II. Indications
- Schizophrenia
- Major Depression (adjunct)
- Agitation in Dementia (FDA approved in 2023)
III. Mechanism
- Atypical Antipsychotic (Second Generation agent)
-
Dopamine D3 partial Agonist (and less D2 Agonist activity than with Aripiprazole)
- D3 > D2 activity may result in less Akathisia than with Aripiprazole
-
Serotonin 5HT1A partial Agonist (more potent activity than with Aripiprazole)
- Anxiolytic effect
-
Serotonin 5HT2A receptor Antagonist (more potent activity than with Aripiprazole)
- Anxiolytic effect
- Alpha-1 Beta Adrenergic Antagonist
- May be associated with lower risk of Akathisia
IV. Medications
- Brexpiprazole (Rexulti) Tablets: 0.5 mg, 1 mg, 2 mg, 3 mg
- Expensive as of 2024 ($1500/month)
V. Dosing: Schizophrenia
- Start 1 mg orally daily
- May increase to 2 mg orally daily after the first 4-5 days
- Maximum: 4 mg/day
- Reduce dose in renal disease (eGFR <60 ml/min) and moderate to severe hepatic Impairment
VI. Dosing Major Depression
- Start 0.5 to 1 mg orally daily
- May increase each week by 1 mg/day
- Maximum: 3 mg/day
VII. Dosing: Agitation in Dementia
- See Agitation in Dementia
- Start 0.5 mg orally daily
- May increase to 1 mg orally daily after 1 week if 0.5 mg dose is tolerated
- May increase to 2 mg orally daily (maintenance) after 1 week if 1 mg dose is tolerated
- May increase to 3 mg orally daily (maximum) after 2 weeks if 2 mg dose tolerated and effective
- Limit to 2 mg maximum dose if GFR <60 ml/minor moderate to severe hepatic Impairment
VIII. Adverse Effects
- See Aripiprazole
- See Atypical Antipsychotic
- Weight gain (more than Aripiprazole, 20% of patients gain 1.3 to 1.6 kg)
- Akathisia (less than Aripiprazole, <=14%)
- Hypertriglyceridemia (5 to 18%)
- Somnolence
- Constipation
- Dizziness (3%)
- Hyperglycemia (9 to 20%)
- Urinary Tract Infection (3%)
- Insomnia (3%)
- Nasopharyngitis (4%)
- Impulse control behaviors (rare)
- Behaviors seen with other Dopamine Agonists (e.g. Compulsive Gambling, hypersexuality, shopping, eating)
- Moore (2014) JAMA Intern Med 174(12):1930-3 [PubMed]
- Increased mortality in older adults with Dementia
- Brexpiprazole black box warning (as with other Atypical Antipsychotics)
- Curiously FDA approved in 2023 for Agitation in Dementia
- Risk marginally increased compared with Placebo
- Avoid in patients living alone and in Cerebrovascular Disease
-
General
- Rate of discontinuation due to adverse effects: 13% (1 patient in 8)
IX. Drug Interactions
- See Aripiprazole
X. Resources
- Brexpiprazole (DailyMed)
XI. References
- (2016) Med Lett Drugs Ther 58(1510): 160-5
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 42-3
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
- Jarrett (2024) Am Fam Physician 110(5): 537-8 [PubMed]
Images: Related links to external sites (from Bing)
Related Studies
| rexulti (on 1/15/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| REXULTI 0.25 MG TABLET | $42.65 each | |
| REXULTI 0.5 MG TABLET | $42.55 each | |
| REXULTI 1 MG TABLET | $42.59 each | |
| REXULTI 2 MG TABLET | $42.64 each | |
| REXULTI 3 MG TABLET | $42.62 each | |
| REXULTI 4 MG TABLET | $42.50 each | |