PDA

View Full Version : Why Does Grapefruit juice enhance opiates



OC'sthewaytobe
04-11-2007, 07:03 PM
What ingredient in grapefruit juice enhances opiete highs? My friend says its vitamin C, but i just called him dumb. I know thats not what does it. But what does?

Woowoo
04-11-2007, 07:08 PM
pla·ce·bo ef·fect 1. An apparent improvement due not to any treatment but only to the patient's belief that he or she will improve.

OxyContinuously
04-11-2007, 07:09 PM
it's def not placebo. I forget the reasoning but the GF juice inhibits some enzyme.

OC'sthewaytobe
04-11-2007, 07:09 PM
Id like to think thats not it, and i do.

euphoria2002
04-11-2007, 07:14 PM
GF juice inhibits some enzyme in your small intestine. This results in increased uptake of many drugs, oxycodone being one of them. Is this guaranteed for sure 100% true? Don't know, but most of the pod users here SWEAR by it.

Euphoria

Woowoo
04-11-2007, 07:20 PM
it's def not placebo. I forget the reasoning but the GF juice inhibits some enzyme.
I was joking ... but only half joking. Given that grapefruit juice boosts opiates, you can't tell me that the placebo effect isn't responsible for at least some of that perceived boost.

There is however a "real" answer to this question. Kidding aside, I'd like to learn about it.

Ragdoll
04-12-2007, 02:32 AM
There's a bunch of info online about the grapefruit juice thing. Pharmacies put the label on prescription bottles ("Do not take with grapefruit juice"), so there is something to it that's a real effect.

ChrisCuts
04-12-2007, 10:26 AM
The flavonoids in grapefruit juice potentiate opiates (and many other drugs) by inhibiting the CYP3A4 metabolite and by proxy increasing the bioavailability. As CYP3A4 is located in the intestinal mucosa I can only see it acting to boost the effects if the drug is ingested orally. Which is why the most hoopla you hear about it acting as a potentiator is from the poppy tea crowd.

Woowoo
04-12-2007, 12:55 PM
The flavonoids in grapefruit juice potentiate opiates (and many other drugs) by inhibiting the CYP3A4 metabolite and by proxy increasing the bioavailability. As CYP3A4 is located in the intestinal mucosa I can only see it acting to boost the effects if the drug is ingested orally. Which is why the most hoopla you hear about it acting as a potentiator is from the poppy tea crowd.
That's very interesting.

I have been thinking of some way to actually test this hypothesis, since it's damn near impossible to figure it out just by observation. If these flavonoids could be swallowed in capsule form then the test would be easy to construct. Plus, what oxy-head would't want to have a bottle of flavonoid capsules lying around? Sure is easier than keeping a suitcase full of grapefruits like Hunter S. Thompson!

The test would go like this: you find an oxy addict who typically enjoys a dose of roughly 100mg. Each day for 10 days in a row he or she gets a 100mg oral dose along with a capsule. For 5 of the days, the capsules will contain grapefruit flavonoids and for the other 5, it will contain an inert compound. The addict "rates the high" on a scale of 1-10. If the premise is correct, then the average rating for the grapefruit days should be higher than the other days. Since the addict doesn't know which capsules he or she is receiving on any given day, the placebo effect is negated.

You could even go one step further, and give the addict extra oxy on the days when they received non-grapefruit capsules. For example we might discover that 100mg oxy + grapefruit = 120mg oxy without grapefruit, according to the "ratings", and we'd learn that the percentage of potentiation is ~ 20%.

OK then, let's get a government grant and begin the study! All we need are some oxy addicts. You think we might be able to find somebody like that around these parts? ;D

THEPAINTER1960
04-12-2007, 12:59 PM
What ingredient in grapefruit juice enhances opiete highs? My friend says its vitamin C, but i just called him dumb. I know thats not what does it. But what does? Grapefruit juice excellent another good one is cimeitadine [tagamet] pardon the spelling. It cuts down on the amount of acid your stomach puts out,keeping the drug longer in your system.

Hammilton
04-13-2007, 12:11 AM
no painter: cimetidine or tagamet, correct spellings, works the exact same way grapefruit juice does. Otherwise famotidine and Calcium Carbonate would be just as good. Probably better.

jinxxx
04-15-2007, 06:25 PM
G juice basically inhibits the P450 liver enzyme family which is responsible for the metabolism (breaking down) of many drugs from mdma to dxm to hydrocodone into weaker, non-psychoactive or even toxic metabolites (MDMA->neurotoxins), so more of the drug stays in your system longer, especially helpful with oral ingestion and attentuation of the first-pass effect. Grapefruit's active ingredient has a really high affinity for the enzyme, bonding strongly and not letting go when a different drug comes around.

However, this is not always preferable if the metabolites are stronger than the drugs itself (prodrugs), like with codeine, which is demethylated by the enzyme into morphine.

Oxycodone's methabolic pathway utilizes different enzymes, hence the uselessness of GJ many users report.

