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Opioids Tianeptine vs Tramadol opioid binding affinity.

W

WellTram

Bluelighter
Joined
Aug 29, 2018
Messages
269
Hi everybody.

I can't find any relevant information about potency of this two atypical opioids ( Tianeptine sodium and Tramadol hydrochloride ) and theyr active metabolites (O-desmethyltramadol and tianeptines active metabolite ).

I would be happy if somebody can help.
Thanks.
 
deficiT said:
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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?
 
Tramalala said:
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?
Click to expand...
Yeah if you're looking for opioid effects you'll want as much of it to be metabolized into ODSMT. Oral is of course the best route since it will pass through the liver before getting into the brain.
Tramadol itself has insignificant opioid effects, O-DSMT is a much much stronger opioid (with about 200-300x more affinity for MOR).

If you go straight into the systemic circulation you will bypass the liver initially, so a significant amount of unmetabolized tramadol is going to get into the brain where it will bind to different receptors (racemic tramadol acts as a SNRI). But it will still undergo metabolism eventually, you can't avoid that entirely.

edit:
Everytime you snort a drug, some of it won't get absorbed and it will end up in the stomach instead (this is where the "drip" is going). Maybe tramadol has a very low intranasal bioavailability and it essentially ends up being the same as eating it (but weaker).

You said snorting works but how does it compare to eating it? I'm pretty sure oral is the best ROA for tramadol, at least if you want to maximize the opioids effects produced by ODSMT.
Otherwise IV seems to be pretty effective as well, mostly because of the increased bioavailability compared to oral administration, though it's a risky practice outside a medical setting.

Also tramadol appears to be kind of useless if you're a poor metabolizer, no matter how you take it (I'm referring to CYP2D6 which is the one that makes O-DSMT).
 
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WellTram said:
So, if I understand it right than tianeptine has higher binding affinity than tramadol and is actually quite potent. If it's wrong please correct me.
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Tianeptine does have a higher binding affinity. But nothing to do with potency by weight.
 
Unlike tramadol, tianeptine has affinity for the MOR in the nanomolar range and is a fair amount more potent.

From my experience, in terms of equianalgesic effect, tianeptine sodium is roughly twice as potent as tramadol by weight, where 400mg of tianeptine sodium is equivalent to about 800mg of tramadol.

The comparison is impefect however since both tianeptine and tramadol are pretty unusual opioids, but a ratio of 2:1 is a pretty decent approximation.
 
negrogesic said:
Unlike tramadol, tianeptine has affinity for MOR in the nanomolar range and is fair amount more potent.

From my experience, in terms or equianalgesic effect, tianeptine sodium is roughly twice as potent as tramadol by weight, where 400mg of tianeptine sodium is equivalent to about 800mg of tramadol.

The comparison is impefect however since both tianeptine and tramadol are pretty unusual opioids, but a ratio of 2:1 is a pretty decent approximation.
Click to expand...
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.
 
WellTram said:
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.
Click to expand...

Definitely of note, that sounds like an extremely high dose.

You've suffered these effects and continue using tramadol/tianeptine? I hope you are doing Ok and are thinking about switching to a less fatal, less pharmacologically complex alternative.

I've had some serious seizures before and it definitely scared me away from doing that again
 
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SnafuInTheVoid said:
Definitely of note, that sounds like an extremely high dose.

You've suffered these effects and continue using tramadol/tianeptine? I hope you are doing Ok and are thinking about switching to a less fatal, less pharmacologically complex alternative.

I've had some serious seizures before and it definitely scared me away from doing that again
Click to expand...
My biggest dose of tram was approximately 2000mg dosed throught the day, it was in form of oral solution called TRAMAL. Its acting much faster than green/yellow capsules. But my favourite form is TRAMAL 100MG RETARD.
 
I was a hardcore tramadol addict for over 10 years. I went through tramadol withdrawal every month, every year, for over a decade.

