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Tianeptine

Tianeptine2DACS.svg

Tianeptine Overview

Tianeptine is an atypical antidepressant.[1] It is a Selective Serotonin Reuptake Enhancer (SSRE) [2] and reduces the amount of serotonin in the synapse. Tianeptine is an effective anxiolytic and antidepressant, with significant applications for elderly patients and those with chronic alcoholism.[1] It also may promote neuronal growth as well as neuroplasticity through BDNF and NGF promotion.[3,4]

Other Names for Tianeptine

Stablon [3], Tianeptine Sodium [6], Coaxil [5], Tatinol, 30123-17-2, NCGC00167725-01, S-1574, sodium;7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoate [6]

Essential Information

Tianeptine is an atypical tricyclic antidepressant. It is structurally related to other TCAs, although instead of working as an SSRI it is an SSRE. It has neuroprotective effects and positive effects on NMDA and AMPA receptors. It also works on Opioid receptors. It is effective in treating anxiety, depression, ADHD, and increasing memory.

Structure

Tianeptine is a tricyclic antidepressant and structurally related to SSRIs[14].

Absorption

Tianeptine is absorbed well orally, with a 99%(+/-28%) bioavailability[8]. When taken with food, tianeptine absorption is delayed by half an hour, although it does not affect the total amount absorbed into plasma[7]. When co-administered with alcohol, oral administration is reduced[8].   Tianeptine has a plasma half life of 2.5 hours, and is excreted through the kidneys[8].

Benefits

  • Tianeptine reduces the atrophy of of neurons associated with stressful situations.[1,3]
  • Tianeptine is effective in treating anxiety.[2]
  • Tianeptine is effective in treating depression.[1]
  • Tianeptine helps restore normal neuroplasticity in stress-affected glutamate transmission.[3]
  • Tianeptine may promote BDNF and NGF.[3]
  • Tianeptine has shown to enhance memory.[9]
  • Tianeptine has significant neuroprotective effects[12].
  • Tianeptine when coadministered with morphine reduced morphine ancioceptive tolerance, and may have applications for patients with long term morphine use[12].
  • Tianeptine is effective in treating Parkinson’s Disease[15].
  • Tianeptine is effective in treating Post-Traumatic Stress Disorder[16].
  • Tianeptine is effective in treating Asthma[17].
  • Tianeptine is effective in treating Attention Deficit Hyperactivity Disorder[18].

Mechanism of Action

Tianeptine is a very interesting chemical. It has challenged the monoamine theory of depression. This theory was one of the major theories for how depression works, and states that monoamine neurotransmitters (serotonin, dopamine, and norepinephrine) deficiencies are responsible for mood disorders[3]. Tianeptine works on NMDA, AMPA, Serotonin, and Opioid receptor subtypes resulting in a complicated mechanism of action.

Tianeptine’s action on Serotonin

Tianeptine challenges the monoamine theory of depression, because it is an SSRE, which actually reduces the amount of serotonin available in the synapse, and has an opposite mechanism than that of SSRIs, which are the most commonly used drugs in the treatment of depression[3].   Based on this, it appears that Tianeptine’s antidepressant action isn’t due to its effects on serotonin. Further studies have examined its other effects, which I will break down below.

Tianeptine’s actions on Glutamate/NMDA/AMPA

Tianeptine helps to reduce stress-related effects on the brain’s glutamate system. Glutamate is one of the major excitatory neurotransmitters in the brain. Tianeptine helps to normalize glutamate levels and uptake in the amygdala, and it’s normalization of the glutamate system has been investigated as a major mechanism of action in its treatment of depression[8].   Tianeptine’s actions on Glutamate are expressed through both NMDA and AMPA receptor subtypes. These actions help to explain both Tianeptine’s antidepressant and memory enhancing effects[10].

Tianeptine’s actions at Opioid receptor sites

Tianeptine was recently discovered to be a full agonist at both mu and delta opioid receptor subtypes, with no action at kappa opioid subtypes. The actions at the mu and delta receptors may contribute to Tianeptine’s anti-anxiety and anti-depressant properties[11].

Tianeptine Safety and Side Effects

  • Tianeptine may reduce appetite.[2]
  • Tianeptine may contribute to sexual dysfunction, but less than SSRIs.[3]
  • Tianeptine may induce nausea, but less than SSRIs.[3]
  • Tianeptine, when administered in high doses in patients with a history of opiate abuse may have a high addiction potential[13].
  • Tianeptine overdose is associated with hepatotoxicity (liver toxicity)[14].

References

  1. http://www.ncbi.nlm.nih.gov/pubmed/11463130
  2. http://www.ncbi.nlm.nih.gov/pubmed/25154197
  3. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2902200/
  4. http://www.ncbi.nlm.nih.gov/pubmed/15177087
  5. http://www.ncbi.nlm.nih.gov/pubmed/16608107
  6. http://pubchem.ncbi.nlm.nih.gov/compound/Tianeptine_sodium
  7. http://www.ncbi.nlm.nih.gov/pubmed/3243929
  8. http://www.ncbi.nlm.nih.gov/pubmed/2341111
  9. http://www.ncbi.nlm.nih.gov/pubmed/12372016
  10. http://www.ncbi.nlm.nih.gov/pubmed/22358100
  11. http://www.ncbi.nlm.nih.gov/pubmed/25026323
  12. http://www.ncbi.nlm.nih.gov/pubmed/20679893
  13. http://www.ncbi.nlm.nih.gov/pubmed/19801742
  14. http://www.ncbi.nlm.nih.gov/pubmed/7890892
  15. http://www.ncbi.nlm.nih.gov/pubmed/17457538
  16. http://www.ncbi.nlm.nih.gov/pubmed/16329631
  17. http://www.ncbi.nlm.nih.gov/pubmed/15632955
  18. http://www.ncbi.nlm.nih.gov/pubmed/15034228