This article was last reviewed, updated, or edited on January 29, 2024.
Brexpiprazole (brand name Rexulti®) is a second-generation (“atypical”) antipsychotic first introduced in the US in 2015.
As of January 2024, it is available only as a brand name preparation (no generic), Rexulti®, that is manufactured by Otsuka Pharmaceutical Company Ltd and co-marketed with H. Lundbeck A/S.
On this page, we present basic information about this medication. Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
Indications
1. “Use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults”
2. “Treatment of schizophrenia in adults and pediatric patients ages 13 years and older”
3. “Treatment of agitation associated with dementia due to Alzheimer’s disease“. Limitations of Use: “REXULTI is not indicated as an as needed (“prn”) treatment for agitation associated with dementia due to Alzheimer’s disease”.
Pharmacological effects
1. Partial agonist at the 5-HT1A, D2, and D3 receptors
2. Antagonist at 5-HT2A, 5-HT2B, 5-HT7, alpha-1 (subtypes A, B, and D), and alpha-2C receptors.
Dosing
1. For adjunctive treatment of major depressive disorder in adults
Starting dosage: 0.5 mg/day or 1 mg/day. Titrate up to the target dosage of 2 mg once daily
Recommended target dosage: 2 mg/day
Maximum dosage: 3 mg/day
2. For the treatment of schizophrenia
Starting dosage: 1 mg/day for four days. Then, 2 mg/day for three days Then 4 mg/day
Recommended target dosage: 2 mg to 4 mg once daily
3. For the treatment of agitation associated with dementia due to Alzheimer’s disease
Starting dosage: 0.5 mg/day during the first week
Titration: 1 mg/day during the second week
Target dosage (after 2 weeks): 2 mg/day
Maximum dosage: 3 mg/day, if needed based on response and side effects.
Potential side effects
Please see THIS PAGE for a handout listing both the common and less common side effects of this medication along with the percentages of patients who report them.
Dosage adjustments
Dose adjustments are recommended for patients who are:
1. Poor metabolizers on the CYP450 2D6 isoenzyme, or
2. Taking strong inducers/ inhibitors of CYP2D6 and/or CYP3A4.
Dosage forms and strengths
Rexulti® is available as tablets in the following dosage strengths: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Related Pages
Potential side effects of brexpiprazole (Rexulti®)
Brexpiprazole: Efficacy for schizophrenia
Brexpiprazole: Efficacy for major depressive disorder
Brexpiprazole: Mechanism of action
Aripiprazole and brexpiprazole: Impulsive or compulsive urges and behavior
Dopamine D2 receptor partial agonists: Receptor binding affinity and intrinsic activity
Do newer antipsychotics have any advantages?
Dose adjustment for second-generation antipsychotics based on drug interactions
Second-Generation Antipsychotics: Dose Equivalents
What should I be doing to monitor patients who are on an antipsychotic?
Monitoring form for second-generation antipsychotics
News: July 6, 2016. Make sure you are discussing increased risk of gynecomastia with risperidone
FDA issues new warning about aripiprazole (impulse control problems)
Changes in rules about clozapine
Second-Generation Antipsychotics: Dose Equivalents
Second-Generation (“Atypical”) Antipsychotics
References
Prescribing information for brexpiprazole (Rexulti®)
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