Aripiprazole: Difference between revisions
| [unchecked revision] | [checked revision] |
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 |
||
| (One intermediate revision by one other user not shown) | |||
| Line 10: | Line 10: | ||
| pill_id = | | pill_id = | ||
| 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> | ||
| Line 17: | Line 17: | ||
| 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. | |||
}} | }} | ||
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
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
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.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
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.