Opioids Tapentadol Megathread

[4DQSAR]

OK - I have noted a few really odd things about tapentadol.

I've read claims that it's affinity for the MOR is just 1/50th that of morphine and a few sources give the affinity µM, not nM which sort of agrees with that statement.

HOWEVER I'm almost certain I've also read that tapentadol is classed as a 'superagonist' i.e. it only weakly binds to the MOR, but it's activity at the MOR is far higher than classical opioids.

This MAY explain why although not that potent (I note the BNF suggests a minimum dose of 50mg although 250mg SR formulations are available), it appears to produce notable analgesic activity but at the cost of a particularly nasty AWS.

In the UK one consultant has even written a paper specifically on the topic of tapentadol detoxification. I'm assuming that for people who get on with or even enjoy the stimulant activity, that AWS might be significantly different in character.

Forensic journals appear to suggest that somewhat like tramadol, fatal overdoses may not present in the same manner as those produced by 'classical' opioid with seizures being a particular issue. I have no idea of the scale of the problem but the UK government was sufficiently concerned to release a warning:

Tapentadol (Palexia): risk of seizures and reports of serotonin syndrome when co-administered with other medicines

Tapentadol may increase seizure risk in patients taking other medicines that lower seizure threshold, for example, antidepressants and antipsychotics. Serotonin syndrome has also been reported when tapentadol is used in combination with serotoninergic antidepressants.

www.gov.uk

I am prepared to bet that tapentadol, like tramadol, will fall out of favour with British clinicians. Maybe not an outright ban, but I can imagine clinicians deciding that in patients for whom tapentadol is will tolerated, they will continue to prescribe... but I suggest that it will become a second-line treatment in new patients. I was never offered the stuff but then again, I am subject to seizures so presume my doctor discounted tapentadol out of hand.

 

[Smyth2]

I don't understand the guide at the start of the thread saying 150mg is considered a "heavy" dose. That's not even threshold for tapentadol.

 

[Esperighanto]

I don't understand the guide at the start of the thread saying 150mg is considered a "heavy" dose. That's not even threshold for tapentadol.

Yeah, on 2-3 weeks straight of no opioid is, at 225 lbs, and missing most of my digestive tract, 500mg was where I started to feel it and I'm not sure why.

For safety's sake, this could easily kill, do not replicate it even if heavier than I was.

 

[4DQSAR]

I don't understand the guide at the start of the thread saying 150mg is considered a "heavy" dose. That's not even threshold for tapentadol.

Then why do they produce 25,50, 75 and 100mg IR formulations?

https://bnf.nice.org.uk/drugs/tapentadol/medicinal-forms/#oral-tablet

If YOU barely feel 150mg either you are in that small group of refractive patients for whom tapentadol simply doesn't work and/or you have developed a huge tolerance to the stuff. Either way - offering ill considered advice can get other killed, so DON'T!

For me, the tremendous anxiety it produced made it intractable as a potential treatment and that was just a single 25mg tablet. I think from that my clinician divined that it simply was not an option.

 

[OcCo]

about 4 years ago I got a box from a usual benzzo vendor and took 4 x 50mg may have even been 100mg tablets when they 1st appeared comparing the dosage to the amount of oxy's (bad mistake) I was taking and felt like I'd just taken a load of MDMA, Very strange and powerful drug. I remeber sliding down a door and gouching out while waking up abruptly every few seconds. I didnt enjoy it felt dirty as hell like tramadol but the 3 others in the room did asking when I'd be getting more...
Needless to say I didnt buy anymore as I didnt want people to end up dead so didnt restock anymore, partly to most addicts being on SSRI/SNRI's and thought in conjunction could cause Serotonin Syndrome or deaths.

 

[4DQSAR]

It's worth noting that in the UK, tapendadol was (in my opinion correctly) added to the list of Class A controlled drugs. Most people do not seem to like it - but enough do for their to be a stealthy on-line trade.

I keep on poining this out but tapendadol is basically just the ring-opened analogue of picenadol. In fact, it's possibly MORE hazardous.

