Antidepressants and anxiolytics: advantages and disadvantages. Tranquilizers without prescriptions: a list of new generation drugs Tranquilizers classification mechanism of action

Anxiety is considered one of the most common affective states. At the same time, it can also occur in a completely healthy person, moreover, everyone has ever encountered such a sensation to one degree or another.

Anxiety is divided into physiological, which occurs with a completely objective or perceived threat, and pathological, which appears without visible reasons. It is the latter that is referred to as anxiety disorders.

They are often accompanied by noticeable discomfort, asthenic condition, insomnia, dizziness, autonomic symptoms. Just such clinical picture and 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.

For creating a sense of threat when analyzing certain factors environment A number of brain structures “respond”:

amygdala (almond-shaped body);
islet located in the cerebral cortex;
ventral striatum;
hypothalamus;
sections of the cingulate and prefrontal cortex;
hippocampus.

The amygdala provides an instant assessment of incoming information and selectively reacts to a threat, forming a sense of anxiety. The hippocampus and prefrontal cortex regulate the strength of the emotional response, and suppress the response when it is no longer appropriate for the situation.

As a result, the production of a number of hormones and neurotransmitters changes, which further exacerbates the changes taking place in the brain. However, timely appointments medications allow you to stop the progression of pathology and return a person to a normal emotional state.

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

The first psychotropic drugs appeared in the early 1950s. These were quite potent medicines that were used in specialized hospitals. Later, experts developed relatively safe, "light" drugs that are suitable for home use. Moreover, some of these drugs are sold without a doctor's prescription.

Psychotropics can be divided into two large groups: drugs with a sedative and stimulating effect.

The first class includes:

antipsychotics (also called antipsychotics);
strong and light tranquilizers (anxiolytics);
sedative medications.

The second class includes:

nootropics;
actoprotectors;
adaptogens;
psychomotor stimulants;
normotimics (lithium preparations);
analeptics.

The action exerted by the preparations of various groups of psychotropic drugs in a certain sense has something in common. So, many antidepressants (especially the first - second generation) have a pronounced anxiolytic and sedative effect. That is why the intake of tranquilizers and other drugs for the treatment of anxiety disorders, sleep disorders, stressful conditions should be controlled by a doctor.

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

Tranquilizers are often addictive, and with uncontrolled intake, the patient has to constantly increase the dosage of the drug. Therefore, the doctor controls the relationship between the amount of the drug taken during the day and the effect. If necessary, the remedy is canceled and replaced with an analogue, but of 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, this group of drugs has been at the top of the list of the most popular and prescribed drugs in psychotherapy and neurology.

By chemical structure tranquilizers are divided into:

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

According to the duration of action (they are guided by pharmacokinetic indicators, in particular, the half-life), tranquilizers are:

prolonged action - 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).

Rather arbitrary, but convenient for a practitioner, the division of tranquilizers into "day" (or small) and "night". This classification is based on the severity of the sedative effect of the drug.

Among the 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 the 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 action of a particular neurotransmitter) of serotonin receptors (Buspirone);
drugs with a different mechanism of action (for example, Amizil).

Tranquilizers are prescribed when there is no effect from other, less potent drugs. Also, such medications are indicated after the use of non-drug treatments for neurosis and anxiety disorders.

Antipsychotics

These medicines used to treat severe disorders of the central nervous system. Antipsychotics have a complex effect on the body. Similar medicines:

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

Some neuroleptics suppress the gag reflex by acting on certain brain structures.

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

phenothiazine derivatives (Aminazine, Thioridazine, Fluphenazine, Triftazin, etc.);
thioxanthene derivatives (Chlorprothixene, Zuklopentiksol);
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 is not well understood. But it is believed that the combination of a sedative and anxiolytic effect is due to the inhibition of the activity of dopamine receptors and the blocking of serotonin ones. This is also associated with adverse reactions that often occur against the background of the use of antipsychotics.

So the most common complication is drug-induced parkinsonism (rigidity and tremor of the muscles). Long-term use of such drugs is also accompanied by neurolytic syndrome (decrease in memory, intelligence, emotional instability).

Psychostimulants

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

Medicines in this class are divided into:

purine derivatives, most famous representative 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, according to the principle of action, it is similar to Sydnocarb, but less effective.

