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Brexpiprazole

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Brexpiprazole, Rexulti

  • See Also
  1. Antipsychotic Medication
  2. Psychosis
  3. Aripiprazole
  • Indications
  1. Schizophrenia
  2. Major Depression (adjunct)
  3. Agitation in Dementia (FDA approved in 2023)
  • Mechanism
  1. Atypical Antipsychotic (Second Generation agent)
  2. Dopamine D3 partial Agonist (and less D2 Agonist activity than with Aripiprazole)
    1. D3 > D2 activity may result in less Akathisia than with Aripiprazole
  3. Serotonin 5HT1A partial Agonist (more potent activity than with Aripiprazole)
    1. Anxiolytic effect
  4. Serotonin 5HT2A receptor Antagonist (more potent activity than with Aripiprazole)
    1. Anxiolytic effect
  5. Alpha-1 Beta Adrenergic Antagonist
    1. May be associated with lower risk of Akathisia
  • Adverse Effects
  1. See Aripiprazole
  2. See Atypical Antipsychotic
  3. Weight gain (more than Aripiprazole)
  4. Akathisia (less than Aripiprazole)
  5. Hyperlipidemia
  6. Somnolence
  7. Constipation
  8. Dizziness
  9. Impulse control behaviors (rare)
    1. Behaviors seen with other Dopamine Agonists (e.g. Compulsive Gambling, hypersexuality, shopping, eating)
    2. Moore (2014) JAMA Intern Med 174(12):1930-3 [PubMed]
  10. Increased mortality in older adults with Dementia
    1. Brexpiprazole black box warning (as with other Atypical Antipsychotics)
    2. Curiously FDA approved in 2023 for Agitation in Dementia
  • Drug Interactions
  1. See Aripiprazole
  1. Start 1 mg orally daily
  2. May increase to 2 mg orally daily after the first 4-5 days
  3. Maximum: 4 mg/day
  4. Reduce dose in renal disease (eGFR <60 ml/min) and moderate to severe hepatic Impairment
  • Dosing Major Depression
  1. Start 0.5 to 1 mg orally daily
  2. May increase each week by 1 mg/day
  3. Maximum: 3 mg/day
  1. See Agitation in Dementia
  2. Start 0.5 mg orally daily
  3. May increase to 1 mg orally daily after 1 week if 0.5 mg dose is tolerated
  4. May increase to 2 mg orally daily (maintenance) after 1 week if 1 mg dose is tolerated
  5. May increase to 3 mg orally daily (maximum) after 2 weeks if 2 mg dose tolerated and effective
    1. Limit to 2 mg maximum dose if GFR <60 ml/minor moderate to severe hepatic Impairment
  • Resources
  1. Brexpiprazole (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2d301358-6291-4ec1-bd87-37b4ad9bd850
  • References
  1. (2016) Med Lett Drugs Ther 58(1510): 160-5
  2. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 42-3
  3. Hamilton (2020) Tarascon Pocket Pharmacopoeia