brexpiprazole (Rx)

Brand and Other Names:Rexulti

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 0.25mg
  • 0.5mg
  • 1mg
  • 2mg
  • 3mg
  • 4mg

Schizophrenia

Indicated for treatment of schizophrenia

Days 1-4: 1 mg PO qDay

Day 5-7: Titrate to 2 mg qDay

Day 8: Titrate to 4 mg/day based on the patient’s clinical response and tolerability

Target dose: 2-4 mg PO qDay; not to exceed 4 mg/day

Periodically reassess to determine the continued need and appropriate dose

Depression

Indicated an adjunctive therapy to antidepressants for major depressive disorder (MDD)

0.5 mg or 1 mg PO qDay initially

Titrate according to clinical response and tolerability in weekly intervals to 1 mg/day and then up to 2 mg/day; not to exceed 3 mg/day

Periodically reassess to determine the continued need and appropriate dose

Agitation Associated With Alzheimer Dementia

Indicated for agitation associated with dementia due to Alzheimer disease

Days 1-7: 0.5 mg PO qDay

Days 8-14: Increase to 1 mg PO qDay

Days 15: Increase to 2 mg PO qDay

Target dose: 2 mg PO qDay

May increase to maximum recommended dosage of 3 mg qDay after at least 14 days, based on clinical response and tolerability

Dosage Modifications

Renal impairment

  • Moderate, severe, or end-stage renal disease (ESRD) (CrCl <60 mL/min)
    • MDD or agitation associated with Alzheimer dementia: Not to exceed 2 mg/day
    • Schizophrenia: Not to exceed 3 mg/day

Hepatic impairment

  • Moderate-to-severe hepatic impairment (Child-Pugh ≥7)
    • MDD or agitation associated with Alzheimer dementia: Not to exceed 2 mg/day
    • Schizophrenia: Not to exceed 3 mg/day

CYP2D6 poor metabolizers

  • CYP2D6 poor metabolizers: Administer half of the usual brexpiprazole dose
  • Known CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitors: Administer a quarter of the usual brexpiprazole dose

CYP2D6 or CYP3A4 inhibitors

  • Strong CYP2D6 inhibitors: Administer half of the usual brexpiprazole dose (see note below for MDD)
  • Strong CYP3A4 inhibitors: Administer half of the usual brexpiprazole dose
  • Strong/moderate CYP2D6 inhibitors plus strong/moderate CYP3A4 inhibitors: Administer a quarter of the usual brexpiprazole dose
  • If the coadministered drug is discontinued, adjust the brexpiprazole dosage to its original level
  • NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD

CYP3A4 inducers

  • Strong CYP3A4 inducers: Double usual dose over 1 to 2 weeks
  • If the coadministered CYP3A4 inducer is discontinued, reduce the brexpiprazole dosage to the original level over 1-2 weeks

Geriatric Dosage & Uses

Antipsychotic drugs increase the risk of death in elderly patients with dementia-related psychosis

Brexpiprazole is not approved for the treatment of patients with dementia-related psychosis (see Black Box Warnings)

Limitations of use: Not indicated as an as needed (PRN) treatment for agitation associated with dementia due to Alzheimer disease

Dosage Forms & Strengths

tablet

  • 0.25mg
  • 0.5mg
  • 1mg
  • 2mg
  • 3mg
  • 4mg

Schizophrenia

Indicated for treatment of schizophrenia in adults and pediatric patients aged ≥13 years

<13 years: Safety and efficacy not established

13-17 years

  • Days 1-4: 0.5 mg PO qDay
  • Days 5-7: Titrate to 1 mg PO qDay
  • Day 8: 2 mg PO qDay based on clinical response and tolerability
  • Target dose: 2-4 mg PO qDay; weekly 1-mg dose increments can be made, not to exceed 4 mg/day
  • Periodically reassess to determine continued need and appropriate dose

Dosage Modifications

Renal impairment

  • Moderate, severe, or end-stage renal disease (ESRD) (CrCl <60 mL/min)
  • MDD: Not to exceed 2 mg/day
  • Schizophrenia: Not to exceed 3 mg/day

Hepatic impairment

  • Moderate-to-severe hepatic impairment (Child-Pugh ≥7) H5
  • MDD: Not to exceed 2 mg/day
  • Schizophrenia: Not to exceed 3 mg/day

CYP2D6 poor metabolizers

  • CYP2D6 poor metabolizers: Administer half of the usual brexpiprazole dose
  • CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitors: Administer a quarter of the usual brexpiprazole dose

CYP2D6 or CYP3A4 inhibitors

  • Strong CYP2D6 inhibitors: Administer half of the usual brexpiprazole dose
  • Strong CYP3A4 inhibitors: Administer half of the usual brexpiprazole dose
  • Strong/moderate CYP2D6 inhibitors plus strong/moderate CYP3A4 inhibitors: Administer a quarter of the usual brexpiprazole dose
  • If the coadministered drug is discontinued, adjust the brexpiprazole dosage to its original level
  • NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD

CYP3A4 inducers

  • Strong CYP3A4 inducers: Double usual dose over 1-2 weeks
  • If coadministered CYP3A4 inducer is discontinued, reduce brexpiprazole dosage to the original level over 1-2 weeks

Antipsychotic drugs increase the risk of death in elderly patients with dementia-related psychosis

Brexpiprazole is not approved for the treatment of patients with dementia-related psychosis

Next:

Interactions

Interaction Checker

and brexpiprazole

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            Contraindicated (2)

            • amisulpride

              amisulpride, brexpiprazole. Either increases toxicity of the other by Other (see comment). Contraindicated. Comment: Increases risk of neuroleptic malignant syndrome.

