Brexpiprazole: Difference between revisions
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MDElliottMD (talk | contribs) Category taxonomy (#23): retag to house-compliant neuroleptic categories |
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| brand = Rexulti | | brand = Rexulti | ||
| classes = Atypical antipsychotic, D2/5HT1A partial agonist with stronger α1A, 5HT2A, 5HT1A activity than aripiprazole | | classes = Atypical antipsychotic, D2/5HT1A partial agonist with stronger α1A, 5HT2A, 5HT1A activity than aripiprazole | ||
| mechanism = Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole | | mechanism = Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. | ||
| uses = Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023 | | uses = Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). | ||
| starting_dose = Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. | | starting_dose = Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. | ||
| preparations = 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets | | preparations = 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets | ||
| Line 14: | Line 14: | ||
| pregnancy = Limited data; National Pregnancy Registry available | | pregnancy = Limited data; National Pregnancy Registry available | ||
| legal = Rx | | legal = Rx | ||
| intro = '''Brexpiprazole''' (brand name Rexulti) is a 'pip' D2/5HT1A partial agonist FDA-approved for schizophrenia (2015), adjunctive treatment of major depressive disorder (2015), and | | intro = '''Brexpiprazole''' (brand name Rexulti) is a 'pip' D2/5HT1A partial agonist FDA-approved for schizophrenia (2015), adjunctive treatment of major depressive disorder (2015), and, in a landmark 2023 approval, '''agitation associated with Alzheimer dementia'''. It is the first FDA-approved medicine specifically for AD agitation. Compared to its 'pip' cousin aripiprazole, brexpiprazole has relatively stronger 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism, proposed to reduce akathisia and enhance affective/cognitive efficacy. | ||
The AD agitation approval carries the antipsychotic class black-box warning for increased mortality in elderly dementia patients; FDA approval rested on demonstrating a favorable risk-benefit ratio in this population specifically for the problem. | The AD agitation approval carries the antipsychotic class black-box warning for increased mortality in elderly dementia patients; FDA approval rested on demonstrating a favorable risk-benefit ratio in this population specifically for the problem. | ||
| Line 22: | Line 22: | ||
}} | }} | ||
[[Category:Second-generation neuroleptics]] | |||
[[Category:Second- | |||
[[Category:Neuroleptics]] | [[Category:Neuroleptics]] | ||
[[Category:Third- | [[Category:Third-generation neuroleptics]] | ||
[[Category:Atypical Antipsychotics]] | [[Category:Atypical Antipsychotics]] | ||
[[Category:Dopamine Partial Agonists]] | [[Category:Dopamine Partial Agonists]] | ||
[[Category:Psychotic Disorders]] | [[Category:Psychotic Disorders]] | ||
[[Category:Adjunctive Antidepressants]] | [[Category:Adjunctive Antidepressants]] | ||
Latest revision as of 14:41, 22 May 2026
Atypical antipsychotic, D2/5HT1A partial agonist with stronger α1A, 5HT2A, 5HT1A activity than aripiprazole
Brexpiprazole
Rexulti
Brexpiprazole (brand name Rexulti) is a 'pip' D2/5HT1A partial agonist FDA-approved for schizophrenia (2015), adjunctive treatment of major depressive disorder (2015), and, in a landmark 2023 approval, agitation associated with Alzheimer dementia. It is the first FDA-approved medicine specifically for AD agitation. Compared to its 'pip' cousin aripiprazole, brexpiprazole has relatively stronger 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism, proposed to reduce akathisia and enhance affective/cognitive efficacy.
The AD agitation approval carries the antipsychotic class black-box warning for increased mortality in elderly dementia patients; FDA approval rested on demonstrating a favorable risk-benefit ratio in this population specifically for the problem.
D2 partial agonist (lower intrinsic activity than aripiprazole). 5HT1A partial agonist. 5HT2A, 5HT2B, 5HT7, α1A, α1B, α2C antagonist. H1 antagonism. Notable: lower D2 intrinsic activity and stronger 5HT2A antagonism may underlie reduced akathisia compared with aripiprazole.
Experience
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Problems
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Effects
Weight gain (especially long-term), akathisia (reduced compared to aripiprazole), restlessness, headache, somnolence, increased fasting glucose. Class warning: increased mortality in elderly dementia-related psychosis. AD agitation problem acknowledges this risk with specific benefit-risk analysis.
Pharmacodynamics
Interactions
Pharmacogenomic + mechanism interactions
Pharmacogenomic guideline recommendationsCPIC and Dutch Pharmacogenetics Working Group clinical guidelines
DPWG guideline: The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group (DPWG) recommends to use half of the normal dose of brexpiprazole for poor metabolizers of CYP2D6.
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Summary
Classes
Atypical antipsychotic, D2/5HT1A partial agonist with stronger α1A, 5HT2A, 5HT1A activity than aripiprazole
Common uses
Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). Agitation associated with dementia due to Alzheimer disease (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline).
Pharmacy
Starting dose
Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily.
Preparations
0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets
US FDA Max
4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct)
Pharmacology
Routes
Oral
Onset
Weeks for psychosis/depression; AD agitation benefit emerges over weeks
Duration
Daily dosing
Half-life
~91 hours
Bioavailability
~95%
Pregnancy
Limited data; National Pregnancy Registry available
Legal status
Rx
Purported mechanism
Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects.