Effects on the Cytochrome P450 Enzyme System

In vivo tests performed using human test subjects showed that kava potently inhibits the cytochrome P450 enzyme CYP2E1, but has no effect on CYP1A2, CYP2D6, CYP3A4, or CYP3A5.[1]

Laboratory in vitro tests using human hepatic microsomes, which often don't relate to actual use in humans, showed that kava potently inhibited CYP2C9, CYP2C19, CYP2D6, and CYP3A4.[2]

1. Clin Pharmacol Ther. 2005 May;77(5):415-26;
In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes; Gurley BJ, Gardner SF, Hubbard MA, Williams DK, Gentry WB, Khan IA, Shah A; Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, 4301 W Markham St, Slot 522, Little Rock, AR 72205, USA; PubMed PMID: 15900287
2. Drug Metab Dispos. 2005 Oct;33(10):1555-63. Epub 2005 Jul 20.
Pharmacokinetics and disposition of the kavalactone kawain: interaction with kava extract and kavalactones in vivo and in vitro. Mathews JM, Etheridge AS, Valentine JL, Black SR, Coleman DP, Patel P, So J, Burka LT; RTI International, P.O. Box 12194, 3040 Cornwallis Road, RTP, NC 27709, USA. PubMed PMID: 16033948
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