Grapefruit Juice... opposite with codeine

Discussion in 'Codeine' started by bcStoner420, Jan 8, 2006.

  1. bcStoner420

    bcStoner420 Silver Member

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    I would just like everyone to know that the grapefruit juice trick is opposite when using codeine, it slows metabolism down so in this case less is converted to morphine, hence, it makes it suck ass. The only reason why he says this is because he has never seen this mentioned on the this forum before..
     
    1. 3/5,
      excellent point and a good notice of exceptions to grapefruit juice "rules"
      Mar 11, 2006
  2. Jaded

    Jaded Newbie

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    Thats pretty interesting, seeing as i always thought that grapefruit juice always potentiated the effects of codeine when taken with it. Where did you find this out?
     
  3. bcStoner420

    bcStoner420 Silver Member

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    Just searched potentiating opiates, and it was on one of the sites. It makes good sense though when you think about it.
     
  4. Jaded

    Jaded Newbie

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    Ah cool, thanks for that. I'll have a search in a moment and have a quick read...
     
  5. thatsall

    thatsall Silver Member

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    So what could increase the effects, anything?
     
  6. ningbar

    ningbar Newbie

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    swim found two drugs that definitely potentiate codeine for him

    1 Quinnine - easy enough to get (as a malaria prophylactic) - swims prescribbed it for muscle cramps

    2 Cyclosporin - impossible to get (for transplant patients and those with autoimmune disorders) - swims one of the latter, its pretty horrible stuff tho you wouldnt want to take it unless you have to - its very liver toxic, swim gets LFTs every 2 weeks because of this (which for me has the advantage that it lets swim know hes not been taking too much acetaminophen)



    I find if he takes his prescribed dose of both drugs an hour before he takes his hoarded prescribed codeine it greatly increases the effects

    bad effects:

    quinnine gives swim a bitter tasting dry mouth the next day, and if you take too much of it you will have a ringing sound in your ears for several days

    cheers
    Ningbar
     
    1. 4/5,
      Interesting anecdotal evidence about cyclosporin.
      Aug 4, 2009
  7. ningbar

    ningbar Newbie

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    forgot to mention that you are right about the grapefruit/codeine

    its also a very bad idea to take grapefruit with cyclosporin (the doc warned me not to but i did anyway)

    because it works on the P450/3A4 enzyme as well as the codeine important P450[SIZE=-1]/CYP2D6 you end up absorbing far too much cyclosporin

    killed the codeine buzz stone dead and made me violently ill the next day, i mean really fookin projectile vomiting sick

    cheers
    Ningbar
     
  8. thatsall

    thatsall Silver Member

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    I am perscribed lyrica, anti seizure med also perscribed for easing pain in patients that suffer from nerve pain. I was perscribed it off-label for anxiety relief. Swim feel like this increases the effects alot, but it is hard to tell because lyrica has a sort off drunken/GHB effect when taken at higher doses, so they might just be working together, but eaither way you look at it I would defintly say this is a very relaxing pharmacutical cocktail. Higly recomended.
     
  9. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    SWIM experienced this the other day. somehow whatever it is in grapefruit juice ties up the p450 liver enzyme and prevents codeine from being converted (i think) into morphine, so pretty much it renders the codeine ineffective. luckily the same chemical in grapefruit juice can potentiate other opiates, so I was lucky to have some hydrocodone on hand too.
     
  10. ojos_de_brujo

    ojos_de_brujo Silver Member

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    Does this apply to grapefruit-aroma as well?
    I have solluble tablets containing codeine and grapefruit-aroma (along with paracetamol, several types of salt, aspartame and sorbitol). I am not very happy about all the rubbish these tablets contain, but it will have to do. Only in small doses because of the paractamol of course. Extraction does not work because of the salts added to secure solution of the paracetamol.
    Swim will have to speak harshly to her doctor for suscribing this scam of a product :)
     
  11. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    The grapefruit juice inhibition of liver enzymes is caused by furanocoumarin compounds, and not by the aromatic compounds in grapefruit, so I do not think that the grapefruit-aroma would work. But, if anyone has tried this and has evidence to the contrary, please share!
     
  12. jonny thaiwongy

    jonny thaiwongy Newbie

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    anyone kno about orange juice? I took 270mg DHC swallowed wit oj it didnt seem as intense as usual, and thats a high dose for swim!
     
