Brexanolone

Brexanolone is a  prescription medication used for the treatment of postpartum depression. 

• Brexanolone is available under the following different brand names: Zulresso

Common side effects of Brexanolone include:

• drowsiness,
• lightheadedness,
• dry mouth, and
• flushing (sudden warmth, redness, or tingly feeling).

Serious side effects of Brexanolone include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• excessive drowsiness,
• lightheadedness,
• sudden changes in mood or behavior,
• new or worsening depression, and
• thoughts of hurting yourself

Rare side effects of Brexanolone include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Intravenous solution: Schedule IV

• 5mg/mL (100mg/20mL single-dose vial)

Postpartum Depression

Adult dosage

• Dosing
• 0-4 hours: Initiate at 30 mcg/kg/hr
• 4-24 hours: Increase to 60 mcg/kg/hr
• 24-52 hours: Increase to 90 mcg/kg/hr (if not tolerated, consider reducing to 60 mcg/kg/hr)
• 52 to 56 hours: Decrease to 60 mcg/kg/hr
• 56 to 60 hours: Decrease to 30 mcg/kg/hr

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Brexanolone has severe interactions with no other drugs.
• Brexanolone has serious interactions with the following drugs:
  • metoclopramide intranasal
  • selinexor
• Brexanolone has moderate interactions with at least 172 other drugs.
• Brexanolone has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Brexanolone?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Brexanolone?”

Cautions

Sedation and sudden loss of consciousness

• Sedation and somnolence occurred during clinical trials that required dose interruption or reduction in some patients during infusion
• There was no clear association between loss or altered consciousness and pattern or timing of dose
• Not all patients who experienced a loss of or altered consciousness reported sedation or somnolence before the episode
• Caution against engaging in potentially hazardous activities requiring mental alertness (e.g., driving) after infusion until sedative effects dissipate
• Monitor oxygenation with continuous pulse oximetry

Suicidal thoughts and behaviors

• In pooled analyses of placebo-controlled trials of long-term administration of antidepressant drugs (SSRIs and other antidepressants) that included ~77,000 adults and 4,500 pediatric patients, the incidence of suicidal thoughts and behaviors in antidepressant-treated patients aged below 24 years was greater than in placebo-treated patients
• Brexanolone does not directly affect monoaminergic systems; because of this and the comparatively low number of exposures to brexanolone, the risk of developing suicidal thoughts and behaviors is unknown

Drug interaction overview

• Coadministration with CNS depressants (e.g., opioids, benzodiazepines) may increase the likelihood or severity of adverse reactions related to sedation
• In the placebo-controlled studies, a higher percentage of brexanolone-treated patients who used concomitant antidepressants reported sedation-related events

Pregnancy & Lactation

• Data are not available regarding use in pregnant women
• Based on findings in animals of other drugs that enhance GABAergic inhibition, brexanolone may cause fetal harm

Antidepressant pregnancy registry

• The pregnancy exposure registry monitors pregnancy outcomes in women exposed to antidepressants during pregnancy
• Clinicians are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185, OR
• Online at: https://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/antidepressants

Lactation

• Data from a lactation study in 12 women indicate that brexanolone is transferred to breastmilk in nursing mothers; however, the relative infant dose (RID) is low, 1-2% of the maternal weight-adjusted dosage
• Available data do not suggest a significant risk of adverse reactions to breastfed infants from exposure
• The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child from the drug or the underlying maternal condition