            • thalidomide

              brexpiprazole and thalidomide both increase sedation. Contraindicated.

            Serious - Use Alternative (34)

            • alfentanil

              brexpiprazole and alfentanil both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • apalutamide

              apalutamide will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • benzhydrocodone/acetaminophen

              benzhydrocodone/acetaminophen and brexpiprazole both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • buprenorphine

              brexpiprazole and buprenorphine both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • buprenorphine buccal

              brexpiprazole and buprenorphine buccal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • buprenorphine subdermal implant

              brexpiprazole and buprenorphine subdermal implant both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

              buprenorphine subdermal implant and brexpiprazole both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • buprenorphine transdermal

              brexpiprazole and buprenorphine transdermal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • buprenorphine, long-acting injection

              brexpiprazole and buprenorphine, long-acting injection both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • butalbital

              brexpiprazole and butalbital both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • chloramphenicol

              chloramphenicol will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dacomitinib

              dacomitinib will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Avoid use with CYP2D6 substrates where minimal increases in concentration of the CYP2D6 substrate may lead to serious or life-threatening toxicities.

            • fentanyl

              brexpiprazole and fentanyl both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • fentanyl intranasal

              brexpiprazole and fentanyl intranasal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

              fentanyl intranasal and brexpiprazole both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • fentanyl iontophoretic transdermal system

              brexpiprazole and fentanyl iontophoretic transdermal system both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • fentanyl transdermal

              brexpiprazole and fentanyl transdermal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • fentanyl transmucosal

              brexpiprazole and fentanyl transmucosal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • fexinidazole

              fexinidazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • givosiran

              givosiran will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP2D6 substrates with givosiran. If unavoidable, decrease the CYP2D6 substrate dosage in accordance with approved product labeling.

            • hydrocodone

              brexpiprazole and hydrocodone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • hydromorphone

              brexpiprazole and hydromorphone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • ivosidenib

              ivosidenib will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • lonafarnib

              lonafarnib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

            • methadone

              brexpiprazole and methadone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • metoclopramide intranasal

              brexpiprazole, 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.

            • morphine

              brexpiprazole and morphine both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • nelfinavir

              nelfinavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • olopatadine intranasal

              brexpiprazole and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.

            • oxycodone

              brexpiprazole and oxycodone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • oxymorphone

              brexpiprazole and oxymorphone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • remifentanil

              brexpiprazole and remifentanil both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate

            • secobarbital

              secobarbital will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • selinexor

              selinexor, brexpiprazole. 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.

            • tucatinib

              tucatinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • voxelotor

              voxelotor will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (271)

            • acetaminophen/phenyltoloxamine

              brexpiprazole and acetaminophen/phenyltoloxamine both increase sedation. Use Caution/Monitor.

            • acrivastine

              acrivastine and brexpiprazole both increase sedation. Use Caution/Monitor.

            • alprazolam

              brexpiprazole and alprazolam both increase sedation. Use Caution/Monitor.

            • amifostine

              amifostine, brexpiprazole. Either increases effects of the other by anti-hypertensive channel blocking. Use Caution/Monitor. Monitor blood pressure and adjust dose accordingly.

            • amiodarone

              amiodarone will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              amiodarone will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • amisulpride

              amisulpride and brexpiprazole both increase sedation. Use Caution/Monitor.

            • amitriptyline

              brexpiprazole and amitriptyline both increase sedation. Use Caution/Monitor.

            • amobarbital

              amobarbital will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              brexpiprazole and amobarbital both increase sedation. Use Caution/Monitor.

            • amoxapine

              brexpiprazole and amoxapine both increase sedation. Use Caution/Monitor.

            • aprepitant

              aprepitant will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • aripiprazole

              brexpiprazole and aripiprazole both increase sedation. Use Caution/Monitor.

            • asenapine

              asenapine and brexpiprazole both increase sedation. Use Caution/Monitor.

            • asenapine transdermal

              asenapine transdermal and brexpiprazole both increase sedation. Use Caution/Monitor.

            • atazanavir

              atazanavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • avapritinib

              avapritinib and brexpiprazole both increase sedation. Use Caution/Monitor.

            • baclofen

              brexpiprazole and baclofen both increase sedation. Use Caution/Monitor.

            • belzutifan

              belzutifan will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • benazepril

              brexpiprazole increases toxicity of benazepril by pharmacodynamic synergism. Use Caution/Monitor. Increases risk of hypotension.

            • bicalutamide

              bicalutamide will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • bortezomib

              bortezomib will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • bosentan

              bosentan will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • brexanolone

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

            • brimonidine

              brexpiprazole and brimonidine both increase sedation. Use Caution/Monitor.

              brimonidine and brexpiprazole both increase sedation. Use Caution/Monitor.

            • brivaracetam

              brexpiprazole and brivaracetam both increase sedation. Use Caution/Monitor.

            • brompheniramine

              brexpiprazole and brompheniramine both increase sedation. Use Caution/Monitor.

            • bupropion

              bupropion will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • butabarbital

              brexpiprazole and butabarbital both increase sedation. Use Caution/Monitor.

            • butorphanol

              brexpiprazole and butorphanol both increase sedation. Use Caution/Monitor.

