Aripiprazole
From Pharmacopedia
More actions
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
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
Summary
Common uses
Schizophrenia (FDA, ages 13+)0, Bipolar mania and mixed episodes (FDA)0, Bipolar maintenance (FDA)0, Major depressive disorder adjunct (FDA)0, Autism spectrum disorder-associated irritability (FDA, pediatric ages 6-17)0, Tourette syndrome (FDA, pediatric)0
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)
Pharmacology
Routes
Oral, intramuscular (acute and long-acting)
Onset
Antipsychotic 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].
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