CV: bradycardia, chest pain, edema, hypertension, orthostatic hypotension, tachycardia.
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), dry skin, ecchymosis, skin ulcer, sweating.
EENT: blurred vision, conjunctivitis, ear pain.
Endo: ↓ prolactin, hyperglycemia.
GI: constipation, ↑ salivation, anorexia, nausea, vomiting.
GU: urinary incontinence.
Hemat: AGRANULOCYTOSIS, anemia, leukopenia, neutropenia.
Metab: dyslipidemia, weight gain, weight loss.
MS: muscle cramps, neck pain.
Neuro: drowsiness, extrapyramidal reactions, tremor, abnormal gait, akathisia, confusion, depression, fatigue, hostility, impaired cognitive function, impulse control disorders (eating/binge eating, gambling, sexual, shopping), insomnia, lightheadedness, manic reactions, nervousness, restlessness, sedation, SEIZURES, SUICIDAL THOUGHTS, tardive dyskinesia.
Resp: dyspnea.
Misc: ↓ heat regulation, HYPERSENSITIVITY REACTIONS, injection site reactions, NEUROLEPTIC MALIGNANT SYNDROME.
If used concurrently with combination of strong, moderate, or weak CYP3A4 and CYP2D6 inhibitors, ↓ oral aripiprazole dose by 75%. Aripiprazole dose should be ↓ by 75% in CYP2D6 PMs who are concomitantly receiving a strong CYP3A4 inhibitor. Do NOT substitute Aristada Initio for Aristada.
Schizophrenia
- PO (Adults): 10 or 15 mg once daily; doses up to 30 mg/day have been used; increments in dosing should not be made before 2 wk at a given dose.
- PO (Children 13–17 yr): 2 mg once daily; ↑ to 5 mg once daily after 2 days, and then to target dose of 10 mg once daily after another 2 days; may further ↑ dose in 5-mg increments if needed (max: 30 mg/day).
- IM (Adults): Abilify Maintena: 400 mg every mo; after 1st injection, continue treatment with oral aripiprazole (10–20 mg/day) for 14 days; if no adverse reactions to 400 mg/mo dose, may ↓ dose to 300 mg every mo. CYP2D6 PMs: ↓ dose to 300 mg monthly; CYP2D6 PMs concomitantly receiving strong CYP3A4 inhibitor: ↓ dose to 200 mg monthly; Concomitant therapy with strong CYP2D6 or CYP3A4 inhibitor: ↓ dose to 300 mg monthly (if originally receiving 400 mg monthly) or 200 mg monthly (if originally receiving 300 mg monthly); Concomitant therapy with strong CYP2D6 and CYP3A4 inhibitor: ↓ dose to 200 mg monthly (if originally receiving 400 mg monthly) or 160 mg monthly (if originally receiving 300 mg monthly); Concomitant therapy with CYP3A4 inducer: Avoid use.
- IM (Adults): Abilify Asimtufii and receiving oral antipsychotics: 960 mg every 2 mo (56 days after previous injection); after 1st injection, if previously receiving oral aripiprazole, continue treatment with oral aripiprazole (10–20 mg/day) for 14 days. If previously stable on another oral antipsychotic (but known to tolerate aripiprazole), after 1st injection, continue treatment with oral antipsychotic for 14 days. Abilify Asimtufii and previously receiving Abilify Maintena: 960 mg every 2 mo in place of the next scheduled Abilify Maintena injection; the 1st injection may be administered in place of the 2nd or later injection of Abilify Maintena; CYP2D6 PMs: ↓ dose to 720 mg every 2 mo; CYP2D6 PMs concomitantly receiving strong CYP3A4 inhibitor: Avoid use; Concomitant therapy with strong CYP2D6 or CYP3A4 inhibitor: ↓ dose to 720 mg every 2 mo; Concomitant therapy with strong CYP2D6 and CYP3A4 inhibitor: Avoid use; Concomitant therapy with CYP3A4 inducer: Avoid use.
- IM (Adults): Aristada with Aristada Initio: administer 675–mg injection of Aristada Initio with first injection of Aristada (dose is based on total daily dose of oral aripiprazole; if patient receiving 10 mg/day of oral aripiprazole, administer 441 mg every mo; if patient receiving 15 mg/day of oral aripiprazole, administer 662 mg every mo, 882 mg every 6 wk, or 1064 mg every 2 mo; if patient receiving ≥20 mg/day of oral aripiprazole, administer 882 mg every mo) (initial Aristada dose can be given on same day as or within 10 days of Aristada Initio) AND one dose of oral aripiprazole 30 mg; Aristada without Aristada Initio: Dose is based on total daily dose of oral aripiprazole; if patient receiving 10 mg/day of oral aripiprazole, administer 441 mg every mo; if patient receiving 15 mg/day of oral aripiprazole, administer 662 mg every mo, 882 mg every 6 wk, or 1064 mg every 2 mo; if patient receiving ≥20 mg/day of oral aripiprazole, administer 882 mg every mo; after 1st injection; continue treatment with oral aripiprazole for 21 days; Concomitant therapy with strong CYP2D6 or CYP3A4 inhibitor for >2 wk: ↓ dose of Aristada to 441 mg monthly (if originally receiving 662 mg monthly) or 662 mg monthly (if originally receiving 882 mg monthly); no dose adjustment necessary if originally receiving 441 mg monthly; avoid use of Aristada Initio; CYP2D6 PMs concomitantly receiving strong CYP3A4 inhibitor for >2 wk: ↓ dose of Aristada to 441 mg monthly (if originally receiving 662 mg or 882 mg monthly); no dose adjustment necessary if originally receiving 441 mg monthly; avoid use of Aristada Initio; Concomitant therapy with strong CYP2D6 and CYP3A4 inhibitor: avoid use of Aristada in patients requiring 662 mg or 882 mg monthly dose; no dose adjustment of Aristada necessary if originally receiving 441 mg monthly; avoid use of Aristada Initio; Concomitant therapy with CYP3A4 inducer: ↑ dose of Aristada to 662 mg monthly (if originally receiving 441 mg monthly); no dose adjustment if Aristada necessary if originally receiving 662 mg or 882 mg monthly; avoid use of Aristada Initio.
