List of psychostimulants. General characteristics of psychostimulants
Before proceeding with the description, I want to convey that there are three main classes of CNS stimulants, which are very different from each other. First of all, these are psychostimulants and nootropics. These are completely two different groups of drugs: psychostimulants act when taken once, their use increases the mental and physical state of a person, which, in turn, leads to an increase in mood and the development of euphoria in some cases; they improve mental activity and the ability to perceive the environment. They cause a sharpening of hearing and vision, improve mental state, sensitivity and psychomotor dynamics, give a feeling of renewal, increased physical condition and its capabilities. After the use of psychostimulants, the associativity of the thinking process increases, but often contrary to rage.
Always, together with the central stimulating effect of psychostimulants with alpha and beta adrenergic effects, there is a more or less pronounced anorectic effect, which consists of suppressing appetite.
Most psychostimulants in addition have central analeptic, anorectic, and sometimes pronounced sympathomimetic effects.
Here we come in passing to the third group of central nervous system stimulants - analeptics. Analeptic (from the Greek analepsis - restoration) drugs are those that, in therapeutic doses, directly or reflexively stimulate the functions of certain parts of the central nervous system, primarily the respiratory and vasomotor centers, thereby improving blood circulation and breathing. Analeptics are those same nonspecific antagonists of compounds that depress the central nervous system (hypnotics, narcotics, etc.). Some analeptics, however, also stimulate mental activity. Large doses of analeptics stimulate other parts of the central nervous system responsible for the development of seizures.
But let’s return to psychostimulants and nootropics to find out what their main difference is. Unlike psychostimulants, stimulation of nerve cells with nootropics leads to increased activity and the completion of tasks that are not qualitative, but quantitative. The effect of nootropics does not occur immediately after the first dose, as is observed with psychostimulants, but with long-term treatment.
It should be noted that a huge number of compounds have psychostimulant properties, in particular many MAOIs, both antidepressants and natural compounds.
It remains to pay attention to the fact that psychostimulants are quite dangerous substances, even as medications. For heart disease, hypertension, hyposomnia, neuroses, psychoses, etc. diseases, the use of psychostimulants is unacceptable due to drug provocation of a critical condition.
I think everyone knows about the development of mental dependence and, as a consequence, abuse of psychostimulants. Substance abuse with psychostimulants entails very severe mental disorders, including suicidal tendencies, all kinds of mania, affective disorders, panic disorders, and even delirium.
Methylxanthine derivatives
Caffeine
Methylcaffeine
Matein
Theobromine
Dimethazine
Phenityline
Kafedrin
Amphetamine derivatives
Amphetamine
Methamphetamine
Perviton
Amphetamine
Deprenaline
Metfendrazine
Prolintan
Phentermine
Fencamfamin
Phenmetrazine
Phendimetrazine
Pyrovalerone
Amphetamine derivatives with less stimulating activity and having additional components in their profile, which determine the pharmaceutical. profile of these connections. However, these are still psychostimulants
Ethylamphetamine
Dimethylamphetamine
Meridil
Ephedrine
Pseudoephedrine
Norpseudoephedrine
Norephedrine
Katin
Cathinone
Fepranon
Ephedrone
Chlorphentermine
Fenfluramine
Benzphetamine
Diphenylmethane derivatives
Pipradol
Methylphenidate
Facetopyran
Derivatives of other structures, in particular MAOI antidepressants with pronounced stimulating activity
Sydnofen
Sidnocarb
Indopan (indole analogue of amphetamine)
Tranylcypromine (cyclic amphetamine analogue)
Metfendrazine
Cefedrine
Carphedon
Bemitil
Acefen
Pemolin
Aminorex ("Euphoria")
Amineptine (an atypical illegal antidepressant with pronounced stimulating and euphoric activity; therefore, it is often sold under the guise of cocaine or other stim).
Note. It is clear that the list is far from complete (I did not mention some dubious and very distant from the structure of pheylethylamine drugs, did not mention amphetamine isomers and did not list cocaine, since this substance is separate from all psychostimulants and has many other types of activity) and may well be supplemented as a particular psychostimulant is recognized. I also did not present a huge list of MAOI antidepressants with strong stimulating activity, since the main one in their action profile is the thymoleptic (antidepressant) effect, however, I did present some substances - amphetamine analogues - from this group.
Psychostimulants include drugs that increase physical and mental performance. There are many different classifications of psychostimulants. But conditionally, psychostimulants can be divided into 2 large subgroups:
1) psychomotor stimulants - caffeine, phenamine and others, giving a quick stimulating effect, temporarily eliminating the feeling of fatigue, improving mood, reducing the need for sleep;
2) nootropic drugs - piracetam, pyriditol and others, which gradually normalize metabolic processes and restore impaired brain functions (memory, speech, etc.).
PSYCHOMOTOR STIMULANTS
PHENAMIN - a strong psychostimulant with central adrenergic and dopaminergic effects. Phenamine reduces fatigue and the need for sleep, temporarily increases performance, and reduces hunger. Phenamine has a peripheral adrenomimetic effect: it constricts blood vessels, increases blood pressure, and increases the heart rate. Phenamine weakens the effect of anesthesia and hypnotics. Phenamine is used mainly for asthenic conditions, subdepression, accompanied by drowsiness, etc. The use of phenamine is limited, as addiction and drug dependence (drug addiction) develop to it. Phenamine requires a special prescription form (as for all other drugs). Side effectswhen appliedphenamine: dizziness, insomnia, arrhythmias, sometimes a paradoxical reaction (CNS depression instead of a stimulating effect). Contraindications to the use of phenamine: insomnia, diseases of the cardiovascular system (arterial hypertension, atherosclerosis), diabetes mellitus, liver disease. Release formfenamina: tablets of 0.01 g. List A.
