Effect of Rifampin, an Inducer of CYP3A and P-glycoprotein, on the Pharmacokinetics of Risperidone

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...

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Bibliographic Details
Published in:Journal of clinical pharmacology 2008-01, Vol.48 (1), p.66-72
Main Authors: Kim, Kyoung-Ah, Park, Pil-Whan, Liu, Kwang-Hyeon, Kim, Kwon-Bok, Lee, Heon-Jeong, Shin, Jae-Gook, Park, Ji-Young
Format: Article
Language:English
Subjects:
9-hydroxyrisperidone
Administration, Oral
Adult
Alleles
Area Under Curve
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
Cross-Over Studies
Cytochrome P-450 CYP2D6 - genetics
Cytochrome P-450 CYP3A - metabolism
cytochrome P450 3A (CYP3A)
Dosage and administration
drug interaction
Genotype
Half-Life
Humans
Isoxazoles - blood
Isoxazoles - metabolism
Male
Metabolic Clearance Rate
P-glycoprotein
Paliperidone Palmitate
Pharmacokinetics
Polymerase Chain Reaction
Polymorphism, Restriction Fragment Length
Pyrimidines - blood
Pyrimidines - metabolism
Rifampin
Rifampin - administration & dosage
Rifampin - pharmacology
Risperidone
Risperidone - blood
Risperidone - metabolism
Risperidone - pharmacokinetics
Time Factors
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Summary: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.
ISSN:0091-2700
1552-4604
DOI:10.1177/0091270007309888