Anxiolytics (tranquilizers) are medicines that can reduce anxiety, fear and emotional tension.
Mechanism of action and pharmacodynamics effects
Tranquilizers can remove the state of mental stress or fear in healthy individuals, as well as with various neurotic and neurosis-like disorders. Unlike neuroleptics, they do not have antipsychotic activity and do not cause extrapyramidal side effects. In addition to the main anxiolytic effect, most tranquilizers note sleeping pills, miorelaxing and anticonvulsant effects, the ratio and severity of which vary significantly.
The chemical structure of tranquilizers is divided into several groups.
Derivatives of propanediol (glycerol) are meprobamate.
Benzodiazepine derivatives – alprazolam, bromazepam, hydazepam, diazepam, clonazepam, lorazepam, medazepam, oxazepam, temazepam, tofizopam, triazolam, phenazepam, flunitrazepam, estazolam, chlordiazepoxide, etc.
The azapyrone derivatives are buspirone.
Other derivatives are benactysine, hydroxysine, mebicar, mexidol, oxylidine, and others.
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It is customary to distinguish six main effects, to a greater or lesser degree characteristic of all tranquilizers.
- Tranquilizing, or anxiolytic (reducing anxiety, fear, emotional tension).
- Sedative (psychomotor retardation, daytime sleepiness, decreased concentration of attention, a decrease in the rate of reactions, potentiation of the action of alcohol and other depressing CNS agents).
- Miorelaxing (manifested in the form of sensations of weakness, lethargy, fatigue).
- Anticonvulsant (suppression of convulsive activity), diazepam IV is used to stop the convulsive syndrome, clonazepam for the treatment of various forms of epilepsy.
Sleeping pills (depending on the applied dose is characteristic for all benzodiazepines, but especially for drugs with short T1 / 2).
Vegetitabilizing (regulation of the vegetative nervous system); the effect is used for arresting neurovegetative manifestations of anxiety and diencephalic crises.
In the spectrum of action of some tranquilizers, some additional effects are sometimes noted.
Psychostimulant (medazepam, oxazepam, tofizopam, hydazepam and other so-called daytime tranquilizers) and thymo-analeptic (alprazolam) effects.
Antiphobic effect (weakening of panic disorders, phobia and obtrusiveness), for example in alprazolam, clonazepam.
Benzodiazepines for oral administration are well absorbed and rapidly penetrate into the blood. Diazepam and chlordiazepoxide are much better absorbed and enter the brain when ingested than with intramuscular injection, which is important to remember when managing acute anxiety conditions. Intravenous diazepam is one of the most effective methods of arresting convulsive syndrome. With intramuscular injection, lorazepam is most rapidly absorbed. The peak concentration in the blood during oral administration varies in individual drugs and is achieved on average after 1-4 hours, which is also of great clinical importance. For example, to quickly achieve an anxiolytic effect, it is better to use diazepam rather than chlordiazepoxide or oxazepam.
Benzodiazepines bind to a large extent (80-95%) with blood albumins, for example diazepam – by 95%, oxazepam – by 90%, alprazolam – by about 85%. Even more important for use is the T1 / 2 preparation (Tables 28-7), according to which all benzodiazepine derivatives can be divided into three groups.
- Long-acting drugs (T1 / 2 more than 20 hours), for example, chlorine diazepoxide, diazepam, phenazepam and medazepam.
- Short-acting drugs (T1 / 2 less than 5 hours), for example triazolam, midazolam.
- Medium-duration drugs (T1 / 2 5-20 h), for example lorazepam, bromazepam, oxazepam, alprazolam.