Brexpiprazole
Brand names: Rxulti, Rexulti
Brexpiprazole is a second-generation antipsychotic used in the treatment of schizophrenia.
Adult dose
Dose adjustments
Creatinine clearance <60 mL/minute: maximum recommended dosage is 2 mg once daily for patients with MDD or agitation associated with dementia due to Alzheimer's disease, and 3 mg once daily for patients with schizophrenia.
Dose auto-extracted from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.
Contraindications
- Known hypersensitivity to brexpiprazole or any of its components (reactions have included rash, facial swelling, urticaria and anaphylaxis)
Side effects
- Metabolic changes — hyperglycaemia/diabetes mellitus, dyslipidaemia and weight gain (monitor)
- Orthostatic hypotension and syncope; falls
- Tardive dyskinesia
- Pathological gambling and other compulsive behaviours
- Leukopenia, neutropenia and agranulocytosis
- Neuroleptic malignant syndrome; seizures; dysphagia; potential for cognitive and motor impairment
Interactions
- Strong CYP3A4 inhibitors — administer half of the recommended dosage
- Strong CYP2D6 inhibitors — administer half of the recommended dosage (no dosage adjustment is needed in MDD, where CYP considerations are already factored into the general dosing recommendations)
- Strong/moderate CYP2D6 inhibitor together with a strong/moderate CYP3A4 inhibitor — administer a quarter of the recommended dosage
- Strong CYP3A4 inducers — double the recommended dosage over 1 to 2 weeks, then adjust to clinical response; reduce back to the original level over 1 to 2 weeks if the inducer is stopped
- Known CYP2D6 poor metabolisers — administer half of the recommended dosage; a quarter if also taking a strong/moderate CYP3A4 inhibitor
Clinical monograph
How it works
It acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at 5-HT2A receptors, modulating dopaminergic and serotonergic signalling.
Prescribing in practice
- Like all antipsychotics, it should not be used to treat dementia-related psychosis in elderly patients because of an increased risk of stroke and death.
- Akathisia, weight gain and metabolic changes can occur, and impulse-control disorders such as pathological gambling have been reported with dopamine partial agonists.
- Dose adjustment is needed in significant hepatic or renal impairment and with strong CYP3A4 or CYP2D6 inhibitors.
Monitoring
Monitor weight, blood glucose, lipids, mental state and for akathisia and impulse-control problems.
Counselling the patient
- It may take several weeks to work fully; keep taking it as prescribed.
- Report restlessness, unusual urges such as gambling, or significant weight gain.
- Avoid alcohol and tell your prescriber about other medicines you take.
Evidence & guidelines
Efficacy in schizophrenia is supported by randomised controlled trials underpinning its licence.
Reference: Thase et al. J Clin Psychiatry 2015 (VECTOR/BEACON MDD trials); Citrome et al. Schizophr Res 2014; MHRA SPC Rxulti; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).
Related
Curated clinical cross-links plus same-class fallbacks.
- Neonatal Partial Exchange Transfusion for Polycythaemia · Neonatal Haematology
- PANSS Brief — Positive and Negative Syndrome Scale (Abbreviated) · Psychosis Assessment
- Abnormal Involuntary Movement Scale (AIMS) · Movement Disorders
- Brief Psychiatric Rating Scale (BPRS) · Psychosis
- Calgary Depression Scale for Schizophrenia (CDSS) · Mood
- RENAL Nephrometry Score · Renal Cancer
- Acute Behavioural Disturbance / Rapid Tranquillisation · RCEM 2022; RCPsych 2022; NICE NG10
- Self-Harm Presentation · NICE NG225 (2022)
- Capacity Assessment (Mental Capacity Act) · MCA 2005; Code of Practice
- Acute Psychosis Management · NICE CG178 2014
- Depression Management · NICE CG90 2022
- Lithium Therapy Monitoring · NICE CG185