^ I agree with that Trunkofmycar, that Drs. overload people with bupe to block opiates basically, and they think their cravings will be less if a shitload of your receptors are occupied by bupe... that can may make sense at some point...
Also my 2 cents:
I've been in bupe mantaintment for like 6 years, and I think it's "basicaly like all drugs" with some *exceptions*. I explain:
If you keep your toleance
low of
any drug, when you feel your system is runing out of that drug, every time you redose you will feel better/stronger reward/effect than if your tolerance is skyrocketed by previous doses. Simply as that, right?
You will enjoy cocaine more, if you keep your tolerance down. You will enjoy LSD more if you keep your tolerance down, etc. Or am I wrong?
BUT also I agree that buprenorphine is "special" because of its partial agonism of mu opioid receptors, also its very high
affinity, that brings us to the famous ceiling effect, and also that high binding affinity makes it very powerful by mass (weight), even if it is not a full agonist, it will activate a lot mu receptors to some point (0.4 over 1 or something like that if I'm not wrong) bc of its
high affinity to the receptors....-chemistry, huh? 8(-
Norbupre is a full agonist, but it seems to poorly cross the BBB bc of its high affinity to that goddamn (lifesaver sometimes) protein G as you guys said... BUT it still might make its way to a mu receptor in the brain and activate it despite that, as Loperamide does, that last one maybe in even very smaller amounts...BUT it still will be overpowered by buprenorphine, but we need to remember that at the same time buprenorphine concentration levels decreases bc of
metabolism into norbupe, norbupe concentration
increases, so it gives it more chance to occupy a mu receptor, because there is
less buprenorphine to compete with during
time, even if it crosses the BBB in very small amounts, norbupe has also a very high affinity, so not much of it would be needed even if it's pump out of the brain...right?
All in all it's still a mystery to me how bupe *really* works. I just know that if I keep my tolerance low, I will enjoy more my bupes and if I double my dose I definitely feel something more...but not always pleasant bc of the nausea and low blood pressure, basically.
Hope all that makes sense...
And remember, keeping your tolerance down is
always better