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Updated: Mar 13, 2026

Self-Administration of Drugs in Mouse Models of Feeding and Obesity
Published on: June 8, 2021
Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice
David Holthoewer1, Christoph Hiemke2, Ulrich Schmitt3
1Department of Psychiatry and Psychotherapy, University Medical Center of the Johannes Gutenberg-University Mainz, Untere Zahlbacher Strasse 8, 55101 Mainz, Germany. holthoewer@psychiatrie.klinik.uni-mainz.de.
Abstract:
Pharmacokinetic interactions, e.g. modulation of drug transporters like P-glycoprotein at the blood-brain barrier, can be a reason for treatment non-response. This study focuses on the influence of induction of drug transporters on the disposition of the antipsychotic drugs risperidone and 9-hydroxyrisperidone. Brain and serum concentrations of risperidone and its active metabolite 9-hydroxyrisperidone, which are known P-glycoprotein substrates, were measured after drug transporter induction with rifampicin, dexamethasone or 5-pregnene-3beta-ol-20-on-16alpha-carbonitrile using high performance liquid chromatography. Disposition of risperidone and 9-hydroxyrisperidone was dramatically decreased in mouse brain and serum after drug transporter induction. The metabolism of risperidone was also affected.
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