# Grapefruit Juice as a Potentiator



## frizzantik

I posted this in OD as the Grapefruit Juice FAQ but i'd appreciate any comments from the ADD crowd as this isn't really my area of expertise 
*Grapefruit Juice FAQ*

Grapefruit juice can act as a potentiator for the following prescription drugs sometimes used recreationally:
codeine
methadone
oxycodone (OxyContin, Percoset)
dextromethorphan (DXM)
alprazolam (Xanax) 
clonazepam (Klonopin, Rivotril)
midazolam (Versed)
triazolam (Halcion)
Caution should be excercised if consuming grapefruit juice before or while taking these drugs.  Though most people report mild potentiation (if any), if one is taking extremely large doses, any potentiation could be dangerous.

*Method of Action*
Grapefruit juice can inhibit the gastrointestinal activity of two enzymes known as cytochrome P450 CYP3A4 and CYP1A2, though the effect on CYP1A2 is minimal.  This causes elevated plasma levels of some drugs, because they are able to pass into the bloodstream without being broken down by enzymes in the intestine.  Due to variations in enzyme levels in the intestine from person to person, effects will vary.  

The specific chemical responsible for this action is not known.  There are a few suspects including various flavonoids and other phytochemicals called furanocoumarins. Concentrations of these compounds vary from one batch of juice to another. Higher concentrations are found in white juice compared to red, and the highest concentrations are found in the pulp of the fresh fruit.  One glass (200 ml) of fresh juice was found to be equal in effect to two or three glasses of double strength reconstituted frozen juice.  This suggests that store bought juice, which is often from concentrate, must be consumed in large quantites to for effects to be noticed.   Consuption of 6-8 glasses of fresh juice may lead to inhibition of CYP3A4 in the liver.  The potentiating effect of grapefuit juice may last 5 or mores hours after ingestion.

*A Note on Codeine & Oxycodone*
Codeine is metabolised by both CYP3A4 and CYP2D6. CYP3A4 metabolised codine into norcodine which isn't very active, while CYP2D6 metabolises codiene into morphine which is responsible for codiene's effect.  When the CYP3A4 enzyme is inhibited by grapefruit juice, more codiene may be metabolised by CYP2D6.  This is theoretical and is not supported by literature at this time.

Like codeine, oxycodone is metabolized by both CYP3A4 and CYP2D6, with the more potent metabolite, oxymorphone, produced by CYP2D6.  When the CYP3A4 pathway is blocked, more oxycodone may be metabolised by CYP2D6.

*Grapefruit Juice and Cimetidine (Tagamet)*
Cimetidine acts on a different enzyme than grapefruit juice, specifically CYP2D6.  CYP2D6 metabolises many opiates and opiods, but grapefruit juice has no effect on CYP2D6.

*Sources:*
http://www.postgradmed.com/issues/1999/11_99/cadieux.htm
http://www.powernetdesign.com/grapefruit/references/ref80abstract.html
http://www.mayo.edu/proceedings/2000/sep/7509r1.pdf
http://www.ncbi.nlm.nih.gov/entrez/...ve&db=PubMed&list_uids=10872589&dopt=Abstract
http://www.tthhivclinic.com/pdf/Recdrug2.pdf


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## BilZ0r

You might want to check out this abstract too. Put in something like "Although grapefruit juice is a well know inhibitors of CYP3A4/5 it also may have some action on CYP1A2, (I know you said that one), 2D6 and 2C9.


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## ebola?

and it tastes great!!!!111one!!@

ebola


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## frizzantik

Bilzor, that abstract says "Inhibitor concentration required for half-maximal rate of inactivation (K(I)) values for bergamottin, DHB, GF-I-1, and GF-I-4 were calculated, respectively, as 40.00, 5. 56, 0.31, and 0.13 microM,"

i take that to mean bergamottin and DHB must have a lot higher concentrations to see inhibition, right?  bergamottin was show to cause inhibition quite a few enzymes but only if it was in a very high concentration. i wonder how much of each of those 4 substances is in a glass of juice


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## BilZ0r

40µM although not as potent as the others, still isn't like, weak. But yes, the most important thing is whether gastric and hepatic concentrations get up to those levels, which is a matter of the concent in the juice, absorption and metabolism... all of which are probably unknown.


