In psychiatric practice, a fairly large group of pharmacological drugs is used. Psychiatry uses tranquilizers more than other medical fields. But they are not only used to treat psychopathic illnesses.
So what are tranquilizers, how do anxiolytics work, and where are they used?
This type of medicine, together with neuroleptics, belongs to the class of psychotropic drugs of an oppressive type of influence.
Historical background
The development of the first drugs of this group began in the 1950s. At the same time, scientific psychopharmacology was born. The mechanism of action of tranquilizers then only began to be studied. The history of application began with the introduction of Meprotan (Meprobamate) into medical practice in 1958 and Elenium (Chlordiazepoxide) in 1959. In 1960, "Diazepam" was released on the pharmacological market, it is also"Sibazon" or "Relium".
Currently, the group of tranquilizers includes more than 100 drugs. Today they are being actively improved.
Tranquilizers (anxiolytics) are used to reduce the level of aggression, anxiety, anxiety, emotional distress. They are quite often prescribed for the treatment of neuroses, as a premedication before a surgical operation. Benzodiazepines are the most extensive group of tranquilizers, which are effectively used to relieve muscle cramps and in the treatment of epilepsy.
Mechanisms of action of tranquilizers are still not clear enough. But this does not prevent their widespread use. Other than that, they are fairly well classified.
Tranquilizers: classification
The mechanism of action is the first condition according to which tranquilizers are divided into three groups:
1. Benzodiazepines (benzodiazepine receptor agonists). These tranquilizers are in turn classified according to their mechanism of action and duration of action:
a.
- short-term (less than 6 hours);
- average duration (6 to 24 hours);
- Long exposure (24 to 48 hours).
b.
Features of biotransformation (with and without FAM formation).
v.
According to the severity of the sedative-hypnotic effect (maximum or minimum).
g.
Absorption rate in the gastrointestinal tract (fast, slow, intermediate absorption).
2. Serotonin receptor agonists.
3. Substances of different types of action.
Description of the mechanism of action of tranquilizers in the medical literature usually boils down to the fact that these are psychopharmacological agents designed to reduce emotional tension, fear, and anxiety. However, that's not all. Tranquilizers are designed not only to calm. The mechanism of action of tranquilizers is associated with their ability to weaken the processes of strong excitation of the hypothalamus, thalamus, limbic system. They enhance the processes of internal inhibitory synapses. They are often used to treat diseases not related to psychiatry.
For example, muscle relaxant action is important not only in the treatment of neurological diseases, but also in anesthesiology. Some substances can cause smooth muscle relaxation, which makes them suitable for the treatment of various diseases that are accompanied by spasms, such as ulcerative manifestations of the gastrointestinal tract.
Benzodiazepines
This is the most common and extensive group of classical anxiolytics. These tranquilizers have hypnotic, sedative, anxiolytic, muscle relaxant, amnestic and anticonvulsant effects. For benzodiazepine tranquilizers, the mechanism of action of which is associated with their effect on the limbic system and, to some extent, on the brainstem sections of the reticular pharmacy and the hypothalamus, an increase in GABAergic inhibition in the central nervous system is characteristic. These drugs have a stimulating effect on the benzodiazepine receptorchloride channel of the GABA-ergic complex, which leads to conformational changes in receptors and an increase in the number of chloride channels. By the way, barbiturates, unlike benzodiazepines, increase the duration of opening.
The current of chloride ions inside cells increases, the affinity (affinity) of GABA to receptors increases. Since an excess of negative charge (chlorine) appears on the inner surface of the cell membrane, the inhibition of neuronal sensitivity and its hyperpolarization begins.
If this happens at the level of the ascending part of the reticular formation of the brain stem, a sedative effect develops, and if it occurs at the level of the limbic system - anxiolytic (tranquilizing). Reducing emotional stress, eliminating anxiety, fear, a hypnotic effect is created (refers to night tranquilizers). The muscle relaxant effect (muscle-relaxing) develops due to the effect of benzodiazepines on polysynaptic spinal reflexes and inhibition of their regulation.
Cons of benzodiazepines
Even if applied at night, during the day there may be a residual effect of their action, which is usually manifested by lethargy, apathy, fatigue, drowsiness, increased reaction time, decreased alertness, disorientation, impaired coordination.
Resistance (tolerance) develops to these drugs, thus increasing doses will be required over time.
