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Brexpiprazole (Rexulti®): Basic Prescribing Information

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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Comments

  1. Nicole Christian-Brathwaite says

    July 18, 2018 at 12:33 pm

    What are your thoughts about choosing between cariprazine, aripiprazole and brexipiprazole?

    Reply

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