The DOI matches its Crossref record; 46 of the 46 references it cites were found in a registry or an index.
Supplementation With Goldenseal (Hydrastis canadensis), but not Kava Kava (Piper methysticum), Inhibits Human CYP3A Activity In Vivo
Abstract
The effects of goldenseal (Hydrastis canadensis) and kava kava (Piper methysticum) supplementation on human CYP3A activity were evaluated using midazolam (MDZ) as a phenotypic probe. Sixteen healthy volunteers were randomly assigned to receive either goldenseal or kava kava for 14 days. Each supplementation phase was followed by a 30-day washout period. MDZ (8 mg, per os) was administered before and after each phase, and pharmacokinetic parameters were determined using standard non-compartmental methods. Comparisons of pre- and post-supplementation MDZ pharmacokinetic parameters revealed significant inhibition of CYP3A by goldenseal (AUC(0-infinity), 107.9+/-43.3 vs 175.3+/-74.8 ng x h/ml; Cl/F/kg, 1.26+/-0.59 vs 0.81+/-0.45 l/h/kg; T(1/2), 2.01+/-0.42 vs 3.15+/-1.12 h; Cmax, 50.6+/-26.9 vs 71.2+/-50.5 ng/ml). MDZ disposition was not affected by kava kava supplementation. These findings suggest that significant herb-drug interactions may result from the concomitant ingestion of goldenseal and CYP3A substrates.
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“Goldenseal supplementation markedly inhibited the metabolism of midazolam, a CYP3A probe substrate, with an increase in exposure on the order of 40–60% [72,73].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [73]
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Self-citationComa from the Health Food Store: Interaction between Kava and Alprazolam
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Daniels, T. F., Puchalski, K., Trapp, S., Jimoh, A., Baravati, B., Shokoohinia, Y., Smith, S., & Langland, J. (2026) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2026.112219
Inhibition of cytochrome P450 2B6 activity by kava extracts
Wang, P., Avula, B., Katragunta, K., Chittiboyina, A. G., & Kharasch, E. D. (2026) · Drug Metabolism and Disposition · doi:10.1016/j.dmd.2026.100395
Metadata
- Authors
- Gurley, B. J., Swain, A., Hubbard, M. A., Hartsfield, F., Thaden, J., Williams, D. K., Gentry, W. B., & Tong, Y.
- Affiliations
- University of Arkansas for Medical Sciences (US)
- Corresponding author
- Gurley, B J
- Venue
- Clinical Pharmacology & Therapeutics
- Publisher
- Wiley
- Published
- 2007-05-09
- Volume
- 83
- Issue
- 1
- Pages
- 61-69
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W2103333792
- Cited by
- 102
- References
- 46
- Citations by year
- 2026: 3 · 2025: 2 · 2024: 6 · 2023: 6 · 2022: 8 · 2021: 8 · 2020: 8 · 2019: 3 · 2018: 4 · 2017: 3 · 2016: 3 · 2015: 5 · 2014: 4 · 2013: 8 · 2012: 12
- FWCI
- 3.69
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Clinical Pharmacology & Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute of General Medical Sciences (R01GM071322, GM71322)
- National Center for Research Resources (M01RR014288, RR-14288)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Complementary and alternative medicine › Complementary and Alternative Medicine Studies
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- goldenseal, Hydrastis canadensis, kava, CYP3A inhibition, herb-drug interactions, CYP3A substrates
- MeSH terms
- Adult, Cytochrome P-450 Enzyme System, Enzyme Induction, Enzyme Inhibitors, Female, Humans, Male, Midazolam, Models, Biological, Phenotype, Rifampin, Substrate Specificity, Clarithromycin, Risk Assessment, Dietary Supplements, Kava, Plant Preparations, Hydrastis, Herb-Drug Interactions, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme Inhibitors
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