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Tianeptine

 
(Last Updated On: January 19, 2019)

tianeptine

 

Overview

Tianeptine (Stablon, Coaxil) is unique, atypical antidepressant drug developed that was developed in 1981 in France.3www.tianeptine.com/tianeptine-stablon.pdf It has anti-depressive, anxiolytic, and nootropic qualities.4www.ncbi.nlm.nih.gov/pubmed/155829225www.ncbi.nlm.nih.gov/pubmed/29029227www.ncbi.nlm.nih.gov/pubmed/19704408

Some of these nootropic qualities include potent neuroprotection and the reversal of stress-related brain damage, which is a profound mechanism which I will expand on later. Tianeptine is also characterized by a distinct lack of sedation or anticholinergic effects (which are common of other antidepressant drugs).

In addition to being used to treat depression, panic disorder, and social phobia, Tianeptine also shows promise for treating asthma, autism, ADHD, IBS, and various neurodegenerative pathologies including “cerebral ischaemia, cerebral traumatism, cerebral aging, Alzheimer’s disease, multiple sclerosis, amyotrophic lateral sclerosis, demyelating pathologies, encephalopathies, chronic fatigue syndrome, myalgic encephalomyelitis post-viral fatigue syndrome, the state of fatigue following a bacterial or viral infection, and the dementia syndrome of AIDS.”3www.tianeptine.com/tianeptine-stablon.pdf

Tianeptine is a very novel drug with a pharmacological profile that is quite unlike other antidepressants. While it is technically classified as a tricyclic antidepressant (a group of antidepressants that contain three rings of atoms in the chemical structure), it is so uniquely unusual that it is considered to be in its own distinct class and is usually referred to as an “atypical” antidepressant.

Tianeptine was discovered to be a full agonist at the μ-opioid and δ-opioid receptors, with a much weaker affinity at the latter.2www.ncbi.nlm.nih.gov/pmc/articles/PMC4119213/ The μ-opioid receptors act as a hedonic hotspot in the brain, causing euphoria, while the role of the δ-opioid receptors in the brain is less understood at this time. Tianeptine’s unique ability to target both of these sites may be critical to its acute and chronic anxiolytic and antidepressant qualities.

Despite it’s affinity for opioid receptors, Tianeptine is non-addictive and does not cause physiological tolerance or dependence.6 www.ncbi.nlm.nih.gov/pubmed/28303899 When Tianeptine is taken at its therapeutic dose range, its affinity for the opioid receptors is very weak in comparison with traditional opioids, and thus has virtually zero risk of addiction or dependence.

While recreational use does exist, it is rare. There are some users of Tianeptine who take large doses to experience a “high” instead of using it therapeutically for its long-term nootropic effects. This is not how Tianeptine is intended to be used, and as a result Tianeptine is subject to criticism due to the actions of uninformed and irresponsible drug users. When Tianeptine is used properly, you may not necessarily  “feel” anything – this is the type of drug that works in the background and may not provide immediate relief.

Tianeptine also acts as a serotonin reuptake enhancer1www.ncbi.nlm.nih.gov/pubmed/18221189, which shows how little we understand about modern psychiatric medicine and the surrounding psychopharmacology. Most antidepressant drugs are serotonin reuptake inhibitors, which increase the availability of serotonin in the synapses. Given that Tianeptine does the exact opposite, this makes the “low serotonin” model of depression seem reductionistic and confounding.

However, as stated earlier, Tianeptine’s most important qualities come not from its opioid or serotonergic properties, but from its nootropic qualities.

Tianeptine has profound effects on glutaminergic neurons. Glutamate is the primary excitatory neurotransmitter in the brain and plays many roles, but it is known that overexcitation of glutamate receptors can cause cell death (excitotoxicity). Tianeptine acts as a neuroprotective agent and prevents excitotoxicity in the hippocampus via modulation of the glutamate receptors. Chronic use of Tianeptine also appears to prevent programmed cell death (apoptosis) in the temporal cortex and hippocampus as well.

