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      For You News & Perspective Drugs & Diseases CME & Education Academy Video Decision Point
      Drugs & Diseases

      brexanolone (Rx)

      Brand and Other Names:Zulresso
      • Print

      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)
      • 52-56 hours: Decrease to 60 mcg/kg/hr
      • 56-60 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

      Dosage Forms & Strengths

      intravenous solution: Schedule IV

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

      Postpartum Depression

      Indicated for treatment of postpartum depression (PPD) in adults and pediatric patients aged ≥15 years

      Administer as a continuous IV infusion over a total of 60 hr (2.5 days) in a monitored health setting that can 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)
      • 52-56 hours: Decrease to 60 mcg/kg/hr
      • 56-60 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

      Next:

      Interactions

      Interaction Checker

      and brexanolone

      No Results

         activity indicator 
        No Interactions Found
        Interactions Found

        Contraindicated

          Serious - Use Alternative

            Significant - Monitor Closely

              Minor

                All Interactions Sort By:
                 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 (172)

                  • 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.

                  • daridorexant

                    brexanolone and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.

                  • 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.

                  • difelikefalin

                    difelikefalin and brexanolone both increase sedation. Use Caution/Monitor.

                  • 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.

                  • ganaxolone

                    brexanolone and ganaxolone both increase sedation. Use Caution/Monitor.

                  • 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

                    Excessive sedation and sudden loss of consciousness

                    • Patients treated with brexanolone are at risk of excessive sedation or sudden loss of consciousness during administration
                    • Owing to the risk of serious harm, monitor for excessive sedation and sudden loss of consciousness and have continuous pulse oximetry monitoring
                    • Patients must be accompanied during interactions with their child(ren)
                    • 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.

                    Create Your List of Plans

                    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.

                    View explanations for tiers and restrictions
                    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.
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