Neurosteroid antidepressants
Neuroactive steroids that boost GABA-A receptors; approved for postpartum depression. Their main risk is heavy sedation.
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)
Drugs in this class
- BrexanoloneAllopregnanolone given as a 60-hour IV infusion for postpartum depression. It boosts GABA-A receptors and can cause…GABA-A receptor (positive allosteric modulator)
- ZuranoloneAn oral neurosteroid antidepressant taken as a short course for postpartum depression. It impairs alertness, so no…GABA-A receptor (neurosteroid site)
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).
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 (MedlinePlus (U.S. National Library of Medicine), 2026); Zuranolone: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).
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Representative model, for educational purposes only.