• BASIC DRUG
    DISCUSSION
    Welcome to Bluelight!
    Posting Rules Bluelight Rules
    Benzo Chart Opioids Chart
    Drug Terms Need Help??
    Drugs 101 Brain & Addiction
    Tired of your habit? Struggling to cope?
    Want to regain control or get sober?
    Visit our Recovery Support Forums

Tapentadol

PureLife

Bluelighter
Joined
Oct 18, 2005
Messages
2,666
Location
New Jersey
I can't for the life of me figure out how people get high on this.



ople get high on this. I've taken up to 1000mg a day. Very light high,if any. I was on auboxone but haven't taken it in some time.

So is this cross tolerance issue? Or does tapentadol just suck?
 
If memory serves me right its around 2 - 3x more potent than tramadol.
So should equal about 2000 - 3000mg tramadol or 200 - 300mg morphine.

Buccal suboxone is around 80x morphine so 1000mg tapentadol should equal 2,5 - 3,75mg buccal buprenorphine

Tapentadol is stated to have no ceiling effect (according to wikipedia) as its a full agonist.
However with your tolerance if you were taking over 4mg subs per day to remain stable id say you probably wont feel anything from tapentadol
 
Are you taking it for pain or just cause? I’m thinking if you’re in any sort of pain you might not be receiving that good good feeling ya know? I personally have never heard of it but if it’s anything like tram then it doesn’t do squat. But anywho, good luck 🤞
 
Because I placed an order with a vendor and they sent the wrong pharm. Now im stuck with 300 tabs of this.
 
Because I placed an order with a vendor and they sent the wrong pharm. Now im stuck with 300 tabs of this.
1000mg of tapentadol, even if u already have a high tolerance for opioids is very high dose which usually results at strange, very noticable mind altering effects little bit ( a lot ) different than classic agonists and tramadol feels different too.

Tapentadol produce strange mixture of noddy + diphenhydramine-like effects ( anticholinergic delusions ) + classic sedation and it should be relatively noradrenergic but this aspect of tapentadols mind alterning effects is much, much less noticable than for example that of tramadols noradrenergic part of mental effect.

If u are at least capable to metabolize tramadol to M1 at normal rate ( functional but not ultrarapid cyp2d6 metabolism ) than 1000mg of tramadol will result in noticable opioid effect with absolutely profound monoaminergic speedy semi-amphetamine effects creating mental high comparable to 80-100mg oxy + dose of amphetamine ( can't tell u how much of racemic amphetamine feels close to that monoaminergic aspect of 1000mg tramadol mental effects because it's highly individual and it's just one part of tramadols high - the other part is produced by effective full mu-opioid agonistic effects of O-DSMT which can be STRONG if u are repid cyp2d6 metaboliser and if u take enough for effects to manifest - this depends also on your tolerance.

But in case of being effective cyp2d6 metaboliser taking 1000mg tramadol results at absolutely noticable speedy+opioid effects.

Taking 1000mg of tapentadol should provide this speedy effect too but for some reason it doesn't. It is more like opioid + deliriant kind of high.

! FOR HARM REDUCTION PURPOSE I ADVICE TO NOT TAKE MORE THAN 700MG OF TAPENTADOL WITHOUT TAKING EFFECTIVE ANTICONVULSANT TOO - for example some diazepam. !

Tramadol requires anticonvulsant agent to be taken if u take more than 400mg ( it's 300mg less than in case of taking tapentadol because speedy aspect of tramadol is much more complex - it's not only NRi but it's SNRi of parent compound, serotonine releasing effect of parent compound and on top of this all even M1 ( O-DSMT ) provides further NRi effects so, it's like total monoaminergic overload combined with indirect dopamine boost from effective opioid mu-agonism and decrease in GABA.

I provided complete explanation of tapentadol and it's effects and for further understanding of 2 atypical opioids mechanism of action I provided information about tramadol too ( why it feels like it feels and what's the difference between 1000mg dose of tapentadol and 1000mg dose of tramadol - two atypical opioids with some simmilar pharmacologic properties but with somehow very different subjective feelings produced by them ).

