Description

Tianeptine Sodium

There are three forms of Tianeptine on the market. They are Tianeptine Sodium Salt, Tianeptine Acid and Tianeptine Sulphate.

A considerable proportion of drugs are organic acid or alkali salt which increases water solubility and is beneficial to the preparation of some water-containing dosage forms, such as water injection and oral liquid. A simple understanding is – a salt form will increase the substance water solubility and absorbency.

Tianeptine it is very hygroscopic. This makes handling and storage a pain. More importantly, its short half life and pharmacodynamic properties make dosing required up to 3 times a day. This is where a more controlled release form comes into play. The salt form has improved the stability, the free acid form is the next outcome from Tianeptine sodium salt.

Tianeptine Hemisulphate Mono-hydrate is an improved salt of Tianeptine. It is not hygroscopic so handling the powder is a lot easier. Since it is not as readily absorbed and excreted from the body, the sulphate salt allows for a more controlled release of the Tianeptine over longer periods. Rather than having to dose three times with rapid peak effects and rapidly falling effects, the sulphate salt allows for one dose to maintain plasma levels in the body much longer than the sodium salt. These improved characteristics make Tianeptine Sulphate a novel addition.

As for the half-life of the three forms, Sodium is the shortest lasting, then comes free acid, and then sulphate. Free acid and sulphate are better suited for a taper because of their slow ramp up and slow ramp down, in addition to lasting quite a bit longer than sodium. Free acid and sulphate really shine at night by letting you sleep through the whole night without waking up in WD’s and having to dose.

Uses and Effects

Tianeptine is proven effective in the following conditions:

– Depression
– Asthma
– IBS
– Various Anxiety Disorders
– Alcohol Withdrawal
– Anticonvulsant
– Analgesic (Pain Killing)
– Depression-induced Cognitive Dysfunction
– Depression in Parkinson’s disease
– PTSD
– Erectile dysfunction
– ADHD
– Neuroprotective
– Prevents hippocampal remodelling from stress

Unapproved or Reported – “off-label” Uses and Effects

– Increased Subjective Motivation
– Anxiolitic (Anti-anxiety)
– Euphoria
– General Nootropic Benefits
– Improved Ability to Focus
– Improved Reaction Time
– Learning and Short-term Memory Retention

Tianeptine’s Mechanism of Action

Like many approved drugs, Tianeptine’s complete mechanism remains elusive to science, and only the best theories are put forward in the literature as best fit models.

Tianeptine is a tricyclic antidepressant (TCA). Usually, TCA’s act by increasing the cerebral levels of serotonin and norepinephrine, via an SNRI mechanism.

Initial studies found that Tianeptine helped alleviate depressive symptoms by decreasing extracellular level of serotonin, rather than increasing the release of serotonin, like other established antidepressants such as TCA’s and SSRI’s.

Therefore, Tianeptine was initially identified as one of the world’s first Selective Serotonin Re-uptake Enhancers (SRE or SSRE). However, upon further investigation, it was found that Tianeptine did not interact with the serotonin monoamine, nor did it alter extracellular levels of Serotonin in long-term studies.

Research Dosage

Based on the official product insert provided by Servier for Stablon branded Tianeptine, the following recommended dosage has been described.

1 tablet (12.5mg) 3 times a day (morning, mid-day and evening) before the main meals of the day.

This dosage has been indicated by Servier to be applicable to the following indications:

Neurotic and reactive depression. Anxiodepressive states with psychosomatic manifestations, especially gastrointestinal. Anxiodepressive States in alcoholics during withdrawal stage.

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