What are tranquilizer tablets? Tranquilizers: classification, list of modern, daytime and over-the-counter drugs. Over-the-counter drug as an alternative to tranquilizers

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 medication. 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(from Latin tranquillium - “calmness”) are one of the most important groups of psychotropic drugs. Recently, they are increasingly called anxiolytics (from the Latin anxius - “anxious” and the Greek lysis - “dissolution”).

Tranquilizers- this is a special group of psychotropic drugs that reduce or eliminate fear, anxiety, restlessness, irritability, emotional tension, the severity of emotional intensity of experiences, that is, they have an anti-neurotic effect.

Indications for prescribing tranquilizers: in addition to a wide range of psychopathological conditions of a neurotic level (fear, tension, anxiety), there may be states of alcohol withdrawal, status epilepticus, petit mal seizures and infantile spasms, insomnia and other sleep disorders, muscle spasms and dystonia, dyskinesias caused by antipsychotics. Intravenous administration of large doses of tranquilizers can cause a distinct sedative effect even with psychomotor agitation. Together with antipsychotics and lithium, they help relieve manic agitation. In other areas of medicine, tranquilizers are used as adjuncts in electrical pulse therapy of cardiac arrhythmias, during endoscopies and bronchoscopy, to enhance analgesia during childbirth, and as a means of preoperative sedation (premedication).

Among psychotropic drugs, tranquilizers are the most widely used in both inpatient and outpatient treatment. The scope of their use goes far beyond psychiatry, covering somatic diseases, neurology, surgery, anesthesiology, oncology, dermatology, gerontology, pediatrics, addiction medicine and, of course, obstetrics and gynecology. This demand for tranquilizers is also confirmed by the fact that since the development of the first drugs with tranquilizing properties, today their group includes more than 100 drugs and active work is still ongoing to create new ones and improve existing ones.

The widespread use of tranquilizers in clinical practice is also facilitated by the fact that, in general, unlike other psychotropic drugs (neuroleptics, antidepressants), they are characterized by the absence of severe side effects and good tolerability. But despite this, there is a certain list of the main adverse effects of tranquilizers, such as hypersedation (dose-dependent daytime sleepiness, decreased level of wakefulness, impaired coordination of attention, forgetfulness), muscle relaxation (relaxation of skeletal muscles, manifested by general weakness, weakness in certain muscle groups), “behavioral toxicity” (mild impairment of cognitive functions and psychomotor skills, manifested even in small doses and detected during neuropsychological testing), etc., which are forcing doctors of various specialties to increasingly pay attention to such a subgroup of tranquilizers as “daytime tranquilizers”.

“Practical Medicine” realized the need for drugs from the group of “daytime tranquilizers”, which have a pronounced anxiolytic effect, but do not cause certain sedative effects (muscle relaxation, impaired coordination of movements and operant activity, drowsiness, etc.) in therapeutic doses. This is especially true for patients who continue to lead an active lifestyle during treatment, sometimes associated with driving vehicles* or working with dangerous mechanisms*, or at heights*, as well as in patients with quite severe concomitant somatic pathology (requiring the exclusion of sedatives and muscle relaxants). effect of drugs).

The following “daytime” tranquilizers are distinguished (E.I. Gusev, A.S. Nikiforov, A.B. Gekht, 2003): (1)* “daytime” tranquilizers that do not have a pronounced sedative effect: gidazepam, prazepam, and also (2) “daytime tranquilizers” that have a mild stimulating effect: mebicar, medazepam, trimetozin, tofisopam. Let's take a closer look at each of these drugs (some authors include daytime tranquilizers and tazepas, alprazolams, as well as phenibut, but they will not be discussed in this article).

* “Daytime” tranquilizers, despite the fact that they do not cause a significant decrease in the ability to concentrate, should be used with caution during work by vehicle drivers and people whose profession is associated with increased concentration.

!!! The question of the ability to drive vehicles is decided after assessing the patient’s individual response to the drug.

Gidazepam(Hydazepam)

“Daytime” anxiolytic drug of the benzodiazepine series (1,4-benzodiazepine derivative). Pharmacological action - anxiolytic. It has an activating effect, vegetative stabilizing properties, and a mild muscle relaxant and hypnotic effect. There is evidence of positive effects on the cardiovascular system in patients with neurological conditions and in healthy people in stressful situations.

Indications for use: neurotic and neurosis-like states, accompanied by anxiety, fear, irritability, emotional lability, insomnia; psychopathy; autonomic lability (including diencephalic pathology); migraine, logoneurosis; in narcology: alcohol withdrawal syndrome, alcoholism (complex treatment); maintenance therapy during remission in patients with alcoholism.

Directions for use and doses. Available in tablet form of 20 mg and 50 mg. Orally, 20–50 mg 3 times a day, gradually increasing the dose. The dosage regimen and duration of treatment are selected individually depending on the indications, the patient's condition, and drug tolerability. Average daily dose for neuroses: 60–200 mg, for migraines and logoneuroses: 40–60 mg, for alcohol withdrawal: 150 mg. Highest daily dose for alcohol withdrawal: 500 mg.

Medazepam(Medazepam)

Trade names with the active ingredient medazepam: mezapam (tablets of 10 mg and granules for children in a package of 2 mg), nobritem (capsules of 5 mg), rudotel (tablets of 10 mg), nobrium.