            • captopril

              brexpiprazole, captopril. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Both drugs lower blood pressure. Monitor blood pressure.

            • carbamazepine

              carbamazepine will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • carbinoxamine

              brexpiprazole and carbinoxamine both increase sedation. Use Caution/Monitor.

            • cariprazine

              brexpiprazole and cariprazine both increase sedation. Use Caution/Monitor.

            • carisoprodol

              brexpiprazole and carisoprodol both increase sedation. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

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

            • ceritinib

              ceritinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • cetirizine

              brexpiprazole and cetirizine both increase sedation. Use Caution/Monitor.

            • chlordiazepoxide

              brexpiprazole and chlordiazepoxide both increase sedation. Use Caution/Monitor.

            • chloroquine

              chloroquine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • chlorpheniramine

              brexpiprazole and chlorpheniramine both increase sedation. Use Caution/Monitor.

            • chlorpromazine

              chlorpromazine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

              brexpiprazole and chlorpromazine both increase sedation. Use Caution/Monitor.

            • chlorzoxazone

              brexpiprazole and chlorzoxazone both increase sedation. Use Caution/Monitor.

            • cimetidine

              cimetidine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              cimetidine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • cinacalcet

              cinacalcet will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • clarithromycin

              clarithromycin will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • clemastine

              brexpiprazole and clemastine both increase sedation. Use Caution/Monitor.

            • clobazam

              clobazam will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and clobazam both increase sedation. Use Caution/Monitor.

            • clomipramine

              clomipramine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and clomipramine both increase sedation. Use Caution/Monitor.

            • clonazepam

              brexpiprazole and clonazepam both increase sedation. Use Caution/Monitor.

            • clonidine

              brexpiprazole and clonidine both increase sedation. Use Caution/Monitor.

            • clorazepate

              brexpiprazole and clorazepate both increase sedation. Use Caution/Monitor.

            • clozapine

              clozapine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and clozapine both increase sedation. Use Caution/Monitor.

            • cobicistat

              cobicistat will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              cobicistat will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • cocaine topical

              cocaine topical will decrease the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • codeine

              brexpiprazole and codeine both increase sedation. Use Caution/Monitor.

            • conivaptan

              conivaptan will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • crizotinib

              crizotinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • cyclobenzaprine

              brexpiprazole and cyclobenzaprine both increase sedation. Use Caution/Monitor.

            • cyclosporine

              cyclosporine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • cyproheptadine

              brexpiprazole and cyproheptadine both increase sedation. Use Caution/Monitor.

            • dabrafenib

              dabrafenib will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • dantrolene

              brexpiprazole and dantrolene both increase sedation. Use Caution/Monitor.

            • daridorexant

              brexpiprazole 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.

            • darifenacin

              darifenacin will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • darunavir

              darunavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • desflurane

              brexpiprazole and desflurane both increase sedation. Use Caution/Monitor.

            • desipramine

              desipramine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and desipramine both increase sedation. Use Caution/Monitor.

            • deutetrabenazine

              brexpiprazole and deutetrabenazine both increase sedation. Use Caution/Monitor.

            • dexamethasone

              dexamethasone will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • dexbrompheniramine

              brexpiprazole and dexbrompheniramine both increase sedation. Use Caution/Monitor.

            • dexchlorpheniramine

              brexpiprazole and dexchlorpheniramine both increase sedation. Use Caution/Monitor.

            • dexmedetomidine

              dexmedetomidine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • diazepam

              brexpiprazole and diazepam both increase sedation. Use Caution/Monitor.

            • diazepam intranasal

              diazepam intranasal, brexpiprazole. 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 brexpiprazole both increase sedation. Use Caution/Monitor.

            • difenoxin hcl

              brexpiprazole and difenoxin hcl both increase sedation. Use Caution/Monitor.

            • diltiazem

              diltiazem will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • dimenhydrinate

              brexpiprazole and dimenhydrinate both increase sedation. Use Caution/Monitor.

            • diphenhydramine

              diphenhydramine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and diphenhydramine both increase sedation. Use Caution/Monitor.

            • diphenoxylate hcl

              brexpiprazole and diphenoxylate hcl both increase sedation. Use Caution/Monitor.

            • disulfiram

              disulfiram will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • doxepin

              brexpiprazole and doxepin both increase sedation. Use Caution/Monitor.

            • doxycycline

              doxycycline will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • doxylamine

              brexpiprazole and doxylamine both increase sedation. Use Caution/Monitor.

            • dronedarone

              dronedarone will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              dronedarone will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • droperidol

              brexpiprazole and droperidol both increase sedation. Use Caution/Monitor.

            • duloxetine

              duloxetine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • duvelisib

              duvelisib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of

            • efavirenz

              efavirenz will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

              brexpiprazole and efavirenz both increase sedation. Use Caution/Monitor.

            • elagolix

              elagolix will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • eliglustat

              eliglustat will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • encorafenib

              encorafenib, brexpiprazole. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • entacapone

              brexpiprazole and entacapone both increase sedation. Use Caution/Monitor.

            • enzalutamide

              enzalutamide will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • erythromycin base

              erythromycin base will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • esketamine intranasal

              esketamine intranasal, brexpiprazole. Either increases levels of the other by sedation. Modify Therapy/Monitor Closely.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • estazolam

              brexpiprazole and estazolam both increase sedation. Use Caution/Monitor.

