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Grapefruit Juice and Codeine

I would have to say that codeine is arguably weakened when combined with grapefruit juice, and especially cimetidine. It works for many other opiates, but from both first hand experience (ive actually tried grapefruit juice and tagamet with codeine, morphine, and the codones etc), and from what ive read, it doesnt work so great on codeine. So just take the codeine with phenergan or proglumide, even quinine/quinidine, if you want a good potentiator. Grapefruit juice is definately questionable, so why not use proven potentiators with actually significant results?
 
I find a six pack potentiates just about anything, but thats just me.

I've tried all sorts of combos with codeine, hyrdocodone, oxycodone and found that it doesn't make a whole lot of difference. The only thing I have not tried is quinine, but I cannot get it over the counter and no one I known would sling it. Perhaps it has do to with my body chemistry or something.

Dunno, take a jab at something else that will give you more bang for your buck.
 
Here's some abstracts:

[Grapefruit juice and drugs: a hazardous combination?]

[Article in French]

Lohezic-Le Devehat F, Marigny K, Doucet M, Javaudin L.

Centre Hospitalier Regional et Universitaire de Rennes, Hopital de Pontchaillou, Service Pharmaceutique, Rennes, France. [email protected]

A single glass of grapefruit juice can improve the oral bioavailability of a drug thus either increasing its efficacy or enhancing its adverse effects particularly if the therapeutic index is narrow. [BOLD]Grapefruit juice acts by inhibiting presystemic drug metabolism mediated by CYP P450 3A4 in the small bowel[/BOLD] and this interaction would appear to be more relevant if the CYP 3A4 content is high and the drug has a strong first pass degradation. Intestinal P-glycoprotein may also be affected by grapefruit juice. The compounds responsible for this food-drug interaction have not as yet been identified but this phenomenon could result from a complex synergy between flavonoids (naringin, naringenin), furanocoumarins (6',7'-dihydroxybergamottin, bergamottin) and sesquiterpen (nootkatone). In our study, we report the mechanisms of action of grapefruit juice and the interactions between grapefruit juice and 42 drugs; to date, only 12 drugs showed no interaction. Taking these results into consideration, patients should be educated about grapefruit juice intake with medication.

Publication Types:
Review
Review, Tutorial

PMID: 12611197 [PubMed - indexed for MEDLINE]


Inhibition of cytochrome P450 3A: relevant drug interactions in gastroenterology.

Sagir A, Schmitt M, Dilger K, Haussinger D.

Klinik fur Gastroenterologie, Hepatologie und Infektiologie des Universitatsklinikums Dusseldorf, Deutschland.

Cytochrome P450 3A (CYP3A) is involved in biotransformation of more than half of all drugs currently available. Drug interactions by inhibition of CYP3A are of major interest in patients receiving combinations of drugs. Some interactions with CYP3A inhibitors also involve inhibition of the multidrug export pump, P-glycoprotein. An increasing number of adverse drug reactions might be avoided on the basis of knowledge about CYP3A substrates and inhibitors. This article summarizes some examples of such interactions relevant to gastroenterologists. Serious cases by coadministration of CYP3A inhibitors resulting in acute hepatitis, hypotension, rhabdomyolyis, torsade de pointes, sedation, or ergotism are presented: interactions with azole antifungals (ketoconazole, itraconazole, fluconazole), HIV protease inhibitors (ritonavir, indinavir, saquinavir, nelfinavir), macrolide antibiotics (clarithromycin, erythromycin), and grapefruit juice. In addition, 1 case is reported who presented the highest trough levels of the CYP3A substrate budesonide in serum ever measured. Practitioners have to be aware of the high potential of metabolic drug interactions when they prescribe a CYP3A inhibitor. It is wise to check carefully comedication in patients complaining of side effects with substrates of CYP3A. Copyright 2003 S. Karger AG, Basel

PMID: 12949438 [PubMed - in process]


But, hey, whatever.
 
Anyway... does anyone know a source for proglumide? besides foreign pharmacies?
 
Domestic chemistry supply companies carry it. Some of the sources in europe are very reliable, and cheap. I dont see what the big deal is ordering overseas.
 
PM me and i will see if i can dig up that link. I know i have a source that sells it in tablet form, and it is marketed as some sort of stomach medication.
 
just curious.. is there enough quinine in tonic water to make any difference at all?
 
ok, i read this whole thread and i've just got one question: does grapefruit potentiate codeine? =D

seems like grapefruit juice inhibits CYP3A4. Codeine is broken down by CYP3A4 and CYP2D6, with CYP2D6 turning it into morphine. so it seems like grapefruit juice should keep the levels of codeine up in the blood. but codeine inhibits 2d6 too so perhaps it doesnt help that much?

http://www.postgradmed.com/issues/1999/11_99/cadieux.htm has a great table showing what each of the p-450 enzymes breaks down. looks like grapefruit juice should only affect codeine (as fas as opi(ate/ods) go.. am i interpreting the data correctly? people drink grapefruit juice with poppy tea for the codeine right, since it doesnt look like it should affect the morphine
 
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so am i right interpreting those tables to mean that grapefruit should doesnt affect the breakdown of opiates aside from codeine?
 
^it sorta looks that way but i'll be honest fizz, i,my g/f and my roomate have tired all sorts of methods w/grapefruit juice and almost every opiate/oid on the street(Hmorphinemethdadone oxy hydro etc.) there doesnt really seem to be any diffrence.if your looking for some magic tolernce recuder,this isent it :(
 
have you tried it with codeine? it looks like that is the one it would work with. I'm not looking for any magic reducer as much as im trying to find out if it is a myth that grapefruit enhances all opi(ate/oid)s. negrogesic gave a link that said it shouldnt work for codeine but i think the site is wrong.. but i dont know a whole lot about what im talking about hehe
 
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