Terminology and origin of the term
Initially, the term "tranquilizers" came from the Latin word tranquillare, meaning "to calm," and was applied exclusively to the benzodiazepine group. However, specialists eventually discovered that other drugs, such as antipsychotics or $\beta$-blockers, also possess antianxiety properties.
As a result, a more precise modern name emerged — anxiolytics. This term is derived from the Latin words anxius (anxious) and lysis (dissolution) and encompasses all medicinal products capable of effectively relieving fear and anxiety.
Classification by duration of effect
The pharmacological classification of anxiolytic agents is based on their chemical structure and duration of action. The largest group — benzodiazepine derivatives — is subdivided into three categories:
- Short-acting (from 1 to 12 hours) — these include midazolam and triazolam.
- Intermediate-acting (from 12 to 40 hours) — include alprazolam, oxazepam, nitrazepam, temazepam, as well as the important drug phenazepam.
- Long-acting (from 40 to 250 hours) — represented by diazepam, flurazepam, and chlordiazepoxide.
Non-benzodiazepine anxiolytics
In addition to benzodiazepine derivatives, modern medical practice distinguishes a separate group of non-benzodiazepine structure anxiolytics. These include:
- Azaspirodecanedione derivatives, a prominent representative of which is buspirone.
- Derivatives of other chemical groups, among which mebicar and benzoclidine stand out.
Briefly: answers to topical questions
What is the mechanism of action of benzodiazepine tranquilizers?
The mechanism of action of benzodiazepine tranquilizers involves the stimulation of allosteric benzodiazepine receptors and an increase in the sensitivity of $GABA_A$ receptors to the neurotransmitter GABA. This leads to an increased frequency of chloride channel opening, enhanced influx of chloride ions into the neuron, and hyperpolarization of the neuronal membrane, which potentiates inhibitory effects in the central nervous system.
What pharmacological effects, besides the anxiolytic one, do benzodiazepines produce?
In addition to the anxiolytic (antianxiety) effect, benzodiazepines produce four other pharmacological effects. Their spectrum of activity includes sedative, hypnotic, anticonvulsant, and muscle-relaxant effects.
What side effects are typical for benzodiazepines?
Benzodiazepines are characterized by a number of common side effects. These include dizziness, headache, drowsiness, and ataxia, as well as the development of tolerance and drug dependence.
Which drug is used as an antidote in benzodiazepine overdose?
Flumazenil is used as a specific antidote in benzodiazepine poisoning. This drug is a competitive antagonist of benzodiazepine receptors and is administered intravenously.
What is the mechanism of action of buspirone?
The mechanism of action of buspirone is associated with the serotonergic system. The drug is a partial agonist of $5-HT_{1A}$ receptors; at the same time, it does not interact with benzodiazepine receptors and does not stimulate the GABAergic system.
Which drug groups, besides tranquilizers, possess anxiolytic activity?
In addition to tranquilizers, other groups of drugs also possess anti-anxiety (anxiolytic) effects. Specifically, these include antipsychotics, $\beta$-blockers, and certain antidepressants such as tianeptine and maprotiline.
Class and exam questions
What are anxiolytics and what is their main task?
Anxiolytics, or tranquilizers, are pharmacological agents whose main task is to eliminate internal emotional tension, feelings of fear, and anxiety.
Why was the term "tranquilizers" replaced by "anxiolytics"?
Initially, only benzodiazepines were called "tranquilizers." Later it turned out that other drugs (such as antipsychotics and $\beta$-blockers) also possess an antianxiety effect, which is why the more precise name "anxiolytics" appeared, combining all drugs for fear and anxiety.
What subgroups are benzodiazepine derivatives divided into?
Benzodiazepine derivatives are divided according to the duration of their therapeutic effect into three groups: short- (1–12 hours), intermediate- (12–40 hours), and long-acting (40–250 hours).
What else to study on this topic
- Evolution and origin of the terms "tranquilizers" and "anxiolytics"
- Detailed analysis of short-acting benzodiazepine derivatives
- Characteristics of intermediate- and long-acting benzodiazepines
- Features of azaspirodecanedione derivatives using buspirone as an example
- Drugs of other chemical groups among non-benzodiazepine anxiolytics
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