Most importantly of all, Tianeptine has been shown to significantly raise levels of BDNF (brain-derived neurotrophic factor), an agent that causes new neurons to form and proliferate. Tianeptine also promotes neuroplasticity, an ability of the brain to adapt and undergo structural changes. Through these neuroplastic mechanisms, Tianeptine has been shown to reverse the damage in the brain that occurs from chronic stress.7www.ncbi.nlm.nih.gov/pubmed/197044088www.ncbi.nlm.nih.gov/pubmed/155503489www.ncbi.nlm.nih.gov/pubmed/1575395710www.ncbi.nlm.nih.gov/pubmed/1822118911www.ncbi.nlm.nih.gov/pubmed/18072812

Chronic stress leads to excessive cortisol levels which can cause pathological changes in the brain. Excess cortisol levels cause dendritic shrinkage in the hippocampus and a growth of dendrites in the amygdala; tianeptine appears to reverse these changes through its neuroplastic mechanisms.

Additionally, Tianeptine has demonstrated direct nootropic benefits; it’s been shown to improve memory consolidation, intellectual performance12www.ncbi.nlm.nih.gov/pmc/articles/PMC2701287/, and facilitate working and reference memory13www.ncbi.nlm.nih.gov/pubmed/2680463, thereby preventing stress-induced memory deficiencies.

I can confidently say that among all the nootropics available today, Tianeptine is my absolute favorite of them all. It causes profound structural changes in the brain that provide immense benefit over time.

It is a travesty how commonly it is mischaracterized by uninformed people as mere opiate that gets you “high”, as they are completely unaware of its immense nootropic and therapeutic potential.

 

 

Where to Purchase Tianeptine

tianeptine

Tianeptine (in the sulfate form) may be purchased at Nootropics.com.

 

They offer certificates of authenticity for Tianeptine and all of their other products, which is something you should always look for when choosing a seller.

As far as I am aware, they are the only reputable vendor left that sells legitimate Tianeptine. Due to the unjust legal scrutiny Tianeptine is facing, it might not be a bad idea to stock up on a lot of it while you still can, as many other sellers have been removing it from their product line due to pushback from payment processing vendors.

While the price is a bit high, I would skip the temptation to order it from other vendors who sell it for cheaper, as you may receive illegitimate or contaminated products.

 

 

 

 

Dosage Information

There are two forms of Tianeptine available: as sodium salt and in sulfate form.

Tianeptine typically comes in a sodium form which has a short half-life at only about 2.5 hours14www.ncbi.nlm.nih.gov/pubmed/3180120, and requires two redoses throughout the day. The standard therapeutic dose in the sodium form is 12.5 mg taken three times daily, for a total of 37.5mg per day.

There is another form of Tianeptine that comes in the sulfate form, however there is no data on the pharmacokinetics of this form so the exact half-life is undetermined. It does appear to last much longer than Tianeptine, and will not require redosing throughout the day. Unlike the sodium form which has a noticeable spike and dip its effects, the sulfate form is much more stable and slow-releasing, making it far more convenient and less susceptible to abuse. If taking the sulfate form it is generally recommend to take 35mg once per day.

 

References

  1. www.ncbi.nlm.nih.gov/pubmed/18221189
  2. www.ncbi.nlm.nih.gov/pmc/articles/PMC4119213/
  3. www.tianeptine.com/tianeptine-stablon.pdf
  4. www.ncbi.nlm.nih.gov/pubmed/15582922
  5. www.ncbi.nlm.nih.gov/pubmed/2902922
  6. www.ncbi.nlm.nih.gov/pubmed/28303899
  7. www.ncbi.nlm.nih.gov/pubmed/19704408
  8. www.ncbi.nlm.nih.gov/pubmed/15550348
  9. .www.ncbi.nlm.nih.gov/pubmed/15753957
  10. www.ncbi.nlm.nih.gov/pubmed/18221189
  11. www.ncbi.nlm.nih.gov/pubmed/18072812
  12. www.ncbi.nlm.nih.gov/pmc/articles/PMC2701287/
  13. www.ncbi.nlm.nih.gov/pubmed/2680463
  14. www.ncbi.nlm.nih.gov/pubmed/3180120

 

Jacob S

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