Tapentadol

[Ham-milton]

Hey, has anyone been watching the development of Tramadol's successor? It's called Tapentadol, but there isn't a whole hell of a lot of info about it.

Everyone says that it's the first new drug of it's class to come out in the last 25 years! I don't know about that- they must not be counting tramadol as an opioid, then (which it really isn't, I guess).

Has anyone seen the structure? I haven't found it yet, but I'm really interested. A still legal drug would be a really nice thing for an addict looking to pick up a huge amount to stay "sober" for a long time.

But anyway, does anyone have technical information on it- where it binds, what subreceptors, nonopioid effects, Dose, halflife, that sort of stuff.

Any help would be greatly appreciated!

 

[sarbanes]

Looks similar to M1, but without tramadol/M1's cyclohexyl moiety. Instead of aryl (tramadol), it is a phenol (like M1). Certainly would be more euphoric than ciramadol, which is actually most similar in effect to pentacozine or buprenorphine, and has a low ceiling effect (because of its u-opioid mixed agonism/antagonism).

 

[Ham-milton]

Oh, you found it's structure? Why couldn't I?

Oh, I found it here: Page 47ish

The study is pretty interesting. Looking at the structure, I definitely agree that it's going to be more abusable than ciramadol and tramadol. Especially since it doesn't have to be metabolized to have any real opioid binding.

Here's another question- does tapentadol technically qualify as an opioid? I wouldn't think so looking at the structure, but if it's binding to the mu receptor, perhaps my understanding of what's neccessary to bind is a little off.

If I didn't know that M1 binds to MOR, I would never have guessed that this would. I suppose there'll need to be new SAR studies done on these NE/Opioid drugs coming out.

Without the cyclohexyl moiety, this should be more potent, no? It's only 37% bioavailable orally, though. I bet when it comes out this'll be a good candidate for pluging.

 

[shamus]

I see it's a Norepinephrine reuptake inhibitor too!


That should make things interesting (as far as I'm aware no other opiods do that?)

 

[Broshious]

I see it's a Norepinephrine reuptake inhibitor too!


That should make things interesting (as far as I'm aware no other opiods do that?)

Tramadol is also one.

 

[Paregoric Kid]

looks interesting. it is similar to o-demethyltramadol, grünenthal has had patents on tramadol analogs for a while. in one study it seems that 200mg of tapentadol provided slightly more analgesia than 60mg of morphine and 100mg of tapentadol was slightly less effective than 60mg of morphine.

 

[fastandbulbous]

Structure wise, it almosts fits (ther benzylic carbon should really be a tertiart carbon instead of a secondary) & looks like either a derivative of dimethylthiambutene (replace one of the thienyl groups with m-hydroxyphenyl and forget the other thienyl) or methadone (lose an aryl group and the keto oxygen). The meta-hydroxyphenyl should increase mu-agonism & this should be a reasonable opioid drug.

 

[LuxEtVeritas]

is this seemingly more favorable than M1?

M1 being 200x as potent as its parent pro-drug tramadol seems to be an ultra-potent mu-opioid agonist and NDRI, though i do not know if its oral bioavailbility approaches tramadol which i think is ~66%

 

[Ham-milton]

Well if 200mg is roughly equal to 60mg of morphine, as an analgesic, this might prove to be pretty enjoyable.

I wonder if that equivalence is based on oral dosing or intravaneous- if it's the former, that's pretty decent, but if it's intravaneous, I dunno.

Tramadol may be a decent NERI, but it's not much of an opioid. A drug that's potent at both routes of analgesia could be one hell of an addictive drug.

I missed the similarity to methadone, not dimethylthiambutene. I guess the mind only sees what it wants to.

 

[GABAking]

I know this thread is really old, but any of you guys actually get to try the drug now that PM docs are startin' to hand it out more?

I was actually prescribed it for a month. Good pain killing properties (low doses, little euphoria...this is the future of pharmaceutical analgesias). At higher doses it was rather stimulating, but then I would nod off too, but then wake up and be stimulated...never had that type of feeling before. It was a unique

However, I had to get off it. The SNRI component was really messing with my vision; couldn't focus on reading for shit

 

[Epsilon Alpha]

A girl I know is on it for nerve pain following a car accident and she's got no complaints. Slightly brighter mood, suppressed appetite, and no neck or shoulder pain is all she said it did.
Worth noting that she hated tramadol with a passion though, too many sides and tolerance was an issue. Gabapentin just made her feel dumb as a rock, and she failed her chem midterm right after starting it.

 

[Limpet_Chicken]

Tramadol seems to be one of those marmite-opioids. You either love it, or hate it, with not much in between.

