Skip to main content
SpringerLink
Log in

Intramuscular Paliperidone Palmitate

  • Adis Drug Profile
  • Published:
CNS Drugs Aims and scope Submit manuscript

Abstract

Intramuscular paliperidone palmitate is a long-acting, atypical antipsychotic that is indicated in the US for the acute and maintenance therapy of adult patients with schizophrenia. Paliperidone is the major active metabolite of risperidone.

The noninferiority of flexible doses of intramuscular paliperidone palmitate 39–156 mg to flexible doses of intramuscular long-acting risperidone 25–50 mg was not established in an initial 53-week study. However, these data were utilized to optimize the intramuscular paliperidone palmitate dosage regimen.

In four randomized, double-blind studies, intramuscular paliperidone palmitate 39–234 mg was generally effective in the treatment of adult patients with acute schizophrenia, inducing significantly greater improvements from baseline in the mean Positive and Negative Syndrome Scale (PANSS) total score than placebo (primary endpoint).

In general, intramuscular paliperidone palmitate recipients achieved significantly better outcomes than placebo recipients with regard to the PANSS subscale, PANSS factor, Personal and Social Performance scale and Clinical Global Impressions-Severity scale scores.

As maintenance therapy, intramuscular paliperidone palmitate 39–156 mg was significantly more effective than placebo in delaying the time to the first relapse of schizophrenia symptoms in adult patients, according to the results of a randomized, double-blind study.

The beneficial effects of intramuscular paliperidone palmitate therapy on the PANSS total score were sustained in a 52-week noncomparative extension phase of the maintenance therapy study.

Intramuscular paliperidone palmitate 39–234 mg was generally well tolerated in adult patients with schizophrenia.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Table I

Similar content being viewed by others

References

  1. Lieberman JA, Fenton WS. Delayed detection of psychosis: causes, consequences, and effect on public health. Am J Psychiatry 2000 Nov; 157(11): 1727–30

    Article  PubMed  CAS  Google Scholar 

  2. World Health Organization. Schizophrenia [online]. Available from URL: http://www.who.int/mental_health/management/schizophrenia/en/ [Accessed 2009 Jul 20]

  3. Ho B-C, Alicata D, Mola C, et al. Hippocampus volume and treatment delays in first-episode schizophrenia. Am J Psychiatry 2005 Aug; 162(8): 1527–9

    Article  PubMed  Google Scholar 

  4. Keith SJ, Pani L, Nick B, et al. Practical application of pharmacotherapy with long-acting risperidone for patients with schizophrenia. Psychiatr Serv 2004 Sep; 55(9): 997–1005

    Article  PubMed  Google Scholar 

  5. Hough D, Lindenmayer J-P, Gopal S, et al. Safety and tolerability of deltoid and gluteal injections of paliperidone palmitate in schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 2009; 33: 1022–31

    Article  PubMed  CAS  Google Scholar 

  6. Nasrallah HA. The case for long-acting antipsychotic agents in the post-CATIE era. Acta Psychiatr Scand 2007 Apr; 115(4): 260–7

    Article  PubMed  CAS  Google Scholar 

  7. Fleischhacker WW, Gopal S, Samtani MN, et al. Optimization of the dosing strategy for the long-acting injectable antipsychotic paliperidone palmitate: results of two randomized double-blind studies and population pharmacokinetic simulations [poster]. American Psychiatric Association Annual Meeting; 2009 May 16–21; San Francisco (CA)

  8. Samtani MN, Vermeulen A, Stuyckens K. Population pharmacokinetics of intramuscular paliperidone palmitate in patients with schizophrenia: a novel once-monthly, long-acting formulation of an atypical antipsychotic. Clin Pharmacokinet 2009; 48(9): 585–600

    Article  PubMed  CAS  Google Scholar 

  9. Ortho-McNeil-Janssen Pharmaceuticals Inc. FDA approves Invega® Sustenna™ for the acute and maintenance treatment of schizophrenia [online]. Available from URL: http://www.janssen.com/janssen/news_release.html?item=073109_1 [Accessed 2009 Aug 5]

