Tapentadol (Nucynta) placed in CII -- a sad...

[resorcinol]

...loss for hope of a little progressivism with scheduling for new psychoactive drugs.

The drug is probably somewhere between hydrocodone and O-desmethyltramadol in potency as a mu agonist, so I guess if the DEA follows their own precedent this scheduling makes sense. However, it's such BS for those of us hoping for more lenient scheduling. It seems like the fuckheads at the DEA make anything with no dose ceiling that is an opioid or stimulant CII, period, despite the wide disparity in fun potential among CII drugs!

PURE codeine and oxymorphone are in the same schedule (CII). Whoops, I was even mistaken above, an opioid prodrug DID find its way into CII (codeine by itself, no APAP or other add on drug in the formulation). That's just ridiculous.

I was expecting CIII and hoping for CIV. When I saw that it got CII, I was floored. So much for patients just entering CP treatment having a drug option that has not yet been stigmatized to all hell by the media --- simply having CII attached to it is enough to spook doctors.

It will be undergoing review / appeal (lets hope for a change to CIII for the pure drug), but I'm not holding my breath.

I hope they AT LEAST make it so it can be CIII or CIV when mixed with APAP, ibuprofen, aspirin, etc.

The brand name will be Nucynta in the united states for tapentadol hydrochloride IR tablets (50 mg, 75 mg, or 100 mg).

On a positive note, the fact that it got hammered with a CII just like Vyvanse did means it showed CLEAR fun potential in the trials.

Source: http://www.deadiversion.usdoj.gov/fe...009/fr0217.htm

[resorcinol]

More info: I'm looking at a study that found that tapendadol and hydromorphone were rated equally in scores of "liking" the feeling of the drug at equianalgesic doses. Folks, this is STRANGE. Tapentadol only has one aromatic ring (and only one ring period) and it APPEARS not to have a dose ceiling for mu agonism. It's weak, but if this study is correct, it's euphoric.

This isn't like tramadol if these studies / the DEA scheduling are on target.

[Paregoric Kid]

given the info I've read on its strength and its potential stimulant properties (from its ability to act as a norepinephrine reuptake inhibitor) its no surprise. I thought it was closer to morphine and oxycodone in strength. one study said it was equivalent to morphine and oxycodone but with less side effects. sounds like it will be good stuff. I've really been wanting to try this stuff forever, I wish people would have synthesized it when reports first came out about it, because back then it wouldn't have fallen under the analog act and it would've been completely legal. perhaps there will be some kind of exception if its a low dose form mixed with tylenol.

[jacky]

more good info that I am not familiar with.
....
I agree that we should hope for IV scheduling when mixed with aspirin. if that comes with a bit of muscle relaxant mixed in there, I would be ok with that as well.

[Synack]

so it's out and can be Rx'd?

[roxi*stardust]

Originally Posted by Synack

so it's out and can be Rx'd?

It was just approved, I wouldn't expect to see it on pharmacy shelves for a bit.

[Synack]

when it appears, I'll have it rx'd so I can try it out then I'll let you know.

[pokergooch]

It was supposed to hit the shelves in March, but they had some delays. I wonder how expensive this is going to be. Im betting it will be around the same cost of opana or even oxycontin. I have read that they are making ER versions as well.

this should be interesting. Ill be a guinea pig as well. Well, maybe ill wait til I hear some reports. I dont know if I want to give up my oc and opana scripts. well, maybe I could for one month......

[Synack]

I'm going to get a few days worth of IR doses... change my IR rx to 25 days of my normal IR med, and 5 days of tapentadol.

[marhatch]

I just called doc and should be getting some tonight- I dont really want to but my greedy insurance company just totally cut me off from the duragesic patches I have been using for the past 5 years. I am ready to snap- they are making insane amountws of money and just cut their list of RX's they will pay for by about 2/3's

[digby]

I ran into the local pharmaceutical rep from Johnson and Johnson when I was sitting in the lobby waiting to see my pain doc. We got to talking briefly and when I asked what he was peddling for pain these days, he said they had this brand new pain reliever - nothing like it in over 10 years. He said he wasn't allowed to share specifics but gave me the name and told me to discuss it with my pain doctor.

Of course I got sidetracked during my oppointment and forgot to bring it up, but proceeded to do some research on the net. Can't describe my disappointment to find out it was simply tapentadol, which I was familiar with, just not the brand name which is Nucynta. Every review I have managed to glean from a very small incidence of people that have actually tried the drug have rated it poorly. Most of the reviews rated it only equal to or below the performance of tramadol, which I guess shouldn't be a surprise as they are both in the same class and developed by the same guy. Everyone has been hugely disappointed with the drug and even more disappointed at its ridiculous scheduling as sched II. Either these people that reviewed the performance are all wet or this drug is going nowhere.