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## AshleighWho

How much grapefruit juice would you need to drink to optimise the effect of 300mg of codeine phosphate? Also should I drink it before I take the codeine? (and if so, how long before?)
Thanks,
Ashleigh


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## mindtools

When is it best to drink the juice?
Few hours before codeine, or just before/after?


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## Coolio

From the scientific studies I've read, you want to drink white grapefruit juice 30 minutes before taking the other drug. 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.

Ruby Red grapefruit juice is low in P450 competitive furanocoumarins and flavonoids compared to white grapefruit juice.


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## Gormur

i _just_ consumed 600ml/20oz of white grapefruit juice, tho i took 2mg alprazolam approx 20 minutes previous; the sedating effects are beginning to kick in once again and much harder this time! wow :D

i will definitely have to see how dosing after drinking the juice works as well and report back with results... if i'm able to type anything by then 

this is great tho, that is, if it isn't too harsh on my liver, i can definitely extend my script further when needed

would dark chocolate/cacao nibs also work as a potentiator? i forget which enzymes it works on

peace


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## seep

Gormur said:


> i _just_ consumed 600ml/20oz of white grapefruit juice, tho i took 2mg alprazolam approx 20 minutes previous; the sedating effects are beginning to kick in once again and much harder this time! wow :D



Sedation is one thing, but I can't imagine that the anxiolytic effect of alprazolam will be augmented with CYP3A4 inhibition. By extension, the recreational/euphoric value of this type of potentiation is poor. It's not exactly the same as increasing your dose, and since alprazolam has an active metabolite, the synergism between drug and metabolite falls out of phase. Qualitatively speaking, it's hard to be calmly active when you're overly sedated.


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## theWorldWithin

I would have to disagree, it seems that in most people's trip reports they clearly experience potentiation of effects in addition to a longer duration. Also what is not recreation about either of these, sound like a plus to me. 

Further most of the drugs we are talking about using GFJ with benefit from less metabolites and more of the parent compound in your blood stream. Oxy and Hydro are primary examples where only an inperceptable dose is converted into active metabolites stronger than the parent compound. For how little hydro/oxy-morphone that is yielded metabolically you are better off with higher concentrations of the parent compound.


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## seep

theWorldWithin said:


> I would have to disagree, it seems that in most people's trip reports they clearly experience potentiation of effects in addition to a longer duration. Also what is not recreation about either of these, sound like a plus to me.
> 
> Further most of the drugs we are talking about using GFJ with benefit from less metabolites and more of the parent compound in your blood stream. Oxy and Hydro are primary examples where only an inperceptable dose is converted into active metabolites stronger than the parent compound. For how little hydro/oxy-morphone that is yielded metabolically you are better off with higher concentrations of the parent compound.



I've always found that GFJ doesn't let me function well while on alprazolam. That tends to kill the buzz for me. Last semester I coadministered the juice before an exam. Usually the xanax helps me concentrate by minimizing cognitive dissonance, but with the GFJ I couldn't even remember what the jacobeans were for spherical integration (rho squared sine phi where phi is the inclination from the positive z axis). I've always attributed this over-sedation to the role of the active metabolite being fucked with. If I'm wrong, then what's actually going on?

I just don't like the "flavor" of the buzz when I potentiate with GFJ. Same goes for hydrocodone. Strangely, the opposite is true for methadone. I even dissolve the Methadose wafers in grapefruit juice, and the high is significantly more intense. Maybe it has to do with the drug's duration of effect?

Thanks


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## theWorldWithin

Hard to say but I will state this: When I drink large amounts of GFJ I feel a definite alteration in perceptions and bodily functioning (specifically urinary problems). Perhaps this is just placebo in anticipation of the goodies I am about to consume but it seems quite defined to me. Something I do not experience in anticipation when there is no GFJ consumed. 

