brexpiprazole REXULTI

Class: Second Generation Antipsychotic
FDA Indications: Schizophrenia, Adjunctive Treatment Of Major Depressive Disorder
Off-Label Use:
Forms: 0.25, 0.5, 1, 2, 3, 4mg tablet
Dose Range: 0.5-4 mg/day
Starting: 0.5-1 mg po qd, titrate to max dose 3 mg qd (MDD) or 4 mg qd (schizophrenia)
Stopping: Recommend taper as rapid d/c can lead to rebound psychosis (though its long t½ allows for faster tapers than others in its class)

NAMI drug fact sheet

Serious Side Effects: , , ,
Not Classified: This drug has been reviewed by CredibleMeds but the evidence available at this time did not result in a decision for it to be placed in any of the four QT risk categories. This is not an indication that this drug is free of a risk of QT prolongation or torsades de pointes since it may not have been adequately tested for these risks in patients.
Side Effects: weight gain, nasopharyngitis, akathisia, headache, sedation/somnolence, tremor, dizziness, anxiety, restlessness, EPS
1° MOA: Serotonin-dopamine activity modulator (SDAM)
Target: Antagonism at: Partial agonist at Postsynaptic 5HT1A, D2 &
  • D3
  • Pharmacokinetics
    t½: 91° TMAX:
    Substrate of: 2D6, 3A4
    Inhibits: ∅ ; Induces:
    Active Metabolites:
    • - Compared with aripiprazole, has ↓ activity at the D2, ↑ antagonism at 5-HT2A & NET & ∴ ↓ potential to induce D2 partial agonist mediated adverse effects
    • - may have procognitive effects
    • - ∅ prolactin ↑
    • - ∅ QTC Δ's
    • - low EPS risk
    Special Populations

    Category Not assigned.—Adequate and well-controlled studies have not been conducted in pregnant women to inform drug-associated risks. May cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure

    Lactation studies have not been conducted to assess the presence of in human milk, the effects on the breastfed infant, or the effects on milk production

    All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.

    2019 BEE℞S Recommendation: Avoid, except in schizophrenia or bipolar disorder. Increased risk of CVA and greater rate of cognitive decline and mortality in persons with dementia. Avoid antipsychotics for behavioral problems of dementia or delirium unless nonpharmacological options have failed or are not possible and the older adult is threatening substantial harm to self or others.

    For patients with moderate, severe or end-stage renal impairment (CLcr<60 mL/min), the max recommended dosage is 2 mg qd for patients with MDD and 3 mg qd for patients with schizophrenia

    For patients with moderate to severe hepatic impairment (Child-Pugh score ≥7), the max recommended dosage is 2 mg qd for patients with MDD and 3 mg qd for patients with schizophrenia


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    Last updated February 29 2024 20:54:18. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.