Brexanolone

Brexanolone, sold under the brand name Zulresso, is a synthetic neuroactive steroid used for the treatment of postpartum depression in adults. It is an intravenous formulation of allopregnanolone, an endogenous neurosteroid produced from progesterone, and acts as a positive allosteric modulator of GABA-A receptors to enhance inhibitory neurotransmission in the brain.

Brexanolone is approved in the United States for postpartum depression. It is administered as a continuous IV infusion over about 60 hours in a healthcare setting. Because of the risk of profound sedation and loss of consciousness, Brexanolone is available only under a risk evaluation and mitigation strategy (REMS) and patients require close monitoring during and after the infusion.

Clinical trials demonstrated a greater reduction in depressive symptoms compared with placebo within 60 hours of starting therapy, with benefits maintained for several weeks post-treatment when used as an adjunct to standard postpartum care.

Common adverse effects include sedation/somnolence, dizziness, flushing, and dry mouth. Concomitant use with other central nervous system depressants such as benzodiazepines or alcohol is discouraged. Brexanolone is not indicated for other depressive disorders.

Developed by Sage Therapeutics, Zulresso represents a targeted neurosteroid approach to postpartum mood disorders. The therapy highlights ongoing interest in GABAergic modulation as a treatment strategy for mood disturbances.