snorting viberzi (eluxadline)?

[AddictedSince11]

soo i have some viberzi and i was wondering if insuffolating it would make it work better in the brain instead of the gut so hopefully its just a normal opioid and i dont accidentally meet god since its a mild kappa agonist

 

[4DQSAR]

From a few Google searches I note that eluxadline does not readily pass the blood-brain barrier. In addition, in vitro studies suggest it to be an MPR2 substrate and possibly other active transports.

It's also very close to the RO5 (HBAs and HBDs) and I would be interested to know what the LogP is.

That said, I note several sorces state that it's MOR affinty is 1.8 nM so low and slow. After all, empirical evidence is the best kind of evidence.

FYI many years ago Fastandbulbous noted that a French (?) manufacturer had introduced racecadotril and their research had also yielded RB-101. I think that's a clever idea. They aren't opioids per se, they simply prevent the human body from metabolizing endorphins.

 

[AddictedSince11]

From a few Google searches I note that eluxadline does not readily pass the blood-brain barrier. In addition, in vitro studies suggest it to be an MPR2 substrate and possibly other active transports.

It's also very close to the RO5 (HBAs and HBDs) and I would be interested to know what the LogP is.

That said, I note several sorces state that it's MOR affinty is 1.8 nM so low and slow. After all, empirical evidence is the best kind of evidence.

FYI many years ago Fastandbulbous noted that a French (?) manufacturer had introduced racecadotril and their research had also yielded RB-101. I think that's a clever idea. They aren't opioids per se, they simply prevent the human body from metabolizing endorphins.

i know chatgpt isnt the best of sources but it says its a 0.90.0 on lipophilicity

 

[Keif' Richards]

Hey @AddictedSince11 and for everyone who is not familiar with this stuff, Eluxalodine (Viberzi) is an Opioid-based medication used to treat symptoms under the umbrella of Irritable Bowel Syndrome. It is not the first drug to be designed with the same basic strategy: Opioid agonists lead to slower intestinal motility as a Hallmark almost as ubiquitous as sedation, itchiness or pinpoint pupils. Many of us here are already familiar with Loperamide (Immodium, arguably the most well-known and well-used medication of this kind.

You may also be familiar with a medication known as Diphenoxylate (Lomotil). The same question has been raised about Dipheoxylate as has been raised about Loperamide. There is no black and white answer here. We are a harm reduction resource, so we are always going to try to give you the most scientifically-minded advice we can. However, for questions like this, I ask people to use their common sense and sense of logic/reason to try to answer these questions for themselves.

In short, the answer is no; no this medication is not going to substitute for an Opioid. It seems in clinical trials, dosages 10x the recommended dosage were registered as "pleasurable" and/or produced feelings of being "high" though these were stated to be mild. Furthermore, these tests were not being done on a cohort of people who like using Opioids recreationally and had a history of doing so.

That is really the best answer you're going to get. You have seen that dosages 10x what is recommended produce results that are "meh" for individuals not like you or I. Trying to use this drug in this fashion is not likely to do anything other than let you down or irritate you. In the case of a drug like Loperamide, we know that larger-than-recommended doses are in fact quite harmful in many cases.

It's possible that insufflation would make the drug more potent, but the logic of the rest of my post still stands. It's just not designed for this purpose and trying to use it as a traditional Opioid agonist is not likely to lead to the results you're seeking.

 

[4DQSAR]

i know chatgpt isnt the best of sources but it says its a 0.90.0 on lipophilicity

I wouldn't have though of using AI. I mean fine if it goes on to provide references, but people like Elsevier are pretty draconian about enforcing their copyright so IF an AI gives a precice bit of data only found in ONE paper, they can employ lawfare.

But 0.9 looks about right to me. Sure, a fair few hydrophobic rings but a primary amide, primary amine and a bare carboxylic acid along with those HBDs.

As noted, I honestly think that if a drug simply increases the endorphin levels, firstly it produces analgesia with none of the usual risks (respiratory collapse and so on), it could be that it's also a potential way to stop AWS. Pure speculation on my part and to be clear, as always, I'm NOT selling anything. But if loperamide is a dangerous detox, I sense racecadotril MAY be safer. But again, speculation.

After all, who knows what types of toxicity higher (absorbed) doses of this stuff might be? Two chiral centres, so I ask why. Sure, it won't be active, but if it just does nothing, it's cheaper to just leave it in there...