Psychostimulants increase physical and mental performance. restore functional activity in case of fatigue, apathy, psychomotor retardation. hypochondria. Drugs used to invigorate healthy people are called doping. to dope - give drugs).

There are psychomotor stimulants and psychostimulants-adaptogens.

Romantic legends tell about the discovery of shrubs containing psychostimulants (tea, coffee, mate). Bodydarma, the son of an Indian Raja and a preacher of Buddhism, traveled to China. He subjected himself to hardships and did not sleep for a long time in order to achieve nirvana after death. However, after three years of testing, fatigue overcame the prince, and he unexpectedly fell asleep. After awakening, Bodydarma cut off his eyelids in despair. In the place where drops of the unfortunate young man’s blood fell, a tea bush grew green, the leaves of which give vigor.

The discoverer of the psychostimulating properties of coffee was the abbot of a monastery in Arabia. He learned from local shepherds that goats, after eating coffee fruits, become very excited and run away into the desert. The abbot prepared a drink from these fruits and began to give it to the monks to increase vigor during night services. In 1819, Runge isolated caffeine, and soon theophylline and theobromine were obtained.

Substances of the phenylalkylamine group are found in katha leaves. The homeland of this shrub is Ethiopia. Somalia, Arabia. From katha, the Bedouins prepare a drink (Arabic tea), which gives vigor and a surge of strength. In 1887, Edelano synthesized an analogue of the alkaloid cathine, amphetamine. Initially, amphetamine found use as a vasoconstrictor for rhinitis and arterial hypotension, then its psychostimulant effect was noticed. During World War II, the amphetamine drug phenamine was taken by intelligence officers to improve performance in extreme situations.

Psychomotor stimulants

Psychomotor stimulants increase physical and mental performance by accelerating the pace of activity. They give vigor, self-confidence, lively interest in the environment, initiative, and delay the need for sleep by 10-12 hours. According to subjective assessments, the flow of thoughts accelerates, associations arise more easily, and the performance of mental operations becomes easier.

Animals respond to the introduction of psychostimulants by increasing exploratory activity, reduced fatigue, and accelerating the development of conditioned reflexes.

The clearest and most reliable results in the form of improved performance were obtained against a background of fatigue. The psychostimulating effect is easy to detect with drowsiness, the action of substances that depress the central nervous system, and low performance. On the contrary, psychostimulants do not improve performance indicators or even worsen them with a sufficient degree of wakefulness, in people with a high level of memory and operator activity, and in well-trained animals.

Impact on neurophysiological processes

Increase brain alertness

Psychostimulants reduce fatigue and drowsiness, improve vision, hearing, and touch. Under the influence of psychostimulants, cortical neurons rearrange impulses to an optimal frequency, providing a flexible response to afferent signals. On the EEG after the introduction of psychostimulants, desynchronization (excitement, alertness, tension) is recorded.

These effects are due to activation of the reticular formation of the midbrain and nonspecific nuclei of the thalamus, which is accompanied by increased excitation in the cerebral cortex.

Psychostimulants suppress REM sleep, with compensation possible during wakefulness in the form of hallucinations and waking dreams. Increasing emotional and motivational response

After taking psychostimulants, a surge of energy occurs. a feeling of ease and efficiency of work, initiative, desire to work, improved mood. There may be anxiety, internal tension, excessive self-confidence, rudeness, and euphoria. In mental illness, psychostimulants enhance delusional ideas. hallucinations, mania, aggravate antisocial behavior.

The improvement in emotional and motivational response is based on the activating effect of psychostimulants on the limbic system and hypothalamus.

Revitalizing movements

Psychostimulants enhance the excitatory effect of the reticular formation and weaken the inhibitory effect of the nigrostriatal system on the spinal cord. They increase motor activity, sometimes causing motor fussiness, tendon hyperreflexia, extrapyramidal muscle rigidity. They disrupt kinesthesia (Greek. kineo - move, a" lsthesis - sensation, feeling) - control over the maximum permissible load: a person, without feeling tired, continues to work until exhaustion.

Influence on psychophysiological processes

Psychostimulants increase vigilance to emergency situations, short-term memory, and have less effect on long-term memory. By accelerating the search for solutions, they improve the performance of stereotypical, automatic mental work. During creative work that requires logical analysis and solving complex problems, they increase the number of errors, cause distraction, “jumping thoughts,” and decrease patience.

Thus, against the background of mild fatigue, psychostimulants mobilize the remaining functional and energy reserves, which allows you to continue working for a short period of time. With severe fatigue, they deplete the body. These are means for single or short-term use in emergency situations, when the risk of not performing the load at the maximum pace is higher than the danger of taking psychostimulants, and there is also the possibility of proper rest and nutrition to restore the energy fund.

