Search
brexpiprazole (Rxulti)
Indications:
- adults with major depression on antidepressant therapy
- psychosis & agitation in the elderly, including Alzheimer's disease*
- schizophrenia
* improves agitation in Alzheimer' disease vs placebo over 12 weeks [2,3]
Contraindications:
- pregnancy category: C
Dosage:
- start 0.5-1.0 mg/day
- 2-3 mg/day (agitation, major depression)
- 2-4 mg/day (schizophrenia)
- maximum 4 mg/day
Tablets: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
Pharmacokinetics:
- metabolized in the liver mainly by CYP3A4
- protein binding: 99%
Dosage adjustment in renal failure:
- maximum dose 2 mg (depression or agitation), 3 mg (schizophrenia)
Adverse effects:
- discontinuance 5.3% vs 4.3% for placebo
- stroke, TIA (elderly with dementia-related psychosis)
- neuroleptic malignant syndrome
- tardive dyskinesia
- leukopenia, neutropenia, granulocytopenia
- orthostatic hypotension, syncope
- seizures
- weight gain (twice risk of placebo)
* Boxed Warning
- increased mortality in elderly with dementia-related psychosis & suicidal thoughts & behaviors
Drug interactions:
- CYP3A4 inhibitors increase levels of brexpiprazole
- cut brexpiprazole dose in 1/2
- CYP3A4 inducers decrease levels of brexpiprazole
- double brexpiprazole dose
- drugs that lower the seizure threshold
Mechanism of action:
- partial serotonin 5-HT1A receptor agonist & dopamine D2 receptor agonist
- serotonin 5-HT2A receptor agonist
Interactions
drug adverse effects of antipsychotic agents
monitor with atypical antipsychotic agents
General
pyrrole
atypical antipsychotic agent; second generation antipsychotic
Database Correlations
PUBCHEM cid=11978813
References
- FDA News Release. July 13, 2015
FDA approves new drug to treat schizophrenia and as an add on
to an antidepressant to treat major depressive disorder.
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm454647.htm
- Monaco K
Rexulti Calms Alzheimer's Dementia-Related Agitation.
But atypical antipsychotic disappoints in borderline personality disorder.
MedPage Today September 19, 2022
https://www.medpagetoday.com/meetingcoverage/psychcongress/100805
- DePeau-Wilson M
Rexulti Works for Agitation in Alzheimer's, Despite Risks, Says FDA Staff.
Increased mortality risk consistent with other antipsychotics in elderly
dementia patients.
MedPage Today April 13, 2023
https://www.medpagetoday.com/neurology/dementia/104000
- US Food & Drug Administration News Release. May 11, 2023
FDA Approves First Drug to Treat Agitation Symptoms Associated with Dementia
due to Alzheimer's Disease.
https://www.fda.gov/news-events/press
- Lee D, Slomkowski M, Hefting N et al.
Brexpiprazole for the Treatment of Agitation in Alzheimer Dementia:
A Randomized Clinical Trial.
JAMA Neurol. 2023 Nov 6:e233810.
PMID: 37930669 PMCID: PMC10628834 Free PMC article
- HIGHLIGHTS OF PRESCRIBING INFORMATION
REXULTI (brexpiprazole) tablets, for oral use
https://www.otsuka-us.com/sites/g/files/qhldwo8676/files/media/static/Rexulti-PI.pdf