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tianeptine as a mood enhancer while on subutex/opiate tolerant

Tryptamite

Tryptamite

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Joined
Dec 5, 2006
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I am interested in trying tianeptine again for its mood enhancing effects, perhaps a few days each week.

I know it is classified as an ssre, but others have suggested and i have experienced that its MOA has something to do with mu opiod rrceptors or endorphin system.

Coaxil/stablon abusers regularly inject 150mg of the drug from tablets. To achieve an opiate like rush.
I myself injected the purepowder when i had a moderate heroin terance i had to shoot doses of 300mg to achieve this rush but it was opiate like qnd did stave off withdrawals for some hours.

Which leads me to believe tianeptine would be useless or its effectiveness dramatically reduced in persons who are opiate tolerant.
Also i would wonder if buprenorphine would block this drug entirely?

I would like to take doses of 50mg x 3 times a day on an irregular basis and will experiment with my situation when i have some extra cash to spend.

In the meantime could anyone shed some light or give me an opinion on this curious drug and its effects?

Perhaps it is only opiate like in super-theraputic doses?...
 
I don't see any reason stablon would have a cross-tolerance with bupe.
I'm in the same boat as you precisely so let me know how that works out for you will ya? I have problems subscribing to threads.
 
Tryptamite said:
I am interested in trying tianeptine again for its mood enhancing effects, perhaps a few days each week.

I know it is classified as an ssre, but others have suggested and i have experienced that its MOA has something to do with mu opiod rrceptors or endorphin system.

Coaxil/stablon abusers regularly inject 150mg of the drug from tablets. To achieve an opiate like rush.
I myself injected the purepowder when i had a moderate heroin terance i had to shoot doses of 300mg to achieve this rush but it was opiate like qnd did stave off withdrawals for some hours.

Which leads me to believe tianeptine would be useless or its effectiveness dramatically reduced in persons who are opiate tolerant.
Also i would wonder if buprenorphine would block this drug entirely?

I would like to take doses of 50mg x 3 times a day on an irregular basis and will experiment with my situation when i have some extra cash to spend.

In the meantime could anyone shed some light or give me an opinion on this curious drug and its effects?

Perhaps it is only opiate like in super-theraputic doses?...
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Is there any evidence that tianeptine acts on the opiate system, besides the fact that it gives an opiate-like high and makes withdrawal less painful? I would guess that the therapeutic effects are more related to its serotonin effects, so it should still be effective (therapeutically) in someone with opiate dependence. That might not be true for the recreational effects though.


edit: It is an effective antidepressant during opiate withdrawal, I still haven't seen anything about using both together though.
 
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Apparently it has no effect on seratonin, and has recently been found to work on NMDA and AMPA. Very Nice! Just ordered some.
 
I have no actual evidence to say it works on opiate receptors but I would be very suprised if it did not have some sort of opiate activity at higher doses. It does not ease WD symptoms, it completely eliminates them in sufficient dosages.

There are others on this forum besides me with more experience using tianeptine as an opiate like drug. I have consumed only 1.25 grams of the substance. I did use ~20mg oral doses a few times per day for a few days during opiate WD until I ran out. It didnt hurt, and I imagine it would have helped a lot more in higher doses.

I just find it difficult to get my head around it's method of action. SSRE? Clearly there is more going on than that. TH, where did you read about it working on NMDA and AMPA?
 
"Formerly it was called a Serotonin Reuptake Enhancer. Newer research suggests that Tianeptine acts through indirect alteration of AMPA and NMDA glutamate receptor activity and seems to involve altered neuroplasticity and release of BDNF.[5][6][7][8][9][10][11][12][13]"

http://en.wikipedia.org/wiki/Tianeptine
 
TriputoryHeadicine said:
"Formerly it was called a Serotonin Reuptake Enhancer. Newer research suggests that Tianeptine acts through indirect alteration of AMPA and NMDA glutamate receptor activity and seems to involve altered neuroplasticity and release of BDNF.[5][6][7][8][9][10][11][12][13]"

http://en.wikipedia.org/wiki/Tianeptine
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This had to of been extremely recent. I was just looking at that article about two weeks ago and they were still calling it a SSRE.
 
Hmmm, tianeptine just became a lot more interesting to me.