            • eszopiclone

              brexpiprazole and eszopiclone both increase sedation. Use Caution/Monitor.

            • ethanol

              brexpiprazole and ethanol both increase sedation. Use Caution/Monitor.

            • ethosuximide

              brexpiprazole and ethosuximide both increase sedation. Use Caution/Monitor.

            • ethotoin

              brexpiprazole and ethotoin both increase sedation. Use Caution/Monitor.

            • etravirine

              etravirine will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • fedratinib

              fedratinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

              fedratinib will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2D6 substrates as necessary.

            • felbamate

              brexpiprazole and felbamate both increase sedation. Use Caution/Monitor.

            • fenfluramine

              brexpiprazole and fenfluramine both increase sedation. Use Caution/Monitor.

            • fexofenadine

              brexpiprazole and fexofenadine both increase sedation. Use Caution/Monitor.

            • flibanserin

              brexpiprazole and flibanserin both increase sedation. Use Caution/Monitor.

            • fluconazole

              fluconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • fluoxetine

              fluoxetine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • fluphenazine

              brexpiprazole and fluphenazine both increase sedation. Use Caution/Monitor.

            • flurazepam

              brexpiprazole and flurazepam both increase sedation. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • fosaprepitant

              fosaprepitant will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • gabapentin

              gabapentin, brexpiprazole. 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.

              brexpiprazole and gabapentin both increase sedation. Use Caution/Monitor.

            • gabapentin enacarbil

              gabapentin enacarbil, brexpiprazole. 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

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

            • grapefruit

              grapefruit will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • guanfacine

              brexpiprazole and guanfacine both increase sedation. Use Caution/Monitor.

            • haloperidol

              haloperidol will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              haloperidol will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

              brexpiprazole and haloperidol both increase sedation. Use Caution/Monitor.

            • hydroxyzine

              brexpiprazole and hydroxyzine both increase sedation. Use Caution/Monitor.

            • idelalisib

              idelalisib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • iloperidone

              iloperidone will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

              brexpiprazole and iloperidone both increase sedation. Use Caution/Monitor.

            • imatinib

              imatinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              imatinib will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • imipramine

              imipramine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and imipramine both increase sedation. Use Caution/Monitor.

            • indinavir

              indinavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • isoflurane

              brexpiprazole and isoflurane both increase sedation. Use Caution/Monitor.

            • isoniazid

              isoniazid will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              isoniazid will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • istradefylline

              istradefylline will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • itraconazole

              itraconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • ketamine

              brexpiprazole and ketamine both increase sedation. Use Caution/Monitor.

            • ketoconazole

              ketoconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              ketoconazole will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • ketotifen, drug-eluting contact lens

              brexpiprazole and ketotifen, drug-eluting contact lens both increase sedation. Use Caution/Monitor.

            • lamotrigine

              brexpiprazole and lamotrigine both increase sedation. Use Caution/Monitor.

            • lapatinib

              lapatinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • lasmiditan

              lasmiditan, brexpiprazole. 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, brexpiprazole. 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.

            • lenacapavir

              lenacapavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

            • levetiracetam

              brexpiprazole and levetiracetam both increase sedation. Use Caution/Monitor.

            • levocetirizine

              brexpiprazole and levocetirizine both increase sedation. Use Caution/Monitor.

            • levoketoconazole

              levoketoconazole will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              levoketoconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • levorphanol

              brexpiprazole and levorphanol both increase sedation. Use Caution/Monitor.

            • lidocaine

              lidocaine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              lidocaine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • lopinavir

              lopinavir will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

              lopinavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • loratadine

              brexpiprazole and loratadine both increase sedation. Use Caution/Monitor.

            • lorazepam

              brexpiprazole and lorazepam both increase sedation. Use Caution/Monitor.

            • lorcaserin

              lorcaserin will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • lorlatinib

              lorlatinib will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • loxapine

              brexpiprazole and loxapine both increase sedation. Use Caution/Monitor.

            • lumacaftor/ivacaftor

              lumacaftor/ivacaftor will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • lumateperone

              brexpiprazole and lumateperone both increase sedation. Use Caution/Monitor.

            • lurasidone

              brexpiprazole and lurasidone both increase sedation. Use Caution/Monitor.

            • maprotiline

              brexpiprazole and maprotiline both increase sedation. Use Caution/Monitor.

            • meclizine

              brexpiprazole and meclizine both increase sedation. Use Caution/Monitor.

            • meperidine

              brexpiprazole and meperidine both increase sedation. Use Caution/Monitor.

            • meprobamate

              brexpiprazole and meprobamate both increase sedation. Use Caution/Monitor.

            • metaxalone

              brexpiprazole and metaxalone both increase sedation. Use Caution/Monitor.

            • metformin

              brexpiprazole decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.

            • methadone

              methadone will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • methimazole

              methimazole will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • methocarbamol

              brexpiprazole and methocarbamol both increase sedation. Use Caution/Monitor.

            • methohexital

              brexpiprazole and methohexital both increase sedation. Use Caution/Monitor.

            • methsuximide

              brexpiprazole and methsuximide both increase sedation. Use Caution/Monitor.

            • metronidazole

              metronidazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • midazolam

              brexpiprazole and midazolam both increase sedation. Use Caution/Monitor.

            • midazolam intranasal

              midazolam intranasal, brexpiprazole. 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.

            • mifepristone

              mifepristone will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mirtazapine

              brexpiprazole and mirtazapine both increase sedation. Use Caution/Monitor.

