Tianeptine

Summary sheet: Tianeptine

Tianeptine
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 system.

While tianeptine is classified as a tricyclic antidepressant (TCA), its pharmacological effects differ from those of typical antidepressants. 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. 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.

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

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. 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. Despite tianeptine's chemical similarity to other TCAs, its effects and mechanisms are unique.

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.

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. 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.

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

It is also sometimes used to treat irritable bowel syndrome or asthma.

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

• • Stimulation
  • 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.
  • Bronchodilation - Tianeptine increases the reuptake of serotonin, which has been found to combat bronchoconstriction.
  • Muscle relaxation
  • Headaches
  • Dizziness
  • Constipation
  • Physical fatigue

Visual effects

• • 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 imagery. This is often accompanied by ill-defined geometry.

Cognitive effects

• • Motivation enhancement
  • Anxiety suppression - Tianeptine has been found to be especially useful in mitigating the effects of panic attacks.
  • 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.
  • 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.
  • Thought acceleration or Thought deceleration
  • Rejuvenation
  • 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:

Additional experience reports can be found here:

• Erowid Experience Vaults: Tianeptine

Toxicity and harm potential

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. 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. 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

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.
• Germany: Tianeptine is a prescription medicine, according to Anlage 1 AMVV.
• Russia: In Russia, since 2010, tianeptine is a Schedule III controlled substance.
• Sweden: Tianeptine is not an approved prescription medicine, and is therefore a controlled substance.
• Switzerland: Tianeptine is not controlled under Buchstabe A, B, C and D. It could be considered legal.
• United Kingdom: Tianeptine is illegal to produce, supply, or import under the Psychoactive Substance Act, which came into effect on May 26th, 2016.
• 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. 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.

See also

• Responsible use
• Opioid

External links

• Tianeptine (Wikipedia)
• 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