  10. Ortho-McNeil-Janssen Pharmaceuticals Inc. Invega® Sustenna™ (paliperidone palmitate) extended-release injectible suspension: prescribing information [online]. Available from URL: http://www.invegasustenna.com/invegasustenna/shared/pi/invegasustenna.pdf [Accessed 2009 Aug 4]

  11. Gopal S, Vijapurkar U, Lim P, et al. Long-term efficacy, safety, and tolerability of paliperidone palmitate in patients with schizophrenia [abstract no. NR1-031 plus poster]. Annual Meeting of the College of Psychiatric and Neurologic Pharmacists; 2009 Apr 19–22; Jacksonville (FL)

  12. Yang LP, Plosker GL. Paliperidone extended release. CNS Drugs 2007; 21(5): 417–25; discussion 426-7

    Article  PubMed  CAS  Google Scholar 

  13. Karlsson P, Dencker E, Nyberg S, et al. Pharmacokinetics and dopamine D2 and serotonin 5-HT2A receptor occupancy of paliperidone in healthy subjects [abstract no. P.1.053]. Eur Neuropsychopharmacol 2005 Oct; 15Suppl. 3: S 386. Plus poster presented at the 18th European Congress of Neuropsychopharmacology; 2005 Oct 22–26; Amsterdam

    Google Scholar 

  14. Remington G, Mamo D, Labelle A, et al. A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone. Am J Psychiatry 2006 Mar; 163(3): 396–401

    Article  PubMed  Google Scholar 

  15. Kapur S, Zipursky R, Jones C, et al. Relationship between dopamine D2 occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia. Am J Psychiatry 2000 Apr; 157(4): 514–20

    Article  PubMed  CAS  Google Scholar 

  16. Kapur S, Zipursky RB, Remington G. Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry 1999 Feb; 156(2): 286–93

    PubMed  CAS  Google Scholar 

  17. Pandina G, Lindenmayer J, Lull J, et al. A randomized, double-blind, placebo-controlled, dose-response study to assess efficacy and safety of paliperidone palmitate in adult subjects with schizophrenia [abstract plus poster]. 12th International Congress on Schizophrenia Research; 2009 Mar 28–Apr 1; San Diego (CA)

  18. Cleton A, Rossenu S, Hough D, et al. Assessment of the dose proportionality of paliperidone palmitate 25, 50, 100 and 150 mg eq., a new long-acting injectable antipsychotic following administration in the deltoid or gluteal muscles [abstract no. PI-74]. Clin Pharmacol Ther 2008 Mar; 83Suppl. 1: S 31. Plus poster presented at the American Society for Clinical Pharmacology and Therapeutics; 2008 Apr 2–5; Orlando (FL)

    Google Scholar 

  19. Cleton A, Rossenu S, Hough D, et al. Evaluation of the pharmacokinetic profile of gluteal versus deltoid intramuscular injections of paliperidone palmitate 100mg equivalent in patients with schizophrenia [abstract no. PI-75]. Clin Pharmacol Ther 2008 Mar; 83Suppl. 1: S 31. Plus poster presented at the American Society for Clinical Pharmacology and Therapeutics; 2008 Apr 2–5; Orlando (FL)

    Google Scholar 

  20. Kern-Sliwa J, Samtani MN, Haskins JT, et al. Initiation dosing of deltoid intramuscular paliperidone palmitate in schizophrenia: pharmacokinetic rationale based on modeling and simulation [abstract no. NR1-046 plus poster]. Annual Meeting of the College of Psychiatric and Neurologic Pharmacists; 2009 Apr 19–22; Jackonville (FL)

  21. Haskins JT, Samtani MN, Alphs L, et al. Maintenance dosing of once-monthly (4-weekly) paliperidone palmitate in schizophrenia: pharmacokinetic rationale based on population simulations [abstract no. NR1-036 plus poster]. Annual Meeting of the College of Psychiatric and Neurologic Pharmacists; 2009 Apr 19–22; Jacksonville (FL)

  22. Samtani MN, Gopal S, Kern-Sliwa J, et al. Management of missed paliperidone palmitate doses based on pharmacokinetic modeling and simulation [poster]. 49th Annual New Clinical Drug Evaluation Unit Meeting; 2009 Jun 29–Jul 2; Hollywood (FL)

