brexanolone (Rx)

Brand and Other Names:Zulresso
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

intravenous solution: Schedule IV

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

Postpartum Depression

Indicated for treatment of postpartum depression (PPD)

Administer as a continuous IV infusion over a total of 60 hr (2.5 days) in a monitored health setting that is able to intervene as necessary with continuous pulse oximetry

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 Modifications

Excessive sedation

  • If excessive sedation occurs at any time, stop infusion until symptoms resolve
  • May resume infusion at the same or lower dose as clinically appropriate

Hypoxia

  • Immediately stop the infusion if pulse oximetry reveals hypoxia
  • After hypoxia, do not resume the infusion

Renal impairment

  • Mild-to-severe (eGFR ≥15 mL/min/1.73m²): No dose adjustment necessary
  • End-stage renal disease (eGFR <15 mL/min/1.73m²): Avoid use; potential accumulation of the solubilizing agent used for brexanolone (ie, betadex sulfobutyl ether sodium)

Hepatic impairment

  • No dose adjustment necessary

Dosing Considerations

Healthcare provider must be available on site to continuously monitor the patient, and intervene as necessary, for the duration of the infusion

Monitor for hypoxia using continuous pulse oximetry equipped with an alarm

Assess for excessive sedation q2hr during planned, nonsleep periods

Initiate treatment early enough during the day to allow for recognition of excessive sedation

Safety and efficacy not established

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Interactions

Interaction Checker

and brexanolone

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (2)

              • metoclopramide intranasal

                brexanolone, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

              • selinexor

                selinexor, brexanolone. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.

              Monitor Closely (169)

              • acetaminophen/phenyltoloxamine

                brexanolone, acetaminophen/phenyltoloxamine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • acrivastine

                brexanolone, acrivastine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • alfentanil

                brexanolone, alfentanil. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • alprazolam

                brexanolone, alprazolam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • amobarbital

                brexanolone, amobarbital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • arbaclofen

                brexanolone, arbaclofen. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • aripiprazole

                brexanolone, aripiprazole. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • asenapine

                brexanolone, asenapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • baclofen

                brexanolone, baclofen. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • benperidol

                brexanolone, benperidol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • benzhydrocodone/acetaminophen

                brexanolone, benzhydrocodone/acetaminophen. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • brexpiprazole

                brexanolone, brexpiprazole. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • brivaracetam

                brexanolone, brivaracetam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • brompheniramine

                brexanolone, brompheniramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine

                brexanolone, buprenorphine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine buccal

                brexanolone, buprenorphine buccal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine subdermal implant

                brexanolone, buprenorphine subdermal implant. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine transdermal

                brexanolone, buprenorphine transdermal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buprenorphine, long-acting injection

                brexanolone, buprenorphine, long-acting injection. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • buspirone

                brexanolone, buspirone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • butabarbital

                brexanolone, butabarbital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • butalbital

                brexanolone, butalbital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • butorphanol

                brexanolone, butorphanol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • calcium/magnesium/potassium/sodium oxybates

                brexanolone, calcium/magnesium/potassium/sodium oxybates. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • carbamazepine

                brexanolone, carbamazepine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • carbinoxamine

                brexanolone, carbinoxamine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • cariprazine

                brexanolone, cariprazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • carisoprodol

                brexanolone, carisoprodol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • cenobamate

                cenobamate, brexanolone. Either increases effects of the other by sedation. Use Caution/Monitor.