One last information = Tapentadol has biological half-life of 4-5 hours, Tramadol has biological half-life of 6-7 hours and M1 ( O-DSMT, active metabolite which is full opioid agonist and noradrenaline reuptake inhibitor ) has biological half-life of 8 hours and after repeated dosing it's half-life is prolonged and reach 9 - 11 hours. Tramadol is considered short acting opioid prodrug and it's often compared to codeine but codeine and it's active opioid metabolites are really short acting. Codeine, morphine and C-6-G biological half-life can reach 4 hours. But tramadol and it's metabolites have biological half-life approximately 2x or 2,5x longer.
It was created like this on purpose - there was a need for longer lasting and less sedating opioid pain medication. So they created long-acting opioid + monoaminergic hybrid.
 
Will I go into precip if I take suboxone maybe. 8 hours after my last tapentadol dose
?

Thanks for the answers guys/gals.
 
Just took 150mg tapentadol an hour ago i have dihydrocodeine would taking some dihydrocodeine poteninate it ?
 
@PureLife I could talk a lot about the intricacies of this drug, Tapentadol (Nucynta). However, I feel it is sufficient to know that you have experiemented with it and had poor results. This should be a good enough idea for you that these are not going to work. I would recommend saving them for a rainy day in which you have no other Opioid agonists at your disposal. If they don't get you high like you want, they should still keep you well, so they are not useless. It's not that strange to hear a person with prior Opioid expeience to find this drug lacking. It's not an uncommon story. I have heard completely naive individuals who really like it.

@chrismeekk feel free to make your own thread in the future if you have a question. No harm done! Yes, taking Codeine is going to increase the total amount of Opioids you have on board. This is not going to be in a synergistic manner though. You are just going to be adding a dose of Codeine to where you are at now. If you have prior experience with Codeine, you should be able to judge things.
 
I can't for the life of me figure out how people get high on this.



ople get high on this. I've taken up to 1000mg a day. Very light high,if any. I was on auboxone but haven't taken it in some time.

So is this cross tolerance issue? Or does tapentadol just suck?
Tapentadol is a weaker opioid to begin with in terms of euphoria offerings at least, decent analgesia capabilities pair that with you being on subs I imagine at a steady maintenance dose, for long periods of time and likely us being junkies your idea of a long time off isint really all that long. Suboxone is a very potent opioid. Itd take months for your tolerance to reset health dependant and legenth of use and at what dosage. Imo id take tramadol before tapentadol. Tapentadol always makes me feel disassociated and dysphoric
 
@PureLife I could talk a lot about the intricacies of this drug, Tapentadol (Nucynta). However, I feel it is sufficient to know that you have experiemented with it and had poor results. This should be a good enough idea for you that these are not going to work. I would recommend saving them for a rainy day in which you have no other Opioid agonists at your disposal. If they don't get you high like you want, they should still keep you well, so they are not useless. It's not that strange to hear a person with prior Opioid expeience to find this drug lacking. It's not an uncommon story. I have heard completely naive individuals who really like it.

@chrismeekk feel free to make your own thread in the future if you have a question. No harm done! Yes, taking Codeine is going to increase the total amount of Opioids you have on board. This is not going to be in a synergistic manner though. You are just going to be adding a dose of Codeine to where you are at now. If you have prior experience with Codeine, you should be able to judge things.
Hey keif, hope youre well my man. Correct me if im wrong but wouldn't the tapentadol just out compete the codeine? I know theyre both pretty weak in terms of binding affinity but ya wouldn't the tapentadol just block the codeine essentially if nothing else just make you slightly more itchy at best?
 
1000mg of tapentadol, even if u already have a high tolerance for opioids is very high dose which usually results at strange, very noticable mind altering effects little bit ( a lot ) different than classic agonists and tramadol feels different too.

