Tianeptine instead of SSRI

[ZenPit]

I've been doing some research on Tianeptine (Stablon) and am considering giving it a shot. Wondering if anyone here has heard about it, used it and how that ended up?

It seems to have a good shot at helping people who previous medications didn't, lacks a lot of the side effects that most anti-anxiety and anti-depressants have.

[SADnomore]

Haven't heard of it before. Apparently it isn't available in the U.S. the U.K., Australia, New Zealand and Canada. ... Maybe this is why?

"According to Servier, cessation of treatment with tianeptine is difficult, due to the possibility of withdrawal symptoms in a person.[27][28][29]
In 2007, according to French Health Products Safety Agency, tianeptine's manufacturer Servier agreed to modify the drug's label, following problems with dependency.[30]
Singapore's Ministry of Health has restricted the use of tianeptine to psychiatrists due to its abuse potential,[31] while Bahrain has classified it a controlled substance due to increasing reports of misuse and abuse by persons.[32] In September 2012, France began treating Stablon as a controlled substance. Its use now requires a "secure prescription" form in France, just as is required for narcotics." Wikipedia

Which kind of makes sense, when you read more about its effects on the opiod receptors:
"Tianeptine has been found to be an efficacious μ-opioid receptor agonist (Ki (human) of 383 ± 183 nM and EC50 (human) of 194 ± 70 nM). The same study revealed that it is also a δ-opioid receptor agonist, although with much lower potency.[9]"

According to tianeptine.com:
"In fact tianeptine may finally reach the USA branded not as an antidepressant, but in the guise of a treatment of Irritable Bowel Syndrome (IBS). For in 2004 Vela Pharmaceuticals registered a patent for the use of tianeptine to treat IBS. In March 2006 Pharmos Corporation acquired Vela. Tianeptine for IBS is now in "late-preclinical development". If and when a medicine gains a US product license, physicians can then prescribe it "off-label" for whatever they see fit, including depression. But this prospect is several years away at best."

Yeah. "At best" would seem to be the operative phrase here. Too bad it appears to be addictive, because certainly otherwise it did sound good. :(

[hanshan]

If it's a mu-opioid receptor agonist, it will probably be treated as potentially addictive and closely controlled (I believe the "mu" is derived from "morphine"). Chances are doctors won't be prescribing it freely.

[ZenPit]

I've been researching it, and it is available in USA so far I've only found one supplier of capsuled Tianeptine. From what I've read it is used well in European countries.

I was not aware of its opioid activity, what does this necessary mean? I was interested in it because of the fact that it is a SSRE and not a SSRI.

[SADnomore]

I don't have a medical background so I don't know the proper way to put it in medical terms, but what it seems to indicate is that it fully activates the morphine receptors in the brain, just as morphine would. We really don't want to poke that particular bear. ...

Well, from what you say, it sounds as though it may have been approved for the U.S. as perhaps the IBS remedy? Good Lord, I would rather have the IBS (back) than a monkey on my back ...

Also, Google searching I found the following ...
"The antidepressant tianeptine was once claimed to be a (selective) serotonin reuptake enhancer (SRE or SSRE), but the role of serotonin reuptake in its mechanism is doubtful. Tianeptine has no affinity to the serotonin transporter, neither increases nor decreases extracellular levels of serotonin in cortico-limbic structures of conscious rats, and it didn't show any other long-term effect on the serotonin pathway.[1]" again, Wikipedia. http://en.wikipedia.org/wiki/Reuptake_enhancer

I know Wikipedia isn't the be-all and end-all (lol!), and there are of course other links that will support the use of tianeptine in anxiety/depression. It's effects/lack of effects on serotonin notwithstanding, if it activates opiod receptors (thereby risking addiction), I can't imagine any reason besides severe physical pain for it's use. And in which case, you'd want to get an actual narcotic if necessary, in a medical setting.

I've read a bit about the SSRE theory, which opposes the current long-held North American practice of increasing available serotonin by inhibiting it's uptake. The article I read argues that serotonin actually creates the stress response, and that it's reuptake is what is required in order to treat anxiety and depression. NOwhere is it mentioned that it binds to the opiod receptors.

Sorry, I honestly think this is a major, major red flag. Not everything that makes us feel good (at first) is a good idea. ...

[ZenPit]

Odd everywhere I look up (pubmed included) there doesn't seem to be a lot of info on it acting similarly to morphine, and they all seem to say the same about it being a SSRE.

Such confused.

[ZenPit]

I ended up ordering Tianeptine through Smart Drugs for Thought since their website had a lot of information regarding it as well as citations to clinical studies that used TIaneptine in them.