en>Opal: Some info

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Some info

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{{SummarySheet}}
{{SubstanceBox/Tianeptine}}

'''Tianeptine''' (trade names '''Stablon''' and '''Coaxil''') is an atypical [[Psychoactive class::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 [[Chemical class::tricyclic antidepressant]] (TCA), its pharmacological effects differ from those of typical antidepressants.<ref>{{cite journal | vauthors=((Defrance, R.)), ((Marey, C.)), ((Kamoun, A.)) | journal=Clinical Neuropharmacology | title=Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials | volume=11 Suppl 2 | pages=S74-82 | date= 1988 | issn=0362-5664}}</ref> This is primarily due to the fact that it is not thought to act immediately through the regulation of monoaminergic [[Neurotransmitter|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]].<ref name="McEwen2010">{{cite journal | vauthors=((McEwen, B. S.)), ((Chattarji, S.)), ((Diamond, D. M.)), ((Jay, T. M.)), ((Reagan, L. P.)), ((Svenningsson, P.)), ((Fuchs, E.)) | journal=Molecular psychiatry | title=The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation | volume=15 | issue=3 | pages=237–249 | date= March 2010 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2902200/ | issn=1359-4184 | doi=10.1038/mp.2009.80}}</ref> 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.<ref>{{cite journal | vauthors=((Wagstaff, A. J.)), ((Ormrod, D.)), ((Spencer, C. M.)) | journal=CNS drugs | title=Tianeptine: a review of its use in depressive disorders | volume=15 | issue=3 | pages=231–259 | date= 2001 | issn=1172-7047 | doi=10.2165/00023210-200115030-00006}}</ref>

In addition to its antidepressant effects, tianeptine also exhibits [[Anxiety suppression|anxiolytic]] (anti-anxiety) properties, specifically having shown promise in the treatment of panic disorders.<ref name="Schruers2004">{{cite journal | vauthors=((Schruers, K.)), ((Griez, E.)) | journal=Journal of Psychopharmacology | title=The effects of tianeptine or paroxetine on 35% CO 2 provoked panic in panic disorder | volume=18 | issue=4 | pages=553–558 | date= December 2004 | url=http://journals.sagepub.com/doi/10.1177/026988110401800413 | issn=0269-8811 | doi=10.1177/026988110401800413}}</ref> Tianeptine also displays neuroprotective properties and has been shown to improve cognition in patients with depression.<ref>{{cite journal | vauthors=((Plaisant, F.)), ((Dommergues, M.-A.)), ((Spedding, M.)), ((Cecchelli, R.)), ((Brillault, J.)), ((Kato, G.)), ((Muñoz, C.)), ((Gressens, P.)) | journal=Neuropharmacology | title=Neuroprotective properties of tianeptine: interactions with cytokines | volume=44 | issue=6 | pages=801–809 | date= May 2003 | issn=0028-3908 | doi=10.1016/s0028-3908(03)00066-2}}</ref><ref>{{cite journal | vauthors=((Klasik, A.)), ((Krysta, K.)), ((Krupka-Matuszczyk, I.)) | journal=Psychiatria Danubina | title=Effect of tianeptine on cognitive functions in patients with depressive disorders during a 3-month observation | volume=23 Suppl 1 | pages=S18-22 | date= September 2011 | issn=0353-5053}}</ref> Tianeptine's anxiolytic and mood-boosting effects, in addition to its purposed neuroprotective and cognitive benefits, make it a popular [[nootropic]].<ref>{{Citation | year=2014 | title=Tianeptine - A Mood Brightening Drug for Depression and Anxiety | url=https://nootriment.com/tianeptine/}}</ref>

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.<ref>TIANEPTINE: WHAT IS TIANEPTINE? | https://smartdrugsforthought.com/what-is-tianeptine/</ref> 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.<ref>{{Citation | title=Tricyclic antidepressants (TCAs) | url=https://www.mayoclinic.org/diseases-conditions/depression/in-depth/antidepressants/art-20046983}}</ref> Despite tianeptine's chemical similarity to other TCAs, its effects and [[Scientific_information#Pharmacology|mechanisms]] are unique.<ref>{{cite journal | vauthors=((Brink, C. B.)), ((Harvey, B. H.)), ((Brand, L.)) | journal=Recent patents on CNS drug discovery | title=Tianeptine: a novel atypical antidepressant that may provide new insights into the biomolecular basis of depression | volume=1 | issue=1 | pages=29–41 | date= January 2006 | issn=1574-8898 | doi=10.2174/157488906775245327}}</ref>

===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.<ref>http://www.ceretropic.com/tianeptine-sulfate-powder/</ref>

