In psychiatric practice, a fairly extensive group of pharmacological drugs is used. Psychiatry uses tranquilizers more often than other medical fields. But they are used not only for the treatment of psychopathic diseases.
So what are tranquilizers, the principle of action of anxiolytics, and where are they used?
This type of medication, together with antipsychotics, belongs to the class of psychotropic drugs of a depressing type of effect.
History reference
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 application history began with the introduction of Meprotana (Meprobamata) in 1958 and Elenium (Chlordiazepoxide) in medical practice in 1959. In 1960, Diazepam, aka Sibazon or Relium, was launched on the pharmacological market.
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 experiences. They are often prescribed for the treatment of neurosis, as premedication before surgery. Benzodiazepines are the most extensive group of tranquilizers, which are effectively used to relieve muscle cramps and in the treatment of epilepsy.
The mechanisms of action of tranquilizers are not yet clear. But this does not interfere with their widespread use. In addition, they are quite well classified.
Tranquilizers: classification
The mechanism of action is the first condition by which tranquilizers are divided into three groups:
1. Benzodiazepines (agonists of benzodiazepine receptors). These tranquilizers, in turn, are classified according to the mechanism of action and the duration of exposure:
a.
- short-term (less than 6 hours);
- average duration of action (from 6 to 24 hours);
- prolonged exposure (from 24 to 48 hours).
b.
Features of biotransformation (with and without the formation of FAM).
in.
By the severity of sedative-hypnotic effects (maximum or minimum).
g.
By the rate of absorption in the gastrointestinal tract (fast, slow, intermediate absorption).
2. Agonists of serotonin receptors.
3. Substances of different types of action.
The description of the mechanism of action of tranquilizers in the medical literature usually comes down to the fact that these are psychopharmacological agents designed to reduce emotional tension, fear, and anxiety. However, that is 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 non-psychiatric illnesses.
So, for example, muscle relaxant effect is important not only in the treatment of neurological diseases, but also in anesthesiology. Some substances can cause smooth muscle relaxation, which allows them to be used to treat various diseases that are accompanied by cramping, for example, 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 stem sections of the reticular pharmacy and hypothalamus, an increase in GABAergic inhibition in the central nervous system is characteristic. These drugs have a stimulating effect on the benzodiazepine receptor of the chlorine channel of the GABAergic complex, which leads to conformational changes in the receptors and to an increase in the number of chlorine channels. By the way, barbiturates, unlike benzodiazepines, increase the duration of the opening.
The flow of chlorine ions inside the cells increases, the affinity (affinity) of GABA for receptors increases. Since an excess of a negative charge (chlorine) appears on the inner surface of the cell membrane, inhibition of neuronal sensitivity and its hyperpolarization begin.
If this occurs at the level of the ascending part of the reticular formation of the brain stem, a sedative effect develops, and if at the level of the limbic system, anxiolytic (tranquilizing). Reducing emotional stress, eliminating anxiety, fear, creating a sleeping pill (applies 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 they may remain residual, which is usually manifested by lethargy, apathy, weakness, drowsiness, an increase in reaction time, decreased alertness, disorientation, and poor coordination.
Resistance (tolerance) develops to these drugs, so more and more doses will be required over time.
Based on the previous paragraph, they are characterized by a withdrawal syndrome, which is manifested by recurrent insomnia. After a long time of admission, insomnia, attention disorder, dizziness, tremor, sweating, dysphoria join insomnia.
Benzodiazepine overdose
In case of overdose, hallucinations, muscle atony (relaxation), impaired articulation occur, and after sleep, coma, inhibition of cardiovascular and respiratory functions, collapse. In case of an overdose, Flumazenil is used, which is an antagonist of benzodiazepines. It blocks benzodiazepine receptors and reduces or eliminates the severity of effects.
Serotonin Receptor Agonists
"Buspirone" refers to a group of serotonin receptor agonists. The mechanism of action of the Buspirone tranquilizer is associated with a decrease in the synthesis and release of serotonin, as well as with 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. He has no sleeping pills, muscle-relaxing, sedative, anticonvulsant effect. Almost not able to cause drug dependence.
Substances of different types of action
The mechanism of action of the Benactizin tranquilizer is due to the fact that it is an M, N-anticholinergic. It has a sedative effect, which is caused, as expected, by the blockade of M-cholinergic receptors in the reticular part of the brain.
It has a mild local anesthetic, antispasmodic effect. It inhibits the effects of the exciting vagus nerve (reduces the secretion of glands, reduces the tone of smooth muscles), a cough reflex. Due to the effect on the effects of the exciting vagus nerve, Benactisin is often used to treat diseases that occur with smooth muscle spasms, such as ulcerative pathologies, cholecystitis, colitis, etc.
Hypnotic tranquilizers
Hypnotic tranquilizers: 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"); antipsychotics ("Aminazine", "Chlorprotixen", "Sonapaks"). Some groups of antidepressants are prescribed for the 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 divided into a new group of imidazopyridines (non-benzodiazepines). These include Zolpidem (Sanval). It is distinguished by the least toxicity, lack of addiction, it does not violate the respiratory function in a dream and does not affect daytime wakefulness. Zolpidem shortens the time of falling asleep and normalizes the phases of sleep. It has an optimal duration effect. It is the standard for the treatment of insomnia.
The mechanism of action of tranquilizers: pharmacology
Medazepam It causes all the effects characteristic of benzodiazepines, however, sedative-hypnotic and myorealixant actions are weakly expressed. Medazepam is considered a daytime tranquilizer.
Xanax (Alprazolam). Almost no hypnotic effect. Briefly relieves feelings of fear, anxiety, anxiety, depression. It is quickly absorbed. The peak concentration of a substance in the blood occurs within 1-2 hours after administration. It can accumulate in the body in people with impaired renal and hepatic function.
"Phenazepam." The famous tranquilizer, which 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 stop seizures, epileptic seizures. Less commonly used as sleeping pills.
"Oxazepam" ("Nozepam", "Tazepam"). It is similar in action to Diazepam, but it is much less active. Anticonvulsant and muscle relaxant effects are mild.
"Chlordiazepoxide" ("Librium", "Elenium", "Chlozepide"). Refers to the first, classic benzodiazepines. It has all the positive and undesirable effects characteristic of benzodiazepines.