“Daytime” anxiolytic agent (1,4-benzodiazepine derivative). Has a pronounced anxiolytic effect. Sedative, hypnotic, central muscle relaxant and anticonvulsant effects appear to a lesser extent. Eliminates anxiety, fear, psychoneurotic tension, motor restlessness, excessive fussiness. Restores a critical assessment of one's own condition. Stabilizes vegetative functions. Relieves symptoms of acute alcohol withdrawal.

Indications for use: neuroses, psychopathy, neurosis-like and psychopath-like states, accompanied by increased excitability, irritability, emotional lability, decreased mood, tension, anxiety, fear; psychovegetative and psychosomatic disorders, incl. vegetative-vascular dystonia, sleep disorders, functional disorders of the cardiovascular system and gastrointestinal tract, migraine (prevention of attacks), menopausal syndrome.; in pediatric practice: mental lability and excessive excitability in children, “school” neuroses; in narcology: alcohol withdrawal syndrome (uncomplicated), complex therapy of delayed neurotic disorders developing in the structure of remission of alcoholism and drug addiction.

Directions for use and doses. Inside. The dosage regimen is set individually depending on the indications, course of the disease, tolerability, etc. Treatment should begin with the lowest effective dose, the daily dose is divided into 2-3 doses, if necessary, increasing the daily dose is recommended by increasing the evening dose. Average doses for adults: single - 10 - 20 mg, average daily - 20-30 mg, maximum - 60 - 70 mg/day. At the beginning of treatment - 5 mg 2 - 3 times a day, then the dose is gradually increased to 30 - 40 mg per day. In outpatient settings, 5 mg is recommended in the morning and afternoon and 10 mg in the evening. Elderly patients, adolescents, as well as those with impaired renal function - 5–10 mg 1–2 times a day or 10 mg at night. For children, the dose is calculated depending on age and body weight. The duration of treatment should be as short as possible (approximately 2 weeks) and should not exceed 2 months (including the period of gradual reduction of the drug dose). Before repeating the course, the break should be at least 3 weeks. When treating alcoholism, 30 mg/day is prescribed for 1–2 weeks.

Tofisopam(Tofisopam)

“Daytime” anxiolytic drug, an atypical diazepine derivative (2,3-benzodiazepine). Trade name Grandaxin (50 mg tablets).

Indications for use: neuroses and neurosis-like conditions; conditions accompanied by emotional stress, autonomic disorders, moderate fear, apathy, decreased activity, obsessive experiences; reactive depression with moderately severe psychopathological symptoms; post-traumatic stress disorder; mental adjustment disorder; cardialgia (alone or in combination with other drugs), menopausal syndrome (as an independent remedy, as well as in combination with hormonal drugs); premenstrual tension syndrome; myasthenia gravis, myopathies, neurogenic muscle atrophy and other pathological conditions with secondary neurotic symptoms, when anxiolytics with a pronounced muscle relaxant effect are contraindicated; in narcology: alcohol withdrawal syndrome, delirious states (to relieve agitation and vegetative symptoms), opium withdrawal syndrome and post-withdrawal state; neurotic, psychopathic disorders in alcoholism, as well as conditions characterized by apathy and decreased activity in alcoholism.

Directions for use and doses. Inside. The dosage regimen is set individually depending on the indications, the patient’s condition, and drug tolerability. Single dose - 50 - 100 mg, average daily dose - 150 - 300 mg in 1 - 3 doses, maximum - 300 mg / day for 4 - 12 weeks, including the time of gradual withdrawal of the drug. In elderly people and patients with renal failure, the dose is reduced by 2 times.

Trimetozin(Trimetozinum)

The active ingredient is 4-(3,4,5-Trimethoxybenzoyl)-morpholine (also included in drugs such as sedoxazine, trioxazine).

It has a moderate tranquilizing effect, combined with activation and a slight increase in mood without drowsiness and intellectual inhibition. It does not suppress mono- and polysynaptic reflexes, and therefore does not have a muscle relaxant effect.

Indications for use. Used for neurotic disorders that occur with a predominance of hyposthenic manifestations (adynamia, lethargy, lethargy). Trimetozin is generally well tolerated and can be used in inpatient and outpatient settings. When taking relatively large doses, weakness, lethargy, mild nausea, drowsiness, and in some cases allergic reactions, dyspepsia, dry mouth and throat may occur. Rarely there is an increase in anxiety, tension, and fear. With long-term use of trimethosine (as well as other tranquilizers), mental addiction may develop.

Directions for use and doses. The drug is prescribed orally (after meals), usually 300 mg (1 tablet) 2 times a day. For mild neurotic conditions, the daily dose can be 600 - 900 mg (1 tablet 2 - 3 times a day), and for severe symptoms, increase the dose after 3 - 4 days to 1.2 - 1.8 g per day (total 4 - 6 tablets; in some cases the dose can be increased to 10 tablets per day). Children are prescribed in smaller doses according to age - 1/2 tablet up to 3 - 5 times a day).

Prazepam(Prazepam)

Trade name: Demethrin. “Daytime tranquilizer” has anti-neurotic, anti-anxiety, antiphobic, vegetative-stabilizing effects. However, in therapeutic doses it does not cause sedation or muscle relaxant effects and usually does not have a significant effect on the speed of reactions.

Prazepam has a wide range of indications, providing a good effect in various neurotic, psychophysiological, psychosomatic disorders, and with withdrawal syndrome in patients with chronic alcoholism. Available in tablet form of 10 mg. Directions for use: adults, orally: 10 mg 3 times a day or 20 - 40 mg 1 time a day at night.

Mebicar(Mebicar)

Active ingredient: tetra(also included in drugs such as adaptol; mebix).