It does not "inhibit opiates" as a general rule, in fact I only know of hydrocodone (and dxm, if you can call that an ope); practically all amphetamines, on the other hand, are affected, not only increasing oral bioavailability, but reducing the amount of much more neurotoxic metabolites.

Peace.

elegua
08-26-2007, 09:54 PM
As mentioned, grapefruit has been known to interfere with the cytochrome P450 enzyme system, which normally breaks down several types of medicines. Stop that enzyme activity, and you'll have increased levels of the medicine in your system. Tagamet has comparable effects on the cytochrome P450 enzyme. However, I should point out that the grapefruit & tagamet affecting medicine issue is NOT established as medical fact. Small studies have indicated some increased activity w/ some medicines, other studies have shown no apparent change in a medicine's bio-availability or general effects. There are larger studies in the works, but so far, it's an open question.

One can't assume that reports of positive effects, or the theory of a medical interaction, has any relation to what actually happens in the human body. Plenty of things work in theory but in practice, the body's back-up systems don't let the theory become practice. Also, and I don't mean this as an insult, but the placebo reaction is FAR greater than most realize, even to the point where many prescription medicines appear to work better when they're first introduced, compared with 10 years down the road (even in people who have never taken the medicine in question). I use grapefruit juice, but I'm not convinced it makes a difference aside from the acidity of the juice improving fluid extraction.


Also, you can quote any study you want, but that doesn't make it fact either...there are so many examples of the public accepting something as medical 'fact' because of preliminary studies that I couldn't begin to list them all...not the least of which includes the notion that bran clearly reduces some types of GI cancer, or that other brans reduce cholesterol, or that reduction of cholesterol has a direct 1 to 1 relation to reduced heart attack/stroke. Other examples that were and sometimes are still accepted as fact but have no clinical proof include the wonderous effects of soy in terms of cancer prevention and heart disease reduction, anti-oxidants (a multi-billion dollar industry) after a long study were shown to not be the wonder-drugs/supplements as was initially assumed (longer-term studies have shown NO specific health improvements or lowered disease percentages in regards to anti-oxidant supplements), or even ulcers -- for decades thought to be the result of stress and personality, and this 'fact' was later shown to be utterly untrue, with peptic ulcers being caused by a bacteria!

So...just because some interesting material makes some suggestions, doesn't mean it's true...just because you think there's some improvement in potentiation does not mean it isn't placebo (and it doesn't matter if you're brilliant or a doofus, placebo can hit us all)...and even things thought to be medical 'fact' may be just a matter of impressive marketing. For example, the anti-oxidant theory seemed very logical and sound -- anti-oxidants would remove or reduce free oxygen particles that could oxidize your cells (like oxygen rusts iron)...similarly, the tagamet/grapefruit theory is also sound. But that doesn't yet mean it is or isn't true.

smartguy
08-28-2007, 06:45 PM
these inhibit P450, a liver enzyme responsible for breakdown of many toxic metabolites.

smartguy
08-28-2007, 06:46 PM
however, doing this may also increase the blood levels of many other drugs metabolized by this set of enzymes.

WarmCyanide
09-06-2007, 09:01 PM
my back is SO fucked. yet i still work to earn the bread

so i'm taking medrol (methyprednisolone acetate) and it's fucking me up worse than the
back pain. making me feel weird in an unfun way.

i look at the novel that comes with the bottle and sure enough,
it says dont drink grapefruit juice with this medicine.

its drug class is corticosteroid.

Synack
11-26-2007, 03:49 AM
I swear the shit works, but I'm not doing it again, I took 1 40mg ER oxy, and 40mg IR oxy, then about 30oz of juice an hour before...and then became madly sick about 4 hours later, vomiting, migranes, solonmance, itchy, slow breathing, apnea, sweating, this lasted for about 36 hours and this was friday night (I really like the shit(White GF juice..plus I'm banned from coke(the soda) after 12:00 noon...bastard family - oh noes, your addicted to caffiene...shit, that's the last of my worries... meanwhile they chug down dr. pepper by the 24pack .every 3 days or so..whereas 12ct case will last me twice as long...fucktards.)

Seedy
12-21-2007, 03:42 PM
Old thread, I know, but does ranitidine also potentiate like cimetidine? Can't get tagamet otc here.

GoddessofRATs
12-21-2007, 04:14 PM
I've gotten prescriptions of antibiotics that say "Do not drink grapefruit while on this medication", so it is NOT a placebo affect.

GOR

WarmCyanide
12-21-2007, 07:52 PM
Hiram provided this in another thread: http://opioids.com/opiates/index.html

and ROxi stardust stickied this: http://forum.opiophile.org/showthread.php?t=12999

HOm did good work here too: http://forum.opiophile.org/showthread.php?t=6340

UTGDMFSE!!!!:)

tptptp
12-21-2007, 09:41 PM
My friend notices a different with GFJ or cimetidine. I've read some research that varies on it. You do need to drink quite a bit though...after drinking it for a while my friend said he noticed it when he went without.