              • chloral hydrate

                brexanolone, chloral hydrate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • chlordiazepoxide

                brexanolone, chlordiazepoxide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • chlorpheniramine

                brexanolone, chlorpheniramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • chlorpromazine

                brexanolone, chlorpromazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • chlorzoxazone

                brexanolone, chlorzoxazone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clemastine

                brexanolone, clemastine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clobazam

                brexanolone, clobazam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clonazepam

                brexanolone, clonazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clonidine

                brexanolone, clonidine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clorazepate

                brexanolone, clorazepate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • clozapine

                brexanolone, clozapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • codeine

                brexanolone, codeine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • cyclobenzaprine

                brexanolone, cyclobenzaprine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • cyproheptadine

                brexanolone, cyproheptadine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • dantrolene

                brexanolone, dantrolene. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • desflurane

                brexanolone, desflurane. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • deutetrabenazine

                brexanolone, deutetrabenazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • dexbrompheniramine

                brexanolone, dexbrompheniramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • dexchlorpheniramine

                brexanolone, dexchlorpheniramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • diazepam

                brexanolone, diazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • diazepam intranasal

                diazepam intranasal, brexanolone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.

              • dimenhydrinate

                brexanolone, dimenhydrinate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • diphenhydramine

                brexanolone, diphenhydramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • diphenoxylate hcl

                brexanolone, diphenoxylate hcl. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • dosulepin

                brexanolone, dosulepin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • doxylamine

                brexanolone, doxylamine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • droperidol

                brexanolone, droperidol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • efavirenz

                brexanolone, efavirenz. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • emedastine

                brexanolone, emedastine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • esketamine intranasal

                brexanolone, esketamine intranasal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • estazolam

                brexanolone, estazolam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • eszopiclone

                brexanolone, eszopiclone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ethanol

                brexanolone, ethanol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ethosuximide

                brexanolone, ethosuximide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ethotoin

                brexanolone, ethotoin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ezogabine

                brexanolone, ezogabine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • felbamate

                brexanolone, felbamate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fenfluramine

                fenfluramine, brexanolone. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration with drugs that increase serotoninergic effects may increase the risk of serotonin syndrome.

              • fentanyl

                brexanolone, fentanyl. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fentanyl intranasal

                brexanolone, fentanyl intranasal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fentanyl transdermal

                brexanolone, fentanyl transdermal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fentanyl transmucosal

                brexanolone, fentanyl transmucosal. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • flibanserin

                brexanolone, flibanserin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fluphenazine

                brexanolone, fluphenazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • flurazepam

                brexanolone, flurazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • fosphenytoin

                brexanolone, fosphenytoin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • gabapentin

                brexanolone, gabapentin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

                gabapentin, brexanolone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • gabapentin enacarbil

                brexanolone, gabapentin enacarbil. Either increases toxicity of the other by sedation. Use Caution/Monitor.

                gabapentin enacarbil, brexanolone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • guanfacine

                brexanolone, guanfacine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • haloperidol

                brexanolone, haloperidol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • hydrocodone

                brexanolone, hydrocodone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • hydromorphone

                brexanolone, hydromorphone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • hydroxyzine

                brexanolone, hydroxyzine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • iloperidone

                brexanolone, iloperidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • isoflurane

                brexanolone, isoflurane. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ketamine

                brexanolone, ketamine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • lamotrigine

                brexanolone, lamotrigine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • lasmiditan

                lasmiditan, brexanolone. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.

              • lemborexant

                lemborexant, brexanolone. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects. .

              • levetiracetam

                brexanolone, levetiracetam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • levorphanol

                brexanolone, levorphanol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • lorazepam

                brexanolone, lorazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • loxapine

                brexanolone, loxapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • loxapine inhaled

                brexanolone, loxapine inhaled. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • loxicodegol

                brexanolone, loxicodegol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • lurasidone

                brexanolone, lurasidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • maprotiline

                brexanolone, maprotiline. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • meclizine

                brexanolone, meclizine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • meperidine

                brexanolone, meperidine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • meprobamate

                brexanolone, meprobamate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • metaxalone

                brexanolone, metaxalone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • methadone

                brexanolone, methadone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • methocarbamol

                brexanolone, methocarbamol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • methohexital

                brexanolone, methohexital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • methsuximide

                brexanolone, methsuximide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • midazolam

                brexanolone, midazolam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • midazolam intranasal

                midazolam intranasal, brexanolone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