            • mitotane

              mitotane will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • molindone

              brexpiprazole and molindone both increase sedation. Use Caution/Monitor.

            • nafcillin

              nafcillin will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • nalbuphine

              brexpiprazole and nalbuphine both increase sedation. Use Caution/Monitor.

            • nefazodone

              nefazodone will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              nefazodone will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • netupitant/palonosetron

              netupitant/palonosetron will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • nevirapine

              nevirapine will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • nicardipine

              nicardipine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

              nicardipine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • nitrous oxide

              brexpiprazole and nitrous oxide both increase sedation. Use Caution/Monitor.

            • nortriptyline

              brexpiprazole and nortriptyline both increase sedation. Use Caution/Monitor.

            • olanzapine

              brexpiprazole and olanzapine both increase sedation. Use Caution/Monitor.

            • oliceridine

              brexpiprazole and oliceridine both increase sedation. Use Caution/Monitor.

            • ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)

              ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

              ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • opicapone

              brexpiprazole and opicapone both increase sedation. Use Caution/Monitor.

            • opium tincture

              brexpiprazole and opium tincture both increase sedation. Use Caution/Monitor.

            • orphenadrine

              brexpiprazole and orphenadrine both increase sedation. Use Caution/Monitor.

            • oxazepam

              brexpiprazole and oxazepam both increase sedation. Use Caution/Monitor.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • paliperidone

              brexpiprazole and paliperidone both increase sedation. Use Caution/Monitor.

            • panobinostat

              panobinostat will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • paroxetine

              paroxetine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • pentazocine

              brexpiprazole and pentazocine both increase sedation. Use Caution/Monitor.

            • pentobarbital

              pentobarbital will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

              brexpiprazole and pentobarbital both increase sedation. Use Caution/Monitor.

            • perampanel

              brexpiprazole and perampanel both increase sedation. Use Caution/Monitor.

            • perphenazine

              brexpiprazole and perphenazine both increase sedation. Use Caution/Monitor.

            • pheniramine

              brexpiprazole and pheniramine both increase sedation. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

              brexpiprazole and phenobarbital both increase sedation. Use Caution/Monitor.

            • phenytoin

              phenytoin will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • pimozide

              brexpiprazole and pimozide both increase sedation. Use Caution/Monitor.

            • pomalidomide

              brexpiprazole and pomalidomide both increase sedation. Use Caution/Monitor.

            • posaconazole

              posaconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • pregabalin

              pregabalin, brexpiprazole. 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.

              brexpiprazole and pregabalin both increase sedation. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

              brexpiprazole and primidone both increase sedation. Use Caution/Monitor.

            • prochlorperazine

              brexpiprazole and prochlorperazine both increase sedation. Use Caution/Monitor.

            • promethazine

              brexpiprazole and promethazine both increase sedation. Use Caution/Monitor.

            • propofol

              brexpiprazole and propofol both increase sedation. Use Caution/Monitor.

            • protriptyline

              brexpiprazole and protriptyline both increase sedation. Use Caution/Monitor.

            • pyrilamine

              brexpiprazole and pyrilamine both increase sedation. Use Caution/Monitor.

            • pyrimethamine

              pyrimethamine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • quazepam

              brexpiprazole and quazepam both increase sedation. Use Caution/Monitor.

            • quetiapine

              brexpiprazole and quetiapine both increase sedation. Use Caution/Monitor.

            • quinidine

              quinidine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

              quinidine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • quinine

              quinine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • ramelteon

              brexpiprazole and ramelteon both increase sedation. Use Caution/Monitor.

            • ranolazine

              ranolazine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • remimazolam

              brexpiprazole and remimazolam both increase sedation. Use Caution/Monitor.

            • reserpine

              brexpiprazole and reserpine both increase sedation. Use Caution/Monitor.

            • ribociclib

              ribociclib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifabutin

              rifabutin will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • rifampin

              rifampin will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • rifapentine

              rifapentine will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • risperidone

              brexpiprazole and risperidone both increase sedation. Use Caution/Monitor.

            • ritonavir

              ritonavir will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

              ritonavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • rolapitant

              rolapitant will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Rolapitant may increase plasma concentrations of CYP2D6 substrates for at least 28 days following rolapitant administration.

            • rucaparib

              rucaparib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • saquinavir

              saquinavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • schisandra

              schisandra will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • scopolamine

              brexpiprazole and scopolamine both increase sedation. Use Caution/Monitor.

            • sertraline

              sertraline will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              sertraline will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • sevoflurane

              brexpiprazole and sevoflurane both increase sedation. Use Caution/Monitor.

            • sodium oxybate

              brexpiprazole and sodium oxybate both increase sedation. Use Caution/Monitor.

            • St John's Wort

              St John's Wort will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Double brexpiprazole dose over 1-2 weeks if administered with a strong CYP3A4 inducer.

            • stiripentol

              stiripentol, brexpiprazole. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

            • sufentanil

              brexpiprazole and sufentanil both increase sedation. Use Caution/Monitor.

            • sufentanil SL

              brexpiprazole and sufentanil SL both increase sedation. Use Caution/Monitor.

            • suvorexant

              brexpiprazole and suvorexant both increase sedation. Use Caution/Monitor.

            • tapentadol

              brexpiprazole and tapentadol both increase sedation. Use Caution/Monitor.

            • tasimelteon

              brexpiprazole and tasimelteon both increase sedation. Use Caution/Monitor.

