Also would like to add other peoples experiences on bupe to this thread to compile information about how everyone reacts on it and how well it works for them day to day.
Buprenorphine is a semi-synthetic opioid in the oripavine/thebaine family of opiates (They tend to be more stimulating than the opiates more similar to morphine (Hydromorphone, Codeine, heroin, etc.) in low doses >4mg a day bupe does act very similar to a full agonist, thats why its prescribed for pain in such low doses. Such as the 35ug/hr patch, up to 75ug actually and the .3, .4mg Temgesic tablets/Buprenex. Partial agonist at the mu opiate receptor, antagonist at the k, and partial to full like its metabolite at the delta receptor. For opiate mait. it comes in two different types Suboxone (Bupe and naloxone) and subutex which they have a generic for(just bupe). Remember though it is 25x stronger than morphine so it can be useful for pain especially when combined with cannabis or otc pain relievers.
This gets a bit complicated, but I’ll do my best. A couple background issues; buprenorphine has a ‘ceiling’ to its effect, meaning that beyond a certain dose, increases in dose do not cause greater opioid effect. That is the mechanism for how buprenorphine blocks cravings.
If the blood level of buprenorphine is ABOVE that ceiling, the opioid receptors are maximally, 100% stimulated. If the person takes more buprenorphine, and the blood level increases, the opioid receptors don’t feel the increase, as they cannot be stimulated more than 100%. But more importantly: when the person takes less, and the blood level of buprenorphine goes DOWN, the receptors also sense nothing– as long as the level stays above the ‘ceiling’ level.Below that ceiling level, the opioid effect from buprenorphine varies directly with dose—just as with oxycodone, hydrocodone, heroin, etc. Medications that have effects that increase with dose are called ‘agonists’. Buprenorphine is a ‘partial agonist;’ it acts like an agonist up to point, the ceiling effect, beyond which increases in blood level have no greater effect.
The ceiling effect is normally reached around 32mg give or take, even at 8mg the agonist effects seem to just flat out and start's to block itself. If you take subs to stay clean and deal with daily pain, I recommend staying in the 2-5mg range for optimal pain relief and to stay well. I notice that bupe doesn't help as much with the pain in higher doses, mostly lower ones.
Metabolites, main one is norbuprenorphine but there's a few other minor ones. It is thought that norbup plays a decent role in the effects you get from taking sub. norbups pharmacology is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, as well as a κ-opioid receptor partial agonist. The half life of this drug is anywhere from 20-60/65 hours max. Most people metabolize it within 24-35 hours, I myself have to dose more than once a day and by the next morning when I need to dose the early w/d signs kick in.
I know alot of people bitch about buprenorphine, that it wont hold them over and is just a nasty drug that will ruin your opiate receptors and liver but just presenting the facts is all I can do. Buprenorphine can be a wonderful drug, especially since the availability compared to methadone. Out of 1-10, bupe's agonist effects are a 6.9 or almost 70% agonist activity which is higher than pentazocine and people tend to like that more. Even with the 70% only being activated for alot of us, that little extra kick you get from it is just enough to get you by day to day. Shit I wish could get scripted methadone instead, if I had the option of choice which opiate I would want to be on for Mait. theres no way in hell i'd stay on bupe. I would probably switch to oral oxycodone/morphine(time release of course) or even hydrocodone. I wouldn't mind maintaining on hydro as long as its pure and maybe a 6 hour time release. Hell methadone would be on my list to since I went to the clinic for 2 years basically and it always held me over for 24hours.
I'd take any full agonist over bupe just has to be medium to high potency. For now the best option and easiest choice for me is sub. I could go back on the methadone if I wanted to, which is tempting but dealing with the whole clinic thing and going in everyday isn't convenient for me. When I get my regular license in the next week or 2 and can drive my truck I might consider going back since I could drive myself, the subs are pretty damn easy to get though and I get basically 2 months worth per visit it's just not quite the same as a full agonist though no matter what you do. There feels like somethings missing after you take it. Like you start to feel those familiar opiate effects for 10mins when you dose then it just disappears as suddenly as it came and your body isn't fully satisfied.
(sorry for going off topic, back to bupe info):
My dose range is anywhere from 1.5-6mg depending on the kinda day i'm having. As I mentioned above I have to redose atleast once during the day or I start to w/d after around 25hour mark. I have a fast metabolism though so its different for everyone.
List of Interactions:
Benzodiazapines
Opiates
Anti-histamines
Stimulants
Marijuana(couldn't call it a psychedelic)
NMDA antagonist/anaesthetics
Possibly SSRIs and anti-psychotics
Feel free to shout out more interactions if you find them, i'll keep adding to it.
Also would like to add other peoples experiences on bupe to this thread to compile information about how everyone reacts on it and how well it works for them day to day.



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