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Lemon Juice potentiation, inhibits CYP450 enzymes almost as well as Grapefruit

socio

Bluelighter
Joined
Dec 14, 2009
Messages
342
Supposedly this was a new finding in 2001. I haven't heard of it. Is it correct?

The forums regularly point out that Grapefruit Juice [GJ] potentiates (or at least delays the elimination/metabolism) of benzos & opioids by inhibiting Cytochrome P450 liver enzymes (3A4, and I believe 2A6 and 2D6 [right?], among others responsible for breaking down many benzos and opioids into less-active or inactive metabolites). Cimetidine aka Tagamet does something similar.

I've seen posts about Lemon Juice [LJ] potentiating mushrooms (supposedly due to vitamin c) & poppy tea (supposedly by acidifying).

I've never heard LJ mentioned as a potentiator via liver enzyme inhibition like GJ. But perusing the web, I noticed that there is research claiming that LJ does this almost as well as GJ (a couple other sources as well).

http://www.ncbi.nlm.nih.gov/pubmed/18968322

Application to drug-food interactions of living cells as in vitro model expressing cytochrome P450 activity: enzyme inhibition by lemon juice.
Baltes MR, Dubois JG, Hanocq M. Talanta. 2001 Jun 21;54(5):983-7.

Abstract
Classical inhibitors of human cytochrome P450 3A4 activity, such as ketoconazol and quercetin, are tested to prove the efficiency of a new metabolisation model using living entire cells. Grapefruit juice is a well-known potent inhibitor of cytochrome P450 3A4 activity. With regard to the clinical relevance of grapefruit juice-drug interactions, an investigation of other common juices is undertaken with this in vitro model.... It is demonstrated for the first time that lemon juice significantly inhibits by 60+/-3% the CYP3A4-mediated oxidation. Grapefruit juice inhibits this activity by 82+/-4%. The mechanism of lemon juice inhibition is competitive, whereas it is mixed for grapefruit juice. ...

There are a couple other references out there.
Am I understanding this correctly, LJ is basically 75% (60%/~80%) as effective at 3A4 enzyme inhibition compared to GFJ?

Anyone know what they mean by "competitive" vs. "mixed" inhibition? (My knowledge of this is practical, not based on formal education; I simply try to figure out what will work and get a sense of why.) Would be nice to know if there are more good options available than GJ and Tag, in case they're not around...
 
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Just take more grapefruit juice. Tastes better.
Why not "Just take more drugs"? Or "Just smoke bud." At the moment I don't have any GFJuice, or money. So I might try if I was an alchemist, but I'm not.

No offense, K12, I hear ya. (Actually I rarely drink GFJ, since the cost compared to cimetidine isn't worth it to me.) But I always wonder why so many folks insist that others choose one specific alternative out of many comparable ones. My view tends to be: More alternatives, more better.

I do have opioids and benzos. And a ton of lemon juice. I doubt I would've drunk straight lemon juice, but then I remembered an old saying -- something about "When life gives you lemons..."

That said, if anyone knows anything about lemon's effect on P450, I would like to know more. Based on just one ref, I'm not entirely confident that lemon juice is a strong inhibitor.
 
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