Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone

Kyoung Ah Kim, Pil Whan Park, Kwang Hyeon Liu, Kwon Bok Kim, Heon-Jeong Lee, Jae Gook Shin, Ji-Young Park

Research output: Contribution to journalArticle

30 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)66-72
Number of pages7
JournalJournal of Clinical Pharmacology
Volume48
Issue number1
DOIs
Publication statusPublished - 2008 Jan 1

Fingerprint

Risperidone
P-Glycoprotein
Rifampin
Pharmacokinetics
Cytochrome P-450 CYP3A
Cytochrome P-450 CYP3A Inducers
Biological Availability
Healthy Volunteers
Placebos
Paliperidone Palmitate

Keywords

  • 9-hydroxyrisperidone
  • Cytochrome P450 3A (CYP3A)
  • Drug interaction
  • P-glycoprotein
  • Rifampin
  • Risperidone

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. / Kim, Kyoung Ah; Park, Pil Whan; Liu, Kwang Hyeon; Kim, Kwon Bok; Lee, Heon-Jeong; Shin, Jae Gook; Park, Ji-Young.

In: Journal of Clinical Pharmacology, Vol. 48, No. 1, 01.01.2008, p. 66-72.

Research output: Contribution to journalArticle

Kim, Kyoung Ah ; Park, Pil Whan ; Liu, Kwang Hyeon ; Kim, Kwon Bok ; Lee, Heon-Jeong ; Shin, Jae Gook ; Park, Ji-Young. / Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. In: Journal of Clinical Pharmacology. 2008 ; Vol. 48, No. 1. pp. 66-72.
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