Brexanolone (U.S. brand name ZulressoTM) is a neuroactive steroid and a gamma-aminobutyric acid (GABA) A receptor positive modulator that is available as an injection for intravenous use. It has to be given as a continuous intravenous infusion over 60 hours, that is, 2.5 days. It was approved by the FDA in March 2019.
On this page, we present basic information about this medication. Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
Treatment of postpartum depression in adults.
Note that brexanolone is the first medication that has been approved by the FDA specifically for the treatment of postpartum depression.
How well does it work?
What is so special about brexanolone? Not that it is more effective than other antidepressants but that it works very quickly–in just a couple of days–so that, if it works, the mother could potentially be back quickly to be her baby with less or no depression. For our review of the efficacy of brexanolone, please see the following article on this website (for subscribers only):
Brexanolone carries a Boxed Warning and has to be prescribed through a special Risk Evaluation and Mitigation Strategy (REMS) program. What this means is that it is only available at health care facilities that have been specifically certified through the brexanolone REMS program and the patient’s information has to be registered with the REMS program before the treatment is given.
Why? Why is a special REMS program needed? Because there is a concern that excessive sedation or sudden loss of consciousness can occur while the intravenous injection of brexanolone is being given. Because of this risk, patients have to carefully monitored during the infusion and continuous pulse oximetry monitoring has to be done (which is easy to do, of course). Also, while the infusion is being given, the mother has to be supervised while interacting with her children.
Potential side effects
Other than possible sedation and loss of consciousness, other side effects reported with brexanolone were dry mouth and flushing.
Brexanolone is administered as a continuous intravenous infusion over 60 hours (about 2.5 days) as follows (source: Prescribing Information):
- 0 to 4 hours: Initiate with a dosage of 30 mcg/kg/hour
- 4 to 24 hours: Increase dosage to 60 mcg/kg/hour
- 24 to 52 hours: Increase dosage to 90 mcg/kg/hour (alternatively consider a dosage of 60 mcg/kg/hour for those who do not tolerate 90 mcg/kg/hour)
- 52 to 56 hours: Decrease dosage to 60 mcg/kg/hour
- 56 to 60 hours: Decrease dosage to 30 mcg/kg/hour
The medication needs to be diluted in preparation for the infusion.
Several precautions need to be taken to make sure the correct dose is given and the patient is appropriately monitored:
1. A programmable peristaltic infusion pump should be used because it ensures more accurate delivery of the correct dose of the medication being infused.
2. No other medications should be mixed into the infusion bag being used for brexanolone or given through the same intravenous line.
3. The patient must be carefully monitored throughout the infusion by some member of the medical team because of the risk of sedation.
4. Continuous pulse oximetry monitoring has to be done throughout the infusion.
5. While the infusion is being given, the mother has to be supervised while interacting with her children.
Dosage forms and strengths
Injection: 100 mg/20 mL (5 mg/mL) single-dose vial.
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
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