An example of a phenamine recipe in Latin:
Rp.: Tab. Phenamini 0.01 N. 10
D.S. 1 tablet per day.
MERIDIL(pharmacological analogues: centedrine ) - is inferior in psychostimulating effect to phenamine, but lacks peripheral adrenomimetic action, and therefore Meridil does not affect the function of the cardiovascular system. Meridil is used for increased mental fatigue and neurotic conditions accompanied by lethargy and apathy. Side effects when using Meridil: insomnia, increased irritability. Contraindications to the use of Meridil: neuroses occurring with increased excitability of the nervous system, irritability; insomnia; old age. Meridil release form: tablets of 0.01 g. List A.
Meridil recipe examplein Latin:
Rp.: Tab. Meridili (Centedrini) 0.01 N. 20
D.S. 1 tablet 2 times a day in the morning.
SIDNOKARB(pharmacological analogues: mesocarb ) is a psychostimulant with a weak peripheral adrenomimetic effect. Sidnocarb is used for asthenic conditions; schizophrenia, occurring with lethargy and apathy; neurotic states accompanied by lethargy, etc. Side effects when using syndocarb: insomnia, headache, increased blood pressure. Sidnocarb is contraindicated for atherosclerosis, hypertension, insomnia, and liver diseases. Sidnocarb release form: tablets of 0.005 g and 0.01 g. List A.
Example of a sidnocarb recipe in Latin:
Rp.: Tab. Sydnocarbi 0.005 N. 20
SIDNOFEN- the action is close to mesocarb. Sidnofen has the same indications for use, side effects and contraindications. Unlike mesocarb, the psychostimulating effect of sydnofen is combined with a moderate antidepressant effect, and therefore sydnofen is a valuable drug for the treatment of asthenodepressive conditions. Sydnofen release form: tablets of 0.005 g. List A.
Example of a sydnofen recipe in Latin:
Rp.: Tab. Sydnopheni 0.005 N. 20
D.S. 1 tablet 2 times a day.
CAFFEINE- found in tea leaves, coffee seeds, cola nuts. Caffeine has a psychostimulant effect; increases mental and physical performance, reduces the need for sleep, regulating and enhancing excitation processes in the cerebral cortex. This effect depends on the type of higher nervous activity, which must be taken into account when dosing caffeine. Caffeine stimulates the respiratory and vasomotor centers. The direct stimulating effect of caffeine on the heart is expressed in an increase in the frequency and strength of heart contractions. The effect of caffeine on blood pressure depends on the predominance of a central (through the vasomotor center) vasoconstrictor effect, or a peripheral (directly on the vascular wall) vasodilator effect. Caffeine generally does not change normal blood pressure levels. Caffeine drugs and derivatives increase urination and increase the secretion of gastric glands.
D The effect of caffeine is mediated through cAMP, and its central effects are realized through adenosine receptors. Side effects when using caffeine can manifest themselves in the form of insomnia, tachycardia, arrhythmia, increased excitability of the central nervous system, which in itself is a contraindication for use, as well as severe atherosclerosis, hypertension, organic heart disease, glaucoma. Caffeine is used for depression of the functions of the central nervous system and cardiovascular system, overdose of drugs that depress the central nervous system, to increase physical and mental performance, as well as for migraines, etc. Caffeine is widely used in combination with other drugs (non-narcotic analgesics, etc.). Caffeine release form: powder.
Example of a caffeine recipe in Latin:
Rp.: Coffeini 0.05 Sacchari 0.2
M. f. pulv.
D.t. d. N. 10
S. 1 powder 2 times a day.
SODIUM CAFFEINE BENZOATE- similar in action, indications for use and contraindications to caffeine. Caffeine sodium benzoate is more soluble in water and is absorbed and eliminated from the body faster. Sodium caffeine benzoate is prescribed orally or injected under the skin. Doses of sodium caffeine benzoate are selected individually. Release form caffeine sodium benzoate: powder, tablets of 0.1 and 0.2 g (for adults), 0.075 g (for children). Ampoules of 1 ml and 2 ml and syringe tubes of 1 ml of 10% and 20% solution of the drug.
Example recipe for caffeine-sodium benzoate in Latin:
Rp.: Tab. Coffeini natrio-benzoatis 0.1 N. 6
D.S. 1 tablet 2 times a day.
Rp.: Sol. Coffeini natrio-benzoatis 10% 1 ml
D.t. d. N. 6 in ampull.
S. 1 ml 2 times a day under the skin.
COFFETAMINE- a combination drug consisting of caffeine (0.1 g) and ergotamine tartrate (0.001 g). The pharmacological properties of caffeamine are determined by its constituent ingredients. Caffeamine is prescribed for arterial hypotension, migraine, to normalize intracranial pressure in vascular, traumatic and infectious lesions of the central nervous system. Caffeamine is taken orally, 1 tablet 2-3 times a day. Caffeamine release form: film-coated tablets. List B.
Example of a caffeamine recipe in Latin:
Rp.: Tab. "Coffetaminum" obducta N. 10
D.S. Take 1 tablet 2 times a day.
MILDRONATE- increases performance, reduces fatigue and overstrain phenomena during physical overload (including among athletes). Mildronate is prescribed for adults orally at 0.25 g 2-4 times a day (30 minutes after meals) or administered intravenously at 0.5 g once a day for 10-14 days. Mildronate release form: capsules 0.25 g ; ampoules of 5 ml of 10% solution.
