Tianeptine Is Awesome

Dean

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Charlie said:
post 106479 [ref]Dean[/ref], which herbal colon cleanse? Having quality cascara sagrada is important.


It's called Colon Clenz by a company called Natural Balance. I'm sure a lot of the herbs in it are unpeaty, but it seems to work better than the cascara I tried in the past.
 
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charlie

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Some of those herbs might cause dependency issues or even nerve damage, I have not found cascara to do that at all.

Paul Jaminet said that "senna" is "risky".
Paul Jaminet said:
"It can be risky to over-use laxatives. The riskiest is probably senna, which promotes bowel movements by (a) inhibiting water absorption by the colon and (b) promoting muscle spasms in the colon wall. Unfortunately, senna is a toxin that can cause lasting damage, notably to nerves."
Bold mine.

More at link:
http://perfecthealthdiet.com/category/d ... stipation/
 
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That's exactly the brute-force kind of mechanism that shouldn't take place with properly aged Cascara Sagrada. It's kind of the point of the whole thing, but people still get put off because it's "weak".
 

Dean

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Thanks for the link, Charlie. Guess I better back off on that stuff. Sigh.

What brand of cascara are you using? I seem to remember that the only one Peat recommended was one from Italy or something. I believe it was the Frontier brand that I tried and, like I said, it didn't really do much for me.
 

narouz

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I was just googling around about Tianeptine
and happened across this.
I don't know anything about the accuracy of the material;
just found it kinda interesting...



https://www.reddit.com/r/Nootropics/comments/2oo1z8/psa_you_dont_need_to_mega_dose_tianeptine_heres/
PSA: You don't need to mega dose Tianeptine. Here's why.
submitted 10 months ago * by photoluminescence
Sorry for the wall of text, but I keep seeing posts about Tianeptine abuse and thought I'd share some info. Just as background: I'm a scientist, specializing in drug delivery, so I just thought I'd share some info reading some info on Tianeptine research and why you don't need to be mega dosing.
Phenomenon: Tianeptine works as an antidepressant.
How does this happen? The mechanism of action not completely understood, but it has been shown that Tianeptine helps with stabilization of glutamate levels in the brain. It is not exactly known how this is happening.
There is a great paper that came out in Nature on July 2014 (link) that showed several things:
Tianeptine does not directly interact with glutamate receptors. Even though studies have shown that glutamate levels are stabalized,
From paper:
It is unlikely that tianeptine modulates glutamatergic neurons and synapses via a direct interaction with glutamate receptors, at least in the concentration range examined in the present study (10 μM).
So this means: any glutamate regulation (thought to be the reason for Tianeptine's antidepressant properties) must occur downstream.
The study also showed that Tianeptine is a full agonist at the μ and δ opioid receptors with negligible effect at the κ opioid receptors.
Reported Human EC50 values:
mu opioid receptor (MOR): 194 nM
delta opioid receptor (DOR): 37 uM
kappa opioid receptor (KOR): No activity
Some Background Info:
What is an agonist?
An agonist is a chemical that binds to a receptor. Upon binding the receptor is activated to produce a biological response.
Effect of receptor activation:
MOR: euphoria, analgesia
DOR: antidepressant , analgesia (pain reduction), also thought to further activate MOR.
EC50
The EC50 is defined as the concentration of agonist that provokes a response halfway between the baseline and maximum response. It is commonly used as a measure of drug's potency. The lower the value the more potent the drug because it takes less of the drug to get a response.
From Paper:
In humans, a single dose of tianeptine (12.5 mg) results in ~ 1 μM maximal concentration of the drug in the plasma
What does this mean?
A 12.5mg dose (the recommended dose) will result an in vivo concentration sufficient for the activation of MOR (EC50 ~ 0.2–1 μM) but not DOR. Activation of DOR (EC50 ~ 12–34 μM) may only become relevant with higher dosing.
So here's some take home info from all this:
MOR activation resulted in downstream glutamate stabilization which results in anti-depressive properties
MOR activation can be achieved with the regular 12.5 mg dose three times a day
Mega doses are also likely activating DOR which is further activating MOR (euphoria) and analgesia. This effect is clearly felt.
Why no need for mega dosing?
So previous studies have shown that drugs that activate DOR will give antidepressant properties. Tianeptine is unique in that it is doing this not using DOR, but MOR. It does this by activating MOR and causing a downstream stabilization of glutamate in the brain. When people are mega dosing they report a clear feeling of euphoria and analgesia but this does not mean that when that feeling is not there you are not getting the antidepressant properties.
TLDR: If you are using Tianeptine to fight depression, 12.5mg three times a day is enough. You wont feel a dramatic change the moment you take it because it is stabilizing you. Mega-doses will give you a sense of euphoria, but also addicting and not necessary if you just want antidepressant properties.
EDITS: Formatting and typos
EDIT 2:Thank you for the comments. One thing I just wanted to mention is that my intention for the post was not to condemn those who are using larger doses of Tianeptine. When I say that larger doses are addicting I am not saying it's on the level of cocaine. Opioid receptors are prone to tolerance build up, these include those related to analgesia/euphoria. Some people, based on comments and messages I've been getting, are taking this post WAY too serious, as if I am attacking them, which I am not. This is information, plain and simple, take it or leave it.

-------

[–]sharkiteuthis 10 points 10 months ago*
Precisely because the plasma half-life is so short, I like to take a little bit of a heavier dose in the morning, ~20mg. If the kinetics are truly first-order, it's relatively straightforward to work out a dosing schedule that keeps plasma levels more even then 12.5mg TID. I haven't done this mainly because I'm kind of lazy.
Personally, I won't ever mega-dose it. I definitely feel 20mg, and I can tell there are acute anxiolytic effects at 10mg - I use hunger as my personal gauge, since the first thing anxiety knocks out is my desire to eat. I don't know what would happen if I took 100mg, but I don't think it would be pleasant.
If idiots get this ***t regulated, I am going to be very upset. It's extremely effective for depression and anxiety without any side effects (for me).
 
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I bought Tianeptine Sodium from Ceretropic...1 Gram. It comes in a little blue tub with the lose powder inside in a little plastic 'barrel'. I hope this is good for our purpose. Yes?
Also, any suggestions on how much to take. Actually I would start with the smallest amount possible because I am quite sensitive to all supplements. But I'm just curious how this product compares to others that are being used here.

Thanks!:)
 

DaveFoster

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I have the free acid form; about a 5-year supply or so. I use it irregularly; it's hard to tell if it has an effect, but I think it does.
 

pepsi

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How do you take tianeptine sodium powder form? Mix it in water or under the tongue? I dont mind the taste. Its almost like a super sour candy taste.
 

Stryker

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How do you take tianeptine sodium powder form? Mix it in water or under the tongue? I dont mind the taste. Its almost like a super sour candy taste.

i have a 10mg spoon and i put 50mg inside a gelatin capsule and swallow with a drink

i wish i could relate to the super sour candy taste.. for me it tastes like if i turned a car battery into a powder and bleached it
 

Greg says

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bump. anybody else try this? specifically the sulfate form?

I prefer the sodium over the sulphate. The sulphate lasts longer, maybe 5 hours, but is milder in effect [no peak]. The sodium powder does clump up into little hard pieces. I don't mind this as the pieces are a handy size [roughly 30-50mg] to swallow with a drink. I also know it's working because I will have a moment where I will think to myself *"god, I feel good". I think this is the mild opioid effect.

*"Mega doses are also likely activating DOR which is further activating MOR (euphoria) and analgesia. This effect is clearly felt."
 
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