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

Normitimics

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

To date, the normotimics include:

lithium preparations (lithium carbonate, Micalit, lithium hydroxybutyrate);
derivatives of valproic acid (Depakine, Depacon, Depakot);
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 drugs comes from the Greek words "noos" - mind and "tropos" - aspiration. It's relative safe means that improve memory, cognitive functions, 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. So, there are derivatives of pyrrolidone (Piracetam), γ-aminobutyric acid (Aminalon, Phenibut), antioxidants (Mexidol). In addition, a number of other medicines have a nootropic effect. These include Pentoxifylline, products based on ginkgo biloba, ginseng, lemongrass, echinacea, Actovegin.

How tranquilizers work: effect, differences between "day" and "night" tranquilizers

The effect exerted 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. At the same time, a channel opens in the cell membranes, selectively passing chloride ions (Cl-). Their accumulation reduces the activity of many neurons of the central nervous system.

The sedative properties of tranquilizers are associated with an effect on another type of benzodiazepine receptors, which are mainly located in the reticular formation of the brain stem and 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 (restoring the normal functional activity of the autonomic nervous system).

Due to the mechanism of how tranquilizers work, these drugs can enhance the effect of other drugs:

sleeping pills;
sedatives;
narcotic analgesics.

Therefore, when combining these groups of medicines, it is necessary to strictly control the dosage and the patient's well-being.

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

The primary metabolism is carried out in the liver, but tranquilizers are excreted through the kidneys, and only a small part through the digestive tract. The pharmacodynamic parameters 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 substances of the drugs is not reached immediately. In general, this period takes from 5 days to two weeks, subject to regular use at the recommended dosage.

Currently, the so-called "daytime" tranquilizers deserve special attention. They are characterized by a minimal sedative and hypnotic effect, so their use affects the quality of life of the patient to a lesser extent. 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 alone because of the risk of addiction and other adverse reactions. Doctors prescribe these drugs for:

neuroses;
anxiety disorders;
seizures panic attacks;
depressive state (practically not used for monotherapy, prescribed in combination with other drugs);
severe withdrawal syndrome caused by the rejection of alcohol, nicotine or drug addiction;
disorders associated with vegetovascular dysfunction;
recurrent epileptic seizures;
nervous disorders provoked 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 associated with the real state of affairs.

So, it is widely believed that anxiolytics:

impair memory, concentration and other brain functions;
are addictive;
cause constant drowsiness;
turn into a "vegetable";
accompanied by a withdrawal syndrome.

Indeed, some of these statements have a real basis. So, when treating with tranquilizers, you can not drive and do other work that requires concentration. However, other complications occur 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 taking

The selection of the right anxiolytic should only be done by a doctor. At the same time, the age of the patient, the severity of the condition, 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 adverse reactions and complications. However, the price of such anxiolytics is quite affordable. tranquilizers latest generation are much more expensive, but practically do not cause adverse reactions.

Popular tranquilizers

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

At the same time, a person retains the ability to learn and work fully. The drug is allowed only for adults (over 18 years old). Assign in a daily dosage of 3 to 10 g (divided into 3 to 4 doses). Against the background of taking Adaptol, a decrease in temperature and indicators is possible. blood pressure, however, the use of the drug is not stopped (subsequently, the patient's condition returns to normal).

Alprazolam (Zolomax). A powerful benzodiazepine tranquilizer that has a characteristic effect for 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. Assign adults to 0.05 - 0.1 g per day (but the maximum daily dose should not exceed 0.3 g). For the elderly and 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 the 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 (the funds are most dangerous in the first trimester);
children's and teenage years up to 18 years (applied according to strict indications);
individual intolerance;
acute alcohol and drug intoxication;
period breastfeeding;
severe depression, since monotherapy with tranquilizers can lead to suicidal tendencies;
coma and shock;
muscle weakness;
glaucoma and other pathologies accompanied by an increase in intraocular pressure.

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

Powerful tranquilizers often cause adverse reactions. Often there is an emotional and physical dependence, a withdrawal syndrome is characteristic. Potent anxiolytics cause lethargy, impaired coordination, memory. In addition, erectile dysfunction and changes in the menstrual cycle are possible.

Tranquilizers are medications used to relieve panic, anxiety, stress, and depression. This group of drugs is also called anxiolytics. The name comes from two Greek words, literally meaning - the dissolution of anxiety.

The tranquilizing effect is manifested as follows:

weakening of internal stress;
reduction of feelings of anxiety, anxiety, fears.

These drugs have no effect on cognitive, that is, cognitive functions of the brain, or it is extremely weakly expressed. They also do not affect mental disorders - hallucinations, delusions.

