Daytime tranquilizers include drugs. Sedatives, tranquilizers. Tranquilizers: what are these drugs and how do they affect the body?

Tranquilizers (from the Latin tranquilo-are - to make calm, serene) are psychotropic drugs that eliminate fear, anxiety, and affective tension in neuroses and neurosis-like conditions. Synonyms of the term are the expressions “anxiolytic agents” (from the English anxiety - fear), “antianxiety agents”, “ataractics” (from the Greek ataraxia - calmness, equanimity), “antiphobic agents”, “general sedatives”. Most tranquilizers have virtually no antipsychotic effect and the ability to eliminate psychotic fear and anxiety. There are, however, powerful tranquilizers with transitional to antipsychotic properties (for example, phenazepam). Tranquilizers do not have a pronounced antidepressant effect, but there are some exceptions in this regard. The main properties of this group of drugs are:

anxiolytic, eliminating anxiety, fear, tension. To a certain extent, tranquilizers can significantly alleviate the emotional state of psychiatric patients, since their depression, fears, and anxiety are not always directly related to the primary damage to neuropsychic processes, but arise as a reaction to the situation or awareness of the disease;

calming and only in this sense hypnotic, that is, facilitating the onset of sleep, so they are not prescribed if the patient performs work that requires a quick mental and motor reaction. Tranquilizers do not have a direct hypnotic effect, although many of them significantly improve the quality of sleep, in particular, freeing patients from painful dreams. The only exceptions are, perhaps, drugs such as natrazepam, flunitracepam and triazolam;

central muscle relaxant, reducing tonic tension of striated muscles;

anticonvulsant; tranquilizers can also be effective for mental attacks;

the ability to potentiate the effect of alcohol, sedatives, sleeping pills, narcotic and analgesic drugs;

the ability to cause addiction and side effects, in particular an increase in intraocular pressure;

stress-protective effect, that is, resistance to the effects of stress;

to a lesser extent antidepressant effect; First of all, we do not mean endogenous depression, but situational depression that occurs as a reaction to the influence of traumatic factors.

The mechanisms of action of tranquilizers are not fully known to this day. It has been established that tranquilizers have a very weak effect on the noradrenergic, dopaminergic and serotonergic systems of the brain. At the same time, it was found that benzodiazepine tranquilizers actively affect GABAergic structures and potentiate the central inhibitory effect of gamma-aminobutyric acid. In the cells of the central nervous system, specific “benzodiazepine” receptors (and their subgroups) have been identified, for which benzodiazepines are exogenous ligands (from the Latin ligo - I bind). Diphenylmethane derivatives (amizil, etc.) actively affect the cholinergic systems of the brain, which is why such drugs are called central anticholinergics. Propanediol derivatives do not have a pronounced effect on benzodiazepine and cholinergic receptors.

Benzodiazepine derivatives

This is a group of drugs, the representatives of which differ significantly from each other in the profile of psychotropic activity. Thus, a pronounced anxiolytic effect is especially characteristic of phenazepam, diazepam, nozepam, lorzepam, alprazolam (described in the section “Other antidepressants”). The sedative-hypnotic effect is more present in nitrazepam, alprazolam, flunitrazepam, triazolam. The anticonvulsant effect is especially pronounced in clonazepam, and to a lesser extent in phenazepam, sibazon and nitrazepam. The muscle relaxant effect is more characteristic of phenazepam, sibazon, lorazepam. “Daytime” tranquilizers have a predominant anti-anxiety effect. Benzodiazepines are generally well tolerated.

1. Chlozepidum (Chlozepidum). Synonyms: Librium, Napoton, Chlordiazepoxide, Elenium, Ansiacal, Droxol, Labiton and many others. etc. Until now, it has not lost its significance in the treatment of neurotic conditions with fears, anxiety, affective tension, irritability, impressionability, as well as shallow hypochondriacal depression, epilepsy, and alcohol withdrawal.

It is prescribed orally up to 3-4 times a day, regardless of meals. Treatment for adults begins with 5–10 mg per day. If necessary, the daily dose is gradually (5–10 mg) increased to 30–50 mg. The dose is also reduced gradually, as there is a possibility of developing withdrawal syndrome. Weakened and elderly patients are prescribed lower doses (up to 20 mg/day). Children, depending on age, are prescribed 2.5–5 mg per dose.

Side effects: dry mouth, drowsiness, slight dizziness, unsteadiness of gait, itching, nausea, constipation, dysmenorrhea, increased appetite, decreased libido, headache, hypotension, impaired concentration, slowed mental and motor reactions, weakened memory, agitation , aggressiveness, fear, muscle weakness. In some cases, excitement occurs at the beginning of treatment. Hallucinations, ataxia, and changes in peripheral blood patterns have also been described. Sometimes paradoxical reactions occur. The drug potentiates the effect of hypnotics and analgesics, and has a moderate hypnotic effect in the first 3–5 days of continuous treatment.

Contraindications for use: hypersensitivity, acute liver and kidney diseases, myasthenia gravis, first trimester of pregnancy, drug and alcohol dependence. The drug is not combined with MAO inhibitors and phenothiazine derivatives. It is not recommended to drink alcohol during the treatment period. Persons whose work requires quick mental and physical reactions should not take chlozepid on the eve of work.

These complications and contraindications to the use of chlozepid are characteristic of other benzodiazepine derivatives.

Release form: tablets of 5 mg in a package of 50 pieces.

2. Sibazon (Sibazonum). Synonyms: Apourin, Bensedin, Valium, Oxazepam, Relanium, Relium, Seduxen, Apozepam, Bensedin, Diazepam, Saromet, Serensin, Vatran, etc. One of the main benzodiazepine tranquilizers. Indicated for use in the treatment of various neuropsychic diseases: neuroses, psychopathy, as well as neurosis-like and psychopath-like conditions (schizophrenia, organic brain lesions, including cerebrovascular pathology and somatic pathology), accompanied by symptoms of emotional stress, anxiety, fear, irritability, senestohypochondriasis , obsessive-phobic disorder, sleep disorders. It is also used to relieve psychomotor agitation, anxious agitation in these diseases, status epilepticus, treatment of convulsive paroxysms and mental equivalents in epilepsy, spastic conditions, withdrawal syndrome in alcoholism (together with other drugs). In pediatric psychoneurological practice, it is used in the treatment of neurotic and neurosis-like conditions with the indicated symptoms, as well as headaches, enuresis, mood and behavior disorders. In somatic medicine it is used in the treatment of itchy dermatoses, gastric ulcers, cardiac arrhythmia, and in preparation for operations.

Prescribed orally, intramuscularly and intravenously. For adults, when taken orally, the drug is prescribed starting from 2.5–5 mg/day 1–2 times, regardless of food intake. If necessary, the single dose is gradually increased to 5–10 mg, and in some cases to 20 mg. The daily dose for inpatient treatment can reach 45 mg, for outpatient treatment - 25 mg. The maximum daily dose is 60 mg (in 2–3 doses). The dose reduction is also gradual. Weakened and elderly patients are prescribed 2.5 mg 1-2 times a day. Single and daily doses for children aged 1 to 3 years are 1 mg and 2 mg, respectively, from 3 to 7 years - 2 mg and 6 mg, from 7 years and older - 3-5 mg and 8-10 mg. For older children, if necessary, the daily dose can be increased to 14–16 mg. The duration of treatment should not exceed 2 months (risk of developing addiction to the drug!).

Sibazon is administered intravenously (drip or stream) and intramuscularly to adults in the treatment of diseases that are accompanied by agitation and convulsions; in the relief of status epilepticus, acute ones of various origins, including withdrawal symptoms and psychoses due to alcoholism. The average single dose is 10 mg (2 ml of 0.5% solution), the daily dose is 30 mg, and the maximum is 30 mg and 70 mg, respectively. A sedative effect is observed a few minutes after intravenous administration and 30–40 minutes after intramuscular administration of the drug. The actual therapeutic effect is detected after 3–10 days.

Status epilepticus is treated with an intravenous (slow!) infusion of 10–40 mg of sibazon. Repeated administration is done intravenously or intramuscularly every 3–4 hours. This technique is especially effective if the status of generalized seizures begins to be stopped in the first 3 hours after its onset.

Possible complications and contraindications for prescribing sibazone are basically the same as for treatment with chlozepid. When administered intravenously or intramuscularly, do not mix the drug with others (to avoid precipitation).

Release form: tablets of 5 mg in a package of 20 pieces; tablets for children 1 mg and 2 mg in a package of 20 pieces; 0.5% solution in ampoules (Solutio Sibazoni pro injectionibus) 2 ml in a package of 10 ampoules. Sibazon is an integral part of the sleeping pill Reladorm.

3.Phenazepamum. The strength of the tranquilizing effect is superior to other tranquilizers, and also has a pronounced anticonvulsant, muscle relaxant and hypnotic effect. Its anti-anxiety activity is not inferior to some neuroleptics. When used together with sleeping pills and narcotic drugs, their mutual potentiation occurs. Indicated for use in the treatment of neuroses, neurosis-like, psychopathic, psychopath-like and reactive conditions, which include anxiety, fear, affective tension, emotional excitability, as well as obsessive-phobic, hypochondriacal phenomena and panic attacks. Used in the treatment of alcohol withdrawal, epilepsy, and sleep deficiency.

It is prescribed orally, regardless of food intake, 2–3 times a day. The daily dose for adults in a hospital can reach 3–5 mg, in outpatient practice - 1.5 mg. For the treatment of epilepsy, it is prescribed in a dose of 2 to 10 mg/day, as a sleeping pill - up to 2.5 mg per dose (20–30 minutes before bedtime). Relief of alcohol withdrawal requires administration of 2.5 to 5 mg/day. The maximum daily dose should not exceed 10 mg.

Possible side effects and contraindications for use are the same as for treatment with chlozepid and sibazon. More often observed, however, are ataxia, drowsiness, muscle weakness, and dizziness.

Release form: tablets of 0.5 mg and 1 mg in a package of 50 pieces; tablets of 2.5 mg in a package of 20 pieces.

4.Nozepamum. Synonyms: Apo-oxazepam, Medazepam, Rudotel, Tazepam, Oxazepam, Oxazepam, Rondar, Serax, etc. Its properties are similar to chlozepid and diazepam, but inferior to them in potency. Somewhat less toxic than them, in some cases it is better tolerated, especially by elderly and somatically weakened patients. Indications for use, side effects, contraindications for use are similar to those for treatment with chlozepid.

It is prescribed orally, regardless of food intake, 2–3 times a day. The initial single dose for adults is 5–10 mg, the average therapeutic dose per dose is 20–30 mg.

Release form: tablets of 10 mg in a package of 50 pieces.

5.Lorazepam. Synonyms: Apolorazepam, Ativan, Lorafen, Merlit, Trapex, etc. Similar to triazolam (see below). It has pronounced tranquilizing activity and can be used in the treatment of mental disorders (panic attacks, reactive psychoses, subpsychotic phenomena). Indications for use, side effects, contraindications for use are similar to those for treatment with chlozepid.

It is prescribed orally, regardless of food intake, 2–3 times a day. For neurotic conditions, it is prescribed in a dose of 1.25–5 mg/day, for the treatment of psychosis - up to 15 mg/day.

Release form: tablets of 2.5 mg in a package of 50 pieces.

6. Bromazepam. Synonyms: Bromazep, Lexotan, Bartul, Deptran, Pascalium and many others. etc. Anxiolytic with sedative-hypnotic, anticonvulsant and muscle relaxant effects. In terms of action, indications for use, side effects and contraindications, it is similar to other benzodiazepines. When taken once, it has a short-term effect.

It is prescribed orally, regardless of food intake, 2–3 times a day at a dose of up to 36 mg/day (in a hospital setting), in outpatient practice - 1.5–3 mg per dose.

Release form: tablets of 1.5 mg, 3 mg and 6 mg.

7.Mezapamum. Synonyms: Nobrium, Rudotel, Anxitol, Imazepam, Merlit, Stratium and many others. etc. The peculiarities of the drug's action are the less pronounced muscle relaxant and general depressant effect, the presence of some stimulating radical. It is considered a “daytime” tranquilizer, suitable for treating children, elderly and somatically weakened patients. Indications, contraindications for use, and side effects are generally similar to those for treatment with other benzodiazepines, excluding acute states of fear and anxiety, reactive psychoses, and status epilepticus.

It is prescribed orally 2-3 times a day, regardless of meals. The average daily dose for adults is 30–40 mg, the highest is 60–70 mg. Elderly and adolescents are prescribed up to 20–30 mg/day, children aged 1–2 years – 2–2.5 mg/day, from 3 to 6 years – 3–6 mg/day, from 7 to 10 years – 6–24 mg/day.

Release forms: tablets 10 mg; granules (20 pieces, containing 40 mg of mezapam) for the preparation of a suspension for children in jars marked 100 ml. The suspension is prepared using freshly boiled chilled water.

8.Gidazepamum. Interacts with benzodiazepine receptors in the limbic system, in the interneurons of the lateral horns of the spinal cord. It has anxiolytic, anticonvulsant and weak muscle relaxant effects. Refers to “daytime” tranquilizers, does not have a hypnotic effect. Unlike many tranquilizers, it has a psychoactivating effect. Indications and contraindications for use, side effects are generally the same as for treatment with chlozepid. Gidazepam is also prescribed for the treatment of migraine.

It is prescribed orally, regardless of meals, 3 times a day, starting from 6–15 mg/day. The dose is gradually increased to 60–200 mg/day. For migraine and logoneurosis, the therapeutic dose is 40–60 mg/day. The duration of the course of therapy is from several days to 3–4 months.

9. Clobazam. Synonyms: Frisium, Clarmyl, Frizin, Sentil, Urbanil, etc. Anxiolytic with anticonvulsant action. Indicated for the treatment of painful conditions with acute and chronic feelings of fear, as well as as an additional remedy - epilepsy, dysphoria, aggressiveness.

It is prescribed orally, regardless of food intake, 2–3 times a day. The dose for adults for neurotic conditions is 10–20 mg/day, for feelings of fear - from 20 to 30 mg/day. The drug is not prescribed for children under 3 years of age; reduced doses are recommended for children over 3 years of age, as well as for elderly patients. When treating epilepsy, the initial dose of the drug is 5–15 mg/day, it can be increased to 80 mg/day (maximum daily dose). Dose increases and decreases should be gradual; As with treatment with other tranquilizers, withdrawal syndrome may occur.

Side effects and contraindications for use are the same as for treatment with other benzodiazepines. When treated with high doses and for a long time, there may be articulation disorders, diplopia, nystagmus, and in elderly patients - impaired consciousness.

Release form: tablets of 5 mg and 10 mg.

10.Alprazolam - see Other Antidepressants.

11.Tetrazepam. Synonyms: Myolastan, Myolastan. Anxiolytic with a pronounced muscle relaxant effect. Indicated for the treatment mainly of muscle contractures, tendovaginitis, myositis, accompanied by muscle pain.

It is prescribed orally, regardless of food intake, 2–3 times a day in doses for adults of 50 to 150 mg/day.

Side effects and contraindications for use are the same as for treatment with other benzodiazepines.

Release form: tablets of 50 mg in a package of 20 pieces.

12.Signopam. Synonyms: Temazepam, Euhuphos, Levanxene, Normison, Planum, Texapan, Veroqual, etc. Anxiolytic with a mild antidepressant effect. Indicated for the treatment of neuroses and neurosis-like conditions, especially those accompanied by depressed mood and hypochondriacal phenomena; shallow depression, increased neuropsychic excitability in thyrotoxicosis. It has a pronounced anticonvulsant and antidysphoric effect.

Prescribed orally, regardless of food intake, 10 mg 2-3 times a day (adults). The dose can be increased to 40 mg/day (in 2–3 divided doses). Doses are increased and decreased gradually over 7–10 days.

Side effects: there may be (rarely) drowsiness, fatigue, dizziness, allergic skin reactions, decreased libido, dysmenorrhea, and in some cases disorientation. Drinking alcohol and driving a vehicle is prohibited.

Contraindications for use: hypersensitivity, drug and alcohol dependence.

13. Tranxene. Synonyms: Anxidin, Belseren, Tranex, Tranxilen. Anxiolytic with sedative, muscle relaxant and anticonvulsant effects. Can be used to relieve psychomotor agitation when administered parenterally. Prescribed orally, intramuscularly and intravenously. The average therapeutic dose when taking the drug orally by adults is 10–30 mg/day. The dose can be increased to 50–100 mg/day. For elderly and senile patients, the drug is prescribed in reduced doses. To relieve psychomotor agitation and attacks of aggressiveness, the drug is administered intramuscularly or intravenously at a dose of 20 to 200 mg/day.

