Tianeptine Sulfate (Sulphate) or Tianeptine Hemisulfate Monohydrate is modern pseudo-analogue of the famous Tianeptine Sodium. Tianeptine Sulfate was first mentioned in October 2009 with US patent number 8198268 B2 – pioneered by Hector Guzman at Janssen Biotech inc. This patent describes, in detail, “a novel sulfate salt of tianeptine with improved properties, more particularly tianeptine hemisulfate monohydrate”.
One key paragraph of this patent, mentions the following:
“The present invention relates to a novel sulfate salt of tianeptine, particularly tianeptine hemisulfate monohydrate, with improved properties. Such improved properties can include, but are not limited to, hygroscopicity, physical stability, and solubility. The invention also provides novel pharmaceutical compositions comprising tianeptine sulfate salt, methods of making tianeptine sulfate salt, and related methods of treatment. For example, tianeptine hemisulfate monohydrate provides an alternative in a pharmaceutical composition to the currently marketed form, tianeptine sodium”.
In short – Tianeptine Sulfate seems to have a similar predicted pharmacological profile to its close relative Tianeptine Sodium, but with different Pharmacodynamics and pharmacokinetics. However, it is claimed to have a slower release rate, with the patent information stating “
However, it is claimed to have a slower release rate, with the patent information stating “compared to the tablets containing tianeptine sodium salt, tablets prepared with the sodium salt release faster, especially during early dissolution times…. formulations based on the hemisulfate monohydrate salt result in much more steady release rates throughout the duration of the dissolution experiment than those for formulations based on the sodium salt”.
This means that Tianeptine Sulfate is able to act as a slow release form of Tianeptine Sodium, with a longer predicted half-life.
Stability – Another major difference is the solubility and stability, with Tianeptine Sulfate described as being much less soluble, subsequently being much less hygroscopic than Tianeptine Sodium. This interesting property has meant that the relative stability of Tianeptine Sulfate in normal conditions is better, with less light sensitivity and an improved general physical stability.
Duration – Tianeptine Sulfate is thought to be absorbed and excreted and a much slower rate than Tianeptine Sodium – however, this information is based on hypothesized patent information and anecdotal user reports. This means that theoretically, if approved, Tianeptine Sulfate would require a less frequent dosing regime of maybe 1 dose per day, instead of the 3 times a day indicated for Tianeptine Sodium.
Tianeptine Sulfate vs Sodium
Click here to see why Tianeptine Sodium is such a unique compound when compared to other drugs used to treat similar symptoms.
Tianeptine Sulfate is a neo-analogue of Tianeptine Sodium, as such, it has different chemicals properties and composition. The official patent for Tianeptine Sulfate describes it as a “novel sulphate salt” with “improved properties” over Tianeptine Sodium, including, but not limited to “hygroscopicity, physical stability, and solubility”.
Tianeptine Sodium is extremely hygroscopic, meaning it readily absorbs water from the atmosphere, rapidly increasing its viscosity as it dissolves with water from the air and becomes thicker in consistency. Notoriously, this has meant that the storage of Tianeptine Sodium requires desiccants (such as Silica Sachets) to reduce humidity.
Tianeptine Sulfate is not hygroscopic, allowing for easier storage. However, Tianeptine Sulfate cannot be dissolved in water-based solutions if required.
Tianeptine Sodium (in its pure form) is light sensitive, and may degrade when exposed to light. Tianeptine Sulfate, however, seems to be more light stable, but this is based on predicted chemical properties and anecdotal reports.
Due to Tianeptine Sulfate’s lack of solubility in water, it is predicted to be absorbed and excreted (in vivo) at a considerably slower rate, when compared with Tianeptine Sodium. This is backed by information within the US patent explaining how Tianeptine Sulfate provides an “alternative in a pharmaceutical composition to the currently marketed form, tianeptine sodium’.
