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What is it in grapefruit juice that potentiates opioids?

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Doug2113

Doug2113

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Pressed for time, so sorry if this has been answered elsewhere. But I was wondering what exactly it was in grapefruit juice that inhibits the enzyme that breaks down opioids, thus, potentiating them? I was just curious so that I might be able to get it in vitamin/pill form from GNC/vitamin section of Walmart/etc. I gotta go hop in the shower, so I hope you guys can get this answered before I have to leave for class. =D

P.S. And will this help tramadol? I know tramadol is weird, and I thought I remember reading that doing something that potentiates other opioids might hinder tramadol.

Thanks in advance,
Doug
 
Furanocoumarins by the name bergamottin and dihydroxybergamottin.

Also grapefruit juice may help with the o-demethylation of tramadol.
 
What is a good brand of grape juice, I don't buy that shit, I don't think I ever have. I'll go to WaWa tonight and grab it.
 
when drugs are metabolized through the liver, they are converted into inactive metabolites, and excreted in urine. most opioids and benzos are metabolized especially through the 2D6 and 3A4 enzymes. grapefruits contain organic compounds which inhibit 3A4. inhibition of these enzymes increases the duration of effect (of drugs metabolized through these enzymes.)

potency and concentration of grapefruit juice vary deeming it undesirable as a reliable inhibitor. tagamet(cimitidine) on the other hand, inhibits 2D6 as well as 3A4 which can be a good or bad thing. for example, someone who consumes pro-drugs (i.e. DXM, tramadol, codeine, ect...) would not wan't to take tagamet because 2D6 is the main of converter of DXM --> DXO, codeine --> morphine, tramadol --> o-desmethyltramadol . however, tagamet is favored by users of full-agonist opiates that do not rely on their parent drugs' effects (oxycodone, methadone, hydrocodone, ect...) because cimitidine inhibits the major hepatic and intestinal enzymes, and because it can be taken in exact doses.
 
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laCster said:
when drugs. are metabolized through the liver, they are converted into inactive metabolites the active most opioids are metabolized especially through the 2D6 and 3A4 enzymes. grapefruits contain organic compounds which inhibit 3A4. inhibition of these enzymes increases the duration of effect of drugs metabolized through these enzymes.

potency and concentration of grapefruit juice vary deeming it undesirable as a reliable inhibitor. tagamet(cimitidine) on the other hand, inhibits 2D6 as well as 3A4 which can be a good or bad thing. for example, someone who consumes pro-drugs (i.e. DXM, tramadol, codeine, ect...) would not wan't to take tagamet because 2D6 is the main of converter of DXM --> DXO, codeine --> morphine, tramadol --> o-desmethyltramadol . however, tagamet is favored by users of full-agonist opiates that do not rely on their parent drugs' effects (oxycodone, methadone, hydrocodone, ect...) because cimitidine inhibits the major hepatic and intestinal enzymes, and because it can be taken in exact doses.
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Good post lacter, but hydrocodone IS A PRODRUG. Although it does have SOME effects on it's own, they are far to weak for anyone with even a slight tolerance to feel unless massive doses are taken.

And to Doug, you probably don't want to mix grapefruit juice/tagament with tramadol, as it requires it's metabolite to have any opioid agonist activity-whatsoever. Otherwise it messes with serotonin and shit. However, you could take a couple of tagament afterward, to extend it's already long half life.

(edit to say that oxycodone also converts to oxymorphone which contributes to a significant portion of it's effects, though it is a strong enough opiate on it's own to not require this conversion; thus meaning tagament will typically make an oxy high longer, but less intense, though, in my experience, way more itchy)
 
lorne667 said:
Good post lacter, but hydrocodone IS A PRODRUG. Although it does have SOME effects on it's own, they are far to weak for anyone with even a slight tolerance to feel unless massive doses are taken.
Click to expand...

hmmm, interesting....but what/where is your source? i've always believed hydrocodone produced the most prominent effects on the CNS, and not the slim amount of hydromorphone that is metabolized by 2D6.
 
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Well I have researched extensively on the subject, so I would have to fish around to find references. But basically hydro and oxy function very similiar, in that they are both metabolized by cyp2d6 into they're morphine based parents, that are far more potent than the -codone versions. But both of them convert into very small amounts, which is why oxycodone bears only a passing resemblance to oxymorphone and hydrocodone is very much different than hydromorphone. But what separates them, to the extent of my knowledge and, perhaps more importantly, experience taking them with/without all the various inhibitors, is that oxy is actually a potent agonist on it's own, allowing it to act independently of it's metabolite, whereas hydrocodone, though definitely active by itself, is much less potent, making the jump to hydromorphone more important. It really varies though, based on individual metabolism, tolerance, etc etc etc.

It is a very interesting subject to me how drugs work in general( in case ya hadn't figurd that out :) ) and this one really interests me, but overall, neither may be "true" prodrugs, since they both have they're own potential, but ultimately I believe hydrocodone does rely on hydromorphone for it's effects, unlike oxy, which is fine on it's own!!!

(Edit to say that the hydromorphone is small in any case, and we all know hydrocodone is one of the weakest opoids, so whether it gets it's effects from the small amount of hydromorphone, or it's own limited effects, it is still lacking in potency. Also, I believe 10-15% of the dose is converted to hydromorphone. that would make 30mg h-codone convert to 2-4mg hydromorphone, which by itself would be very weak orally due to low oral BA, but since it is metabolized in-vivo, this is less of an issue, giving you much better effects)
 
lorne, that is basically correct, except because it is metabolised in vivo all of that 10-15% gets into your bloodstream (so we're talking .5 - 2mg of Hydromorphone which equals 4-16mg of morphine, so obviously (for many people) hydrocodone is mainly a pro-drug.
 
bergamottin, as in the same flavinoid contained in the flavoring of 'Earl Grey Tea' ? probably not in any amount of the concentration needed for potenciaron, but just an interesting tidbit? Of course i'm a bit under the influence, alcohol, a small dose of benzo and herbal relaxation tea... maybe i'm not thinking this thru enough
 
Oh, bummer. I thought that inhibiting the 4A3 would help but inhibiting the other would hinder. I just drank grapefruit juice and waited 40 minutes to take my last dose. I guess I'll see what happens.
 
So I pretty much just wasted my meds? Fuckin great. I try to boost my meds for MEDICAL purposes and it shits in my face. Wonderful. And goddamn does that shit taste horrible.
 
Noted. I'm not trying to get high. That's not going to happen, and I realize this. I had two generic v Norco's this morning and that gave me the very slightest head change. I hurt a little less and had more energy, but other than that, not much. I just want to get my pain levels down (hence the angry breakdown three posts ago).
 
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