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Pharmaceutics 2010, 2(2), 258-274; doi:10.3390/pharmaceutics2020258
Article

Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice

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Received: 24 May 2010; Accepted: 1 June 2010 / Published: 2 June 2010
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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 drug transporter; P-glycoprotein; risperidone; 9-hydroxyrisperidone; antipsychotics; disposition
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Holthoewer, D.; Hiemke, C.; Schmitt, U. Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice. Pharmaceutics 2010, 2, 258-274.

AMA Style

Holthoewer D, Hiemke C, Schmitt U. Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice. Pharmaceutics. 2010; 2(2):258-274.

Chicago/Turabian Style

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.


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