Echinacea to potentiate codeine?

[Tortoise]

Hi guys, I stumbled across this page on wikipedia:http://en.wikipedia.org/wiki/CYP3A4#CYP3A4_ligands

It states in the list down the bottom that echinacea has the effect of inhibiting CYP3A4. If this were true, then echinacea could theoretically be used to potentiate codeine, right?

Anybody know of somebody who has tried this?

[imyourlittlebare]

Not codeine. Because If my memory is correct, codeine has to be processed by something (probably the liver) and converted into morphine. I think someone told my friend that if they drank grapefruit juice, it would inhibit the effect of codeine.

[Paracelsus]

^^^ The conversion of codeine into morphine is catalyzed by CYP2D6 and not CYP3A. CYP3A catalyzes N-demethylation into (inactive) norcodeine, which is why CYP3A inhibitors potentiate codeine (and many other opiates, as lots of them are "deactivated" through CYP3A). Grapefruit juice is also a CYP3A inhibitor which potentiates codeine. The common old statement that grapefruit juice inhibits the effects of codeine was probably spread by people who knew about cytochrome P450 in general, but not about the particular isozymes.

I guess that if someone already uses Echinacea, this is a welcome side effect for many. But for potentiation of opiates one should prefer grapefruit juice, as it probably is the most researched CYP3A inhibitor.

[Tortoise]

Swim will try Ecinacea next time he uses codeine.

Oh and Paracelsus: What's your opinion on the use of St John's Wort to potentiate codeine? I was reading on another forum that somebody had good results with it, by my internet research has suggested that it a CYP3A4 inducer with no effect on CYP2D6, so theoretically it shouldn't work, right?

[imyourlittlebare]

Doesnt St. Johns wort cause your liver to overactively work. I know it decreases the effect of birthcontrol and antibiotics by up to 35 %.

And thanks alot para (yeah were on a nickname basis). I dont know alot about the liver or its enzymes. The brain is and always will be my favorite organ.

[Ethyl]

st john wort should induce 3a4 so it should make codeine less potent.

[Tortoise]

Ethyl, you're absolutely right that St John's Wort induces 3A4, BUT it also induces CYP2D6 (which would convert more codeine to morphine) and some dude Swim was chatting to on some other forum believes that there is an overall net positive effect, especially if taken with another 3a4 inhibitor such as grapefruit juice.

Swim has to admit though, he tried echinacea and St John's the other day and the results were pretty lousy. But that could also be a tolerance issue. He plans to try again soon.