[kellyblue]

Yeah... I did the same thing yesterday when I heard about it on another "disease/pain" board that I frequent. Of course, I came HERE first... then spent a couple hours researching it. Everyone (well, almost everyone) said it sucks for pain and at least 90% of them complained of horrible headaches. Don't think this one's for me, but it's worth watching.

[resorcinol]

I don't doubt that tapentadol (Nucynta) is more euphoric in a mu-agonist fashion than tramadol is, but I have a really really hard time believing that it's CII worthy euphoric. It seems that the DEA just wants to put ANY mu agonist that shows any substantial recreational potential (even if only to those with a low or nonexistant tolerance) in CII. Opioids are so fucking blacklisted as evil. If I had to GUESS, it's better than tramadol and codeine by quite a bit, perhaps equal to hydrocodone in desirability but weaker mg for mg and with more non-opioid feelings due to the monoamine reuptake inhibitor stimulant properties, and not as desirable as the established strong opioid painkillers like oxycodone, hydromorphone, morphine, oxymorphone, and heroin.

This seems to me to call for CIII scheduling at the strictest, but really, CIV would be more appropriate and a move away from the draconian nature of drug scheduling and the DEA policies in general (sadly, it'll take a miracle for that to happen). God forbid an APAP free, NSAID free, antihistamine free, anticholinergic free opioid preparation -- an opioid only prep like Nucynta -- was available in CIII or CIV -- which would mean REFILLS and would be GREAT for patients in milder chronic pain who would do GREAT on Nucynta (but don't do well on tramadol because it's TOO weak ... tramadol is really for just mild pain). It'd be a great upgrade from T-4 or Hydrocodone/APAP to a pure opioid drug without the inconvenience of the no refills on CII drugs crap.

The same shit happened with Shire's Vyvanse (lisdexamfetamine). They were angling for a CIII decision bigtime, but didn't get it because "a higher dose gave the same euphoria as a lower dose of dextroamphetamine" ... it got CII. Well, true, but what about it lasting so long (not an upside for recreational use since the crash will be so much worse ... deterrent number one), and about it needing oral use so protease enzymes can act on it to convert it to free l-lysine and d-amphetamine (needing oral use immediately ruins its desirability to speed users who need to snort or IV for satisfaction) ... these are other factors besides purely oral abuse liability that should be factored in but aren't. A CIII for Vyvanse would have been fine and a GREAT help to adult ADHD patients and parents of kids with ADHD as the ability to have refills written and to call the meds in would make life easier in an already too hectic world. The DEA is as usual the sucky draconian DEA, though.

When some of those water soluble cannabinoids are eventually approved for chronic pain and maybe even post-op pain as standalone drugs or opioid sparing add on drugs, watch them get the CII hammer too. A water soluble drug that produces effects practically indistinguishable from weed, OMFG!... the DEA will think "That means more ROA possibilities that weren't there with THC -- plugging, snorting, dissolving in water and chugging, and.... *gulps*, IM, SC, and ... dun dun dun ... IV USE!". I'm thinking of WIN 55 212,2 here. It sounds absolutely ideal for pharma cannabinoid therapy. It's got more consistent and higher oral bioavailability than dronabinol (THC) or nabilone, because it can be made into a salt like WIN 55 212,2 sulfate it is absorbed far more rapidly from the GI tract making it a better choice for breakthrough pain than dronabinol by far. Again because it can be administered as the salt, inhalers, buccal pellets, and nasal sprays are all new routes opened up easily since it would dissolve in simple distilled deionized water or saline. IV use would not require alcohol (burns) like dronabinol would. I could easily see a pharma company trying to get it into clinical trials or a CB1 agonist that is an analog of it into clinical trials sometime soon to market as the first "fast acting" and "reliable" cannabinoid painkiller. I'm ALL for that, BUT .... it'll get the CII hammer of death, due to the potential for IV use of a drug causing a very weed-like high ... very uncharted territory for the DEA, and they'll be spooked. It's also a FULL agonist at CB1 where dronabinol (THC) is only a partial agonist, which I have no doubt the DEA would use to claim that WIN 55 212,2 and its salts have the "potential to cause more psychological and physical addiction than dronabinol and older, cannabis derived cannabinoid analgesic drugs, and a potential for overdose that is potentially higher" or something like that -- and use that unsubstantiated crap as an excuse for CII classification. It's insanity.