Features of action and use of psychomotor stimulants

Psychomotor stimulants are classified into 3 groups based on their chemical structure and pharmacological properties.

Phenylalkylamine derivatives

PHENAMIN - mixture d- and /-isomers of amphetamine. It is structurally similar to ephedrine, but lacks hydroxyls in the aromatic ring and side chain. Penetrates well into the brain. It excites the reticular formation, the thalamus, the hypothalamus, and the limbic system, as it promotes the release of dopamine, norepinephrine and serotonin, inhibits the neuronal uptake of these neurotransmitters, and inhibits MAO. Increases the release of adrenaline from the adrenal glands.

Phenamine is a strong psychostimulant. Already 30-60 minutes after taking it orally, a surge in performance occurs. Phenamine promotes macroerg energy consumption, enhances glycogenolysis and lipolysis, which increases the delivery and utilization of glucose and free fatty acids. However, it uncouples oxidation and phosphorylation, increases the organs’ need for oxygen, and disrupts ATP synthesis. Against the background of the action of phenamine, energy is spent uneconomically and is dissipated in the form of heat with an increase in body temperature. A negative aftereffect (exhaustion) quickly sets in, requiring rest and proper nutrition for several days. Work against a background of exhaustion ends in death from cardiac paralysis.

Phenamine also has other effects:

It has a strong anorexigenic effect, suppressing the hunger center and activating the satiety center in the hypothalamus (this has a positive effect when performing work with the inability to eat);

Tones the respiratory center;

Dilates the pupils, causes tachycardia, arrhythmia, increases stroke and minute blood volumes, blood pressure;

Increases the blood levels of glucose, pyruvate, lactate, and fatty acids, causing metabolic acidosis.

Phenamine is currently not prescribed for medical reasons due to the danger of undesirable effects (rapid development of aftereffects, disorders of the cardiovascular system, mental dependence). The storage and dispensing of phenamine is carried out with the same restrictions as other List A drugs that cause drug addiction.

In 10-15% of people, taking phenamine is accompanied by a paradoxical reaction: depression, drowsiness, depression, anger, and low performance are observed. Before prescribing phenamine, it is necessary to check the individual sensitivity of the patient.

In acute poisoning with phenamine (toxic doses are only 1.5-3 times higher than therapeutic doses), anxiety appears, developing into panic, aggressiveness and motor restlessness with unmotivated actions. Less commonly, acute psychosis occurs with auditory hallucinations, delusions and suicidal attempts. Adrenomimetic symptoms are pronounced - wide pupils, moist skin, dry mucous membranes, hyperthermia, tachycardia, arrhythmia, chest pain, arterial hypertension. In severe cases, seizures and coma develop. Treatment for poisoning includes gastric lavage, the use of tranquilizers and antipsychotics. To stabilize blood pressure and cardiac activity, nitroglycerin or nifedipine is prescribed sublingually, α-blockers (tropafen, phentolamine), α,β-blockers (labetolol), clonidine or sodium nitroprusside are injected into a vein. Acute cerebrovascular accidents are treated with nicergoline or nimodipine. For arrhythmia, venulidocaine and magnesium sulfate are infused. The elimination of phenamine can be accelerated by acidifying the urine (ascorbic acid, ammonium chloride).

Phenamine belongs to the class of hallucinogens that cause mental dependence. Symptoms of phenamine euphoria are a surge of strength, a need for active and energetic activity, a deceptive feeling of noticeably increased performance combined with a significantly less pronounced improvement in objective performance indicators or the absence of such improvement. Psychostimulation lasts several hours and is replaced by a depressed mood.

Subsequently, hallucinatory-paranoid psychosis develops with the expression of delusional ideas, stereotypical visual, auditory and tactile hallucinations (patients remove imaginary insects and worms from the body). Phenamin psychosis without a detailed history cannot be distinguished from the paranoid form of schizophrenia.

The amphetamine derivative methylenedioxymethamphetamine called ecstasy has become popular in American colleges due to the idea that it increases intuition and self-awareness. This hallucinogen, suppressing the function of serotonergic neurons of the central nervous system, causes agitation, hallucinations, panic, hyperthermia, clenching of teeth, tachycardia, and muscle pain.

Psychostimulants are a group of psychotropic drugs that increase mental and physical performance, improve the ability to perceive external stimuli (sharpen vision, hearing, etc., speed up responses), improve mood, relieve fatigue, invigorate and temporarily reduce the need for sleep.

