I'm not an expert on Nucynta (tapentadol) but I have been on it (with the exception of trying to downgrade to Vicodin) for over a year now and am very experienced with its effects, side effects, usefulness, tolerance, ect, so i'll try to answer some of your concerns. Again, only personal experience and person research speaking here :)
Nucynta was intended to be a schedule III (reports indicate some advocates thought it should be a IV) AFTER phase 3 trails involving hundreds of patients, and when the application was pushed up to the FDA and DEA, they came back after their own tests and stated it had the abuse scoring of hydromorphone, therefore it must be a schedule II (despite the results of the trails that demonstrated a lower addiction potential). Also, it has no tylenol so that gave it another strike (with APAP in it, I think it might have inched by with a schedule III rating....maybe, sighs).
Also Nucynta was intended to improve on the design of tramadol as it is made by the same manufacturer. Nucynta is very similiar in structure to the small amount of an m1 metabolite that tramadol breaks down to in the system (in the same manner codeine breaks down into a small amount of morphine). Basically, tramadol has almost no opioid activity on its own, but an hour later when the m1 metabolite is present, it is potent enough to produce mild opioid related anglesia. Also note that with tramadol, the majority of its pain killer effects come from Seratonin and Norephedrine reuptake inhibition (SNRI) so essentially we have a drug with quick anti depressant action and mild opiod action to combat the pain in 3 different ways. This is especially helpful for nueropathic pain, not to mention there is some evidence to link depression and nuero pain together, so kind of a 2 birds with 1 stone pill, in my opinion. Tramadol also has slower tolerance building. (Note: Both Nucynta and Tramadol are centrally acting anaglesics but both are also narcotics).
However, tramadol can interact negatively with other medications that raise seratonin levels and cause seratonin syndrome. Also, many patients found that while it was more effective for pain than codeine, it was less effective than stronger medications like hydrocdone and oxycodone. Also, it still requires that same emzyme set as codeine to break it down into the m1 metabolite so some people with a deficiency in that emzyme do not get as much pain relief. So with this the manufacturer went back to the drawing board.
What they came out with (Nucynta) basically took the m1 metabolite idea and improved upon it (this is my opinion that the result was improved). The first difference with tramadol is that nucynta is a single molecule entity. It is orally active with ALL of its effects without having to be broken down into metabolites, so its full anaglesia action is quicker and can be utilized by people with the codeine emzyme deficiency. Secondly, its opioid action was considerably stronger than the m1 metabolite opioid action of tramadol. Although the narcotic action is still weaker than that of oxycodone and morphine so there is some reduced liability in its addiction potential. Thirdly, nucynta has stronger norephedrine reuptake inhibition than tramadol but very little seratonin reuptake activity. By changing nucynta to an NRI, they reduced the risk of seratonin syndrome. However, the medication STILL has some SRI action and can still produce seratonin syndrome, but the reduction in total risk from tramadol and lessened seratonin side effects made nucynta more tolerable for some people.
So what you have a single molecule entity with two pathways MOR +NRI ( morphine/Mu opioid receptor ascending pathway and norephedrine reuptake inhibition decending pathway). The strong NRI effects also have some opioid sparing effects on anglesia. The strong NRI effects also deter abuse because NRI overdose causes high levels of anxiety and mild distortions in percpetion (After my rhizotomy, I was still in pain and was told to take a second 75mg nucynta. It caused mild closed eye visuals, sweating, and anxiety so even though my pain was down to zero, the side effects were undesirable.)
IMO nucynta is difficult to abuse....atleast at higher doses. I do believe people can becoming addicted to lower doses and abuse it for its mood elevating properties, but IMO that would make it a candidate for schedule III or even IV, certainly not a II. IMO this medication is overscheduled and is less addictive than oxycodone and morphine and more comparable to the addiction risk of the milder opioids. Its also builds tolerance at HALF the rate that morphine and related drugs do. This is due to its NRI sparing effects.
However the FDA/DEA (in their infinite wisdom) don't pay attention to the fact that its weaker in opioid stregnth compared to oxycodone, they rather recognize that its stronger than tramadol. They also don't recognize that it has a built in deterant against abuse (the max instant release dose is 100mgs but my doc gave permission for 150 (2 -75s)after the procedure. This medication is VERY unpleasant beyond the 100mg dose!!). #3, it did comparably well as a pain reliever when pared up against oxycodone, so the DEA rather than realize "ohhh, it has two mechs of action" simply thinks oxycodone #2, OVERCLASSIFY! The FDA also fails to realize this medication has a demonstrated SLOWER tolerance building than the morphine related drugs. That alone should put it in schedule III.
Me and my pain management doctor have had legnthy conversations about
this drug, its acceptance, its REAL abuse potential, its differentiation with other opioids, ect. She very much agrees that this medication has a lower risk of addiction, less overall side effects at normal dosing, and good relief specifically with neuro patients. My doc has told me the same dose seems to work for a long period of time as it has with me, again demonstrating the lower tolerance building properties.
I'm really sorry this was so long, but there's no way to make this short OP. The problem is that because the DEA has put the schedule II curse on this medication (despite trails, despite statements from PM doctors on the lower risk of abuse), to doctors that don't know, its basically oxycodone part II. Thats exactly how its going to be stimatized too until the FDA/DEA drop it to a schedule III.
OP, do be careful with nucynta though. It CAN be addictive and have had it stolen from me before (basically a friend living with me at that time basically got into them while I was at work). It IS a narcotic.....but to view it in the same light as oxycodone would be wrong. Its a less addictive safer alternative for nuero pain. I hope this has helped you. Again, I'm no expert so my advice would be speaking to a pharmacist about
any questions you have. Take care and good luck. -James
MRI revealed disc bulge and test injections revealed RA. Radio Freq procedures helped for months, but pain is up and im having the procedure done again. Currently on 75 mgs of Nucynta (tapentadol - A MOR + NRI) 2 to 3 time per day and Soma 350 as needed.
Post Edited (grainofsalt) : 10/7/2011 1:51:24 AM (GMT-6)