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Rexulti
brexpiprazole
Black Box Warnings .
Dementia-Related Psychosis
not approved for dementia-related psychosis without agitation associated with dementia due to Alzheimer disease; incr. mortality risk in elderly patients on antipsychotic tx for dementia-related psychosis; most deaths due to cardiovascular or infectious events
Suicidality
incr. suicidality risk in peds and young adult patients in short-term studies; observe all antidepressant-treated patients for clinical worsening, suicidality, or unusual behavior changes; advise families and caregivers of need for close observation and communication with prescriber; not approved for depression in peds patients
Adult Dosing .
Dosage forms: TAB: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
major depressive disorder, adjunct tx
- [2 mg PO qd]
- Start: 0.5-1 mg PO qd, may incr. dose qwk; Max: 3 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
schizophrenia
- [2-4 mg PO qd]
- Start: 1 mg PO qd x4 days, then 2 mg PO qd x3 days, then may incr. to 4 mg PO qd; Max: 4 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
dementia-associated agitation, patients with Alzheimer disease
- [2 mg PO qd]
- Start: 0.5 mg PO qd x7 days, then 1 mg PO qd x7 days, then 2 mg PO qd, then may incr. to 3 mg PO qd after at least 14 days; Max: 3 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
renal dosing
- [schizophrenia]
- CrCl <60: max 3 mg/day
- HD/PD: not defined
- [all other indications]
- CrCl <60: max 2 mg/day
- HD/PD: not defined
hepatic dosing
- [schizophrenia]
- Child-Pugh Class B or C: max 3 mg/day
- [all other indications]
- Child-Pugh Class B or C: max 2 mg/day
Peds Dosing .
- Dosage forms: TAB: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
schizophrenia
- [13-17 yo]
- Dose: 2-4 mg PO qd; Start: 0.5 mg PO qd x4 days, then 1 mg PO qd x3 days, then may incr. to 2 mg PO qd, then may incr. by 1 mg/day qwk; Max: 4 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
renal dosing
- [adjust dose amount]
- CrCl <60: max 3 mg/day
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B or C: max 3 mg/day
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- caution: cardiovascular disease
- caution: MI history
- caution: ischemic heart disease
- caution: heart failure
- caution: hypovolemia
- caution: dehydration
- caution: hypotension, orthostatic
- caution: hepatic impairment, moderate-severe
- caution: CrCl <60
- caution: aspiration pneumonia risk
- caution: elderly patients
- caution: cerebrovascular disease
- caution: psychosis, dementia-associated
- caution: seizure history
- caution: seizure threshold, lowered
- caution: CYP2D6 poor metabolizers
- caution: diabetes mellitus
- caution: diabetes mellitus risk
- caution: environmental temperature, high
- caution: patients <25 yo (depression use)
- caution: leukopenia history, drug-induced
- caution: neutropenia history, drug-induced
- caution: leukopenia
- caution: neutropenia
Drug Interactions .
Overview
brexpiprazole
atypical antipsychotic
- CYP2D6 substrate
- CYP3A4 substrate
- CNS depression
- decreases central histamine effects
- extrapyramidal effects
- hyperglycemic effects
- hyperthermia
- hypotensive effects
- lowers seizure threshold
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- neuroleptic malignant syndrome
- extrapyramidal symptoms, severe
- tardive dyskinesia
- dystonia
- stroke
- TIA
- syncope
- hypotension, orthostatic
- seizures
- hyperglycemia
- diabetes mellitus
- dysphagia, severe
- aspiration
- hyperthermia
- leukopenia
- neutropenia
- agranulocytosis
- suicidality
- depression exacerbation
Common Reactions
- weight gain
- hyperglycemia
- dyslipidemia
- akathisia
- extrapyramidal symptoms
- somnolence
- weight loss
- restlessness
- tremor
- nasopharyngitis
- nausea
- dizziness
- insomnia
- anxiety
- headache
- appetite incr.
- impaired body temperature regulation
- fatigue
- dyspepsia
- diarrhea
- constipation
- cortisol decr.
- CPK incr.
- sedation
- compulsive behaviors
- hyperprolactinemia
Safety/Monitoring .
Monitoring Parameters
fasting glucose, lipid profile at baseline, then periodically; CBC with diff frequently during initial tx if pre-existing or history of leukopenia/neutropenia; weight; BP, HR in patients with orthostatic hypotension risk; symptoms of suicidality, clinical worsening, and/or unusual behavior changes, especially during initial tx or after dose changes
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy, especially in 3rd trimester; no human data available, though risk of neonatal extrapyramidal and withdrawal symptoms based on human data with other antipsychotics; no known risk of fetal harm based on animal data at up to 73x and 146x MRHD
Pregnancy Registry
encourage patients to enroll in National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or www.womensmentalhealth.org
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for brexpiprazole: liver; CYP450: 2D6, 3A4 substrate; Info: CYP2D6 poor metabolizers have 4.8 fold increased active drug exposure
Excretion: for brexpiprazole: feces 46% (14% unchanged), urine 25% (<1% unchanged); Half-life: 91h
Subclass: Antipsychotics, 2nd generation
Mechanism of Action
for brexpiprazole: exact mechanism of action unknown; partially agonizes dopamine D2 and serotonin 5-HT1A receptors, antagonizes serotonin 5-HT2A receptors
Formulary .
No Formulary Selected
Manufacturer/Pricing .
Manufacturer: Otsuka America Pharmaceuticals, Inc.
DEA/FDA: Rx
Retail Price
Estimated prices only. For current pricing, visit GoodRx.
oral tablet:
- 0.25 mg (30 ea): $1,281.00
- 0.5 mg (30 ea): $1,281.00
- 1 mg (30 ea): $1,281.00
- 2 mg (30 ea): $1,281.00
- 3 mg (30 ea): $1,281.00
- 4 mg (30 ea): $1,281.00
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