Although the vast majority of neurons in the mammalian brain are formed prenatally, parts of the adult brain retain the ability to grow new neurons from neural stem cells in a process known as neurogenesis. Neurotrophins are chemicals that help to stimulate and control neurogenesis, BDNF being one of the most active.[9][10][11] Mice born without the ability to make BDNF suffer developmental defects in the brain and sensory nervous system, and usually die soon after birth, suggesting that BDNF plays an important role in normal neural development.[12]
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http://en.wikipedia.org/wiki/BDNF

Sounds like tianeptine might actually be a true nootropic if this new research pans out. No wonder it isn't prescribed in the US.
 
MagickalKat777 said:
Hmmm, tianeptine just became a lot more interesting to me.



http://en.wikipedia.org/wiki/BDNF

Sounds like tianeptine might actually be a true nootropic if this new research pans out. No wonder it isn't prescribed in the US.
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The increase in BDNF is not a feature particular to tianeptine; it seems to a be a common shared trait of many antidepressants, and it may be predictive of their effectiveness in an individual:

What you can see here is a correlation between the BDNF levels and a change in depression score. It turns out that those patients with the highest levels of BDNF to begin with, had the best improvements in depression score when treated with antidepressants.

From a SciAm quick summary:

http://blogs.scientificamerican.com/scicurious-brain/2012/02/20/using-bdnf-to-predict-antidepressant-response/
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Anyway, I'm not sure if I'd say this would make it a nootropic in the way you're suggesting. Depression has a dumbing effect, but can we say that this release of BDNF will somehow make non-depressed individuals "smarter"? Maybe we don't want excess BDNF! Take a look at this:

Brain-derived neurotrophic factor (BDNF) overexpression in the forebrain results in learning and memory impairments.
Cunha C1, Angelucci A, D'Antoni A, Dobrossy MD, Dunnett SB, Berardi N, Brambilla R.
Author information
Abstract
In this study we analyzed the effect on behavior of a chronic exposure to brain-derived neurotrophic factor (BDNF), by analysing a mouse line overexpressing BDNF under the alphaCaMKII promoter, which drives the transgene expression exclusively to principal neurons of the forebrain. BDNF transgenic mice and their WT littermates were examined with a battery of behavioral tests, in order to evaluate motor coordination, learning, short and long-term memory formation. Our results demonstrate that chronic BDNF overexpression in the central nervous system (CNS) causes learning deficits and short-term memory impairments, both in spatial and instrumental learning tasks. This observation suggests that a widespread increase in BDNF in forebrain networks may result in adverse effects on learning and memory formation.

http://www.ncbi.nlm.nih.gov/pubmed/19095063
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Now, obviously that's a very different situation, but it illustrates the problems we have with assuming that more of a good thing is always a good thing.
 
Depression has a dumbing effect
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I think that depression exerts a far greater skewing effect on self-assessment of intelligence than it does on intelligence itself.

Now, obviously that's a very different situation, but it illustrates the problems we have with assuming that more of a good thing is always a good thing.
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Good point, and a good corrective to our tendency toward over-enthusiasm about singular pathways.

ebola
 
ebola? said:
I think that depression exerts a far greater skewing effect on self-assessment of intelligence than it does on intelligence itself.



Good point, and a good corrective to our tendency toward over-enthusiasm about singular pathways.

ebola
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God point yourself madame, depression and dumbing. Can I have your autograph? I'm an Ebola fanboy : P
 
Whilst it could skew ones perception on their intellect, that is not a dumbing effect.
The dumbing effect comes from dull affect/apathy, if you don't care about things you once did you don't put in the effort to learn about them.
Doing nothing also has an effect. I've found my verbal communication skills degraded from a few years of not talking that much.
Words become harder to find, information is harder to recall, the will to do so isn't even there.

I think depression facilitates stupidity not through a purely emotion basis but through taking away the driving force to not be stupid/encouraging intellectual atrophy.
 
so anyone on suboxone try this recreationally? I would love to get some if every week or two I could get a nice opaite like high while not screwing up my subs.
 