So I certainly do not discount it altering the 'flavor' of the experience for you. I can say without a doubt there is more going on that a simply lengthened experience. However I can not explain the pharmacodynamics at play.


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## gubulars

Now I think I'm correct on this, but the grapefruit will work as a potentioner regardless if you eat the oxycodone/snort it/ etc ... because this is working at the liver level at this point so it really wouldn't matter what route it enters the body.. correct?


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## Korn3x

how good is the Ruby Red Grapefruit juice form Publix? (the one that's 100% grapefruit juice and NOT made from concentrate)

would i be better switching to some brand of white grapefruit juice with pulp?\

oh and i'm using the potentiation effects for oxycodone


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## 10YR AA Gone

Just a thought with oxyxodone...

Those liver enzymes you are blocking???

Sure they metabolize oxycodone out of your body quicker, BUT

They also are responsible for metabolizing oxycodone into OXYMORPHONE

So when you do this you are missing out on part of what the enzymes break the drug into, which are other potent opiates.

The best potentiator to oxycodone is FAT.  Yep FAT.  Eat a ton of peanut butter.

http://www.purduepharma.com/PI/Prescription/Oxycontin.pdf



> However, the peak plasma concentration of oxycodone increased by 25% when a OxyContin. 160 mg Tablet was administered with a high-fat meal



So you can potentiate and still get all those yummy metabolites.

Let me tell you though - doing this will raise your tolerance quickly, be careful what you wish for!


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## avcpl

So would eating a high-fat meal help if you are plugging? (I have to due to nausea with opiates). 
I mean would you have to take it orally with a "ton of peanut butter", or would your serum lipids be increased and any ROA would be potentiated?


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## seep

Korn3x said:


> how good is the Ruby Red Grapefruit juice form Publix?



It's OK for the price. I mean, there are better tasting Ruby Reds on the shelves, but with grapefruit juice who cares? 

Winn-Dixie's is another story altogether. It tastes like straight ass.

Dole is also a good option. My personal favorite is Indian River, with Florida's Best running a close second.


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## Unbreakable

It also does the same thing with Paxil.


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## Korn3x

seep said:


> It's OK for the price. I mean, there are better tasting Ruby Reds on the shelves, but with grapefruit juice who cares?
> 
> Winn-Dixie's is another story altogether. It tastes like straight ass.
> 
> Dole is also a good option. My personal favorite is Indian River, with Florida's Best running a close second.



ya i love indian river. i usually get their orange juice, but haven't had their gfj yet.


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## BrutalRollar

Would this apply to mdma? Or any mdxx chemicals?


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## Tdaddy

man...i really cant find white gfj...or am i just gonna have to buy white GF'S?


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## anarchogen

it should potentate diphenhydramine hcl too,
since from what i've read it is metabolized by CYP2D6/CYP3A4.
but fuck that stuff.

grapefruit juice definitely works for potentating dxm/codeine in a way, but the diarrhea after dxm is horrendous.


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## puckboy

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

I'm curious about diazepam in particular.


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## puckboy

bump

anyone? All benzos or just the ones listed?


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## /navarone/

Do you think wine could possibly have similar properties?

Me likes wine a lot :D


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## StrawPipes

I'm curious about the grape fruit juice.  I get my Methadone prescribed to me on Wednesday and hopefully this will work a good as people say it does.  Should i dissolve my dones in the GFJ or should i drink a shit ton of GFJ then take the dones 30 minutes later?


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## Hoes call me santa

Just want to add a little personal experience.

I work in a drugstore, and have to change garbage bags where the pharmacist and his crew work. I often see him make methadone and mix it with Tang powder, to give it a little taste I guess, or make it more potent. 

Would "Tang" contain the same potentiators as grape fruit or is it only for the taste? Because I see people drinking it on place, and they seem not to like it really, looks like it taste bad also!


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## NomNomNom

Will it work with wine? No. Wine is an inebriating substance so it may augment the feeling from opiates or interact with, but not really potentiate. Personally I almost never adulterated my opiate buzz with booze because I can get booze any time but not so much percocet =-) I think of potentiation as something achieved by a substance with no active ingredients that's more or less mundane on its own.

