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Opioids How Much Grapefruit Juice?

tackyjan

Greenlighter
Joined
Nov 28, 2011
Messages
33
I read on these forums that grapefruit juice potentiates opioid drugs. How much does one have to drink? Is the amount a function of the strength/amount of opioid taken? Does drinking more cause more and more potentiation or is there a point of diminished return?

Thanks!
 
I find taking diphenhydramine to be much better.
Cheaper, more effective potentiation, and has slight sedative properties on its own.
I think it can only be white grapefruit juice IIRC (that's what I used), and that stuff is a bitch to find.

As far as how much to drink, I'm sure it caps off after a certain point, but I'm not positive at what amount.
I drank about half a litre when I tried it out.
 
GFJ is more suited to potentiating benzodiazepines like Alprazolam, it increases peak plasma levels by something like ~80% (iirc), and inhibits elimination by plugging up liver enzymes like Tagamet, making the drug last much longer.

Potentiators are a bad idea in general, since all they do is either increase the peak plasma level, or keep the drug in your bloodstream longer. This seems like a good thing, but, in turn, your tolerance catches up to the "new," higher levels of potentiated drug, and you'll be forced to use potentiators every time you dose to gain the same effect.
 
I used to drink about 12-16 ounces of grapefruit juice before taking my dose. Did that for a long time...I'd drink it about 45 mins to an hour before I was planning to take my dose. It never made it more intense...but would make the opiate effect last quite a bit longer...would extend things maybe an hour or so. I'd notice that when I didn't have grapefruit juice. I guess it coulda been a placebo type effect...but really seemed to extend the feeling to me. I used ocean spray white grapefruit juice. I do know it doesnt seem to work for everybody.
 
What ErgicMergic said - "you'll be forced to use potentiators every time you dose to gain the same effect"...I surely found that to be true. So keep that in mind.
 
GFJ is more suited to potentiating benzodiazepines like Alprazolam, it increases peak plasma levels by something like ~80% (iirc), and inhibits elimination by plugging up liver enzymes like Tagamet, making the drug last much longer.

Potentiators are a bad idea in general, since all they do is either increase the peak plasma level, or keep the drug in your bloodstream longer. This seems like a good thing, but, in turn, your tolerance catches up to the "new," higher levels of potentiated drug, and you'll be forced to use potentiators every time you dose to gain the same effect.

Really? My alprazolam does not say anything about interactions with GFJ on the bottle or package insert.

The effects of repeated ingestion of grapefruit juice, an inhibitor of cytochrome P450 3A4 (CYP3A4), on the pharmacokinetics and pharmacodynamics of both single and multiple oral doses of alprazolam, a substrate of CYP3A4, were examined. In study 1, eight healthy volunteers ingesting 600 ml/day water or grapefruit juice for 10 days took a single oral 0.8-mg dose of alprazolam on the eighth day. Plasma drug concentrations were monitored up to 48 h after alprazolam dosing together with evaluation of psychomotor function. Grapefruit juice altered neither the plasma concentrations of alprazolam at any time points, any pharmacokinetic parameters, nor the majority of psychomotor function parameters in subjects. In study 2, 11 patients with anxiety disorders receiving alprazolam (0.8-2.4 mg/day) ingested grapefruit juice (600 ml/day) for 7 days. Blood samples were collected before and during grapefruit juice ingestion and 1 week after its discontinuation together with an assessment of clinical status. Grapefruit juice altered neither the steady-state plasma concentration of alprazolam nor the clinical status in patients. The present study shows that grapefruit juice is unlikely to affect pharmacokinetics or pharmacodynamics of alprazolam due to its high bioavailability.

Source: http://www.ncbi.nlm.nih.gov/pubmed/10907671
 
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