Amphetamines (amphetamine, dextroamphetamine and methamphetamine) were first synthesized at the end of the 19th century. Their medical use began in the 20s of the XX century. and has been associated with the treatment of cold symptoms, obesity, narcolepsy, and attention deficit hyperactivity disorder in children. These drugs were used as stimulants during World War II on both sides of the front. In America, it was prescribed to treat heroin addiction until the 1960s, which led to a surge in amphetamine abuse. In the USSR, amphetamines were produced starting in the 40s; they were used in the medical field to a limited extent and were inaccessible. Currently, amphetamines are practically not used in clinical practice due to severe side effects and a high risk of developing drug dependence. According to the World Health Organization classification, amphetamines are classified as narcotic drugs.

Classification of psychostimulants.

1) Amphetamines:

Arylalkylamine (phenylalkylamine) derivatives: amphetamine.

Phenylalkylpiperidine derivatives: methylphenidate, Pemoline (not registered in Russia).

2) Sydnone imines (phenylalkyl sydnone imine derivatives): mesocarb, feprosidnine.

3) Methylxanthine derivatives: caffeine.

4) Drugs of other pharmacological groups with a psychostimulating effect: salbutiamine, ethylthiobenzimidazole hydrobromide (Bemitil), deanol aceglumate, meclofenoxate, Semax.

The psychostimulant effect of amphetamines is based on the release of norepinephrine and dopamine from the vesicular pool of presynaptic nerve endings in the central nervous system, as well as inhibition of their reuptake. Amphetamines inhibit catechol-o-methyltransferase, an enzyme that catalyzes the breakdown of catecholamines at adrenergic synapses. These mechanisms determine not only the psychostimulating, but also the peripheral adrenomimetic effect with various vegetative manifestations (increased blood pressure, tachycardia, extrasystole, etc.).

Caffeine competitively inhibits the activity of phosphodiesterases, promoting the intracellular accumulation of cAMP and cGMP and the activation of various types of intracellular metabolism in the central nervous system, heart, smooth muscle organs, adipose tissue, and skeletal muscles; stabilizes the transmission of nervous excitation in dopaminergic, noradrenergic and cholinergic synapses of the cortex, hypothalamus and medulla oblongata. The mechanism of action of caffeine involves competition for receptors with adenosine, which limits the spread of excitation in the central nervous system.

The psychostimulating effect is manifested by a decrease in lethargy, drowsiness, a feeling of cheerfulness, and an increase in physical and intellectual performance. This effect is most pronounced in phenylalkylamine derivatives (amphetamine), less so in methylphenidate, mesocarb, and even weaker in caffeine. Psychostimulants from the group of arylalkylamine derivatives also have a moderate antidepressant effect and reduce appetite.

Peripheral effects are most pronounced in amphetamine, to a lesser extent in methylphenidate, caffeine, and slightly in mesocarb. Amphetamine and caffeine stimulate cardiac activity (increased heart rate, increased heart contractions). Amphetamine causes peripheral vasoconstriction. The effect of caffeine on blood vessels and blood pressure is ambiguous: it has a vasodilator effect on the vessels of skeletal muscles, heart, kidneys, skin and a vasoconstrictor effect on the vessels of the brain and abdominal organs. Caffeine increases the tone of venous vessels and has a diuretic effect. Amphetamine and caffeine have a bronchodilator effect.

The most typical side effects of psychostimulants are increased excitability, anxiety, sleep disturbance, nausea, tachycardia, arrhythmia, and increased blood pressure. While taking amphetamines and sydnonimines, a decrease in appetite, exacerbation of delusions and hallucinations are also possible; with long-term use of amphetamine - the development of drug dependence, severe neuropsychiatric disorders, schizophrenia-like psychosis.

Psychostimulants are prescribed orally (with the exception of sodium benzoate caffeine), are generally well absorbed from the gastrointestinal tract and penetrate the BBB. To prevent sleep disturbances, take in the first half of the day (before 15:00).

Psychostimulants reduce the effect of sedatives and enhance the effect of drugs with central nervous system stimulating properties. When used simultaneously with antipsychotics, exacerbation of schizophrenia is possible. Psychostimulants cannot be combined with MAO inhibitors.

The main indications for the use of psychostimulants are a decrease in physical and mental performance, drowsiness, lethargy, lethargy, apathy in asthenic conditions of various origins, depression, incl. depression with symptoms of social alienation or psychomotor retardation in elderly patients, the presence of severe somatic pathology, chronic alcoholism, narcolepsy. These drugs reduce the side effects of tranquilizers, antipsychotics, and sleeping pills. They are intended for a short-term increase in mental and physical performance in healthy individuals in extreme, stressful situations (caffeine, mesocarb are used, and amphetamine is used for a short time in exceptional situations). For attention deficit hyperactivity disorder in children (in the USA and a number of Western countries), methylphenidate and amphetamine are used.

