Bupe Norbuprenorphine

[polarthedog]

Ok, so I know that norbuprenorphine is a full agonist unlike buprenorphine. So if you had pure norbuprenorphine, would it not have the ceiling effect?

Is that a legal pharmaceutical? If not, that seems odd.

 

[JTemperance]

Ok, so I know that norbuprenorphine is a full agonist unlike buprenorphine. So if you had pure norbuprenorphine, would it not have the ceiling effect?

Is that a legal pharmaceutical? If not, that seems odd.

I thought the new consensus opinion was that norbuprenorphine doesn't cross the blood-brain barrier, so isn't responsible for any of the psychoactive effects?

 

[polarthedog]

I thought the new consensus opinion was that norbuprenorphine doesn't cross the blood-brain barrier, so isn't responsible for any of the psychoactive effects?

Do you have links? I haven’t heard that, why wouldn’t it cross?

 

[JTemperance]

Do you have links? I haven’t heard that, why wouldn’t it cross?

I don't have great links at hand since I mainly got that impression from reading Bluelight over the years. So you could find most of the same material by searching through BL threads/posts on norbuprenorphine and seeing what's been posted on the subject over the past decade or so.

I only had time to do a quick search right now, but from that, it seems to be still somewhat of an open question, with norbupe having been found to cause respiratory depression but not to contribute to pain relief, either because of its low lipophilicity or because it is a high-affinity Pgp substrate.

Here's one study to look at on the Pgp aspect, and here's another which says:

Approximately one-third of buprenorphine is metabolized predominantly by cytochrome P450 3A4 in the liver, yielding the active metabolite norbuprenorphine – about 40 times less potent [1]. It is known from animal studies that norbuprenorphine possesses an analgesic effect and has high affinity for δ-receptors [36, 37]. Nevertheless, the contribution of norbuprenorphine to the central clinical effect of buprenorphine is questionable as norbuprenorphine is less lipophilic and thereby does not readily cross the blood–brain barrier, at least after acute administration [38, 39]. On the other hand, a study in sheep demonstrated that norbuprenorphine might contribute to the central effect of buprenorphine. In that study, significant respiratory depression was demonstrated after administration of norbuprenorphine [40]. In the present study, norbuprenorphine was measurable in the plasma after 24hr and stayed stable over the treatment period. Nevertheless, the measured plasma concentration of norbuprenorphine was three times lower than the measured plasma concentration of buprenorphine. Both drugs were detectable over the period of time where blood samples were collected. The contribution of norbuprenorphine to the analgesic effect after transdermal administration of buprenorphine could not be distinguished in the present study and might not be of importance in the present study.

 

[axe battler]

Oh wow I hadn't heard this either. Funny cos I really felt like the 2mg limit to bupe seemed correct from my experience.

 

[Feretile]

It doesn't cross the BBB.

 

[axe battler]

So why isn't the dose curve the same with bupe as it is with say morphine?
With a low tolerance bupe feels great, but once my tolerance would require me to use more than around 2mg it would no longer be euphoric? Is this like a reverse placebo? Is it bupe's long half life causing this?

 

[Feretile]

Because bupe is a partial agonist. It has a ceiling also happen to fine bupe Awful. H is OK, Oxy is OK but only dextromoramide, levorphanol and nketobemidone are truly euphoric.

But I see people take rubbish like pregabalin for fun.... low standards.

 

[polarthedog]

Because bupe is a partial agonist. It has a ceiling also happen to fine bupe Awful. H is OK, Oxy is OK but only dextromoramide, levorphanol and nketobemidone are truly euphoric.

But I see people take rubbish like pregabalin for fun.... low standards.

Where the hell do you get those? And when I have no tolerance, bupe feels AMAZING, maybe your just a hard head when it comes to opiates

 

[JTemperance]

Because bupe is a partial agonist. It has a ceiling also happen to fine bupe Awful. H is OK, Oxy is OK but only dextromoramide, levorphanol and nketobemidone are truly euphoric.

But I see people take rubbish like pregabalin for fun.... low standards.

I, too, much prefer strong opiates like heroin, oxy & methadone (+Palfium/Ketogan almost surely, if I could try), followed by strong stimulants like meth, prolintane & MDPV. Pregabalin is pretty far down my personal list.

But here, I recall the old adage "something is better than nothing." It's less reliable than alcohol, but at its best, the pregabalin/baclofen combo has given me a more intense enjoyment than I ever got from alcohol. It certainly makes you feel "different," which is something, and it also helps to pass the time...

 

[Juicewrldfan]

I thought the new consensus opinion was that norbuprenorphine doesn't cross the blood-brain barrier, so isn't responsible for any of the psychoactive effects?

A Narrative Pharmacological Review of Buprenorphine: A Unique Opioid for the Treatment of Chronic Pain - Pain and Therapy

Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid receptor agonists. The structure of buprenorphine allows for multimechanistic interactions with opioid receptors μ, δ, κ, and...

link.springer.com

Doesn’t cross like you said. Recent study 2020. So less is more is bs

 

[DeathIndustrial88]

A Narrative Pharmacological Review of Buprenorphine: A Unique Opioid for the Treatment of Chronic Pain - Pain and Therapy

Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid receptor agonists. The structure of buprenorphine allows for multimechanistic interactions with opioid receptors μ, δ, κ, and...

link.springer.com

Doesn’t cross like you said. Recent study 2020. So less is more is bs

I think people mistake the less is more as norbupe, but in reality, it's because your blood levels of bupe drop significantly more in between low doses, which means you'll feel it when you dose again.


My confusion comes from the fact that some sites say that bupe produces no respiratory depression at all & that only norbupe does. But if norbupe doesn't get into the CNS, how does it cause respiratory depression? And clearly respiratory depression from bupe, while rare, does happen. So it's very confusing.