  13. Paracelsus

    Paracelsus Platinum Member & Advisor

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    Orange juice doesn't inhibit CYP3A like grapefruit does, having no effect on the metabolism of dihydrocodeine.
     
    Last edited: May 30, 2007
  14. darkglobe

    darkglobe Silver Member

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    This has all been discussed in the Codeine Potentiators thread, guys.

    Grapefruit Juice theoretically has no positive net effect on Codeine metabolism. End of.
     
  15. snapper

    snapper Gold Member

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    To potentiate codeine, one needs to upregulate cytochrome enzymes (ie-trigger the formation of more enzyme genetically due to demand). Two drugs that come to mind that do this over time are corticosteroids and phenobarbital (along with other barbituates, though pheno for sure). This would increase cytochomes and metabolize more codeine to morphine faster...
     
  16. Paracelsus

    Paracelsus Platinum Member & Advisor

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    If you think grapefruit juice inhibits CYP2D6, think again. Read this thread.

    So codeine should actually be potentiated with grapefruit juice because less norcodeine is formed (CYP3A is inhibited).

    The internet is full of statements that codeine’s effects are weakened by GFJ, because "it interferes with codeine to morphine conversion". Yet none of these statements has any factual basis since they all state that GFJ inhibits CYP2D6. Actually, at least two members that I am aware of have reported definite potentiation of codeine with GFJ: frizzantik (13,000+ posts) and redeemer (2,000+ posts).

    Same would also stand for dihydrocodeine (DHC).

    It would be great if we had some experience reports about codeine or DHC with GFJ. SWIP might conduct such an experiment when he will have access to codeine/DHC again.

    Snapper: While corticosteroids and barbiturates are known inducers of some P450 enzymes, they do not induce the enzyme relevant here (CYP2D6).
     
    1. 3/5,
      Thanks for pointing this out
      May 16, 2011
  17. Ethyl

    Ethyl Newbie

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    Allways taken for granted the statment that GFJ inhibits p450d26. I will say to Swie this stuff, and he will experiment.
     
  18. Ethyl

    Ethyl Newbie

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    Swie just took 150mg of CWE (including 5% loss) and he previously have drunk/eaten 2 grapefruits (ruby red), he eat the rind too, cause there wheres the goodies are..
    He tells me he is experiencing a possible increase in effects (maybe it feels like 200/250mg), but there are other variables that may have influenced, including it's a new extract, and so potency may vary...; swie has lost some tolerance in the last days cause he weened himself.

    In the next days Swie will experiment more, and exclude every other variable to see if it really works.. But it looks that it works!

    Thanks Paracelsus for opening my eyes.. I should never taken for granted that GFJ inhibited 2d6. Never take things for granted, explore.. Thanks
     
  19. Zaprenz

    Zaprenz Gold Member

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    ^ Inconsistent reports on Grapefruit juice interacting with codeine doesn't surprise SWIZ.

    There are too many variables involved as well as codeine taken alone is still under debate exactly its main mode of action.

    Mode(s) of action:
    Variables:
    • Genetic variability in metabolism (inhibition of conversion to more active compounds, inhibition of breakdown of active compounds, variability in uptake etc)
    • absorption & distribution - Inc Form of grapefruit (juice, fruit, extract), acidity, interactions with codeine preperation (tablet, solution, CWE)
    • and many more
    ^Add to the above the placebo effects of anecdoctal reports means I would guess there is no easy answer to whether or not grapefruit increases or decreases effect, duration, "high".
     
  20. Paracelsus

    Paracelsus Platinum Member & Advisor

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    Ethyl: glad that it seems to work. SWIE could try an identical amount of CWE in a week (a medical paper shows that inhibition of CYP3A is quasi-irreversible; CYP3A activity probably takes some 8 days to return to baseline). Just to see if it was placebo or not. Also, SWIP has noticed that (for him) red grapefruit potentiates tramadol but not DXM. White grapefruit potentiated DXM. SWIP hasn't tried white grapefruit with tramadol. Maybe white is more effective.

    Zaprenz: Those compounds aren't modes of action. They're just codeine and some of its metabolites, of which morphine and morphine-6-glucuronide are active. That means that only CYP2D6 makes the codeine active. And grapefruit simply reduces the rate of N-demethylation of all these compounds (which to my knowledge are all inactive), probably also raising bioavailability in some other way.