Anxiolytic agent (anxiolytic, tranquilizer) with properties of nootropics, antidepressants, biocorrectors, adaptogens, lipid-lowering and antianginal agents. Experience with the use of Mebicar in the treatment of mental disorders has shown that the drug has the properties of a daytime tranquilizer and has nootropic activity. The tranquilizing effect is not accompanied by muscle relaxation and impaired coordination of movements. Mebicar is better tolerated than benzodiazepine tranquilizers: it does not cause emotional dullness, decreased initiative and activity, deterioration of attention and memory, lethargy, muscle relaxation, drowsiness, etc. In addition to moderate tranquilizing activity, Mebikar also has anticonvulsant activity. Mebicar mainly acts on the serotonergic system of the body. In small and medium doses, Mebicar enhances the effect of the serotonin precursor tryptophan. Mebikar is applicable not only as a tranquilizer, but also as an antidepressant.

Indications for use: neuroses and neurosis-like conditions, incl. in patients with alcoholism during remission; mild hypomanic and anxiety-delusional states without gross behavioral disturbances and psychomotor agitation; residual states after acute psychosis with symptoms of affective instability and residual productive symptoms; chronic verbal hallucinosis of organic origin; stress disorders in people working under extreme professional stress (prevention and treatment); cardialgia (not associated with ischemic heart disease); IHD and rehabilitation after myocardial infarction (complex therapy); nicotine withdrawal (as part of complex therapy; to reduce the desire to smoke); reducing craving for psychoactive drugs; to improve the tolerability of neuroleptics and tranquilizers.

Directions for use and doses. Mebicar is available in tablet form, 300 mg. Mebicar is usually prescribed orally at 300–600 mg 2–3 times a day, regardless of meals. If the disorder lasts a long time, treatment is continued for several weeks, prescribing Mebicar according to an individual regimen from 1.8 to 10 g per day. As a means of reducing the desire to smoke tobacco (in complex therapy) - 300 - 900 mg per day for 5 - 6 weeks. The maximum single dose of Mebicar is 3 g, the maximum daily dose is up to 10 g. The duration of treatment is from several days to 2-3 months; for mental illness - up to 6 months. Mebicar can be used in combination with antipsychotics and other tranquilizers.

Medicines should be taken only as prescribed by a doctor
(self-medication can be harmful to your health)

Stress, mental overload, and a busy schedule leave an imprint on a person’s health. There are situations in which it is impossible to calm down and return to the normal rhythm of life without outside help. For these purposes, there is a group of drugs that reduce anxiety and have a sedative and hypnotic effect. You can buy mild tranquilizers without a prescription, but it is better to consult a specialist.

Tranquilizers: what are these drugs and how do they affect the body?

Feelings of anxiety, restlessness, and irritability distract you from everyday activities, unsettle you, and interfere with your normal lifestyle. Often these feelings do not have any real basis, and this causes even more harm.

A person, even understanding in the depths of his soul that he needs to calm down, pull himself together and soberly assess the current situation, physically cannot do this. In cases where fear, panic, anxiety are the result of stress or depression, qualified help is needed.

The pharmaceutical industry quickly responds to changes in lifestyle, providing modern people with the tools to help them get back on track and lead a normal life.

Tranquilizers are a group of drugs that have a psychotropic effect on the human body and relieve anxiety, panic, fear, and depression.

Since tranquilizers are far from harmless drugs, these drugs are addictive and seriously dependent; they are prescribed by a specialist, selecting the dosage, type of drug and course duration based on each specific situation.

Most often, treatment is carried out in short courses; self-medication, even when purchasing tranquilizers without a prescription, is strictly not recommended.

What types of tranquilizers are there?

The list of drugs is quite extensive and includes drugs of varying intensity. The classification is based on the active substance and the effect it has on the body.

First generation drugs

This group includes derivatives of various chemical groups. These include:

• hydroxyzine,
• benactizine,
• meprobamate.

They are prescribed for asthenic and neurotic reactions, anxiety syndrome, mild phobias and depression, neurodermatitis, and sleep disorders. Hydroxyzine is well tolerated with long-term use and is not addictive.

First generation drugs can be combined with each other and antipsychotics.

Second generation tranquilizers

This group includes strong drugs, which include:

• Benzodiazepine drugs- phenazepam, seduxen, lorafen, nozepan. Medicines and “heavy artillery” discharges are dispensed by prescription with a doctor’s prescription.
• Derivatives of different chemical groups– afobazole, proroxan. Unlike benzodiazepine drugs, afobazole and proroxan are not addictive and have no side effects– lethargy, absent-mindedness, decreased reaction, emotional dullness. They reduce anxiety, improve sleep, relieve nervous tension, and reduce the manifestation of autonomic disorders.

Daytime tranquilizers

These are light pills, the use of which does not have a significant effect on memory, attention, or reaction. This group includes:

• Benzodiazepine drugs – Grandaxin, Rudotel, Adaptol. These medications do not have a sedative effect; on the contrary, they stimulate the nervous system and do not cause dependence or withdrawal symptoms.
• Derivatives of different chemical groups - spitomin, phenibut. The use of drugs is advisable for depressive and panic disorders, anxiety syndrome, and disorders of the autonomic nervous system. Not used as a sedative, muscle relaxant or hypnotic. They do not affect reaction, memory, attention, and do not depend on the effects of alcohol. Phenibut speeds up reaction speed and attention. Since withdrawal syndrome is not observed, medications are taken in long courses, they have a cumulative effect and the maximum therapeutic effect is achieved 4 weeks after the start of treatment.

