What is the recommended use and dosage of Rexulti (brexpiprazole)?

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Last updated: July 6, 2025View editorial policy

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From the Research

Rexulti (brexpiprazole) is recommended for the treatment of schizophrenia at a target dose of 2-4 mg daily, and as an adjunctive treatment for major depressive disorder (MDD) at a target dose of 2 mg daily, with dosage adjustments necessary for patients with hepatic or renal impairment, or those taking CYP2D6 or CYP3A4 inhibitors. The medication should be taken at the same time each day with or without food, and patients should not abruptly discontinue Rexulti, as gradual tapering is recommended to avoid withdrawal symptoms 1. Rexulti works by modulating serotonin and dopamine activity in the brain, acting as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors, with a pharmacological profile that suggests a lower propensity for activating adverse events and extrapyramidal symptoms compared to other antipsychotic agents 2. Some key points to consider when prescribing Rexulti include:

  • Initial dose: 1 mg once daily for schizophrenia, with gradual increase to target dose
  • Target dose: 2-4 mg daily for schizophrenia, and 2 mg daily for MDD
  • Dosage adjustments: necessary for patients with hepatic or renal impairment, or those taking CYP2D6 or CYP3A4 inhibitors
  • Common side effects: weight gain, akathisia (restlessness), and increased risk of suicidal thoughts in young adults, requiring careful monitoring during initial treatment 3, 4, 5. It is essential to carefully monitor patients for potential side effects and adjust the dosage accordingly to minimize the risk of adverse events.

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This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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