Example of a mildronate recipe in Latin:
Rp.: Caps. Mildronati 0.25 N. 100
D.S. 1 capsule 3 times a day (after meals).
Rp.: Sol. Mildronati 10% 5 ml
D.t. d. N. 10 in ampull.
S. Administer 5 ml intravenously once a day.
BEMITIL- belongs to the group of actoprotectors; has psychoenergizing and antihypoxic activity. Bemitil increases the body's resistance to physical stress, preserves and restores performance. Bemitil is used for patients with neuroses, neurosis-like conditions in cases of cerebrovascular accident, traumatic brain injury, and in the postoperative period. Bemitil is prescribed to adults orally after meals, 0.25-0.5 g. The daily dose of bemitil is 0.5-1 g. The course of treatment is 15-30 days (there may be other treatment regimens). Side effects when using bemitil: possible nausea, vomiting, discomfort in the stomach and liver, facial flushing, runny nose, headache. Bemitil release form: tablets of 0.25 g. List B.
Example of a bemitil recipe in Latin:
Rp.: Tab. Bemithyli 0.25 N. 100
D.S. 1 tablet 2 times a day (after meals).
NOOTROPIC AND GABA-ERGIC DRUGS (PIRACETAM, PYRITHINOL, ACEPHEN)
Of interest are drugs whose introduction into the body causes an improvement in metabolic processes in brain cells, as a result of which mental activity is stimulated, perception, memory, and thought processes are improved. The effect of these drugs is manifested when metabolic processes in the brain are disrupted due to various diseases: inflammatory, atherosclerosis, alcoholic encephalopathies, traumatic brain injuries, etc. Such drugs are called metabolic psychostimulants (nootropics). They do not cause excitement, they do not develop addiction and drug dependence. GABA-ergic drugs are also close to nootropics, also acting on metabolic processes in the brain, improving its blood supply, restoring memory, etc.
PIRACETAM(pharmacological analogues: nootropil ) - used for various diseases of the nervous system caused by metabolic disorders in the brain tissue, accompanied by impairments of memory, attention, speech, and dizziness; for atherosclerosis of cerebral vessels, etc. Piracetam is a typical nootropic agent: it normalizes metabolic processes in the brain, cerebral circulation, and increases the resistance of brain tissue to hypoxia and toxic effects. Side effects when using piracetam: increased irritability, sleep disturbances, dyspeptic symptoms; in older people there may be an exacerbation of coronary insufficiency. Piracetam is contraindicated for kidney disease and pregnancy. Piracetam release form: tablets of 0.2 g; capsules 0.4 g; ampoules of 5 ml of 20% solution. List B.
Example of a piracetam recipe in Latin:
Rp.: Tab. Pyracetami 0.2 N. 60
D.S. 2 tablets 3-4 times a day.
Rp.: Sol. Pyracetami 20% 5 ml
D.t. d. N. 6 in ampull.
S. Administer intramuscularly (or intravenously) 10-20 ml per day.
PYRITINOL(pharmacological analogues: pyriditol, encephabol ) - like piracetam, activates metabolic processes in the central nervous system. Pyritinol is used for the same indications as piracetam; has the same side effects. Pyritinol is contraindicated in cases of psychomotor agitation, convulsive conditions, and epilepsy. Pyritanol release form: tablets of 0.05 g and 0.1 g; "Encephabol" in the form of syrup, 200 ml (5 ml - 0.1 g of the drug) - for children.
Example of a recipe for pyritanol in Latin:
Rp.: Tab. Pyritinoli 0.1 N. 60
D.S. 1 tablet 2-3 times a day.
ACEPHEN- activates metabolic processes in the central nervous system, has a psychostimulating effect. Acefen is used for cerebrovascular accidents, traumatic and vascular diseases of the brain, etc. Acefen is contraindicated for infectious diseases of the central nervous system. The drug acefen is well tolerated; in some cases, patients with mental illness experience exacerbation: delirium, hallucinations. Release form of acephen: tablets of 0.1 g. List B.
Example of acephen recipe in Latin:
Rp.: Tab. Acepheni 0.1 N. 50
D.S. 1 tablet 3-4 times a day.
AMINALONE(pharmacological analogues: gammalon ) - is a gamma-aminobutyric acid, which is a mediator of the central nervous system and is involved in bioenergetic processes in the brain. Aminalon is used for diseases affecting memory, attention, speech, for example, for cerebrovascular accidents after a stroke, for mental retardation in children with decreased mental and motor activity, etc. Side effects when using aminalon: dyspeptic disorders, sleep disorders, feeling of fever , fluctuations in blood pressure that disappear when the dose of the drug is reduced. Aminalon release form: 0.25 g film-coated tablets.
Example of an aminalon recipe in Latin:
Rp.: Tab. Aminaloni 0.25 obductae N. 100
D.S. 1-2 tablets 3 times a day.
CEREBROLYSIN- contains essential amino acids. Indications for use and side effects when using Cerebrolysin are the same as for aminalon. Cerebrolysin release form: ampoules of 1 ml of 5% solution.
Example of a Cerebrolysin prescription in Latin:
Rp.: Sol. Cerebrolysini 5% 1 ml
D.t. d. N. 10 in ampull.
