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Benzos Benzo Potentiators?

O-P-IT

Bluelighter
Joined
May 6, 2004
Messages
34
Does anyone know of any potentiators for valium (diazepam) or for any other benzos. Does DXM or Grapefruit juice potentiate benzos? I know they work for opiates (somewhat) but need to find something that will make my Diazapam (valium), Alprazolam (xanax), clonozepam (Klonopin), and lorazepam (ativan).
 
Grapefruit juice works only with diazepam (Valium). It potentiates it very much. Do a search on google with "grapefruit diazepam" words and it will show up.
 
Nope.

Using grapefruit juice to potentiate benzodiazepines actually works the best with alprazolam (Xanax).
Valium is not the only benzo this works with...:\
 
Can you show some links to studies on alprazolam + grapefruit? I've tried to find any connection between the two, but found only diazepam + grapefruit.
 
I would, but I'm pretty tired right now after a double shift in the E.R...:\
Check Google, though, "xanax; grapefruit" should get you where you need to start looking...
 
The only benzodiazepine that grapefruit juice has even potenated for me was alprazolam. Never Valium...
 
Actually I was right.

Grapefruit + Xanax (alprazolam) = no difference

Grapefruit + Valium (diazepam) = potentiation


Studies:

1)

http://www.ncbi.nlm.nih.gov:80/entr...ve&db=pubmed&dopt=Abstract&list_uids=10907671


Psychopharmacology (Berl). 2000 Jun;150(2):185-90. Related Articles,Links

Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam.

Yasui N, Kondo T, Furukori H, Kaneko S, Ohkubo T, Uno T, Osanai T, Sugawara K, Otani K.

Department of Neuropsychiatry, Hirosaki University School of Medicine, Japan.

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.



2)

http://www.ncbi.nlm.nih.gov:80/entr...eve&db=pubmed&dopt=Abstract&list_uids=9625273


Eur J Drug Metab Pharmacokinet. 1998 Jan-Mar;23(1):55-9. Related Articles,Links

Interaction between grapefruit juice and diazepam in humans.

Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A.

Department of Pharmacology, Medical Faculty, University of Osmangazi, Eskisehir, Turkey.

Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine. Because these drugs are metabolized by the hepatic cytochrome P450 isozyme (CYP) 3A4, the inhibitory effect of grapefruit juice is thought to results from inhibition of CYP3A4. In this study, our aim was to investigate the effects of grapefruit juice on plasma concentrations of diazepam. Eight healthy male and female subjects participated in this study. Oral (5 mg) diazepam was administered with either 250 ml water and grapefruit juice. Blood samples were collected for a 24 h period, and whole blood concentrations of diazepam were measured enzyme immunoassay. The mean AUC(0-24) of diazepam was increased 3.2-fold (P < 0.001) and Cmax was increased 1.5-fold (P < 0.05) by the grapefruit juice. Grapefruit juice postponed the tmax of diazepam from 1.50 h to 2.06 h (P < 0.01).
 
^ No, actually you are wrong. Grapefruit juice has been proven to increasse plasma levels of almost all benzodiazpeines. The strongest ones effected are: alprazolam, triazolam, midazolam.
 
Please post studies proving that. (PubMed is a great source - google.com "PubMed" and you'll find the link to the database). I'm not saying you are incorrect - I just want some back-up studies/proof whenever i hear such statements.
 
Actually there are many studies out about this interaction, with only a miniscule handfull saying that it (grapefruit) doesn't do much one way or the other.
I know that as a pharmacist, my training has told me that substances that affect the metabolism of alprazolam, do so by inhibiting hydroxylation catalyzed by cytochrome P450 3A (CYP 3A4). Substances that inhibit this metabolic pathway may have a profound effect on the CLEARANCE of alprazolam. I know that if I don't put that little sticker on a bottle of Xanax that I fill (Do not eat grapefruit/drink grapefruit juice while taking this medication), I would probably be severely reprimanded or fired. I also know that while involuntarily weaning myself from Xanax, I used grapefruit juice to lengthen the effect of Xanax/slow down its metabolism with great success (the yellow juice works better than the red). This works by inhibiting the intestinal metabolism of benzos, thereby increasing the plasma concentration.

Some personal experience of mine finds this to be true. I almost died from Xanax withdrawl, and towards the end of my supply, I stretched them (1 mg Xanax) WAY out with (you guessed it...) grapefruit juice.

From the PDR: "Available data from clinical studies of benzodiazepines suggest a possible drug interaction with alprazolam for the following: diltiazem, isoniazid, macrolide antibioticssuch as erythromycin and clarithromycin, and grapefruit juice."

See also: www.fhma.com/grapefruit.htm

You are partially right Bouncer, as this also is the case with diazepam...;)
 
Last edited:
vicodelicious said:
...but yes you're right.

I should hope so...I took out several large loans and studied long and hard hours to be able to put that little "R.Ph." behind my name...;)
 
Yeah, you guys were right. Although studies on Xanax (alprazolam) do show that sometimes grapefruit interacts with it and sometimes it doesn't. But overally I think it does, just like with Valium (diazepam).
 
Thanks for all the info guys, last night I ate half of a very large grapefruit, took 2 10mg valiums and 1 flexeril then smoked a bowl of some decent pot. After they kicked in it seemed to be a lot stronger than normal. I ended up passing out upstairs on the couch, I dont remember much but when I woke up at 4 a.m. there were doritos all over the whole couch lol. I think I went on a munchie frenzy ha ha. Thanks to everyone who helped me out with all this great info........ Can anyone say that it works from personal experiance. From what happened last night I think it does, but I havent taken any benzos for at least 2 weeks so Im not sure if They just hit me really hard from not doing them forever or maybe the flexeril and pot did something to increase the effects. Im not sure, any replies would be appreciated. THANKS
 
Any drug which is metabolized by CYP3A4 is going to be affected by grapefruit juice.


X
 
Does anyone have a link of a website or something that shows which drugs are metabolized by CYP3A4??? Thanks
 
well on my xanax script description print out it says grapefruit juice potinates alprazolam
 
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