I have no experience with methadone but if it were me I'd choose to slam 16-32oz of WHITE gfj about  a half hour before taking the dose. I would just be concerned that something could go wrong with soaking the (wafers? WTF? Heh, I'm a noob) drug in juice. Furthermore drinking the juice in advance is a proven thing.

The pharmacist is likely mixing with just Tang and no potentiators. A pharmacist's job is to reduce harm and avoid potential interactions so it would seem counterintuitive for one to load up the drug with goodies to make it hit harder. 

Also just to re-stress this, this works with WHITE grapefruit juice. From what I gather the ruby red might offer some benefit if you drink about a gallon but is largely worthless. ALSO just as a heads up - it took me FIVE stores to find a place with white grapefruit so plan ahead if you're looking to amp up your buzz like this. I'd suggest strongly that you go straight to a supermarket since I paid $3.49 for one quart at a convenience store.


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## pirat3

I didn't believe any of this until i read in in a medical textbook a few months ago. I just wish that they found a way to pill whatever does this and sell it as a supplement or something, i would rather pop a couple supplements than drink a ton of GFJ....the stuff gives me heartburn and tastes kinda icky...


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## Coolio

pirat3, what you're looking for is 6',7'-dihydroxybergamottin. There's a commercial product on the market, it may or may be bullshit, I dunno, but it's called SciFit Liquid DHB. It's supposedly just 50mg of pure 6',7'-dihydroxybergamottin per serving, the main CYP3A4 inhibiting furanocoumarin found in grapefruit.


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## Free_Man**

AshleighWho said:


> How much grapefruit juice would you need to drink to optimise the effect of 300mg of codeine phosphate? Also should I drink it before I take the codeine? (and if so, how long before?)
> Thanks,
> Ashleigh



please dont anyone try taking 300mg of codeine unless ur tolerance is sky high - even then proceed with caution


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## Free_Man**

puckboy said:


> bump
> 
> anyone? All benzos or just the ones listed?



please be careful with benzos and opiates combined ... dont over do it - and learn ur stuff first


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## Coolio

Free_Man** said:


> please dont anyone try taking 300mg of codeine unless ur tolerance is sky high - even then proceed with caution



What? 300mg is a normal recreational dose for non-tolerant...


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## boohigh

It's always wondering me how opiate naive i am, abusing meth, amp and alpha-ppp for 3 years intravenous, i have never done more then 160 mg of codeine and it was kicking my ass.
Maybe it's more stronger opiates you have used before, they tend to escalate the dose even you you use them rarely.



Coolio said:


> What? 300mg is a normal recreational dose for non-tolerant...


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## Free_Man**

Coolio said:


> What? 300mg is a normal recreational dose for non-tolerant...



i would disagree with that , i would NOT recommend taking 300mg unless you had built up a tolerance .

this is a harm reduction forum. if opiate naive people take 300mgs of codeine they are likely to throw up - and feel very ill and itchy - im sure you agree with me on this my friend?

300mg is not a normal recreational dose for the non tolerant in my opinion.

start at 120mg and work your way up from there - over a period of days...
imo there isnt much point going much above 300mg as a MAX dose.

codeine has a ceiling doseage limit , the liver and cyp-2d6 can only convert so much of the stuff into morphine. if you wanna get higher switch to a stronger opiate...

peace


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## Coolio

Vomiting and itching are requisite parts of recreational opioid use, I thought...


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## puckboy

Free_Man** said:


> please be careful with benzos and opiates combined ... dont over do it - and learn ur stuff first



Uh, never said I was going to combine them. Just wanted to know if GFJ potentiated all benzos.