Psychostimulants are contraindicated in cases of hypersensitivity, agitation, anxiety, sleep disorders, arterial hypertension, atherosclerosis, and organic diseases of the cardiovascular system. Amphetamine is contraindicated in case of liver failure, and caffeine in case of glaucoma.

In domestic medical practice, mesocarb and caffeine are mainly used (including as part of combination drugs).

Drugs

Drugs - 162 ; Trade names - 11 ; Active ingredients - 4

Active substance	Trade names

The effects of drugs in this group develop quickly (within tens of minutes after use) and are highly dependent on the dosage.

A characteristic effect is the ability to weaken the effect of hypnotics and sedatives and reduce appetite. As a rule, they also cause increased cardiac activity, increased blood pressure, stimulate breathing and dilate the bronchi. Most psychomotor stimulants activate the sympathetic system, a characteristic sign of this is strong dilation of the pupils.

An overdose causes fussiness, inability to concentrate, talkativeness, the need to move and constantly change position. At an even higher dose, unpleasant physiological effects occur: nausea, dizziness, tachyarrhythmia, dry mouth, chills, etc.

A small dose of psychostimulants can cause, especially in a tired or exhausted person, so-called “paradoxical reactions” - drowsiness, apathy, a feeling of melancholy and a sharp decrease in mood.

Amphetamines (Phenamine, Speed)

Amphetamines are stimulants of the central nervous system. They do not produce energy like food, but rather use the energy that is already in the body. They are the closest synthetic analogues of the psychostimulant cocaine.

Amphetamines (phenylisopropylamines) are divided according to their chemical properties into:

u Salts or racemates.

u Dextroamphetamines.

u Methamphetamines (phenylmethylisopropylamines) are the most powerful.

Pure amphetamines are white or slightly creamy, finely crystalline powders that are soluble in water.

Dosage of amphetamines: amphetamines do not become an addiction, but become a habit and its apparent harmlessness leads to the fact that the dose is constantly increasing. Long-term use of it causes paranoia and real mental disorientation. This is especially true for mephedrine. Amphetamine is a nasty business, whether it comes in pill or powder form, and things can be just as bad, if not worse, than with heroin.

Methamphetamine dosage (single doses). 3-10 mg - mild effect, vigor, increased attention, performance, relieving fatigue and drowsiness. 10-25 mg - average, decreased attention, increased motor activity, pronounced mental agitation, peripheral effects, slight increase in blood pressure and increased heart rate. 25-50 mg - strong, strong mental arousal, physical activity, noticeable increase in blood pressure, tachycardia, duration of action up to 2 days; 50-100 mg - toxic, strong mental arousal, increased anxiety and suspiciousness, strong increase in blood pressure, possible arrhythmia, long-term effect.

Single doses of amphetamines are approximately 2-3 times greater than for methamphetamine.

Feelings when taking amphetamines: After taking amphetamines, an active state occurs within half an hour to an hour. The uplift in mood is combined with a pronounced increase in mental and physical activity, a surge of energy, self-confidence, one’s strengths and capabilities.

Increased mental and physical performance is confirmed by objective data. The need for rest and sleep disappears. With large doses, active wakefulness lasts 2-3 days, with small doses - 4-8 hours. There are differences in the effects of the drugs. Amphetamines, unlike methamphetamine, cause a paradoxical reaction in ten percent of people in the form of drowsiness, lethargy, and decreased performance. Amphetamines end their effects abruptly; when administered intravenously, a “high” is observed. Methamphetamine has a stronger effect, but is milder and lasts longer.

Amphetamines often end their effects suddenly. Getting up after 6-8 hours is sharply replaced by exhaustion, a feeling of fatigue, and irritability. The effect of methamphetamine passes slowly and almost imperceptibly: after a short 2-3 hour rest, performance and well-being remain high. Frequent use of amphetamines without breaks causes exhaustion of the nervous system and a rapid increase in tolerance.

Sidnocarb

Sidnocarb and phenamine belong to the group of amphetamines in terms of their chemical structure, and in terms of their pharmacological action they belong to psychostimulants. These are drugs that increase mental activity, causing increased clarity of consciousness, brightness of perception, mental performance, preventing drowsiness and falling asleep.

Sidnocarb is widely used to treat various conditions of mental asthenia - weakness, lack of desire to work, drowsiness. If these symptoms are a manifestation of depression, then the use of psychostimulants alone is ineffective, although use in combination with antidepressants may be justified.

