Tapentadol (Palexia Retard) - Retrospective - Underrated Opioid

[Fertile]

I think it's time I take issue with data sources. Many say it has only 1/50 or 1/18 or some other small fraction of the affinity for the mu receptors than morphine does.But the Royal College of Anaesthetists gives 10mg oral morphine per 24 hours equalling 25mg of oral tapentadol. But that is in terms of analgesia, not mu affinity.

As I have mentioned before, tapentadol's closest relative is picenadol. But tapentadol is a partial agonist which picenadol is a mixture of 2 isomers - one an agonist, the other an antagonist. Tahexadol (see what I did with tapentadol there?) is likely to be more potent but from what I know if this scaffold, reaching M potency is hard enough. You cannot swap that N-methyl (or N,N-dimethyl) for anything else.

 

[themediumlebowski]

i've seen people mention a ceiling dose but no information on what that dose actually is.

Anyone got a link or any info?

Also re: redosing, would taking tramadol after the tapentadol wears off be a waste or do they target slightly different receptors?

 

[themediumlebowski]

The advice very much is to not mix benzos and opioids. Pregabalin along with tapentadol will also increase side effects and it won’t be a nice feeling. It goes without saying it’s also dangerous.

Oddly enough i have been prescribed those at the same time
along with an ssri, endep and serc.

i try not to take all each day as that cocktail seems a bit much, especially when one psych suggested upping the ssri from 50 to 200mg without any incrementall steps
then he suggested suboxone instead of the tap, though i am hesitant to make that switch

 

[themediumlebowski]

Super unusual. First few hours are a very much so an upper, and then it takes a 180 and you start to nod 3+ hrs after dosing.
Alot of noise & visual hallucinations, like being in a dream but you respond to the dream while sitting in a room by yourself. First time it happened it scared the shit out of me. Now i'm quite a fan. I also dose it with valium & soma in small doses, while the opioid i keep at around 200-300mg per session.

I don't know if it is common to get the "upper" effect, but honestly i just pop another valium and it calms down. I'm much more interestd in the NOD not the busy mind bullshit

i am guessing that is with the ER version as opposed to the IR?

nods 3 hours after dosing is something i have not experienced, usually i have to fight the urge to redose around that point.
3 hours is also roughly the time i sleep for if that particular dose knocks me out funnily enough

 

[themediumlebowski]

Yeah I've never mixed that combo before.

Do you know any painkillers effective for nocioplastic pain? From what I understand it's a relatively poorly understood field - a bit like phantom limb syndrome. After 25 years I finally saw a consultant who suggested that might be what I have

Mobic?
works on different receptors to celebrex afaik

 

[themediumlebowski]

You need to get that dose down, whilst I said the seizure risk is lower there is still a risk. Tapentadol max dose is 500mg. I would really caution you with taking those big doses.

Take a tolerance break or taper down to a lower dose.

i thought it was 600mg though i could be wrong

i was prescribed 550 (2x200ER + 3x50IR)

 

[SpiralusSancti]

Well things like that should be but aren’t really exact science. You might be big, didn’t respond to lower dose, guidelines in your place might be different or you just got a plain stupid doctor.

Oddly enough i have been prescribed those at the same time
along with an ssri, endep and serc.

Nothing odd about it. Many times exceptions are made when prescribing medicine for x reasons.

But here’s a “folks wisdom” advice. Do not take all the meds at the same time. It’s not an advice you’ll usually get from your doctor cuz of reasons again but often you can minimise risks of combining certain medicine by spacing it properly.

 

[AlsoTapered]

Well, the closest drug to tapentadol is picenadol. It's a shame because tapentadol is a mixed agonist/antagonist. So CLOSE to being good. I strongly suggest that tahexadol (full agonist) will turn up as an RC.

Even though it's suppose to have quite low affinity to the mu receptor, dependence IS known in the UK... and it's almost never used in the UK.

I guess if you like buprenorphine and tramadol, it's possibly 'your thing'. In all cases, they seem to lower seizure threshold. So just be wary of that.

 

[Buditas]

Tapentadol is no better for me for analgesia (pain relief) than any other opioids I've tried - my pain doctor is now suggesting Capsaicin (!) - that's the same stuff as in chilli peppers. Apparently you can get Capasaicin patches for nocioplastic pain relief.

However, recreationally I do get something from Tapentadol - moreso than from the (admittedley limited) other opioids I've tried - Codeine, DHC, Tramdol and Kratom. None of which have done anything for me. I only tried Tramadol once as I was too wary to take too much due to seizure risk.

Anyway my experience with Tapentadol:

Been using Tapentadol for a while now. Started off with a 100mg and gradually increased the dose over time by using it daily so of course my tolerance started to increase and now I'm taking somewhere in the region of 800mg-1000mg at a time to feel the same effects. Also sometimes combine it with Soma (Carisoprodol). Not willing to risk combining it with Benzos

When it works, Tapentadol is strange but I quite like it - it gives a sort of buzzy-type high. Sometimes when I stare at something like the carpet or the wall I could swear it looks like it's shifting and moving. However the duration doesn't usually last for long. And sometimes it doesn't have any effect at all which is a bit frustrating. Also - a bit like with Benzos - I've found that it's made me do some strange shit that I have no memory of doing- like discovering that I've moved objects and put them in weird places during the night - so that's slightly alarming and something to be careful of. Another side effect is it makes it difficult to urinate - After a Tapentadol session I find I'm standing over the toilet willing my bladder to empty as it trickles out....

I'm abstaining for a while to bring my tolerance down though. I obviously didn't learn from my Pregabalin expereince - with Preg I really enjoyed the buzz so I started using it daily and saw a rapid tolerance rise which eventually saw me taking very high doses to feel the same effect. Discipline! Discipline! Discipline!

That's so cool!