Opioids Tianeptine vs Tramadol opioid binding affinity.

[4meSM]

So taking tramadol orally will always convert to ODSMT as long as you have the right liver enzymes. Am I correct?

Yeah, a percentage of it will be converted to ODSMT. The exact amount of ODSMT produced will vary from person to person.

 

[MDPV_Psychosis]

Damn I loved tianeptine sodium. I remember production and sales had largely ceased around the 2018/19 targeted attacks by the FDA to ban kratom. It would be sweet if it were back in circulation.

I always found tianeptine sodium to have stronger opioid effects than tramadol.

Tianeptine market is alive and kicking here in the US (except in Alabama and Michigan where it's been scheduled at the state level). Some places are still selling it in those bottles in fucking gas stations, which is nuts. Things did slow down a bit in that 2018/2019 time you mentioned but it almost immediately picked back up again. So it's still in circulation, just no longer quite as easy to find as most nootropics vendors who are legitimately trying to sell an array of nootropics no longer carry it due to the risk/stigma and the fact that most payment processors refuse to work with them if they do sell it. So it's still out there, just a little more hidden (aside from gas station products that are sold in some areas still)

 

[Abitofeverything]

Kind of offtopic but one interesting thing about tramadol is that people claim it needs to be metabolized to O-DSMT in the liver to have effect. With people saying that injecting, snorting or taking it sublingual shouldnt have (much) effect. I'm talking about this now because I saw IV tramadol mentioned in your picture. Personally I've found snorting it to work, takes away withdrawals. Someone has any more info on this?

It is a prodrug, and is essentially not active until metabolized

 

[Abitofeverything]

I'm in the US. I think ODSMT is illegal here now. I could be wrong but I think anything that is a metabolite or analogue of an already controlled substance is illegal. So I'm not sure where to look. I've had my card info swiped from somewhere before, which makes me pretty paranoid.

I think I may have had kratom laced with ODSMT back in like 2011ish. Cause it was the only time I got a nod and a high from kratom & ODSMT laced kratom was going around back then. I've tried kratom about 50 times (all different strains & brands) since then and have never had that same experience. In fact, I've never achieved any opioid effects from kratom whatsoever.

There's definitely something special about trams. They are definitely long lasting & they have this component to their effect that make you just feel complete joy for life & the things you love. I use to be able to nod out and listen to music for hours and hours on tramadol and NEVER get bored. Or I'd get up and clean the entire house and actually ENJOY doing it! I got so much done in my creative life & in my personal life on them.

Only other opioid that even comes close to giving me those same effects is heroin. Some people compare buprenorphine to tramadol but personally I have been on buprenorphine for the past 5 years and while it does have it's own "stimulating" come up, it is nothing like the all out bliss & joy I use to get from tramadol. Buprenorphine doesn't make me want to get up and clean like trams did. Bupe also makes music sound dull and boring and makes everything I love feel dull & boring too. Nothing like tramadol at all.

I wonder what it is that makes tramadol so special. It can't simply be the SNRI effect. I've taken effexor with my bupe,thinking it might feel similar to tramadol and effexor feels nothing like it. So it must be something else going on with trams. Maybe it's the serotonin release, rather than the uptake inhibition?

Idk but after having access to and feeling that bliss for over 10 years, only to be cut off and stuck with shitty buprenorphine actually makes me not sure if I wanna stick around for the rest of my time on this boring ass prison planet.

It’s not actually an SSRI it is a SERT or seretonin enhancer which is why the danger of serotonin syndrome and seizures are relatively high compared to things like tapentadol

 

[brokedownpalace10]

Thanks for reply. I am chronic tramadol and once in a while tianeptine user. 250mg tianeptine sodium is deff "stronger" than 250mg tramadol in terms of cassual opiate effects, like feeling warm and anxiolysis, pupil constriction but it lasts about 3 hour since tramadol produce less intense opioid feeling but it has that long lasting speedy feeling, sometimes even 12 hours but after couple hours it shifts to more sedating, noddy high.

This is off-topic but high (700+)mg of tramadol coupled with a nice dose of alprazolam produce serious, strong opioid high but it is potentially dangeroes. I have suffered 3 hardcore seizures and 1 blood-circulation collapse. This is for little bit of harm-reduction.

As you have found, Tianeptine lasts a significantly shorter time than Tramadol. Doesn't have that initial antidepressant effect but, damn, it goes away as quick as it hits for me.
So, people end up doing a lot real quickly.
I have a low opiate tolerance, so YMMV definitely depending on that, but I love Tramadol. I can work up to a good dose taking it every hour or two and then fade into a long lasting opiate high. It used to be great for back pain. I'd ride the up effect all day at work and then coast into a nice drowsy high all night.

