Aripiprazole (Abilify)

Contents

Clinical Information

HALF-LIFE: Aripiprazole 74 hours; Active metabolite 94 hours

METABOLISM: Hepatic. Metabolized by CYP2D6 and CYP3A4

STARTING DOSE: 2mg-15mg daily

TARGET DOSING RANGE: 2mg-30mg PO daily

BEST TIME TO DOSE: Any

HOW TO DOSE:

Schizophrenia and Bipolar Mania: Initial 10mg-15mg PO daily. Max dose 30mg PO daily

Adjunct for depression: Initial 2mg-5mg PO daily. Increase dose by 5mg per day at intervals of >1 week. Max dose 15mg PO daily

Autism and Tourette’s disorder: Initial 2mg PO daily. Increase dose by 5mg/day at intervals of >1 week. Max dose 10mg-15mg PO daily

PREGNANCY: Minimal data on safety

BREASTFEEDING: Minimal data on safety

Side Effects

Akathisia (inner feeling of restlessness or urge to move), sedation, drowsiness, nausea, upset stomach, heartburn, diarrhea, tremors, muscle weakness, movement disorders, muscle cramping, restlessness, increased appetite, dry mouth, emotional “blunting,” seizures (very rare), lethargy, fatigue, headache, Neuroleptic Malignant Syndrome (Very rare), compulsive behaviors (such as compulsive gambling). Some of these side effects (e.g., nausea, jitteriness, restlessness, increased anxiety, upset stomach, headache, sedation, dry mouth, daytime fatigue) are common initially but typically go away after 5-7 days of consistently taking the medication as prescribed. 

FDA Indications

1) Schizophrenia, 13yo and older
2) Acute mania/mixed episodes, 10yo and older
3) Bipolar maintenance
4) Adjunct for Unipolar depression
5) Autism-related irritability, 6-17yo
6) Tourette’s disorder, 6-18yo
7) Acute agitation associated with schizophrenia or bipolar disorder (IM)

Off Label Uses: Bipolar Depression, Obsessive Compulsive Disorder, PTSD, Personality Disorders

Mechanism(s) of Action

Aripiprazole’s antipsychotic effects are hypothetically related to partial agonist actions at D2 receptor

Aripiprazole’s 5HT2A affinity is less than D2 affinity

Aripiprazole’s 5HT1A partial agonist actions are more potent than 5HT2A antagonist actions

Aripiprazole’s antidepressant effects are partially explained by 5HT1A partial agonism and 5HT7 antagonism

Additional Information

  • Usually not sedating (lacks M1 and H1 antagonism)
  • Minimal weight gain, rare dyslipidemia, rare insulin resistance (except in some children and adolescents)
  • Minimal to no QTc prolongation
  • Lower doses may be more activating than higher doses
  • Long acting depot formulations available (Maintena (monthly injection), Aristada (injection every 2-3 months)

References

  1. Cooper, J. R., Bloom, F. E., & Roth, R. H. (2003). The biochemical basis of neuropharmacology (8th ed.). New York, NY, US: Oxford University Press.
  2. Iversen, L. L., Iversen, S. D., Bloom, F. E., & Roth, R. H. (2009). Introduction to neuropsychopharmacology. Oxford: Oxford University Press.
  3. Puzantian, T., & Carlat, D. J. (2016). Medication fact book: for psychiatric practice. Newburyport, MA: Carlat Publishing, LLC.
  4. J. Ferrando, J. L. Levenson, & J. A. Owen (Eds.), Clinical manual of psychopharmacology in the medically ill(pp. 3-38). Arlington, VA, US: American Psychiatric Publishing, Inc.
  5. Schatzberg, A. F., & DeBattista, C. (2015). Manual of clinical psychopharmacology. Washington, DC: American Psychiatric Publishing.
  6. Schatzberg, A. F., & Nemeroff, C. B. (2017). The American Psychiatric Association Publishing textbook of psychopharmacology. Arlington, VA: American Psychiatric Association Publishing.
  7. Stahl, S. M. (2014). Stahl’s essential psychopharmacology: Prescriber’s guide (5th ed.). New York, NY, US: Cambridge University Press.
  8. Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY, US: Cambridge University Press.
  9. Whalen, K., Finkel, R., & Panavelil, T. A. (2015). Lippincotts illustrated reviews: pharmacology. Philadelphia, PA: Wolters Kluwer.