A systematic review and combined analysis of therapeutic drug monitoring studies for long-acting paliperidone

Georgios Schoretsanitis, Edoardo Spina, Christoph Hiemke, Jose de Leon

Research output: Contribution to journalReview articlepeer-review

38 Scopus citations


Introduction: This is a combined analysis of therapeutic drug monitoring (TDM) studies of long-acting injectable paliperidone formulations: monthly (PP1M) and three-month (PP3M) injections. Areas covered: Fourteen PP1M articles and one PP3M article were identified. Using the paliperidone concentration/dose (C/D) ratio as a measure of clearance provided a weighted mean of 7.7 ng/ml per mg/day among 69 patients from three steady-state PP1M studies (twice as high as oral paliperidone). C/D ratios were: 1) higher by a factor of 1.26 in 12 geriatric patients, 2) lower in obese patients, and 3) 50% lower in three patients taking carbamazepine. No clinically meaningful PP3M pharmacokinetic data have been published. Expert commentary: Half-life studies and more TDM PP1M studies using steady state are urgently needed. Early TDM studies may help orient PP1M dosing but steady state may not be reached until after the ninth injection (8 months). PP3M may take > 1 year to reach steady state. Any clinician considering switching patients to PP1M: 1) should switch from oral risperidone to PP1M rather than from oral paliperidone to PP1M, and 2) become proficient in paliperidone TDM to use during switches. TDM is highly recommended for patients with abnormal clearance (from obesity, geriatric age, or potent inducers).

Original languageEnglish
Pages (from-to)1237-1253
Number of pages17
JournalExpert Review of Clinical Pharmacology
Issue number12
StatePublished - Dec 2 2018

Bibliographical note

Funding Information:
No commercial organizations had any role in the writing of this paper for publication. In the past few years, E. Spina has participated in speakers/ advisory boards and lectured, supported by Arcapharma, Janssen Pharmaceuticals, Lundbeck, Otsuka and Recordati. C. Hiemke has received speaker´s or consultancy fees from the following pharmaceutical companies: Janssen and Servier. He declares no conflict of interest related to this article. J. de Leon personally develops his presentations for lecturing, has never lectured using any pharmaceutical or pharmacogenetic company presentations, and has never been a consultant for pharmacogenetic or pharmaceutical companies. In the past, J. de Leon received researcher-initiated grants from Eli Lilly (one ended in 2003 and the other, as coinvestigator, ended in 2007); from Roche Molecular Systems, Inc. (ended in 2007); and, in a collaboration with Genomas, Inc., from the NIH Small Business Innovation Research program (ended in 2010). J. de Leon has been on the advisory boards of Bristol-Myers Squibb (2003/04) and AstraZeneca (2003). Roche Molecular Systems supported one of his educational presentations, which was published in a peer-reviewed journal (2005). His lectures were supported once by Sandoz (1997), twice by Lundbeck (1999 and 1999), twice by Pfizer (2001 and 2001), three times by Eli Lilly (2003, 2006, and 2006), twice by Janssen (2000 and 2006), once by Bristol-Myers Squibb (2006), and seven times by Roche Molecular Systems, Inc. (once in 2005 and six times in 2006). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript.

Publisher Copyright:
© 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.


  • Antipsychotic agents/administration & dosage
  • antipsychotic agents/pharmacology
  • delayed-action preparations
  • drug monitoring
  • injections
  • paliperidone palmitate
  • risperidone/administration & dosage
  • risperidone/blood
  • risperidone/metabolism
  • risperidone/pharmacokinetics
  • schizoaffective disorder/drug therapy
  • schizophrenia/drug therapy

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics (all)
  • Pharmacology (medical)


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