Inhibition of CYP3A4 by kava Kava significantly lengthening the 1/2 life of ketamine.

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PowerHungryGandhi is anyone

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Case report and citation

https://www.reddit.com/r/askdrugs/comments/b2k1uc/ketamine_lozenges_and_kava_serious_interaction/?utm_source=share&utm_medium=ios_app&utm_name=iossmf

“Whole kava extract caused 78% inhibition of 3A4”

“The major metabolic pathway is N-demethylation to an active metabolite norketamine by CYP3A4”

Whole kava extract (normalized to 100 microM total kavalactones) caused concentration-dependent decreases in P450 activities, with significant inhibition of the activities of CYP1A2 (56% inhibition), 2C9 (92%), 2C19 (86%), 2D6 (73%), 3A4 (78%), and 4A9/11 (65%) following preincubation for 15 min with HLMs and NADPH;

N-demethylation to an active metabolite norketamine by CYP3A4 occurs. norketamine is only 1/5 as potent as ketamine but may have unique effects.

Mathews JM, Etheridge AS, Black SR. Inhibition of human cytochrome P450 activities by kava extract and kavalactones. Drug Metab Dispos. 2002 Nov;30(11):1153-7. doi: 10.1124/dmd.30.11.1153. PMID: 12386118.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6197107/

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