In healthy people, it is possible to use sydnocarb in case of need to perform some work in a short time to eliminate the feeling of fatigue and drowsiness, although after this sufficient rest, of course, is necessary, since it is the feeling of fatigue that is eliminated through the use of energy reserves.

Unlike phenamine, sidnocarb has less pronounced stimulation with a single dose, and its gradual increase is observed from dose to dose.

Sidnocarb is usually well tolerated, does not cause dependence or addiction, and its use may increase blood pressure, decrease appetite, and also hyperstimulation phenomena.

Caffeine is found in tea, coffee, mate leaves, as well as guarana and kola nuts. Produced as a by-product of decaffeinated coffee.

Toxic dose: The confirmed lethal dose is 10 g, although there is one documented case of survival after an injection of 24 g. In young children, ingestion of 35 mg/kg may cause moderate toxicity. Children metabolize caffeine very slowly. Theophylline, which may be contained in medications for bronchial asthma, is also dangerous for them.

Overdose symptoms: acute caffeine poisoning produces early symptoms of anorexia (lack of appetite), tremor (trembling, including fingers) and anxiety. This is followed by nausea, tachycardia, hypertension and confusion. Severe intoxication can cause delirium tremens, convulsions, supraventricular and ventricular tacharhythmias, hypokalemia and hyperglycemia. Chronic use of high doses of caffeine can lead to nervousness, irritability, anger, persistent tremors, muscle twitching, insomnia and hyperreflexia. When testing blood: concentrations of 1..10 mg/l, concentrations of 80 mg/l are fatal.

Caffeine increases circulating levels of fatty acids and has been shown to promote their oxidation and utilization. For years, caffeine has been used by long-distance runners to enhance fat metabolism. In this regard, it is quite effective for those who are not yet used to it and can help get rid of excess fat. However, caffeine does not suppress appetite, but rather stimulates it. In addition, it increases the secretion of gastric juice, so consuming caffeine without food can lead to gastritis and even peptic ulcers.

How much caffeine is in different products? According to the American National Soft Drinks Association, a 340 ml can of soda contains the following amounts of caffeine (in milligrams):

Variations in the amount of caffeine per 1 cup of coffee or tea are very large, even if the drink is prepared by the same person, with the same equipment, recipe, ingredients, day after day.

Other names are coca, coconut, coke, Si, Tse. Cocaine is an extract from the leaves of a plant native to South America. Erythroxylum Coca

Cocaine belongs to the group of psychomotor drugs. It starts working almost instantly - immediately after the powder hits the nasal mucosa, a “high” occurs - a flash of high. Motor activity increases sharply, the brain thinks “faster,” and there is a general increase in mental and physical strength. The effect is not felt for long - 10..15 minutes, and then depression sets in, which lasts about 30-40 minutes.

The dosage depends on the duration of consumption. The starting dose is two “tracks”.

Long-term use of cocaine causes paranoia, deafness, delirium, indigestion and uncontrollable convulsions. In addition, there is a very high probability of problems with the nasal mucosa or hardening of the veins (depending on the method of administration); sleep phase disturbance (a person stops getting enough sleep). There is an effect on potency.

The most unpleasant side effect of psychostimulants is the “recoil” in the form of a decrease in motivation, performance and mood, which can lead to the formation of psychological dependence if repeated doses of the stimulant are used to overcome these consequences.

Crack, a type of cocaine that is smoked, is called an express drug because of its low price: a dose costs between $10 and $15 on the street. At the same time, crack is the most addictive drug; it is 10 times more dangerous than cocaine. Since it enters the bloodstream through the lungs, it reaches the brain in a matter of seconds, meaning instant addiction. As with cocaine use, a state of euphoria occurs, but it lasts only 5-20 minutes. Then severe depression sets in. The person is caught instantly, the next dose is needed immediately, in a few minutes.

Dissociatives

Dissociative are drugs (of different chemical classes - phencyclidine anesthetics, anticholinergics, etc.) that can cause “separation” (dissociation) of consciousness from the physical body and / or temporarily disrupt the integrity of the psyche, “dispersing” consciousness. The effects of these substances are varied, most often they are unpleasant, but some people consider the experience gained from their use to be unique and very valuable.

Dissociatives, as a rule, do not cause physiological dependence. Psychological dependence is possible, but extremely rare, because The use of drugs of this class for the vast majority of people is usually episodic.

They claim that ketami is an uninteresting and unpleasant drug. For some, it separates the mind from the body too much; for others, ketamine is a powerful and flexible drug whose effects can be easily modulated by varying the dose and environment.