Tapentadol produce strange mixture of noddy + diphenhydramine-like effects ( anticholinergic delusions ) + classic sedation and it should be relatively noradrenergic but this aspect of tapentadols mind alterning effects is much, much less noticable than for example that of tramadols noradrenergic part of mental effect.

If u are at least capable to metabolize tramadol to M1 at normal rate ( functional but not ultrarapid cyp2d6 metabolism ) than 1000mg of tramadol will result in noticable opioid effect with absolutely profound monoaminergic speedy semi-amphetamine effects creating mental high comparable to 80-100mg oxy + dose of amphetamine ( can't tell u how much of racemic amphetamine feels close to that monoaminergic aspect of 1000mg tramadol mental effects because it's highly individual and it's just one part of tramadols high - the other part is produced by effective full mu-opioid agonistic effects of O-DSMT which can be STRONG if u are repid cyp2d6 metaboliser and if u take enough for effects to manifest - this depends also on your tolerance.

But in case of being effective cyp2d6 metaboliser taking 1000mg tramadol results at absolutely noticable speedy+opioid effects.

Taking 1000mg of tapentadol should provide this speedy effect too but for some reason it doesn't. It is more like opioid + deliriant kind of high.

! FOR HARM REDUCTION PURPOSE I ADVICE TO NOT TAKE MORE THAN 700MG OF TAPENTADOL WITHOUT TAKING EFFECTIVE ANTICONVULSANT TOO - for example some diazepam. !

Tramadol requires anticonvulsant agent to be taken if u take more than 400mg ( it's 300mg less than in case of taking tapentadol because speedy aspect of tramadol is much more complex - it's not only NRi but it's SNRi of parent compound, serotonine releasing effect of parent compound and on top of this all even M1 ( O-DSMT ) provides further NRi effects so, it's like total monoaminergic overload combined with indirect dopamine boost from effective opioid mu-agonism and decrease in GABA.

I provided complete explanation of tapentadol and it's effects and for further understanding of 2 atypical opioids mechanism of action I provided information about tramadol too ( why it feels like it feels and what's the difference between 1000mg dose of tapentadol and 1000mg dose of tramadol - two atypical opioids with some simmilar pharmacologic properties but with somehow very different subjective feelings produced by them ).

One last information = Tapentadol has biological half-life of 4-5 hours, Tramadol has biological half-life of 6-7 hours and M1 ( O-DSMT, active metabolite which is full opioid agonist and noradrenaline reuptake inhibitor ) has biological half-life of 8 hours and after repeated dosing it's half-life is prolonged and reach 9 - 11 hours. Tramadol is considered short acting opioid prodrug and it's often compared to codeine but codeine and it's active opioid metabolites are really short acting. Codeine, morphine and C-6-G biological half-life can reach 4 hours. But tramadol and it's metabolites have biological half-life approximately 2x or 2,5x longer.
It was created like this on purpose - there was a need for longer lasting and less sedating opioid pain medication. So they created long-acting opioid + monoaminergic hybrid.
Buddy buddy buddy buddy what're we doing recommending 1000MGS OF TRAMADOL TO ANYBODY FOR??? If your opioid tolerance is that high you got no buisness touching tramadol to begin with imo and you should really try to find better opioids if youre gonna be reckless anyways. that's a retarded high dose. The main issue isint even the breathing suppression its serotonin syndrome and seizures and id reckon potential nerve damage at doses like that for any substantial amount of time
 
Buddy buddy buddy buddy what're we doing recommending 1000MGS OF TRAMADOL TO ANYBODY FOR??? If your opioid tolerance is that high you got no buisness touching tramadol to begin with imo and you should really try to find better opioids if youre gonna be reckless anyways. that's a retarded high dose. The main issue isint even the breathing suppression its serotonin syndrome and seizures and id reckon potential nerve damage at doses like that for any substantial amount of time
Well at least you recommended anticonvulsants with it but not really safe at all let alone smart especially if you intend on being addicted bc what's gonna happen is eventually the anticonvulsant drugs will stop working and end up making you even more likely to have some really bad shit happen
 
Hey @Kurt Cobain!