              • mirtazapine

                brexanolone, mirtazapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • molindone

                brexanolone, molindone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • morphine

                brexanolone, morphine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • nalbuphine

                brexanolone, nalbuphine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • nitric oxide gas

                brexanolone, nitric oxide gas. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • olanzapine

                brexanolone, olanzapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • oliceridine

                brexanolone, oliceridine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • opium tincture

                brexanolone, opium tincture. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • orphenadrine

                brexanolone, orphenadrine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • oxazepam

                brexanolone, oxazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • oxycodone

                brexanolone, oxycodone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • oxymorphone

                brexanolone, oxymorphone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • paliperidone

                brexanolone, paliperidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pentazocine

                brexanolone, pentazocine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pentobarbital

                brexanolone, pentobarbital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • perampanel

                brexanolone, perampanel. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • perphenazine

                brexanolone, perphenazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pheniramine

                brexanolone, pheniramine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • phenobarbital

                brexanolone, phenobarbital. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • phenytoin

                brexanolone, phenytoin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pimavanserin

                brexanolone, pimavanserin. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.

              • pimozide

                brexanolone, pimozide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pomalidomide

                brexanolone, pomalidomide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • pregabalin

                brexanolone, pregabalin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

                pregabalin, brexanolone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • primidone

                brexanolone, primidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • prochlorperazine

                brexanolone, prochlorperazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • promazine

                brexanolone, promazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • promethazine

                brexanolone, promethazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • quazepam

                brexanolone, quazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • quetiapine

                brexanolone, quetiapine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ramelteon

                brexanolone, ramelteon. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • remifentanil

                brexanolone, remifentanil. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • remimazolam

                remimazolam, brexanolone. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.

              • risperidone

                brexanolone, risperidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • scopolamine

                brexanolone, scopolamine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • secobarbital

                brexanolone, secobarbital. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.

              • sevoflurane

                brexanolone, sevoflurane. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • sodium oxybate

                brexanolone, sodium oxybate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • stiripentol

                brexanolone, stiripentol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • sufentanil

                brexanolone, sufentanil. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • sufentanil SL

                brexanolone, sufentanil SL. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • sulpiride

                brexanolone, sulpiride. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • suvorexant

                brexanolone, suvorexant. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • tapentadol

                brexanolone, tapentadol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • tasimelteon

                brexanolone, tasimelteon. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • temazepam

                brexanolone, temazepam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • tetrabenazine

                brexanolone, tetrabenazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • thalidomide

                brexanolone, thalidomide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • thioridazine

                brexanolone, thioridazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • thiothixene

                brexanolone, thiothixene. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • tiagabine

                brexanolone, tiagabine. Either increases levels of the other by sedation. Use Caution/Monitor.

              • tizanidine

                brexanolone, tizanidine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • topiramate

                brexanolone, topiramate. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • tramadol

                brexanolone, tramadol. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • triazolam

                brexanolone, triazolam. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • trifluoperazine

                brexanolone, trifluoperazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • triprolidine

                brexanolone, triprolidine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • valerian

                brexanolone, valerian. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • vigabatrin

                brexanolone, vigabatrin. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • zaleplon

                brexanolone, zaleplon. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ziconotide

                brexanolone, ziconotide. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • ziprasidone

                brexanolone, ziprasidone. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              • zolpidem

                brexanolone, zolpidem. Either increases toxicity of the other by sedation. Use Caution/Monitor.

