Brexpiprazole: Difference between revisions
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Expand Brexpiprazole with Stahl-sourced detail (with skepticism) |
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{{MedTemplate | {{MedTemplate | ||
| brand = Rexulti | |||
| brand | | 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 — proposed to reduce akathisia and enhance affective/cognitive effects. | |||
| classes | | 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 indication). Investigational for PTSD (combined with sertraline). | ||
| mechanism | | 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. | ||
| uses | | preparations = 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets | ||
| starting_dose | | fda_max = 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) | ||
| preparations | | routes = Oral | ||
| fda_max | | onset = Weeks for psychosis/depression; AD agitation benefit emerges over weeks | ||
| routes | | duration = Daily dosing | ||
| onset | | halflife = ~91 hours | ||
| duration | | bioavailability = ~95% | ||
| halflife | | pregnancy = Limited data; National Pregnancy Registry available | ||
| bioavailability | | legal = Rx | ||
| pregnancy | | 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 medication 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. | ||
| legal | |||
| intro | 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 indication. | ||
| pharmacodynamics= 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. | |||
| pharmacodynamics | | 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 indication acknowledges this risk with specific benefit-risk analysis. | ||
| interactions = <pharmaInteractions/> | |||
| effects | |||
| interactions | |||
}} | }} | ||
[[Category:Antipsychotics / Neuroleptics]] | |||
[[Category:Second-Generation Antipsychotics (SGAs / Atypicals)]] | |||
[[Category:Neuroleptics]] | [[Category:Neuroleptics]] | ||
[[Category:Third-Generation Antipsychotics]] | |||
[[Category:Atypical Antipsychotics]] | |||
[[Category:Antipsychotics]] | |||
[[Category:Dopamine Partial Agonists]] | |||
[[Category:Psychotic Disorders]] | |||
[[Category:Adjunctive Antidepressants]] | |||