Side effects: drowsiness, muscle weakness, anterograde amnesia, euphoria, paradoxical mental reactions (increased fear, aggressiveness, etc.). With a sharp reduction in dosage, withdrawal syndrome may develop.

Contraindications for use: hypersensitivity, respiratory and heart failure, pregnancy, breastfeeding, childhood.

14.Nitrazepam. Synonyms: Berlidorm, Neozepam, Radedorm, Eunoktin, Apodorm, Benzalin, HinpaxInsomin, Magadon, Nitrodiazepam, Senerex and many others. etc. Increases the sensitivity of benzodiazepine receptors to the mediator, enhances the inhibitory effect of GABA in the central nervous system, reduces the excitability of cells in the cortex and subcortical areas of the brain, and inhibits cells of the reticular formation. It has a tranquilizing, muscle relaxant, anticonvulsant effect, inhibits conditioned reflexes, suppresses polysynaptic spinal reflexes. A distinctive feature is its hypnotic, hypnotic effect; it prolongs sleep and improves its quality. Indicated for the treatment of various sleep disorders, neuroses and psychopathy with symptoms of anxiety, fear, and affective tension. In combination with other drugs, it is used in the treatment of schizophrenia, affective and schizoaffective psychoses, some organic and toxic damage to the central nervous system, in particular cerebrovascular disorders and chronic alcoholism. In combination with anticonvulsants, it is used in the treatment of epilepsy.

It is prescribed orally regardless of food intake. As a hypnotic, it is used once half an hour before bedtime at a dose of 5–10 mg for adults, 2.5–5 mg for elderly patients. For this purpose, the drug is also prescribed to children in a smaller dose: under 1 year of age - 1.25–2.5 mg; from 1 year to 5 years - 2.5–5 mg; from 6 to 14 years - 5 mg. The maximum single dose as a sleeping pill for adults is 20 mg.

As a tranquilizer and anticonvulsant, nitrazepam is used 2–3 times a day, 5–10 mg (for adults). If necessary, the dose for the treatment of epilepsy can be increased. The highest daily dose of the drug is 30 mg. The course of treatment averages 4–6 weeks.

Side effects: daytime drowsiness, feeling of lethargy, ataxia, impaired coordination of movements, headache, stupor, dizziness, less often - nausea, tachycardia, hyperhidrosis, skin allergic reactions. In most cases, these phenomena are observed in elderly and somatically weakened patients. The dose of the drug should be reduced or treatment should be stopped.

Contraindications for use: first trimester of pregnancy, myasthenia gravis, liver and kidney diseases with impaired function, working with patients who require a quick mental and physical reaction. Consumption of alcoholic beverages is prohibited. One should keep in mind the possibility of enhancing the effect of analgesics and other neurotropic drugs.

Release form: tablets of 5 mg in a package of 20 pieces.

15.Flunitrazepam. Synonyms: Rohypnol, Somnubene, Hypnodorm, Narcozep, Primum, Sedex, etc. Close to nitrazepam. Has a sedative, hypnotic, anticonvulsant effect. Indicated for the treatment of insomnia. In anesthesiological practice it is used for premedication and immersion in anesthesia.

Prescribed orally half an hour before bedtime in a dose of 1–2 mg for adults, 0.5 mg for elderly patients; Children under 14 years of age are prescribed extremely rarely and only 0.5–1 mg. Parenterally used for premedication (1–2 mg intramuscularly), for induction of anesthesia - 1 mg intravenously (administered slowly).

Side effects and contraindications for use are the same as for treatment with nitrazepam. There is a possibility of developing withdrawal syndrome.

Release forms: tablets of 2 mg in packages of 10, 30 and 100 pieces; in ampoules of 2 mg of the drug and with the addition of ampoules with 1 ml of sterile water for injection, in a package of 25 ampoules (the drug cannot be administered without a solvent).

16. Triazolam (Triazonam). Synonyms: Somneton, Halcion, Apo-Triazo, Clorazolam, Nuctan, Somneton, Songar, etc. Similar in structure to alprazolam. Short-acting hypnotic, other aspects of action have not been studied enough.

Prescribed orally 20–30 minutes before bedtime at a dose of 0.25–0.5 mg (adults).

Release form: tablets of 0.25 mg (blue) and 0.5 mg (white). Foreign analogues of triazolam: Fluracepam, synonyms - Benozil,

Fluzepam, Waldorm, etc.; Lorazepam, synonyms - Almazin, Ansilor, Ativan, Durazolam, Sedatival, etc.; Tomazepam, synonyms - Cerepax, Levaxol, Temazepam, Temazin, etc.

17.Zopiclone. Synonyms: Piclodorm, Relaxon, Somnol. Activates GABAergic mechanisms of synaptic transmission in the brain. Has a sedative and hypnotic effect. It is prescribed mainly for the treatment of deficiency and deterioration in sleep quality of various origins, including depression, as well as for the treatment of nocturnal asthma (in combination with theophylline).

It is prescribed orally half an hour before bedtime as a single 7.5 mg tablet (for adults), for elderly patients - ½ tablet. The course of treatment is no more than 1 month. The maximum dose is 15 mg.

Side effects: lethargy, drowsiness, bitter and metallic taste in the mouth, nausea, irritability, depressed mood, withdrawal syndrome, allergic skin reactions, impaired consciousness. The drug reduces the concentration of trimipramine in the blood and reduces its effect. Strengthens the effect of sedatives and alcohol.

Contraindications for use: hypersensitivity, severe degrees of respiratory failure, pregnancy, breastfeeding, age under 15 years.

Release form: 7.5 mg tablets.

18.Estazolam. Excites benzodiazepine receptors, enhances GABAergic transmission and its inhibitory effect. Anxiolytic with sedative, hypnotic and central muscle relaxant effects. Indicated for the treatment of neuroses and neurosis-like conditions with depressive-phobic symptoms, anxiety, affective tension, sleep disorders, as well as epilepsy (as an adjuvant).

It is prescribed orally, regardless of meals, several times a day. The average therapeutic dose for adults is 4–6 mg/day. The tablets should be swallowed whole with a small amount of water. As a sleeping pill, 2-4 mg is prescribed (for elderly patients - 1 mg) half an hour before bedtime. The increase and decrease in dosage is gradual; with long-term treatment, there may be a withdrawal syndrome with restlessness, anxiety, and fears. Drinking alcohol is prohibited.

Side effects: daytime drowsiness, fatigue, weakness, irritability, headache, dizziness, ataxia, disorientation, impaired memory and thinking, addiction, dependence. The drug enhances the effect of sedatives. It should be prescribed with caution to persons whose work requires rapid physical and mental reactions. A paradoxical reaction to the drug is possible.

Contraindications for use: hypersensitivity, myasthenia gravis, ataxia, severe respiratory failure, impaired consciousness, closed-angle glaucoma, dependence on alcohol and drugs, pregnancy, breastfeeding, age under 18 years.

Release form: 1 mg tablets.

19.Clonazepam. Synonyms: Antelepsin, Rivotril, Clonopin, Ictorivil, Rivatril, etc. Interacts with benzodiazepine receptors, has a GABAergic effect in the limbic system, reticular formation, interneurons of the spinal cord. Reduces the excitability of the subcortical structures of the brain and disrupts their interaction with the cerebral cortex. Anxiolytic with anticonvulsant, antiepileptic and sedative activity, has a hypnotic and central muscle relaxant effect. It is used mainly for the treatment of epilepsy with large, temporal, focal and minor seizures, paroxysmal fear syndromes, phobias (in patients over 18 years of age) and manic states, especially in epilepsy; psychomotor agitation in reactive psychoses, as well as insomnia and muscle hypertension.

It is prescribed orally, regardless of food intake, 3 times a day. The initial dose for adults is 4.5 mg/day. The dose can be gradually, every 3 days, increased by 0.5–1 mg to 4–8 mg/day. The maximum dose is 20 mg/day. In the syndrome of paroxysmal fear in adults, 1 mg / day is prescribed, up to a maximum of 4 mg / day. The dose for children is 0.01–0.03 mg/kg/day for 3 doses. Children under the age of 1 year are given 0.1-1 mg / day, from 1 year to 5 years - 1.5-3 mg / day, from 6 to 16 years - 3-6 mg / day. The maximum dose for children is 0.05 mg/kg/day for 3 doses.