Can't stand the stuff myself. Shitty opioid, and the noradrenergic reuptake inhibitor properties make me feel altogether shitty, and it makes me overload, autie-wise. The serotonergic effects make it have way too many contraindications for comfort too IMHO.

 

[adder]

I totally agree. I couldn't stand it myself either. It was nothing like classic opioids when I first tried it. Actually, it didn't do much. No real opioid action, just little lightheadedness and that dirty feeling S(N)RIs have when you dose once and too much. Years later when I was prescribed it for TAPERING OFF levorphanol and morphine, I felt nothing after taking 1.6g. Well, I'd probably wake up in a hospital if I didn't take clonazepam.

Such drugs are as great analgesics as (S)(N)(D)RIs are great antidepressants, i.e. neither really help in conditions they're indicated for. I'm not in a physical pain but BPD kills me, yet I prefer to stay away from these "fantastic" antidepressants, mood stabilizers, and novel anxiolytics. A bunch of drugs messing up with your neurotransmitters/hormones and you start to feel real pain when you have to get off them.

Just like I haven't seen any breakthrough in pain management (there are a few opioids, e.g. levorphanol, that aren't used for reasons unknown and they may be better in some cases because of wider spectrum of action), I haven't seen any breakthrough in helping people suffering from mental illnesses and disorders (same happens here, there are quite a few substances shown to be far superior to (S)(N)(D)RIs and no more trials are run... e.g. ketamine helped me better for depressive episodes than any used antidepressants, smoking marihuana always helps me fight all these thoughts I'm tired of, buprenorphine always lightened me up with no dirty feeling - none of these caused manic episode, I'm not saying these drugs should be used but it's just to show that there are already classes of drugs known to scientists and they don't seem to be researched). Psychiatry "crawls on all four" compared to most fields of medicine. Sad but true.

 

[Limpet_Chicken]

I'd love to be on levorphanol, tried to get my doc to rx it, due to the NMDA antagonist properties would make it better for my neuropathic pain, then I could knock the pregabalin on the head. They don't use levorphanol here though :/

NMDA antagonists have a wonderful afterglow, I can see how they are excellent antidepressants. I feel perfectly set up to go and do whatever I want in life after a hit of MXE for days afterwards. Full of energy etc.

 

[TW58]

Hello everyone-I'm taking dilantin, tramadol and hydrocodone. How do they affect one anothers metabolism?

 

[PoppyLlama]

I was on this medication for a couple months due to post-herpetic neuralgia. It work ed okay for pain killing properties. I used to take 200 mgs of tapentadol and 10 mgs of cyclobenzaprine and I'd be pretty faded for the night. However, I gained tolerance fast. after a couple weeks I needed 400 mgs to get high, and that was too much.

Here the thread regarding my experiences with tapentadol

Nucynta (Tapentadol) HALLUCINATIONS

It was a crazy experience, I was hallucinating like crazy, I've also read about other people who hallucinated, or would mistake objects for other things that they werent, examples: specks of dirt were spiders or bugs, shadows in an empty car looked like there was people in it, there were other things too but I haven't read about this subject in a while as I haven't taken the tapentadol for at least 3 years now. It's definitely a SUPER strange drug though.

 

[bpayne]

for what it's worth.. my 2 cents... I loved tramadol from the very first time I took it, and it wasn't for the opioid effects mostly, It was the first time I actually felt motivated to get off my ass and do something and have an organized mind about it, I was able to start projects and finish them for once. .whereas I usually just start a hundred things and finish none of them.. I actually had a feeling of Tranquility or contentment about me.. it provided no real high whatsoever like oxycodone or hydrocodone does, but that was my whole point of taking it, I liked the speedy effects much more than the sedated opiate aspect... However after using it for over a year, I developed severe withdrawals when I tried to stop and ended up needing to take Other "harder" opiates when I couldn't get any.. which propelled me into tolerance land.. I ended up taking buprenorphine just for tramadol withdrawals.. then withdrew for a whole month and a half off the bupe.. and It still was easier than the tramadol withdrawals that I would experience.. all in all I took it for 3 years progressing to much harder opiates during each period when I could not obtain tramadol.. strangely enough the newfound opiate tolerance did not effect my tolerance for tramadol.. it still kept me functioning quite well, those three years I was probably more productive than I have ever been in my adult life..... Sadly I realized that Tramadol is a dangerous drug and tapered myself down off of all pills and onto Kratom.. which I take now at about 100 grams a week.... I have resumed being the disorganized, unproductive, dolt that I guess I was born to be... sigh... and still get sick If I run out of kratom, That is my tramadol Tale..
B

 

[ebola?]

Here the thread regarding my experiences with tapentadol

Nucynta (Tapentadol) HALLUCINATIONS

Thanks. Let's continue to make this thread about tapentadol, not tramadol.

ebola