Based on the previous paragraph, they are characterized by a withdrawal syndrome that manifests itselfrecurrent insomnia. After a long time of admission, irritability, attention disorder, dizziness, tremor, sweating, dysphoria join insomnia.
Benzodiazepines overdose
With overdoses, hallucinations, muscle atony (relaxation), articulation disorders, and after sleep, coma, depression of cardiovascular and respiratory functions, collapse occur. In case of an overdose, Flumazenil is used, which is a benzodiazepine antagonist. It blocks benzodiazepine receptors and reduces or eliminates the effects completely.
Serotonin receptor agonists
"Buspirone" belongs to the group of serotonin receptor agonists. The mechanism of action of the tranquilizer "Buspirone" is associated with a decrease in the synthesis and release of serotonin, as well as a decrease in the activity of serotonergic neurons. The drug blocks post- and presynaptic dopamine D2 receptors, accelerates the excitation of dopamine neurons.
The effect of the use of "Buspirone" develops gradually. It has no hypnotic, muscle-relaxing, sedative, anticonvulsant effect. Virtually incapable of causing drug addiction.
Substances of different types of action
The mechanism of action of the tranquilizer "Benactizine" is due to the fact that it is an M, N-anticholinergic. It has a sedative effect, which is supposedly caused by the blockade of M-cholinergic receptors in the reticular part of the brain.brain.
It has a moderate local anesthetic, antispasmodic effect. Inhibits the effects of the excitatory vagus nerve (reduces the secretion of glands, reduces the tone of smooth muscles), cough reflex. Due to its influence on the effects of the excitatory vagus nerve, Benaktizin is often used to treat diseases that occur with spasms of smooth muscles, such as ulcerative pathologies, cholecystitis, colitis, etc.
Sleeping pills tranquilizers
Tranquilizers-hypnotics: the main mechanism of action on the body is associated with a hypnotic effect. They are often used to correct sleep disorders. Often, tranquilizers of other groups are used as sleeping pills ("Relanium", "Phenazpem"); antidepressants ("Remeron", "Amitriptyline"); neuroleptics ("Aminazine", "Chlorprothixen", "Sonapax"). Some groups of antidepressants are prescribed at night ("Lerivon", "Remeron", "Fevarin"), since the effect of drowsiness from them develops quite strongly.
Hypnotics are divided into:
- benzodiazepines;
- barbiturates;
- melatonin, ethanolamines;
- non-benzodiazepine hypnotics.
Imidazopyridines
Now there is a new generation of tranquilizers, which is subdivided into a new group of imidazopyridines (nonbenzodiazepines). These include Zolpidem("Sanval"). It is distinguished by the least toxicity, lack of addiction, it does not disrupt the function of breathing during sleep and does not affect daytime wakefulness. "Zolpidem" shortens the time to fall asleep and normalizes sleep phases. It has an optimal effect in terms of duration. Is the standard for the treatment of insomnia.
Mechanism of action of tranquilizers: pharmacology
"Medazepam". It causes all the effects characteristic of benzodiazepines, however, the sedative-hypnotic and myorealixant effects are poorly expressed. Medazepam is considered a daytime tranquilizer.
"Xanax" ("Alprazolam"). Virtually no sedative effect. Briefly relieves feelings of fear, anxiety, restlessness, depression. Absorbed quickly. The peak concentration of the substance in the blood occurs 1-2 hours after ingestion. Able to accumulate in the body in people with impaired kidney and liver function.
"Phenazepam". A well-known tranquilizer that was synthesized in the USSR. It appears to have all the effects characteristic of benzodiazepines. It is prescribed as a sleeping pill, as well as for the relief of alcohol withdrawal (withdrawal syndrome).
"Diazepam" ("Seduxen", "Sibazon", "Relanium"). It has a pronounced anticonvulsant and muscle-relaxing effect. It is often used to relieve convulsions, epileptic seizures. Less commonly used assleeping pills.
"Oxazepam" ("Nozepam", "Tazepam"). It is similar in action to Diazepam, but it is much less active. Anticonvulsant and muscle relaxant effects are weak.
"Chlordiazepoxide" ("Librium", "Elenium", "Chlosepide"). It belongs to the first classical benzodiazepines. It has all the positive and negative effects that are characteristic of benzodiazepines.
