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# Neurosteroid antidepressants

Neuroactive steroids that boost GABA-A receptors; approved for postpartum depression. Their main risk is heavy sedation.

Updated Nov 1, 2026

## What they are

Antidepressants with a mechanism unlike monoamine drugs. Brexanolone is given as a continuous intravenous infusion in a medical facility; zuranolone is a short oral course.

## Mechanism of action

Allopregnanolone, a natural derivative of progesterone, is a positive allosteric modulator of GABA-A receptors: it increases the chloride current opened by GABA. Reduced levels of this neurosteroid have been associated with depression, and these drugs may restore the signal. Because they enhance inhibition throughout the brain, sedation and loss of consciousness are the key risks.

Target: GABA-A receptor (positive allosteric modulation)

## Key points

- Brexanolone is allopregnanolone itself, given by continuous IV infusion over about 2.5 days under a restricted programme.
- Brexanolone can cause excessive sedation and sudden loss of consciousness, so the patient is observed throughout the infusion.
- Zuranolone is taken by mouth for a short course; driving and other risky activities are avoided for at least 12 hours after each dose.
- Alcohol, benzodiazepines, opioids and other CNS depressants add to the sedation.
- Like other antidepressants they carry a warning about suicidal thoughts in young people.

## Drugs in this class

- [**Brexanolone** Allopregnanolone given as a 60-hour IV infusion for postpartum depression. It boosts GABA-A receptors and can cause… GABA-A receptor (positive allosteric modulator)](https://durgical.com/en/pharmacology/brexanolone/)
- [**Zuranolone** An oral neurosteroid antidepressant taken as a short course for postpartum depression. It impairs alertness, so no… GABA-A receptor (neurosteroid site)](https://durgical.com/en/pharmacology/zuranolone/)

## Test yourself

Think of the answer, then tap the question to see it.

## On which receptor do neurosteroid antidepressants act, and how?

On GABA-A receptors, as positive allosteric modulators that increase GABA's chloride current.

## Which natural steroid is brexanolone?

Allopregnanolone, a derivative of progesterone.

## What is the main safety risk of this class?

Excessive sedation, with loss of consciousness (brexanolone) and impaired driving (zuranolone).

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Brexanolone Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619037.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Zuranolone: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a623048.html) (MedlinePlus (U.S. National Library of Medicine), 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/classes/neurosteroid-antidepressants/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/classes/neurosteroid-antidepressants/