            • tazemetostat

              tazemetostat will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • temazepam

              brexpiprazole and temazepam both increase sedation. Use Caution/Monitor.

            • terbinafine

              terbinafine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Assess need to reduce dose of CYP2D6-metabolized drug.

            • tetrabenazine

              brexpiprazole and tetrabenazine both increase sedation. Use Caution/Monitor.

            • tetracycline

              tetracycline will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • thioridazine

              thioridazine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and thioridazine both increase sedation. Use Caution/Monitor.

            • thiothixene

              brexpiprazole and thiothixene both increase sedation. Use Caution/Monitor.

            • tiagabine

              brexpiprazole and tiagabine both increase sedation. Use Caution/Monitor.

            • ticagrelor

              ticagrelor will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • ticlopidine

              ticlopidine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • tipranavir

              tipranavir will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • tizanidine

              brexpiprazole and tizanidine both increase sedation. Use Caution/Monitor.

            • tolcapone

              brexpiprazole and tolcapone both increase sedation. Use Caution/Monitor.

            • topiramate

              brexpiprazole and topiramate both increase sedation. Use Caution/Monitor.

            • tramadol

              brexpiprazole and tramadol both increase sedation. Use Caution/Monitor.

            • tranylcypromine

              tranylcypromine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

            • trazodone

              trazodone will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.

              brexpiprazole and trazodone both increase sedation. Use Caution/Monitor.

            • triazolam

              brexpiprazole and triazolam both increase sedation. Use Caution/Monitor.

            • trifluoperazine

              brexpiprazole and trifluoperazine both increase sedation. Use Caution/Monitor.

            • triprolidine

              brexpiprazole and triprolidine both increase sedation. Use Caution/Monitor.

            • valproic acid

              brexpiprazole and valproic acid both increase sedation. Use Caution/Monitor.

            • verapamil

              verapamil will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • vigabatrin

              brexpiprazole and vigabatrin both increase sedation. Use Caution/Monitor.

            • voriconazole

              voriconazole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP3A4 inhibitors. If also administered with a strong/moderate CYP2D6 inhibitor, administer a quarter of brexpiprazole dose.

            • zaleplon

              brexpiprazole and zaleplon both increase sedation. Use Caution/Monitor.

            • ziconotide

              brexpiprazole and ziconotide both increase sedation. Use Caution/Monitor.

            • zileuton

              zileuton will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.

            • ziprasidone

              brexpiprazole and ziprasidone both increase sedation. Use Caution/Monitor.

            • zolpidem

              brexpiprazole and zolpidem both increase sedation. Use Caution/Monitor.

            • zonisamide

              brexpiprazole and zonisamide both increase sedation. Use Caution/Monitor.

            Minor (4)

            • acetazolamide

              acetazolamide will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • anastrozole

              anastrozole will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • cyclophosphamide

              cyclophosphamide will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • larotrectinib

              larotrectinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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            Adverse Effects

            >10%

            MDD

            • Akathisia (4-14%)

            1-10%

            MDD

            • Headache (4-9%)
            • Increased weight (6-8%)
            • Nasopharyngitis (3-7%)
            • Somnolence (4-6%)
            • Fatigue (3-5%)
            • Tremor (2-5%)
            • Dizziness (1-5%)
            • Blood cortisol decreased (3-4%)
            • Anxiety (2-4%)
            • Restlessness (2-4%)
            • Increased appetite (2-3%)
            • Constipation (1-3%)

            Schizophrenia (adults)

            • Akathisia (4-7%)
            • Dyspepsia (2-6%)
            • Increased weight (3-4%)
            • Blood creatinine phosphokinase increased (3-4%)
            • Tremor (2-3%)
            • Sedation (2-3%)
            • Diarrhea (1-3%)

            Agitation associated with Alzheimer dementia

            • Headache (7-9%)
            • Insomnia (2-5%)
            • Dizziness (1-5%)
            • Nasopharyngitis (2-4%)
            • Somnolence (2-4%)
            • EPS-related adverse reactions (3%)
            • Urinary tract infection (2-3%)
            • Akathisia (1%)

            Frequency Not Defined

            • Eye disorders: Blurred vision
            • Gastrointestinal disorders: Nausea, dry mouth, salivary hypersecretion, abdominal pain, flatulence
            • Infections and infestations: Urinary tract infection
            • Investigations: Blood prolactin increased
            • Musculoskeletal and connective tissue disorders: Myalgia
            • Psychiatric disorders: Abnormal dreams, insomnia
            • Skin and SC tissue disorders: Hyperhidrosis

            Postmarketing Reports

            Neuroleptic malignant syndrome

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            Warnings

            Black Box Warnings

            Increased mortality in elderly patients with dementia-related psychosis

            • Elderly patients with dementia-related psychosis when treated with antipsychotic drugs are at an increased risk of death
            • Not approved for treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer disease

            Suicidal thoughts and behaviors

            • Antidepressants increased the risk of suicidal thoughts and behaviors in patients aged ≤24 years
            • Closely monitor for clinical worsening, and for emergence of suicidal thoughts and behaviors
            • Safety and effectiveness not established in pediatric patients with MDD

            Contraindications

            Hypersensitivity to brexpiprazole or any of its components; reactions have included rash, facial swelling, urticaria, and angioedema

            Cautions

            Increased mortality in elderly patients with dementia-related psychosis; in placebo-controlled trials, majority of patients treated with atypical antipsychotic drugs had a 1.6-1.7x higher risk of death than placebo

