsy, to prevent pathological drowsiness (narcolepsy);

3) obesity;

4) as an analeptic in case of poisoning with narcotic analgesics.

Pyridrol and meridol are similar to phenamine in terms of their effect on the central nervous system. They do not have undesirable peripheral adrenomimetic effects.

In addition to phenamine, the active psychostimulant sydnocarb (mesocarb) also belongs to the group of phenylalkylsindnonimines. This is an original domestic drug, slightly different in chemical structure from phenamine. In Russian clinics, sidnocarb is currently the main psychostimulant. Compared with phenamine, it is much less toxic and does not show a pronounced peripheral sympathomimetic effect. The psychostimulating effect develops gradually, but it is longer, not accompanied by euphoria and motor excitement. As a rule, there are no tachycardia and a sharp increase in blood pressure. After the action of the drug, the patient does not experience general weakness and drowsiness. The drug is used for various types of asthenia, occurring with lethargy and lethargy, with apathy, decreased performance, hypochondria, increased drowsiness. psychostimulant nootropic analeptic general tonic

The drug is used as a psychostimulant for asthenic and neurasthenic disorders in patients who have undergone intoxication, infection and brain injury, in some forms of psychosis.

In addition, sydnocarb is used to relieve asthenic manifestations after the use of neuroleptics, tranquilizers, as well as in the treatment of patients with alcoholism (stopping of asthenoneurotic reactions during the period of "alcohol withdrawal", to reduce the withdrawal phenomenon).

Sidnokarb is also used in the treatment of children with oligophrenia, accompanied by adynamia, aspontaneity, lethargy, lethargy, asthenia.

Side effects. In case of an overdose, increased irritability, anxiety, loss of appetite are possible. In patients with psychosis, delusions and hallucinations may increase. Sometimes there is a moderate rise in blood pressure.

The drug is available in tablets of 0.005; 0.01; 0.025.

The industry also produces a combined preparation Sidnogluton containing 0.025 sidnocarb and 0.1 glutamic acid. The latter potentiates the psychostimulating effect of sidnocarb.

Xanthine alkaloids and caffeine

Xanthine alkaloids (purine derivatives; metalxanthines), a typical representative of which is caffeine, also belong to the drugs that stimulate mainly the cerebral cortex.

Xanthine alkaloids have been found in several plants throughout the world. Three natural xanthine alkaloids were found in these plants: caffeine, theobromine, theophylline, which are purine bases. When heated with nitric acid, they form a yellow precipitate, hence the term xanthines (Greek - xanthos - yellow). Caffeine is found in tea leaves (Thea sinensis - 2%), coffee seeds (Coffea arabica - 1-2%), cocoa seeds (Theobroma acuminata), etc.

Pharmacological effects. Caffeine has the most pronounced effect on the central nervous system, followed by theophylline and theobromine. The effect of caffeine on higher nervous activity depends on the dose and type of nervous system. In small doses, caffeine increases the activity of the cortex, in large doses it depresses it. In small doses, it helps to speed up the process of thinking and makes it clearer, brings clarity to the train of thought, reduces drowsiness, fatigue and gives the ability to perform intellectually complex tasks. It reduces reaction time, increases motor activity and reinforces conditioned reflexes. These effects can be observed after 1-2 cups of coffee. One cup contains about 1500 mg of caffeine.

Higher doses cause increased excitability, confusion, insomnia, headache, tremor. Theophylline in large doses can even cause convulsions.

Medulla. High doses directly stimulate the respiratory, vasomotor and vagus nerve centers. This leads to increased breathing (increase and deepening), increased blood pressure, tachycardia. True, in large doses, tachycardia and arrhythmias occur, that is, its peripheral effect predominates (cardiac output increases).

Spinal cord. Very large doses increase the reflex excitability of the spinal cord and may lead to clonic convulsions.

Blood vessels. Xanthines have a myotropic effect on blood vessels, but this vasodilating effect is short-lived. It cannot be used to treat peripheral vascular disease.