Anyone keeping tabs on The Lancet or other journals aimed at clinicians will have noted that entirely different detoxification protocols for patient unlucky to have developed physical dependence to the drug.

I strongly suggest that the whole tramadol debacle has made the UK EXTREMELY dubious of any claims made by Grünenthal so we are one of the few nations where it isn't commonly used and doctors. The BNF devotes vastly more space to tapendadol than it does to every other opioid combined!

https://bnf.nice.org.uk/drugs/tapentadol/

 

[Mushoku_Sensei]

After going through almost 20 g of it by now thought I should also add my 2 ct... Hope it's not all boring repetition...
Roa:
snorting: hurts af, easily one of the most painful things I tried - never again
Oral: works well, but since I read about the bioavailability that was it.. I'm sticking largely to:
Rectal: that shit hurts. It's an irritant and it can cause local reactions. I've had pain and cramps that made me break in sweat and clutch the wash bassin trying not to lose it . So now I do it max twice a day, dilute it to 5 ml (no matter 100 or 200 mg) and rinse the syringe a few times so it's approximately 10 ml plus I do a real prep with oil to protect the tissue and avoid any bowel movement that could cause a loss...
Effect -wise I like it coming up but it makes my tremor worse, I'm more shaky and rushy than usual. Also when I get tired or approach nod zone I always end up hallucinating. No colorful patterns like a psychedelic, but usually things that could happen IRL, often it's just hearing voices of my family and I catch myself replying sooner or later...
WD: imo like any other opioid and it can also be replaced by any other.

 

[4DQSAR]

You know - being found dead while in the act of boofing tapetadol is not an obituary I would want to write.

Guess who is developing a tapentadol prodrug with higher oral bioavailability?

Sci-Hub : {title} [{doi}]

The thing is, acetylation of the phenol (like M-->H) would also work. I guess shelf-life wouldn't be as good but something three times more potent than tapentadol that's LEGAL almost everywhere seems like a no-brainer for the Indians knocking out generic tapentadol.

But in all seriousness - it's bad stuff. Every opioid user I knew in the 90s said 'well, OK for emergencies... but only just. Some even said they would go with nalbuphene first (not fun).

 

[Mushoku_Sensei]

You know - being found dead while in the act of booing tapetnadol it not an obituary I would want to write.

Lmao not nice fs. But I'd hardly die while boofing it - it's way more likely to happen when it's taking effect already isn't it?

Guess who is developing a tapentadol prodrug with higher oral bioavailability?

Sci-Hub : {title} [{doi}]

Oh right... Who else indeed?

The thing is, acetylation of the phenol (like M-->H) would also work. I guess shelf-life wouldn't be as good but something three times more potent than tapentadol that's LEGAL almost everywhere seems like a no-brainer for the Indians knocking out generic tapentadol.

I see... Though it would hardly stay legal then I suppose - at least never ever here, where the original is already class A (not called that here but same meaning)

But in all seriousness - it's bad stuff. Every opioid user I knew in the 90s said 'well, OK for emergencies... but only just. Some even said they would go with nalbuphene first (not fun).

I know that actually - those hallucinations are not fun, they're risky (at least for me in my family) and I definitely prefer other opioids as well - but I don't have much money to spend on drugs and Tapentadol is the most affordable stronger opioid for me... Nor would I ever throw any opi for the matter - I decided that I won't order more though.

 

[4DQSAR]

I think Grünenthal's slightly dubious path in drug development might be at least partly cultural. I don't know the proper German term but is the term 'Wirtschaftsmotor' about right? The concept that Germany is the economic dynamo of Europe and if a few rules ignored, it's the goal that really matters.

I only mention the above when I read about Peter Walaschek whose actions were morally awful, but he made use of the fact that bending the rules is (was) culturally acceptable if it increases trade. He saw a system with a loop-hole.

 

[Mushoku_Sensei]

I think Grünenthal's slightly dubious path in drug development might be at least partly cultural. I don't know the proper German term but is the term 'Wirtschaftsmotor' about right? The concept that Germany is the economic dynamo of Europe and if a few rules ignored, it's the goal that really matters.

