Posted 10/9/2010 12:43 PM (GMT 0)
Bomba,
First off, welcome to healing well. You will find that many members here are very knowledgable.
Secondly, I have been on Nucynta for 6 months now and am very knowledgable on its effects, efficiency, and risks. I'm going to provide you with details I found on my own via medical sites as well as the details that my doctor has told me. Please take what I say though as just my viewpoint. I'm certainly not an expert and only a doctor or pharmacist is qaulified to give you definative answers, so take this with a grain of salt :)
Ok, I'll start off by explain what nucynta is not. Its not ramped up tramadol. It's not a dervivitive form of the M1 metabolite of tramadol. It is however, modeled to act in a similiar fasion to the M1 Tramadol metabolite. Tramadol itself is very weak, but a small portion of it gets turned into M1 by the liver, which that metabolite is actually has actionable opioid activity. The issue is that only a small portion of tramadol is turned into M1, so its opioid activity is still very limited. The tramadol itself is active as both a medium-low potency Serotonin Re-uptake Inhibitor (SRI or SSRI) and a Norephrinedine Re-uptake Inhibitor (NRI). This makes it a daul action medication that essentially acts as an SNRI and a very mild opioid. In order to get the Opioid activity though, tramadol has to be broken down by the liver. Nucynta does not as it has active Opioid activity on its own and doesn't need to be process by the liver first to be opioid active, so that right there is a huge difference. Nucynta is also a medium potency NRI medication so like tramadol it has dual action. However, Nucynta is not considered a SRI/SSRI, even though it does slightly boost seratonin levels indirectly. The Opioid activity in Nucynta is also considerably stronger than that of tramadol, although weaker than most opioids, so this is a key differance too. Tapentadol is a single molecule medication so the medication is both an NRI and opioid without the body having to break it down. This is very important for people with liver issues or those that don't process Codeine into morphine well.
So to put all that in summary, Nucynta is a moderately strong NRI, so its like combining Prozac and Vicodin in 1 little pill.
Its considered to be 3 times as strong as tramadol as far as pain relief efficiency goes, and to be similiar in potency to percocet. Its moderately potent NRI abilities help to intensify its opioid effects. Its NRI effects also have pain killing properties as it helps to block pain signals before they reach the brain. It is considered to be *roughly* 1/3rd the potency of oral morphine. So 100 mgs of tapentadol is considered (atleast according to studies) to be equipotent to a 30 mg morphine tablet (some sources say its closer to 1/2th the stregnth). 100 mgs is also considered to be roughly = to 15 mgs of percocet (some sources say 10mgs). The fact that trails show the medication to be 1/3rd the potency of morphine is especially important because tapentadol has 18 times less efficiency in binding to Mu Opioid receptors (morphine receptors in the body, the same ones other opioid bind to). It is considered to "activate" the Mu receptor sites very effectively though.
To compare it to other opioids, Nucynta is stronger in its opioid effects than Darvocet and Tramadol and comparable to vicodin, though a bit weaker. Vicodin has 10 fold less binding power for opioid receptors than morphine and as I stated Nucynta has 18 fold less bind power. Its only a somewhat less potent opioid than vicodin though because it activates and "covers" the sites very well. Its NRI abilities are considered to be comparable to but slightly weaker than those of the anti depressant Effexor (keep in mind effexor has to build up for its NRI effects to take place where as tapentadol is immediately active).
Tolerance to Nucynta builds very slowly in comparison to other opioids. Its believed that its NRI effects slow down the body's response to build tolerance. Even after tolerance builds, since roughly 2/3rds of its pain relieving action is attributed to its NRI effects, it still retains pain fighting power after weeks of use.
Only about 36 percent of tapentadol gets absorbed in the GI track (when taken with food, which helps) so in that respect its similiar to morphine as only 25 percent of oral morphine gets absorbed. By comparison, about 90 percent of vicodin gets absorbed. This is why nycynta is prescribed in 50, 75, and 100 mgs tablets, its a moderately potent medication with low absorbtion.
Its considered to be less addictive than percocet, opana, and morphine. However, its considered to be a schedule II because it still has some euphoric properties and its onset of effects is fairly quick, though it does not cause a rush. It does not create the intense "cravings" that some of its stronger schedule II buddies do. Actually it was supposed to be released as a schedule III do to a limited liability. However, do to its "supposed" liking factor and the fact that no APAP is mixed with it, its a schedule II. My PM doctor thinks it should be a schedule III or IV and so do I. If you want stronger pain relief than Vicodin, but are affraid of the addictive risks associated with percocet and opana, I personally think this is a great in-between option.
It's effects last for about 5 hours. The medication literally feels like taking prozac and codeine together, but it feels more like an anti depressant than an opioid. It causes less sedation that most opioid medications thanks to its NE properties. At higher doses, it still will cause the dreaded opioid sedation though. As for side effects, at 50 - 75 mgs, the side effects are almost un-noticable. It causes a slight upping anti depressant like feeling and a desire to socialize, but it very little impairment on cognitive abilities at this dosage. At 100 mgs, the euphoric effects are more noticable but again theres no rush. Also at this dose, after about 2 hours, there is some slight noticable sedation but its very tolerable. At 150 mgs (which is my breakthrough pain dose), significant side effects are experienced and they seem to mostly be related to its NE properties. At 150 mgs, ive experienced mild halucinations and strong anxiety (I have a theory that these might be pre-seratonin syndrome symptoms). However, the NE negative side effects have always went away without serious incident. Its opioid properties are also fairly noticable at this dose side effects wise too though, with strong sedation setting in after the NE effects start to wear off. I accidentally took 150 mgs with a juice mix that had grapefruit in it (i should have checked the label). Well grapefruit intensifies the opioid effect and on that day I felt my breathing slow down. I don't say any of this to scare you guys. For the most part ive had very few side effects, ESPECIALLY when I use it at 50, 75, or 100 mgs (1 1.5 or 2 pills). I'm just stating that the side effects increase DRAMATICALLY at the 150 mg mark. When going off the medication, if you took it for 60 days or less, you probably won't have any withdraw. There is a moderate but tolerable withdraw effect when tappering off this medication after the 2 month mark, with the biggest effect being an energy crash.
As far as pain relief goes, for me 100 mgs generally brings considerable relief for moderate level pain. It bring noticable relief for moderate-severe pain, but at a level 7 pain, it takes about 90 minutes to achieve the desired relief, where as at level 5 to 6 pain, the relief is acheived in about 45 to 60 minutes. At level 8 severe pain, 100 mgs is not adequate and hardly touches the pain. However, 150 mgs works EXCELLENT to relieve even level 8 pain most of the time. A few times that I could rate my pain as level 9 or very severe, the nucynta did very little to help, and in my humble option, I feel this medication is best for those in the moderate to moderate-severe spectrum pain range (5 to 7.5) For those that consistantly have level 8-10 pain, if you can tolerate the side effects for the 200mg max dose, I could see this working.
Overall I would summarize it like this. Very effective for pain and can be used long term. Less addiction risk. Low side effects for low and moderate doses but strong side effects at higher doses. Allows you to go out and live your life due to its low sedation and relatively good potency. My doctor (and from what I've understood other docs feel this way too) feels much more comfortable prescribing this for me than other schedule IIs.
This medication in my opinion is a life saver and has given me a better qaulity of life. I pay a 20 dollar co-pay and without the co-pay, I'd be paying about 400 bucks a fill. However, PM docs have a voucher that will allow you to get your first fill for 25 bucks if your insurance wont cover it.
I really hope this helps :)