Aripiprazole: Difference between revisions
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MDElliottMD (talk | contribs) Comprehensive categorization: +Third-Generation Antipsychotics |
Safety wave: FDA 2016 impulse-control labeled Warning (May 3 2016 DSC); labeled, not boxed |
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{{MedTemplate | {{MedTemplate | ||
| generic | | generic = Aripiprazole | ||
| brand | | brand = Abilify (oral), Abilify Maintena (monthly IM LAI), Aristada (aripiprazole lauroxil IM LAI), Abilify Asimtufii (bi-monthly IM LAI), Abilify MyCite (digital ingestion sensor) | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:Neuroleptics|Neuroleptic]], [[:Category:Atypical neuroleptics|Atypical neuroleptic]], [[:Category:Third-generation neuroleptics|Third-generation neuroleptic]], [[:Category:Mood stabilizers|Mood stabilizer]] | ||
| | | uses = <vote slug="schizophrenia-use">Schizophrenia (FDA, ages 13+)</vote>, <vote slug="bipolar-mania-mixed-use">Bipolar mania and mixed episodes (FDA)</vote>, <vote slug="bipolar-maintenance-use">Bipolar maintenance (FDA)</vote>, <vote slug="mdd-adjunct-use">Major depressive disorder adjunct (FDA)</vote>, <vote slug="autism-irritability-use">Autism spectrum disorder-associated irritability (FDA, pediatric ages 6-17)</vote>, <vote slug="tourette-syndrome-pediatric-use">Tourette syndrome (FDA, pediatric)</vote> | ||
| | | starting_dose = Schizophrenia/bipolar mania: 10-15 mg PO once daily, target 15-30 mg. MDD adjunct: 2-5 mg/day, target 5-15 mg. Pediatric autism irritability: 2 mg, titrate to 5-15 mg. Maintena LAI: 400 mg IM every 4 weeks after oral overlap | ||
| | | preparations = Tablets 2, 5, 10, 15, 20, 30 mg; ODT 10, 15 mg; oral solution 1 mg/mL; acute IM injection 9.75 mg/1.3 mL; Maintena LAI 300, 400 mg monthly; Aristada LAI 441, 662, 882, 1064 mg (4-8 week dosing); Asimtufii bi-monthly | ||
| | | fda_max = 30 mg/day (adult schizophrenia); 15 mg/day (MDD adjunct) | ||
| | | pill_id = | ||
| routes | | routes = Oral, intramuscular (acute and long-acting) | ||
| onset | | onset = Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days | ||
| duration | | duration = 24 hours (oral); 4-8 weeks (LAI) | ||
| halflife | | 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> | ||
| bioavailability = ~87% (oral)<ref name="abilify-label" /> | |||
| pregnancy = Limited human data; signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.{{citation needed}} | |||
| 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" />. | ||
| 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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== References == | |||
<references /> | |||
[[Category:Neuroleptics]] | [[Category:Neuroleptics]] | ||
[[Category:Third- | [[Category:Atypical neuroleptics]] | ||
[[Category:Third-generation neuroleptics]] | |||
[[Category:Mood stabilizers]] | |||
Latest revision as of 18:33, 29 June 2026
Aripiprazole
Abilify (oral), Abilify Maintena (monthly IM LAI), Aristada (aripiprazole lauroxil IM LAI), Abilify Asimtufii (bi-monthly IM LAI), Abilify MyCite (digital ingestion sensor)
Experience
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Problems
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+ Add a problemTitration strategies
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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.[2] 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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Relevant Literature
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Pharmacy
Starting dose
Schizophrenia/bipolar mania: 10-15 mg PO once daily, target 15-30 mg. MDD adjunct: 2-5 mg/day, target 5-15 mg. Pediatric autism irritability: 2 mg, titrate to 5-15 mg. Maintena LAI: 400 mg IM every 4 weeks after oral overlap
Preparations
Tablets 2, 5, 10, 15, 20, 30 mg; ODT 10, 15 mg; oral solution 1 mg/mL; acute IM injection 9.75 mg/1.3 mL; Maintena LAI 300, 400 mg monthly; Aristada LAI 441, 662, 882, 1064 mg (4-8 week dosing); Asimtufii bi-monthly
US FDA Max
30 mg/day (adult schizophrenia); 15 mg/day (MDD adjunct)
Common uses
Classification(s)
Pharmacology
Routes
Oral, intramuscular (acute and long-acting)
Onset
Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days
Duration
24 hours (oral); 4-8 weeks (LAI)
Half-life
~75 hours (long, accumulates over weeks)[1]
Bioavailability
~87% (oral)[1]
Pregnancy
Limited human data; signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.[citation needed]
Legal status
Purported mechanism
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.0 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[1].
Pharmacopedia is intended for reference. Nothing here is advice. In an emergency call 911; US Poison Control 1-800-222-1222. See the full disclaimer.
References
- ↑ 1.0 1.1 1.2 1.3 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
- ↑ 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.