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

From the Department of Clinical Pharmacology & Toxicology (Dr K-A Kim, Dr J-Y Park) and Department of Psychiatry (Dr Lee), Anam Hospital, Korea University College of Medicine, Seoul; Department of Laboratory Medicine, Gachon Medical School Gil Medical Center, Incheon (Dr P-W Park); and Department of Pharmacology and Pharmacogenomics Research Center, Inje University College of Medicine, Busan (Dr Shin, Dr Liu, Mr K-B Kim), Korea.

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.

Key Words: rifampin • risperidone • 9-hydroxyrisperidone • cytochrome P450 3A (CYP3A) • P-glycoprotein • drug interaction

Address for reprints: Ji-Young Park, MD, PhD, Department of Clinical Pharmacology & Toxicology, Anam Hospital, Korea University College of Medicine, 126-1, Anam-dong 5-ga, Sungbuk-gu, Seoul 136-705, Korea; e-mail: jypark21{at}korea.ac.kr.

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