Pharm

Aripiprazole

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Aripiprazole, Abilify, Aristada

  • Indications
  1. Schizophrenia
  2. Bipolar Disorder
  3. Major Depression (adjunct in refractory cases)
  4. Autism (irritability)
  5. Tourette's Syndrome
  • Advantages
  1. Lower weight gain than other second generation Antipsychotic agents
  2. Lower diabetes and Hyperglycemia risk than other second generation Antipsychotic agents
  3. Lower risk of Hyperlipidemia and Hyperprolactinemia than other second generation Antipsychotic agents
  • Precautions
  1. Despite generic in 2015, price still approaches $800 per month
  2. Primary role remains as an Antipsychotic for Schizophrenia and Bipolar Disorder
    1. Only consider adjunctively in severe Major Depression refractory to other measures
  • Mechanism
  1. Atypical Antipsychotic (Second Generation agent)
  2. Dopamine D2 and D3 partial Agonist
  3. Serotonin 5HT1A partial Agonist
  4. Serotonin 5HT2A receptor Antagonist
  • Drug Interactions
  1. Metabolized by CYP3A3/4 and CYP2D6
  2. Increase Antipsychotic levels (toxicity risk): Monitor for Aripiprazole toxicity
    1. Clarithromycin
    2. Erythromycin
    3. Grapefruit juice
  3. CYP3A3/4 Inhibitors increase Antipsychotic levels (toxicity risk): Lower Aripiprazole dose to one quarter to one half dose
    1. Itraconazole
    2. Ketoconazole
    3. Quinidine
  4. CYP3A3/4 Inducers decrease Antipsychotic levels (lower efficacy)
    1. Double Aripiprazole dose over 1-2 weeks while taking these meds (and avoid longer than 2 weeks with IM Aripiprazole)
    2. Barbiturates
    3. Carbamazepine
    4. Phenytoin
  • Efficacy
  • Depression
  1. Major Depression remits in 25% of patients by 6 weeks (effects may be seen by 1 week)
  • Safety
  1. Unknown safety in pregnancy
  2. Unknown safety in Lactation
  • Adverse Effects
  1. Headache
  2. Restlessness or Agitation
  3. Insomnia
  4. Anxiety
  5. Extrapyramidal Side Effects in up to 17% of patients
  6. Akathisia
  7. Nausea
  8. Constipation
  9. Fatigue or sedation
  10. Impulse control behaviors (rare)
    1. Behaviors seen with other Dopamine Agonists (e.g. Compulsive Gambling, hypersexuality, shopping, eating)
    2. Moore (2014) JAMA Intern Med 174(12):1930-3 [PubMed]
  • Monitoring
  1. Oral Dosing
    1. Adult
      1. Start: 10-15 mg once daily
      2. Maximum dose: 30 mg/day
        1. Dose >15 mg do not appear more effective than the 15 mg dose
    2. Child (age 13 to 17 years)
      1. Start: 2 mg orally daily
      2. May increase to 5 mg daily after 2 days
      3. May increase to 10 mg daily after another 2 days
      4. Target: 10 mg/day
      5. Maximum: 15-30 mg/day (not more effective than 10 mg/day)
  2. Immediate Release IM Injection for Agitation
    1. Adults: 9.75 mg IM (range 5.25 to 15 mg IM)
    2. May repeat after 2 hours, up to maximum of 30 mg/day
  3. Monthly IM Dosing
    1. Trial oral dosing before administering IM Dose
    2. Oral dosing is coadministered only with the first IM dose
      1. Continue oral dose daily only for the first 14 days
    3. Abilify Maintena 400 mg IM once monthly
      1. Lower dose of 300 mg IM may be used to reduce adverse effects
  4. Every 2 Month IM Dosing
    1. Trial oral dosing before administering IM Dose
    2. Abilify Aristada
      1. Oral dosing is coadministered only with the first IM dose
        1. Continue oral dose daily only for the first 21 days
      2. Lower dose (equivalent to 10 mg/day): 441 mg IM monthly
      3. Higher dose (equivalent to 15 mg/day)
        1. Monthly: 662 mg IM
        2. Every 6 weeks: 882 mg IM
        3. Every 2 months: 1064 mg IM
    3. Abilify Asimtufii
      1. Dose 960 mg IM gluteal every 2 months
      2. Oral dosing is coadministered only with the first IM dose
        1. Continue oral dose daily only for the first 14 days
  • Dosing
  • MIscellaneous
  1. Major Depression (in refractory and atypical cases, as adjunctive therapy)
    1. Starting dose: 2-5 mg/day
    2. Maximum dose: 15 mg/day (up to 30 mg/day has been used)
  2. Tourette's Syndrome (for child age 6 to 18 years)
    1. Start: 2 mg orally daily
    2. May increase to 5 mg daily after 2 days
    3. May increase weekly to a maximum of 10 mg daily (if weight <50 kg) or 20 mg daily (if weight >50 kg)
  • References
  1. (2016) Med Lett Drugs Ther 58(1510): 160-5
  2. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 42-3
  3. Hamilton (2020) Tarascon Pocket Pharmacopoeia