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The term << tranquilizers >> (from the Latin. Tranquillo-are - to make calm, serene) entered the medical literature in 1957 to refer to psychotropic drugs, used mainly for neurosis, states of mental stress and fear. Unlike neuroleptic substances, most tranquilizers have no pronounced antipsychotic effect. "Their action, addressing mainly to the psychopathological disorders of the neurotic level, unlike neuroleptic drugs, helps to eliminate a wide range of neurotic and neurosis-like disorders, reducing primarily emotional tension, anxiety and fear" (G. Ya. Avrutsky).
In modern literature, the terms << anxiolytic means >> and << anti-anxiety agents >> (antianxiety agents) are also used to refer to drugs of the same group. The term “tranquilizers” remains, however, the most common. It should be borne in mind that the drugs in this group have not only an anxiolytic effect. In varying degrees, they have four pharmacodynamic properties: anxiolytic, hypnotic, muscle relaxant and anticonvulsant.
Anxiolytic (antiphobic) and general restraining effect is the most important feature of tranquilizers. The hypnotic effect is expressed in facilitating the onset of sleep, enhancing the effect of hypnotic drugs; the effect of narcotic and analgesic drugs also increases. Therefore, tranquilizers are often used in neuroleptic algesia.
The muscle relaxant effect of tranquilizers is associated with an effect on the central nervous system, and not with peripheral curare-like action; therefore, they are sometimes called central relaxants. This effect is often a positive factor when using tranquilizers to relieve tension, feelings of fear, arousal, but it limits the use of drugs that have a pronounced muscle relaxant effect in patients whose work requires a quick, concentrated reaction (transport drivers, etc.).
Clinical aspects of the use of tranquilizers are characterized by the fact that in the process of therapy various emotional disorders and, above all, anxiety and fear of neurotic origin, which occur in the absence of productive psychotic symptoms, are reduced rather quickly. In contrast, acute delusional, hallucinatory, affective and other disorders, accompanied by anxiety and fear, with the appointment of tranquilizers almost never reduced. Due to the tranquilizing effect, a temporary decrease in affective tension and a slight decrease in the intensity of delusional hallucinatory and other disorders can sometimes be observed >>.
It should be noted that powerful tranquilizers (in particular, phenazepam) created in recent years can have a therapeutic effect in psychotic and psychopathic states.
When choosing a tranquilizer for clinical use, it is necessary to take into account the differences in the spectrum of their action. Some drugs have all the properties characteristic of tranquilizers (for example, diazepam), while others have a more pronounced anxiolytic effect. Some drugs (see Mezapam) have a relatively weak muscle relaxant property, and therefore they are more convenient for use during daytime hours and are often called daytime tranquilizers. However, in relatively large doses, all tranquilizers can show all pharmacological properties characteristic of this group of drugs.
By structure, tranquilizers belong to different classes of chemical compounds. The main modern drugs of this group are benzodiazepine derivatives. In addition, the value of carbamates propandiol (meprotan, etc.), derivatives of diphenylmethane (amisyl, etc.), representatives of some other chemical groups, have remained the same.
The mechanisms of action of tranquilizers are still not sufficiently clear. Neurophysiological studies indicate a decrease under the influence of tranquilizers on the excitability of the subcortical brain regions (the limbic system, the thalamus, the hypothalamus), which are responsible for carrying out emotional reactions, and the inhibition of the interaction between these structures and the cortex of the large brain. Tranquilizers also have an inhibitory effect on polysynaptic spinal reflexes, thereby causing muscle relaxation.
In the neurochemical aspect, different tranquilizers differ in their action. The effect on noradrenergic, dopaminergic, serotonergic systems is expressed in their relatively weak degree. However, benzodiazepine tranquilizers actively affect GABAergic systems; potentiating the central inhibitory effect of γ-aminobutyric acid (see Aminalon). Specific benzodiazepine receptors (and their subgroups), for which benzodiazepines are exogenous ligands, are found in the CNS cells. The nature of the endogenous ligand for these receptors is not completely understood.
There is a close relationship between benzodiazepine and GABA receptors. Benzodiazepines promote the release of GABA and its effect on synaptic transmission.
Derivatives of diphenylmethane (amisyl, etc.) actively influence the cholinergic systems of the brain, in connection with which they are also called central anticholinergics. Propandiol derivatives (meprotan and others) do not have a pronounced effect on benzodiazepine and cholinergic receptors.
Different tranquilizers are effective in various neurotic and neurosis-like states. Therefore, they have found wide application not only in psychiatric and neurological practice, but also in other areas of practical medicine. Widespread tranquilizers in outpatient practice. It should be emphasized that, despite the relatively low toxicity of the main tranquilizers (benzodiazepines, propanediol carbamates), they can be used only if there are appropriate indications and under medical supervision. Unreasonable and uncontrolled use of them can cause side effects, psychological dependence and other undesirable effects.
Tranquilizers should not be assigned to be taken before and during work by drivers of cars and persons of other professions who require rapid mental and motor responses. In exceptional cases, when increased nervous excitability interferes with successful production activities, it is possible to assign tranquilizers subject to the individual selection of the drug and its dose and careful medical observation of the patient.
It should also be borne in mind that alcohol potentiates the action of tranquilizers, so during their use you can not drink alcoholic beverages.
In the literature there are few indications that tranquilizers, not only having anticholinergic properties (amisyl, etc.), but others, such as meprobamate (meprotan) and especially diazepam (sibazon, seduxen, Relanium), can cause an increase in the secretion of aqueous humor of the eye , the difficulty of its outflow and increased intraocular pressure. In this regard, it is recommended to prescribe these drugs to patients with glaucoma with caution and not for a long time.