With that said, my first go with tianpetine was tianpetine sulfate from a well respected vendor. My experience was completely null all the way up to 400mg of tianeptine sulfate. Absolutely no opioid effects whatsoever.

So I'm very confused why anyone would think tianeptine would be stronger than a good dose of tramadol (which is metabolized in ODSMT which is much stronger than the parent compound). They felt nothing alike either. Is it because it was sulfate? Does this form really make that big of a difference? I understand the sulfate version is suppose to be like an extended release, so it won't hit you as hard or as fast, but that's like saying nobody can enjoy extended release morphine or methadone. Hell I even enjoyed extended release tramadol at one point. So why would the sulfate version be any different? It should have still produced a long duration mild opioid-type effect, but it did not.
 
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@DeathIndustrial88 There is a significant difference in the intensity and speed of onset between Tianeptine Sulfate and Tianeptine Sodium, so much so that an equal oral dose of each almost feels like they are a different drug not just a different version of the same drug. The sulfate absorbs into the blood stream through the stomach and intestines markedly slower whereas the sodium version very rapidly does, so much so that a large oral dose of Tianeptine Sodium actually can have somewhat of a decent rush to it as it kicks in.

it's also possible that your opioid tolerance was just too high at the moment to appreciate the effects of the sulfate dose you took. Some people don't get much out of or don't really like Tianeptine's effects, you might fall into one of these categories.
 
MDPV_Psychosis said:
@DeathIndustrial88 There is a significant difference in the intensity and speed of onset between Tianeptine Sulfate and Tianeptine Sodium, so much so that an equal oral dose of each almost feels like they are a different drug not just a different version of the same drug. The sulfate absorbs into the blood stream through the stomach and intestines markedly slower whereas the sodium version very rapidly does, so much so that a large oral dose of Tianeptine Sodium actually can have somewhat of a decent rush to it as it kicks in.

it's also possible that your opioid tolerance was just too high at the moment to appreciate the effects of the sulfate dose you took. Some people don't get much out of or don't really like Tianeptine's effects, you might fall into one of these categories.
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Aaah ok. Thanks MDPV.
Damn. That's unfortunate, cause I was a hardcore lover of tramadol and would love if there were some kind of easily accessible legal version of it. (some say kratom is, but I highly disagree).

I was on low doses of buprenorphine at the time, but was easily able to feel high dose tramadol (400mg range) at the time. Was disappointed when I tried the tianpetine sulfate.
I did notice an effect from the tianeptine and it wasn't necessarily bad, but it was very much a subjective head change (not a high) but felt nothing similar to an opioid or tramadol. I figured I should have at least felt some kind of mild extended duration opioid effect but wasn't able to perceive much of anything all the way up to 400mg of the sulfate and was cautious to raise the dosage any further.

I'd give tianpetine sodium a shot but i'm a little weary of messing with online vendors and need to hang onto my pennies. Maybe one day though.

I'm actually an oddball out there and having tried morphine, heroin, methadone, fentanyl, hydrocodone, oxycodone and buprenorphine, I still loved the unique effects that only tramadol seems to have and the rest don't. Most people pin this down simply to it's "SNRI" type of profile, but I think it's that + a whole combo of actions that tramadol has that aren't fully understood. But it surely is a fantastic compound.
 
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DeathIndustrial88 said:
Aaah ok. Thanks MDPV.
Damn. That's unfortunate, cause I was a hardcore lover of tramadol and would love if there were some kind of easily accessible legal version of it. (some say kratom is, but I highly disagree).

I was on low doses of buprenorphine at the time, but was easily able to feel high dose tramadol (400mg range) at the time. Was disappointed when I tried the tianpetine sulfate.
I did notice an effect from the tianeptine and it wasn't necessarily bad, but it was very much a subjective head change (not a high) but felt nothing similar to an opioid or tramadol. I figured I should have at least felt some kind of mild extended duration opioid effect but wasn't able to perceive much of anything all the way up to 400mg of the sulfate and was cautious to raise the dosage any further.