Most agree that ketamine is well tolerated, with little discomfort the next day and a mild “hangover.” The setting plays a critical role in the manifestation of its effects. Most believe that ketamine should not be used without some experience with psychedelic drugs.

After the drug begins to act, fragmentation will occur - the world falls into pieces and begins to rotate, without causing dizziness. The music falls to pieces. With sufficient dosage, at some point ordinary reality and the body disappear. Events beyond this point vary greatly, but most speak of alternate spaces, loneliness, visions of the past and future, and strange machines of all kinds.

It is very difficult to communicate under the influence of ketamine because... it is impossible to see and hear others. Some visions are extremely difficult, and some are frightening, but this fear usually does not remain after, so these experiences cannot be called truly terrible. The return to normal reality occurs in the reverse order; normal vision is gradually acquired. The effects continue gently for about an hour, gradually subsiding.

Taren is an antidote to OPA (organophosphorus compounds) and is included in the military individual first aid kit.

When used internally (in an unsent state) of 2 capsules, a clear hallucinogenic effect is observed, expressed in confusion, memory loss and the presence of vivid visual hallucinations.

The drug begins to act 20-30 minutes after administration, the effect lasts 4-5 hours. Somatic manifestations: dry mouth and throughout the body, dilated pupils.

Taren is tolerant - to achieve the same effect, the dose must be increased. There is no psychological craving for further use, because there is no euphoria and repetition of sensations.

Medicines and drugs of the psychostimulant group activate the mental activity of the body, stimulating higher functions and accelerating the thinking process. Under their influence fatigue is relieved quickly, drowsiness and lethargy disappear. Using psychotropic substances motivation appears and performance increases, a person under their influence becomes more sociable and sociable.

Along with improved mood in a person under psychostimulants the ability to perceive external stimuli improves, vision, hearing, and color discrimination are enhanced. To some extent, psychotropic substances improve coordination of movements, increase endurance and strength.

Most drugs from this group cause drug addiction, which is difficult to get rid of. Psychostimulants include medications, drugs and commonly available drinks - tea, coffee, Coca-Cola.

Best video:

List of psychostimulants

;
Methamphetamine;
MDMA (methylenedioxymethamphetamine);
;
Cathinone;
Ephedrine and pseudoephedrine;
Methcathinone (ephedron);
Phenylpropanolamine;
Methylone;
;
Flephedrone;
MDPV (methylenedioxypyrovalerone);
Oxazoline;
Phentermine;
Amfepramone;
Aminorex;
4-Methylaminorex
Pemoline;
Ampakines;
Norepinephrine;
Caffeine;
Nicotine.

Mechanism of action and use of psychostimulants

Psychotropic substances act at the level of brain cells. They release certain substances from nerve endings and block their reuptake. Because of this, the excitatory processes of the brain intensify.

For example, the mechanism of the stimulating effect of caffeine leads to the accumulation of cAMP and cGMP in cells, which causes adrenaline-like effects.

Psychostimulants are used in medicine to treat ADHD (attention deficit hyperactivity disorder) in children, and also treat depression and narcolepsy.

The use of psychostimulants will be effective in treatment apato-abulic and stuporous states, neurotic disorders with lethargy and asthenic conditions, accompanied by lethargy and drowsiness. Psychotropic drugs help improve mood and interest in life in seriously somatic patients who have severe apathy and lack of interest in life.

For example, under the influence of amphetamine, the negative symptoms of schizophrenia do not completely, but practically disappear.

One of the most popular psychostimulants, caffeine is used not only to eliminate drowsiness and increase mental and physical performance, but also in case of poisoning with drugs that depress the central nervous system.

Consequences of psychostimulant abuse

Excessive use of psychostimulants causes a number of complications, which can be irreversible and lead to fatal outcome.
Namely:
Mental dependence;
Anorexia;
Irritability;
Insomnia;
Tachycardia;
High blood pressure;
Stimulant psychosis.

In mentally ill people, psychotropic substances cause an exacerbation of mental symptoms; they should also not be used by people with Tourette syndrome, since psychostimulants will only worsen the course of the disease.

If the article “List of psychostimulant drugs” was useful to you, do not hesitate to share the link. You may save someone's life with this simple solution.

(psychotonics) improve mood, psychomotor activity, and the ability to perceive external stimuli. These drugs reduce the feeling of fatigue, increase physical and mental performance (especially when tired), and temporarily reduce the need for sleep.

