1 RCT 2008
A controlled human study found goldenseal significantly inhibited the drug-metabolizing enzyme CYP3A4.
Supplementation with goldenseal (Hydrastis canadensis), but not kava kava (Piper methysticum), inhibits human CYP3A activity in vivo. Gurley BJ et al. · Clinical pharmacology and therapeutics (2008)
Goldenseal strongly inhibited CYP3A4 (midazolam probe) Major drug-interaction potential Among the most CYP-active botanicals A controlled study confirmed goldenseal altered CYP-mediated drug metabolism (unlike kava).
Effect of goldenseal (Hydrastis canadensis) and kava kava (Piper methysticum) supplementation on digoxin pharmacokinetics in humans. Gurley BJ et al. · Drug metabolism and disposition: the biological fate of chemicals (2007)
Goldenseal inhibited CYP enzyme activity Clinically relevant interaction signal Human probe-drug design An in-vivo study found goldenseal (among botanicals) modulated cytochrome P450 activity.
In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes. Gurley BJ et al. · Clinical pharmacology and therapeutics (2005)
Goldenseal affected CYP2D6/CYP3A4 in vivo Confirms interaction risk Healthy-volunteer study 4 Systematic Review 2012
A systematic review identified goldenseal among herbal 'perpetrators' of pharmacokinetic drug interactions.
Clinical evidence of herbal drugs as perpetrators of pharmacokinetic drug interactions. Hermann R et al. · Planta medica (2012)
Goldenseal a notable CYP inhibitor High interaction-risk classification Clinical caution warranted 5 RCT 2025
A pharmacokinetic study examined goldenseal's interaction with metformin (a transporter substrate).
The Pharmacokinetic Interaction Between Metformin and the Natural Product Goldenseal Is Metformin Dose-Dependent: A Three-Arm Crossover Study in Adults With Type 2 Diabetes. Nguyen JT et al. · Clinical and translational science (2025)
Goldenseal altered metformin pharmacokinetics Transporter-mediated interaction 6 Open-Label 2021
A study assessed goldenseal in transporter-mediated natural-product–drug interactions.
Assessing Transporter-Mediated Natural Product-Drug Interactions Via In vitro-In Vivo Extrapolation: Clinical Evaluation With a Probe Cocktail. Nguyen JT et al. · Clinical pharmacology and therapeutics (2021)
Goldenseal implicated in transporter interactions Mechanistic/PK focus Adds to interaction profile 7 Systematic Review 2005
A systematic review of natural-product–HIV-drug interactions flagged goldenseal's CYP inhibition.
Natural health product-HIV drug interactions: a systematic review. Mills E et al. · International journal of STD & AIDS (2005)
Goldenseal flagged for antiretroviral interactions CYP3A4 inhibition mechanism Avoid with affected drugs