Indications for use for all tranquilizers are different. They are also prescribed to eliminate acute - for a short course of treatment.

65 years ago...

The first tranquilizer was created in 1951. It was called Meprobamate. It was clinically tested only four years later, in 1955. year. And the name of the group - tranquilizers - appeared even later, in 1957.

Tranquilizers of the benzodiazepine series were created in 1959, the first drug was. At the same time, anxiolytic efficacy was found in antihistamine Hydroxyzine.

To date, the group of tranquilizers includes about a dozen substances under international non-proprietary names, the list of drugs according to trade names is much larger - several dozen.

The difference between tranquilizers and antidepressants

Tranquilizers by their action reduce the severity of emotional manifestations - whether positive or negative emotions.

Antidepressants, on the other hand, "uplift the mood", that is, they contribute to the strengthening of positive emotions and the reduction of negative ones.

There is also a difference in the mechanism of action. Anxiolytics stimulate the activity of benzodiazepine and GABAergic receptors, suppressing the limbic system.

Antidepressants, on the other hand, are serotonin reuptake inhibitors, a substance that improves mood. Under the action of antidepressants, the concentration of serotonin in the synaptic cleft increases - as a result, its effectiveness increases.

Classification of group drugs

The entire group of tranquilizers is divided into subgroups - according to the interaction of drugs with different types receptors:

benzodiazepine receptor agonists(benzodiazepine tranquilizers) - Clozepid, Mezapam, Tofisopam;
serotonin receptor agonists — ;
substances with different types of action-, Amizil, Mebikar.

The first subgroup is used most often. It includes drugs that are derivatives of benzodiazepines. For them, too, there is a classification based on the duration of the drug:

long-acting agents- these include Phenazepam and Chlorazepam, their action lasts up to 48 hours;
means with an average duration of action- these are Alprazolam and Nozepam, they remain effective for 24 hours;
to the third group short action- includes the drug Midazolam, the duration of its action is less than six hours.

There is another type of classification - by generations:

the very first tranquilizers, or first generation- Hydroxyzine and Meprobamate;
to second generation include benzodiazepine tranquilizers - Chlorazepam;
in third generation drug is included.

According to the chemical structure, they distinguish:

benzodiazepine derivatives - Phenazepam, Diazepam;
carbamic esters - Meprobamate;
derivatives of diphenylamine -;
derivatives of different groups - .

This is a separate group of drugs in which sedative and hypnotic effects are minimized. There is no suppression of cognitive functions. Thanks to this, drugs can be taken during the working day.

One of the representatives of daytime anxiolytics is Grandaxin. The active substance of this drug is tofisopam.

Produced in the form of tablets. pharmachologic effect similar to the action of benzodiazepine tranquilizers, except for the manifestation of a hypnotic effect. It is indicated for stressful situations, with severe premenstrual and menopausal syndrome.

The dosage is selected individually, on average it is 150 mg per day for three doses. From side effects noted headache and dyspepsia.

Contraindicated in respiratory failure, during pregnancy and breastfeeding.

Benzodiazepines

Benzodiazepine tranquilizers can have the following effects on the body:

anxiolytic- the main thing for this group, eliminating anxiety;
sedative- mild soothing effect;
hypnotic action;
muscle relaxant, that is, contributing to the elimination of muscle tension;
anticonvulsant.

The presence of these effects is due to the influence of drugs on the limbic system of the brain. The strongest effect benzodiazepine tranquilizers have on the hippocampus. A less pronounced effect is on the hypothalamus and the reticular formation of the brain. In the hippocampus, these drugs inhibit the process of the reverse passage of the nerve impulse.

This mechanism of action is associated with the effect of these drugs on benzodiazepine receptors. They, in turn, have a close relationship with GABAergic receptors.

Therefore, when benzodiazepine anxiolytics stimulate "their" receptors, other receptors are also stimulated. Due to this, an anxiolytic and sedative effect occurs.

The ability to relax tense muscles in tranquilizers is due to the inhibition of spinal reflexes - impulses emanating from the spinal cord. The same effect causes and .

By their structure, benzodiazepine tranquilizers are lipophilic substances. Due to this property, they are able to easily penetrate the biological barriers of the body, including the blood-brain barrier.

In the body, these drugs form a bond with plasma proteins. In addition, they are able to accumulate in adipose tissue. They are excreted through the kidneys and in small quantities through the intestines.

