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At a glance

Brexpiprazole is an atypical antipsychotic used for the treatment of schizophrenia and as adjunctive therapy to antidepressants for major depressive disorder (MDD). It works through modulatory activity at serotonin and dopamine systems.

Indications
  • Schizophrenia
  • Major Depressive Disorder (MDD) - adjunctive therapy with antidepressants
Pharmacology

Brexpiprazole is an atypical antipsychotic agent. Its pharmacology is mediated by modulatory activity at serotonin and dopamine systems, combining partial agonist activity at serotonergic 5-HT1A and dopaminergic D2 receptors (at similar potency) with antagonist activity at serotonergic 5-HT2A and noradrenergic α1B/2C receptors.

Dosage

Schizophrenia:
Recommended starting dose: 1 mg PO qDay on Days 1-4 (with or without food).
Recommended target dose: 2-4 mg PO qDay.
Titration: 2 mg/day on Days 5-7, then 4 mg/day on Day 8 (based on clinical response and tolerability).
Maximum daily dose: 4 mg.

Major Depressive Disorder (Adjunctive Therapy):
Recommended starting dose: 0.5 mg or 1 mg PO qDay (with or without food).
Recommended target dose: 2 mg PO qDay.
Titration: Weekly intervals to 1 mg/day, then up to 2 mg/day (based on clinical response and tolerability).
Maximum daily dose: 3 mg.

Hepatic impairment (Moderate-severe, Child-Pugh ≥7):
MDD: Not to exceed 2 mg/day; Schizophrenia: Not to exceed 3 mg/day.

Renal impairment (Moderate, severe, or ESRD, CrCl <60 mL/min):
MDD: Not to exceed 2 mg/day; Schizophrenia: Not to exceed 3 mg/day.

Periodically reassess to determine the continued need and appropriate dose.

Side effects

>10%: Akathisia (4-14%)

1-10%: Headache (4-9%), Weight increased (3-8%), Nasopharyngitis (1-7%), Extrapyramidal symptoms (excluding akathisia) (5-6%), Somnolence (4-6%), Dyspepsia (2-6%), Constipation (1-6%), Tremor (2-5%), Fatigue/sedation (2-5%), Dizziness (1-5%), Increased CPK blood levels (2-4%), Decreased cortisol levels (2-4%), Anxiety (2-4%), Restlessness (2-4%), Increased appetite (2-3%), Diarrhea (1-3%)

Frequency Unknown: Dystonia, QT prolongation, Neuroleptic malignant syndrome (NMS), Tardive dyskinesia, Leukopenia, Neutropenia, Agranulocytosis, Orthostatic hypotension, Syncope.

Use in pregnancy

Adequate and well-controlled studies have not been conducted in pregnant women. Neonates exposed to antipsychotics during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms. Animal studies showed no teratogenicity but increased perinatal deaths at high doses.

Precautions & warnings
  • Increased mortality in elderly patients with dementia-related psychosis (cerebrovascular adverse reactions).
  • Suicidal thoughts and behaviors reported in children, adolescents, and young adults taking antidepressant drugs.
  • Neuroleptic malignant syndrome (NMS): If suspected, immediately discontinue therapy and provide intensive symptomatic treatment and monitoring.
  • Tardive dyskinesia: Potentially irreversible, involuntary dyskinetic movements reported with antipsychotic drugs (highest in elderly women).
  • Monitor for metabolic changes including hyperglycemia/diabetes mellitus, dyslipidemia, and body weight gain.
  • May cause leukopenia, neutropenia, and agranulocytosis; monitor CBC.
  • Orthostatic hypotension or syncope may occur (rare); risk greatest during initial dose titration and dose increases.
  • May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and fractures.
  • Caution with history of seizures or conditions/drugs that lower seizure threshold.
Overdose effects

Overdose symptoms: Somnolence, dizziness, orthostatic hypotension, nausea, vomiting, tachycardia. Consult your doctor immediately if overdose is suspected.

Storage conditions

Do not store above 30°C. Keep away from light and moisture. Keep out of reach of children.

Brexpiprazole — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.