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Paliperidone

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Paliperidone, Paliperidone Palmitate, Invega, Invega Sustenna, Invega Trinza

  • See Also
  1. Antipsychotic Medication
  2. Psychosis
  3. Risperidone
  • Indications
  1. Schizophrenia
  • Mechanism
  1. Atypical Antipsychotic, a benzisoxazole derivative, and active metabolite of Risperidone
  2. Dopamine D2 Receptor Antagonist
  3. Serotonin 5HT2 Receptor Antagonist
  1. Child Oral Dosing (age 12 to 17 years old)
    1. Start 3 mg orally each morning
    2. May increase by 3 mg/day up to every 5 days to maximum of 6 mg/day (max 12 mg/day if weight >=51 kg)
  2. Adult Oral Dosing
    1. Start 6 mg orally each morning (may consider starting at 3 mg)
    2. May increase by 3 mg/day up to every 5 days to maximum of 12 mg/day
    3. Renal Dosing
      1. CrCl 50 to 79 ml/min: Start 3 mg/day (maximum 6 mg/day)
      2. CrCl 10 to 50 ml/min: Start 1.5 mg/day (maximum 3 mg/day)
  3. Adult Sustained Release Monthly Injection (Invega Sustenna)
    1. Trial oral dosing before IM dosing
    2. Start 234 mg IM in Deltoid Muscle or Gluteal Muscle
    3. Next, in one week, administer 156 mg IM in Deltoid Muscle or Gluteal Muscle
    4. Next administer 117 mg IM in Deltoid Muscle or Gluteal Muscle every month
      1. Adjust dose range 78 mg to 234 mg IM monthly depending on response and tolerability
      2. Doses as low as 39 mg IM monthly may be effective
    5. Renal Dosing
      1. CrCl 50 to 79 ml/min: First 156 mg IM, second 117 mg IM, then 78 mg IM
      2. CrCl 50 ml/min: Avoid Invega Sustenna
  4. Adult Sustained Release Quarterly Injection (Invega Trinza)
    1. Trial Invega Sustenna IM dosing for at least 4 months before starting Invega Trinza
    2. Invega Trinza dosing is based on prior Sustenna dosing
      1. Sustenna 78 mg IM qMonth: Use Trinza 273 mg IM every 3 months
      2. Sustenna 117 mg IM qMonth: Use Trinza 410 mg IM every 3 months
      3. Sustenna 156 mg IM qMonth: Use Trinza 546 mg IM every 3 months
      4. Sustenna 234 mg IM qMonth: Use Trinza 819 mg IM every 3 months
    3. Renal Dosing
      1. CrCl 50 to 79 ml/min: Transition from renally appropriate Invega Sustenna dose
      2. CrCl 50 ml/min: Avoid Invega Trinza
  5. Adult Extended Release Biannual Injection (Invega Hafyera)
    1. Trial Invega Sustenna >=4 months (or Trinza >=3 months) before starting Invega Hafyera
    2. Invega Hafyera dosing is based on prior Sustenna dosing
      1. Sustenna 156 mg qMonth or Invega 546 q3month: Use Hafyera 1092 mg IM every 6 months
      2. Sustenna 234 mg qMonth or Invega 819 q3month: Use Hafyera 1560 mg IM every 6 months
  • Adverse Effects
  1. See Antipsychotic Medication
  2. Similar adverse effects to Risperidone (Paliperidone's parent drug)
  3. Increased Serum Prolactin
  4. Extrapyramidal Side Effects
  5. Nausea
  6. Somnolence
  7. Dizziness
  8. Tachycardia
  9. QTc Prolongation
  10. Weight gain
  11. Hyperglycemia and increased risk of Diabetes Mellitus
  • Drug Interactions
  1. Metabolized by CYP3A4 and CYP2D6
  2. Inhibits P-Glycoprotein (as does Risperidone)
  • Safety
  1. Pregnancy Category C
  2. Avoid in Lactation
  • Resources
  1. Paliperidone Extended Release Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=7b8e5b26-b9e4-4704-921b-3c3c0d159916
  2. Paliperidone Sustenna Extended Release Monthly IM Injection (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1af14e42-951d-414d-8564-5d5fce138554
  3. Paliperidone Trinza Extended Release quarterly IM Injection (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c39e65d7-fa44-4e4c-8b12-a654d3ed0eae
  4. Paliperidone Hafyera Extended Release Biannual IM Injection (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6cd61892-d2cb-434d-83ed-5c1b2c4e7a0b
  • 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