New generation anxiolytics

• Diphenylmethane derivatives – atarax, amizil. The drugs reduce muscle tension, normalize sleep, and do not cause addiction.
• Derivatives of different chemical groups - buspirone, etifoxine, hydroxymethylethylpyridine succinate. This group of drugs is considered the best in the treatment of anxiety. They have versatile activity, in some cases they are allowed during pregnancy and in pediatrics.

Medicines that can be bought without a prescription

Some drugs that reduce anxiety and fear and stimulate the nervous system can be bought at the pharmacy without a prescription. These include

• rudotel,
• zoloft,
• atarax,
• tofisopam,
• phenazepam,
• etifoxine,
• paxil

But the decision about whether they can be taken in each specific situation should be made by a specialist.

New generation drugs

Drugs –

• buspirone,
• adaptol,
• atarax,
• afobazole,
• etifoxine,
• cuts,
• amizil,
• Mexidol,
• oxylidine,
• phenibut

are not addictive and do not have withdrawal symptoms. They are easily tolerated by the body and can be combined with medications from other groups.

Daytime medications

Grandaxin, gidazepam, medazepam, trimetozin, trioxazine, prazepam have a pronounced anti-anxiety effect, but do not have muscle relaxant, sedative and hypnotic effects.

Taking these medications is advisable for mild anxiety and does not affect reaction speed or attention.

Classification by impact

List of drugs that have an effect:

1. pronounced anti-anxiety effect - diazepam, alprazolam, phenazepam and lorazepam (the two extreme ones are the strongest).
2. moderate effect - bromazepam, oxazepam, gidazepam, clobazam.
3. action – triazolam, flunitrazepam, midazolam, nitrazepam.
4. and muscle relaxant effect - diazepam, clonazepam.

How do tranquilizers work?

Depending on the effect that tranquilizers have, they are divided into:

• Anti-anxiety
• Sedatives
• Sleeping pills
• Relaxing
• Anticonvulsants

The drugs affect the nervous system, including nerve endings and subcortical centers of the brain. In one case, the reaction is “inhibited”, the body calms down, becoming stupefied. In another case, the nervous system is stimulated, removing it from a state of anxiety and fear.

Indications for use

Symptoms indicating the need to take tranquilizers:

• Fear
• Panic attacks
• Increased anxiety
• Mood swings, irritability, nervousness

When choosing a drug, the question often arises: what is the difference between tranquilizers and antidepressants? If we talk about first-generation drugs and strong tranquilizers, their long-term use causes dependence and addiction, followed by withdrawal symptoms.

Antidepressants, like daytime tranquilizers and new generation drugs, do not cause addiction or dependence.

What is better, tranquilizers, antidepressants or antipsychotics, is decided by the doctor in each case.

Side effects and overdose

Side effects and exceeding the dose negatively affect the state of the nervous system: blood pressure decreases, bowel movements are disrupted, urinary incontinence may occur, libido decreases, and erections disappear.

In combination with alcohol, tranquilizers can provoke hallucinations and mental disorders. In addition, vision deteriorates, concentration and memory decrease, drowsiness, fatigue, muscle weakness appear, dizziness, hands tremble, and coordination is impaired.

Choosing the right drug for increased anxiety is not an easy task. Intrusive advertising, which guarantees quick results and absence of addiction, is silent about possible complications and side effects.

Tranquilizers are a class of drugs that originally included drugs intended primarily to treat symptoms of anxiety and sleep disorders. The absence of both an antipsychotic effect and the ability to cause extrapyramidal disorders in the range of psychopharmacological activity served as the basis for their isolation from other psychotropic drugs. According to their chemical structure, tranquilizers are predominantly represented by derivatives of benzodiazepine, glycerol, and trihydroxybenzoic acid; azapirone derivatives and a number of other chemical compounds.

Mechanism of action of benzodiazepine derivatives

The mechanism of action of benzodiazepine derivatives became known in 1977, when benzodiazepine receptors, which are directly related to GABA, one of the main inhibitors of neurotransmitter systems, were discovered and localized in the central nervous system. When GABA combines with its receptors, the channels of chloride ions open and they enter the neuron, which forms its resistance to excitation. GABA is active predominantly in the following parts of the brain: stellate interneurons in the cerebral cortex, striatal afferent pathways globus pallidus and substantia nigra, Purkinje cells of the cerebellum. Benzodiazepine tranquilizers have a GABAergic effect, i.e. stimulate the production of this neurotransmitter and facilitate GABAergic transmission at the pre- and postsynaptic levels.

Clinical effects of benzodiazepine derivatives

The clinical effects of benzodiazepine derivatives include 6 main ones: tranquilizing or anxiolytic, sedative, central muscle relaxant, anticonvulsant or anticonvulsant, hypnotic or hypnotic, vegetostabilizing and 2 optional ones: thymoanaleptic, antiphobic. The degree of severity of various effects in the spectrum of psychotropic activity of various benzodiazepine derivatives is not the same, which forms the individual profile of a particular drug.

The use of benzodiazepine derivatives is advisable for symptoms of maladjustment caused by anxiety. The use of these drugs is not recommended in cases where the severity of anxiety is low and does not go beyond the normal response to a stressful situation. In therapy for situational and acutely developed anxiety, preference is given to low-potency drugs with a long half-life, which reduces the risk of drug dependence and withdrawal symptoms, in particular diazepam (no more than 30 mg/day). The duration of the course is determined by the time of exposure to the stress factor that contributed to the development of anxiety. When treating anxiety as part of somatic diseases, these same drugs are used.