 

[DeathIndustrial88]

It’s not actually an SSRI it is a SERT or seretonin enhancer which is why the danger of serotonin syndrome and seizures are relatively high compared to things like tapentadol

I didn't say it was an "SSRI"..... Tramadol is absolutely a very weak SNRI. It's structurally similar to another SNRI, venlafaxine. It's SNRI properties are so weak that they're almost irrelevant in terms of effects, but they're there.


It's also a TAAR1 agonist, so it's not just "enhancing" serotonin, rather it causes a release of serotonin. Any drug that causes serotonin release (meth, MDMA) has the potential to cause serotonin syndrome. And seizures.


But those things are unlikely to happen just from taking tramadol alone. I used tramadol every month for over 10 years.
I've mixed it with methamphetamine & dextromethorphan a few times. Which is incredibly dangerous & theoretically should have given me serotonin syndrome or seizures, but I survived. So I think SS & seizures from tramadol tend to be overblown.

 

[jambabomba]

I didn't say it was an "SSRI"..... Tramadol is absolutely a very weak SNRI. It's structurally similar to another SNRI, venlafaxine. It's SNRI properties are so weak that they're almost irrelevant in terms of effects, but they're there.


It's also a TAAR1 agonist, so it's not just "enhancing" serotonin, rather it causes a release of serotonin. Any drug that causes serotonin release (meth, MDMA) has the potential to cause serotonin syndrome. And seizures.


But those things are unlikely to happen just from taking tramadol alone. I used tramadol every month for over 10 years.
I've mixed it with methamphetamine & dextromethorphan a few times. Which is incredibly dangerous & theoretically should have given me serotonin syndrome or seizures, but I survived. So I think SS & seizures from tramadol tend to be overblown.

Have you mixed Tramadol with Methadone? I am worried about possible serotonin interactions as I have also inte past mixed DXM and Tramadol with bad results. Don't want to repeat that experience so that is why - by knowing Methadone's and Tramadol's serotonin enchancing activity - I now want to be especially carefull and rather neurotic than regret later.

I also love Tramadol and it is the preferred opioid for me as it truly has these unique effects. It really increases ability to function but on the same time it allows you to relax like no other compound. It just increases overall quality of life and consciousness in general. Allows your potential to be filled.

Now I am using Methadone but really want to change ASAP back to Tramadol. Methadone makes me tired and doesn't give much if any high. I think Bupre was better than Methadone but Tramadol was absolutely better than Buprenorphine even though Bupre too helps with my depression and anxiety but it also same time gives this strange anxiety. Maybe it is related to kappa agonism.

 

[jambabomba]

I don't also like NMDA-antagonism properties of Methadone. I think I have done too much DXM/Nitrous oxide and become sensitive to NMDA-antagonism. Small doses of NMDA-antagonists especially inhibit GABAergic neurons and so the overall effect seems to be increased glutamatergic activity and even psychotic symptoms from excessive firing of glutamatergic pyramidal neurons and so excessive dopamine and serotonin too.

I am also tapering Gabapentin and benzos atm so I am especially sensitive to any increase in glutamatergic, serotonergic or dopaminergic activity.

 

[DeathIndustrial88]

Have you mixed Tramadol with Methadone? I am worried about possible serotonin interactions as I have also inte past mixed DXM and Tramadol with bad results. Don't want to repeat that experience so that is why - by knowing Methadone's and Tramadol's serotonin enchancing activity - I now want to be especially carefull and rather neurotic than regret later.

I also love Tramadol and it is the preferred opioid for me as it truly has these unique effects. It really increases ability to function but on the same time it allows you to relax like no other compound. It just increases overall quality of life and consciousness in general. Allows your potential to be filled.

Now I am using Methadone but really want to change ASAP back to Tramadol. Methadone makes me tired and doesn't give much if any high. I think Bupre was better than Methadone but Tramadol was absolutely better than Buprenorphine even though Bupre too helps with my depression and anxiety but it also same time gives this strange anxiety. Maybe it is related to kappa agonism.

I've never mixed tramadol with methadone.
I do think there a possibility of serotonin syndrome mixing both. But there are also people who are able to mix SSRIs/SNRIs with methadone just fine. So I'm not really sure.


The way you describe tramadol is exactly how it worked for me (at least from the age of 19-31). Tramadol just made me feel so amazing & it gave me this urge to listen to music, make music, be creative, made me wanna walk around & exercise a lot. Just this over all feeling of total contentedness. Heroin gives me a similar effect but not as quite stimulating or creativity-inducing as tramadol did.