There are synthetic psychostimulants and general tonics of plant origin, which have a milder effect on the central nervous system (ginseng preparations, Rhodiola rosea, Eleutherococcus senticosus, etc.). The latter exhibit adaptogenic (stimulate the immune system, improve tolerance to adverse environmental factors) and some psychostimulating effects, which are inferior in severity to synthetic psychostimulants.

Chemically psychomotor stimulants are classified as follows:

1. Phenylalkylamines (amphetamine).
2. Piperidine derivatives (pyridrol, meridyl).
3. Derivatives of sydnonimine (mesocarb).
4. Methylxanthines (caffeine).

Phenylalkylamines: amphetamine

A typical psychomotor stimulant is amphetamine (phenamine). The mechanism of the central action of this drug is explained by its ability to release mediators from presynaptic nerve endings. The released norepinephrine, dopamine and serotonin stimulate the corresponding types of receptors in the central nervous system (CNS). In addition, amphetamine slightly reduces the neuronal uptake of these neurotransmitters and inhibits monoamine oxidase (MAO). Amphetamine also has some direct effects on adrenergic receptors.

Characteristic of amphetamine is its anorexigenic effect: appetite is suppressed as a result of suppression of the activity of the hunger center and stimulation of the satiety center in the hypothalamus. The drug has a direct stimulating effect on the respiratory center, which manifests itself mainly against the background of its inhibition. In this case, amphetamine acts as an analeptic.

Amphetamine acts not only on the central nervous system, but also on peripheral innervation. The drug has an indirect stimulating effect on α- and β-adrenergic receptors, acting as a sympathomimetic. Amphetamine increases the release of adrenaline from the adrenal glands. Peripheral properties manifest themselves mainly in increased blood pressure (BP). With prolonged use of amphetamine, tolerance develops. In addition, the drug has the ability to accumulate.

In 10-15% of people, taking amphetamine is accompanied by a paradoxical reaction: depression of psychomotor activity, drowsiness, depression, anger, and decreased performance are observed. In this regard, before prescribing an amphetamine, the individual sensitivity of the patient should be checked; for this purpose, as a rule, half the usual dose is administered.

In medical practice, amphetamine can be used for narcolepsy, neurotic subdepression, to increase performance in case of fatigue (with the possibility of subsequent proper rest), as an analeptic in case of poisoning with narcotic-type substances. It is not advisable to use amphetamine to reduce appetite, since it causes agitation, increases blood pressure and is a potentially dangerous drug in relation to the development of drug dependence.

Amphetamine poisoning

Toxic doses of amphetamine are only 1.5-3 times higher than therapeutic doses. In acute amphetamine poisoning, a feeling of anxiety appears, developing into panic, aggressiveness and motor restlessness with unmotivated actions. Less commonly, acute psychosis occurs with auditory hallucinations, delusions and suicidal attempts. Adrenomimetic symptoms are pronounced - wide pupils, moist skin, dry mucous membranes, hyperthermia, tachycardia, arrhythmia, chest pain, arterial hypertension. In severe cases, seizures and coma develop.

Treatment for poisoning includes gastric lavage, tranquilizers and antipsychotics are also used. To stabilize blood pressure and cardiac activity, nitroglycerin or nifedipine, α-blockers (tropafen, phentolamine), α,β-blockers (labetalol), clonidine (clonidine) or sodium nitroprusside are prescribed. Acute cerebrovascular accidents are treated with nicergoline or nimodipine. For arrhythmia, it is advisable to use lidocaine and magnesium sulfate. The elimination of amphetamine can be accelerated by acidifying the urine (ascorbic acid, ammonium chloride).

Piperidine derivatives: pyridrol and meridyl

Piperidine derivatives are similar to amphetamine in their effect on the central nervous system. pyridrol And meridil. In terms of stimulating activity, pyridrol is not inferior to amphetamine. Meridil is somewhat weaker.

The undoubted advantage of these drugs is their absence of unwanted peripheral adrenomimetic effects. In particular, unlike amphetamine, they have virtually no effect on the cardiovascular system.

Meridril and pyridrol are used in psychoneurological practice as psychostimulants for asthenia, depressive states, narcolepsy, increased fatigue, etc. The drugs are prescribed in the first half of the day. They are contraindicated for insomnia, exhaustion, hyperthyroidism, atherosclerosis, and angina. As with amphetamines, drug dependence may develop when using these drugs.

Sydnonimine derivatives: mesocarb

An active psychostimulant is mesocarb- a drug that, when used in a course of 2-3 days, has a mild psychostimulating effect without initial euphoria and subsequent mediator depletion. The mechanism of action of this psychostimulant is associated with its central sympathomimetic effect. That is, mesocarb increases the amount of norepinephrine in the synaptic cleft, which leads to stimulation of the corresponding receptors.

