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  • BDD Moderators: Keif’ Richards | negrogesic

Grapefruit Potentiation of Klonopin

D

DroidOpioid

Bluelighter
Joined
May 26, 2010
Messages
85
Hi, I have a grapefruit tree that I bought years ago when I was like 10 yrs. old that finally had a few fruits! Also, I have 1.75mg Klonopin left from a prescription from a few months ago that I've kept for some time in the future.

I've never liked grapefruits before, at least not store-bought ones, but MY grapefruits are delicious :) I was wondering, if I were to eat a grapefruit a couple hours before dosing the small amount of Klonopin I have left (1.75mg) would it potentiate it noticeably?

Also, I've searched the web, but I can't tell if it is known exactly what chemical in grapefruit is responsible for the potentiation.
 
akmoler said:
Warnings on meds usually explicitly mention juice. You may notice your buzz lasting longer, if anything, after just eating a grapefruit. Don't quote me, but I think the dangers of it are if you're drinking lots of juice and popping pills everyday.
Click to expand...

My question was regarding recreational use. I got over the anxiety I was scripted for after a day of DXM when I realized that I was causing all the anxiety myself. I stopped caring what people though, and ta-dah. Literally. It's been two weeks since then and I'm still fine. And I had this anxiety for 10 years. If only I had known it was this simple... people tell you to stop worrying, but it's hard to stop if you don't even realize that you ARE worrying and being self-conscience. :\

Anyways... yea, I'm not worried about any dangers of over-potentiation. I want to have fun with my last bit of Klonopin 1.75mg, but I will barely notice it at this dose. My preferred dose for fun is like 20mg Valium + 4mg Klonopin, but my Valium and the rest of my Klonopin has been long gone.

I think I have a rather large natural tolerance to benzodiazepines, because threshold effects of Valium for me start at ~15mg, and for Klonopin it's about 3mg. One time I took ~25mg Valium and ~4mg Klonopin, and I went to school and did fine on all my tests. Got an A and a B. If I wasn't bored, I could have stayed up easily. The only times I actually got kind of tipsy from benzos without taking alcohol was when I mixed it with 50mg Meperidine + 100mg Promethazine. I couldn't walk straight, but I still remember it fairly well and it's like my motor functions were affected more than anything else.
 
grapefruit juice works as a potentiator.
white grapefruit juice is better than say ruby red.

From my understanding, and someone please correct me if I am wrong, but the gf juice won't make the effects any stronger, just make them last longer. So plan ahead, if you have something important to do and don't want to be in a benzo daze, then keep that in mind before dosing.

Clonazepam has a decently sized half life on its own. And I can't give any numbers on how long the gf juice will increase the half life by.

Here is a link for a long thread about the subject:
http://www.bluelight.ru/vb/showthread.php?t=139536

"Any drug which is metabolized by CYP3A4 is going to be affected by grapefruit juice."
 
Actually you are right I think.
I must have been thinking of alprazolam.

shed some light on why clonazepam isn't affected? or why its only mildly affected? Isn't it metabolized by CYP 3A4 ?
 
from the old thread on benzo potentiation:

what I've gathered is that no one was quite sure about Clonazepam and GFJ.

The general rule was the Triazolo subclass (such as alprazolam [xanax]) are certainly affected.
Nitro sub class seems to be affected to.

I would assume Clonazepam falls under the nitro class of benzos, from looking here:
http://en.wikipedia.org/wiki/Benzodiazepine#Pharmacology

and here:
http://en.wikipedia.org/wiki/Clonazepam

Clonazepam has a substituted nitro group on the 7 position (when looking at the standard numbering from the first link)

However, I am still uncertain, if GFJ doesn't work on clonazepam, why GFJ doesn't work on all benzos metabolized by cyp 3a4

perhaps this would be better suited for ADD?
 
Well, I'm not sure if eating my red grapefruit had any effect (I ate half a grapefruit yesterday) but the Klonopin I took this morning was actually 1.25mg, not 1.75mg like I had originally thought.

It also had a stronger effect then I thought it would. I took it this morning and was feeling mentally 'dull' but not really tired, or maybe I didn't notice it, but when the last bell rang for end of school (and this bell is loud) I didn't wake up. I woke up like 3 minutes after.

Reminded me of the days when I would go super benzo'd up with alcohol or opiates. Not good during school, and there is absolutely no euphoria involved for me. I woke up feeling horrible. (horrible like sad).


Does anyone know what chemical in Grapefruit Juice is responsible for affecting the metabolism of some drugs? Has it been isolated?
 
mgrady3 said:
from the old thread on benzo potentiation:

what I've gathered is that no one was quite sure about Clonazepam and GFJ.