S. Administer 1-2 ml intramuscularly every 2-3 days (course of injections).
SODIUM OXYBUTYRATE- penetrates well through the blood-brain barrier, gives a sedative effect, and in large doses causes anesthesia (see section “Anesthetics”). Sodium hydroxybutyrate has an antihypoxic effect on the tissues of the brain, heart, and retina. Sodium hydroxybutyrate is used for hypoxic cerebral edema, to eliminate retinal hypoxia, as a sedative, for anesthesia, etc. Sodium oxybutyrate is contraindicated for hypokalemia and myasthenia gravis. Sodium hydroxybutyrate release form: powder; ampoules of 10 ml of 20% solution; bottles - 5% syrup (400 ml) and 66.7% solution (37.5 ml).
Example of a recipe for sodium hydroxybutyrate in Latin:
Rp.: Sirupus Natrii oxybutyratis 5% 400 ml
D. S. Take 2-3 tablespoons at night (as a sleeping pill), 1 tablespoon 2-3 times a day as a sedative for neuroses.
PHENIBUT- its properties are similar to sodium hydroxybutyrate. Phenibut is used for neuroses and psychopathic conditions, as a sedative. Phenibut release form: tablets of 0.25 g.
Example of a Phenibut recipe in Latin:
Rp.: Tab. Phenibuti 0.25 N. 50
D.S. 1 tablet 3 times a day.
PANTOGAM- its action is similar to aminalon and sodium hydroxybutyrate, it has the same indications for use. Pantogam release form: tablets of 0.25 g and 0.5 g.
An example of a pantogam recipe in Latin:
Rp.: Tab. Pantogami 0.5 N. 50
D.S. 1 tablet 4-6 times a day
PICAMILON- improves blood circulation and the functional state of the brain, normalizes metabolic processes in brain tissue. Picamilon is used as a nootropic and vasoactive agent for acute and chronic cerebrovascular accidents, vegetative-vascular dystonia, as well as for conditions accompanied by anxiety and increased irritability. Picamilon can be used for asthenic conditions of various etiologies, depressive disorders in people of the older age group, to restore performance and increase resistance to physical and mental stress. Picamilon is prescribed orally at a dose of 0.02-0.04 g 2-3 times a day. The average daily dose of picamilon is 0.06 g. Side effects when using picamilon: possible increased irritability, agitation, anxiety, dizziness, headache, allergic rash (in this case, reduce the dose or discontinue the drug). Picamilon is contraindicated in case of kidney disease and individual intolerance to the drug. Picamilon release form: tablets of 0.02 g and 0.05 g. List B.
Example of a picamilon recipe in Latin:
Rp.: Tab. Picamiloni 0.02 N. 30
D.S. 1 tablet 3 times a day (for 1-2 months).
Psychostimulants (psychotonics) are a group of medications that have a stimulating effect on the central nervous system, under the influence of which fatigue, weakness, fatigue are reduced, the perception of the surrounding world and information processing is facilitated, and mental performance is increased.
Classification of psychostimulants
Psychostimulants can be divided into the following main groups:
I. Psychostimulants that have a stimulating effect on brain functions and activate the mental and physical activity of the body. These include a number of purine derivatives (caffeine, etc.), phenylalkylamines (phenamine, pervitin, etc.) and phenylalkyl sydnonimines (sydnocarb, etc.) and other drugs that can be considered as psychomotor stimulants. Under experimental conditions, these drugs quickly change the functional indicators of brain activity (activate the bioelectrical activity of the brain, change conditioned reflexes, etc.), increase endurance for physical work. When used therapeutically, they have a relatively quickly onset stimulating effect.
II. Analeptic drugs that primarily stimulate the centers of the medulla oblongata - vascular and respiratory. The main representatives of this group are camphor, corazol, and cordiamine. From the group of analeptic drugs, there is a group of respiratory analeptics (cytiton, lobeline), which are especially characterized by a stimulating effect on the respiratory center.
III. Drugs acting primarily on the spinal cord; the main representatives of this group are strychnine and securine.
Previously, psychostimulants were used quite widely, but side effects of these drugs quickly emerged in the form of irritability, aggressiveness, increased anxiety, the emergence of suicidal tendencies, exacerbations of sluggish psychotic processes, increased blood pressure, gastrointestinal disorders, sexual dysfunctions, rapid development of mental and physical dependence. Most of the drugs were banned and withdrawn from production.
In medical practice, to achieve a psychostimulating effect, drugs from other groups are used:
- antidepressants (moclobemide, nortriptyline, melipramine, bupropion, befol, fluoxetine);
- nootropics (pyriditol, piracetam, acephen);
- tranquilizers (trioxazine, oxazepam, grandaxin);
- neuroleptics (eglonil, frenolone).
Also, the following can be used as a psychostimulant: Schisandra tincture, alcoholic extract of Rhodiola rosea, tincture of lure, tincture of Aralia high, tincture of Sterculia, ginseng-based preparations, Eleutherococcus extract, Leuzea extract. The drugs Pantocrine, Rentarin, Ecdisten, Saparal have a psychostimulating effect.
Recently, a new group of stimulants with the code name “actoprotectors” has been proposed. These include bemitil, which has a psychostimulating effect, has antihypoxic activity, increases the body's resistance to hypoxia and increases performance during physical activity; There is evidence of the immunostimulating effect of bemitil.
The use of psychostimulants is possible in case of pre-neurotic and neurotic conditions occurring in somatically ill patients, including asthenic, astheno-hypochondriacal and astheno-depressive, apathetic states. They are prescribed only in the first half of the day. Combination with other psychotropic drugs is possible.