            Increased mortality in elderly patients with dementia-related psychosis; in placebo-controlled trials; most of reported deaths were either cardiovascular or infectious in nature

            Higher incidence of stroke and transient ischemic attack, including fatal stroke reported; not approved for treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer’s disease

            Suicidal thoughts and behaviors reported in patients ≤24 years who are taking antidepressant drugs; unknown whether risk of suicidal thoughts and behaviors in children, adolescents, and young adults extends to longer-term use (ie, >4 months)

            May cause leukopenia, neutropenia, and agranulocytosis; monitor and discontinue if severe neutropenia (ANC <1000/mm3); in patients with a pre-existing low WBC or ANC or a history of drug-induced leukopenia or neutropenia, perform a complete blood cell count (CBC) frequently during the first few months of therapy

            Orthostatic hypotension or syncope may occur; the risk is greatest during initial dose titration and when increasing the dose; monitor orthostatic vital signs in patients who are vulnerable to hypotension, (eg, elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medication, patients with known cardiovascular disease, patients with cerebrovascular disease)

            May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; perform complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy

            Caution with a history of seizures or with conditions/drugs that potentially lower the seizure threshold

            May disrupt the body’s ability to reduce core body temperature; use with caution in patients who experience these conditions

            Esophageal dysmotility and aspiration pneumonia reported; use cautiously in patients at risk for aspiration

            Sedation and hypersomnia reported that may cause impaired judgement, thinking, or motor skills; exercise caution if operating hazardous machinery, including motor vehicles, until certain therapy does not adversely affect them

            Postmarketing case reports suggest that patients can experience intense urges, particularly for gambling, and inability to control urges; consider dose reduction or stopping medication if a patient develops such urges

            Neuroleptic malignant syndrome (NMS)

            • Potentially fatal NMS has been associated with antipsychotic drugs administration
            • Clinical manifestations are hyperpyrexia, muscle rigidity, altered mental status, and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis and cardiac dysrhythmia); additional signs may include elevated creatinine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure
            • If NMS is suspected, immediately discontinue therapy, and provide intensive symptomatic treatment and monitoring

            Tardive dyskinesia

            • Tardive dyskinesia reported in patients treated with antipsychotic drugs
            • Incidence highest in elderly persons, especially elderly women
            • Increased duration of treatment and cumulative dose increases may increase risk of tardive dyskinesia and the potential for it to be irreversible
            • Use lowest dose and shortest duration of treatment needed to produce a satisfactory clinical response; periodically reassess the need for continued treatment
            • If signs and symptoms of tardive dyskinesia appear, consider discontinuing therapy
            • Reserve chronic antipsychotic treatment for the following patients
              • Who suffer from chronic illness and is responsive to antipsychotics
              • For whom alternative therapies are not available or appropriate

            Metabolic changes

            • Atypical antipsychotic drugs have been associated with metabolic changes that include hyperglycemia/diabetes mellitus (including extreme cases associated with ketoacidosis or hyperosmolar coma or death), dyslipidemia, and body weight gain
            • Assess fasting plasma glucose, fasting lipid profile, and weight before or soon after initiation of antipsychotic medication, and monitor periodically during long-term treatment

            Drug interaction overview

            • Strong CYP3A4 inhibitors
              • Reduce brexpiprazole dose
              • Strong CYP3A4 inhibitors may increase exposure of brexpiprazole
            • Strong CYP2D6 inhibitors
              • Reduce brexpiprazole dose
              • Strong CY2D6 inhibitors may increase exposure of brexpiprazole
            • Both CYP3A4 and CYP2D6 inhibitors
              • Reduce brexpiprazole dose
              • Drugs that are strong or moderate CYP3A4 and CYP2D6 inhibitors may increase exposure of brexpiprazole
            • Strong CYP3A4 inducers
              • Increase brexpiprazole dose
              • Strong CYP3A4 inducers may decrease exposure of brexpiprazole
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            Pregnancy

            Pregnancy

            Adequate and well-controlled studies have not been conducted with brexpiprazole in pregnant females inform drug-associated risks

            Pregnancy exposure registry

            Clinical considerations

            • Neonates whose mothers are exposed to antipsychotic drugs, like brexpiprazole, during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms (eg, agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder)

            Animal studies

            • No teratogenicity was observed with oral administration to pregnant rats and rabbits during organogenesis at doses up to 73x and 146x, respectively, of maximum recommended human dose (MRHD) of 4 mg/day on a mg/m2 basis
            • However, when pregnant rats were administered brexpiprazole during organogenesis through lactation, the number of perinatal deaths of pups was increased at 73x the MRHD

            Lactation

            Unknown if distributed in human breast milk

            Present in rat milk

            The development 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 infant 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

            Serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency, and an antagonist at 5-HT2A and noradrenaline alpha1B/2C receptors

            Absorption

            Absolute bioavailability: 95%

            Peak plasma time: 4 hr

            Steady-state concentration: 1-12 days

            Distribution

            Protein bound: >99% to serum albumin and alpha-1-acid glycoprotein; its protein binding is not affected by renal or hepatic impairment

            Brexpiprazole protein binding is not affected by warfarin, diazepam, or digitoxin

