How Do Nonbenzodiazepine Anxiolytics Work?

Reviewed on 1/10/2022

How Do Nonbenzodiazepine Anxiolytics Work?

Nonbenzodiazepine anxiolytics are medications usually prescribed as a second line treatment for anxiety disorders. Nonbenzodiazepine anxiolytics work on the central nervous system to induce mild sedation and relieve anxiety.

Nonbenzodiazepine anxiolytics work by balancing the activity of chemicals (neurotransmitters) in the brain. Nonbenzodiazepine anxiolytics activate or block protein molecules (receptors) on nerve cells (neurons) which stimulate inhibitory or excitatory action in response to signals from the neurotransmitters.

Currently, two nonbenzodiazepine anxiolytics are used to treat anxiety and each works in a different way to relieve symptoms:

  • Buspirone: Buspirone enhances the activity of 5HT1A serotonin receptors which are inhibitory and inhibit D2 dopamine receptors, which are excitatory. Serotonin and dopamine are neurotransmitters that regulate many functions including mood and emotions. It is not fully clear how buspirone reduces anxiety, but the effect is thought to be from increased serotonin activity in the anxiety/fear circuitry of the brain. Buspirone has no sedative effects.
  • Meprobamate: Meprobamate has an inhibitory effect on the limbic system of the brain, which regulates emotional and behavioral responses. The precise mechanism of meprobamate is unclear but it is believed to stimulate gamma aminobutyric acid (GABA) receptors which are inhibitory. Meprobamate has mild sedative, muscle relaxing and anticonvulsant effects.

How Are Nonbenzodiazepine Anxiolytics Used?

Nonbenzodiazepine anxiolytics are oral tablets used in the treatment of the following conditions:


  • Anxiety
  • Anxiety disorders
  • Preoperative sedation

Off-label uses:

What Are Side effects of Nonbenzodiazepine Anxiolytics?

Side effects of nonbenzodiazepine anxiolytics 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 Nonbenzodiazepine Anxiolytic Drugs?

Generic and brand names of nonbenzodiazepine anxiolytic drugs include:

  • buspirone
  • meprobamate

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