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
Class Membership
Psychoactive class Antidepressant / Opioid / Nootropic
Chemical class Dibenzothiazepine
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
Bioavailability 99%
Threshold 3 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.

Interactions


Tianeptine (trade names Stablon and Coaxil) is an atypical antidepressant. While primarily a prescription drug, it is sometimes used in high doses for recreational opioid effects. It has a unique and poorly-understood mechanism of action consisting of modulation of the brain's monoaminergic and glutamatergic systems.

While tianeptine is classified as a tricyclic antidepressant (TCA), its pharmacological effects differ from those of typical antidepressants.[1] This is primarily due to the fact that it is not thought to act immediately through the regulation of monoaminergic neurotransmitters (such as serotonin, dopamine, or noradrenaline.) Rather, it is theorized to act upon glutamate and glutamatergic mechanisms, causing the brain to adapt more readily to stress and depression.[2] Clinical trials of tianeptine suggest that it is just as effective as other, more popular antidepressants such as fluoxetine (i.e., SSRI) and amitriptyline (i.e., TCA). However, tianeptine seems to exhibit fewer side effects and complications than traditional antidepressants.[3]

In addition to its antidepressant effects, tianeptine also exhibits anxiolytic (anti-anxiety) properties, specifically having shown promise in the treatment of panic disorders.[4] Tianeptine also displays neuroprotective properties and has been shown to improve cognition in patients with depression.[5][6] Tianeptine's anxiolytic and mood-boosting effects, in addition to its purposed neuroprotective and cognitive benefits, make it a popular nootropic.[7]

Subjective effects of recreational doses include sedation and/or stimulation, anxiety suppression, motivation enhancement, and euphoria. Prescription guidelines indicate that tianeptine should be taken in 12.5 mg doses and taken three times daily, waiting 3-4 hours between doses.[8] However, doses of 12-35 mg are more commonly used by recreational users.

It is worth noting that very little is known about the potential toxicity of recreational tianeptine use. Some users have reported that its opioid effects can cause both physical and psychological dependence like traditional opioids (e.g. heroin, morphine, hydrocodone). It is highly advised to use harm reduction practices if using this substance.

Chemistry

Tianeptine is a tricyclic antidepressant, as its molecular structure is composed of three cyclic compounds.[9] Despite tianeptine's chemical similarity to other TCAs, its effects and mechanisms are unique.[10]

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, suggested as being superior to the sodium salt, especially with respect to having a longer half-life and duration.[11]

There is no formal research to suggest 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.[12][13] The sulfate form is not more potent, but it is metabolized slower by the body, thus making a single dose per day more 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 its peak antidepressant effect more quickly and returns 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.[14]

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.[15] 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.[16] Such increases in brain plasticity have been linked to a significant reduction of stress and depression symptoms.[2] More recent studies have concluded that tianeptine is also an effective μ-opioid receptor agonist, which could contribute to its antidepressant and anxiolytic properties.[17]

It is also sometimes used to treat irritable bowel syndrome or asthma.[18][19]

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe 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 a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it.
Note: Always conduct independent research and use harm reduction practices if 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.[22] 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.[23] 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. Due to the fact that Tianeptine generally has weaker recreational properties compared to other opioids, the withdrawal of this substance can feel significantly worse than an equally euphoric dose of a more traditional opioid.

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.

  • Canada: Tianeptine is uncontrolled in Canada, meaning it is legal to possess without any sort of license or prescription.[citation needed]
  • Germany: Tianeptine is a prescription medicine, according to Anlage 1 AMVV.[24]
  • Russia: In Russia, since 2010, tianeptine is a Schedule III controlled substance.[25]
  • Sweden: Tianeptine is not an approved prescription medicine, and is therefore a controlled substance.[26]
  • Switzerland: Tianeptine is not controlled under Buchstabe A, B, C and D. It could be considered legal.[27]
  • United Kingdom: Tianeptine is illegal to produce, supply, or import under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[28]
  • 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.[29] 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.[30]