I'd give tianpetine sodium a shot but i'm a little weary of messing with online vendors and need to hang onto my pennies. Maybe one day though.

I'm actually an oddball out there and having tried morphine, heroin, methadone, fentanyl, hydrocodone, oxycodone and buprenorphine, I still loved the unique effects that only tramadol seems to have and the rest don't. Most people pin this down simply to it's "SNRI" type of profile, but I think it's that + a whole combo of actions that tramadol has that aren't fully understood. But it surely is a fantastic compound.
Click to expand...
Never tried O-DSMT my friend? It still is legal in most places, but I think you can't find it any headshop or other store. So you'd have to use an online vendor though, it's honestly not hard. Everything just on the clearweb, no need to load up Tails & Tor.

Many people like it better than Tramadol but I think I'm more like you, there is something very special about tramadol. This long lasting blissful effect where you are just so happy to live and want to do stuff but at the same time you can just relax and chill if you want. O-DSMT does give some energy too because of its NRI effect but its not quite like tramadol. Personally tramadol doesn't work as good for me anymore as it once did though but O-DSMT hits the spot.
 
Tramalala said:
Never tried O-DSMT my friend? It still is legal in most places, but I think you can't find it any headshop or other store. So you'd have to use an online vendor though, it's honestly not hard. Everything just on the clearweb, no need to load up Tails & Tor.

Many people like it better than Tramadol but I think I'm more like you, there is something very special about tramadol. This long lasting blissful effect where you are just so happy to live and want to do stuff but at the same time you can just relax and chill if you want. O-DSMT does give some energy too because of its NRI effect but its not quite like tramadol. Personally tramadol doesn't work as good for me anymore as it once did though but O-DSMT hits the spot.
Click to expand...

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.
 
Hi,
So for years u have been on tramadol instant release and have always enjoyed them, I have now been put on th ER tramadol and I am wondering if I crush them I can experience the same pleasant effects from the ER?

Any advice would be appreciated.

Peace and love
BB
 
BILLY-BLUNT said:
Hi,
So for years u have been on tramadol instant release and have always enjoyed them, I have now been put on th ER tramadol and I am wondering if I crush them I can experience the same pleasant effects from the ER?

Any advice would be appreciated.

Peace and love
BB
Click to expand...

Yes, I think so.
Just be careful because the ER form usually comes in higher doses and crushing a high dose and swallowing it could lead to a seizure or ill effects.

Tramadol's opioid effects work better if you stack your doses. And no matter what you do, it still needs to be metabolized by the liver, which can take up to 1-2 hours.
 
4meSM said:
Yeah if you're looking for opioid effects you'll want as much of it to be metabolized into ODSMT. Oral is of course the best route since it will pass through the liver before getting into the brain.
Tramadol itself has insignificant opioid effects, O-DSMT is a much much stronger opioid (with about 200-300x more affinity for MOR).

If you go straight into the systemic circulation you will bypass the liver initially, so a significant amount of unmetabolized tramadol is going to get into the brain where it will bind to different receptors (racemic tramadol acts as a SNRI). But it will still undergo metabolism eventually, you can't avoid that entirely.

edit:
Everytime you snort a drug, some of it won't get absorbed and it will end up in the stomach instead (this is where the "drip" is going). Maybe tramadol has a very low intranasal bioavailability and it essentially ends up being the same as eating it (but weaker).

You said snorting works but how does it compare to eating it? I'm pretty sure oral is the best ROA for tramadol, at least if you want to maximize the opioids effects produced by ODSMT.
Otherwise IV seems to be pretty effective as well, mostly because of the increased bioavailability compared to oral administration, though it's a risky practice outside a medical setting.

Also tramadol appears to be kind of useless if you're a poor metabolizer, no matter how you take it (I'm referring to CYP2D6 which is the one that makes O-DSMT).
Click to expand...
So taking tramadol orally will always convert to ODSMT as long as you have the right liver enzymes. Am I correct?
 
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