The most pronounced effect of benzodiazepine derivatives in the treatment of panic attacks is observed provided that they are not accompanied by persistent reactions of avoidance of the situation on the part of patients. The rapid onset of the anxiolytic effect allows you to completely stop a panic attack or prevent it if you take the drug immediately before a situationally significant event. Given the high frequency of relapses, most patients are prescribed combination therapy or the use of several drugs with sequential changes during the course. Despite the relatively greater safety of long-acting drugs, their therapeutic dose can be so high that it will cause excessive sedation. If there are symptoms of depression in the structure of panic disorder, antidepressants are used in combination therapy, with preference given to selective serotonin and norepinephrine reuptake inhibitors.

In the treatment of generalized anxiety disorder, which, according to various data, has a higher degree of comorbidity with major depressive disorder than with other anxiety disorders, the target symptoms are clinical anxiety phenomena specific to this nosology, such as muscle tension, hyperactivity of the autonomic nervous system and increased level of wakefulness. In most cases with this pathology, benzodiazepine derivatives are used in conjunction with SSRIs and dual-acting antidepressants (selective serotonin and norepinephrine reuptake inhibitors). Moreover, both with monotherapy with benzodiazepine derivatives and with combined use, the effectiveness and safety are higher for prolonged drugs with a long half-life. On the contrary, when using powerful drugs with a short T1/2 (for example, alprazolam), the risk of drug dependence and relapse of anxiety between doses is increased. It is advisable to use 15-30 mg/day of diazepam or another drug in an equivalent dose. As a rule, long-term therapy (6 months or more) is effective and safe in most patients, although the dose of the drug must be reduced, monitoring the possible appearance of anxiety symptoms.

Benzodiazepine derivatives in the treatment of simple phobias are not considered drugs of choice in all cases, except for anticipatory anxiety, when it is possible to use diazepam (10-30 mg/day) as a counteract to phobic stimuli. The basis of treatment for this pathology should probably be behaviorally oriented psychotherapy.

In the treatment of obsessive-compulsive disorders, benzodiazepine derivatives are less effective than SSRIs and selective serotonin and norepinephrine reuptake inhibitors in combination with psychotherapy.

Somatoform disorders that occur in the form of isolated dysfunction of certain organs are subject to treatment with benzodiazepine derivatives only when taking into account the direct effect of these drugs on various vegetative and algic components of the pathological condition. Moreover, the effectiveness of benzodiazepine derivatives is significantly higher for leading vegetative symptoms than for isolated algic symptoms.

Despite the widespread clinical use of benzodiazepine derivatives for depressive conditions, their own antidepressant activity is low even in cases where anxiety is clearly represented in the clinical picture (anxiety-depressive disorders). In such patients, benzodiazepine derivatives should be used only as concomitant therapy to enhance the activity of antidepressants. In other words, treatment for anxiety depression begins with the use of antidepressants and, for the period necessary for the development of their therapeutic effect, a course of tranquilizers lasting 1-4 weeks is additionally prescribed. A special place in the treatment of depressive disorders is occupied by dyssomnias resistant to antidepressant therapy. In such cases, longer-term administration of benzodiazepine derivatives (diazepam, phenazepam in average therapeutic doses) is indicated.

In cases of hyperthymia and mild mania, the administration of benzodiazepine derivatives helps to reduce the insomnia disorders, irritability, anger, and feelings of bodily discomfort associated with manic affect.

In the treatment of schizophrenia, tranquilizers are used in a complex psychotropic effect as adjuvant agents intended to relieve psychotic anxiety and to reduce the manifestations of neuroleptic akathisia.

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Pharmacokinetics of benzodiazepine derivatives

Most benzodiazepines are completely absorbed when taken orally, with peak plasma concentrations of these compounds occurring within a few hours. The metabolic transformation of benzodiazepine derivatives occurs in the liver under the influence of cytochromes P450 (CYP) ZA4, ZA7 and CYP 2C19. Most of the drugs in this group (alprazolam, diazepam, medazepam, chlordiazepoxide) form active metabolites, which significantly increases their half-life. Compounds that do not form active metabolites (oxazepam, lorazepam) immediately bind to glucuronic acid and are quickly eliminated from the body, which explains their significantly better tolerability and lower risk of drug interactions. Based on the duration of their half-life, benzodiazepine derivatives are divided into long-acting drugs (T1/2 more than 20 hours): chlordiazepoxide, diazepam and medazepam; fast acting (T1/2 less than 5 hours); average duration of action (T1/2 from 5 to 20 hours); lorazepam, bromazepam, oxazepam, etc.

Characteristics of benzodiazepine derivative tranquilizers

Side effects of tranquilizers

At the early stage of therapy, the most significant effect is considered to be a sedative effect, which disappears on its own within a few weeks as the anxiolytic effect develops. Also, when using standard doses of drugs, due to individual sensitivity, confusion, ataxia, agitation, exaltation, transient hypotension, dizziness and gastrointestinal disorders may occur.

Mental disinhibition is the most serious side effect of benzodiazepine derivatives, characterized by hostility, dysphoria, and loss of control over one's own actions. The leading role of alcohol in their development has been proven when used together with benzodiazepine derivatives. The incidence of these disorders is less than 1%.

Cognitive dysfunction is observed in patients taking minimal therapeutic doses of benzodiazepine derivatives for a long time. The quality of visual-spatial activities decreases and attention deteriorates. As a rule, patients themselves do not feel this.

Classification of tranquilizers

The main groups of tranquilizers, divided depending on their mechanism of action, are shown in the table.