The general rule was the Triazolo subclass (such as alprazolam [xanax]) are certainly affected.
Nitro sub class seems to be affected to.

I would assume Clonazepam falls under the nitro class of benzos, from looking here:
http://en.wikipedia.org/wiki/Benzodiazepine#Pharmacology

and here:
http://en.wikipedia.org/wiki/Clonazepam

Clonazepam has a substituted nitro group on the 7 position (when looking at the standard numbering from the first link)

However, I am still uncertain, if GFJ doesn't work on clonazepam, why GFJ doesn't work on all benzos metabolized by cyp 3a4

perhaps this would be better suited for ADD?
Click to expand...

Yes but I don't know if the nitrobenzodiazepines are affected by grapefruit juice. The only ones I'm aware of that grapefruit juice affects is the triazolobenzodiazepines. But this is just what I've read. I found no sign of proof, just a website that could have been written by some 18 year old or something.

But the OP said it affected him but then again placebo is a "very" powerful effect.
 
K'd-OUT-in-AZ said:
Yes but I don't know if the nitrobenzodiazepines are affected by grapefruit juice. The only ones I'm aware of that grapefruit juice affects is the triazolobenzodiazepines. But this is just what I've read. I found no sign of proof, just a website that could have been written by some 18 year old or something.

But the OP said it affected him but then again placebo is a "very" powerful effect.
Click to expand...

I didn't say that I thought that the juice affected me; I said it might have. The Klonopin did for sure.
 
I have seen many people claim both: it does potentiate (or extend the effects); it does not. My feeling is it does, but I don't really know.

At least for alprazolam, most opioids, etc. -- everything else it potentiates -- I believe that what does it are quercetin, bergamottin, and related chemicals in gfj.

White grapefruit juice is better, supposedly (not that I have any particular knowledge about the manufacturing processes of fruit juices), because it includes the peel..
 
Well i've got a bottle full of klonopin, I'll try to remember get some white GFJ this weekend and do a few tests for myself.

again this is only from wiki but reading here:
http://en.wikipedia.org/wiki/Grapefruit#Drug_interactions

I gives a list of the 2-3 chemicals in grapefruit responsible for CYP 3A4 inhibition. But also interestingly enough it says hepatic inhibition only occurs at higher doses (of GFJ). So perhaps the reason Clonazepam, and I assume then other nitro-substituted benzos are only weakly (if at all) affected by GFJ is that you simply need to ingest a lot of it to get hepatic inhibition.

Clonazepam is metabolized hepaticly (not sure if that's the correct term), ie. in the liver via the CYP3A4 enzyme. Thus, in order for potentiation to occur, you need the hepatic CYP3A4 enzymes to be inhibited not just those that exist in your gut.

Alprazolam [xanax] is listed on the right side of wiki as being metabolized by hepatic CYP3A4 also, but under the pharmacokinetics section it claims that it is rapidly absorbed in the GI track.

This leads me to believe that perhaps those benzos and other drugs that get absorbed better in the GI track can be potentiated better with GFJ simply because it primarily inhibits CYP3A4 enzymes in the GI track and only weakly inhibits those enzymes in the liver.

this is just speculation however
 
Last edited:
yeah i'm on this too yall. Blasted all that jack a couple hours ago. I keep forgetting what I'm trying to do. I think I was gonna... fry some burgers, but that's in the kitchen. Did I start it? Fuck it. Back to benzos plus bonus fun:
anything noteworthy will be reported.
anything non-noteworthy will be reported if i don't black out a lot in the next 24 hours.

Wait, where is this? How did I get here.
 
http://www.ncbi.nlm.nih.gov/pubmed/10907671

Abstract

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.
 
No idea, they don't mention anything about avoiding Grapefruit juice on the bottles in Oz
 
been over a year since i had a xanax Rx, now on cloanzepam and temazepam. but i definitely remember the xanax bottle here having a mention about grapefruit. [usa]

never bothered to look on my others, checking now:
nope just the generic stickers saying no booze!


but looking at the actual paperwork Rx's (I keep them with me incase i ever get in trouble with the law and they find a bottle of pills in my bag..)

nothing special on the temazepam except mentioning valproic acid.
but clonazepam paper mentions a whole big list of other drugs that may require "additional monitoring of your condition" some noteworthy are birth control, ghb, cimetidine (this is a known potentiator right? or am I mistaken), a bunch of anti-depressants, methadone, and St. John's Wort.
 
Yeah here it just says booze nothing about grapefruit. Everywhere i read on this site everyone says it potentiates the effects of Xanax but that study says it doesn't?
 
Sorry if this has already been asked, but does it just extend the duration of the high or does it also weaken it (basically just stretch the dose out a little)
 
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