How Do Benzodiazepine Anxiolytics Work?

Reviewed on 10/5/2021

How Do Benzodiazepine Anxiolytics Work?

Benzodiazepine anxiolytics are medications prescribed to treat anxiety and related disorders. Benzodiazepines work on the central nervous system to reduce hyperactivity in the brain and induce a calming effect. Benzodiazepine anxiolytics are also used for sedation, as muscle relaxants and to prevent seizures.

Benzodiazepines work on the limbic system of the brain, which regulates emotional and behavioral responses, and reticular formation which regulates sleep and consciousness. Benzodiazepines stimulate the activity of gamma aminobutyric acid (GABA), a chemical messenger (neurotransmitter) in the brain that inhibits nerve signals.

Benzodiazepines bind to GABA receptors, protein molecules on the surfaces of nerve cells (neuron) that respond to GABA, and increase the inflow of chloride ions, enhancing GABA’s effects. GABA inhibits electrical activity in the brain and produces sedation.

How Are Benzodiazepine Anxiolytics Used?

Benzodiazepine anxiolytics may be administered as:

  • Oral: Tablets, capsules, solutions and syrups
  • Injections:
    • Intravenous (IV): Injected into the vein
    • Intramuscular (IM): Injected into the muscle
  • Rectal: Gel applied inside the rectum

Benzodiazepine anxiolytics are used to treat the following conditions:


Orphan designation:

  • Hyperekplexia (a rare hereditary neurological disorder that causes excessive startle reaction to sudden noise or touch)
  • Recurrent, acute, repetitive seizures
  • Repetitive seizures caused by Dravet syndrome, a rare type of epilepsy
  • Organophosphorus poisoning (exposure to a neurotoxic substance that can cause muscle weakness, cramps and paralysis)

Off-label uses:

What Are Side Effects of Benzodiazepine Anxiolytics?

Side effects of antianxiety agents may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What Are Names of Some Benzodiazepine Anxiolytic Drugs?

Generic and brand names of benzodiazepine anxiolytic drugs include:


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