Classification of tranquilizers by mechanism of action (Voronina Seredenin S.V., 2002)

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Non-benzodiazepine anxiolytics

Despite the fact that benzodiazepine derivatives occupy the leading position in terms of the degree of study and breadth of application, other anxiolytics are also used in medical practice.

Afobazole (INN:azole) is a domestic pharmacological drug from the group of anxiolytics, the world's first selective anti-anxiety drug of the non-bendiazepine series. Afobazole is free from the side effects of benzodiazepine derivatives: hypnosedative effects, muscle relaxant effects, memory disorders, etc.

Afobazole has an anxiolytic effect with an activating component, not accompanied by hypnosedative effects (the sedative effect of afobazole is detected in doses 40-50 times higher than the ED50 for anxiolytic action). The drug does not have muscle relaxant properties or a negative effect on memory and attention; Drug dependence does not form and withdrawal syndrome does not develop. Reducing or eliminating anxiety (preoccupation, apprehension, apprehension, irritability), tension (fearfulness, tearfulness, restlessness, inability to relax, insomnia, fear), and therefore somatic (muscular, sensory, cardiovascular, respiratory, gastrointestinal) symptoms), autonomic (dry mouth, sweating, dizziness) and cognitive (difficulty concentrating, weakened memory) disorders are observed after 5-7 days of treatment with afobazole. The maximum effect occurs by the end of 4 weeks of treatment and persists in the post-therapeutic period for an average of 1-2 weeks.

The drug is indicated for use in the treatment of neurotic disorders. It is especially advisable to prescribe afobazole to persons with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, and a tendency to emotional stress reactions.

Afobazole is non-toxic (LD50 in rats is 1.1 g with ED50 - 0.001 g). The half-life of afobazole when taken orally is 0.82 hours, the average maximum concentration (Cmax) is 0.130±0.073 mcg/ml, the average drug retention time in the body (MRT) is 1.60±0.86 hours. Afobazole is intensively distributed throughout well-vascularized organs. Use internally after meals. The optimal single doses of the drug are 10 mg, daily doses are 30 mg, divided into 3 doses during the day. The duration of the course of use of the drug is 2-4 weeks. If necessary, the dose of the drug can be increased to 60 mg/day.

Benzoclidine inhibits the activity of cortical neurons and the reticular formation of the brain stem, reduces the excitability of the vasomotor center, and improves cerebral circulation. This drug is used to treat anxiety disorders, including anxiety-depressive conditions (especially mild ones and associated with cerebrovascular insufficiency). In addition, benzoclidine is prescribed to elderly patients with atherosclerosis with cerebral disorders, arterial hypertension, and paroxysmal tachycardia.

Hydroxyzine is a blocker of central M-cholinergic receptors and H1 receptors. Pronounced sedative and moderate anxiolytic effects are associated with inhibition of the activity of some subcortical structures of the central nervous system. Hydroxyzine is characterized by a fairly rapid development of anxiolytic action (during the first week of treatment) and the absence of an amnestic effect. Unlike benzodiazepines, with long-term use, hydroxyzine does not cause addiction or dependence, and no withdrawal or rebound syndromes have been observed.

Benactizine is a diphenylmethane derivative, the anxiolytic effect of the drug is due to the reversible blockade of central M-cholinergic receptors. Due to its pronounced effect on central cholinergic structures, benactizine is classified as a central anticholinergic. The effect on the central nervous system is clinically manifested by a calming effect, inhibition of the convulsive and toxic effect of anticholinesterase and cholinomimetic substances, increased action of barbiturates and other hypnotics, analgesics, etc. Currently, due to the presence of effective tranquilizers, as well as due to unwanted side effects associated with atropine-like effects (dry mouth, tachycardia, mydriasis, etc.), benactizine is practically not used as an anxiolytic.

Representatives of the third generation anxiolytics are buspirone, oxymethylethylpyridine succinate (Mexidol), etc. The anxiolytic effect of Mexidol is associated with its modulating effect on membranes, including the GABA receptor complex, and is manifested by an improvement in synaptic transmission.

Buspirone is a partial serotonin receptor agonist and has high affinity for serotonin 5-HT1a receptors. The mechanism of action is not fully understood. Buspirone is known to reduce the synthesis and release of serotonin and the activity of serotonergic neurons, including in the dorsal raphe nucleus. In addition, it selectively blocks (antagonizes) pre- and postsynaptic D2 dopamine receptors (moderate affinity) and increases the firing rate of midbrain dopamine neurons. Some evidence suggests that buspirone has effects on other neurotransmitter systems. Effective in the treatment of mixed anxiety-depressive conditions, panic disorders, etc. The anxiolytic effect develops gradually, manifests itself after 7-14 days and reaches a maximum after 4 weeks. Unlike benzodiazepines, buspirone does not have a sedative effect, a negative effect on psychomotor functions, does not cause tolerance, drug dependence and withdrawal symptoms, and does not potentiate the effect of alcohol.

In addition to drugs belonging to the group of anxiolytics, drugs from other pharmacological groups have an anti-anxiety effect to varying degrees: some TNF-adrenergic blockers (propranolol, oxprenolol, acebutolol, timolol, etc.), α-adrenergic agonists (clonidine). Thus, propranolol is effective in the treatment of anxiety states associated with hyperreactivity of the sympathetic nervous system and accompanied by severe somatic and autonomic symptoms; clonidine has the ability to reduce somatovegetative manifestations in the withdrawal syndrome of opium addiction.

