Brexpiprazole
REXULTI
What it isDopamine D2 partial agonist; schizophrenia, adjunctive depression and agitation in Alzheimer dementia.
Why this oneLess akathisia than aripiprazole at equivalent efficacy, and it is the only agent approved for agitation in Alzheimer dementia.
What limits itWeight gain is greater than aripiprazole. CYP2D6 and CYP3A4 dependent; akathisia and restlessness remain.
FDA-approved for
- schizophrenia (2015)
- adjunct for depression (2015)
- agitation in Alzheimer dementia (2023)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Major depressive disorder (adjunctive to antidepressant) | Adults | 0.5–1 mg QD | 2 mg QD | 3 mg QD |
| Schizophrenia | Adults | 1 mg QD | 2–4 mg QD | 4 mg QD |
| Schizophrenia | Adolescents 13–17 yr | 0.5 mg QD | 2–4 mg QD | 4 mg QD |
| Agitation associated with Alzheimer's dementia | Adults | 0.5 mg QD | 2 mg QD | 3 mg QD |
Titration Increase dosage at weekly intervals
Renal CrCl <60 mL/min: max 2 mg QD (MDD or agitation) or 3 mg QD (schizophrenia)
Hepatic Moderate-to-severe impairment (Child-Pugh ≥7): max 2 mg QD (MDD or agitation) or 3 mg QD (schizophrenia)
Instructions
- Take once daily with or without food
- Adjust dose for CYP2D6 poor metabolizers and with CYP inhibitors/inducers
Cautions
- Cerebrovascular reactions in elderly with dementia (stroke, TIA)
- Neuroleptic malignant syndrome
- Tardive dyskinesia
- Metabolic changes (hyperglycemia/diabetes, dyslipidemia, weight gain)
- Pathological gambling and other compulsive behaviors
- Leukopenia, neutropenia, agranulocytosis
- Orthostatic hypotension and syncope
- Seizures
- Body temperature dysregulation
- Dysphagia
- Cognitive and motor impairment
Adverse reactions
- Weight increased
- Akathisia
- Somnolence
- Extrapyramidal symptoms (adolescents)
Pregnancy No adequate studies; third-trimester exposure risks extrapyramidal/withdrawal symptoms in neonates; pregnancy registry available
Lactation Present in rat milk; human data lacking; weigh benefits against maternal need
⚠ BOXED WARNINGS
- Increased mortality in elderly patients with dementia-related psychosis
- Suicidal thoughts and behaviors in patients under 25
Cost, est. cash$300–$2,500/month
Generic entry2029 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.
Mechanism of action: Brexpiprazole ballicule
Open Brexpiprazole in the interactive console ↗
Memory aids: mascots and interaction avatars
Polka dots on pink → α1 blocker → syncope if titrated too quickly (hit the floor)