Speaking of all of this .... why is pure codeine still CII? This boggles my mind the most second only to weed still being CI (and GHB being CI). Why is codeine mixed with other ingredients that falls under CV legally able to be sold OTC to folks with a nasty non-productive cough but not a pharmacist in the country (well, maybe a few RARE ones, especially if they're older and more old school in their practice) will do it no matter what? I know it does happen (the family run place I go to stocks it and I know some older people are sold it from time to time since NY allows this practice for CV codeine preps and the pharm I go to is OK with it when it's obviously a good option for somebody who can't afford to see doctors all the time for the Rx's needed for Tussionex or the like). Every other country in the world pretty much sells codeine with either APAP or Ibuprofen ON THE SHELF next to the other pain meds. Nurofen plus is the most famous. Tylenol #1 is another. Codeine can cause a MILD opioid dependence if abused, but MILD has to be stressed here -- it would be a cinch to kick compared to strong mu agonists.

Darvocet shouldn't even still be in the formulary of this country. It's only as effective as aspirin yet causes significant cardiotoxicity and respiratory depression. It hits the wrong mu-opioid receptor subtype for the analgesic (and euphoric) effects. It's a waste of everyone's time. If you won't Rx codeine or better yet Vicodin or Percocet, please make it tramadol and leave the Darvocet to collect dust where it belongs ... it's shit, it's worthless. Better yet, grow a pair and Rx T4 for mild to moderate pain from injuries and mild chronic pain, and Rx Vicodine for moderate injury pain or mild to moderate CP that doesn't respond well enough to codeine. Stop adding SNRIs, Lyrica, etc to compensate for underprescribing what you docs know will really work with less side effects. The only add on I can think of that I agree with at the moment is Soma (carisoprodol), which is a GABA(A) agonist carbamate class CNS acting muscle relaxer that is genuinely opioid dose-sparing for a lot of different pain, but especially pain involving skeletal muscle problems. Of course, it's got a nice little stigma now too despite being unscheduled due to its known powerful boost in the opioid euphoria when taken above the recommended dose. Antihistamines are actually another addition that I approve of in some cases as some of them have genuine opioid dose sparing effects (cyclizine is possibly the most potent in this effect, with meclizine and hydroxyzine showing this effect to a weaker degree also). Again though, we run into the issue that these antihistamines that show dose sparing effects on opioids also seem to show powerful potentiation of the euphoria of the opioid when injected IV along with the opioid. Diconal (dipipanone (opioid) + cyclizine (CNS active antihistamine) ) was by many hailed as better than heroin for the rush and high ... thanks to the cyclizine. Dipipanone alone seemed to rate inferior to heroin. Antihistamines have a "rush" of their own when booted that isn't particularly "euphoric", but seems to BECOME euphoric when added on to an opioid rush occuring at the same time ... leading to a feeling that the opioid rush is much more powerful.

I believe the above is why cyclizine isn't available either OTC or by Rx in the U.S. to treat hayfever and other allergic symptoms. The FDA probably feels that it would be shot up with heroin, oxycodone, morphine, hydromorphone, etc ... to boost the rush and high and that it would increase the addictiveness of the opioids. Note that this rush and high boosting when done by IV along with the dope effect does apply to other antihistamines, especially diphenhydramine, but the effect is not as pronounced as with cyclizine (which seems quite unique in the potency with which it can do this intensification of an opioid rush and high). Still, adding 25 mg of diph to your shot of dope CAUTIOUSLY (remember, antihistamines are downs and cause respiratory depression), might just be worth a try from what I hear floating through the grapevine. Just please, please use wheel filters if you shoot drugs that come from a pill!!!

Wow, sorry for the long ass post. I got on a roll there!

[DCBA]

maybe combined with paracetamol or aspirin will be CIV or something...
It hasnt been aproved for use in portugal for now.

[Paregoric Kid]

yeah I assume its actually more like hydrocodone or oxycodone in terms of strength. I think a lot of people are put off when they hear its an analog of tramadol. once they know that they may have some preconceived notions as to its strength. that it is an analog of tramadol isn't a bad thing. morphine is an analog of codeine, methadone is an analog of propoxyphene, hydromorphone is an analog of hydrocodone, yet hydromorphone, methadone, and morphine are all much, much more potent than those analogs and I suspect the same is true with tapentadol. would like to hear more people review it, especially from people who didn't know its relation to tramadol or who haven't tried tramadol. it would also be interesting to hear reviews from people who are either on or have used and didn't have negative opinions about tramadol.