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Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice
Department of Psychiatry and Psychotherapy, University Medical Center of the Johannes Gutenberg-University Mainz, Untere Zahlbacher Strasse 8, 55101 Mainz, Germany
* Author to whom correspondence should be addressed.
Received: 24 May 2010; Accepted: 1 June 2010 / Published: 2 June 2010
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.
Keywords: drug transporter; P-glycoprotein; risperidone; 9-hydroxyrisperidone; antipsychotics; disposition
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Holthoewer, D.; Hiemke, C.; Schmitt, U. Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice. Pharmaceutics 2010, 2, 258-274.
Holthoewer D, Hiemke C, Schmitt U. Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice. Pharmaceutics. 2010; 2(2):258-274.
Holthoewer, David; Hiemke, Christoph; Schmitt, Ulrich. 2010. "Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice." Pharmaceutics 2, no. 2: 258-274.