The neurosteroid allopregnanolone, a derivative of progesterone, is a positive modulator of GABA-A receptors. Because GABA-mediated signaling has previously been implicated in depressive disorders, researchers have focused on medications targeting allopregnanolone-mediated signaling in the search for antidepressants with a novel mechanism of action.
Treatment with an analog of allopregnanolone, intravenously administered brexanolone, has been shown to improve depressive symptoms in women with postpartum depression. Brexanolone is the first drug approved by the FDA to treat postpartum depression. In contrast to conventional antidepressants, the antidepressant effects of brexanolone are evident in a matter of days.
In this thorough review (FULL TEXT available), Edinoff and colleagues discuss the development of brexanolone for the treatment of postpartum depression.
Edinoff AN, Odisho AS, Lewis K, Kaskas A, Hunt G, Cornett EM, Kaye AD, Kaye A, Morgan J, Barrilleaux PS, Lewis D, Viswanath O, Urits I. Brexanolone, a GABAA Modulator, in the Treatment of Postpartum Depression in Adults: A Comprehensive Review. Front Psychiatry. 2021 Sep 14;12:699740. Free article. Review.