TaperCommunityaripiprazole
Boxed Warning
Increased mortality in elderly patients with dementia-related psychosis. Suicidality risk in children, adolescents, and young adults (for MDD adjunct indication).
Aripiprazole is an atypical antipsychotic with a unique mechanism as a partial agonist at dopamine D2 receptors. It is approved for schizophrenia, bipolar I disorder, adjunctive treatment of MDD, irritability in autism, and Tourette disorder.
2mg, 5mg, 10mg, 15mg, 20mg, 30mg
Tablets: 2mg, 5mg, 10mg, 15mg, 20mg, 30mg; Orally disintegrating tablets: 10mg, 15mg; Oral solution: 1mg/mL; Intramuscular injection: 9.75mg/1.3mL; Extended-release injection (Abilify Maintena): 300mg, 400mg
Category C (risk cannot be ruled out)
Partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and antagonist at serotonin 5-HT2A receptors. This unique "dopamine stabilizer" profile means it can act as a functional antagonist in hyperdopaminergic states and a functional agonist in hypodopaminergic states.
Very long half-life. Liquid formulation (1mg/mL) available. Often used as adjunct to antidepressants.
Long half-life provides some buffering. Oral solution (1mg/mL) allows precise reductions. Reduce gradually despite long half-life.
Toxicity
Akathisia is the most common dose-limiting side effect. Less metabolic burden than other atypicals (lower weight gain, lipid changes). Compulsive behaviors (gambling, eating, shopping) reported. NMS and tardive dyskinesia rare.
Pharmacokinetics
Well absorbed after oral administration. Bioavailability ~87%. Tmax 3–5 hours. Food does not significantly affect absorption.
~4.9 L/kg
Hepatic via CYP3A4 and CYP2D6 to the active metabolite dehydro-aripiprazole, which has similar D2 receptor affinity. Dehydro-aripiprazole represents ~40% of parent drug AUC in plasma.
Fecal (~55%) and renal (~25%). Less than 1% excreted unchanged in urine.
>99% (primarily albumin)
~3.5 mL/min/kg
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