What is the mechanism of action of benzodiazepine tranquilizers?

The mechanism of action of benzodiazepine tranquilizers involves binding to allosteric benzodiazepine receptors and increasing 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, other than anxiolytic, do benzodiazepines produce?

In addition to the anxiolytic (antianxiety) effect, benzodiazepines produce four other pharmacological effects: sedative, hypnotic, anticonvulsant, and muscle relaxant.

What side effects are characteristic of benzodiazepines?

Benzodiazepines are associated with several common side effects, including 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 overdose. This drug is a competitive antagonist at benzodiazepine receptors and is administered intravenously.

What is the mechanism of action of buspirone?

The mechanism of action of buspirone involves the serotonergic system. The drug acts as a partial agonist at $5-HT_{1A}$ receptors, while not interacting with benzodiazepine receptors or stimulating the GABAergic system.

Which drug groups, aside from tranquilizers, exhibit anxiolytic activity?

In addition to tranquilizers, other drug groups exhibit an antianxiety (anxiolytic) effect. Specifically, these include antipsychotics, $eta$-blockers, and certain antidepressants such as tianeptine and maprotiline.

What are anxiolytics and what is their primary objective?

Anxiolytics, or tranquilizers, are pharmacological agents whose primary objective is to relieve internal emotional tension, fear, and anxiety.

Why was the term "tranquilizers" replaced by "anxiolytics"?

Originally, only benzodiazepines were called "tranquilizers." Later, it was discovered that other drugs (such as antipsychotics and $\beta$-blockers) also possess an antianxiety effect, prompting the more precise term "anxiolytics" to encompass all anti-fear and anti-anxiety medications.

What are the subgroups of benzodiazepine derivatives?

Benzodiazepine derivatives are divided into three groups based on the duration of their therapeutic effect: short-acting (1–12 hours), intermediate-acting (12–40 hours), and long-acting (40–250 hours).

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Anxiolytics

For medical students2 min readUpdated 2026-10-10

Anxiolytics, also known as tranquilizers, are medications capable of relieving fear, anxiety, and internal emotional tension. Modern classification of these agents accounts for their chemical structure and duration of therapeutic action.

Alternative nameTranquilizers

Main effectRelief of fear and anxiety

Duration of action1 to 250 hours

Main groupsBenzodiazepines and non-benzodiazepines

Terminology and Etymology

Originally, the term tranquilizers came from the Latin word tranquillare, meaning "to calm," and was applied exclusively to the benzodiazepine group. However, specialists later discovered that other medications, such as antipsychotics or $\beta$-blockers, also possess antianxiety properties.

As a result, a more precise modern term emerged — anxiolytics. This term is derived from the Latin words anxius (anxious) and lysis (dissolution), encompassing all medical drugs capable of effectively relieving fear and anxiety.

Classification by Duration of Effect

The pharmacological classification of anxiolytics is based on their chemical structure and duration of action. The largest group — benzodiazepine derivatives — is subdivided into three categories:

Short-acting (1 to 12 hours) — includes midazolam and triazolam.
Intermediate-acting (12 to 40 hours) — includes alprazolam, oxazepam, nitrazepam, temazepam, and phenazepam.
Long-acting (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, with buspirone as a prominent representative.
Derivatives of other chemical groups, notably mebicar and benzoclidine.

Frequently asked questions

What is the mechanism of action of benzodiazepine tranquilizers?: The mechanism of action of benzodiazepine tranquilizers involves binding to allosteric benzodiazepine receptors and increasing 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, other than anxiolytic, do benzodiazepines produce?: In addition to the anxiolytic (antianxiety) effect, benzodiazepines produce four other pharmacological effects: sedative, hypnotic, anticonvulsant, and muscle relaxant.
What side effects are characteristic of benzodiazepines?: Benzodiazepines are associated with several common side effects, including 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 overdose. This drug is a competitive antagonist at benzodiazepine receptors and is administered intravenously.
What is the mechanism of action of buspirone?: The mechanism of action of buspirone involves the serotonergic system. The drug acts as a partial agonist at $5-HT_{1A}$ receptors, while not interacting with benzodiazepine receptors or stimulating the GABAergic system.
Which drug groups, aside from tranquilizers, exhibit anxiolytic activity?: In addition to tranquilizers, other drug groups exhibit an antianxiety (anxiolytic) effect. Specifically, these include antipsychotics, $eta$-blockers, and certain antidepressants such as tianeptine and maprotiline.
What are anxiolytics and what is their primary objective?: Anxiolytics, or tranquilizers, are pharmacological agents whose primary objective is to relieve internal emotional tension, fear, and anxiety.
Why was the term "tranquilizers" replaced by "anxiolytics"?: Originally, only benzodiazepines were called "tranquilizers." Later, it was discovered that other drugs (such as antipsychotics and $\beta$-blockers) also possess an antianxiety effect, prompting the more precise term "anxiolytics" to encompass all anti-fear and anti-anxiety medications.
What are the subgroups of benzodiazepine derivatives?: Benzodiazepine derivatives are divided into three groups based on the duration of their therapeutic effect: short-acting (1–12 hours), intermediate-acting (12–40 hours), and long-acting (40–250 hours).

Go deeper

Evolution and etymology of the terms "tranquilizers" and "anxiolytics"
Detailed review 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