A systematic review and combined analysis of therapeutic drug monitoring studies for oral paliperidone

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

Research output: Contribution to journalReview articlepeer-review

32 Scopus citations


Introduction: This article includes a combined analysis of therapeutic drug monitoring (TDM) studies and a review of the marketer’s data on pharmacological mechanisms. Areas covered: An article search led to the inclusion of 21 paliperidone studies in the systematic review plus 2 case reports. Paliperidone clearance was calculated from: 1) steady-state studies using concentration/dose (C/D) ratios, and 2) single-dose studies describing 24-h area under the curve calculations. The marketed extended-release formulation has 28% bioavailability. Calculated mean C/D ratios (ng/ml/mg/d) were: 1) 4.09 in 6 studies of 221 non-Korean and non-geriatric adult patients, 2) 2.59 in 2 studies of 100 Korean adult patients, and 3) 6.89 in 1 study with 15 elderly Japanese patients. The limited drug–drug interaction studies indicated that carbamazepine is a clinically relevant inducer requiring three times the dosage, and that valproate, probably an inhibitor, requires half the dosage. Renal impairment markedly decreased paliperidone elimination, and other antipsychotics should be considered. Expert Commentary: We recommend more use of: 1) paliperidone TDM in clinical practice, 2) TDM when moving from oral to long-acting paliperidone, 3) better designs for paliperidone TDM studies, 4) laboratory studies on paliperidone pharmacokinetic mechanisms, and 5) TDM studies comparing paliperidone and risperidone dosing.

Original languageEnglish
Pages (from-to)625-639
Number of pages15
JournalExpert Review of Clinical Pharmacology
Issue number6
StatePublished - Jun 3 2018

Bibliographical note

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


  • Antipsychotic agents/administration & dosage
  • antipsychotic agents/pharmacology
  • drug monitoring
  • paliperidone palmitate
  • risperidone/pharmacokinetics
  • schizoaffective disorder/drug therapy
  • schizophrenia/drug therapy

ASJC Scopus subject areas

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


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