Aripiprazole: Difference between revisions
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MDElliottMD (talk | contribs) parser-claude: Aripiprazole MedTemplate refill, Top 300 stub upgrade |
Safety wave: FDA 2016 impulse-control labeled Warning (May 3 2016 DSC); labeled, not boxed |
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| routes = Oral, intramuscular (acute and long-acting) | | routes = Oral, intramuscular (acute and long-acting) | ||
| onset = | | onset = Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days | ||
| duration = 24 hours (oral); 4-8 weeks (LAI) | | duration = 24 hours (oral); 4-8 weeks (LAI) | ||
| halflife = ~75 hours (long, accumulates over weeks)<ref name="abilify-label">FDA Prescribing Information, Abilify (aripiprazole), Otsuka/Bristol-Myers Squibb, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021436s038,021713s030,021729s022,021866s023lbl.pdf</ref> | | halflife = ~75 hours (long, accumulates over weeks)<ref name="abilify-label">FDA Prescribing Information, Abilify (aripiprazole), Otsuka/Bristol-Myers Squibb, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021436s038,021713s030,021729s022,021866s023lbl.pdf</ref> | ||
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| legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis, and the antidepressant suicidality '''Boxed Warning''' when used for MDD adjunct in patients under 24<ref name="abilify-label" /> | | legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis, and the antidepressant suicidality '''Boxed Warning''' when used for MDD adjunct in patients under 24<ref name="abilify-label" /> | ||
| mechanism = <vote slug="aripiprazole-mech-claim">'''D2 and D3 dopamine receptor partial agonist''' (the third-generation neuroleptic signature, distinct from olanzapine/risperidone full D2 antagonism), with additional 5-HT1A partial agonism and 5-HT2A receptor antagonism. The D2 partial agonism is the "dopamine system stabilizer" rationale: in hyperdopaminergic states (psychosis, mania) aripiprazole functions as a partial antagonist; in hypodopaminergic states (prefrontal cortex, MDD adjunct) it functions as a partial agonist.</vote> '''Akathisia''' is the most common dose-limiting adverse effect, particularly with the MDD-adjunct dose range. Lower weight gain, lower metabolic burden, and lower prolactin elevation than most second-generation neuroleptics, the principal pharmacological selling points. CYP2D6 and CYP3A4 metabolism; CPIC PGx guidance applies for CYP2D6 dose individualization<ref name="abilify-label" />. | | mechanism = <vote slug="aripiprazole-mech-claim">'''D2 and D3 dopamine receptor partial agonist''' (the third-generation neuroleptic signature, distinct from olanzapine/risperidone full D2 antagonism), with additional 5-HT1A partial agonism and 5-HT2A receptor antagonism. The D2 partial agonism is the "dopamine system stabilizer" rationale: in hyperdopaminergic states (psychosis, mania) aripiprazole functions as a partial antagonist; in hypodopaminergic states (prefrontal cortex, MDD adjunct) it functions as a partial agonist.</vote> '''Akathisia''' is the most common dose-limiting adverse effect, particularly with the MDD-adjunct dose range. Lower weight gain, lower metabolic burden, and lower prolactin elevation than most second-generation neuroleptics, the principal pharmacological selling points. CYP2D6 and CYP3A4 metabolism; CPIC PGx guidance applies for CYP2D6 dose individualization<ref name="abilify-label" />. | ||
| effects = In May 2016 the FDA warned that aripiprazole can cause intense, uncontrollable urges, most often compulsive gambling, but also compulsive eating, shopping, and hypersexuality; these urges can arise at any dose, are easily missed, and generally resolve when the dose is lowered or the medicine is stopped.<ref>U.S. Food and Drug Administration. Drug Safety Communication: FDA warns about new impulse-control problems associated with mental health drug aripiprazole (Abilify, Abilify Maintena, Aristada). May 3, 2016.</ref> The association is commonly linked to aripiprazole's dopamine D2 partial agonism, though the FDA stated the mechanism is not established. This is a labeled Warning, separate from the medicine's boxed warnings. | |||
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