              Minor (0)

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                Adverse Effects

                >10%

                Sedation, somnolence (13-21%)

                Dizziness, presyncope, vertigo (12-13%)

                Dry mouth (3-11%)

                1-10%

                Loss of consciousness (3-5%)

                Flushing, hot flush (2-5%)

                Tachycardia (3%)

                Diarrhea (2-3%)

                Oropharyngeal pain (2-3%)

                Dyspepsia (2%)

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                Warnings

                Black Box Warnings

                Patients treated with brexanolone are at risk of excessive sedation or sudden loss of consciousness during administration

                Because of the risk of serious harm, monitor patients for excessive sedation and sudden loss of consciousness and have continuous pulse oximetry monitoring

                Patients must be accompanied during interactions with their child(ren)

                Because of these risks, brexanolone is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the Zulresso REMS

                Patient must enroll in REMS before receiving drug; healthcare facilities and pharmacies must be registered and certified in the REMS program

                Contraindications

                None

                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 (eg, 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 ≤24 yr 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, risk of developing suicidal thoughts and behaviors is unknown

                Drug interaction overview

                • Coadministration with CNS depressants (eg, 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
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                Pregnancy

                Pregnancy

                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

                • 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

                Animal studies

                • Malformations were not seen in rats or rabbits at plasma levels up to 5 and 6 times the maximum recommended human dose (MRHD), respectively
                • Developmental toxicities were seen in the fetuses of rats and rabbits at 5 and ≥3 times the plasma levels at the MRHD, respectively
                • Brexanolone administered to pregnant rats during pregnancy and lactation resulted in lower pup survival at doses associated with ≥2 times the plasma levels at the MRHD and a neurobehavioral deficit in female offspring at 5 times the plasma levels at the MRHD

                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 from the underlying maternal condition

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Mechanism of action for the treatment of PPD is not fully understood

                It is believed to be related to positive allosteric modulation of both synaptic and extrasynaptic GABA-A receptors

                Absorption

                Plasma concentration (mean steady-state)

                • 52 ng/mL (at 60 mcg/kg/hr)
                • 79 ng/mL (at 90 mcg/kg/hr)

                Distribution

                Vd: 3 L/kg

                Protein bound: >99%

                Metabolism

                Extensively metabolized by non-CYP based pathways via keto-reduction (AKRs), glucuronidation (UGTs), and sulfation (SULTs)

                3 major circulating metabolites are pharmacologically inactive

                Elimination

                Half-life: ~9 hr

                Total plasma clearance: ~1 L/hr/kg

                Excretion: 47% feces (primarily as metabolites); 42% urine (<1% unchanged)

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                Administration

                IV Preparation

                Supplied in vials as a concentrated solution that requires dilution prior to administration

                After dilution, product can be stored in infusion bags under refrigerated conditions for up to 96 hr; however, the diluted product can be used for only 12 hr at room temperature

                Each 60-hr infusion requires preparing at least 5 infusion bags (additional bags needed if weight ≥90 kg

                Visually inspect vials for particulate matter and discoloration; solution should appear clear and colorless; do not use if discolored or particulate matter observed

                For each infusion bag

                • Prepare and store only in polyolefin, non-DEHP, and nonlatex bag
                • Dilute drug in the infusion bag immediately after the initial puncture of the vial
                • Withdraw 20 mL (100 mg) from the vial and place in the infusion bag, and then dilute with sterile water for injection 40 mL, and then further dilute with 0.9% NaCl 40 mL (total volume of 100 mL) to achieve a target concentration of 1 mg/mL
                • Immediately refrigerate infusion bag until use

                IV Administration

                Brexanolone is available only through a restricted program that requires the drug be administered by a health-care provider in a certified healthcare facility to provide constant monitoring and provide necessary intervention if needed

                Patient must have continuous pulse oximetry with an alarm and be monitored q2hr during planned nonsleep periods

                Infuse by continuous IV infusion using a programmable peristaltic infusion pump to ensure accurate infusion rate

                Administer via a dedicated IV line; do not inject other medications into the infusion bag or mix with brexanolone

                Fully prime infusion administration sets with admixture before inserting into the pump and connecting the venous catheter

                Use a PVC, non-DEHP, nonlatex infusion set; do not use in-line filter infusion sets

                Storage

                Unopened vial: Store at 2-8°C (36-46°F); do not freeze and protect from light

                Diluted solution in infusion bag: Store room temperature for up to 12 hr or refrigerate for up to 96 hr

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.