6533b861fe1ef96bd12c4397

RESEARCH PRODUCT

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

Ulrich SchmittDavid HolthoewerChristoph Hiemke

subject

Drugmedia_common.quotation_subjectmedicine.medical_treatmentlcsh:RS1-441Pharmaceutical ScienceP-glycoproteinPharmacologyArticlelcsh:Pharmacy and materia medicaPharmacokineticsMedicineAntipsychoticDexamethasoneActive metaboliteP-glycoproteinmedia_commonrisperidoneRisperidonebiologybusiness.industryTransporterdrug transporterantipsychoticsdispositionbiology.protein9-hydroxyrisperidonebusinessmedicine.drug

description

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.

yearjournalcountryeditionlanguage
2010-06-02Pharmaceutics
https://doi.org/10.3390/pharmaceutics2020258