Beta blockers
Differentiated measures using beta blockers are possible when the patient’s fear manifests itself somatistically or in the form of panic attacks. The more pronounced the vegetative symptoms, the less the patient is aware of psychogenic their cause, the more effective beta blockers are in these cases. Their advantage is that they do not cause a pronounced sedative effect, do not negatively affect psychomotor skills and do not cause addiction. When used, nervousness, sweating, tremors are reduced, and the heart rate is reduced.
Beta blockers have been shown to be beneficial in treating “normal,” natural nervous reactions, such as fear of performing or exams. Before an event that causes fear, 40 mg of obsidan (anaprilin) or its analogues can be given one-time 1-2 hours before it. However, preliminary testing of the effect in a specific patient is recommended.
Indications for the use of beta blockers:
- functional cardiac symptoms (cardiophobia, neurovegetative tachycardia, cardiac neuroses);
- situational and “phobic” fears (fear of driving a vehicle or flying on an airplane, fear of animals, fear of performances, exams, fear of interviews, fear of medical intervention);
- as an adjuvant in a pharmacotherapeutic complex in the treatment of conditions accompanied by hypochondria, increased excitability, and emotional lability.
Some authors recommend treating various depressive conditions with beta blockers, completely forgetting that these drugs themselves can cause the development of depression when taken for a long time.
Contraindications
Sick sinus syndrome and bradycardia less than 50 beats per minute in old age can be considered as an absolute contraindication. Relative contraindications are associated with the occurrence of rare side effects - headaches, fatigue, gastrointestinal disorders, hypoglycemia.
Recommended doses of obzidan and trazicor (oxprenolol) when taken systematically are from 20 mg per day to 20 mg 3 times a day during the first week, up to 40 mg 3 times a day in the next three weeks. In the future, it is recommended to gradually reduce the dosage.
Psychodysleptics
More than fifty years have passed since April 16, 1943, when Swiss chemist Albert Hoffmann accidentally discovered the powerful psychoactive properties of lysergic acid diethylamide (LSD). Psychedelics - this is how these substances began to be called in the late 50s.
They were known only to a narrow circle of specialists. Psychiatrists viewed LSD as an interesting and promising remedy for the treatment of a number of mental illnesses, psychoanalysts saw it as a tool for quick access to the unconscious of their patients, and experimental psychologists were interested in LSD as one of the methods for studying mental processes and their disorders, especially in the field of perception.
But at the very beginning of the 60s, a number of famous cultural and scientific figures, for example, the English writer A. Huxley, a group of psychologists from Harvard University led by Professor T. Leary and others, proclaimed that psychedelics - this is the key to human self-knowledge, the path to higher forms of consciousness and the basis of a new religion. These ideas were quickly picked up by various intellectual and youth movements, especially hippies in the USA.
Psychedelics, according to A. Hoffman, can be defined as substances that cause changes in thinking, perception and affect, observed separately from each other or together, without significant disorders of the autonomic nervous system, such as confusion or other serious disorders. In the literature, in addition to the term “psychedelics,” others are often used, which, in essence, are synonyms: psychotomimetics, psychodysleptics, hallucinogens, science fiction, illusionogens, hypersenses, etc.
Classification of psychodysleptics
A. T. Shulgin gives a classification of psychodisleptics based on the criterion of the similarity of their molecular structure to the structure of neurotransmitters:
I. Psychotomimetics related to serotonin:
- tryptamines (DMT, DET, DPT, psilocybin, CZ-74, CEY-19, etc.);
- beta-carbolines (harmaline, harmine);
- lysergamide derivatives (LSD-25, ALD-52, LSM-775).
II. Psychotomimetics related to dopamine:
- phenethylamines (mescaline, 2C-D, 2C-B, 2C-C, 2C-E (“ESTET”), 2C-P (“DOPROPET”));
- phenylisopropylamines (PMA, MDA, TMA, DOET, MMDA, MDMA (“ecstasy”)).
III. Psychotomimetics related to acetylcholine (Ditran, JB-318, JB-336).
IV. Other psychotomimetics (Ibogaine, Muscimol, Ketamine, etc.).
Mechanism of action of psychodisleptic drugs
The mechanism of action of psychotomimetics has not yet been fully elucidated. Research into the stages of synaptic transmission has shown that some drugs act by enhancing or inhibiting neurotransmitter release. For example, under the influence of psychotomimetics - analogues of amphetamine (phenylisopropylamine), the nerve endings of the brain release dopamine - a transmitter associated with the wakefulness and pleasure systems. The real situation in the picture of the mechanism of action of psychotomimetics is complicated by the fact that these drugs act not only on the neurotransmission system, but also on the course of other neurobiochemical processes.
The use of psychotomimetic substances such as LSD, psilocybin, mescaline in psychotherapy began in the mid-50s of the 20th century. in a number of research centers in Europe and North America. The pioneers of LSD therapy were the English therapist R. A. Sandteon, H. Osmond, significant work in the next decade was carried out by the West German psychiatrist H. Leuner, the Czech psychiatrist S. Grof (St. Grof), American psychiatrists H. Abramson, S. Cohen, a group of psychologists from Harvard University led by T. Leary and many others.
In the former Soviet Union, G.V. Stolyarov, who used LSD to treat mental disorders, did a lot in this area. In his work “Drug Psychoses and Psychotomimetic Drugs,” he outlined in great detail and quite exhaustively the entire experience of using psychodisleptic drugs for therapeutic purposes in mentally ill patients.
Short-term side effects of psychotomimetics
Most often, when using psychotomimetics, short-term (from 1 to 24 hours) psychological complications were observed in the form of acute panic reactions (APR). Symptoms of OPD include frightening, disturbing illusions or hallucinations (usually visual or auditory); overwhelming anxiety, panic, fear of death or madness; sometimes aggressive behavior; depression with suicidal tendencies; confusion and fear due to paranoid delusions.
