View Full Version : My experience with Tianeptine


Darksanity
05-15-13, 02:57 AM
So basically I've trialed tianeptine twice and so will leave some 'review' of it.

Intro to Tianeptine:

Tianeptine is labeled a selective serotonin reuptake enhancer (SSRE), technically opposite to the action of "SSRIs". :eyebrow: In practice in doesn't literally result in the opposite effect of SSRIs though. :scratch:

Interesting studies on tianeptine:

Neuropharmacology. 1992 Mar;31(3):221-7.
Tianeptine increases the extracellular concentrations of dopamine in the nucleus accumbens by a serotonin-independent mechanism.
Invernizzi R, Pozzi L, Garattini S, Samanin R.
Source
Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.
Abstract
The effect of various doses of tianeptine on the extracellular concentrations of dopamine was studied in the striatum and nucleus accumbens of the rat. At 5 (but not 2.5) mg/kg intraperitoneally, tianeptine increased the extracellular dopamine only in the nucleus accumbens. At 10 mg/kg, the effect was also seen in the striatum but it was less marked and shorter-lasting. At 10 mg/kg (i.p.), tianeptine significantly raised the extracellular concentrations of dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in both regions. The effect of 10 mg/kg tianeptine on dopamine and its metabolites was not significantly changed in animals which had received this dose twice daily for 15 days. Intracerebroventricular administration of 150 micrograms/20 microliters 5,7-dihydroxytryptamine, which markedly depleted serotonin in the brain, did not modify the effect of 10 mg/kg tianeptine on the extracellular concentrations of dopamine and HVA in the nucleus accumbens but reduced the effect on DOPAC. Various doses of tianeptine (1, 3 and 10 mg/kg i.p.) did not change the synthesis of serotonin and dopamine in the striatum and nucleus accumbens. The results show that tianeptine increased the extracellular concentrations of dopamine more in the nucleus accumbens than in striatum. The effect on the output of DA in the nucleus accumbens could be involved in the antidepressant activity of tianeptine.
PMID: 1630590 [PubMed - indexed for MEDLINE]

Effect of repeated treatment with tianeptine and fluoxetine
on central dopamine D(2) /D(3) receptors
by
Dziedzicka-Wasylewska M, Rogoz Z, Skuza G, Dlaboga D, Maj J.
Institute of Pharmacology,
Polish Academy of Sciences,
Krakow, Poland.
wasyl@if-pan.krakow.pl
Behav Pharmacol. 2002 Mar;13(2):127-38.

ABSTRACT

Tianeptine (TIA) is an antidepressant drug that has been shown to decrease extracellular serotonin level and reveals no affinity for neurotransmitter receptors. The present study was aimed at determining whether repeated TIA treatment induced any adaptive changes in the central dopamine D(2)/D(3) system (behavioural and biochemical) similar to those reported earlier for tricyclic antidepressants. Experiments were carried out on male Wistar rats. TIA was administered at a dose of 5 and 10 mg/kg once or repeatedly (twice daily for 14 days). Fluoxetine (FLU), used as a reference compound, was also administered at a dose of 10 mg/kg. The results obtained showed that TIA or FLU administered repeatedly increased the hyperlocomotion induced by D-amphetamine and 7-hydroxy-dipropylaminotetralin (7-OH-DPAT). Biochemical study revealed a decrease in the [(3)H]7-OH-DPAT binding sites after acute and repeated treatment with TIA or FLU in the islands of Calleja minor, as well as in the shell part of nucleus accumbens septi. On the other hand, both TIA and FLU administered repeatedly increased the binding of [(3)H]quinpirole (a D(2)/D(3) receptor agonist) in the nucleus caudatus as well as in the core part of the nucleus accumbens septi. Similar effects have been observed when dopamine D(2)/D(3) receptors were visualized with the use of [3H]raclopride, a dopamine D(2)/D(3) receptor antagonist. However, TIA and FLU induced a decrease in the level of mRNA encoding for dopamine D(2) receptors, not only after repeated but also after acute treatment. These results indicate that repeated TIA and FLU administration induces adaptive changes in the dopaminergic D(2)/D(3) system and especially enhances the functional responsiveness of dopamine D(2) and D(3) receptors. However, the question of whether this increased responsiveness is important for clinical antidepressant efficacy remains open.