Xanthines have an ambiguous effect on different vascular regions. The latter helps with migraines. Caffeine has a weak myotropic antispasmodic effect on smooth muscle organs (bronchi, biliary tract). This is of great importance for the clinic. It has long been known that theophylline eliminates bronchospasm in anaphylactic shock, stimulates skeletal muscles, increases their metabolism, eliminates their fatigue.

Caffeine increases basal metabolism. Increases glycogenolysis, causing hyperglycemia. Increases lipolysis, releases adrenaline from the adrenal medulla.

Diuresis. Xanthines increase diuresis. Theophylline is the strongest in this regard, followed by theobromine and caffeine.

Xanthines increase the volume, acidity and pepsin content in gastric juice.

Mechanism of action associated with two areas:

1) xanthines inhibit cyclic nucleotide phosphodiesterase and prevent the transition of cAMP to 5-AMP;

2) cause changes in the distribution of calcium at the level of intracellular processes.

Adverse reactions:

1) Confusion, tremor, headache, insomnia. Ringing in the ears, headache, tachycardia, shortness of breath, arrhythmias. With these reactions, sedatives should be prescribed.

2) Xanthines are contraindicated in patients with peptic ulcer and gastritis.

3) Xanthines develop addiction, to a greater extent - mental dependence, which, however, is not dangerous.

Indications for use. To stimulate mental activity. With fatigue, in the presence of symptoms of asthenia, with migraine, hypotension. With absent-mindedness, impaired attention, exhaustion.

Caffeine is a part of many combined preparations with non-narcotic and narcotic analgesics: citramon, panadol extra, solpadeine, as well as with ergot alkaloids - the drug caffeamine.

NOOTROPS, NOOTROPIC MEDICINES

The term is derived from the Greek - noos - thinking, tropos - aspiration, affinity. Means that have a special effect on the higher integrative functions of the brain, stimulate memory, learning, improve mental activity.

Improving mental, mental activity is the main effect of this group of funds. This is manifested in mental insufficiency associated with organic lesions of the brain.

Mechanisms of action of nootropic drugs at the neurophysiological level: influence on transchannel and other types of polysynaptically evoked potentials recorded on the EEG.

The direction of action of nootropic drugs indicates their pronounced effect on the integrative activity of the brain and the processes of information transmission in the brain. Probably, under the influence of nootropics, various brain formations and information transfer processes in the brain are adjusted to the theta rhythm. The ability of nootropics to improve learning and memory processes is based on the process of increasing the level of spatial synchronization of brain biopotentials.

It should be noted that these drugs do not affect the higher nervous system of healthy animals and the psyche of a healthy person. They normally do not change many behavioral reactions, conditioned reflexes, bioelectrical activity of the brain, motor activity.

The basis of the pharmacotherapeutic action of nootropics at the molecular level in pathological conditions is a beneficial effect on neurometabolism and brain energy. Therefore, this group of drugs is also called psychometabolic stimulants. The main nootropics used in practice mimic the metabolic effects of aminobutyric acid (GABA).

The first drug synthesized abroad in the late 60s in the research laboratory of UCB (Belgium) was named NOOTROPIL. In our country there is an analogue - PIRACETAM (Piracetamum; in the table, 0.2; in amp. 20% solution, 5 ml; capsules - 0.4). It is a classic nootropic agent, therefore it is most often used by doctors of various specialties.

Pharmacological effects. Piracetam (nootropil) is a cyclic derivative of GABA. Nootropics improve the metabolism of brain cells and, above all, the metabolism of glucose and oxygen in them, increase the resistance of cells to hypoxia, improve blood supply to the brain, and communication between the hemispheres. Nootropics increase memory, reduce fatigue. But the effects appear gradually, not immediately after ingestion. Piracetam has anticonvulsant activity, and in recent years, its immunomodulatory effects and immunopotentiating effects have also been described.

Indications for use:

In conditions after a concussion;

In mentally retarded children, with varying degrees of mental retardation; in children with impaired memory, attention, speech;

The elderly, the elderly, in geriatrics to improve memory, mood;

In chronic treatment of drug addicts, alcoholics;

In patients after a stroke;

Nootropics are indicated for enuresis in young children.

In addition, they are prescribed to potentiate the effects of immunostimulants.