Long-term negative psychological reactions were the most severe complications when using psychotomimetics. Prolonged depression and psychotic episodes have been observed. Their duration varied from several days to months. Although it is indicated that the frequency of this kind of complications when using LSD in a contingent of mentally ill patients did not exceed 2% (3 cases out of 158 sessions). The picture of protracted psychotic episodes was, as the researchers put it, a caricature of their state before the introduction. It is emphasized that in most cases the emergence of long-term psychopathological reactions was preceded by latent or true forms of mental pathology. A number of scientists think that long-term mental complications were the result of the provoking (exacerbating) properties of psychodysleptics.
Long-term side effects of psychotomimetics
Another type of psychological complications when using psychotomimetics - long-term psychotic reactions - differs from the previous ones in that they do not appear immediately, but some time after the end of the drug's effect. The period free from any deviations can vary from several weeks to months. Symptoms of long-term mental reactions can be very varied and include psychopathic behavior, inappropriate emotions, emotional lability, depression and agitated depression, acute anxiety and panic reactions, thought disorders, hallucinations and illusions (visual and auditory), delusions, regression, depersonalization and feelings of unreality. , apathy, confusion, disorder of the sense of time, etc. The connection of these disorders with the use of psychodisleptic drugs is also very controversial, since the disorders that arose were quite rare and had a clear “endogenous” coloring.
Complications in the form of reminiscences
The last type of complications when using psychotomimetics are “vivid reminiscences”, or, as they are commonly called in foreign literature, “flashback” phenomena. They represent acute, unpredictable, spontaneous returns of psychic phenomena experienced under the influence of psychotomimetics (usually LSD). They may suddenly appear months after using the drug, although before this time the patient did not experience the slightest deviation from the normal state. The frequency of reminiscences reported by different authors ranges from 15 to 77%. The likelihood of their occurrence increases with the number of sessions using psychotomimetics. R. Matefi and his colleagues, in a series of articles, described comparative studies of patients, one group of whom experienced vivid reminiscences after using psychotomimetics, and the other did not. The authors did not find significant psychopathological differences during the examination. However, the group of “flashbackers” was highly suggestible.
Further practice of “psychedelic” therapy was curtailed due to the prohibition of the use of LSD and a number of other psychotomimetics in working with people. A major role in this was played by the spread of psychodisleptic drugs on the streets (“street acid”) and the emerging information about the mutagenic properties of LSD.
However, recently a number of “new wave” monographs have appeared, summarizing the results of the use of psychedelics as an adjuvant in psychotherapy. More correctly conducted genetic studies have not confirmed the mutagenic properties of LSD. It should be noted that the vast majority of psychologists, psychotherapists and psychiatrists who have worked in this area find this method very promising. It is possible that, on the initiative of some enthusiasts, research in this area will be resumed. In some American states, researchers have paid attention to the so-called “minor” psychodisleptic drug - tetrahydrocannabinol, contained in hemp, which is even available in the form of the drug “dronobitol”, or “THC”. This remedy is widely used in oncological practice.
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Start of activity (date): 06/25/2013 06:35:00
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Stimulants are conventionally divided into 4 large groups:
1. PSYCHOSTIMULANTS
a) psychomotor:
Phenamine;
Sidnocarb.
b) psychometabolic (nootropics):
Nootropil (piracetam);
Cerebrolysin;
Gamalon et al.
2. ANALEPTICA
a) direct action:
Bemegrid;
Etimizole, etc.
b) reflex action:
Tsititon et al.
c) mixed action:
Cordiamin et al.
3. SPINAL CORD STIMULATORS
Strychnine;
Sekurenin et al.
4. GENERAL TONIZERS (ADAPTOGENS)
a) of plant origin:
Ginseng preparations, Eleutherococcus
ka, aralia, golden root, ma
Raleigh root, Bittner's balm and
b) animal origin:
Pantocrinus et al.
PSYCHOSTIMULANTS 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), and temporarily reduce the need for sleep (drugs that invigorate a tired body are called “doping” - from English to dope - to give drugs).
Unlike CNS depressants, stimulants are less important because they lack selectivity of action. In addition, stimulation of the central nervous system is accompanied by its subsequent inhibition.
Classification of psychostimulants
1) Means acting directly on the central nervous system:
a) stimulating primarily the cerebral cortex (xanthine alkaloids, phenamine, sydnocarb, methylphenamine, meridol, etc.);
b) stimulating mainly the medulla oblongata (cortex
ash, cordiamine, bemegride, camphor, carbon dioxide);
c) stimulating primarily the spinal cord (strychnine).
2) Drugs that act on the central nervous system reflexively(lobelin, verat
rum, nicotine).
It should be remembered that this 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; table of 0.005; drops in the nose, in the eye 1% solution). Chemically it is a phenylalkylamine, that is, similar in structure to adrenaline and norepinephrine.
MECHANISM OF ACTION associated with the ability to release NORADRENALINE and DOPAMINE from presynaptic endings. In addition, phenamine reduces the reuptake of norepinephrine and dopamine.
Phenamine stimulates the ascending activating reticular formation of the brain stem.
PHARMACOLOGICAL EFFECTS
INFLUENCE ON THE CNS
Powerful central nervous system stimulant. It increases mental and physical performance, improves mood, causes euphoria, insomnia, tremors, 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. Tachyphylaxis is known in relation to the hypertensive effect of phenamine.
