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pubmed-article:18094221pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:18094221pubmed:authorpubmed-author:KimKyoung-AhK...lld:pubmed
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pubmed-article:18094221pubmed:authorpubmed-author:LeeHeon-Jeong...lld:pubmed
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pubmed-article:18094221pubmed:articleTitleEffect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone.lld:pubmed
pubmed-article:18094221pubmed:affiliationDepartment of Clinical Pharmacology & Toxicology, Anam Hospital, Korea University College of Medicine, 126-1, Anam-dong 5-ga, Sungbuk-gu, Seoul 136-705, Korea.lld:pubmed
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