I haven't had many chances to use tramadol anymore in the past few years. And when I did, it was only ever a few at a time. And it didn't seem to have that same magic anymore for some reason. But I think it's because I've been on bupe for 8 years now & I really think bupe alters your receptors or alters the way you experience other opioids. I don't know how or why. And I don't just mean it's blocking properties. I can feel as little as 10mg of hydrocodone on Subs, but it never feels totally euphoric or creativity-inducing anymore.


You're actually the 2nd person I've come across in the past 6 months who said they prefer bupe to methadone, which is interesting. You would think most people would prefer methadone since it's a full agonist. I actually don't have much experience with methadone unfortunately.
I've had a few one-off experiences with methadone in the past & I thought it felt alright. It was a little more hollow feeling than heroin or tramadol, but I remember it made me feel really sedated but content & comfy.

Bupe is a weird one. Some days I actually enjoy the mild effects from it, but other days it just makes me really tired & makes my emotions & mind feel flat, which I hate. I would absolutely prefer to be on 400mg of tramadol a day. I was so much more energetic & ate less on tramadol. But with bupe, I get hardcore food cravings & end up feeling like I have to pop a bunch of other drugs (caffeine, epehedrine, benzos, gabapentin, etc...etc..) just to make up for the lack of content & mood lift that subs don't give. Not that popping the other shit every truly works or helps anyway.


I've also done so much DXM in my life time. And now I'm terrified of taking DXM for whatever reason. lol I had some incredibly magical, mystical experiences on DXM just back in like 2015-2018. But now it fucks me up in a way that just makes me freaked out & anxious. Even just a little bit of DXM changes my perceptions. it also fucks with my stomach pretty bad.

Sounds like we have a bit in common my friend!

 

[Skorpio]

I just want to add that you can't really compare binding affinities between different studies. Depending on the assay done, binding affinities can vary quite a bit. To compare two drugs, you would want to measure them both in the same experiment, so that you can compare the two binding affinities.

Also binding affinity only determines potency of a drug. Efficacy at the receptor will determine strength. Buprenorphine illustrates this concept, as it has a very high affinity for the mu opioid receptors, but a low efficacy, so that doses are sub to single milligram, but there is a limit to how strong of an effect one can feel.

 

[jambabomba]

I've never mixed tramadol with methadone.
I do think there a possibility of serotonin syndrome mixing both. But there are also people who are able to mix SSRIs/SNRIs with methadone just fine. So I'm not really sure.


The way you describe tramadol is exactly how it worked for me (at least from the age of 19-31). Tramadol just made me feel so amazing & it gave me this urge to listen to music, make music, be creative, made me wanna walk around & exercise a lot. Just this over all feeling of total contentedness. Heroin gives me a similar effect but not as quite stimulating or creativity-inducing as tramadol did.

I haven't had many chances to use tramadol anymore in the past few years. And when I did, it was only ever a few at a time. And it didn't seem to have that same magic anymore for some reason. But I think it's because I've been on bupe for 8 years now & I really think bupe alters your receptors or alters the way you experience other opioids. I don't know how or why. And I don't just mean it's blocking properties. I can feel as little as 10mg of hydrocodone on Subs, but it never feels totally euphoric or creativity-inducing anymore.


You're actually the 2nd person I've come across in the past 6 months who said they prefer bupe to methadone, which is interesting. You would think most people would prefer methadone since it's a full agonist. I actually don't have much experience with methadone unfortunately.
I've had a few one-off experiences with methadone in the past & I thought it felt alright. It was a little more hollow feeling than heroin or tramadol, but I remember it made me feel really sedated but content & comfy.

Bupe is a weird one. Some days I actually enjoy the mild effects from it, but other days it just makes me really tired & makes my emotions & mind feel flat, which I hate. I would absolutely prefer to be on 400mg of tramadol a day. I was so much more energetic & ate less on tramadol. But with bupe, I get hardcore food cravings & end up feeling like I have to pop a bunch of other drugs (caffeine, epehedrine, benzos, gabapentin, etc...etc..) just to make up for the lack of content & mood lift that subs don't give. Not that popping the other shit every truly works or helps anyway.


I've also done so much DXM in my life time. And now I'm terrified of taking DXM for whatever reason. lol I had some incredibly magical, mystical experiences on DXM just back in like 2015-2018. But now it fucks me up in a way that just makes me freaked out & anxious. Even just a little bit of DXM changes my perceptions. it also fucks with my stomach pretty bad.

Sounds like we have a bit in common my friend!