For tranquilizers of the benzodiazepine series, there is an antagonist used in case of overdose - Flumazenil. Its action is based on the blocking of benzodiazepine receptors. As a result, tranquilizers cannot form a bond with them and do not have their effect.

Phenazepam - he is the most popular

Available in the form of tablets and solution for injection. Pharmacological action is characterized by a pronounced anxiolytic effect, moderate anticonvulsant, muscle relaxant and hypnotic effects.

The action is based on the stimulation of GABA receptors mediated through the stimulation of benzodiazepine receptors. At the same time, the excitability of subcortical formations in the brain decreases, and the activity of spinal neurons decreases.

The drug is indicated for the following pathological conditions:

feelings such as anxiety, fear, emotional instability;
acute reactive psychoses;
sleep disorders.

Phenazepam tablets are prescribed in a dose of up to 1 mg. In the treatment of sleep disorders, a single dose is 0.25 mg. Acute stress or reactive psychosis require an increased dose - up to 3 mg.

Of the side effects, minor cognitive disorders are noted - impaired memory and attention. Dizziness and headache, dyspeptic disorders, allergic reactions may occur. Long-term use contributes to the development of addiction syndrome.

The drug is contraindicated in the following conditions:

congenital muscle weakness;
severe pathology of the kidneys and liver;
taking other tranquilizers and antipsychotics;
period of pregnancy and breastfeeding.

Nozepam - popular and inexpensive

A drug from the second subgroup of benzodiazepine tranquilizers. Active substance- oxazepam. It has a pronounced anxiolytic and sedative effect. There is a moderate anticonvulsant effect. The mechanism of action is similar to Phenazepam.

Indicated in the following pathological conditions:

especially in menopausal women.

The dosage of the drug is selected individually and can reach 120 mg per day. Side effects include dizziness and headache, impaired attention and gait.

Disorders of mental balance may appear - emotional instability,. Leukopenia and agranulocytosis may be detected in the blood. Dyspeptic disorders and urination disorders. With prolonged use, addiction syndrome may also develop.

Contraindicated if there is:

disturbances of consciousness - shock, coma;
acute alcohol poisoning;
taking other psychotropic drugs with a depressant effect on the central nervous system;
congenital muscle weakness;
angle-closure glaucoma;
chronic obstructive pulmonary disease;
depressive disorders;
the period of pregnancy and breastfeeding;
age less than six years.

Serotonin tranquilizer

A drug from the second subgroup - a serotonin receptor agonist - or. It is able to bind to serotonin and dopamine receptors. The main effect, as with benzodiazepine tranquilizers, is anxiolytic.

It develops more slowly, within two weeks. Sedative, hypnotic and muscle relaxant effects are not characteristic of Buspirone.

In the body, the drug also binds to plasma proteins. Its entire metabolism takes place in the liver, and the substance is excreted in the form of metabolites through the kidneys.

Indicated for the treatment of various anxiety states, . In contraindications to taking the drug, such conditions as pregnancy and breastfeeding, severe pathology of the heart, liver and kidneys.

The initial dose for treatment is 15 mg per day, divided into three doses. If necessary, the dose can be increased to 25 mg.

Unclassified drugs

The third group includes several tranquilizers that cannot be classified.

Amizil

Amizil is a central anticholinergic drug. Its main effect is sedation. It is associated with the suppression of m-cholinergic receptors located in the brain.

It also has an anticonvulsant effect and is able to inhibit the cough center in the medulla oblongata.

Hydroxyzine (Atarax)

Hydroxyzine, or, is a derivative of diphenylmethane. This is one of the oldest tranquilizers that has not lost its effectiveness to this day. The anxiolytic effect is moderate. This drug has other effects:

soothing;
antiemetic;
antihistamine.

The drug is able to penetrate the biological barriers of the body. Metabolism occurs in the liver, the main metabolite is cetirizine is a strong antihistamine.

Atarax is indicated for the following pathological conditions:

severe anxiety;
neurological and mental disorders accompanied by internal tension and emotional instability;
in the treatment of chronic alcoholism.

The drug is contraindicated during pregnancy and breastfeeding, with intolerance to hydroxyzine itself or its metabolites.
The therapeutic dose is from 25 to 100 mg, divided into several doses during the day.

What can be bought without prescriptions?

Almost all tranquilizers are available in pharmacies by prescription, however, daytime anxiolytics can be purchased without prescriptions from doctors, a list of these funds was proposed above.

