Brexanolone

What is Brexanolone?

• Brexanolone (ZULRESSO) is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator used in adults to treat a certain type of depression called Postpartum Depression.

What are the uses of this medicine?

• This medicine is used in adults to treat a certain type of depression called Postpartum depression.

How does this medicine work?

• The mechanism of action of brexanolone in the treatment of PPD in adults is not fully understood, but is thought to be related to its positive allosteric modulation of GABAA receptors.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid usage of ZULRESSO with CNS depressants (e.g., opioids, benzodiazepines) may increase the likelihood or severity of adverse reactions related to sedation.
• Avoid usage of ZULRESSO with antidepressants. ZULRESSO-treated patients who used concomitant antidepressants reported sedation-related events.

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

• A healthcare provider must be available on site to continuously monitor the patient, and intervene as necessary, for the duration of the infusion.
• Monitor patients for hypoxia using continuous pulse oximetry equipped with an alarm. Assess for excessive sedation every 2 hours during planned, non-sleep periods.

Recommended Dosage Administer ZULRESSO as a continuous intravenous (IV) infusion over a total of 60 hours (2.5 days) as follows:

• 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 (a reduction in dosage to 60 mcg/kg/hour may be considered during this time period for patients 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

• Dilution required prior to administration.

Administration

• ZULRESSO is given to you by continuous intravenous (IV) infusion into your vein.
• Your ZULRESSO infusion will last for a total of 60 hours (2.5 days).
• Use a programmable peristaltic infusion pump to ensure accurate delivery of ZULRESSO.
• Administer ZULRESSO via a dedicated line.
• Do not inject other medications into the infusion bag or mix with ZULRESSO.
• Fully prime infusion administration sets with admixture before inserting into the pump and connecting to the venous catheter.
• Use a PVC, non-DEHP, nonlatex infusion set.
• Do not use in-line filter infusion sets.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 100 mg/20 mL (5 mg/mL) single-dose vial.

This medicine is available in fallowing brand namesː

• ZULRESSO

What side effects can this medication cause?

The most common side effects of this medicine include:

• sleepiness
• dry mouth
• passing out
• flushing of the skin or face

ZULRESSO can cause serious side effects, including:

• Excessive sedation and sudden loss of consciousness

What special precautions should I follow?

• ZULRESSO may make you feel dizzy and sleepy.
• Do not drive a car or do other dangerous activities after your ZULRESSO infusion until your feeling of sleepiness has completely gone away.
• Do not drink alcohol while receiving ZULRESSO.
• During your ZULRESSO infusion, tell your healthcare provider right away if you feel like you cannot stay awake during the time you are normally awake or if you feel like you are going to pass out. Your healthcare provider may lower your dose or stop the infusion until your symptoms go away.
• You must have a caregiver or family member with you to help care for your child(ren) during your ZULRESSO infusion.
• Because of the risk of serious harm resulting from excessive sedation or sudden loss of consciousness, ZULRESSO is only available through a restricted program called the ZULRESSO REMS.

What to do in case of emergency/overdose?

• Overdosage may result in excessive sedation, including loss of consciousness and the potential for accompanying respiratory changes.

Management for overdosage

• In case of overdosage, stop the infusion immediately and initiate supportive measures as necessary.
• Brexanolone is rapidly cleared from plasma.
• Consult a Certified Poison Control Center at 1-800-222-1222 for latest recommendations.

Can this medicine be used in pregnancy?

• There are no available data on ZULRESSO use in pregnant women to determine a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants during pregnancy.
• Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185.

Can this medicine be used in children?

• The safety and effectiveness of ZULRESSO in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• brexanolone

Inactive ingredients:

• betadex sulfobutyl ether sodium, citric acid monohydrate, sodium citrate dihydrate, and water for injection.
• Hydrochloric acid or sodium hydroxide may be added during manufacturing to adjust pH.

Who manufactures and distributes this medicine?

Manufactured for:

• Sage Therapeutics, Inc.,Cambridge, MA 02142

What should I know about storage and disposal of this medication?

• Store the undiluted ZULRESSO product at 2°C to 8°C (36°F to 46°F).
• Do not freeze.
• Store protected from light.
• The diluted product in the infusion bag can be used at room temperature for up to 12 hours.
• If the diluted product is not used immediately after dilution, store under refrigerated conditions for up to 96 hours.

• Dailymed label info on Brexanolone
• FDA Brexanolone

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