Aminalon is a GABA drug. Obtained synthetically. GABA is an inhibitory mediator that plays an important role in the metabolic processes of the nervous tissue. The drug stimulates tissue respiration, activates the enzymes of the Krebs cycle, improves the utilization of glucose by neurons.

Indications for use: vascular diseases of the brain, mental retardation in children.

Side effects of nootropics: brain stimulation can lead to irritability, sleep disturbance, moodiness, anxiety in children, increased blood pressure, sexual excitability. Therefore, they are used in courses (for 2-3 weeks).

In recent years, the group of nootropics has expanded significantly. This is the Hungarian drug Cavinton (Gedeon Rihter), cerebrolysin, etc.

Cavinton (table. 0.005; amp. 0.5% solution, 2 ml). Ethyl ester of apovinkaminic acid (vinca minor alkaloid preparation).

Cavinton has the following effects:

1) dilates the vessels of the brain;

2) enhances cerebral blood flow, improves blood supply to the brain with oxygen;

3) improves the utilization of glucose by neurons, promotes the accumulation of cAMP, ATP;

4) reduces platelet aggregation;

5) increases the content of catecholamines in the central nervous system.

It is used primarily in neurology for:

1) neurological and mental disorders associated with disorders of cerebral circulation (stroke, trauma, sclerosis);

2) memory disorders;

3) dizziness;

4) aphasia;

5) hypertensive encephalopathy;

6) atherosclerosis of retinal vessels, i.e. in ophthalmology, etc.;

7) hearing loss of toxic genesis.

ANALEPTICLES (ANALEPTICS)

Analeptics (from the Greek analeptikos - restoring, strengthening) mean a group of drugs that primarily stimulate the vital centers of the medulla oblongata - vascular and respiratory. In high doses, these drugs can excite the motor areas of the brain and cause convulsions.

In therapeutic doses, analeptics are used for weakening vascular tone, for respiratory depression, for infectious diseases, in the postoperative period, etc.

Currently, the group of analeptics according to the localization of action can be divided into three subgroups:

1) Preparations directly, directly activating (revitalizing) the respiratory center:

Bemegrid;

Etimizol.

2) Means that reflexively stimulate the respiratory center:

Cititon;

Lobelin.

3) Means of mixed type of action, having both direct and reflex action:

Cordiamin;

Camphor;

Corazol;

Carbon dioxide.

Bemegrid (Bemegridum; in amp. 10 ml of 0.5% solution) is a specific barbiturate antagonist and has a "revitalizing" effect in case of intoxication caused by drugs of this group. The drug reduces the toxicity of barbiturates, relieves respiratory and circulatory depression. The drug also stimulates the central nervous system, so it is effective not only for barbiturate poisoning.

Bemegrid is used for acute poisoning with barbiturates, to restore breathing at the exit from anesthesia (ether, halothane, etc.), to remove the patient from a severe hypoxic state. Enter the drug intravenously, slowly until the restoration of breathing, blood pressure, pulse.

Side effects: nausea, vomiting, convulsions.

Etimizol occupies a special place among direct-acting analeptics.

Etimizol (Aethimizolum; in tab. 0, 1; in amp. 3 and 5 ml of 1% solution). The drug activates the reticular formation of the brain stem, increases the activity of the neurons of the respiratory center, enhances the adrenocorticotropic function of the pituitary gland. The latter leads to the release of additional portions of glucocorticoids. At the same time, the drug differs from bemegrid by a slight inhibitory effect on the cerebral cortex (sedation), improves short-term memory, and promotes mental work. Due to the fact that the drug promotes the release of glucocorticoid hormones, it has a secondary anti-inflammatory effect.

Indications for use. Etimizol is used as an analeptic, a respiratory stimulant in case of poisoning with morphine, non-narcotic analgesics, in the recovery period after anesthesia, with lung atelectasis. In psychiatry, its sedative effect is used in states of anxiety. Given its anti-inflammatory effect, it is prescribed for the treatment of patients with polyarthritis and bronchial asthma, as well as an anti-allergic agent.

Side effects: nausea, dyspepsia.

