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.