Most importantly, the Sulfate form of Tianeptine, due to its differing solubility, is predicted to be absorbed and excreted (in vivo) at a much slower rate. When compared with the relatively short half-life of Tianeptine Sodium (2.5-3 hours), the Sulfate version would act like an extended release formulation. With the patent stating “formulations based on the hemisulfate monohydrate salt result in much more steady release rates throughout the duration of the dissolution experiment than those for formulations based on the sodium salt”.
Tianeptine Sulfate Unapproved Uses
As the patent is currently still ongoing, and Tianeptine Sulfate remains unapproved and unregulated – there are no official approved uses for this compound.
It is recommended to read Tianeptine Sodium’s Uses.
As the actual physiological and psychological properties of Tianeptine Sulfate are predicted to match those of Tianeptine Sodium, the only main difference in usage is attributed to its differing storage, stability, duration and excretion.
Tianeptine Sulfate Approval
Tianeptine Sulfate has not been officially approved anywhere in the world. Although a patent exists, indicating the potential use of Tianeptine Sulfate for similar indications, there does not seem to be any further official progress with this compound.
For full details on the politics and financial pressures surround Tianeptine’s approval, please read this.
Tianeptine Sulfate Mechanism Of Action.
Much like Tianeptine Sodium’s mechanism of action, the Sulfate version is predicted to have a similar profile. However, pharmacokinetics (how your body processes a drug) and pharmacodynamics (how a drug affects the body) definitely differ .
Tianeptine Sulfate is thought to act in the same way as Tianeptine Sodium, with regards to its alleviation of symptoms associated with Tianeptine Sodiums approved and unapproved indicated uses.
For more information on how Tianeptine Sulfate differs from Tianeptine Sodium, please view our Sodium vs Sulfate.
Tianeptine Sulfate Unofficial Dosage
There’s no official information on the in vivo therapeutic dosage of Tianeptine Sulfate. Tianeptine Sulfate does not have sufficient human pharmacodynamics data to accurately describe an in vivo dosage .
However, based on user reports, predicted chemical analysis and anecdotal information, there seems to be a loose consensus that approximately 3.5 times the amount of Tianeptine Sulfate is required to reach the same blood concentrations as an equivalent amount of Tianeptine Sodium. This hypothesized dose, may also be attributed to the molar mass of Tianeptine Sulfate being (98g/mol) or approximately 4.5 times that of Tianeptine Sodium (22g/mol).
Importantly, due to the longer duration of the Sulfate form, only one dose would be required per day, unlike the indicated 3 doses per day for the Sodium form.
Therefore, a single dose of 40mg Tianeptine Sulfate could be equivalent to 12.5mg of Tianeptine Sodium. However, some sources have indicated that the Tianeptine Sulfate dosage is approximately double that of Tianeptine Sodium, meaning only 25mg of Tianeptine Sulfate would equal 12.5mg of Tianeptine Sodium.
Tianeptine Sulfate Precautions
There are no official precautions to be observed for Tianeptine Sulfate. However, due to its similarity to Tianeptine Sodium, it’s strongly advised to follow the same precautions for Tianeptine Sodium.
Tianeptine Sulfate Storage Instructions
Unlike Tianeptine Sodium, the Sulfate form is not hygroscopic or light sensitive. However, as with most chemicals, storage should be within an airtight container, away from direct sunlight.
12. Charles Malen, Bernard Danrée, Jean-Claude Poignant. Nouveaux dérivés tricycliques et leur procédé de préparation. French Patent FR 2104728, 7 September 1971.
15. Tianeptine Sodium.Martindale: The Complete Drug Reference(London, UK: Pharmaceutical Press). 5 December 2011. Retrieved2 December 2013.
21. “The etiology of depression and the therapeutic implications” (https://www.worldcat.org/issn/2249-4618)
26. http://www.controlled-trials.com/ISRCTN16400909/ (“ISRCTN16400909 – Tianeptine for the treatment of fibromyalgia: a prospective double-blind, randomised, single-centre, placebo-controlled, parallel group study”