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Bupe Interesting fact about Bupe that I haven't heard mentioned anywhere here before.

A

Animoe

Bluelighter
Joined
Apr 13, 2012
Messages
250
Yes, Buprenorphine does indeed inhibit CYP3A4. And yes, it is indeed interesting. It also appears to inhibit CYP2d6. However, it is not a "major inhibitor". I mean whether it is more effective than Cimetidine I'm not sure. I know cimetidine is actually a mild inhibitor, which is why it should always be mixed with grapefruit juice or another more potent inhibitor. However with cimetidine you can overcome this, since it is such a safe drug you can take high doses, for days at a time to achieve the inhibition. Buprenorphine would be impractical to use as an inhibitor, of course, but the fact that it inhibits it's own metabolism is interesting information nonetheless.
 
Lorne??? said:
However, it is not a "major inhibitor".
Click to expand...


This is a direct quote from one of the links I posted.. "Buprenorphine strongly inhibited the CYP3A4- and CYP2D6" - http://www.ncbi.nlm.nih.gov/pubmed/12033517

Sorry, I should have used the word 'strongly' or 'potent' rather than 'major'. My mistake.

Also.. "Buprenorphine exhibited potent, competitive inhibition of CYP2D6 (Ki 10 ± 2 μM and 1.8 ± 0.2 μM) and CYP3A4 (Ki 40 ± 1.6 μM and 19 ± 1.2 μM)" - http://dmd.aspetjournals.org/content/31/6/768.long

And I know that wikipedia puts Buprenorphine as the same strength of inhibition of CYP3A4 as Cimetidine, and list it as "weak", but I have found wikipedia not to be the most reliable source of information.



Aslo, I did not know this was old and/or brought up before, but maybe there's some on here that have not known this so it might be useful to some.
 
Btw, I have know about the 3A4 inhibition for years, but only recently learned of 2D6


Also, Methadone inhibits 3A4, as well, so that it also inhibits it's own metabolism. However this effect is temporary, as with long term use, methadone actually begins inducing it's own metabolism! So initially, methadone has a "normal" half-life, but after a few days it increases because of tissue saturation. Several more, it gets even longer, because of enzyme inhibition. But after an extended time, the half-life returns to baseline, as auto-induction begins. Eventually the half-life is even shorter than it started! Now they're is some interesting, random information... But, I wonder if bupe is subject to a similar mechanism, as the half life is MUCH shorter with chronic use, even though it is supposed to be longer...
Anyway, nice to see someone else with similar interest to mine...
 
No disrespect man, I know Wiki is not exactly the most reliable! But I know it is not a very potent inhibitor, as I have studied it extensively. And aside, I have used potent inhibitors enough to know the difference. Then again, it makes tramadol frakkin useless, but tramadol is useless anyway, so who knows? But my main curiosity, is it like methadone, in that it is an initial inhibitor but subsequent inducer? That would make sense to me, as IV Bupe does not last NEARLY as long with chronic use. I mean that is a part of tolerance, but it is just ridiculous, how with even a couple weeks straight, it goes from lasting 12 hours or more, to sometimes just 3 or 4... But alas, I have found no info to the effect...
 
No disrespect taken, no worries. We'll just agree to disagree, or better yet leave it open for debate because I too, have done extensive research on the subject.
 
That is great too hear! Buprenorphine is an interesting drug, that is not studied enough, IMO. Really, we're almost splitting hairs, though, it could be a potent inhibitor I can't say for sure. But a "strong" inhibitor increases AUC of substrates by 5x or more. All you have to do is a shot of bupe, wait 12 hours, then take methadone+clonopin, and it is clearly not a "strong" inhibitor in the strictest sense of the word. On the other hand, drink a half gallon of good white grapefruit juice, or even take a few erythromycin/telithyr(can't remember the other one) and the level of inhibition is ridiculous! But as I've said, I suspect Bupe might induce them with chronic use, but I have absolutely no evidence to that effect!!!
 
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