Tianeptine

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Summary sheet: Tianeptine
Tianeptine
Tianeptine.svg
Chemical Nomenclature
Common names Tianeptine, Stablon, Coaxil, Tatinol
Substitutive name Tianeptine
Systematic name (RS)-7-(3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-ylamino)heptanoic acid S,S-dioxide
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold Common Heavy
3 - 6 - 12 - 35 - 100 mg
Light Strong
Bioavailability 99%
Threshold 3 - 6 mg
Light 6 - 12 mg
Common 12 - 35 mg
Strong 35 - 100 mg
Heavy 100 mg +
Duration
Total 2 - 3 hours
Onset 30 - 60 minutes
Come up 15 - 30 minutes
Peak 60 - 90 minutes
Offset 30 - 60 minutes









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Tianeptine (trade names Stablon and Coaxil) is a pharmaceutical compound most commonly used for the treatment of clinical depression. It is also sometimes used to treat irritable bowel syndrome or asthma.[1][2] At heavy doses, tianeptine produces opioid-like effects such as sedation and stimulation, motivation enhancement, and euphoria via μ-opioid agonism when administered.

In terms of chemical classification, tianeptine is a tricyclic antidepressant (TCA). However, its pharmacology and effects vary from those of typical antidepressant and anxiolytics[3], mainly in the fact that it is not thought to act immediately through the regulation of monoaminergic neurotransmitters (such as serotonin, dopamine, and noradrenaline.) Rather, tianeptine is theorized to act upon glutamate and glutamatergic mechanisms, causing the brain to adapt more readily to stress and depression.[4]

Clinical trials of tianeptine suggest it is just as effective as other more popular antidepressants such as fluoxetine (a SSRI) and amitriptyline (a TCA). However, Tianeptine seems to exhibit fewer side effects and complications than traditional antidepressants.[5]

In addition to its antidepressant effects, tianeptine also exhibits anxiolytic (anti-anxiety) properties, specifically showing promise in the treatment of panic disorders.[6] Tianeptine also displays neuroprotective properties and improves cognition in patients with depression.[7][8] Tianeptine's anxiolytic and mood-boosting effects, in addition to its neuroprotective and cognitive benefits, make it a popular nootropic.[9]

Prescription guidelines indicate that tianeptine should be taken in 12.5 mg doses and taken three times daily, waiting 3-4 hours between doses.[10]

Chemistry

In terms of molecular structure and chemistry, tianeptine is a tricyclic antidepressant as its molecular structure is composed of three cyclic compounds.[11] Despite tianeptine's chemical similarity to other TCAs, its effects and mechanisms is completely unique. This is due to Tianeptine's structure and action on the glutamatergic system, completely unique to this compound, it may challenge the way we understand how depression affects the brain, paving the way for further research into the mechanism of this selective reuptake enhancer.[12]

Sodium and sulfate salts

Like many drugs, tianeptine can be manufactured into various salt forms to achieve maximum bioavailability, absorption, and overall effectiveness. Tianeptine is most commonly found in its sodium salt form because it is the only version that is sold by pharmacies and prescribed by doctors. However, the sulfate salt is now also being marketed on nootropic vendor sites, purveyed as being superior to the sodium salt.[13]

There is no formal research to prove any increased efficacy of the sulfate form, but anecdotal reports from users suggest that it may be more effective and have a longer duration than the sodium salt.[14][15] The sulfate form is not necessarily more potent, but it is metabolized slower by the body, thus making a single dose a day effective. Anecdotal reports by users of both salt forms indicate that because the sulfate is metabolized more slowly, there is less potential for addiction. The sulfate form appears to provide a more level experience, as opposed to the sodium form, which reaches a peak in its antidepressant effect and also comes back to baseline more suddenly.

Tianeptine's structure compared to those of more typical TCAs. Note that tianeptine possesses more functional groups than the others, contributing to its unique pharmacological profile.

Pharmacology

Unlike most prescribed antidepressants, tianeptine appears to have negligible direct effects on monoamines like dopamine and serotonin. Tianeptine slightly increases extracellular levels of dopamine, although it is not known how exactly it causes this release.[16]

Experiments conducted on rats revealed that tianeptine does not increase levels of serotonin in subjects. Rather, it has been found to increase the reuptake of serotonin, being labeled a selective serotonin reuptake enhancer.[17] This lies in contrast to the most popularly prescribed antidepressants, which are selective serotonin reuptake inhibitors (SSRIs). However, tianeptine's alteration of serotonin is likely not relevant to its mechanism.

Tianeptine also contributes to a significant increase in neuroplasticity through the modulation of glutamate and its receptors, most notably through the indirect modulation of NMDA receptors.[18] Such increases in brain plasticity have been linked to a significant reduction of stress and depression symptoms.[19] More recent studies have concluded that tianeptine is also an effective μ-opioid receptor agonist, which could contribute to its antidepressant and anxiolytic properties.[20]

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Visual effects
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Cognitive effects
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Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

Additional experience reports can be found here:

Toxicity and harm potential

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This toxicity and harm potential section is a stub.

As such, it may contain incomplete or even dangerously wrong information. You can help by expanding upon or correcting it.
We also recommend that you practice diligent independent research and the most thorough harm reduction practices when using this substance.

The toxicity and long-term health effects of recreational tianeptine use have not been studied in any scientific context, and the exact toxic dosage is unknown.