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.<ref>{{Citation | vauthors=((Gorthaur111)) | year=2015 | title=Tianeptine Sulfate is VASTLY SUPERIOR to Tianeptine Sodium | url=https://www.reddit.com/r/Nootropics/comments/30w63b/tianeptine_sulfate_is_vastly_superior_to/}}</ref><ref>{{Citation | year=2015 | title=Tianeptine sulfate is so great. | url=https://www.reddit.com/r/Nootropics/comments/33or7s/tianeptine_sulfate_is_so_great/}}</ref> 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.
[[File:Tianeptine_and_TCAs.png|250px|thumb|right|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.<ref>{{cite journal | vauthors=((Invernizzi, R.)), ((Pozzi, L.)), ((Garattini, S.)), ((Samanin, R.)) | journal=Neuropharmacology | title=Tianeptine increases the extracellular concentrations of dopamine in the nucleus accumbens by a serotonin-independent mechanism | volume=31 | issue=3 | pages=221–227 | date= March 1992 | issn=0028-3908 | doi=10.1016/0028-3908(92)90171-k}}</ref>

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''.<ref>{{cite journal | vauthors=((Mennini, T.)), ((Mocaer, E.)), ((Garattini, S.)) | journal=Naunyn-Schmiedeberg’s Archives of Pharmacology | title=Tianeptine, a selective enhancer of serotonin uptake in rat brain | volume=336 | issue=5 | pages=478–482 | date= November 1987 | issn=0028-1298 | doi=10.1007/BF00169302}}</ref> This lies in contrast to the most popularly prescribed antidepressants, which are selective [[serotonin]] [[reuptake inhibitor]]s (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.<ref>{{Citation | title=Tianeptine ( Stablon ) | url=https://www.tianeptine.com/}}</ref> Such increases in brain plasticity have been linked to a significant reduction of stress and depression symptoms.<ref name="McEwen2010" /> More recent studies have concluded that tianeptine is also an effective [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]] [[agonist]], which could contribute to its antidepressant and [[Anxiety suppression|anxiolytic]] properties.<ref>{{cite journal | vauthors=((Gassaway, M. M.)), ((Rives, M.-L.)), ((Kruegel, A. C.)), ((Javitch, J. A.)), ((Sames, D.)) | journal=Translational Psychiatry | title=The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist | volume=4 | pages=e411 | date=15 July 2014 | issn=2158-3188 | doi=10.1038/tp.2014.30}}</ref>

It is also sometimes used to treat irritable bowel syndrome or asthma.<ref>{{Citation | title=The serotonin reuptake enhancer tianeptine ( Stablon ) prevents asthma attacks | url=https://www.tianeptine.com/asthma.html}}</ref><ref>{{Citation | title=The Tianeptine Story: Irritable Bowel Syndrome, VelaPharm and Pharmos Corporation | url=https://www.tianeptine.com/ibs/index.html}}</ref>

==Subjective effects==
{{Preamble/SubjectiveEffects}}

{{effects/base

|{{effects/physical|
*'''[[Effect::Stimulation]]'''
*'''[[Effect::Physical euphoria]]''' - More pronounced feelings of euphoria have been reported at doses near or above 100 mg. These feelings are extremely similar to that of a typical [[opioid]].
*'''[[Effect::Bronchodilation]]''' - Tianeptine increases the reuptake of serotonin, which has been found to combat bronchoconstriction.<ref>{{Citation | title=The serotonin reuptake enhancer tianeptine ( Stablon ) prevents asthma attacks | url=https://www.tianeptine.com/asthma.html}}</ref>
*'''[[Effect::Muscle relaxation]]'''
*'''[[Effect::Headaches]]'''
*'''[[Effect::Nausea]]''' - Nausea is experienced in high dosages, taken for its euphoric effects.
*'''[[Effect::Itchiness]]''' - Like traditional opioids, itchiness may manifest at recreational doses, and can range from mild to severe depending on dosage and tolerance.
*'''[[Effect::Dizziness]]'''
*'''[[Effect::Constipation]]''' - As a full mu-opioid agonist at heavy doses, tianeptine slows down gut motility, causing constipation identical to other opioids.
*'''[[Effect::Physical fatigue]]'''
*'''[[Effect::Pupil constriction]]''' - Pinpoint pupils are common after taking recreational doses.

}}
{{effects/visual|
*'''[[Effect::Internal hallucination]]''' - One may experience a state of semi-consciousness and [[hypnagogia]] during heavy dosage nodding which results in dream-like states and up to level 3 [[Lucid_dreaming#Internally_sourced_sensory_input|imagery]]. This is often accompanied by ill-defined [[geometry]].

}}
|{{effects/cognitive|
*'''[[Effect::Motivation enhancement]]'''
*'''[[Effect::Anxiety suppression]]''' - Tianeptine has been found to be especially useful in mitigating the effects of panic attacks.<ref name="Schruers2004"/>
*'''[[Effect::Cognitive euphoria]]''' - More pronounced feelings of euphoria have been reported at doses near or above 100 mg. These feelings feel extremely similar to that of a typical [[opioid]].
*'''[[Effect::Focus enhancement]]''' - In addition to enhancing the ability to focus, tianeptine also improves the retention of short-term memories, stimulates quicker learning, and improves reaction time.<ref>{{cite journal | vauthors=((Klasik, A.)), ((Krysta, K.)), ((Krupka-Matuszczyk, I.)) | journal=Psychiatria Danubina | title=Effect of tianeptine on cognitive functions in patients with depressive disorders during a 3-month observation | volume=23 Suppl 1 | pages=S18-22 | date= September 2011 | issn=0353-5053}}</ref>
*'''[[Effect::Thought acceleration]]''' or '''[[Effect::Thought deceleration]]'''
*'''[[Effect::Rejuvenation]]'''
*'''[[Effect::Ego inflation]]'''
*'''[[Effect::Cognitive fatigue]]''' - Although rare, some users may experience adverse effects in terms of cognition such as the impairment of thought processes.

