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aripiprazole

Brand: Abilify, Abilify Maintena, Aristada

⚠ BBW Beers Criteria Prototype: risperidone
Drug Class: antipsychotic
Drug Family: antipsychotic
Subclass: atypical antipsychotic / dopamine partial agonist
Organ Systems: cns

Mechanism of Action

Unique partial agonist at D2 and 5-HT1A receptors, acting as a functional stabilizer — activates when dopamine is low (preventing EPS and cognitive effects) and dampens activity when dopamine is high (preventing psychosis); also antagonizes 5-HT2A.

dopamine D2 partial agonistserotonin 5-HT1A partial agonist5-HT2A antagonist

Indications

  • schizophrenia
  • bipolar I mania
  • major depressive disorder (adjunct)
  • irritability associated with autism spectrum disorder
  • Tourette's syndrome
  • agitation in schizophrenia (IM)

Contraindications

  • dementia-related psychosis

Adverse Effects

Common

  • akathisia (most prominent EPS — dose-dependent)
  • nausea
  • headache
  • insomnia
  • dizziness
  • weight gain (less than other atypicals)

Serious

  • tardive dyskinesia
  • NMS
  • orthostatic hypotension
  • compulsive behaviors (pathological gambling, hypersexuality, binge eating)
  • dysphagia

Pharmacokinetics (ADME)

Absorption ~87% bioavailability; not affected by food
Distribution Protein binding >99%; Vd ~4.9 L/kg
Metabolism CYP2D6 (primary) and CYP3A4 to active dehydro-aripiprazole
Excretion Fecal (~55%) and renal (~25%)
Half-life 75 hours (aripiprazole); 94 hours (dehydro-aripiprazole) — very long; enables missed-dose tolerance
Onset Days to weeks
Peak 3–5 hours
Duration 24 hours or longer
Protein Binding >99%
Vd ~4.9 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
CYP2D6 inhibitors (fluoxetine, paroxetine) increase aripiprazole levels by ~70–112%; reduce aripiprazole dose by 50% major
CYP3A4 inducers (carbamazepine) reduce aripiprazole levels by ~70%; double aripiprazole dose major
CYP3A4 inhibitors increase aripiprazole levels moderate

Nursing Considerations

  1. Monitor for akathisia (subjective restlessness, inability to sit still) — distinguish from psychomotor agitation; akathisia responds to beta-blockers (propranolol) or benzodiazepines, not dose increase
  2. Metabolic monitoring is required but aripiprazole has a significantly better metabolic profile than olanzapine or quetiapine
  3. Assess for impulse control disorders: gambling, hypersexuality, compulsive eating — have occurred with aripiprazole; mechanism involves partial D2 agonism in reward pathways
  4. The long half-life means steady-state is not reached for 2 weeks; full clinical effect assessment requires this timeframe

Clinical Pearls

  • Aripiprazole's partial agonism mechanism makes it conceptually distinct from all other antipsychotics — it is a 'dopamine stabilizer' that provides antipsychotic effect with minimal EPS and metabolic burden
  • Aripiprazole lauroxil (Aristada) and aripiprazole monohydrate (Maintena) are long-acting injectable formulations dosed monthly or every 6 weeks, dramatically improving adherence in chronic schizophrenia

Safety Profile

Pregnancy use-with-caution
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

Agitation In Schizophrenia (IM) Antipsychotic Bipolar I Mania Irritability Associated With Autism Spectrum Disorder Major Depressive Disorder (adjunct) Schizophrenia Tourette's Syndrome
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