Opioids How to make tapentadol ER instant release?

[UK Warrior]

Hello everyone, I was given a blister strip of 100MG Tapentadol extended release tablets, and wanted to know if there was a way to bypass this and make them instant release?

I have taken 4 of them today and do have a nice high from them, but would like to be able to take just a couple at a time to get a nice buzz going.

If I chew the tablet until it is all broken up will this bypass the extended release mechanism? Also, if it can be done the psychonaut wiki says anything over 150MG is a Strong+ dose, so I would only need one or two tablets maximum and get a better high versus the extended release.

Thanks everyone.

 

[4DQSAR]

I don't know the format or excipients found in tapentadol extended release tablets. But it's been my experience that every time a new 'abuse resistant' formulation arrives, someone finds a way to defeat it within a few weeks.

I would be extremely careful with tapentadol. It's almost never prescribed in the UK and while I'm sure part of the reason is that it's new and that it's a class A contolled drug. But also case-studies in The Lancet uncovered the fact that it's dependence liability poses unique challanges.

It turns out that while tapentadol doesn't have that much affiity for the opiate receptors, it's a SUPERagonist which partly explains that liability,

So be aware. In the 90s every friend in the US considered it to be their DLR to prevent AWS but none reckoned the high was much good.

So proceed with caution. No high is worth your life.

 

[UK Warrior]

I don't know the format or excipients found in tapentadol extended release tablets. But it's been my experience that every time a new 'abuse resistant' formulation arrives, someone finds a way to defeat it within a few weeks.

I would be extremely careful with tapentadol. It's almost never prescribed in the UK and while I'm sure part of the reason is that it's new and that it's a class A contolled drug. But also case-studies in The Lancet uncovered the fact that it's dependence liability poses unique challanges.

It turns out that while tapentadol doesn't have that much affiity for the opiate receptors, it's a SUPERagonist which partly explains that liability,

So be aware. In the 90s every friend in the US considered it to be their DLR to prevent AWS but none reckoned the high was much good.

So proceed with caution. No high is worth your life.

It is in the UK that the person got prescribed them, they owed me a bottle of oramorph which I usually drink in 1 so 200MG of oral morphine, but unfortunately they didn't get it with their prescription so offered me the tapentadol instead.

I realise it is a class A controlled drug unlike weaker opiods/opiates like Dihydrocodeine etc. It is in the same category as morphine and diamorphine.

So it doesn't work that well with the receptors, but where it is such a strong agonist that explains its effects?

I do apologise but what does DLR and AWS mean?

I will be careful and understand no high is worth my life, thank you for your concern.

Does anyone know if I chew them up that it will bypass the slow release? They are actual tablets, not something filled with beads that slow release.

 

[UK Warrior]

Well, I chewed one up just after I posted, and I think it does bypass it by simply crushing it in your mouth, I can walk around and function fine but sitting at the computer I am nodding HARD.

Must say this is very enjoyable, I may even prefer it to my usual dose of 200MG of oral morphine. This makes me nod properly, whereas the morphine might give a slight nod but nothing this heavy.

 

[4DQSAR]

DLR = Drug of Last Resort
AWS = Acute Withdrawal Syndrome

As I mentioned, tapentadol has turned up in The Lancet a few times. Specifically how difficult it was to treat patients who developed physical dependence to the medication.

The affinity data for tapentadol is only about 1/50th that of morphine and for a while nobody could work out how it worked. Then further research shoed it to be a SUPERagonist i.e. if physical dependence occurs, methadone and buprenorphine may not prevent AWS.

 

[UK Warrior]

DLR = Drug of Last Resort
AWS = Acute Withdrawal Syndrome

As I mentioned, tapentadol has turned up in The Lancet a few times. Specifically how difficult it was to treat patients who developed physical dependence to the medication.

The affinity data for tapentadol is only about 1/50th that of morphine and for a while nobody could work out how it worked. Then further research shoed it to be a SUPERagonist i.e. if physical dependence occurs, methadone and buprenorphine may not prevent AWS.

I see, I am glad I only have one blister strip of 7 them- I took my last two around about an hour ago.

I would not want to get a physical dependence to anything, especially something that might not even be treatable with Buprenorphine or methadone. Where the Buprenorphine may not even work does this mean it sticks to the opiate receptors better than bupe?

 

[4DQSAR]

Where the Buprenorphine may not even work does this mean it sticks to the opiate receptors better than bupe?