}}
}}
===Experience reports===
Anecdotal reports which describe the effects of this compound within our [[experience index]] include:
{{#ask: [[Category:Tianeptine]][[Category:Experience]]|format=ul|Columns=1}}
Additional experience reports can be found here:

*[https://www.erowid.org/experiences/subs/exp_Pharms_Tianeptine.shtml Erowid Experience Vaults: Tianeptine]

==Toxicity and harm potential==
{{toxicity}}
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). [https://www.google.com/ 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 [[responsible drug use|harm reduction practices]] when using this substance.

===Lethal dosage===
The [[LD50|LD<sub>50</sub>]] of tianeptine has not yet officially been established; however, it seems to have a [[Toxicity::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.<ref>{{cite journal | vauthors=((Proença, P.)), ((Teixeira, H.)), ((Pinheiro, J.)), ((Monsanto, P. V.)), ((Vieira, D. N.)) | journal=Forensic Science International | title=Fatal intoxication with tianeptine (Stablon®) | volume=170 | issue=2–3 | pages=200–203 | date= August 2007 | url=https://linkinghub.elsevier.com/retrieve/pii/S0379073807005683 | issn=03790738 | doi=10.1016/j.forsciint.2007.03.035}}</ref> 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 [[Addiction potential::mildly addictive]] and is capable of causing both physical and psychological dependence. When physical dependence has developed, [[Opioids#Discontinuation|withdrawal symptoms]] may occur if a person suddenly stops their usage.

Tolerance to many of the effects of tianeptine develops [[Time to full tolerance::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 [[Time to half tolerance::3 - 7 days]] for the tolerance to be reduced to half and [[Time to zero tolerance::1 - 2 weeks]] to be back at baseline (in the absence of further consumption). This compound may share a cross tolerance with other [[Cross-tolerance::[[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 [[opiate|opiates]].<ref>{{cite journal | vauthors=((Gassaway, M. M.)), ((Rives, M.-L.)), ((Kruegel, A. C.)), ((Javitch, J. A.)), ((Sames, D.)) | journal=Translational Psychiatry | title=The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist | volume=4 | issue=7 | pages=e411–e411 | date= July 2014 | url=https://www.nature.com/articles/tp201430 | issn=2158-3188 | doi=10.1038/tp.2014.30}}</ref> However, as with most people looking to discontinue their antidepressant medications (both [[SSRI]]s and [[TCA]]s), 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==
{{LegalStub}}
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.<ref>{{Citation | title=AMVV - Verordnung über die Verschreibungspflicht von Arzneimitteln | url=https://www.gesetze-im-internet.de/amvv/BJNR363210005.html}}</ref>
*'''Russia:''' In Russia, since 2010, tianeptine is a Schedule III controlled substance.<ref>{{Citation | title=Resolution of the Government of the Russian Federation от 30.06.2010 N 486 | url=https://www.consultant.ru/cons/cgi/online.cgi?req=doc&base=LAW&n=136223&fld=134&dst=100001,0&rnd=0.12167570485188983#017679654459079552}}</ref>
*'''Sweden''': Tianeptine is not an approved prescription medicine, and is therefore a controlled substance.<ref>https://www.lakemedelsverket.se/sv/sok-lakemedelsfakta/substans?id=E4POFBUAVAHVERT1</ref>
*'''Switzerland''': Tianeptine is not controlled under Buchstabe A, B, C and D. It could be considered legal.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref>
*'''Turkey''': Tianeptine is a 'green prescription' only substance<ref>https://www.titck.gov.tr/dinamikmodul/43</ref> and illegal when sold or possessed without a prescription.
*'''United Kingdom:''' Tianeptine is illegal to produce, supply, or import under the Psychoactive Substance Act, which came into effect on May 26th, 2016.<ref>{{Citation | title=Psychoactive Substances Act 2016 | url=https://www.legislation.gov.uk/ukpga/2016/2/contents/enacted}}</ref>
*'''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.<ref>{{Citation | vauthors=PutItOnaTshirt | year=2016 | title=Powder City has discontinued the selling of Tianeptine | url=https://www.reddit.com/r/Nootropics/comments/4a1oq2/powder_city_has_discontinued_the_selling_of/}}</ref> 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.<ref>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</ref>

==See also==

*[[Responsible use]]
*[[Opioid]]

==External links==

*[http://en.wikipedia.org/wiki/Tianeptine Tianeptine (Wikipedia)]
*[https://isomerdesign.com/PiHKAL/explore.php?id=3241 Tianeptine (Isomer Design)]

==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==
{{reflist|2}}
[[Category:Psychoactive substance]]
[[Category:Dibenzothiazepine]]
[[Category:Nootropic]]
[[Category:Opioid]]
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Tianeptine - Revision history

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