            Vd: 1.56 L/kg

            Metabolism

            Metabolized primarily by CYP2D6 and CYP3A4 isoenzymes

            Elimination

            Half-life: 91 hr

            Clearance: 19.8 mL·hr/kg

            Excretion: 25% urine; 46% feces

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            Administration

            Oral Administration

            Take with or without food

            Storage

            Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Rexulti oral
            -
            4 mg tablet
            Rexulti oral
            -
            1 mg tablet
            Rexulti oral
            -
            0.5 mg tablet
            Rexulti oral
            -
            3 mg tablet
            Rexulti oral
            -
            2 mg tablet
            Rexulti oral
            -
            0.25 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            brexpiprazole oral

            BREXPIPRAZOLE - ORAL

            (brex-PIP-ra-zole)

            COMMON BRAND NAME(S): Rexulti

            WARNING: There may be a slightly increased risk of serious, possibly fatal side effects (such as stroke, heart failure, fast/irregular heartbeat, pneumonia) when this medication is used by older adults with dementia. This medication is not approved for the treatment of dementia-related behavior problems without agitation that may occur with dementia due to Alzheimer's disease. Discuss the risks and benefits of this medication, as well as other effective and possibly safer treatments for dementia-related behavior problems, with the doctor. See also Uses section.Brexpiprazole is used to treat certain mental/mood disorders (such as schizophrenia, depression). Drugs used to treat depression can help prevent suicidal thoughts/attempts and provide other important benefits. However, studies have shown that a small number of people (especially people younger than 25) who take antidepressants for any condition may experience worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. It is very important to talk with the doctor about the risks and benefits of drugs used to treat depression (especially for people younger than 25), even if treatment is not for a mental/mood condition.Tell the doctor right away if you notice worsening depression/other psychiatric conditions, unusual behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes (including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms when a new drug to treat depression is started or when the dose is changed.

            USES: This medication is used to treat certain mental/mood disorders (such as schizophrenia, depression). Brexpiprazole is also used to treat agitation that may occur with dementia due to Alzheimer's disease. Brexpiprazole belongs to a class of drugs known as atypical antipsychotics. It works by helping to restore the balance of certain natural substances in the brain.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking brexpiprazole and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily. The dosage is based on your medical condition, response to treatment, and other drugs you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Continue taking this medication exactly as prescribed, even if you are feeling better and thinking more clearly. Do not increase your dose or take this drug more often than prescribed. Your symptoms will not improve any faster, and your risk of side effects will increase. Do not stop taking this medication without consulting your doctor.Tell your doctor if you do not get better or if you get worse. It may take several weeks before you feel the full benefit of this medication.

            SIDE EFFECTS: See also Warning section.Drowsiness, dizziness, lightheadedness, shaking, increased appetite, weight gain, restlessness, and inability to keep still may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.This medication may cause a serious drop in blood pressure, especially after starting or increasing your dose of this medication. Dizziness and lightheadedness can increase the risk of falling. Get up slowly when rising from a sitting or lying position.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: trouble swallowing, fainting, interrupted breathing during sleep, unusual strong urges (such as increased gambling, increased sexual urges).Brexpiprazole may rarely cause a condition known as tardive dyskinesia. In some cases, this condition may be permanent. Tell your doctor right away if you develop any unusual/uncontrolled movements (especially of the face, lips, mouth, tongue, arms, or legs).This medication may rarely make your blood sugar rise, which can cause or worsen diabetes. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.This drug may also cause weight gain and a rise in your blood cholesterol (or triglyceride) levels. These effects, along with diabetes, may increase your risk for developing heart disease. Discuss the risks and benefits of treatment with your doctor.Rarely, this medication may increase your blood level of a certain hormone (prolactin). In females, an increase in prolactin levels may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. In males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. If you develop any of these symptoms, tell your doctor right away.Get medical help right away if you have any very serious side effects, including: seizure.This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms: fever, muscle stiffness/pain/tenderness/weakness, severe tiredness, severe confusion, sweating, fast/irregular heartbeat, dark urine, signs of kidney problems (such as change in the amount of urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: See also Warning section.Before taking brexpiprazole, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, liver problems, personal or family history of diabetes, high cholesterol/triglyceride levels, heart problems, seizures, stroke, trouble swallowing, low white blood cell count, breathing trouble during sleep (sleep apnea).This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication may make you sweat less, making you more likely to get heat stroke. Avoid doing things that may cause you to overheat, such as hard work or exercise in hot weather, or using hot tubs. When the weather is hot, drink a lot of fluids and dress lightly. If you overheat, quickly look for a place to cool down and rest. Get medical help right away if you have a fever that does not go away, mental/mood changes, headache, or dizziness.Older adults may be more sensitive to the side effects of this drug, especially drowsiness, dizziness, and lightheadedness. Drowsiness, dizziness, and lightheadedness can increase the risk of falling.During pregnancy, this medication should be used only when clearly needed. Babies born to mothers who have used this drug during the last 3 months of pregnancy may rarely develop symptoms including muscle stiffness or shakiness, drowsiness, feeding/breathing difficulties, or constant crying. If you notice any of these symptoms in your newborn, especially during their first month, tell the doctor right away.Since untreated mental/mood problems (such as schizophrenia, depression) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, talk with your doctor right away about the benefits and risks of using this medication during pregnancy.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: metoclopramide.Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood sugar, blood pressure, kidney/liver function, weight, cholesterol/triglyceride levels) may be done while you are taking this medication. Keep all medical and lab appointments.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised October 2023. Copyright(c) 2023 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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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.