Grapefruit Juice as a Potentiator

[fastandbulbous]

No one seems to have mentiuoned it extends the actuion of ketamine as well - CYP3a4 TURNS KET INTO NORKETAMINE

 

[SpunkySkunk347]

my psychiatrist told me that b/c I reacted so quickly and intensely to celexa (citalopram) and due to my past experience w/ other antidepressants and certain anti-psychotics that my cytochrome enzyme system, specifically the P450 enzyme and the CYP2D6 are probably inactive. Is this possible?

Also, he told me that I won't even feel codeine b/c my body can't "turn water into wine" by making the codeine into morphine (which is what is mostly responsible for the sedative and analgesic effects...or "wine")..

anyways, I guess I can't feel certain drugs to my enzymes being inactive and I can REALLY feel other ones? the whole thing is confusing to me and if anyone has any advice it would be of much help

Thanks

It's actually true. It's an enzyme deficiency that about 8% of the population has I think. Codeine won't work

 

[laCster]

important note:

A food's acid or alkaline-forming tendency in the body has nothing to do with the actual pH of the food itself. For example: Though lemons, limes, and grapefruits are chemically acid, tests show that when they are metabolized in the body they actually have an alkalizing effect and are very beneficial.

source: http://www.pureliquidgold.com/acid-alkaline-forming-foods.htm

 

[stumblestoprepeat]

I'm confused. My taking on the subject is that codeine is metabolized into morphine (desirable) by CYP2D6, while CYP3A4 turns it into norcodeine (undesirable). Sooo by potentiating with GFJ, you're lowering your levels of CYP3A4/1A2, resulting in more codeine being turned into morphine. Sound about right?

I'm also curious as to why hydrocodone isn't potentiated, while most other opiods are. Does it lack the methyl group cleaved by CYP3A4?
Edit: I see a methyl group in a 2d molecular picture of hydrocodone..hm.

 

[avcpl]

You'll want to drink at least 200mL, perhaps 500 to 750mL. One study I looked at used 600mL to represent "a lot of grapefruit juice" and 200mL to represent a standard cup of GFJ; they found that 600mL was much much more effective at potentiation than 200mL.

.

Since 750ml is a pretty massive amount, what does anyone think about putting a large amount like this over very low heat to reduce to volume?

Of course not so low that it becomes a syrup, since that wouldn't be too easy to drink (though maybe it could be mixed with a drink like 7-up or Sprite to make something akin to "Squirt".)

 

[CoReCoNTAX]

Does anyone know how much potentiation is reduced by if you drink grapefruit juice during an opiate high instead of drinking it before taking the opiates?

 

[WabbaJack]

Does grapefruit juice potentiate all benzos or just the ones listed?

I'm curious about diazepam in particular.

You'll see very little benefit, if any, with any Diazepam. The mechanism the GFJ is improving is absorbtion, but nearly 100% of Diazepam is absorbed orally anyway, so there's no room for improvement. Additionally, Diazepam is fully utilized by the body with no waste during excretion, so even if the GFJ worked as a *different* mechanism, such as keeping the Diazepam in your system longer, it would still have almost no increased effect. Diazepam is a very good drug for these reasons, you can't improve on perfection except by upping your dose.

 

[webbykevin]

I remember hearing once or twice from various people (a citrus farmer, a dietician, some health doco on tv etc) that the most effective way to get the maximum vitamin C out of an orange or a lemon or a grapefruit was to pick it and eat it right there next to the tree, and that vit C starts degrading in strength as soon as the fruit is picked, and the amount lost was quite staggering, like 10 minutes after picking it the vit c loss was 50% or some crazy figure, Anyone know if there is any truth in this ?

I remember the farmer said just poke a hole in the side and suck the juice out, don't even peel or break it up cos the air degrades it, if that is true then surely juice that has been through a processing plant, and then spent days sitting on a supermarket shelf is going to give vastly different results in potentiation or health benefits than a freshly picked fruit.

 

[mindtools]

Yeah, vit C is very sensitive to everything - it is broken down by heat, few days storage, cutting etc;
But it's not the vit C that plays the potentiator role in GF.

 

[persuasoria]

I was just going to make a post about GF juice. I'm new to the forums, so I'm glad to see this here but I'll want to bump this up so others can see it.

Looks like there's been some confusion in this thread. To clear some things up, the white juice does contain the most furanocoumarins (the CYP-450 inhibitors), however I have extensive experience with pink GF juice a 'la Tropicana, and it works fantastically if a large glass is taken up to four hours from dosing or during dosing (you gotta down that shit).

The furanocoumarins in grapefruits specifically--and most potently--inhibit the isoform CYP34A of the CYP450 class of enzymes (but it may inhibit other isoforms). Piperine does this as well (an alkaloid found in black pepper and other members of Piper). You can find black pepper extracts online, but I live in a fairly large city and as far as I've seen it's not carried anywhere here. In any case, BP extract is a very helpful substance to have on hand as it also inhibits p-glycoprotein, an enzyme responsible for decreasing absorption of a wide variety of drugs and toxins. Like I said, I've not really been able to find the extract around and I rarely order from the net so I've not been able to do much experimentation with this substance, but I do know it will potentiate the effect of certain steroids. Anyways, back to GF.

Some are confused about the interaction of GF and codeine. Codeine is metabolized by the liver to morphine by the isoform CYP2D6. Isoform CYP34A metabolizes codeine into norcodeine, and there are some other enzymes which metabolize codeine into various other forms, such as codeine salts. These various metabolites work synergistically to produce the characteristic effects of codeine. Without metabolism, codeine is likely inactive. Norcodeine (the metabolite produced by 34A) seems to be inactive, and since GF juice has only been proven to inhibit the 34A enzyme, it is unlikely that GF juice will potentiate the effects of codeine-- but you can certainly try it because it may inhibit other isoforms of CYP450.

The most important thing to remember about any compound is that it works synergistically with an incredibly large amount of other compounds both in your body and in whatever substance from which it was originally sourced. The action of GF juice is likely due to various other interactions apart from that produced by the furanocoumarins. From experience I know that GF juice potentiates MDMA, LSD, and has a claritive effect when I drink it on the comedown of sativa highs. There is no substantial scientific evidence for its effect on marijuana or LSD, yet I know that GF juice affects these substances within my body because of extensive use of the two together. So, just keep that in mind with your research-- everything is synergistic, everything works together to produce a substance's unique effects in your body.

As a side note somewhat related to this topic, if you are experiencing negative effects from smoking too much of... anything, take some coltsfoot in a tea. It contains mucilage, which is a demulcent and will form a sort of film over the mucous membranes in your mouth and throat, soothing cotton mouth and other inflammations. However, coltsfoot contains some really nasty alkaloids in low concentrations, called pyrrolizidine alkaloids. These alkaloids are only toxic, however, when they are metabolized by the CYP450s! So take a glass of GF juice with your coltsfoot. If you're not drinking coltsfoot every day then there isn't an issue, but these alkaloids are hepatotoxic, so don't take coltsfoot if you drink alcohol.

Anyways....

 

[aced126]

Nice post. But surely drinking GF juice will mean less codeine is metabolised into norcodeine, thus more codeine is available for metabolism into morphine?

 

[persuasoria]

That's a good point, and I'm sure that's the case. Do you have experience taking GF with codeine? I'm not one for the opiates really, but I'd be interested to know if there is a marked effect or potentiation.

 

[aced126]

Nah not really, only taken codeine a few times so I couldn't possibly comment anecdotally.

 

[Nightraver]

I always find the best potentiator of benzos is good old fashioned tea with milk and sugar