I only mention the above when I read about Peter Walaschek whose actions were morally awful, but he made use of the fact that bending the rules is (was) culturally acceptable if it increases trade. He saw a system with a loop-hole.

Wirtschaftsmotor is something/-one that is increasing the whole economic success of the country (or a state,)
Indeed economic success is a very high ranking value here. Isn't that the same in other countries as well?

 

[4DQSAR]

Wirtschaftsmotor is something/-one that is increasing the whole economic success of the country (or a state,)
Indeed economic success is a very high ranking value here. Isn't that the same in other countries as well?

I should have been more specific but hoped the name would give you an idea of the period I was thinking of. As I said, one German citizen saw a loophole in export control laws and exported some very bad things to some very dangerous leaders.

Which is why I did sort of say is OR was, as the definition may well have changed over the 40ish years since it happened.

No insult intended, I assure you.

 

[Mushoku_Sensei]

I should have been more specific but hoped the name would give you an idea of the period I was thinking of. As I said, one German citizen saw a loophole in export control laws and exported some very bad things to some very dangerous leaders.

Which is why I did sort of say is OR was, as the definition may well have changed over the 40ish years since it happened.

No insult intended, I assure you.

At that time I couldn't read the news yet . But afaik there are and were lots of dangerous exports by many big German companies, arms and chemicals especially. I'm bad with dates and names though

 

[gmanzalready1]

used it for years with pregablin and soma.never trippy never anywhere near like morphine painkiller waste of money imo olenty6of better alternatives

 

[silver_lining]

used it for years with pregablin and soma.never trippy never anywhere near like morphine painkiller waste of money imo olenty6of better alternatives

for me it's a good pain killer and gives a boost of energy, easy on my digestive track and CHEAP. Oddly enough it clears up my allergies too. Easy to take breaks without much struggles to.i take small doses tho, 50-100 mg 2-3 times a day, always early, never past 2pm.

 

[4DQSAR]

At that time I couldn't read the news yet . But afaik there are and were lots of dangerous exports by many big German companies, arms and chemicals especially. I'm bad with dates and names though

Err... can you read the news now?

 

[PhatBoy714]

I hate Tapentadol.... Way too much of a dirty feeling and I don't like blanking out mid sentence all the time... I can literally hear voices that are not there and see things moving in my peripherals on Tap... I get a bit paranoid on it as well.... It's warm and fuzzy but uncomfortable at the same time

There's also a huge quality difference in those nasty Indian made orange tabs vs like the American pharmacy grade Nucyntas....

 

[4DQSAR]

I hate Tapentadol.... Way too much of a dirty feeling and I don't like blanking out mid sentence all the time... I can literally hear voices that are not there and see things moving in my peripherals on Tap... I get a bit paranoid on it as well.... It's warm and fuzzy but uncomfortable at the same time

There's also a huge quality difference in those nasty Indian made orange tabs vs like the American pharmacy grade Nucyntas....

Hallucinations Following Intravenous Use of Tapentadol

The authors describe 2 cases of individuals who developed tapentadol-induced hallucinations in clear consciousness following nonprescribed intravenous use.

www.psychiatrist.com

I don't know what dose or ROA you employ, but this isn't unknown.

 

[PhatBoy714]

Hallucinations Following Intravenous Use of Tapentadol

The authors describe 2 cases of individuals who developed tapentadol-induced hallucinations in clear consciousness following nonprescribed intravenous use.

www.psychiatrist.com

I don't know what dose or ROA you employ, but this isn't unknown.

I've never done anything else besides taking them orally.... It wasn't full on hallucinations... More like a dream state like it was mentioned in here... But uncomfortable.... More of a delusional feeling....

 

[4DQSAR]

I've never done anything else besides taking them orally.... It wasn't full on hallucinations... More like a dream state like it was mentioned in here... But uncomfortable.... More of a delusional feeling....

Well, YMMV.

But overall, tapentadol does not seem well tolerated at theraputic doses. A lot of people simply seeking relief from pain are having to choose between the lesser of two evils.

It's a medication I absolutely would avoid. If you are prescribed tapentadol, doctors will only know if patients tell them.