Side effects: drowsiness, dizziness, ataxia, choreic hyperkinesis, dysarthria, weakness, fatigue, nervousness, insomnia, visual disturbances, memory and speech disorders, emotional lability, hypersalivation or xerostomia, constipation, abdominal pain, muscle pain, dysmenorrhea, increased frequency urination or urinary retention, decreased appetite and libido, depression, disorientation, paradoxical reactions to the drug, allergic skin reactions, alopecia, hirsutism, erythro-, leukemia and thrombocytopenia, increased concentrations of transaminases and alkaline phosphatase in the blood, withdrawal syndrome, addiction, dependence, etc. The drug enhances the effect of barbiturates, neuroleptics, antidepressants, anticonvulsants, narcotic analgesics, alcohol and drugs that reduce skeletal muscle tone. Cases of pathological intoxication have been reported when drinking alcohol.

Contraindications for use: hypersensitivity, impaired liver and kidney function, myasthenia gravis, pregnancy, impaired consciousness, central respiratory failure, respiratory failure, glaucoma.

Release form: tablets of 0.5 mg and 2 mg.

Currently, a large number of so-called neuropsychotropic drugs are widely used - drugs that in one way or another affect the state of the patient’s emotional sphere by balancing the processes of excitation and inhibition in the central nervous system. These primarily include sedatives that enhance and concentrate the process of inhibition in the cerebral cortex, neuroleptics ("major" tranquilizers) - sedatives that weaken the process of excitation in the brain, and tranquilizers ("small") that have a calming effect. Certain neuropsychotropic drugs have different mechanisms of action and pharmacological activity in the patient's body, as well as a predominant effect on various emotional disorders (fear, anxiety, melancholy, increased nervous excitability, anger, etc.). Depending on the nature, severity and duration of emotional disorders, the choice of medication is made in each specific case. Tranquilizers and, especially, neuroleptics also have an analgesic effect and potentiate the effect of hypnotics, analgesics and muscle relaxants.

a) Sedatives

Sodium bromide (Natrii bromidum) and potassium bromide (Kalii bromidum) are more often used orally in mixtures and tablets - in doses from 0.1 to 1.0 g. Sodium bromide, in addition, can also be administered intravenously in 5 - 10 ml 5 - 20% solution. Bromides are slowly excreted from the body, due to cumulation, side effects ("bromism") can be observed: runny nose, cough, skin rash, memory loss, etc.

Bromcamphara is prescribed orally at a dose of 0.15 - 0.5 g 2 - 3 times a day.

Valerian is used in the form of infusion and alcohol tincture. Infusion of valerian (Infusum radicis Valerianae) is prepared at the rate of 6 - 10 g of root per 180 - 200 ml of distilled water and is administered orally 1 tablespoon 2 - 4 times a day. Often, valerian infusion is included in a mixture with sodium bromide. Valerian tincture (Tinctura Valerianae) is taken orally at a dose of 20-30 drops 2-4 times a day.

Motherwort herb is also used in the form of infusion and alcohol tincture. An infusion of motherwort herb (Infusum herbae Leonuri) is prepared at a ratio of 10-15 g of herb and 180-200 ml of water, prescribed 1 tablespoon 3-4 times a day. Motherwort tincture (Tinctura Leonuri) is administered orally 30-50 drops 3-4 times a day.

b) Neuroleptics

These include phenothiazine derivatives and drugs of other pharmacological groups.

Phenothiazine derivatives:

Aminazine (Aminasi-num) - chlorpromazine - is taken orally in a dragee of 0.025 - 0.1 g, and the course of treatment begins with lower dosages (0.025 - 0.075 g per day), then increases to 0.3 - 0.6 g, and by the end of the course it decreases again to the original level. Intramuscularly, the drug can be administered as a 0.25 - 0.5% solution (2 - 5 ml), and intravenously - 2.5% solution (1-2 ml of the drug is diluted in 10 - 20 ml of 5% glucose solution and injected slowly) . With prolonged use of chlorpromazine or other phenothiazine derivatives, side effects may develop in the form of neuroleptic parkinsonism, the clinical picture of which resembles the syndrome of vascular or post-infectious parkinsonism described in Chapter II. The occurrence of such complications requires immediate discontinuation of the drug and the appointment of antiparkinsonian drugs, described below. Included in List B.

Levomepromazine (Levomepromazinum) - tizercin - is prescribed orally in tablets of 0.025 - 0.1 g 3 - 4 times a day or intramuscularly in the form of a 2.5% solution (1-2 ml). Belongs to list B.

Triftazinum - stelazine - can be used orally and intramuscularly. It is prescribed orally with a dose of 0.001-0.005 g per dose (after meals), with a gradual increase to 0.01-0.03 g, 2 - 4 times a day. The drug is administered intramuscularly in a dose of 0.001 - 0.002 g, up to 4 - 6 times a day. A peculiarity of the action of trifazine is its ability to cause in patients an increase in interest in the environment and physical activity, to facilitate their involvement in productive work. Belongs to list B.

Thioridazine (Thioridazinum) - sonapax, melleril - has, along with a sedative, a beneficial effect on pathologically altered mood - a thymoleptic effect. Oral administration is carried out in doses of 0.005 - 0.01-0.025 g 2 - 3 times a day. Belongs to list B.

All phenothiazine derivatives, with the exception of thioridazine, are contraindicated in diseases of the liver and kidneys in the decompensation phase, diseases of the hematopoietic organs, rheumatic carditis, thromboembolic disease, in severe cases of bronchiectasis, and glaucoma.

Other antipsychotics:

Haloperidol (Haloperidolum) is a sedative and antiemetic. It is prescribed orally, administered intramuscularly and intravenously. Oral dose: 0.005 - 0.01 g per day (3 - 5 doses). 0.4-1 ml of a 0.5% solution of the drug is administered parenterally 2 - 3 times a day. Belongs to list B.

Trifluperidol (Trifluperidolum) - trisedyl - is similar in action to haloperidol, but also has anticonvulsant activity. It is prescribed orally and also intramuscularly. The initial dose of oral administration is 0.00025-0.0005 g per day (2-3 doses), subsequently it increases to 0.001-0.002 g per day over 4 to 6 days. For intramuscular injection, 0.00125 - 0.0025 g of the drug (0.25 - 0.5 ml of 0.1% solution) is administered. Belongs to list B.

Haloperidol and trifluperidol with long-term use can cause extrapyramidal disorders (parkinsonism), which requires the prescription of antiparkinsonian drugs. Both drugs are contraindicated in case of organic lesions of the central nervous system, decompensated diseases of the kidneys and cardiovascular system.

Indole derivatives in the form of rauwolfia alkaloids have a calming and hypotensive effect. They are used in all cases where the use of antipsychotics is indicated, especially in patients with arterial hypertension and impaired renal function.

Reserpine (Reserpinum) - rausedil, serpasil - is taken orally after meals in tablets of 0.00025 - 0.0005 g 3 - 4 times a day; the course of treatment is 1-6 months. There may be side effects in the form of gastrointestinal disorders (nausea, vomiting, diarrhea), bradycardia, dizziness. Contraindications: severe organic cardiovascular diseases, bradycardia, peptic ulcer of the stomach and duodenum. Belongs to list A.

Raunatin (Raunatinum) has a weaker sedative and hypotensive effect than reserpine. Taken orally after meals in tablets of 0.002 g, starting with 1 tablet at night, and then 3 - 6 tablets per day. Belongs to list B.

c) Tranquilizers

Tranquilizers have a slightly less pronounced sedative effect compared to neuroleptics, but they are better tolerated by patients and are less likely to cause side effects. Many tranquilizers have the properties of central muscle relaxants, reducing pathologically increased skeletal muscle tone.

Meprotanum - andaxin, meprobamate - is a sedative that causes relaxation of striated muscles. Taken orally in tablets of 0.2 - 0.4 g 2 - 3 times a day. Belongs to list B.

Isoprotanum (Isoprotanum) - scutamil - is also a central muscle relaxant and at the same time a tranquilizer, potentiates the effect of hypnotics and analgesics. Prescribed orally after meals, 0.2 g (1 tablet) 2 to 4 times a day. Possible side effects: drowsiness, dyspeptic symptoms. Contraindication: epilepsy. One of the forms of release of this drug is Scutamul-C, which contains 0.15 g of isoprotan and 0.1 g of the painkiller paracetamol in 1 tablet. Prescribed 1 tablet 3 times a day after meals if necessary to reduce skeletal muscle tone or reduce pain. Isoprotan and scutamyl-C are included in list B.