The drugs of this group are indispensable in the treatment of anxiety disorders, neurosis and sleep disorders. However, all of them, with the exception of daytime, are prescribed for a short course, because they quickly develop addiction and drug dependence.

The name of the drug group tranquilizers with Latin translates to "calm down". Indeed, these drugs are able to calm a person and eliminate symptoms such as anxiety, fear. That is why tranquilizers are prescribed for neurotic spectrum disorders.

Pharmacological groups of tranquilizers

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

Tranquilizing properties have different chemical structure drugs. Depending on the origin, the following groups of tranquilizers are distinguished:

Derivatives of the benzodiazepine series (Diazepam, Phenazepam, Oxazepam, Chlordiazepoxide);
Diphenylmethane derivatives (Hydroxyzine (Atarax), Benactizine);
Carbamates (Meprobamate);
Miscellaneous (Trioxazine, Adaptol, Afobazol).

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

Indications for the use of tranquilizers

How do tranquilizers work? Drugs of different groups have a different mechanism of action. So, benzodiazepines activate GABA receptors through special benzodiazepine receptors located in the central nervous system. This leads to an increase in the susceptibility of receptors to GABA, a neurotransmitter that has an inhibitory effect on the nervous system. Such a pharmacological effect leads to the fact that a person calms down, relaxes.

Tranquilizers reduce the excitability of the subcortical structures of the central nervous system responsible for the emotional reaction of a person, 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, anxiety, internal tension.
Sedative- is expressed in a decrease in psychomotor arousal, a decrease in concentration of attention, the speed of mental, motor reactions.
Muscle relaxant- Manifested by the elimination of muscle tension.
Anticonvulsant- is expressed in a decrease in convulsive activity.
Hypnotic- expressed in accelerating the onset of sleep, improving its qualities.

These effects have various drugs expressed to varying degrees, which should be considered when choosing a medicine. 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, 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, heartbeat, elimination of excessive sweating, etc.

Note!Tranquilizers have a potentiating effect. Their use enhances the effect of sleeping pills, painkillers, anesthetics. That 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 psychoses, which are successfully stopped by taking tranquilizers.

Thus, indications for the use of anxiolytics are:

(accompanied by anxiety, fear, restlessness);
anxiety disorders;
panic disorder;
obsessive-compulsive disorder;
with alcoholism, metal-alcohol psychosis;
Hyperkinesis, tics,;
Premedication (preparation for surgery).

It should be noted that the range of anxiolytics has long gone beyond the treatment of mental illness. So, these drugs are prescribed for psychosomatic diseases: peptic ulcer, as well as for dermatological diseases accompanied by itching.

Application features

The decision on 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 optimum. The duration of use should not exceed two to three weeks. At the end of the course of treatment, the dose of the drug is reduced gradually. If necessary long-term treatment 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, when treating with tranquilizers, you should not drive a car. The least pronounced sedative effect of "daytime" tranquilizers - Gidazepam, Trimetozin, Mebikar, Atarax.

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

Side effects, contraindications

Possible side effects when treated with tranquilizers, they are mainly associated with depression of the nervous system. This manifests itself in the form of daytime sleepiness, lethargy, a feeling of "brokenness", dulling of emotional reactions,. It is also possible the appearance of such side effects as muscle weakness, arterial hypotension, dry mouth, dyspepsia, potency disorders.

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

Contraindications to the appointment of tranquilizers:

Pregnancy, lactation;
myasthenia;
Liver failure;
respiratory failure;
Alcoholic, (with the exception of the relief of withdrawal symptoms);
(for benzodiazepine tranquilizers).

Benzodiazepine tranquilizers are not prescribed to persons under the age of eighteen. Only in cases of extreme necessity can their appointment 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 origin are sold without recipe and therefore are more popular among patients. But it is worth reiterating , 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 sedating effect appears a few minutes after intravenous and half an hour after intramuscular administration.

The medicine effectively eliminates anxiety, fear, normalizes night sleep. Therefore, Diazepam is prescribed for neurosis, panic and obsessive-compulsive disorders, with 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 convulsive 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 action is manifested by a decrease in feelings of anxiety, fear and anxiety. The drug is prescribed for the treatment of neurosis, psychopathy, autonomic lability, logoneurosis (stuttering), alcohol withdrawal syndrome.

