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  • BDD Moderators: Keif’ Richards | negrogesic

Diazepam, Grapefruit juice and cytochrome P450 CYP3A4

Dopam1ne

Dopam1ne

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Joined
Apr 19, 2012
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21
Not sure if this should be posted in the basic drug discussion tbh, so mods feel free to move this post!

I'm fully aware this has been discussed many times before, but I'm unsure as to how exactly gfj affects diazepam.
Does it simply just increase the bioavailability by inhibiting the enzyme, or is there more to it than that? IE it will increase the half life of the drug too. Will consuming gfj hours/days before or after ingestion have some effect?

And lastly, is the potentiation very significant or is it just a slight boost? Obviously there are a ton of variables that are in play here, such as the amount of gfj consumed, dosage of diazepam, etc.

Links to good sources would be appreciated too :)
 
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After a little research it seems like it simply increases the bioavailability, due to it only affecting these enzymes in the intestines. Please correct me if I'm wrong! (sorry for the double post)
 
It seems like if definitely potentiates diazepam, and the science backs this up, although it's somewhat minimal imo. It's Probably due to the very high oral bioavailability, which is > 90%. Oh and btw, don't underestimate the placebo effect ;)
 
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The issue with a placebo is that the user has to perceive it as effective otherwise it's worthless. His underestimation of the placebo is probably spot on for his own person.
 
Personally i didnt really notice a difference when drinking bio grapefruit juice with my xanax. If something it made me slightly more sleepy but im not even sure lol
 
euphoricnod said:
The issue with a placebo is that the user has to perceive it as effective otherwise it's worthless. His underestimation of the placebo is probably spot on for his own person.
Click to expand...
I concur, but placebos can be effective if given to the right individual.
 
Grapefruit juice (1 hr before for best results) can increase the bioavailability and half-life (length of time drug stays in your body) of drugs that are primarily metabolized by CYP3A4. Diazepam has a half-life of 2-3 days. That's huge. Most drugs are nowhere near that (hydro and oxy are about 5 hrs for comparison). Drugs that have high bioavailability and long half life will not be seriously affected by GFJ. GFJ will be in and out of your system before diazepam is even getting warmed up. Might have better luck with Xanax, half life is about 12 h.

One note of caution about GFJ. If a drug has a low bioavailability and is primarily CYP3A4-metabolized, you will get a huge dose increase. The natural oral bioavailability of hydro and oxy is very high. If it was a lot lower (like 20% or so), adding GFJ to your usual dose would probably be enough to make you OD. People die from heroin OD this way. They're used to 25% pure stuff and then they get a batch that's 90% and it's way more than they can handle. Same principle with adding GFJ.
 
Tried this again today with 1 Litre of White Grapefruit Juice and 50 mg Diazepam.

About 45 minutes ago I took the Diazepam, which I took around 45 minutes or so after the Juice..

Sorry old thread and all that, but it didn't warrant a new one, as the Benzo-Grapefruit potentiation thing has been done to death!
 
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