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## Free_Man**

puckboy said:


> Uh, never said I was going to combine them. Just wanted to know if GFJ potentiated all benzos.



ok got ya but grapefruit juice is generally used to potentiate opiates not benzos.

to be honest it wont do much with opiates either.  

if u wanna potentiate benzo-s then there are other ways - the effective methods usually involve other drugs - and with the sensible user who wishes to survive - caution

peace


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## fastandbulbous

Will only potentiate drugs with a methyl group removed by CYP3A4


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## alantis360

theWorldWithin said:


> Hard to say but I will state this: When I drink large amounts of GFJ I feel a definite alteration in perceptions and bodily functioning (specifically urinary problems). Perhaps this is just placebo in anticipation of the goodies I am about to consume but it seems quite defined to me. Something I do not experience in anticipation when there is no GFJ consumed.
> 
> So I certainly do not discount it altering the 'flavor' of the experience for you. I can say without a doubt there is more going on that a simply lengthened experience. However I can not explain the pharmacodynamics at play.



i feel the same way


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## Arzi

I remember it was a very sunny day...


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## mindtools

http://en.wikipedia.org/wiki/List_of_drugs_affected_by_grapefruit


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## fluxy

pirat3 said:


> I didn't believe any of this until i read in in a medical textbook a few months ago. I just wish that they found a way to pill whatever does this and sell it as a supplement or something, i would rather pop a couple supplements than drink a ton of GFJ....the stuff gives me heartburn and tastes kinda icky...



THey DO!!!!

(more or less)  its called Cimetidine,  brand name tagamet.  ITs not the same chemical at all, but the effect your looking for is the same.   Prescription only in Australia,  But its not like your gonna be denied by your doctor for essentially something for an uspet stomach/reflux,  in my oppinion! and OTC in the states i think


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## mindtools

There are pills with grapefruit extract, used for losing weight


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## Self-Aware

It'd be nice if there was a final word on the matter. I only skimmed this thread, but from the research I've done it seems if it's morphine you're taking, then grapefruit juice is the potentiator (is that even a word?) but if it's codeine you're dosing then grapefruit juice actually inhibits, at least some part, of the conversion to morphine by the liver.


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## ebola?

To my knowledge, the above post is correct.  So, then, is it CYP34A that metabolizes codeine into morphine?



> 300mg is a normal recreational dose for non-tolerant...



for those non-tolerant looking to get FUUUCCCKKKED up.  Isn't 400 mg the ceiling for codeine dosing?  Wouldn't 300 mg codeine be equipotent with 50 mg hydrocodone?

I have an oddly high natural tolerance to opioids, but no acquired tolerance, and 20 mg is my sweet spot for the latter, for light-moderate fx.  Then again, I don't particularly enjoy 'nodding', and nausea is a near deal-breaker for me.

ebola


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## jorder1010

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


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## dread

If those specific enzymes that metabolize codeine to morphine are inactive or nonexistent in you, then you won't feel codeine because it needs to metabolize into morhpine or it will not bind to your mu receptors.

However this will not affect any drugs that do not require metabolism by those particular enzymes to become active.


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## Hodor

So is there any major difference in "potentiating potential" in different colours of grapefruits of varying degrees of bitterness?

Since the actual inhibitor seems to be the aglycone (i.e. the non-sugar part of the glycosides), a glycoside that has had some of its sugars cleaved off may taste significantly less bitter, but should still work just as well as an inhibitor.


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## Self-Aware

Big fan of the 'opiate nod'  and cannabis takes care of the nausea for me.


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## badwolf

boy can I attest to the dxm burst,

seemed like i had got the wrong bottle till I realised I had gotten gf juice that day - I didnt even think.... stupid me, but wow..  double the fun, twice as long, but scary...

as they say, you dont get to heaven if you're afrad to fly!


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## Self-Aware

Does grapefruit  juice work well as an opioid potentiator for eating morphine tablets? (oral)

What about antihistamines?


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## negrogesic

Coolio said:


> Vomiting and itching are requisite parts of recreational opioid use, I thought...



Not at all. Opioids, even at massive doses, dont make me vomit. Itching, yes....


