Talk:Oxymorphone

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[edit] dependence liability

if its 6-8x as potent as morphine that means its 3-4x as potent as heroin. on wiki's heroin & morphine pages it says "extremely high" for dependence liability yet for oxymorphone which is 3-4x and 6-8x as potent, and yet it says only "high" dependence liability. heroin is legal in most european countries for medical use, and i dont understand how more potent opioids can be said to be less addictive, fentanyl, oxymorphone and hydromorphone are all legal for prescriptions and are all at least 2x if not MUCH more potent than heroin. are the dependence liability ratings on the wikipedia pages from the FDA or what source?

even in the illict use section of this Oxymorphone wiki page it says: "Until its removal from the United States market in the early 1970s, oxymorphone in the form of Numorphan 10 mg instant-release tablets was one of the most sought-after and well-regarded opioids of the IV drug using community. Known popularly as "blues" for their light blue color, the tablets contained very few insoluble binders — making them easy to inject — and were extremely potent when used intravenously. "Blues" were also considered to be especially euphoric; comparable to or better than heroin"

dependence liability should be extremely high for both or for at least oxymorphone if heroin & morphine are going to have that.

• Not quite - the current version is time-release only, making it virtually impossible to convert to an injectable for drug users. The low efficiency of orally administered opiods (hence, higher cost), further decreased through time-release, makes this drug much less euphoric and desirable for addicts. If anything, the time-release formula makes it more suited for substitution treatment. —Preceding unsigned comment added by 128.195.186.78 (talk) 11:21, 27 September 2007 (UTC)

Not Quite- You are so very wrong about thisItalic text. This drug is high, extremely addictive. The time release is being by passed by high school kids. (I will not say how I don't want to teach someone that may not kwow.) I have a 18 year old daughter that will be enjoying her 19th birthday in rehabilation due to the highly additive nature of this drug when used outside of doctors supervision. So don't beleive that this time release is component makes this drug anyless addictive. Don't fool yourself.--Fatherwithrehabdaughter (talk) 02:25, 10 May 2008 (UTC)Link title

[edit] Image

note:the image of oxymorphone is a not right, the single bonded o's hould be OH's, as in dihydroxy. (comment moved from page by Dirk Beetstra ^{T C} 08:53, 13 November 2006 (UTC)).

[edit] Origin of propenyl and cinnamyl ester info

Where did this chemistry info about propenyl and cinnamyl esters come from? I've studied opioids extensively and have never heard of this. I would be hard pressed to find research to back it up. I would think if those groups were known to be potent, there would be research. Furthermore, acetic acid can form an ester with the hydroxy groups, but since cinnamyl and propenyl groups are not carboxylic acids, they cannot form an ester bond. If one were to condense cinnamyl and propenyl alcohols with the 6 and 14 hydroxys, you would have a propenyl ether and cinnamyl ether.-Junky getting a PhD—Preceding unsigned comment added by 144.92.229.97 (talk • contribs)

I'm not sure who added the info about the SAR but it's accurate. I have a couple of journal articles about the development and testing of the compounds mentioned in the article and would post them as citations if I could find them but they are currently unavailable due to computer trouble. I will post them as soon as I can find them, unless someone beats me to it. Also, it would be nice to know what's being measured when the article says such and such a derivative is "(x) times more potent than" the parent compound (or morphine? the article's not clear about that either), how exactly it's more potent. As an analgesic? In the rat tail-flick test? The formalin test? In vitro K_i values for opioid receptors? MOR, KOR, DOR, ORL-1? Et cetera.

As for the 14- derivatives of oxymorphone, I'm pretty sure they are ethers and not esters. Again, I would have to check the referenced (though not cited) articles in order to be certain. Another modification that increases potency that isn't mentioned is the substitution of a phenethyl group for the N-methyl group. As far as I know, no one has synthesized and tested N-phenethyl-3-acetyl-14-cinnamoyloxymorphone yet, so its effects are idle speculation at this point. Porkchopmcmoose 02:40, 31 December 2006 (UTC)

I have also run across the cinnamic acid esters at the 14 position of oxycodone, but not oxymorphone. I'm afraid my citation was from an online module of a US university degree paper & it's no longer on-line. A Citation would be appreciated.

Found the reference...