[{"id":61,"uid":"NPDI-twVQgQ","name":"Supplementation With Goldenseal (Hydrastis canadensis), but not Kava Kava (Piper methysticum), Inhibits Human CYP3A Activity In Vivo","napdiIdentifier":"PMID: 17495878","overallSummary":"<div class=\"page\" title=\"Page 1\">\r\n<div class=\"layoutArea\">\r\n<div class=\"column\">\r\n<p>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–N), 107.9743.3 vs 175.3774.8 ng x h/ml; Cl/F/kg, 1.2670.59 vs 0.8170.45 l/h/kg; T1/2, 2.0170.42 vs 3.1571.12 h; Cmax, 50.6726.9 vs 71.2750.5 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.</p>\r\n</div>\r\n</div>\r\n</div>","pubmedId":17495878,"embaseId":null,"croIdentifier":"University of Arkansas for Medical Sciences","croInformation":"Department of Pharmaceutical Sciences","dateStart":null,"dateEnd":null,"internalComment":null,"status":"published","compoundId":null,"naturalProductUid":"NP-002d7e9a-2baf-47cb-a936-51ba9cbb36a7","naturalProductSampleId":null,"studySourceTypeId":1,"naturalProduct":{"uid":"NP-002d7e9a-2baf-47cb-a936-51ba9cbb36a7","binomial":"Hydrastis canadensis","name":"Goldenseal","itis":null,"srs":"66690655-f406-4d67-96e3-2066aafee8d5","source_id":"","conceptId":null},"compound":null,"studySourceType":{"id":1,"name":"Published report"},"experiments":[{"id":277,"uid":"NPDI-Aw3yIw","name":"CYP3A4 Experiment - MDZ probe","overallEffect":1,"isControlData":false,"isIc50Shift":false,"croCutoff":null,"croIdentifier":null,"comment":null,"experimentalConditionsComment":null,"resultsComment":"Control is pre-goldenseal administration <br />Test is post-goldenseal administration<br />Data from Table 1/Table 2","internalComment":null,"objectCompoundId":26,"objectMetaboliteCompoundId":null,"precipitantCompoundId":127,"cytochromeB5Id":null,"studyId":61,"experimentTypeId":9,"testSystemId":null,"ic50ShiftExperimentId":null,"controlDataExperimentId":null,"controlDataForExperimentId":null,"naturalProductSampleId":null,"experimentType":{"id":9,"name":"In Vivo Interaction","isInVitro":false,"isTransporter":false,"isEnzyme":false,"purl":"http://purl.obolibrary.org/obo/DIDEO_00000071"},"objectCompound":{"id":26,"name":"midazolam","unii":"R60L0SM5BC","inChIKey":"DDLIGBOFAVUZHB-UHFFFAOYSA-N","publicDescription":null,"internalComment":null,"conceptId":708298,"enantiomerOfId":null},"precipitantCompound":{"id":127,"name":"goldenseal root extract","unii":null,"inChIKey":null,"publicDescription":null,"internalComment":null,"conceptId":null,"enantiomerOfId":null},"objectMetaboliteCompound":null,"enzymes":[{"id":13,"name":"CYP3A4","conceptId":4306811,"experiment_enzyme_xref":{"enzymeId":13,"experimentId":277}}],"transporters":[],"quantifiedMetabolites":[]}]}]