FDA approved brexanolone intravenous infusion as the first-ever drug indicated for the treatment of depression after childbirth (Zulresso).
Postpartum depression is associated with impaired mother-infant bonding and with adverse affects in the cognitive, behavioral, and emotional development of the child.
It is administered under medical supervision as a continuous infusion over a total of 60 hours (2.5 days).
Continuous pulse oximetry should be used to monitor patient, and if hypoxemia occurs treatment is stopped and not resumed.
Women receiving the drug should be monitored every two hours for excessive sedation.
Brexanolone is chemically identical to endogenous allopregnanolone, a hormone that decreases after childbirth.
It acts as a positive allosteric modulator of gamma-aminobutyric acid-A (GABAA) receptors, which become dysregulated in the postpartum period.
Positively modulate neuronal activation inhibitory GABAA receptors.
It is chemically identical to the endogenous neoroactive steroid allopregnanalone, the major metabolite of Progesterone.
Allopregnanolone levels increase during pregnancy and peak in the third trimester, and then drop sharply after parturition.
Has a REMS element.
Risks, include excessive sedation or sudden loss of consciousness during administration.
Patients must have continuous pulse oximetry monitoring during the whole 60-hour infusion and must be accompanied during interactions by their child(ren) while receiving the infusion.
Patients should not drive, operate machinery, or do other dangerous activities until feelings of sleepiness from the treatment have completely gone away.
In two placebo-controlled studies, brexanolone demonstrated superiority to placebo in improvement of depressive symptoms at the end of the first infusion.
The most common adverse reactions included sleepiness, dry mouth, loss of consciousness, dizziness and flushing.
The CDC estimates that 1 in 9 women ― and possibly as many as 1 in 5 experience postpartum depression.
Should not be used in pregnant women as developmental toxicities have occurred in animal fetuses.
The drug has low oral bioavailability.
Coadministration with other antidepressants is associated with an increased risk of sedation related events.
Oral version now approved, Zuranolone.