Acute Manic or Mixed Episodes Associated with Bipolar I Disorder
- PO (Adults): 15 mg once daily as monotherapy or 10–15 mg once daily with lithium or valproate; target dose is 15 mg once daily; may ↑ to 30 mg once daily, if needed.
- PO (Children 10–17 yr): 2 mg once daily; ↑ to 5 mg once daily after 2 days, and then to target dose of 10 mg once daily after another 2 days; may further ↑ dose in 5-mg increments if needed (max: 30 mg/day).
Maintenance Treatment of Bipolar I Disorder
- PO (Adults): Abilify Mycite: 15 mg once daily as monotherapy or 10–15 mg once daily with lithium or valproate; target dose is 15 mg once daily; may ↑ to 30 mg once daily, if needed.
- IM (Adults): Abilify Maintena: 400 mg every mo; after 1st injection, continue treatment with oral aripiprazole (10–20 mg/day) for 14 days; if no adverse reactions to 400 mg/mo dose, may ↓ dose to 300 mg every mo. CYP2D6 PMs: ↓ dose to 300 mg monthly; CYP2D6 PMs concomitantly receiving strong CYP3A4 inhibitor: ↓ dose to 200 mg monthly; Concomitant therapy with strong CYP2D6 or CYP3A4 inhibitor: ↓ dose to 300 mg monthly (if originally receiving 400 mg monthly) or 200 mg monthly (if originally receiving 300 mg monthly); Concomitant therapy with strong CYP2D6 and CYP3A4 inhibitor: ↓ dose to 200 mg monthly (if originally receiving 400 mg monthly) or 160 mg monthly (if originally receiving 300 mg monthly); Concomitant therapy with CYP3A4 inducer: Avoid use.
- IM (Adults): Abilify Asimtufii and receiving oral antipsychotics: 960 mg every 2 mo (56 days after previous injection); after 1st injection, if previously receiving oral aripiprazole, continue treatment with oral aripiprazole (10–20 mg/day) for 14 days. If previously stable on another oral antipsychotic (but known to tolerate aripiprazole), after 1st injection, continue treatment with oral antipsychotic for 14 days. Abilify Asimtufii and previously receiving Abilify Maintena: 960 mg every 2 mo in place of the next scheduled Abilify Maintena injection; the 1st injection may be administered in place of the 2nd or later injection of Abilify Maintena; CYP2D6 PMs: ↓ dose to 720 mg every 2 mo; CYP2D6 PMs concomitantly receiving strong CYP3A4 inhibitor: Avoid use; Concomitant therapy with strong CYP2D6 or CYP3A4 inhibitor: ↓ dose to 720 mg every 2 mo; Concomitant therapy with strong CYP2D6 and CYP3A4 inhibitor: Avoid use; Concomitant therapy with CYP3A4 inducer: Avoid use.
Depression
- PO (Adults): 2–5 mg once daily, may titrate upward at 1-wk intervals to 5–10 mg once daily (max: 15 mg/day).
Irritability Associated with Autistic Disorder
- PO (Children 6–17 yr): 2 mg once daily; ↑ to 5 mg once daily after at least 1 wk; may further ↑ dose in 5-mg increments if needed at ≥1-wk intervals (max: 15 mg/day).
Tourette's Disorder
- PO (Children 6–18 yr and ≥50 kg): 2 mg once daily; ↑ to target dose of 5 mg once daily after 2 days; may further ↑ dose if needed at ≥1-wk intervals (max: 10 mg/day).
- PO (Children 6–18 yr and <50 kg): 2 mg once daily; ↑ to 5 mg once daily after 2 days, and then to target dose of 10 mg once daily after 5 days; may further ↑ dose in 5-mg increments if needed at ≥1-wk intervals (max: 20 mg/day).
Abilify, Abilify Asimtufii, Abilify Maintena, Abilify Mycite, Aristada, Aristada Initio
Therapeutic Classification: antipsychotics
Pharmacologic Classification: serotonin-dopamine activity modulators (SDAM)
Absorption: Well absorbed (87%) following oral administration; 100% following IM injection.
Distribution: Extensive extravascular distribution.
Protein Binding: >99%.
Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A4 and CYP2D6 isoenzymes; the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers (PMs) and may have significantly ↑ aripiprazole concentrations and an ↑ risk of adverse effects (↓ dose by 50% in PMs); one metabolite (dehydro-aripiprazole) has antipsychotic activity. 18% excreted unchanged in feces; <1% excreted unchanged in urine.
Half-life: Aripiprazole: 75 hr; dehydro-aripiprazole—94 hr; ER injectable suspension: 30–46 days (Abilify Maintena); 29–35 days (Aristada).
