Opioids Narcotics -- Benzhydrocodone

[Nicomorphinist]

This is a prodrug of hydrocodone which was developed especially to get an abuse-deterrent narcotic analgesic by modifying hydrocodone at the molecular level by making is essentially inactive until it begins to be taken apart by enzymes in the stomach and small intestine. Does anyone have any experience with this?

Other companies like Endo are apparently working on oxymorphol and derivatives for some of the same reasons.

My opinion is that hydrocodone it not broken, so do not try to fix it.

What would work better for the stated objective would be, for example, morphine esters and similar drugs rather than putting effort into developing fentanils-based pharmaceuticals for purposes which require medication stronger than morphine, and use the codeine, dihydrocodeine. and hydrocodone analogues of them for moderate to severe pain. For example, in the United States, acetylmorphone and nicomorphine, nicocodeine, thebacon and similar drugs can fill those niches, and they have already been in the literature for at least 100 years in most cases. I believe the prize for most potent opioid is once again in the semi-synthetic category, viz 14-methoxymetopon, and there are many others. Heterocodeine would be an interesting possible pharmaceutical as well, six to nine times stronger than morphine.

There are also drugs like acetylpropionylmorphine and dibenzoylmorphine which are inexpensive to manufacture, and in the same range and with identical effects to smack which can be used for 14 days or fewer or in patient controlled analgesia pumps and do not have the political baggage of smack . . . there are certainly enough reasons dealing with the pharmacology of morphine, dihydromorphine, hydromorphinol, ketones like hydromorphone and esters like smack and dibenzoylmorphine to warrant their use alongside each other in both human and veterinary medicine. Speed of onset, solubility, receptor activation profile and so on and so forth.

 

[sekio]

this is the benzoate analog of thebacon

esterases are usually pretty damn fast so I would expect this would just be another moderate strength opioid

 

[Shortec Stublue!!]

Is Thebacon any relation to Thebaine? Isn’t the objective to narrow roa’s, so only worthwhile getting it to the liver orally?

 

[Nicomorphinist]

Thebacon is named after thebaine and can be derived from it as it is acetylated hydrocodone . . . it has been quite some time since I have seen this anti-tussive and analgesic on the market but back in the day it was marketed in Continental Europe and some other places. In fact, it was long enough ago that I would take the thebacon with glutethimide . . . in all cases, thebacon was a little stronger than hydrocodone and lasted longer.

 

[Shortec Stublue!!]

Was Bayer the only manufacturer?

 

[Nicomorphinist]

I believe that Merck made thebacon at some time in the past; perhaps Mundipharma and/or Hoechst too . . . I believe that Merck was manufacturing five to eight metric tons of its close relative acetylmorphone a year in the late 1920s before the League of Nations outlawed acerylmorphone as one of the three or so first designer drugs in 1930 which people were using as a heroin replacement -- the come-up and rush of smack and the bang and lingering euphoria of hydromorphone with a longer duration of action . . .

 

[Shortec Stublue!!]

I may be thinking of Heroin and Bayer, Oxy is derived from Thebaine though yes?

 

[Nicomorphinist]

Oxycodone and other 14-dihydromorphinones are made most economically from thebaine and/or tetrahydrothebaine, and there are high-yield synthesis routes from the latter to the dihydrocodeine/dihydromorphine series of opioids. Prior to the 1900 publication of the dihydromorphine synthesis from tetrahydrothebaine, thebaine was more or less considered useless.