Preclinical study of a potent P-glycoprotein and cytochrome P450 enzyme inducer rifampicin changing pharmacokinetic parameters of risperidone and its metabolite, 9-hydroxyrisperidone, using a rat model

The objective of the present investigation is to examine the effects of rifampicin, which is a P-glycoprotein (P-gp) and cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, in rats. To determine the plasma levels of risperidone an...

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Bibliographic Details
Published in:Journal of pharmaceutical investigation 2012, 42(6), , pp.345-351
Main Authors: Lee, Kyoung Sin, Park, Jung Hyun, Lee, Hwa Jeong, Rhie, Sandy
Format: Article
Language:English
Subjects:
Biomedical and Life Sciences
Biomedicine
Research Article
약학
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Summary:The objective of the present investigation is to examine the effects of rifampicin, which is a P-glycoprotein (P-gp) and cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, in rats. To determine the plasma levels of risperidone and 9-hydroxyrisperidone in rats, a high performance liquid chromatographic method was developed using a liquid–liquid acid back extraction. After pretreated with rifampicin (600 mg/kg) for 6 days, the mean C max and AUC 0–10 values of risperidone were significantly decreased and the Cl t of the drug was significantly increased compared with control ( p  
ISSN:2093-5552
2093-6214
DOI:10.1007/s40005-012-0045-0