Tianeptine

Tianeptine
Molecular structure of Tianeptine
Chemical Nomenclature
Common names	Tianeptine
Substitutive name	Stablon, Coaxil, Tatinol
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
Oral Dosage WARNING: The dosages listed here are for the sodium salt version of tianteptine which is the most common form. Tianeptine sodium is usually taken in three separate doses spaced through the day. The numbers listed here are the amount of a single dose. Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. 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 20 - 60 minutes Peak 1 hour

Summary sheet: Tianeptine

Tianeptine (trade names Stablon and Coaxil) is a drug most commonly used for the treatment of clinical depression, although it is sometimes used to treat irritable bowel syndrome or asthma. In terms of chemical classification, tianeptine is a tricyclic antidepressant (TCA). However, its pharmacology and effects vary from those of typical antidepressant and anxiolytics, 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.

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

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

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

Chemistry

Tianeptine's structure compared to more typical TCAs. Note that tianeptine possesses quite a few more functional groups than the others, contributing to its uniqueness.

In terms of molecular structure and 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 fairly 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, due to the fact that 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. 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. 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.

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 labelled 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.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

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.

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 hallucinations - 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.

Toxicity and harm potential

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 from people within the nootropics community who have tried tianeptine 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 worth noting, however, that as this compound is a commonly prescribed prescription medication, it is considerably less likely to have adverse health effects than that of a research chemical.

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

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's worth nothing that because of tianeptine's short duration of effects, it may compel some to continual 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.

Legal issues

This legality section is a stub. As such, it likely contains incomplete or wrong information. You can help by expanding it.

Tianeptine is available in many European, Asian, and South American countries only by prescription and distributed under brand names such as Stablon and Coaxil. It is currently an unscheduled substance in the United States and can be found on many nootropic vendor websites.

• United Kingdom - This drug is illegal under the Psychoactive Substance Act, which came into effect on May 26th, 2016.

See also

• Responsible use
• Nootropics
• Anxiety suppression

External links

• Tianeptine (Wikipedia)
• Tianeptine (TripSit)
• Tianeptine: a review of its use in depressive disorders (NCBI)
• Tianeptine experiences (Erowid)