Clinical Studies of Abuse-Resistant OxyContin begin..

[PhreeX]

http://www.oxycontin.com/pressroom/news/oxycontinNews/purdue_pharma_begins_clinical.htm

"Purdue Pharma L.P. has begun clinical studies of a new pharmaceutical product combining the opioid analgesic oxycodone in a controlled-release formulation with an opioid antagonist, naloxone."
We have our work cut out for us...

 

[zorn]

This is better than I thought. These guys should only prevent injection... you can still snort 'em or eat them crushed, but if you shoot, nothing, and you might even start withdrawing if you're badly addicted. The new formulation they just patented, using naltrexone instead, will fuck you as soon as you crush the tablet. Both these will be somewhat hard to break, since nalox/trexone are chemically similar to oxycodone.
I've been told that naloxone and oxycodone have greatly differing solubilities in chloroform, which would allow for a quick extraction. Not sure of the validity of this though.

 

[quale]

No, the ones with naltrexone shouldn't work if you snort them. If naltrexone is absorbed orally you can better bet it is absorbed nassally.
For the nalaxone ones...I was wondering if the following would work. Mix it with a the right (and I can't figure this our) amount of glucuronic acid (availible overthecounter). As this is the priomary means nalaxone is metabolized, and oxycodone have a meth oxy group is one of the slower metabolized opiates by this compound, one should be able to nuetralize it before shooting.
Man, when this shit comes up I bet alot of stupid people are going to be very unhappy when their ass is blasted into withdrawal.
[ 16 December 2001: Message edited by: quale ]

 

[zorn]

This is what I said -- the FIRST one to come out, which is in trials now, uses naloxone, so you can snort it but can't shoot it. The next one, which has only been patented, would use naltrexone, which would prevent you from doing anything but eating it whole.
A chemistry friend of mine looked into the chloroform thing, said the solubities are similar. Bummer.
That's interesting thought about glucuronidation... we need a chemist to look into this.

 

[PhreeX]

Well, I have a supply of naloxone - I keep it on hand for "just in case" .. so, who has ideas about what I should be doing with this? The way I look at it is like this - the new OxyContin's (which still wont be out for a few years) will really be useless to the current OC junkies - so prices should drop, and once they are billed as "abuse restitant" more and more doctors will be willing to prescribe them... this means that if someone has a way to isolate the oxycodone, there should be a huge supply available and it sohuld be fairly cheap too ... ya catching my drift? An 80mg OxyContin could sell for $10, and in the right hands, it could be 80mg of pure oxy ..
So, I have a fair amount of naloxone - lets hear some ideas on what to do with it...

 

[zorn]

Oh, cool. Here's what you do, Phreex:
[EDIT: I fucked up earlier, fixed]
1) See if you can get some glucuronic acid... quale says this is OTC, but I dunno where you can find it... maybe a health food store. You could probably order it from a chem supplier somewhere, if that is an option.
2) Make sure you feel comforable injecting your acid! If it comes in pill form, you'll probably want to extract it. Not sure how much you need, if anyone can really get it, then it's worth figuring out... I am guessing you can make a cc's worth that has enough acid yet is safe to inject.
3) Mix 5-10mg naloxone with a crushed-up regular oxy pill. Voila! you have an "abuse-resistant" oxy pill.
4) Dissolve the oxy/naloxone in the acid, cold-water filter, and bang. If this works, you should feel nothing, and cheap oxy is just on the horizon. If it doesn't work, well you won't get high, and if you're opiod-dependent, hello withdrawal.
----
Alternatively, if you have access to some chem lab reagents, well, then, that naloxone isn't too far from say oxymorphone, assuming you've got some chemistry down. Alas, I've been told the reagents aren't available OTC.
[ 17 December 2001: Message edited by: zorn ]

 

[Deus121]

I think PhreeX was trying to start a discussion about how to isolate the naloxone from the oxycodone. Not how to use it to flush the opoid receptors.

 

[PhreeX]

Correct, I have the naloxone and I am trying to figure out what it's soulable in but Oxy isn't, or vice-versa.. basically I want to see how we can seperate the oxy from the naloxone ..
I checked one of my many health-nut catalogs.. I can get 100 of the 250mg glucuronic acid caps for $49.79 ..not sure what form it comes in (ie liquid gels or powder - it only said "caps") ..
So, where do we go from here?

 

[Grand Master of Somniferon]

Would adding antagonists to oxycontin make them a CIII, and therefore easier to perscribe, since they have less abuse potential? That would really be a blessing to the folks that need them. I realize that oxy/apap is still a CII, but apap doesn't have antagonist properties.

 

[RJW]

No, it will still stay in CII even if it is reformulated. The primary active drug is still oxycodone and that is a CII.

 

[tathra]

its my understanding that the Scheduling of a drug has to do with its potential for abuse and its medical value. if these new oxy's are abuse resistant, then the scheduling should go down. oxycodone would still be Schedule 2, but the new specific type of oxycontin should change because of its decreased abuse potential.

 

[Grand Master of Somniferon]

Originally posted by RJW:
No, it will still stay in CII even if it is reformulated. The primary active drug is still oxycodone and that is a CII.
Yes, but as the other person said, CII's are CII because they have a high potential for abuse. An opiate with a antagonist added greatly lowers the potential for abuse, at least in the eyes of the gvmt, so in theory, oxy+an antagonist would have a lower potential for abuse, but still have an accepted medical use. Phreex, what is your opinion on this?