Actually, sounds like we have more than a little common now when I read your story - it was like I had wrote it myself :D

I mean, if I go chapter by chapter there is nothing I wouldn't agree. Even your age/timeline you said Tramadol worked best (19-31y) is exactly the age it worked it's magic for me too. I also wasn't at all interested in alcohol during times of Tramadol and hanging on and drinking at bups&discos seemed boring and waste of time. I would rather - like you described - do sports, hang out bymyself, spend time on listening music, reading science stuff, being creative and so on. I bet my level of consciousness was at the highest that it ever has been during this lifetime within those years. Maximal use of frontal lobes with passion to life in general achieving the level of love. One thing though, I also had Baclofen&Phenibut combined years 2011-2015 and they were definitily additive to Tramadol's positive effects.

Also when you described DXM, your story sounded exactly like mine. I used it extensively/daily after/between Tramadol's use somewhere 2012-2015 and also had major spiritual experiences and overall my whole point of using it so much became down to spiritual search/search of God/Truth and so on. I just ended up using it too much for too long, inflated ego too much, developed chronic egomania and ended up in mental hospital thinking ego is God. I also have aversion nowdays to DXM, serotonin (except when it is induced by Tramadol which I still like, still do and need and have prescription) but also like you said it doesn't work exactly like it did at age 19-31y but part reason is my major spiritual crash and crisis at year 2022 which made me severely depressed, anxious and put me through severe spiritual agony of hell which caused me to relapse and use again opioids and benzos and other stuff after being sober over 4 years.

Also your description of the effects of Buprenorphine are exactly how I perceive and would describe them. Even though I (like you said) sometimes find it pleasurable and good for relaxing (nodding). Nothing like soberheaded, clear, energetic pro-life high, like with Tramadol but just boring, tired, flat...tiredness. Well, relaxed yes..that is nice part of it... but really not functional. I allmost lost my functionality and work ability when my dosed escalated day by day. So it is not good for me in the long run. And I guess I don't like Methadone much because of it's NMDA-antagonism even though it is also pure agonist.

Edit: Yes, I guess it is Methadone's NMDA-activity. What I've understood is that with small doses NMDA-antagonists mostly inhibit just GABAergic neurons. When doses become larger they also inhibit more glutamatergic neurons. I get allmost same kind of feeling from NMDA-antagonists that I get from THC and both have common effect that they inhibit GABAergic neurons. If I am remembering correctly, THC can at small doses inhibit also glutamatergic neurons but when doses get higher it starts to inhibit more gabaergic neurons and can cause everything from anxiety&paranoia to seizures (rare). For some reason, I am nowdays very sensitive also to THC and suspect that even low doses inhibit more gabaergic neurons in me. Because I get quite similar anxiogenic effect from both NMDA-antagonists and THC. It reminds me of benzo withdrawals. And I am tapering from benzos and gabapentin.. I bet that will put the treshold down.

 

[DeathIndustrial88]

Actually, sounds like we have more than a little common now when I read your story - it was like I had wrote it myself :D

I mean, if I go chapter by chapter there is nothing I wouldn't agree. Even your age/timeline you said Tramadol worked best (19-31y) is exactly the age it worked it's magic for me too. I also wasn't at all interested in alcohol during times of Tramadol and hanging on and drinking at bups&discos seemed boring and waste of time. I would rather - like you described - do sports, hang out bymyself, spend time on listening music, reading science stuff, being creative and so on. I bet my level of consciousness was at the highest that it ever has been during this lifetime within those years. Maximal use of frontal lobes with passion to life in general achieving the level of love. One thing though, I also had Baclofen&Phenibut combined years 2011-2015 and they were definitily additive to Tramadol's positive effects.

Also when you described DXM, your story sounded exactly like mine. I used it extensively/daily after/between Tramadol's use somewhere 2012-2015 and also had major spiritual experiences and overall my whole point of using it so much became down to spiritual search/search of God/Truth and so on. I just ended up using it too much for too long, inflated ego too much, developed chronic egomania and ended up in mental hospital thinking ego is God. I also have aversion nowdays to DXM, serotonin (except when it is induced by Tramadol which I still like, still do and need and have prescription) but also like you said it doesn't work exactly like it did at age 19-31y but part reason is my major spiritual crash and crisis at year 2022 which made me severely depressed, anxious and put me through severe spiritual agony of hell which caused me to relapse and use again opioids and benzos and other stuff after being sober over 4 years.

Also your description of the effects of Buprenorphine are exactly how I perceive and would describe them. Even though I (like you said) sometimes find it pleasurable and good for relaxing (nodding). Nothing like soberheaded, clear, energetic pro-life high, like with Tramadol but just boring, tired, flat...tiredness. Well, relaxed yes..that is nice part of it... but really not functional. I allmost lost my functionality and work ability when my dosed escalated day by day. So it is not good for me in the long run. And I guess I don't like Methadone much because of it's NMDA-antagonism even though it is also pure agonist.

