Brexpiprazole ($ Rexulti)
Second generation antipsychotic (Low dose: dopamine-D3 serotonin partial agonist and antagonist; Upper dose: dopamine, serotonin receptor partial agonist (D2, 5-HT1A) receptor antagonist (5-HT2A))
- Treatment resistant depression3
- Low risk akathisia
- Aggression in Alzheimer’s dementia2
- PTSD3 (augmentation of sertraline)
- Schizophrenia3 (10+)
- Ineffective: mania
Features
Dosing
Antidepressant augmentation (1mg 1/2 qd x7days, 1 qd x7days then 2 qd).
Management
Raise by 1.5-2x if using with carbamazepine. Lower to 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.
Similar to aripiprazole but less akathisia. Does not work in mania.
Although approved for agitation in Alzheimer’s, antipsychotics are dangerous in Lew’s Body dementia and worsen Parkinson’s disease.
TOLERABILITY: Weight gain, sedation, akathisia, EPS (dystonia, stiffness), anticholinergic.
RISKS: Tardive dyskinesia (25% over 10 years, higher in elderly), metabolic, prolactinemia (can lead to breast cancer, osteopenia, sexual dysfunction), orthostasis (falls), QTc prolongation, temperature imbalance in elderly, NMS (muscle rigidity, fever, tachycardia).
EMR Text
Depression
Brexpiprazole use based on FDA approval in major depression (as antidepressant augmentation)
Antipsychotic side effects, including metabolic, prolactinemia, and TD, reviewed with patient.
PTSD
Brexpiprazole use based on large controlled trials as augmentation in PTSD.
Antipsychotic side effects, including metabolic, prolactinemia, and TD, reviewed with patient.
Schizophrenia
Brexpiprazole use based on FDA approval in schizophrenia.
Antipsychotic side effects, including metabolic, prolactinemia, and TD, reviewed with patient.
Dementia
Brexpiprazole use based on FDA approval for behavioral symptoms of dementia.
Antipsychotic side effects, including metabolic, prolactinemia, and TD, reviewed with patient.