As If Suboxone Had Disappeared

supersmoker27 said:
so anyone on suboxone try this recreationally? I would love to get some if every week or two I could get a nice opaite like high while not screwing up my subs.
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I just want to say: I was quite amazed with this compound and felt compelled to create an account here to respond. I have been slowwwwwwwly tapering off Subs for over a year now (currently taking .25mg/day, yet I start to noticeably withdraw within ~15 hours from my last dose). I've been experimenting with a wide assortment of noots, so figured I may as well try Tianeptine. [no sources no prices] I decided to take a slightly-megadose for my initial attempt (~200mg), which coincidentally happened to be around an hour after I dosed my Sub. I must say, I felt as if I had blown ~15mg of oxycodone after NEVER having taken Subs. The Buprenorphine/Nalaxone seems to have absolutely no effect in blocking whichever receptors the Tianeptine makes sweet receptor love to. It also did not in any way disturb my Suboxone cycle. In all honesty, I seemed to no longer NEED the Suboxone the next two days while I continued to dose the Tianeptine. AND, to make things better, I was even able to HALVE my daily Suboxone dose after the Tianeptine ran out (was taking .5mg, now taking .25mg), and my normal taper reduction would be more like .5mg --> .4mg. I was amazed. I have since ordered 20g more Tianeptine. I would say that the 1g I had ended up being equivalent to ~3 Oxycodone 30mg pills

And, from what I've read, even if Tianeptine will have withdrawals, they should be pale in comparison to the months-long Suboxone withdrawals that were awaiting me.

Awesome legal, cheap high!

(Disclaimer: The substance above [erm... the nootropic supplement, not the life-ruining narcotics supplied by my psychiatrist—AKA dealer] is for research only and should not be consumed by humans.)
 
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This doesn't sound all that suprising given that tianeptine is an opioid agonist. It is very probably that any opioid you took would produce a similar effect. The tianeptine withdrawal may not last as long as the buprenorphine withdrawal but the same is true for codeine. I'm not convinced that tianeptine is a good solution for you because tianeptine is abused and produces a withdrawal syndrome, so in the end it might not work any better than codeine would to wean you off of buprenorphine.
 
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According to the binding data it shouldn't be causing an opioid high, especially one that is comparable to oxycodone. Tianeptine - Ki Human of 383±183nM and EC50 Human of 194±70nM at MOR. Enough to activate the receptors, sure, but it's mood lifting properties are more likely mediated through it's effect on glutamate receptors in the hippocampus.

For reference some pKi values for other MOR agonists:

Morphine - 4.55nM
Methadone - 3.16nM
Oxycodone - 23.4nM
7-OHM - 8.01 nM

I have used Tianeptine recently and I will say that it has potential as a drug to include at the end of a taper.
 
pinpoint said:
According to the binding data it shouldn't be causing an opioid high, especially one that is comparable to oxycodone. Tianeptine - Ki Human of 383±183nM and EC50 Human of 194±70nM at MOR. Enough to activate the receptors, sure, but it's mood lifting properties are more likely mediated through it's effect on glutamate receptors in the hippocampus.

For reference some pKi values for other MOR agonists:

Morphine - 4.55nM
Methadone - 3.16nM
Oxycodone - 23.4nM
7-OHM - 8.01 nM

I have used Tianeptine recently and I will say that it has potential as a drug to include at the end of a taper.
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I don't see how you can reach the conclusion you did based on the binding data. The Ki and EC50 determine the concentration that a drug will be active at, not how efficacious it is. Just because tianeptine has lower affinity then morphine doesn't mean that it couldn't produce just as strong an effect, as long as it is present in the brain at a high enough concentration to occupy mu receptors.

(BTW, I don't think the values you cited for morphine et al are pKi since they were in nM)
 
According to the binding data it shouldn't be causing an opioid high
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serotonin2a's essentially correct about this: binding affinity and efficacy are only part of the picture, pharmacokinetics looming large in particular.* However, I'm seeing tianeptine's binding as being just one order of magnitude weaker than oxycodone's, the latter being a pretty strong opioid...so it still seems plausible that tianeptine functions as a week opioid (but that this activity could still plausibly prove key in its subjective effects).

*in some sense, both binding affinity and efficacy are abstractions from qualitatively unique interactions between ligand and active site, resulting change in receptor geometry, and following signaling cascade, reducing such processes to singular quantitative indicators.

ebola
 
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