Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone
- Authors
- Kim, Kyoung-Ah; Park, Pil-Whan; Liu, Kwang-Hyeon; Kim, Kwon-Bok; Lee, Heon-Jeong; Shin, Jae-Gook; Park, Ji-Young
- Issue Date
- 1월-2008
- Publisher
- SAGE PUBLICATIONS INC
- Keywords
- rifampin; risperidone; 9-hydroxyrisperidone; cytochrome P450 3A (CYP3A); P-glycoprotein; drug interaction
- Citation
- JOURNAL OF CLINICAL PHARMACOLOGY, v.48, no.1, pp.66 - 72
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF CLINICAL PHARMACOLOGY
- Volume
- 48
- Number
- 1
- Start Page
- 66
- End Page
- 72
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/124534
- DOI
- 10.1177/0091270007309888
- ISSN
- 0091-2700
- Abstract
- The authors studied the effect of rifampin, a dual inducer of CYP3A and P-glycoprotein, on the pharmacokinetics and pharmacodynamics of risperidone in humans. Ten healthy male subjects were treated daily for 7 days with 600 mg rifampin or with placebo. On day 6, a single dose of 1 mg risperidone was administered. Plasma risperidone and 9-hydroxyrisperidone concentrations were measured. Rifampin significantly decreased the mean area under the plasma concentration-time curve by 51% for risperidone. by 43% for 9-hydroxyrisperidone, and by 45% for the active moieties (risperidone + 9-hydroxyrisperidone). Rifampin also decreased the peak plasma concentration of risperidone by 38%, 9-hydroxyrisperidone by 46%, and the active moieties by 41%. The apparent oral clearance of risperidone approximately doubled after rifampin treatment. Thus, rifampin reduced the exposure to risperidone, probably because of a decrease in its bioavailability through the induction of CYP3A and probably P-glycoprotein.
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Collections - Graduate School > Department of Biomedical Sciences > 1. Journal Articles
- College of Medicine > Department of Medical Science > 1. Journal Articles
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