No, it acts as a SUPERagonist i.e. it activates the receptor more than endorphins do. So while it's possible methadone and buprenorphine might reduce the AWS, as I mentioned previously, The Lancet published case studies and rather than substitution, the amount of tapentadol was reduced using a technique called 'see-sawing' where, over a 24 hour period, one of the two doses was reduced until AWS subsided, then the other... and repeat.

That the BNF expends more words on the topic of tapentadol dependence than it does to dependence in every other opiate combined should also be a clue.

Put simply, it's dependence-forming capacity isn't well understood. But Grünenthal told doctors tramadol was safer than codeine and we all know how that ended so when they got a GSL for tapentadol, the ADMD, wisely in my opinion, declined to trust them a second time - hence it being a Class A controlled drug.

Also be aware that tapentadol lowers a person's seizure threshold, especially if that person is taking an SSRI or SDRI. I mean more than other opioids (all of which reduce seizure threshold a bit).

I'm not trying to scare you, merely making certain you are as well informed as possible - then you can make an informed choice and whatever that is, BL will always support you.

 

[UK Warrior]

No, it acts as a SUPERagonist i.e. it activates the receptor more than endorphins do. So while it's possible methadone and buprenorphine might reduce the AWS, as I mentioned previously, The Lancet published case studies and rather than substitution, the amount of tapentadol was reduced using a technique called 'see-sawing' where, over a 24 hour period, one of the two doses was reduced until AWS subsided, then the other... and repeat.

That the BNF expends more words on the topic of tapentadol dependence than it does to dependene in every other opiate combined should also be a clue.

Put simply, it's dependence-forming capacity isn't well understood. But Grünenthal told doctors tramadol was safer than codeine and we all know how that ended so when they got a GSL for tapentadol, the ADMD, wisely in my opinion, declined to trust them a second time - hence it being a Class A controlled drug.

Also be aware that tapentadol lowers a person's seizure threshold, especially if that person is taking an SSRI or SDRI. I mean more than other opioids (all of which reduce seizure threshold a bit).

I'm not trying to scare you, merely making certain you are as well informed as possible - then you can make an informed choice and whatever that is, BL will always support you.

Right I see, it actually activates them more than endorphins do, so technically it activates them more than heroin and other opiates? Is this why I am finding I get more of a nod and also feel a lot higher than with say 200MG of morphine?

I realise it is a class A controlled drug here, so gathered it was stronger than the other things such as dihydrocodeine are class B, and I know they give a good feeling in high enough doses.

Thanks for letting me know about the reduced seizure threshold, I did do some reading whilst I was taking the tapentadol and came across that.

My friend has given me their last 3 tablets, so I took 300MG of the ER 100MG tablets, I chewed them as this seems to bypass the slow release, not until they was a paste but very small chunks.

I know you are not trying to scare me, thank you for making me as up to date with things as possible when it comes to tapentadol, and it is nice to know BL is always here.

 

[4DQSAR]

Well, as we say on BL, YMMV (your milage may vary) i.e. subjective effects are unique to each person. But there just isn't that much data on tapentadol so I had to piece together what I said from one source in each case. I'm never totally happy unless I have two or three. It also increses norepinephrine levels which is supposed to increase analgesia but I'm prepared to bet is to make higher doses dysphoric.

BTW oral morphine is sort of infamous for it's low oral bioavailability (20%) so I guess tapentadol would seem potent. I 100% do not suggest anyone use pins but other parentheral routes will increase bioavailability a LOT.

 

[surely_a_few_wont_hurt]

BTW oral morphine is sort of infamous for it's low oral bioavailability (20%) so I guess tapentadol would seem potent. I 100% do not suggest anyone use pins but other parentheral routes will increase bioavailability a LOT.

Similar to morphine, tapentadol has relatively low oral bioavailability (around 32–42%) due to significant first-pass metabolism.

Unlike (what are referred to as 'prodrug opioids' such as codeine), it does not require metabolic activation to produce its analgesic effect. The parent drug itself is pharmacologically active, while its metabolites are largely inactive.

Although a substantial portion of the dose is metabolised before reaching systemic circulation, the remaining fraction is sufficient to exert its effects via µ-opioid receptor agonism and noradrenaline ('norepinepherine' for US resders) reuptake inhibition. Because it does not rely on metabolic activation, tapentadol tends to have more predictable effects compared to opioids like codeine or tramadol, where genetic differences in metabolism can significantly alter response. However, variability between patients can still occur due to other physiological factors.

Similar to morphine, its oral bioavailability remains relatively low despite being clinically effective.