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. Defrance, R., Marey, C., Kamoun, A. (1988). "Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials". Clinical Neuropharmacology. 11 Suppl 2: S74–82. ISSN 0362-5664. 
  2. 2.0 2.1 McEwen, B. S., Chattarji, S., Diamond, D. M., Jay, T. M., Reagan, L. P., Svenningsson, P., Fuchs, E. (March 2010). "The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation". Molecular psychiatry. 15 (3): 237–249. doi:10.1038/mp.2009.80. ISSN 1359-4184. 
  3. Wagstaff, A. J., Ormrod, D., Spencer, C. M. (2001). "Tianeptine: a review of its use in depressive disorders". CNS drugs. 15 (3): 231–259. doi:10.2165/00023210-200115030-00006. ISSN 1172-7047. 
  4. 4.0 4.1 Schruers, K., Griez, E. (December 2004). "The effects of tianeptine or paroxetine on 35% CO 2 provoked panic in panic disorder". Journal of Psychopharmacology. 18 (4): 553–558. doi:10.1177/026988110401800413. ISSN 0269-8811. 
  5. Plaisant, F., Dommergues, M.-A., Spedding, M., Cecchelli, R., Brillault, J., Kato, G., Muñoz, C., Gressens, P. (May 2003). "Neuroprotective properties of tianeptine: interactions with cytokines". Neuropharmacology. 44 (6): 801–809. doi:10.1016/s0028-3908(03)00066-2. ISSN 0028-3908. 
  6. Klasik, A., Krysta, K., Krupka-Matuszczyk, I. (September 2011). "Effect of tianeptine on cognitive functions in patients with depressive disorders during a 3-month observation". Psychiatria Danubina. 23 Suppl 1: S18–22. ISSN 0353-5053. 
  7. Tianeptine - A Mood Brightening Drug for Depression and Anxiety, 2014 
  8. TIANEPTINE: WHAT IS TIANEPTINE? | https://smartdrugsforthought.com/what-is-tianeptine/
  9. Tricyclic antidepressants (TCAs) 
  10. Brink, C. B., Harvey, B. H., Brand, L. (January 2006). "Tianeptine: a novel atypical antidepressant that may provide new insights into the biomolecular basis of depression". Recent patents on CNS drug discovery. 1 (1): 29–41. doi:10.2174/157488906775245327. ISSN 1574-8898. 
  11. http://www.ceretropic.com/tianeptine-sulfate-powder/
  12. Gorthaur111 (2015), Tianeptine Sulfate is VASTLY SUPERIOR to Tianeptine Sodium 
  13. Tianeptine sulfate is so great., 2015 
  14. Invernizzi, R., Pozzi, L., Garattini, S., Samanin, R. (March 1992). "Tianeptine increases the extracellular concentrations of dopamine in the nucleus accumbens by a serotonin-independent mechanism". Neuropharmacology. 31 (3): 221–227. doi:10.1016/0028-3908(92)90171-k. ISSN 0028-3908. 
  15. Mennini, T., Mocaer, E., Garattini, S. (November 1987). "Tianeptine, a selective enhancer of serotonin uptake in rat brain". Naunyn-Schmiedeberg’s Archives of Pharmacology. 336 (5): 478–482. doi:10.1007/BF00169302. ISSN 0028-1298. 
  16. Tianeptine ( Stablon ) 
  17. Gassaway, M. M., Rives, M.-L., Kruegel, A. C., Javitch, J. A., Sames, D. (15 July 2014). "The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist". Translational Psychiatry. 4: e411. doi:10.1038/tp.2014.30. ISSN 2158-3188. 
  18. The serotonin reuptake enhancer tianeptine ( Stablon ) prevents asthma attacks 
  19. The Tianeptine Story: Irritable Bowel Syndrome, VelaPharm and Pharmos Corporation 
  20. The serotonin reuptake enhancer tianeptine ( Stablon ) prevents asthma attacks 
  21. Klasik, A., Krysta, K., Krupka-Matuszczyk, I. (September 2011). "Effect of tianeptine on cognitive functions in patients with depressive disorders during a 3-month observation". Psychiatria Danubina. 23 Suppl 1: S18–22. ISSN 0353-5053. 
  22. Proença, P., Teixeira, H., Pinheiro, J., Monsanto, P. V., Vieira, D. N. (August 2007). "Fatal intoxication with tianeptine (Stablon®)". Forensic Science International. 170 (2–3): 200–203. doi:10.1016/j.forsciint.2007.03.035. ISSN 0379-0738. 
  23. Gassaway, M. M., Rives, M.-L., Kruegel, A. C., Javitch, J. A., Sames, D. (July 2014). "The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist". Translational Psychiatry. 4 (7): e411–e411. doi:10.1038/tp.2014.30. ISSN 2158-3188. 
  24. AMVV - Verordnung über die Verschreibungspflicht von Arzneimitteln 
  25. Resolution of the Government of the Russian Federation от 30.06.2010 N 486 
  26. https://www.lakemedelsverket.se/sv/sok-lakemedelsfakta/substans?id=E4POFBUAVAHVERT1
  27. "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020. 
  28. Psychoactive Substances Act 2016 
  29. PutItOnaTshirt (2016), Powder City has discontinued the selling of Tianeptine 
  30. 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