Currently, an intensive search continues for new drugs that have an anxiolytic effect and, at the same time, are safer and more effective than existing drugs. Screening of benzodiazepine derivatives is aimed at identifying the most selectively acting drugs with the most pronounced anxiolytic effect with a minimum of side effects. The search is also carried out among substances that affect serotonergic transmission, antagonists of excitatory amino acids (glutamate, aspartate), etc.

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When prescribing benzodiazepine derivatives, special attention is paid to the personality and behavioral profile of the patient, which helps to avoid cases of abuse of these drugs.

Characteristics of people taking benzodiazeline tranquilizers for treatment and using these drugs for non-medical purposes

Withdrawal syndrome

All benzodiazepine derivatives can cause withdrawal symptoms to one degree or another. This pathological condition, as a rule, occurs in the form of various disorders of the digestive tract, hyperhidrosis, tremor, convulsions, tachycardia, drowsiness, dizziness, cephalgia, hyperacusis, irritability.

In some cases, when therapy is abruptly discontinued, severe symptoms such as severe and prolonged depression, acutely developing psychotic states, hallucinations, and opisthotonus are noted. choreoathetosis, myoclonus. delirious states with catatonic episodes, etc.

Withdrawal syndrome rarely develops if the course of therapy with benzodiazepine derivatives does not exceed 3-4 weeks. Withdrawal phenomena also include the so-called interdose symptoms, or breakthrough symptoms - the resumption of symptoms between doses of benzodiazepine derivatives (adapted from data from the American Psychiatric Association, 1990). When discontinuing treatment with benzodiazepine derivatives, it is important to follow the following basic recommendations.

• Develop a clear scheme for the therapeutic use of the drug in order to avoid its abuse.
• It is correct to take into account the ratio of benefits and possible negative aspects of treatment.
• Gradually reduce the dose and carefully monitor for possible withdrawal symptoms.
• Resolve the issue of alternative treatment (psychotherapy, behavioral therapy or medication).
• It is necessary to maintain a spirit of cooperation in the relationship with the patient to strengthen compliance.

The general recommendation for reducing the daily dose of benzodiazepine derivatives to avoid the occurrence of withdrawal syndrome is the possibility of a fairly rapid reduction by 50% of what the patient takes; however, subsequent reductions should be made more slowly (by 10-20% of the new dosage every 4-5 days).

Introduction

The problem of side effects of drugs has been relevant throughout the history of the development of psychopharmacology. In recent years, the methodology of the systems approach, which has already penetrated into psychiatry under the guise of the well-known axial diagnosis (ICD-10, DSM-IV), the so-called biopsychosocial model of the disease (G. Engel, 1980) and the concept of the barrier to mental adaptation (Yu.A. Aleksandrovsky , 1993), quite quickly finds its justification in the field of psychopharmacotherapy, which, according to many researchers, is based on the priority of the safety of the use of psychotropic drugs. Taking into account the risk of side effects and complications is one of the main criteria for prescribing effective psychopharmacological treatment (S.N. Mosolov, 1996; F.J. Yanichak et al., 1999). A.S. Avedisova (1999) points out the need when using psychotropic drugs to distinguish and compulsorily compare their clinical effectiveness (the so-called benefit of treatment) and unwanted, side effects or tolerability (the so-called risk of treatment).

This approach, associated with a shift in emphasis from the clinical effectiveness of treatment to its safety and which is essentially the general line of development of modern psychopharmacology, primarily corresponds to the principles and objectives of the treatment of borderline mental disorders. Taking this into account, such “non-clinical” concepts as “quality of life” (D.R. Lawrence, P.N. Benitt, 1991) of mentally ill patients during the period of drug exposure, the index of so-called behavioral toxicity (1986), showing the degree of impairment of psychomotor and cognitive functioning under the influence of psychotropic drugs, as well as a number of other concepts. All of the above must be taken into account when introducing into practice the formulary system (2000) for the use of medicines, including psychotropic ones.

General characteristics of tranquilizers

The main groups of tranquilizers according to their chemical structure include:

1) glycerol derivatives (meprobamate);

2) benzodiazepine derivatives (Elenium, diazepam, lorazepam, phenazepam, clonazepam, alprazolam and many others);

3) derivatives of trimethoxybenzoic acid (trioxazine);

4) azapirone derivatives (buspirone);

5) derivatives of another chemical structure (amizil, hydroxyzine, oxylidine, mebicar, mexidol and others).

The following clinical and pharmacological effects of tranquilizers are distinguished:

1) tranquilizing or anxiolytic;

2) sedative;

3) muscle relaxant;

4) anticonvulsant or anticonvulsant;

5) hypnotic or hypnotic;

6) vegetative stabilizing.

Additionally, psychostimulating and antiphobic effects are indicated.

Consequently, the main target of the use of tranquilizers is considered to be various anxiety-phobic syndromes of a non-psychotic level, both acute and chronic, developing within the framework of the so-called borderline states (Yu.A. Aleksandrovsky, 1993). Moreover, the side effects that occur during their use are usually associated with an excess of the above pharmacological effects of these drugs, that is, according to the generally accepted classification of types of adverse reactions, they are classified as reactions of the first type (type A).

Side effects of tranquilizers

As is known, tranquilizers, unlike neuroleptics and antidepressants, do not produce significant side effects and are well tolerated by patients. This is largely why, immediately after the introduction of chlordiazepoxide (Elenium) into clinical practice in 1959, the number of newly synthesized tranquilizers grew like an avalanche, and at present they have become the most widespread among all drugs, since they are widely used not only in psychiatry, but also in somatic medicine, as well as healthy people to relieve the negative component of emotional stress. According to some data, from 10 to 15% of the total population in different countries receive prescriptions containing one or another tranquilizer once a year. It should be added that the intensity of the search for new drugs of this class in modern psychopharmacology continues to remain at a very high level, and to date the group of the most popular of them - benzodiazepine tranquilizers - includes more than 50 items.

