Brexpiprazole: Difference between revisions
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MDElliottMD (talk | contribs) Sweep: "indications" -> "problems" sitewide terminology update (preserves MedTemplate param name) |
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| 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 — proposed to reduce akathisia and enhance affective/cognitive effects. | | 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 — first agent specifically approved for this | | 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 | ||
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| 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. | | 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 | 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. | ||
| 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= 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. | ||
| 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 | | 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. | ||
| interactions = <pharmaInteractions/> | | interactions = <pharmaInteractions/> | ||
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