Chlordiazepoxide (Chlordiazepoxidum) - elenium, librium - also has a calming and muscle relaxant effect, and has an anticonvulsant effect. It is prescribed orally in the form of tablets of 0.005 - 0.01 g 2 - 4 times a day. Occasionally, side effects such as drowsiness, dizziness, and general weakness are possible.

Contraindications: acute liver and kidney diseases. Belongs to list B.

Diazepam (Seduxen) is pharmacologically more active than chlordiazepoxide and helps improve sleep. Taken orally in tablets of 0.005 - 0.01 g (1-2 tablets) 2 - 3 times a day, 2 ml of a 0.5% solution of the drug diluted with 20 ml of a 40% glucose solution is slowly injected intravenously. Belongs to list B.

Nitrazepam (Nitrazepamum) - eunoctine, radedorm - has a pronounced sedative and especially hypnotic effect. Relaxes skeletal muscles. It is taken orally in tablets of 0.005 - 0.01 g, usually 30 minutes before bedtime. Belongs to list B.

Oxylidinum is a sedative and antihypertensive drug. It is used in gradually increasing dosages orally, subcutaneously or intramuscularly. Oral administration begins with 1 tablet (0.02 g) 3-4 times a day, and then the single dose is increased to 2-4 tablets per dose. For parenteral administration, the initial dose is 0.02 g (1 ml of a 2% solution), and then increases to 0.05 - 0.1 g (1-2 ml of a 5% solution). Long-term use of the drug is possible for 1/7 to 4 months. Belongs to list B.

Trioxazin is prescribed orally at 0.3 - 0.6 g (1 - 2 tablets) 2 - 3 times a day, with a gradual increase in the single and daily dose. Side effects may occur in the form of general weakness, nausea, drowsiness, dry mouth and pharynx. Belongs to list B.

Phenibut (Phenibut) - fenigama - a new drug that has a pronounced tranquilizing effect. Being a derivative of gamma-aminobutyric acid, which is involved in metabolic processes in the central nervous system, phenibut has no contraindications and does not cause side effects. Taken orally at 0.25 - 0.5 g (1-2 tablets) 2 - 4 times a day.

Tacitin (Tacitinum) has a tranquilizing and muscle relaxant effect. Taken orally in tablets of 0.01-0.02 g (1 - 2 tablets) 2 - 3 times a day. Side effects: general weakness, dry mouth. Contraindications: severe damage to the liver and kidneys.

Magnesium sulfate (Magnesium sulfuricum) has a sedative, hypnotic, anticonvulsant, choleretic and hypotensive effect. When treating neurological patients, the drug is administered parenterally (intramuscularly or intravenously): 5 - 20 ml of 20% or 25% solution; intravenous medication should be administered slowly.

Demidenko T. D., Goldblat Yu. V.

"Sedatives, neuroleptics and tranquilizers" and others

Anxiety is considered one of the most common affective states. Moreover, it can also occur in a completely healthy person; moreover, everyone has experienced a similar sensation to one degree or another.

Anxiety is divided into physiological, which occurs when there is a completely objective or perceived threat, and pathological, which appears for no apparent reason. It is the latter that is classified as anxiety disorders.

They are often accompanied by noticeable discomfort, asthenic condition, insomnia, dizziness, and vegetative symptoms. It is this clinical picture that requires the prescription of certain medications. Strong tranquilizers are one of the most common groups of psychotropic drugs, but their use should be under the supervision of a physician.

A number of brain structures are responsible for the formation of a sense of threat when analyzing certain environmental factors:

• amygdala (almygdala);
• an insula located in the cerebral cortex;
• ventral striatum;
• hypothalamus;
• areas of the cingulate and prefrontal cortex;
• hippocampus

The amygdala provides instant assessment of incoming information and selectively responds to threats, creating a feeling of anxiety. The hippocampus and prefrontal cortex regulate the strength of the emotional response, and suppress the response when it is no longer appropriate to the situation.

As a result, the production of a number of hormones and neurotransmitters changes, which further exacerbates the changes occurring in the brain. However, timely prescribed medications can stop the progression of the pathology and return a person to a normal emotional state.

The class of psychotropic drugs is very broad and includes several groups of drugs, each of them classified separately according to the principle and duration of action, chemical structure and other parameters.

The first psychotropic drugs appeared in the early 50s of the twentieth century. These were quite potent medications that were used in specialized hospitals. Later, experts developed relatively safe, “light” medications that are suitable for use at home. Moreover, some such drugs are sold without a doctor’s prescription.

Psychotropics can be divided into two large groups: drugs with sedative and stimulant effects.

The first class includes:

• neuroleptics (also called antipsychotic drugs);
• strong and mild tranquilizers (anxiolytics);
• sedative medications.

The second class includes:

• nootropics;
• actoprotectors;
• adaptogens;
• psychomotor stimulants;
• mood stabilizers (lithium preparations);
• analeptics.

The effects of drugs from different groups of psychotropic medications overlap in some sense. Thus, many antidepressants (especially the first and second generation) have a pronounced anxiolytic and sedative effect. That is why the use of tranquilizers and other drugs for the treatment of anxiety disorders, sleep disorders, and stress conditions should be monitored by a doctor.

The dosage of such drugs is also selected individually. On the one hand, the drug must have a pronounced therapeutic effect, and on the other hand, it must be accompanied by a minimum of unwanted reactions. The duration of therapy is also of great importance.

Tranquilizers are often addictive, and if taken uncontrolled, the patient has to constantly increase the dosage of the medicine. Therefore, the doctor monitors the relationship between the amount of the drug taken during the day and the effect. If necessary, the drug is canceled and replaced with an analogue, but from a different pharmacological group.

Classification and brief description

Drugs of this class are widely used to treat a variety of anxiety disorders, accompanied by characteristic symptoms. Since 1955, medications of this group have taken leading positions in the list of the most popular and prescribed drugs in psychotherapy and neurology.

According to their chemical structure, tranquilizers are divided into:

• benzodiazepines (benzodiazepine derivatives) - Phenibut, Nozepam, Chlozepid, Rohypnol, Phenazepam, etc.;
• propanediol derivatives - Meprotan, Scutamil, Meprobamate;
• diphenylmethane derivatives - Amizil, Benactizine;
• derivatives of various chemical groups (they are also called unclassified tranquilizers) - Oxylidene, Mebicar, Buspirone.

According to the duration of action (based on pharmacokinetics, in particular, half-life), tranquilizers are:

• long-acting - longer than 24 hours (Diazepam, Phenazepam, Alprazolam);
• average duration of action - from 6 hours to a day (Lorazepam, Nozepam);
• short-acting - up to 6 hours (Midazolam, Triazolam).

It is quite arbitrary, but convenient for a practicing physician, to divide tranquilizers into “day” (or minor) and “night” ones. This classification is based on the severity of the sedative effect of the drug.

Among benzodiazepine derivatives, several groups are also distinguished:

• with a predominance of anxiolytic action (Diazepam, Phenazepam);
• with a pronounced sedative effect (Nitrazepam);
• with a predominance of anticonvulsant action (Clonazepam).

According to their mechanism of action, tranquilizers are divided into:

• drugs that interact with the so-called benzodiazepine receptors, “working” in tandem with γ-aminobutyric acid receptors (for example, Diazepam, Phenazepam, etc.);
• agonists (substances that enhance the activity and response of the receptor in response to the influence of a particular neurotransmitter) of serotonin receptors (Buspirone);
• drugs with different mechanisms of action (for example, Amizil).

Tranquilizers are prescribed when the effect of other, less potent drugs is absent. Also, such medications are indicated after the use of non-drug treatments for neuroses and anxiety disorders.

Neuroleptics

These drugs are used to treat severe disorders of the central nervous system. Neuroleptics have a complex effect on the body. Similar medications:

• reduce psychomotor agitation;
• reduce feelings of fear and anxiety;
• eliminate aggressiveness;
• suppress delusions, hallucinations and other psychopathic syndromes;
• cause a drowsy state, but do not have a pronounced sedative effect.

Some antipsychotics suppress the gag reflex by affecting certain structures of the brain.

The classification of such drugs is also based on their chemical structure. There are:

• phenothiazine derivatives (Aminazine, Thioridazine, Fluphenazine, Triftazine, etc.);
• thioxanthene derivatives (Chlorprothixene, Zuclopenthixol);
• butyrphenone derivatives (Haloperidol, Droperidol);
• indole derivatives (Carbidine, Sertindole);
• substituted benzamides (Sulpiride, Tiapride);
• drugs of different pharmacological groups (Pimozide, Risperidone, Azaleptin).

The principle of action of neuroleptics has not been sufficiently studied. But it is believed that the combination of sedative and anxiolytic effect is due to inhibition of the activity of dopamine receptors and blocking of serotonin receptors. This is also associated with undesirable reactions that often occur during the use of antipsychotics.

So the most common complication is drug-induced parkinsonism (muscle rigidity and tremors). Long-term use of such medications is also accompanied by neurolytic syndrome (decreased memory, intelligence, emotional instability).

Psychostimulants

Psychomotor stimulants are drugs that enhance mental and physical activity. Such drugs are characterized by a high speed of onset of effect and stimulation of brain function. However, such an effect is accompanied by a rapid depletion of the reserves of the central nervous system, so the use of psychostimulants requires compliance with rest and sleep.

Medicines in this class are divided into:

• purine derivatives, the most famous representative of this group is caffeine;
• derivatives of phenylalkylamines, the reference drug - phenamine (amphetamine sulfate) is prohibited in most countries due to rapidly developing addiction, therefore Sidnocarb is prescribed;
• Piperidine derivatives, this group includes Meridil; its principle of action is similar to Sidnocarb, but less effective.

Psychostimulants are used for asthenic syndrome, lethargy, and neurotic conditions. Sometimes they are prescribed to patients with indolent schizophrenia.

Normitimiki

The literal translation of this term means mood stabilizers. This is the first time that lithium salts have been named in this way. But with the accumulation of clinical and practical experience in the treatment of mania, pathological anger and irritability, and bipolar disorders, the group of mood stabilizers was supplemented by anticonvulsants and other drugs that, at first glance, do not have a direct effect on a person’s mental state.

Today, normotimics include:

• lithium preparations (Lithium carbonate, Micalit, Lithium oxybutyrate);
• derivatives of valproic acid (Depakine, Depakone, Depakote);
• anticonvulsants (Lamotrigine, Gapabentin);
• antiepileptic drugs (Carbamazepine);
• calcium channel blockers (Verapamil).

However, they are prescribed with caution due to the high risk of liver and kidney damage.

Nootropic drugs

The name of this class of medications comes from the Greek words “noos” - mind and “tropos” - desire. These are relatively safe drugs that improve memory, cognitive function, and mental activity. They have the ability to increase stress resistance.

There are so-called true nootropics, which are divided into groups depending on the chemical structure and mechanism of action. Thus, there are derivatives of pyrrolidone (Piracetam), γ-aminobutyric acid (Aminalon, Phenibut), antioxidants (Mexidol). In addition, a number of other medications have a nootropic effect. These include Pentoxifylline, products based on ginkgo biloba, ginseng, lemongrass, echinacea, Actovegin.

How do tranquilizers work: the effect they have, the differences between “day” and “night” tranquilizers

The effect produced by the use of tranquilizers is associated with the influence on the functions of certain structures of the limbic system and the cerebral cortex. The active substances of the drugs interact with specific benzodiazepine GABAergic receptors, causing their activation. In this case, a channel opens in the cell membranes, selectively allowing chloride ions (Cl-) to pass through. Their accumulation reduces the activity of many neurons in the central nervous system.

The sedative properties of tranquilizers are associated with the effect on another type of benzodiazepine receptors, which are predominantly located in the reticular formation of the brain stem and the thalamus.

Tranquilizers have the following spectrum of therapeutic action:

• anxiolytic (reduce fear, eliminate delusions, hallucinations and other symptoms of anxiety disorders);
• sedative;
• hypnotic;
• anticonvulsant;
• muscle relaxant (anticonvulsant);
• vegetostabilizing (restores normal functional activity of the autonomic nervous system).

Due to the mechanism of how tranquilizers act, such drugs can enhance the effect of other drugs:

• sleeping pills;
• sedatives;
• narcotic analgesics.

Therefore, when combining these groups of medications, it is necessary to strictly monitor the dosage and well-being of the patient.

When taken in tablet form, the active substances of tranquilizers are quickly absorbed into the systemic bloodstream (the maximum concentration is achieved within a period of 30 minutes to several hours). Such drugs penetrate well through the blood-brain barrier and are therefore distributed throughout the tissues of the brain and central nervous system. Also, the active ingredients of tranquilizers are found in muscles and other tissues.

Primary metabolism occurs in the liver, but tranquilizers are excreted through the kidneys, and only a small part through the digestive tract. The pharmacodynamics of such drugs depend on the age factor. Therefore, for elderly patients and children, the dosage is selected individually.

The equilibrium concentration of the active ingredients of the drugs is not achieved immediately. In general, this period takes from 5 days to two weeks, provided that it is used regularly in the recommended dosage.

Currently, the so-called “daytime” tranquilizers deserve special attention. They have minimal sedative and hypnotic effects, so their use has less impact on the patient’s quality of life. In addition, their use is not accompanied by cognitive disorders, memory impairment and other adverse reactions.

The list of “daytime” tranquilizers includes the following drugs:

• Gidazepam;
• Mezapam (Medazepam);
• Grandaxin (Tofisopam);
• Trioxazine (currently not used due to license expiration);
• Spitomin (Buspirone).

Anxiolytics cannot be used independently due to the risk of addiction and other unwanted reactions. Doctors prescribe similar drugs for:

• neuroses;
• anxiety disorders;
• panic attacks;
• depression (practically not used for monotherapy, prescribed in combination with other drugs);
• severe withdrawal syndrome caused by withdrawal from alcohol, nicotine or drug addiction;
• disorders associated with vegetative-vascular dysfunction;
• frequently recurring epileptic seizures;
• nervous disorders caused by dermatological diseases, pathologies of the digestive tract, musculoskeletal system and other organs and systems;
• preoperative preparation (in combination with drugs for anesthesia);
• convulsive syndrome.

But despite the pronounced therapeutic effect, many patients refuse to use anxiolytics. This is due to the fact that the principles of how various tranquilizers work are shrouded in many myths that are not always related to the real state of affairs.

Thus, it is widely believed that anxiolytics:

• impair memory, concentration and other brain functions;
• addictive;
• cause constant drowsiness;
• turned into a “vegetable”;
• accompanied by withdrawal syndrome.

Indeed, some of these statements have a real basis. Thus, when treated with tranquilizers, you should not drive or engage in other work that requires concentration. However, other complications arise only in case of overdose or exceeding the recommended duration of therapy. Treatment is also stopped gradually, gradually reducing the dose until the drug is completely discontinued.

Powerful tranquilizers: a list of the most effective and popular drugs, contraindications for use

Only a doctor should select the right anxiolytic. In this case, the patient’s age, severity of the condition, and the presence of concomitant diseases are taken into account.

The financial aspect also plays an important role. First generation drugs are quite effective, but their use is often accompanied by unwanted reactions and complications. However, the price of such anxiolytics is quite affordable. The latest generation tranquilizers are much more expensive, but practically do not cause adverse reactions.

Popular tranquilizers

Adaptol. The drug is quite weak, so it can be purchased without a doctor’s prescription. It affects the main neurotransmitter systems, but taking the drug does not affect muscle tone or learning ability. The drug is prescribed for relatively mild neurotic disorders and nicotine withdrawal.

At the same time, the person retains the ability to study and work fully. The drug is approved only for adults (over 18 years of age). Prescribed in a daily dosage of 3 to 10 g (divided into 3 - 4 doses). While taking Adaptol, a decrease in temperature and blood pressure is possible, but the use of the medicine is not stopped (the patient's condition subsequently normalizes).

Alprazolam (Zolomax). A powerful benzodiazepine tranquilizer that has an effect characteristic of this group of drugs. The dosage is selected individually, starting with the minimum (0.25 - 0.5 mg up to three times a day). If necessary, the daily dose is increased to 4.5 mg. Cancel gradually, 0.5 mg per day.

Grandaxin (Tofisopam). It has a pronounced anxiolytic effect, but the sedative, anticonvulsant and hypnotic effect is weakly expressed. Adults are prescribed 0.05 - 0.1 g per day (but the maximum daily dose should not exceed 0.3 g). For elderly people and those with kidney pathology, this amount is halved.

Phenazepam (Fezanef, Elzepam). It has an anxiolytic, sedative, hypnotic and muscle relaxant effect. It can be used parenterally (intravenously or intramuscularly), but the daily dose should not exceed 9 mg. When taken in tablets, the dosage depends on the indications and condition of the sick person and ranges from 0.5 to 5 mg per day. The drug is often addictive, so the average duration of therapy is 2 weeks, in severe cases - up to 2 months.

