DOI: 10.1055/a-1221-5293
Original Paper

Lack of Smoking Effects on Pharmacokinetics of Oral Paliperidone-analysis of a Naturalistic Therapeutic Drug Monitoring Sample

1  The Zucker Hillside Hospital, Psychiatry Research, Northwell Health, Glen Oaks, New York, USA
2  Clinical Pharmacology, Department of Psychiatry and Psychotherapy and Department of Pharmacology and Toxicology, University of Regensburg, Regensburg, Germany
Andreas Conca
3  Servizio Psichiatrico del Comprensorio Sanitario di Bolzano, Bolzano, Italy
Daria Piacentino
4  Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, The National Institutes of Health, Bethesda, USA
Florian Ridders
1  The Zucker Hillside Hospital, Psychiatry Research, Northwell Health, Glen Oaks, New York, USA
Christoph Hiemke
5  Department of Psychiatry and Psychotherapy and Institute of Clinical Chemistry and Laboratory Medicine, University Medical Center of Mainz, Germany
Gerhard Gründer
6  Department of Molecular Neuroimaging, Central Institute of Mental Health, Medical Faculty Mannheim, University of Heidelberg, Mannheim, Germany
Michael Paulzen
7  Alexianer Hospital Aachen, Aachen, Germany, and Department of Psychiatry, Psychotherapy and Psychosomatics, RWTH Aachen University, and JARA – Translational Brain Medicine, Aachen, Germany
› Author Affiliations
Funding Information: This research did not receive any funding.


Introduction Major smoking effects have been reported for a series of psychotropic agents, mainly including substrates of CYP450 1A2, although smoking may also affect alternative metabolic pathways. To our knowledge, smoking effects on paliperidone pharmacokinetics have not been assessed yet.

Methods We compared plasma concentrations of paliperidone as well as dose-corrected-plasma concentrations (C/D) from a naturalistic database between smokers and nonsmokers using nonparametrical tests, such as the Mann-Whitney U-test (MWU). Additionally, we compared light and heavy smokers with nonsmokers separately.

Results Comparing 55 smokers with 37 nonsmokers treated with oral paliperidone, no differences in the percentage of females, age, body weight, body mass index, and daily paliperidone dose were reported (p=0.709 for χ2, p=0.26, p=0.38, p=0.67, and p=0.8 for MWU). No differences were detected in plasma concentrations or C/D values (p=0.50 and p=0.96 for MWU). Likewise, differences in daily dose, plasma concentrations, or C/D values were not significant between light smokers (n=17) and nonsmokers (p=0.61, p=0.81, and p=0.33 for MWU) or heavy smokers (n=22) and nonsmokers (p=0.874, p=0.38, and p=0.59; MWU in all cases).

Discussion Paliperidone is not affected by smoking, and paliperidone dose-adjustments in smokers may not be necessary. This may be seen as an essential difference to risperidone, whose cytochrome-mediated metabolism might be affected by smoking.

Publication History

Received: 18 June 2020
Received: 11 May 2020

Accepted: 09 July 2020

Publication Date:
06 August 2020 (online)

© Georg Thieme Verlag KG
Stuttgart · New York