Brexanolone

Products

Brexanolone was approved in the United States in 2019 in the form of an infusion product (Zulresso).

Structure and properties

Brexanolone (C21H34O2, Mr = 318.5 g/mol) corresponds to allopregnanolone, the major metabolite of the progestogen progesterone.

Effects

Brexanolone corresponds to the progesterone metabolite allopregnanolone, which peaks in the third trimester of pregnancy and whose concentration declines rapidly after delivery. Allopregnanolone is a neuroactive steroid that interacts with GABAA receptors (positive allosteric modulation). Declining levels appear to be involved in disease development. The half-life of brexanolone is in the range of 9 hours. The effect is rapid and persistent.

Indications

For the treatment of postpartum depression (postpartum depression).

Dosage

According to the SmPC. The drug is administered as an intravenous infusion at various doses for 60 consecutive hours. Because of the risk of severe sedation and loss of consciousness, patients require continuous medical monitoring.

Contraindications

Refer to the drug label for complete precautions.

Interactions

Central depressant drugs and antidepressants may increase adverse effects (sedation).

Adverse effects

The most common possible adverse effects include drowsiness, dry mouth, a loss of consciousness, and flushing.