The main side effects of tranquilizers include:

1. The phenomena of hypersedation are subjectively noted, dose-dependent daytime sleepiness, decreased level of wakefulness, impaired concentration, forgetfulness and others.

2. Myorelaxation - general weakness, weakness in various muscle groups.

3. “Behavioral toxicity” - mild impairment of cognitive functions and psychomotor skills that is objectively noted during neuropsychological testing and manifests itself even at minimal dosages.

4. “Paradoxical” reactions - increased agitation and aggressiveness, sleep disturbances (usually resolve spontaneously or when the dose is reduced).

5. Mental and physical dependence - occurs with long-term use (6-12 months of continuous use) and is manifested by phenomena similar to neurotic anxiety.

The most common side effect observed during the use of tranquilizers (primarily benzodiazepines) is lethargy and drowsiness - in approximately 10% of patients (H. Kaplan et al., 1994). These symptoms may be present throughout the next day after taking the drug the night before (called residual daytime sleepiness). Less than 1% of patients experience dizziness and less than 2% experience ataxia, largely due to the degree of muscle relaxant effect of tranquilizers. It should be noted that our preliminary data indicate a much higher incidence of these adverse events, especially in the elderly. More serious adverse reactions may occur with the combined use of benzodiazepine tranquilizers and alcohol: severe drowsiness, psychomotor retardation, and even respiratory depression.

Other, much less common side effects of tranquilizers are associated with mild cognitive deficits (“behavioral toxicity”), which nevertheless often lead to decreased performance and cause complaints from patients. Short-term periods of anterograde amnesia usually occur when short-acting benzodiazepine hypnotics are used at the peak of their concentration in the blood (S.N. Mosolov, 1996). Our data indicate mild reversible impairments in memory and reproduction, subjectively noted by patients taking diazepam (Valium) and phenazepam in average therapeutic dosages for a long time. At the same time, relatively new drugs in this group - Xanax (alprazolam) and Spitomin (buspirone) - practically did not cause any significant symptoms of “behavioral toxicity”.

“Paradoxical” reactions, such as increased agitation and aggressiveness, have not yet found definitive confirmation of their connection with the use of certain tranquilizers. However, there is evidence that triazolam, for example, often contributes to the manifestation of severe aggressive behavior to such an extent that the company that produces this drug recommended limiting its use to a 10-day course and using it only as a hypnotic. In isolated cases, paradoxical reactions in the form of anxiety and sleep disturbances were noted by us in patients taking pitomina (buspirone).

We should not forget that tranquilizers freely penetrate the placental barrier and can depress the child’s respiratory activity, as well as disrupt the proper development of the fetus (“benzodiazepine children” - L. Laegreid et al., 1987). In this regard, they are not recommended for use during pregnancy and lactation. The UK Medicines Safety Committee lists among the side effects of benzodiazepines taken by pregnant and lactating women: hypothermia, hypotension and respiratory depression in the fetus, as well as physical dependence and withdrawal syndrome in newborns.

The occurrence of withdrawal syndrome, indicating the formation of addiction, directly correlates with the duration of treatment with tranquilizers. Moreover, some studies confirm its likelihood in some patients, even in relation to the course use of small doses of benzodiazepines. The most common signs of tranquilizer withdrawal syndrome include: gastrointestinal disorders, increased sweating, tremors, drowsiness, dizziness, headaches, intolerance to harsh sounds and smells, tinnitus, depersonalization sensations, as well as irritability, anxiety, and insomnia. In a number of patients, manifestations of tranquilizer withdrawal syndrome can be very severe and last up to 0.5-1 year (H. Ashton, 1984, 1987; A. Higgitt et al., 1985). H. Ashton argues that the severity and duration of the disorders are often underestimated by medical personnel who mistakenly take withdrawal symptoms for neurotic phenomena.

During our observations, we also identified cases of the formation of a unique non-toxicomanic (non-pathological or psychological) form of dependence during treatment, when any attempt or proposal to reduce the dose of the drug caused a rapid increase in the level of anxiety and hypochondriacal mood, and the idea of ​​a possible psychotraumatic situation in the future led to additional use of the drug .

Speaking about the role of side effects of tranquilizers in the treatment of borderline mental disorders, one should point out the relatively frequent refusals of patients, especially those engaged in active professional activities, to continue treatment with certain drugs of this group. In addition, it is also necessary to note the occurrence of so-called secondary neurotic and non-pathological or psychological reactions (in the form of short-term anxious and anxious-hypochondriacal states), at least temporarily worsening the general mental state of patients and requiring psychotherapeutic correction.

Conclusion

Summarizing the information presented, you must first point out that:

1. Various side effects quite often occur even during therapy with such “mild” and in this sense safe psychotropic drugs as tranquilizers, especially classic benzodiazepines.

2. In this case, so-called secondary, both pathological (i.e., neurotic) and non-pathological (i.e., psychological), mainly anxious and anxious-hypochondriacal reactions may arise, which, despite their short duration, require psychotherapeutic correction.

3. In some cases, patients may refuse therapy due to the occurrence of certain side effects of tranquilizers.

4. It is possible to develop special non-toxicomaniacal (psychological) forms of drug dependence, which nevertheless may pose a problem in the course of further rehabilitation of patients.

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