Influence of panax ginseng on cytochrome P450 (CYP)3A and p-glycoprotein (P-gp) activity in healthy participants

Christine Y. Malati, Sarah M. Robertson, Jennifer D. Hunt, Cheryl Chairez, Raul M. Alfaro, Joseph A. Kovacs, Scott R. Penzak

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59 Scopus citations

Abstract

A number of herbal preparations have been shown to interact with prescription medications secondary to modulation of cytochrome P450 (CYP) and/or P-glycoprotein (P-gp). The purpose of this study was to determine the influence of Panax ginseng on CYP3A and P-gp function using the probe substrates midazolam and fexofenadine, respectively. Twelve healthy participants (8 men) completed this open-label, single-sequence pharmacokinetic study. Healthy volunteers received single oral doses of midazolam 8 mg and fexofenadine 120 mg, before and after 28 days of P ginseng 500 mg twice daily. Midazolam and fexofenadine pharmacokinetic parameter values were calculated and compared before and after P ginseng administration. Geometric mean ratios (postginseng/preginseng) for midazolam area under the concentration-time curve from zero to infinity (AUC 0-∞), half-life (t1/2), and maximum concentration (Cmax) were significantly reduced at 0.66 (0.55-0.78), 0.71 (0.53-0.90), and 0.74 (0.56-0.93), respectively. Conversely, fexofenadine pharmacokinetics were unaltered by P ginseng administration. Based on these results, P ginseng appeared to induce CYP3A activity in the liver and possibly the gastrointestinal tract. Patients taking P ginseng in combination with CYP3A substrates with narrow therapeutic ranges should be monitored closely for adequate therapeutic response to the substrate medication.

Original languageEnglish
Pages (from-to)932-939
Number of pages8
JournalJournal of Clinical Pharmacology
Volume52
Issue number6
DOIs
StatePublished - Jun 2012

Keywords

  • HIV
  • Panax ginseng
  • cytochrome P450
  • drug interaction
  • herb
  • midazolam

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    Malati, C. Y., Robertson, S. M., Hunt, J. D., Chairez, C., Alfaro, R. M., Kovacs, J. A., & Penzak, S. R. (2012). Influence of panax ginseng on cytochrome P450 (CYP)3A and p-glycoprotein (P-gp) activity in healthy participants. Journal of Clinical Pharmacology, 52(6), 932-939. https://doi.org/10.1177/0091270011407194