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Serum concentrations of paliperidone versus risperidone and clinical effects

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

Purpose

The major aim of this multicenter retrospective analysis was to examine the relationship between paliperidone serum concentrations and clinical effects in patients treated with this new antipsychotic drug. Intra-individual variability in trough serum concentrations was also analyzed in patients under treatment with either the paliperidone-extended release (ER) formulation or the risperidone immediate-release formulation.

Methods

Data were obtained from 217 patients of four medical centers who were being followed by therapeutic drug monitoring (TDM). Serum concentrations were associated with clinical response using Clinical Global Impressions (CGI) scores.

Results

The mean concentration of paliperidone was 36 ± 25 ng/ml, and the mean dose corrected concentration (C/D) was 4.7 ± 2.9 ng/ml/mg. Among patients receiving paliperidone as antipsychotic monotherapy and who showed at least a much improved level according to the CGI scores, the 25th–75th percentiles of paliperidone concentrations were 20–52 ng/ml; these were very similar to the recommended therapeutic range of 20–60 ng/ml for risperidone plus 9-hydroxy-risperidone (active moiety). In 13 patients treated with paliperidone ER and 17 patients treated with risperidone, all of whom had repeated drug measurements, the intra- and inter-individual variabilities of trough serum concentrations were similar for the paliperidone and risperidone active moiety, ranging between 30 and 35%.

Conclusion

Based on these results, we conclude that risperidone and paliperidone have a similar therapeutic range and similar intra-individual variability in terms of trough serum levels. For treatment optimization, monitoring of plasma concentrations may be as useful for paliperidone as for risperidone.

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Authors and Affiliations

  1. Department of Psychiatry and Psychotherapy, University Medical Center, Johannes Gutenberg University Mainz, Untere Zahlbacher Str. 8, 55131, Mainz, Germany

    Yasmin Nazirizadeh, Friederike Vogel & Christoph Hiemke

  2. Clinical Pharmacology/Psychopharmacology of the Department of Psychiatry, Psychosomatic and Psychotherapy, University of Regensburg, Regensburg, Germany

    Wolfgang Bader & Ekkehard Haen

  3. Department of Psychiatry and Psychotherapy, University of Würzburg, Würzburg, Germany

    Bruno Pfuhlmann

  4. Department of Psychiatry and Psychotherapy, RWTH Aachen University and JARA–Brain: Translational Brain Medicine, Aachen, Germany

    Gerhard Gründer & Michael Paulzen

  5. Hospital for Psychiatry and Psychotherapy, Ludwig-Maximilians-Universität, Munich, Germany

    Markus Schwarz

  6. Experimental Psychiatry Unit, Department of General Psychiatry and Social Psychiatry, Medical University Innsbruck, Innsbruck, Austria

    Gerald Zernig

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  1. Yasmin Nazirizadeh
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Correspondence to Christoph Hiemke.

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Nazirizadeh, Y., Vogel, F., Bader, W. et al. Serum concentrations of paliperidone versus risperidone and clinical effects. Eur J Clin Pharmacol 66, 797–803 (2010). https://doi.org/10.1007/s00228-010-0812-7

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  • DOI: https://doi.org/10.1007/s00228-010-0812-7

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