RCs Novel opioid Despropionylbezitramide

[roi]

Metabolite of Bezitramide.

CAS# 83898-28-6

DrugBank on the parent compound:

Bezitramide acts in the body to relieve pain with a potency 20 times that of methadone. Its duration of action is relatively long, lasting up to 12 hours post oral administration, after the achievement of steady state. Its onset of action is slow, with a peak in analgesic effect noted between 2.5-3.5 hours after dosing. It is noted to illicit a strong antitussive effect, which could be of benefit to patients with bronchial carcinoma.

Not sure how potent this metabolite will be. Anyone have some more information?

 

[Hodor]

I dunno, you'd expect that Propionyl group to be good for... something? Maybe that's what's responsible for the slow-ass onset? Maybe they could have gone for Acetyl-Bezitramide instead?

 

[roi]

Well, if benzimidazoles are similar to indoles, it shouldn't really matter if it's there or not.

 

[Gordon's]

These long lasting opiates sound dangerous, methadone alone causes alot of overdose's / people getting sick due to the long ass onset and duration. Hopefully its not as potent as its parent compound.

 

[bingey]

does strong anti-tussive effect correlate with strong respiratory depression?

 

[mysafehome01]

does strong anti-tussive effect correlate with strong respiratory depression?

Yes, I believe so. For lack of the technical statement they kind of go 'hand in hand'

 

[XANAX XR]

Oh, this is awesome... of course with caution, dosing under 5mg would be ideal... probably looking at .5mg for a really good high and 1mg for a very strong high.

U4 requires way too much redosing..... way way too much.

 

[keeping]

hmm

 

[Neithman]

This is dangerous as hell if ots really 20 times stronger than methadone plus a long onset

 

[XANAX XR]

If dosed properly, it could be a really nice drug.

 

[SKL]

If dosed properly, it could be a really nice drug.

this, basically
this drug sounds quite appealing to me
but from an HR perspecitve the danger is the long onset
tempting people to redose
and don't get me wrong this is scary af in the mainstream population
but if that temptation is ignored it is something I could see being really enjoyable
even methadone is kind of underrated in this regard IME
(basically only because of the way it's dosed in MMT not because of it's intrinsic qualities)
I would give it a go if still inclined to opiate

 

[XANAX XR]

Methadone is my favorite for duration, body/warm fuzzy feeling relaxation high, mind-set and euphoria. It beats all opiates for me, with a tolerance 5mg makes me feel like I'm in heaven, however, I have to take 10mg in order to make it worth while.

So if this was 20x more potent, 1mg might be OD worthy... hopefully someone makes this in uG liquid. This would be right up my ally either way.,

 

[AlsoTapered]

The dose-response curve of bezitramide is not linear and the value x20 is PER 24 hours.

For the treatment of acute, post-operative pain, it was compared to the much shorter-acting dextromoramide:

Dextromoramide Bezitramide
10 9
15 11
20 12.5
30 15
35 16
40 17
45 18
50 18.5
60 20
70 21.5

Now dextromoramide is no longer used because of it's unreliable pharmacokinetics but was generally considered to be some 3.5x morphine in potency. Both bezitramide and despropanoyl-bezitramide are supposed to have a similar action ALTHOUGH it should be noted that on oral administration, the peak-plasma level of bezitramide is supposed to be reached at 2.5-3.5 hours and to have a relatively show onset.

I suggest that despropanoyl-bezitramide has a significantly faster onset making it very hazardous. It's an interesting compound containing as it does 3 aromatic rings (identified as key moieties in mu receptor ligands) as well as a positively ionizable function (the basic amide) and an amide moiety akin to fentanyl.

It's also interesting that brorphine shares some of bezitramides structure as does methadone. Like dextromoramide itself, it represents an extremely small class of opioid.