SMOOTH MUSCLE
Phenamine increases the tone of the bladder sphincter 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).
According to the modern classification, psychomotor stimulants are divided into purine and imidazole derivatives (caffeine, caffeine-sodium benzoate, etimizol), arylalkylamines (meridil, sydnocarb, phenamine), benzimidazole derivatives (bemityl). The last drug, bemitil, is currently considered as a representative of a new group of drugs - actoprotectors.
BEMITHYL (Bemithylum)
Pharmacological action. It has a psychostimulating effect, has antihypoxic (increasing tissue resistance to lack of oxygen) activity, increases the body's resistance to hypoxia (insufficient supply of oxygen to tissues or impaired utilization / absorption) and increases performance during physical activity. It is considered as a representative of a new group - actoprotective (increasing the body's resistance to extreme influences) drugs. Slowly absorbed when taken orally.
Indications for use. Prescribed to adults for asthenic conditions (weakness), neuroses, after injuries and other conditions in which stimulation of mental and physical functions is indicated.
There is evidence of the immunostimulating (increasing the body's defenses) effect of bemitil and its effectiveness in this regard in the complex therapy of certain infectious diseases.
Method of administration and dose. Take bemitil after meals, 0.25-0.5 g 2-3 times a day. The daily dose is 0.5-1 g. The course of treatment is 10-20 days in a row or 2-3 courses of 3-5 days at intervals of 2-5 days. It is recommended to eat foods rich in carbohydrates during treatment.
Side effect. When using bemitil, nausea, rarely vomiting, discomfort in the stomach, headache, hyperemia (redness) of the face are possible.
Contraindications. The drug is contraindicated for hypoglycemia (low blood sugar).
Release form. Tablets of 0.125 and 0.25 g, film-coated, in a package of 100 pieces.
Storage conditions.
CAFFEINE (Cofleinum)
Synonyms: Caffeine, Guaranine, Theine.
Pharmacological action. Central nervous system stimulant.
Indications for use.
Method of administration and dose. Orally 0.05-0.1 g 2-3 times a day.
Side effect. Caffeinism (painful addiction to caffeine), sleep disturbance.
Contraindications. Increased excitability, insomnia, severe hypertension (persistent rise in blood pressure), atherosclerosis, organic diseases of the cardiovascular system, old age, glaucoma (increased intraocular pressure).
Release form. Powder.
Storage conditions.
COFFETAMINE (Conetaminum)
Synonyms: Kofergot, Ergofein, Ergoffin.
Pharmacological action. A combination drug containing caffeine and ergotamine tartrate. The effect is associated with the vasoconstrictor effect of ergotamine and the improvement of brain functions under the influence of caffeine.
Indications for use. It is used for migraines (vasoparalytic form), arterial hypertension (increased blood pressure), and also as a means of lowering intracranial pressure in vascular, traumatic, and infectious lesions of the nervous system.
Method of administration and dose. Prescribed orally 1-2 tablets per dose during a headache attack 2 times a day, then 1 tablet 2-3 times a day for several days (up to 1 month).
Side effects and Contraindications. Same as for caffeine.
Release form. Tablets (coated) containing caffeine 0.1 g and ergotamine tartrate 0.001 g (1 mg), in glass tubes of 10 pieces.
Storage conditions. List B. In a place protected from light.
Caffeine is also included in the combination drugs avamigran, anapirin, angisedin, antasman, askofen, askofen P, benalgin, vasobral, gevadal, dixafen, caffetin, menopause, coldrex, coldrex Teva, cofitil, novomigrofen, panadol extra, peitalgin, pyramein, plivalgin, remidon, ringn, rodavan, saridon, sedalgin, solpadeine, pyrcofen tablets, theofedrine, theofedrine N, tomapirin, toff plus, fencik, citramon, andrews ansver.
SODIUM CAFFEINE BENZOATE (Coneinum natrii-benzoas)
Synonyms: Caffeine is sodium benzoate.
Pharmacological action. The pharmacological properties are similar to caffeine and are used in the same cases.
Indications for use. Central nervous system depression, drug poisoning, cardiovascular failure.
Method of administration and dose. Prescribed orally 0.1-0.2 g 2-3 times a day, subcutaneously - 1-2 ml of 10% and 20% solution.
Side effects and Contraindications. Same as for caffeine.
Release form. Powder; tablets of 0.075 g (for children) in a package of 10 pieces; tablets of 0.1 and 0.2 g in a package of 6 pieces; ampoules of 10% solution, 1 ml and 2 ml in a package of 10 pieces; ampoules of 20% solution of 1 and 2 ml in a package of 10 pieces.
Storage conditions. List B. In a cool, dry place.
PASUMA
Pharmacological action. Combined drug. The active components of pasuma have a general strengthening effect in cases of physical and mental exhaustion, and functional disorders in the genital area. The drug enhances potency and improves the course of male menopause.
Indications for use. A state of physical and mental asthenia (weakness) and exhaustion, especially in the sexual sphere; functional impotence in men after organic diseases, with de-
depressed states (states of depression), as well as frigidity (sexual coldness) of women. In these cases, taking medications without a doctor is not advisable
Method of administration and dose. Prescribe 1-2 tablets 3 times a day after meals or 1 ampoule intramuscularly daily or every other day. The positive effect of treatment is achieved with long-term use of the drug - for 1-2 months. It is recommended to alternate intramuscular injections with oral tablets every week.