  23. Nasrallah HA, Gopal S, Quiroz JA, et al. Efficacy and safety of three doses of paliperidone palmitate, an investigational long-acting injectable antipsychotic, in schizophrenia [abstract NR4-036 plus poster]. 161st Annual Meeting of the American Psychiatric Association; 2008 May 3–8; Washington, DC

  24. Kramer M, Litman R, Hough D, et al. Paliperidone palmitate, a potential long-acting treatment for patients with schizophrenia: results of a randomized, double-blind, placebo-controlled efficacy and safety study. Int J Neuropsychopharmacol. Epub 2009 Nov 27

  25. Johnson & Johnson Pharmaceutical Research & Development L.L.C. A study to evaluate the effectiveness and safety of 3 doses of paliperidone palmitate in treating subjects with schizophrenia [ClinicalTrials.gov identifier NCT00210548]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://clinicaltrials.gov [Accessed 2009 Oct 8]

  26. Johnson & Johnson Pharmaceutical Research & Development L.L.C. A study to evaluate the effectiveness and safety of 3 doses of paliperidone palmitate in treating subjects with schizophrenia [online]. Available from URL: http://download.veritasmedicine.com/PDF/CR002353_CSR.pdf [Accessed 2009 Oct 8]

  27. Hough D, Gopal S, Vijapurkar U, et al. Paliperidone palmitate maintenance treatment in delaying the time-to-relapse in patients with schizophrenia: a randomized, double-blind, placebo-controlled study. Schizophr Res. Epub 2009 Dec 1

  28. Johnson & Johnson Pharmaceutical Research & Development L.L.C. Efficacy and safety of a long acting anti-psychotic versus placebo in patients with schizophrenia [ClinicalTrials.gov identifier NCT00101634]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://www.clinicaltrials.gov [Accessed 2009 Dec 15]

  29. Johnson & Johnson Pharmaceutical Research & Development L.L.C. Efficacy and safety of a long acting anti-psychotic versus placebo in patients with schizophrenia [online]. Available from URL: http://download.veritasmedicine.com/PDF/CR003562_CSR.pdf [Accessed 2009 Dec 15]

  30. Alphs L, Bossie C, Kern-Sliwa J, et al. Paliperidone palmitate: clinical response in subjects with schizophrenia with recent vs. longer-term duration of illness [abstract no. NR6-027 plus poster]. 162nd Annual Meeting of the American Psychiatric Association; 2009 May 16–21; San Francisco (CA)

  31. Data on file, Ortho-McNeil-Janssen Pharmaceuticals Inc., 2009

  32. American Psychiatric Association. Diagnostic and statistical manual of mental disorders. 4th ed. Washington, DC: American Psychiatric Association, 1994

    Google Scholar 

  33. American Psychiatric Association. Diagnostic and statistical manual of mental disorders. 4th ed., text revision. Washington, DC: American Psychiatric Association, 2000

    Google Scholar 

Download references

Acknowledgements and Disclosures

This manuscript was reviewed by: W. Fleischhacker, Biological Psychiatry Division, Department of Psychiatry and Psychotherapy, Medical University of Innsbruck, Innsbruck, Austria; J.-P. Lindenmayer, Manhattan Psychiatric Center-Nathan Kline Institute for Psychiatric Research, Psychopharmacology Research Unit, New York University, New York, New York, USA; H.A. Nasrallah, Department of Psychiatry, University of Cincinnati College of Medicine, Cincinnati, Ohio, USA; D.M. Taylor, Pharmacy Department, Maudsley Hospital, London, UK.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Author information

Authors and Affiliations

  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand

    Sheridan M. Hoy, Lesley J. Scott & Gillian M. Keating

Authors
  1. Sheridan M. Hoy
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Lesley J. Scott
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Gillian M. Keating
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Sheridan M. Hoy.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Hoy, S.M., Scott, L.J. & Keating, G.M. Intramuscular Paliperidone Palmitate. CNS Drugs 24, 227–244 (2010). https://doi.org/10.2165/11203810-000000000-00000

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/11203810-000000000-00000

Keywords

Search

Navigation