Atarax

The active substance is hydroxyzine, a derivative of piperazine. Atarax is a non-benzodiazepine anxiolytic, belongs to the group of H1-histamine blockers. The drug is classified as a "soft" tranquilizers, it has a moderate anxiolytic effect. Produced in the form of tablets, a sedative effect develops after fifteen to thirty minutes.

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

Afobazole

Non-bezodiazepine anxiolytic, available in the form of tablets. The active ingredient is fabomotizol. It has a moderate anxiolytic and activating effect.

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

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

Grigorova Valeria, medical commentator

Tranquilizers (anxiolytics) are a group of psychotropic drugs that reduce or eliminate fear, anxiety, restlessness, irritability, emotional tension, i.e. have an anti-neurotic effect.

According to the chemical structure, tranquilizers are divided into several groups:

1. Derivatives of propanediol (glycerol)- meprobamate.
2. benzodiazepine derivatives- alprazolam, bromazepam, gidazepam, diazepam, clonazepam, lorazepam, medazepam, oxazepam, temazepam, tofisopam, triazolam, phenazepam, flunitrazepam, estazolam, chlordiazepoxide.
3. Azapirone derivatives- Buspirone.
4. Other derivatives- benactizine, hydroxyzine, mebicar, mexidol, oxylidine.

Benzodiazepine derivatives:
They are the main group of tranquilizers. They have the most pronounced antineurotic effect and are less likely to cause side effects than other groups of drugs.
Benzodiazepines for oral intake well absorbed and quickly penetrate into the blood. Diazepam and chlordiazepoxide are much better absorbed and penetrate the brain when taken orally than when intramuscular injection, which is important to remember when stopping acute anxiety states. Peak blood concentrations following oral administration vary between individual drugs and is achieved on average in 1-4 hours, which is also of great clinical importance.
Benzodiazepines are largely (80-95%) bound to blood albumin (diazepam - 95%, oxazepam - 90%, alprazolam - about 85%).
The duration of the antineurotic action is largely dependent on the half-life of the drug:
T 1/2 benzodiazepine tranquilizers and their active metabolites:

INN	T 1/2	Active metabolites T 1/2
Duration of action (T 1/2 more than 20 hours)
Chlordiazepoxide	9-18	Desmethylchlordiazepoxide (10-18), demoxepam (35-50)
Diazepam	33; 53 (when retaken)	N-desmethyldiazepam (50-99), oxazepam (5-12)
Medazepam	1-2	Diazepam
Bromazepam	12-24	-
Lorazepam	10-20	-
Nitrazepam	28-31	-
flunitrazepam	15-25	7-aminoflunitrazepam (23), N-desmethylflunitrazepam (31)
Alprazolam	12-15	-
Clonazepam	40	-
Benzodiazepines of medium duration of action (T 1/2 about 10 hours)
Oxazepam	5-12	-
temazepam	8-16	-
Short-acting benzodiazepines (T 1/2 about 5 hours)
Midazolam	2	-
Triazolam	2-3	7a-hydroxytriazolam (4-8)

Some benzodiazepines do not form active metabolites; they immediately turn into water-soluble compounds and are quickly excreted from the body, so these drugs are much easier to tolerate by patients, even if there is a violation of liver function or interaction with other drugs metabolized in the liver.
Benzodiazepines are excreted mainly by the kidneys, intestines (10%) in the form of conjugates, as well as 0.5-2% of the dose - unchanged.
The rate of elimination of benzodiazepines also depends on their lipophilicity. Drugs that are more lipid soluble, such as diazepam, penetrate the BBB more quickly and, therefore, their psychotropic effect manifests itself faster. However, it is faster and ends due to the redistribution of the drug in peripheral adipose tissues. Drugs that are less lipid soluble, such as lorazepam and oxazepam, act more slowly but for a longer duration.
Propanediol derivatives (Meprabomate):
Well absorbed from the gastrointestinal tract. Undergoes biotransformation in the liver with the formation of inactive metabolites. T_1/2 from plasma - 10 hours Passes through the placenta, passes into breast milk (concentration in breast milk 2-4 times higher than the concentration in the mother's blood plasma). Excreted mainly by the kidneys (8-19% unchanged).
Derivatives of azaspirodecanedione (Buspirone):
When taken orally, it is rapidly and completely absorbed, although bioavailability is only 4%, Cmax - 40-90 minutes, T1 / 2 - 2-3 hours; undergoes intensive biotransformation in the liver with the formation of an active metabolite (1-pyrimidinylpiperazine).