General contraindications to taking tranquilizers are:

• pregnancy (drugs are most dangerous in the first trimester);
• children and adolescents up to 18 years of age (used according to strict indications);
• individual intolerance;
• acute alcohol and drug intoxication;
• breastfeeding period;
• severe depression, since monotherapy with tranquilizers can lead to suicidal tendencies;
• coma and shock;
• muscle weakness;
• glaucoma and other pathologies accompanied by increased intraocular pressure.

Tranquilizers and other psychotropic drugs are not prescribed to all patients. In the initial stages of neurosis, herbal sedatives, psychotherapy, and nootropic medications are indicated. Also, anxiolytics are not prescribed for sleep disorders (unless such disorders are caused by neurosis or anxiety disorders).

Powerful tranquilizers often cause adverse reactions. Emotional and physical dependence often occurs, and withdrawal syndrome is typical. Potent anxiolytics cause lethargy, impaired coordination and memory. In addition, erectile dysfunction and changes in the menstrual cycle are possible.

Tranquilizers are used in the treatment of a wide range of mental disorders.

• Neurosis-like and reactive states with severe anxiety, fears or obsessions;

  Panic attacks;

  Depression of various etiologies;

  Reactive psychoses;

  Schizophrenia and schizoaffective psychoses;

  Epilepsy;

  Alcohol withdrawal;

  Sleep disorders, etc.

Side effects of tranquilizers: drowsiness, dizziness, unsteadiness of gait; muscle weakness; with long-term use, decreased libido; sometimes - menstrual irregularities, skin itching, somatovegetative disorders (hypotension, nausea, constipation); worsening of subdepressive disorders.

17. Classification of sleeping pills, effects, indications, undesirable effects.

Classification

GABA A (benzodiazepine) receptor agonists:

• Benzodiazepines: Nitrazepam, Lorazepam, Nozepam, Temazepam, Diazepam, Phenazepam, Flurosepam;

  Drugs of different chemical structures: Zolpidem, Zopiclone, Zaleplon.

Narcotic-type sleeping pills:

• Heterocyclic compounds, barbiturates: Phenobarbital, Sodium etaminal;

  Aliphatic compounds: chloral hydrate;

Selected drugs from other groups:

• H1 histamine receptor blockers: Diphenhydramine, Doxylamine;

  Anesthesia: sodium hydroxybutyrate;

  Preparations of the pineal gland hormone melatonin.

Sleeping pills are divided into three classes. First class (generation) hypnotics are represented by barbiturates, antihistamines and drugs containing bromine (brominated, for example). Barbiturates interact with barbiturate receptors located on chemo-gated chloride ion channels, and the neurotransmitter for these channels is GABA. Barbiturates interact with these receptors, which leads to an increase in the sensitivity of chemo-dependent channels to GABA and leads to an increase in the period of opening of ion channels for chloride ions - the nerve cell polarizes and loses activity. The action of barbiturates, however, is not selective, and they cause not only a sedative-hypnotic effect, but also muscle relaxation, anticonvulsant and anxiolytic effects throughout the entire dose range. Barbiturates vary widely in their duration of action. Sleep induced by barbiturates is different from natural sleep. Antihistamines block histamine H1 receptors. Histamine is one of the key neurotransmitters of wakefulness, and blockade of histamine receptors, accordingly, leads to a sedative effect. Antihistamines, as well as barbiturates, disrupt sleep architecture. Second generation hypnotics are represented by numerous benzodiazepine derivatives. If barbiturates cause an increase in the period of opening of chemo-dependent channels, then benzodiazepines increase the frequency of opening.

Indications

Sleep disorders (difficulty falling asleep, early or night awakening), including secondary sleep disorders in mental disorders.

Side effect

Side effects are observed more often with long-term use of sleeping pills. The most commonly noted residual effects or aftereffect symptoms are characterized by increased sleepiness during the day, decreased performance, concentration, and deterioration of mood. These symptoms are sometimes called behavioral toxicity of the drug, making it difficult to perform tasks that require concentration and quick reactions. Behavioral toxicity is more pronounced in hypnotics with a long T1/2. Chloral hydrate has a pronounced irritating effect on the mucous membrane of the gastrointestinal tract, has a very small breadth of therapeutic action, and also often causes allergic skin reactions.

Often, when taking sleeping pills, mainly benzodiazepine derivatives, memory impairment in the form of anterograde amnesia is noted. When prescribing hypnotics to elderly patients, the possibility of changes in sensitivity to drugs, as well as their pharmacokinetic parameters, should be taken into account; therefore, therapy is started with small doses (about half the usual amount) with a very gradual increase with careful monitoring of the patients’ condition.

Sleeping pills should be used with particular caution in patients with impaired respiratory function, chronic respiratory diseases and sleep apnea syndrome. It is believed that most sleeping pills cause depression of the respiratory center (zopiclone has the least effect).

Long-term prescription of sleeping pills can lead to the development of tolerance and drug dependence. Initial signs of addiction manifest themselves as the inability to discontinue the drug due to a rapid relapse of insomnia. In some patients, symptoms of addiction appear after 2-3 weeks of therapy. The risk of developing dependence can be reduced by using intermittent courses with changes in medications, as well as careful monitoring of the patient and constant monitoring of the dose taken.

Compared to the most common hypnotics (nitrazepam, triazolam), zopiclone and zolpidem have a more physiological effect. They do not have muscle relaxant, anticonvulsant and residual hypnotic or sedative effects, do not affect the patient's daily functioning and have a lower likelihood of dependence and tolerance development. The drugs are well tolerated. In some patients, zopiclone may cause a feeling of bitterness or dry mouth, and zolpidem may cause mild impairment of memory and psychomotor coordination.

Effects

Barbiturates have a rapid hypnotic effect even in severe cases of insomnia, but significantly disrupt the physiological structure of sleep, shortening the paradoxical phase. The main mechanism of the hypnotic, anticonvulsant and sedative effects of barbiturates is allosteric interaction with a site of the GABA receptor complex, which leads to an increase in the sensitivity of the GAB K receptor to the mediator and an increase in the duration of the activated state of chloride channels associated with this receptor complex. The result is, for example, inhibition of the stimulating influence of the reticular formation of the brainstem on its cortex.

Benzodiazepine derivatives are most widely used as sleeping pills. Recipe for hedgehogs in the oven. Recipe for cooking hedgehogs in the oven. . Unlike barbiturates, they disrupt the normal structure of sleep to a lesser extent, are much less dangerous in relation to the formation of addiction, and do not cause pronounced side effects.

Zopiclone and zolpidem are representatives of new classes of chemical compounds. Zolpidem selectively interacts with benzodiazepine ω receptors, which facilitates GABAergic transmission. Zopiclone binds directly to the chloride ionophore regulated by GABA. An increase in the flow of chloride ions into the cell causes hyperpolarization of the membrane and, accordingly, a strong inhibition of the neuron Pax Forte can be bought online in Moscow here. . Unlike benzodiazepines, the new drugs bind only to central benzodiazepine receptors and have no affinity for peripheral ones. Zopiclone, unlike benzodiazepines, does not affect the duration of the paradoxical phase of sleep, which is necessary for the restoration of mental functions, memory, learning ability, and somewhat lengthens the slow-wave phase, which is important for physical recovery. Zolpidem to a lesser extent increases the duration of slow-wave sleep, but more often, especially with prolonged use, prolongs REM sleep.

Like barbiturates, meprobamate also inhibits paradoxical sleep, and dependence develops.

Clomethiazole and chloral hydrate have a very rapid hypnotic effect and practically do not disturb the structure of sleep, but clomethiazole is classified as a drug with a pronounced ability to cause drug dependence.

Bromoureids have been rarely used in recent years. They are rapidly absorbed, but have an extremely slow metabolism, which often causes the development of cumulation and bromism (skin inflammatory diseases, conjunctivitis, ataxia, purpura, agranulocytosis, thrombocytopenia, depression or delirium).

Some antihistamines are still often used as sleeping pills: diphenhydramine, hydroxyzine, doxylamine, promethazine. They cause oppression of the paradoxical phase of sleep, a strong aftereffect (headaches, drowsiness in the morning) and have anticholinergic properties. The most important advantage of antihistamines is the absence of dependence formation even with long-term use.

In major psychiatry in psychotic conditions, sedative antipsychotics or sedative antidepressants are used to correct sleep disorders, depending on the leading syndrome.