Mesocarb is used for asthenic conditions, asthenoneurotic disorders after infections, intoxications or traumatic brain injuries, physical and mental fatigue, to correct the side effects of neuroleptics (asthenic phenomena), benzodiazepines, etc.

Compared to amphetamine, mesocarb does not have a pronounced peripheral sympathomimetic effect. This manifests itself in relatively stable hemodynamics. The drug is devoid of anorexigenic properties. Like other psychostimulants, mesocarb should not be taken in the evening as it may disrupt sleep.

Methylxanthines: caffeine

Xanthine is an oxidized purine, an analogue of uric acid. Several xanthine derivatives are used in medical practice: caffeine (1,3,7-trimethylxanthine), theophylline (1,3-dimethylxanthine), theobromine (3,7-dimethylxanthine).

Dimethylxanthines (theophylline, theobromine) are poorly soluble in water, so solid (powder, tablets) or soft (suppositories) dosage forms are prepared from them, which are prescribed as myotropic antispasmodics, bronchodilators, diuretics, cardiotonics, and antiplatelet agents. They are also included in a large number of combination drugs (theophedrine, terminal and etc.). The water-soluble salt of theophylline, aminophylline (aminophylline), is also available in the form of a solution for intravenous and intramuscular administration.

Of the xanthines, only caffeine. It is an alkaloid, found in tea leaves, coffee seeds, chocolate tree seeds, kola nuts, etc. The drug is also obtained synthetically.

Caffeine combines psychostimulant and analeptic properties. Its direct stimulating effect on the cerebral cortex is especially pronounced. Caffeine stimulates mental activity, increases mental and physical performance, motor activity, and shortens reaction time. After taking it, vigor appears, fatigue and drowsiness are temporarily reduced or eliminated.

The analeptic activity of caffeine is due to its effect on the centers of the medulla oblongata. It has a direct stimulating effect on the respiratory center. There is an increase and deepening of breathing, which is especially clearly manifested when this center is depressed. In addition, caffeine stimulates the vasomotor center and the centers of the vagus nerves.

The effect of caffeine on the cardiovascular system is significant. It consists of peripheral and central effects. Thus, caffeine has a direct stimulating effect on the myocardium, causing tachycardia. However, the centers of the vagus nerves are simultaneously excited, trying to cause bradycardia. Therefore, the final effect for a particular person will depend on the predominance of one or another influence.

There are central and peripheral components in the action of caffeine in relation to vascular tone. By stimulating the vasomotor center, caffeine increases vascular tone, leading to hypertension, and with a direct effect on vascular smooth muscles, it weakens their tone, which should lead to a decrease in blood pressure. Thus, during the administration of caffeine, blood pressure changes ambiguously, since it depends on the cardiotropic, central and direct vascular effects of the drug.

Caffeine has mixed effects on different vascular areas. For example, coronary vessels most often dilate due to a direct antispasmodic effect. At the same time, the cerebral vessels are somewhat toned, which is due to the central effect of caffeine and explains its beneficial effect on migraines.

To a small extent, caffeine increases diuresis, which is associated with a decrease in the reabsorption of sodium and water ions in the renal tubules. In addition, caffeine dilates the blood vessels of the kidneys and increases filtration in the renal glomeruli.

Caffeine enhances basal metabolism. Glycogenolysis is stimulated, causing hyperglycemia. Lipolysis increases - the content of free fatty acids in plasma increases. In large doses, caffeine causes the release of adrenaline; from the adrenal medulla.

With prolonged use of caffeine, mild addiction develops. In addition, mental dependence may occur - theism.

Synthetic psychostimulants- means of single or short-term use in emergency situations, when the risk of not performing the load at the maximum pace is higher than the danger of taking these drugs, and there is also the possibility of adequate rest and nutrition to restore the energy level. Due to such a narrow clinical focus, synthetic psychostimulants are not used to restore performance in a wide range of patients. For this purpose, plant adaptogens are usually used, which are less toxic, have a milder effect and do not cause such depletion of nervous activity (extracts and tinctures of ginseng, Eleutherococcus senticosus, etc.).

Sources:
1. Lectures on pharmacology for higher medical and pharmaceutical education / V.M. Bryukhanov, Ya.F. Zverev, V.V. Lampatov, A.Yu. Zharikov, O.S. Talalaeva - Barnaul: Spektr Publishing House, 2014.
2. Pharmacology with formulation / Gaevy M.D., Petrov V.I., Gaevaya L.M., Davydov V.S., - M.: ICC March, 2007.