Anecdotal evidence suggests that there are no negative health effects attributed to simply trying the drug by itself at low to moderate doses and using it very sparingly (but nothing can be completely guaranteed). Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

It is strongly recommended that one use harm reduction practices when using this substance.

Lethal dosage

The LD50 of tianeptine has not yet officially been established; however, it seems to have a large therapeutic index and margin of safety. In 2007, a 26-year-old man committed suicide by taking an excessive amount of tianeptine in combination with alcohol.[24] However, the amount required to overdose is not likely to be taken on accident. To ensure safety while using tianeptine, it is advised to not exceed 100 mg in a single dose or 300 mg total in one day.

Tolerance and addiction potential

The chronic use of tianeptine can be considered as mildly addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of tianeptine develops with prolonged use, including therapeutic effects. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). This compound may share a cross tolerance with other trycyclic antidepressants and opioids.

It is worth noting that because of tianeptine's short duration of effects, it may compel some to frequent redosing. The potential euphoric effects of high doses (> 100 mg) may cause some users to exceed recommended dosages, which could quickly raise tolerance and intensify negative side effects. In addition, tianeptine possesses certain properties as a μ-opioid agonist, possibly leading to addiction and withdrawal mechanics similar to that of opiates.[25] However, as with most people looking to discontinue their antidepressant medications (both SSRIs and TCAs), daily users of tianeptine should taper off their usage instead of suddenly halting it. This will ensure that negative discontinuation symptoms are kept to a minimum.

Tianeptine withdrawal can occur with as little as ~500mg per day, and increases in severity with the amount of daily dosage and time spent using the drug. Withdrawal symptoms are similar to opioids (flu-like symptoms, watery eyes, and nose, dry heaves et al.) and may include emotional instability. However, the withdrawal of this substance can potentially be significantly stronger compared to opioids.

Legal status

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

Tianeptine is available by prescription in many European, Asian, and South American countries and distributed under brand names such as Stablon and Coaxil.

  • United Kingdom - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[26]
  • United States - Tianeptine is currently a federally uncontrolled substance in the United States. However, many nootropics vendors have ceased carrying it due to its recreational use and abuse potential.[27] In March of 2018, the Michigan state legislature passed a bill to classify tianeptine sodium salt as a Schedule II controlled substance, making it the first state to schedule the drug.[28]

See also

External links

Literature

  • Ormrod, D.J., Spencer, C.M., & Wagstaff, A.J. (2001). Tianeptine: a review of its use in depressive disorders. CNS Drugs, 15 3, 231-59. PMID: 11463130

References

  1. Treatment of bronchial asthma with tianeptine | http://www.tianeptine.com/asthma.html
  2. Vela Pharmaceuticals Awarded Patent for use of Tianeptine in Irritable Bowel Syndrome (IBS) and Nonulcer Dyspepsia (NUD) | http://www.tianeptine.com/ibs/index.html
  3. Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2902922
  4. The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2902200/
  5. Tianeptine: a review of its use in depressive disorders (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/11463130
  6. The effects of tianeptine or paroxetine on 35% CO2 provoked panic in panic disorder | http://jop.sagepub.com/content/18/4/553
  7. Neuroprotective properties of tianeptine: interactions with cytokines (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/12681378
  8. Effect of tianeptine on cognitive functions in patients with depressive disorders during a 3-month observation. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21894095
  9. Tianeptine - A Mood Brightening Drug for Depression and Anxiety. | http://nootriment.com/tianeptine/
  10. TIANEPTINE: WHAT IS TIANEPTINE? | https://smartdrugsforthought.com/what-is-tianeptine/
  11. Tricyclic antidepressants and tetracyclic antidepressants | http://www.mayoclinic.org/diseases-conditions/depression/in-depth/antidepressants/art-20046983
  12. Tianeptine: a novel atypical antidepressant that may provide new insights into the biomolecular basis of depression (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/18221189
  13. http://www.ceretropic.com/tianeptine-sulfate-powder/
  14. https://www.reddit.com/r/Nootropics/comments/30w63b/tianeptine_sulfate_is_vastly_superior_to/
  15. https://www.reddit.com/r/Nootropics/comments/33or7s/tianeptine_sulfate_is_so_great/
  16. Tianeptine increases the extracellular concentrations of dopamine in the nucleus accumbens by a serotonin-independent mechanism (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/1630590
  17. Tianeptine, a selective enhancer of serotonin uptake in rat brain.|https://www.ncbi.nlm.nih.gov/pubmed/3437921
  18. Tianeptine.com | http://tianeptine.com/
  19. The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2902200/
  20. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/25026323
  21. http://www.tianeptine.com/asthma.html
  22. http://jop.sagepub.com/content/18/4/553
  23. http://www.ncbi.nlm.nih.gov/pubmed/21894095
  24. Fatal Intoxication with tianeptine (Stablon (R)) | http://www.researchgate.net/publication/6208457_Fatal_intoxication_with_tianeptine_(Stablon_(R))
  25. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist | http://www.nature.com/tp/journal/v4/n7/full/tp201430a.html
  26. Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted
  27. Powder City has discontinued the selling of tianeptine | https://www.reddit.com/r/Nootropics/comments/4a1oq2/powder_city_has_discontinued_the_selling_of/
  28. Michigan's Legislature has passed a statewide ban on the antidepressant tianeptine sodium. | https://www.usnews.com/news/best-states/michigan/articles/2018-03-21/snyder-to-receive-bill-on-statewide-tianeptine-sodium-ban