The name of the drug group tranquilizers is translated from Latin as “to calm.” Indeed, these drugs can calm a person and eliminate symptoms such as anxiety and fear. That is why tranquilizers are prescribed for neurotic spectrum disorders.

Pharmacological groups of tranquilizers

Tranquilizers (synonymous with anxiolytics) have been around for more than sixty years. The first representatives of this group are Meprobamate, Chlordiazepoxide and Diazepam. Now the group of tranquilizers includes about a hundred drugs.

Medicines with different chemical structures have tranquilizing properties. Depending on their origin, the following groups of tranquilizers are distinguished:

1. Benzodiazepine derivatives (Diazepam, Phenazepam, Oxazepam, Chlordiazepoxide);
2. Diphenylmethane derivatives (Hydroxyzine (Atarax), Benactizine);
3. Carbamates (Meprobamate);
4. Various (Trioxazine, Adaptol, Afobazol).

The most commonly used group of tranquilizers are benzodiazepines. They have the most pronounced tranquilizing effect. However, incorrect use of benzodiazepines can lead to addiction and dependence. Modern medications such as Atarax, Afobazol do not have such side effects, but at the same time have a less pronounced tranquilizing effect.

Indications for the use of tranquilizers

How do tranquilizers work? Drugs from different groups have different mechanisms of action. Thus, benzodiazepines activate GABA receptors through special benzodiazepine receptors located in the central nervous system. This leads to increased sensitivity of receptors to GABA, a neurotransmitter that has an inhibitory effect on the nervous system. This pharmacological effect causes the person to calm down and relax.

Tranquilizers reduce the excitability of the subcortical structures of the central nervous system, which are responsible for a person’s emotional reaction, and also slow down the interaction between these structures and the cerebral cortex.

Tranquilizers have several pharmacological effects:

• Tranquilizing (anxiolytic)- manifests itself in the form of elimination of anxiety, fear, restlessness, internal tension.
• Sedative- is expressed in a decrease in psychomotor agitation, a decrease in concentration, and the speed of mental and motor reactions.
• Muscle relaxant- manifested by the elimination of muscle tension.
• Anticonvulsant- is expressed in a decrease in convulsive activity.
• Hypnotic- is expressed in accelerating the onset of sleep, improving its quality.

These effects are expressed to different degrees in different drugs, which should be taken into account when choosing a drug. So, for example, the sedative effect is very pronounced in Diazepam, Phenazepam and weakly expressed in Mezapam. And the anticonvulsant effect is most pronounced in Diazepam and Clonazepam.

Some tranquilizers have a vegetative stabilizing effect, that is, they normalize the activity of the autonomic nervous system. This is manifested by a decrease in blood pressure, heart rate, elimination of excessive sweating, etc.

Note!Tranquilizers have a potentiating effect. Their use enhances the effect of sleeping pills, painkillers, and anesthetics. This is why tranquilizers are often administered to patients before surgery.

Tranquilizers practically do not eliminate psychotic disorders (hallucinations, delusions), and therefore are not used in the treatment of endogenous mental illnesses: bipolar disorder. The exception is metal-alcohol psychosis, which can be successfully treated with tranquilizers.

Thus, the indications for the use of anxiolytics are:

1. (accompanied by anxiety, fear, motor restlessness);
2. Anxiety disorders;
3. panic disorder;
4. Obsessive-compulsive disorder;
5. for alcoholism, metal-alcohol psychosis;
6. Hyperkinesis, tics,;
7. Premedication (preparation for surgery).

It is worth noting that the range of use of anxiolytics has long gone beyond the treatment of mental illnesses. Thus, these drugs are prescribed for psychosomatic diseases: peptic ulcer, as well as for dermatological diseases accompanied by itching.

Features of application

The decision about the need for treatment with tranquilizers is made only by a doctor. The use of this group of drugs requires compliance with special conditions. First of all, it is necessary to take into account the fact that the use of most tranquilizers, especially benzodiazepines, can lead to addiction. To avoid this, the dose of the tranquilizer is increased gradually, reaching the optimal one. The duration of use should not exceed two to three weeks. At the end of the course of treatment, the dose of the medication is reduced gradually. If long-term treatment is necessary, a tranquilizer is prescribed in courses with breaks between them.

Note! Modern anxiolytics of non-benzodiazepine origin are not addictive, so they can be used longer. The duration of treatment is determined by the doctor.

Tranquilizers, as already mentioned, have a sedative effect on a person, which can manifest itself in a deterioration in concentration. Therefore, you should not drive a car while being treated with tranquilizers. The least pronounced sedative effect is found in “daytime” tranquilizers - Gidazepam, Trimetozin, Mebicar, Atarax.

Important! The combined use of anxiolytics and alcohol is contraindicated, as this leads to severe depression of the nervous system.

Side effects, contraindications

Possible side effects during treatment with tranquilizers are mainly associated with depression of the nervous system. This manifests itself in the form of daytime drowsiness, lethargy, a feeling of “being overwhelmed,” dulling of emotional reactions, etc. It is also possible that side effects such as muscle weakness, arterial hypotension, dry mouth, dyspepsia, and potency disorders may occur.

The use of benzodiazepine tranquilizers can lead to the formation of addiction, drug dependence, manifested in the form of withdrawal syndrome. This syndrome manifests itself after abrupt drug withdrawal in the form of insomnia, fear, irritability, tremors, convulsions, and sometimes even depersonalization and hallucinations. The risk of drug dependence increases with long-term tranquilizer therapy.

Contraindications to the use of tranquilizers:

1. Pregnancy, lactation period;
2. myasthenia;
3. Liver failure;
4. Respiratory failure;
5. Alcohol (except for relief of withdrawal symptoms);
6. (for benzodiazepine tranquilizers).

Benzodiazepine tranquilizers are not prescribed to persons under eighteen years of age. Only in cases of extreme necessity can their use in this age group be justified.

Popular tranquilizers

Important! Benzodiazepine tranquilizers are prescription drugs, which are dispensed in a pharmacy as prescribed by a doctor. Anxiolytics of other origins are sold over the counter, therefore they are more popular among patients. But it is worth emphasizing once again , that self-medication with psychotropic drugs is unacceptable.

One of the oldest tranquilizers, belongs to the group of benzodiazepines. Also known under such names as “Sibazon”, “Relanium”, “Seduxen”, “Valium”. Available in the form of tablets and solution for injection. The sedative effect appears a few minutes after intravenous and half an hour after intramuscular administration.

The medicine effectively eliminates anxiety, fear, and normalizes night sleep. Therefore, Diazepam is prescribed for neuroses, panic and obsessive-compulsive disorders, Tourette's syndrome, as well as for the relief of withdrawal symptoms.

In addition, Diazepam has pronounced anticonvulsant and muscle relaxant effects. Therefore, it is often prescribed to eliminate seizures. Diazepam is used for premedication before endoscopy and operations.

Gidazepam

It belongs to the group of benzodiazepines, however, unlike other representatives of this group, it has an activating effect, and the hypnotic and muscle relaxant effects are weakly expressed.

Gidazepam is classified as a “daytime” tranquilizer. Its anxiolytic effect is manifested by a decrease in feelings of anxiety, fear and restlessness. The drug is prescribed for the treatment of neuroses, psychopathy, autonomic lability, logoneurosis (stuttering), and alcohol withdrawal syndrome.

Atarax

The active ingredient is hydroxyzine, a derivative of piperazine. Atarax is a non-benzodiazepine anxiolytic, belongs to the group of H1-histamine blockers. The drug is considered a “mild” tranquilizer; it has a moderate anxiolytic effect. Available in tablet form, the sedative effect develops after fifteen to thirty minutes.

The main indications for its use are anxiety, increased excitability, dermatological diseases accompanied by itching, and alcohol withdrawal syndrome. In addition to sedative and anxiolytic, it also has an antiemetic effect. Unlike benzodiazepines, Atarax is not addictive or dependent..

Afobazole

A non-bezodiazepine anxiolytic, available in tablet form. Active ingredient: fabomotizol. It has moderate anxiolytic and stimulating effects.

Indications for use: neurasthenia, anxiety disorder, withdrawal syndrome, adaptation disorders, psychosomatic diseases. A noticeable effect develops on the fifth to seventh days of treatment, and the maximum effect occurs after four weeks.

The effect of the drug is very mild and less pronounced than the effect of benzodiazepines. However, the advantage of Afobazole is that its use does not lead to addiction and dependence.

Grigorova Valeria, medical observer