Reflex acting stimulants are N-cholinomimetics. These drugs are cytiton and lobelin. They excite H-cholinergic receptors in the carotid sinus zone, from where afferent impulses enter the medulla oblongata, thereby increasing the activity of the neurons of the respiratory center. These funds act for a short time, within a few minutes. Clinically, there is an increase and deepening of breathing, an increase in blood pressure. The drugs are administered only intravenously. It is used for the only indication - for carbon monoxide poisoning.

In mixed-type agents, the central effect (direct excitation of the respiratory center) is supplemented by a stimulating effect on the chemoreceptors of the carotid glomerulus (reflex component). These are, as stated above, cordiamine and carbonic acid. In medical practice, carbogen is used: a mixture of gases - carbon dioxide (5-7%) and oxygen (93-95%). Assign in the form of inhalations, which increase the volume of breathing by 5-8 times.

Carbogen is used for overdose of general anesthetics, carbon monoxide poisoning, and neonatal asphyxia.

Cordiamin, a neogalenic drug, is used as a respiratory stimulant (it is prescribed as an official one, but it is a 25% solution of nicotinic acid diethylamide). The action of the drug is realized by stimulation of the respiratory and vasomotor centers.

Assign for heart failure, shock, asphyxia, intoxication.

DRUGS THAT STIMULATE PRIMARY FUNCTIONS OF THE SPINAL CORD

In this group, essentially two drugs are used: strychnine and securinine.

Strychnine (Strichninum; powder; in amp. 1 ml of 0.1% solution) is the main alkaloid of chilibukha seeds (vomit).

In medical practice, nitrate salt is used - strychnine nitrate.

In addition to strychnine, dry chilibukha extract and chilibukha tincture are also used.

Strychnine and other preparations of chilibukha excite the central nervous system and, first of all, increase reflex excitability. The reflex reactions of the patient become more generalized. Strychnine improves the activity of the sense organs (vision, taste, hearing, tactile sensation), excites the vasomotor and respiratory centers, tones the skeletal muscles, myocardium.

Strychnine preparations are used as tonics with a general decrease in metabolic processes, rapid fatigue, and hypotension. weakening of cardiac activity due to intoxication and infections, with some functional disorders of the visual apparatus, with paresis and paralysis (of diphtheria origin, for example), with atony of the stomach.

Side effects occur with an overdose and are manifested by tension in muscle groups (facial, occipital), difficulty breathing, convulsions.

The drug securinin, obtained from the herb securenegi, is similar in nature to strychnine, but less active (10 times). Used for asthenic conditions, paresis and paralysis, with hypo- and asthenic form of neurasthenia, with impotence due to functional disorders.

GENERAL TONING AGENTS (ADAPTOGENS)

Preparations of this group by origin can be divided into means of plant and animal nature. Herbal remedies are more commonly used, namely various herbal preparations of plants (ginseng root extracts, extracts of leuzea, Rhodiola rosea or golden root, eleutherococcus, tincture of zamaniha, lemongrass, Transbaikal skullcap, aralia). Of the means of animal origin, we can name the drug pantocrine, obtained from reindeer antlers, and produced as a neogalenic drug for oral (in drops) and parenteral administration.

The pharmacological action of these drugs is due to the content of salonin glycosides-ginsenoids, essential oils, sterols, peptides and minerals in them. These biologically active substances bring a stimulating effect on the central nervous system, increase efficiency, regulate the functioning of the endocrine glands, moderately reduce blood pressure, the level of atherogenic lipids (cholesterol) and glucose in the blood, and activate the activity of the adrenal glands.

The use of these funds leads to a decrease in the incidence of acute respiratory infections, an increase in the patient's resistance to viral and other infections, and an improvement in well-being and appetite.

These drugs are indicated for mental and physical overstrain during the period of convalescence after long and serious illnesses, in particular, of an infectious nature (dysentery, typhoid and viral infections, etc.). The drugs are also prescribed to cancer patients in the rehabilitation period, after courses of chemotherapy and radiation exposure.

As a rule, drugs are prescribed for a long time, for 1-2 months. Acceptance of adaptogens is advisable in the morning, after breakfast. The appointment of these funds in the afternoon is not shown, since sleep disturbance is possible in the form of difficulty falling asleep. Individuals may experience hypersensitivity to certain drugs.

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