Paliperidone (Invega)

Contents

Clinical Information

 

HALF-LIFE: 23 hours

METABOLISM: Not metabolized by Liver, therefore few drug-drug interactions

STARTING DOSE: 6mg PO daily

TARGET DOSING RANGE: 6mg-9mg per day

BEST TIME TO DOSE: Any

HOW TO DOSE:
>> Initial 6mg PO daily for one week then 9mg starting week two
>> May increase to 12mg PO daily starting week three (if needed)

Long-acting depot formulations available:

Monthly Injection: Invega Sustenna

Initiation dose: 234mg IM

Booster dose: 156mg IM 4-12 days after initiation dose

Maintenance dose: 117mg IM q3-5 weeks

Three month Injection: Invega Trinza

PREGNANCY: Minimal data on safety.

BREASTFEEDING: Minimal data on safety.

Side Effects

Sedation, dizziness, dry mouth, nausea, upset stomach, metabolic side effects (insulin resistance), weight gain, increased appetite, elevated prolactin levels (menstrual irregularities, sexual dysfunction, breast tenderness, headaches, galactorrhea), orthostatic hypotension, movement disorders, seizures (rare), Neuroleptic Malignant Syndrome (Rare), Arrhythmias (rare), extrapyramidal symptoms (parkinsonism, dystonia), akathisia/restlessness

FDA Indications

  1. Schizophrenia, 12yo and older
  2. Schizoaffective disorder

Off Label Uses: Bipolar Disorder, Agitation

Mechanism(s) of Action

  • Dopamine 2 (D2) Receptor Antagonist, 5HT2A Antagonist, 5HT2C Antagonist, alpha-1 receptor antagonist, alpha-2 receptor antagonist, H1 receptor antagonist

Additional Information

  • Paliperidone is the active metabolite of risperidone (9-hydroxy-risperidone)
  • Paliperidone comes in a controlled/sustained-release oral formulation and can be dosed once daily 

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.