 

[PhreeX]

Wellm lets not forget that Hydrocodone (by itself) IS a C-II drug .. but if you throw in some APAP/Aspirn/Ibuprofen it becomes a C-III compund.. but Oxycodone, regardless of whats in it is a C-II drug.. in my professional opinion, no matter WHAT they do to it, it will be a C-II drug/compound .. because hey, even if you don't try to break the 'abuse resistant' mechanisim, if you orally take an OC-40, that will FUX0R you up good (to a non-opioid tollerant person) ...
So no, the "new OC" will still be C-II ..

 

[AbraMontague]

I imagine that DEA pressure was at least partially responsible for the development of these abuse resistant forms of OxyContin but I'm still confused about something. Are state governments still trying to sue Purdue or get the drug banned anyway?
I was just watching a tape of the "House Appropriations Subcommittee" on the Use of OxyContin (taped from 12/11/01) on CSPAN2. From what I gathered, its basically a lot of representatives and esteemed people attacking the Purdue VP of Research and Development. The New York Rep (Jose Serrano) said that if things don't change in the magnitude of current abuse then the drug will likely be banned in the future.
It is fairly informative, although totally one-sided (One Purdue Rep vs. a Panel of Representatives). I actually learned that during one quarter of this year, the sharpest increase in the prescribing of OxyContin was in Myrtle Beach, SC. The quarterly revenue was $1,000,000, the highest in the nation, just in Myrtle Beach. I guess that explains why OC's are so plentiful and cheap around here, at least for now...
Seriously though, how many people die from abusing Oxy? Weren't most of them asking for it when they snorted a 160 and didn't even know what it was or ate a couple and drank a 6 pack? And even then, I don't think a few dead (and ignorant) addicts carries that much weight against the legitimate use of the drug. The American Cancer Society Rep. made a good point that Oxy is just one opiate and it doesn't make sense to demonize it because another opiate analgesic will just take its place in the future (hell, a lot of them already exist, they would probably just be prescribed more in its place).

 

[RJW]

Originally posted by AbraMontague:
Seriously though, how many people die from abusing Oxy? Weren't most of them asking for it when they snorted a 160 and didn't even know what it was or ate a couple and drank a 6 pack? And even then, I don't think a few dead (and ignorant) addicts carries that much weight against the legitimate use of the drug. The American Cancer Society Rep. made a good point that Oxy is just one opiate and it doesn't make sense to demonize it because another opiate analgesic will just take its place in the future (hell, a lot of them already exist, they would probably just be prescribed more in its place).
The thing is the strength of the drug in ONE pill. Before OC arrived when did you ever hear of anyone dieing from ingesting ONE or even two PHARMECUETICAL pills? Never. So, a lot of people assume that they will get f&#$%ed up but nothing worse will happen since it is a legitimate drug. Think of how many post here AFTER they take something and wanting to know what it was. No other medicine has as much of a powerfull drug in one pill. Stupid people die. More than likely a few will be young teens "with there whole lives ahead of them blah, blah, blah", the parents get interviewed "how can this happen? who is responsible for this drug?" (surely their own children aren't responsible!). The media blows it WAY out of proprtion "the OC epidemic!" Congress gets involed "OC is the Devil's work!" It lands in the DEA's lap as the next target for the drug police.

 

[Deus121]

There are many pharmacutical pills out there stronger than oxycontin, and more deadly. Oxycontin was just very highly prescribed, so recreational use is soaring. This is a result of stupid users use. All the good drugs are lost by stupid users abusing them and dying, or getting addicted. Its a real shame.

 

[AbraMontague]

"Before OC arrived when did you ever hear of anyone dieing from ingesting ONE or even two PHARMECUETICAL pills? Never."
Ever heard of MSContin 200mg? One or two of those is helluva lot for someone without a tolerance. And while not a pill, a teaspoon or two of Roxinal or Roxicodone Intensol could put a few people out cold (dead cold).
Actually, Deus makes a good point. When there is so much of something on the streets, more people will take it, some of which aren't very intelligent and end up dead. OC was a top 200 prescription drug last year, probably the strongest opiate to be prescribed in such quantity.
But Purdue still has a valid argument. Any MD with a DEA license # can prescribe any controlled substance in almost any quantity for any condition they see fit, all at their own discretion.

 

[RJW]

Ever heard of MSContin 200mg? One or two of those is helluva lot for someone without a tolerance. And while not a pill, a teaspoon or two of Roxinal or Roxicodone Intensol could put a few people out cold (dead cold).[/QB]
Ok, I was in error with that statement. But, you can see my point. Before the vast numbers of scripts were written for OC the general public was never exposed to very powerful pain meds. I do have a question...why is OC so widely used for chronic pain patients and MSContin not? Seems they would both fit the same purpose. I realize a lot of the OC scripts are the reult of aggressive marketing by Purdue but it's not like chronic pain is a new thing.

 

[PhreeX]

RJW is totally correct.. it was the fault of over-marketing by Purdue back in the mid/late 1990's .. they sold the pill to doctors as "safe" and a means of delievering a constant dose of narcotics to patients without the risk of addiction - and it's ture, when used properly, less then 1% of users will get hooked.. so doctors that didn't have a background in pain medicine were writing scripts left and right..
Don't worry, OC isn't going anywhere .. the only reason for the abuse-resistant form is for good PR ..