brexpiprazole (Rexulti)
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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
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
Dosage adjustment in renal failure
- maximum dose 2 mg (depression or agitation), 3 mg (schizophrenia)
Pharmacokinetics
- metabolized in the liver mainly by CYP3A4
- protein binding: 99%
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)
- increased mortality in elderly with dementia-related psychosis & suicidal thoughts & behaviors
- drug adverse effects of antipsychotic agents
- drug adverse effects of atypical antipsychotic agents
- drug adverse effects of psychotropic agents
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
- drug interaction(s) of antipsychotics & dopamine receptor agonists
- drug interaction(s) of antipsycotics with benzodiazepines
Mechanism of action
- partial serotonin 5-HT1A receptor agonist & dopamine D2 receptor agonist
- serotonin 5-HT2A receptor agonist
More general terms
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
- ↑ 2.0 2.1 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 - ↑ 3.0 3.1 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: https://www.ncbi.nlm.nih.gov/pubmed/37930669 PMCID: PMC10628834 Free PMC article
- ↑ HIGHLIGHTS OF PRESCRIBING INFORMATION REXULTI <TM> (brexpiprazole) tablets, for oral use https://www.otsuka-us.com/sites/g/files/qhldwo8676/files/media/static/Rexulti-PI.pdf