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Hyperforin in St. John’s wort drug interactions

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

Recently, interactions of herbal medicines with synthetic drugs came into focus of particular interest. In the past 3 years, more than 50 papers were published regarding interactions between St. John’s wort (Hypericum perforatum L.; SJW) and prescription drugs. Co-medication with SJW resulted in decreased plasma concentrations of a number of drugs including amitriptyline, cyclosporine, digoxin, indinavir, irinotecan, warfarin, phenprocoumon, alprazolam, dextrometorphane, simvastatin, and oral contraceptives. Sufficient evidence from interaction studies and case reports indicate that SJW is a potent inducer of cytochrome P450 enzymes (particularly CYP3A4) and/or P-glycoprotein. Recent studies could show that the degree of enzyme induction by SJW correlates strongly with the amount of hyperforin found in the product. Products that do not contain substantial amounts of hyperforin (<1%) have not been shown to produce clinically relevant enzyme induction. On the other hand, some evidence suggests that hyperforin may also contribute to the antidepressant activity of SJW. However, clinical studies using SJW preparations with a low hyperforin amount (<1%) clearly demonstrated the superiority of this plant extract over placebo and its equivalence to imipramine and fluoxetine in the treatment of mild to moderate forms of depression. In the present paper clinical significant SJW interactions are critically evaluated against the background of hyperforin.

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, University of Florida, P.O. 100494, Gainesville, FL, 32610, USA

    Rajanikanth Madabushi, Hartmut Derendorf & Veronika Butterweck

  2. Kneipp Werke Würzburg, Germany, Würzburg

    Bruno Frank

  3. Institute of Clinical Pharmacology, University of Rostock, Germany, Rostock

    Bernd Drewelow

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  1. Rajanikanth Madabushi
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Correspondence to Veronika Butterweck.

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Madabushi, R., Frank, B., Drewelow, B. et al. Hyperforin in St. John’s wort drug interactions. Eur J Clin Pharmacol 62, 225–233 (2006). https://doi.org/10.1007/s00228-006-0096-0

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