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St John's Wort: effect on CYP3A4 activity.

C A Roby1, G D Anderson, E Kantor

  • 1Department of Pharmacy, St Agnes Hospital, University of Maryland, Baltimore, USA.

Clinical Pharmacology and Therapeutics
|May 29, 2000
PubMed
Summary

St John's Wort significantly increased the urinary 6-beta-hydroxycortisol/cortisol ratio, indicating it induces CYP3A4 activity. This highlights potential drug interactions for patients using this popular herbal supplement.

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Area of Science:

  • Pharmacology
  • Herbal Medicine Research

Background:

  • St. John's Wort is a commonly used herbal product.
  • Understanding its drug interaction potential is crucial for patient safety.
  • Cytochrome P450 3A4 (CYP3A4) is a key enzyme in drug metabolism and drug-drug interactions.

Purpose of the Study:

  • To investigate the in vivo impact of St. John's Wort extract on CYP3A4 enzyme activity.
  • To assess CYP3A4 induction by measuring urinary 6-beta-hydroxycortisol to cortisol ratios.

Main Methods:

  • A 14-day trial involving 13 healthy young adults (18-25 years).
  • Participants ingested 300 mg of St. John's Wort extract three times daily.
  • CYP3A4 activity was measured by the urinary 6-beta-hydroxycortisol/cortisol ratio before and after treatment.

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Main Results:

  • The mean urinary 6-beta-hydroxycortisol/cortisol ratio increased by 114% (P = .003).
  • The ratio rose from a baseline of 7.1 to 13 post-treatment.
  • Nearly all subjects exhibited an increased ratio, suggesting consistent induction.

Conclusions:

  • St. John's Wort treatment for 14 days significantly elevates CYP3A4 activity.
  • The findings strongly suggest St. John's Wort acts as an inducer of the CYP3A4 enzyme.
  • This induction has implications for potential drug interactions with St. John's Wort.