I'm not totally sure if I understand. I don't think there would be anything in the pharmacokinetic profiles of either drug that would lead to a canceling-out kind of effect. There is no enzymatic activity that I'm aware of that would make either drugs potency blunted. They both eventually require glucuronidation to be metabolized, though I don't think that is very relevant here.

Help me out brotha, are we discussing binding affinities at the MOR? Subjective effects I.e. "Tapentadol is strong, so you probably won't even feel the Codeine"?

In general, it would just lead to an additive effect as your total MOR agonist quantity increases. I usually reference Morphine Milligram Equivalents (MME). You are just increasing your total MME's without any exotic pharmacokinetic interactions that I'm aware of.
 
Hey @Kurt Cobain!

I'm not totally sure if I understand. I don't think there would be anything in the pharmacokinetic profiles of either drug that would lead to a canceling-out kind of effect. There is no enzymatic activity that I'm aware of that would make either drugs potency blunted. They both eventually require glucuronidation to be metabolized, though I don't think that is very relevant here.

Help me out brotha, are we discussing binding affinities at the MOR? Subjective effects I.e. "Tapentadol is strong, so you probably won't even feel the Codeine"?

In general, it would just lead to an additive effect as your total MOR agonist quantity increases. I usually reference Morphine Milligram Equivalents (MME). You are just increasing your total MME's without any exotic pharmacokinetic interactions that I'm aware of.
Is tapentadol noncompetitive???
 
Is tapentadol noncompetitive???
If theyre both competing for the same exact receptor spaxes sub units of the mu and all wouldnt it just blunt or.nullify the effects of whichever has the lowest binding affinity is what im asking in a less than educated way
 
At this point, I don't want to be the type of guy who talks out of his ass when he doesn't know. I have some opinions. It would be great if we could get @4DQSAR on this one. I feel he would be able to explain this easily.
Ya I legit dont know how all that would exactly work i just figured if theyre both competitive agonsits like I think that taking a moderate dose of codeime omtop of tapentadol would do next to nothing if codeine has a weaker binding affinity and cant push the tapentadol off those same.receptor sites theyre competing for. I've been up for like a week withdrawling so im probably being a big ole dummy here
 
Ya I legit dont know how all that would exactly work i just figured if theyre both competitive agonsits like I think that taking a moderate dose of codeime omtop of tapentadol would do next to nothing if codeine has a weaker binding affinity and cant push the tapentadol off those same.receptor sites theyre competing for. I've been up for like a week withdrawling so im probably being a big ole dummy here
Now im.sure codeine has little.sub units that tapentadol doesnt even bind too that could add an effect but the overall effect were looking for would be marginal at best. Im sure itd be different with stronger opioids of course and that effect would be magnified if Im.thinking right.

Idk I've never found mixing opioids does much of anything and I've always found it best to stick to one at a time at least for a dependant addict it could be different for.someones brain whose less sensitive to opioids in general
 
Tapentadol is a VERY strange opioid. On one hand it has low affinity (comparible with dihydrocodeine), is a mixed-agonist BUT appears biassed TOWARDS beta 2 arrestin recruitment.

It's like a codeine-strength opiod that provided morphine-strength dependency! Truely another marvel brought to you by Grünenthal.

I had to use an AI to untangle the patent as on-purpose it's designed not to be human-readable by using what amounts to a tree of Markush structures which are named, but never shown as a diagram.

I looked because for the life of me I simply could not work out why they had not produced what I can only call 'tahexadol' which is a much more potent full agonist (so the dose would be far lower). The reason is that as usual, Grünenthal posits that a promiscuous ligand that monkeys around with monoamines is somehow 'less abusable' but turns out to appeal to a niche but dedicated group of users for whom that nasty monoamine modulation is a sought effect.
 
Top