Release form. Coated tablets; ampoules of 2 ml. 1 tablet contains: sodium benzoate caffeine - 15 mg, methyltestosterone - 5 mg, tocopherol acetate (vitamin E) - 3 mg, ephedrine hydrochloride - 1 mg, strychnine glycerophosphate - 0.35 mg, yobiquine hydrochloride - 3 mg. 1 ampoule contains: testosterone propionate - 10 mg, tocopherol acetate (vitamin E) - 20 mg, strychnine glycerophosphate - 0.5 mg, yobiquine glycerophosphate - 8 mg.
Storage conditions. List B. In a cool, dry place.
Sodium caffeine benzoate is also included in the preparations amidopyrin, ankofen, gluferal, pagluferal, Sereysky mixture, Anapirin tablets, Pentalgin tablets.
MERIDIL (Meridiltim)
Synonyms: Centedrine, Methylphenidate hydrochloride, Relatin, Rilatin.
Pharmacological action. In structure and action, Meridil is close to phenamine, but has a less strong stimulating effect and less influence on peripheral adrenergic systems; does not cause a significant increase in blood pressure.
Indications for use. Psychostimulant for asthenic conditions (weakness), increased fatigue. Can be used for depression of the nervous system caused by antipsychotic drugs.
Method of administration and dose. Take orally (in the first half of the day) 0.01-0.015 g per dose. Daily dose -0.01-0.03 g (10-30 mg). The course of treatment is from 2-4 weeks. up to 3-4 months
Side effect. Insomnia, nausea, sometimes agitation and anxiety, exacerbation of psychopathic symptoms. Causes addiction (weakening or lack of effect with prolonged repeated use).
Contraindications. Contraindicated for insomnia, vascular sclerosis, angina pectoris, hyperthyroidism (thyroid disease), severe exhaustion, mental agitation.
Release form. Tablets 0.01 g (10 mg).
Storage conditions.
SYDNOCARB (Sydnocarbum)
Synonyms: Mesocarb.
Pharmacological action. It has a pronounced stimulating effect on the central nervous system; unlike phenamine, it does not have a distinct peripheral sympathomimetic activity and is not addictive (there is no weakening or absence of effect with prolonged repeated use).
Indications for use. Asthenic conditions (weakness) as a result of physical and mental fatigue, after serious illnesses and traumatic brain injuries, neurotic disorders with lethargy, sluggish schizophrenia with apatoabulic disorders (lethargy, lack of will). There is evidence of the effectiveness of the drug for bedwetting.
Method of administration and dose. Prescribed in the form of tablets 1-2 times a day in the morning (before meals). Doses are selected individually. The initial dose is usually 0.005 g (5 mg); if necessary, the dose is gradually increased in adults to 0.015-0.025-0.05 g per day.
Maintenance doses - 0.005-0.01 g per day. For patients with lucid catatonia (a mental disorder with a predominance of motor disturbances in the form of agitation, stupor, or their alternation with preserved consciousness), the dose of the drug can be increased to 0.125-0.15 g (125-150 mg) per day.
For children, debilitated patients and the elderly, the drug is prescribed in reduced doses (daily dose 0.0025-0.005 g in 2 doses).
Higher doses for adults orally: single - 0.075 g, daily - 0.15 g.
Side effect. In case of overdose, headache, insomnia, loss of appetite, increased blood pressure.
Contraindications. Increased arousal, severe atherosclerosis, stage III hypertension (persistent rise in blood pressure).
Release form. Tablets of 0.005 g, 0.01 g and 0.025 g in packs of 50 pieces.
Storage conditions. List A. In a place protected from light.
Sidnocarb is also included in the drug dimethcarb.
PHENAMIN (Phenaminum)
Synonyms: Amphetamine, Amphetamine sulfate, Bezpropamine, Psychoton, Simpamin, Actedrin, Alenthol, Amphamine, Amphedrine, Benzedrine sulfate, Eufodin, Isoamine, Orthedrin, Psychedrin, Racefen, Raphetamine, Simpatedrin, etc.
Pharmacological action. An active stimulant of the central nervous system, it also has a peripheral adrenomimetic effect.
Indications for use. Asthenic conditions (weakness) caused by overwork, asthenic depressive. states (weakness, depressed state), to stimulate labor.
Method of administration and dose. Orally (in the first half of the day) 0.005-0.01 g per day. The dose must be selected individually.
Side effect. Dizziness, nausea, chills, insomnia, cardiac conduction disturbances (arrhythmias), tachycardia (increased heart rate). Possible addiction (weakening or lack of effect with prolonged repeated use) and addiction (drug dependence).
Contraindications. Liver diseases, severe atherosclerosis, persistent increase in blood pressure, sleep disturbance.
Release form. Tablets of 0.01 g in a package of 10 pieces.
Storage conditions. List A. In a cool, dry place.
ETIMIZOL (Aethimizolum)
Pharmacological action. It has an exciting effect on the central nervous system and stimulates the respiratory center.
Indications for use. In psychiatry for asthenodepressive states (weakness, depression), for diseases accompanied by feelings of anxiety. To stimulate breathing after anesthesia and prevent respiratory depression during barbiturate anesthesia, to prevent pneumonia (pneumonia) in the postoperative period.
Method of administration and dose. Orally 0.05-0.1 g 3 times a day, intravenously (slowly) - 2-3 ml, intramuscularly and subcutaneously - 4-5 ml of 1.5% solution.
Side effect. Nausea, vomiting, motor agitation.
Contraindications. Excitation of the central nervous system.
Release form. Tablets of 0.1 g in a package of 50 pieces; 1% and 1.5% solution in ampoules of 3 ml in a package of 10 pieces.
Storage conditions. List B. In a place protected from light.