Edit: Yes, I guess it is Methadone's NMDA-activity. What I've understood is that with small doses NMDA-antagonists mostly inhibit just GABAergic neurons. When doses become larger they also inhibit more glutamatergic neurons. I get allmost same kind of feeling from NMDA-antagonists that I get from THC and both have common effect that they inhibit GABAergic neurons. If I am remembering correctly, THC can at small doses inhibit also glutamatergic neurons but when doses get higher it starts to inhibit more gabaergic neurons and can cause everything from anxiety&paranoia to seizures (rare). For some reason, I am nowdays very sensitive also to THC and suspect that even low doses inhibit more gabaergic neurons in me. Because I get quite similar anxiogenic effect from both NMDA-antagonists and THC. It reminds me of benzo withdrawals. And I am tapering from benzos and gabapentin.. I bet that will put the treshold down.

Wow, yeah I see a lot of parallels with us here!

I never drank on tramadol either, cause I didn't want the alcohol buzz to ruin my my tramadol. lol I did drink a lot in between scripts though.
My mom was prescribed tramadol. And a lot of it at first. Back when it was still unscheduled & doctors/pharmacists really thought it was "just like another tylenol", so they'd even double fill the script in one month some times.

But I went through tramadol withdrawal every month from the age of 19-30ish (which was around 2008-2018). Every single month for 11 years. I eventually got on Subs & then I'd just switch back n forth.

I also went through some soul crushing things around the same time frame as you. I lived with my mom for 11 years in Iowa. And we were having problems with the asshole neighbors above us that had moved in. My mom got diagnosed with cancer in late 2019. My heroin dealer also murdered some one & went to prison in 2019. Cutting off my access to heroin. I then spent all of 2020 in a very dark place, going on meth binges, taking my mom to chemo treatments, dealing with the neighbors above us who would stomp & fight all day & night (landlord wouldn't do anything about it, sheriffs wouldn't do anything about it). So I became crazy really.

And I started banging on our ceiling whenever these assholes would keep me awake, which eventually started a war & they turned around & complained about me. Which resulted in our asshole landlord kicking me & my 70 year old mother out. So my mom went to live one of my sisters in another state & I decided to move in with an ex of mine who turned out to be super abusive. And then my mom passed away on Mother's Day of 2021 unexpectedly. I was a wreck. They had also tapered her tramadol down to only like 30 a month or something by that point too, so my access to tramadol was gone by then too.

So from 2021-current day, I've had to totally readjust to a new a life without any access to tramadol or heroin. Only bupe. And it's been pretty difficult honestly. Most days when I wake up, I can't understand why I continue to stay in this world. I use to have friends to hang out with, access too all these great drugs & an interesting life. And now I have nothing whatsoever.

I went through a spiritual journey on DXM as well during those years of 2015-2018ish. That shit felt like it unlocked something paranormal that I was able to use. Whenever I'd use DXM, something fun & interesting would happen only a few days later. Lots of synchronicities. I became really popular with a lot of people (including my heroin dealer) and was always going out & having fun & meeting new people. Would have weird paranormal glitches & things that would happen to me while actively on DXM too that my mom & friends even witnessed with me. It got so bad that one of my best friends would always ask me "are you on DXM", whenever something weird would happen to her. lol I would take DXM a few times a week, usually when I was in opioid withdrawal & had to wait for either my moms tramadol to get filled or for my heroin dealer to come around.

I even did "ritual magic" on DXM to try & win my ex back. lol I won't get into too much about that here though.

But eventually I had to stop because DXM was giving me these trips where I felt like I was dying, especially if I smoked a lot of weed on it. And I think I also became very sensitive to serotonergic drugs. I can't handle SSRIs/SNRIs at all anymore, because just one dose gives me hand tremors, projectile vomiting & internal burning sensations. Where as in my 20's, I could easily stomach & handle an SSRI/SNRI.


And right now I'm currently dealing with a heart arrhythmia that came out of nowhere. So I'm afraid to take anything that might make it act up (like caffeine, ephedrine, DXM, etc..) when just 2 months ago, I was a person who had no issues handling any of these drugs (except maybe the DXM). So now I dunno wtf to do with myself but if I have to live with feeling like my heart is being squeezed over & over 30+ times a day, then that's gonna be really difficult for me to grapple with. Especially after all this hell I went through from 2019 to the current day.

Hopefully I wrote all this out right, as I'm just getting up over here. lol