Brexpiprazole is an atypical antipsychotic indicated for:

• Use as an adjunct to antidepressant therapy in the treatment of major depressive disorder (MDD)
• Treatment of schizophrenia.

Brexpiprazole is an atypical antipsychotic agent. Its pharmacological effects are thought to result from its modulatory action on serotonin and dopamine systems. It acts as a partial agonist at serotonergic 5-HT₁A receptors and dopaminergic D₂ receptors, while exhibiting antagonist activity at serotonergic 5-HT₂A receptors. It has high affinity for these receptors and also demonstrates antagonist activity at noradrenergic alpha receptors.

Adjunctive Treatment of Major Depressive Disorder: The recommended starting dosage for Brexpiprazole as adjunctive treatment is 0.5 mg or 1 mg once daily, taken orally with or without food. Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient's clinical response and tolerability. The maximum recommended daily dosage is 3 mg. Periodically reassess to determine the continued need and appropriate dosage for treatment.

Treatment of Schizophrenia: The recommended starting dosage for Brexpiprazole is 1 mg once daily on Days 1 to 4, taken orally with or without food. The recommended target Brexpiprazole dosage is 2 mg to 4 mg once daily. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient's clinical response and tolerability. The maximum recommended daily dosage is 4 mg.

Brexpiprazole is contraindicated in patients with known hypersensitivity to brexpiprazole or any of its ingredients. Reported reactions include rash, facial edema, urticaria, and anaphylaxis.

Common adverse effects include:

• Extrapyramidal symptoms
• Akathisia
• Suicidal thoughts (suicidality)
• QT interval prolongation
• Weight gain
• Neuroleptic malignant syndrome
• Nausea

A pregnancy exposure registry is available to monitor outcomes in women exposed to Brexpiprazole during pregnancy. There are no adequate studies regarding the presence of brexpiprazole in human milk, its effects on the breastfed infant, or its impact on milk production. Brexpiprazole has been detected in animal (rat) milk. The benefits of breastfeeding should be weighed against the mother’s need for treatment and potential risks to the infant.

• Elderly patients with dementia-related psychosis may have an increased risk of cerebrovascular events such as stroke or transient ischemic attack.
• Neuroleptic malignant syndrome may occur; immediate discontinuation and close monitoring are required.
• Tardive dyskinesia may develop; discontinue treatment if appropriate.
• Monitor metabolic changes including hyperglycemia, diabetes, dyslipidemia, and weight gain.
• Pathological gambling and other compulsive behaviors may occur; dose reduction or discontinuation should be considered.
• Leukopenia, neutropenia, and agranulocytosis may occur; monitor complete blood count and discontinue if significant decline in WBC is observed.
• Orthostatic hypotension and syncope may occur; monitor blood pressure and heart rate, especially in at-risk patients.
• Use cautiously in patients with a history of seizures or conditions lowering seizure threshold.

Hepatic Impairment: In moderate to severe hepatic impairment, the maximum dose is 2 mg/day for MDD and 3 mg/day for schizophrenia.

Renal Impairment: In moderate to severe renal impairment (CrCl <60 mL/min), the maximum dose is 2 mg/day for MDD and 3 mg/day for schizophrenia.

Pediatric Use: Safety and effectiveness in children have not been established. Increased risk of suicidal thoughts has been observed.

Geriatric Use: Dose selection should be cautious, starting at lower doses due to possible reduced organ function and comorbidities.

Antipsychotic agent

Store below 30°C, protected from light and moisture. Keep out of reach of children.