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## beamish

i dunno about grape fruit juice. ive tried it but the differences in high are easily chocked up to variables like diet, sleep, stress, etc. 
one good rule of thumb for all opiates though is the more acidic your system is - the quicker the drug will go through your system, but also it will hit a little harder. whereas the more base your system is, the less peak euphoria you will get but the high will last longer.
eat some tums, drink some orange juice - see what works out. just don't over do it with the basifiers. I suppose the same goes for anything acidic, but you should feel the warning burn before you can eat a harmful amount.
I personally prefer sodium bicarbonate to calcium-based basification. 
Also, don't expect some miracle, this is all marginal changes at best.


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## deejvy

I have a small amount of these two "drugs":

*Alprazolam
*Codeine

Will they both be intensified by drinking GFJ, or not?  Want to get the best out of the little I have left!

I am soooo confused, all these contradicting statements regarding codeine. Yes/no, Yes/no?!?! 

Take care ya guys 

Quick respond appraciated!


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## ranunky

deejvy said:


> I have a small amount of these two "drugs":
> 
> *Alprazolam
> *Codeine
> 
> Will they both be intensified by drinking GFJ, or not?  Want to get the best out of the little I have left!
> 
> I am soooo confused, all these contradicting statements regarding codeine. Yes/no, Yes/no?!?!
> 
> Take care ya guys
> 
> Quick respond appraciated!



codeine, no. alpraz, yes.


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## Unlucky

If garepfruit acts as an inducer for the cytochrome p450 enzymes like cyp2d6 to give a better high then what if your already overly sensitive to drugs and you want less high or side effect will using the something that *inhibits* the CYP2D6 enzyme result in less side effects ? 

I know for a fact that ultra metoblisers have adverse effects and so too poor metobolisers, so its only the normal metobolisers (extensive metobolisers) like yourselves who are able to sucessfully use potentiaters but for some who is already sensitive what would an inhibitor do ?


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## Supreme

*Grapefruit/Tegamet Booster*

On my Triazolam(Halcion) perscription bottle it always comes with a sticker that says avoid taking with grapefruit juice.In my personal experience Ketoconazole 200 mg boosts Alprazolam 3-fold and in my Mosby which says the same thing as the PDR,co-administration with cimetidine increases the maxima plasma concentration of Alprazolam by 86%,decreases clearence by 42%,and increases half life by 16%.Under Triazolam interactions coadministation of cimetidine increases the maxima plasma concentration by 51%,decreased clearence by 53% and increased half-life by 36% and coadministartion withgrapefruit juice(doesnt say red or white increases maxima blood plasma25%increased area under the curve by48% and increases half life-by18%.I know the last bit wont do many people any good,because Im the only one I know of who has a Halcion script.$ of those 0.25 and your out like a light even if your wired.For Morphine it says cimetadine in a isolated report when taken together I.V'ed confusion and severe depressionwhen taken by a hemodialysis patient.And it oxycodone is a known inhibitor of P450 2D6 so drugs like soma,hydroxazine HCL,Phenegren should boost it.As far as 300 mg of codiene I was locked up for around 2 months when a kid in my dorm seperated his shoulder and the nurse was giving him codiene#4's (60mg) and I didnt have anything for 2 months so I traded some of my candy and took 7 of them I did not get a buzz what so-ever.And I heard him ask the nurse what they were and she said codiene 4's plus I looked it up when I got out and they were real.Codiene is by far the weakest opiate,well its got a good fight with Darvon for that spot.Ive read a few times a codiene 3 is as effective as 2 aspirins in a controlled study.After 4 months of jail I got released and bought my friends vicoprofin script only 15 qtybut 7.5mg of hydro-codone and ate 10 off the bat and didnt feel anything its like my tolerance never lowers no matter how long im away from opiates,I think 17 years of methadone has done this.Sorry for typin a book


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## savageIB14dabooks

thats cool..... thanks for that...


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## fastandbulbous

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


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## SpunkySkunk347

jorder1010 said:


> 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


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## 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_


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## 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.


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## avcpl

Coolio said:


> 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".)


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## 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?


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## WabbaJack

puckboy said:


> 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.


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## 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.


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## 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.


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## 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 CYP*34A* 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 CYP*2D6*. Isoform CYP*34A* 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....


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## 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?


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## 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.


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## aced126

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


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## Nightraver

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


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