Mol Psychiatry. Author manuscript; available in PMC 2010 September 1.
Published in final edited form as:
Mol Psychiatry. 2010 March; 15(3): 237–249.
Published online 2009 August 25. doi: 10.1038/mp.2009.80
PMCID: PMC2902200
NIHMSID: NIHMS201077
The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation
Bruce S. McEwen, Sumantra Chattarji, David M. Diamond, Thérèse M. Jay, Lawrence P. Reagan, Per Svenningsson, and Eberhard Fuchs
The publisher's final edited version of this article is available at Mol Psychiatry

Abstract
Tianeptine is a clinically used antidepressant that has drawn much attention, because this compound challenges traditional monoaminergic hypotheses of depression. It is now acknowledged that the antidepressant actions of tianeptine, together with its remarkable clinical tolerance, can be attributed to its particular neurobiological properties. The involvement of glutamate in the mechanism of action of the antidepressant tianeptine is consistent with a well-developed preclinical literature demonstrating the key role of glutamate in the mechanism of altered neuroplasticity that underlies the symptoms of depression. This article reviews the latest evidence on tianeptine’s mechanism of action with a focus on the glutamatergic system which could provide a key pathway for its antidepressant action. Converging lines of evidences demonstrate actions of tianeptine on the glutamatergic system, and therefore offer new insights into how tianeptine may be useful in the treatment of depressive disorders.

CNS Drugs. 2008;22(1):15-26.
Neurobiological and clinical effects of the antidepressant tianeptine.
Kasper S, McEwen BS.
Source
Department of Psychiatry and Psychotherapy, Medical University of Vienna, Vienna, Austria. sci-biolpsy@meduniwien.ac.at
Abstract
The precise neurobiological processes involved in depression are not clear, but it is recognized that numerous factors are involved, including changes in neurotransmitter systems and brain plasticity. Neuroplasticity refers to the ability of the brain to adapt functionally and structurally to stimuli.
Impairment of neuroplasticity in the hippocampus, amygdala and cortex is hypothesized to be the mechanism by which cognitive function, learning, memory and emotions are altered in depression.
The mechanisms underlying alterations in neuroplasticity are believed to relate to changes in neurotransmitters, hormones and growth factors. Structural changes in the hippocampus that have been proposed to be associated with depression include dendritic atrophy, reduced levels of cerebral metabolites, decreased adult neurogenesis (generation of new nerve cells) and reduced volume.
Increased dendritic branching occurs in the basolateral nucleus of the amygdala. Reduced neuronal size and glial cell density occur in the prefrontal cortex. Clinically, tianeptine is an antidepressant effective in reducing symptoms of depression in mild to moderate-to-severe major depression, including over the long term. Tianeptine is also effective in alleviating the symptoms of depression-associated anxiety. It is generally well tolerated, with little sedation or cognitive impairment.
The efficacy profile of tianeptine could be explained by its neurobiological properties observed in animal models.
Tianeptine prevents or reverses stress-associated structural and cellular changes in the brain and normalizes disrupted glutamatergic neurotransmission. In particular, in the hippocampus, it prevents stress-induced dendritic atrophy, improves neurogenesis, reduces apoptosis and normalizes metabolite levels and hippocampal volume. Tianeptine also has beneficial effects in the amygdala and cortex and can reverse the effects of stress on neuronal and synaptic functioning. The neurobiological properties of tianeptine may provide an explanation not only for its antidepressant activity, but also for its anxiolytic effects in depressed patients and its lack of adverse effects on cognitive function and memory.

Darksanity
05-15-13, 03:47 AM
Honestly this looks like a perfect drug on paper. And from my experience it's the best antidepressant I've tried and also helps with ADHD with no noticeable side-effects. And yet, IT'S NOT APPROVED BOTH IN THE US AND CANADA. What a wonderful system we have! Where huge amount of red-tape and the enormous amount of money needed to get through the FDA or Health Canada makes 'Big Pharma' (the only ones with the means to get through) ignore any unpatentable drugs. The incestous relationship between regulators, doctors, and Big Pharma doesn't help either. Forget about about a relatively small company or NPO getting unpatentable drugs through the FDA or Health Canada). :doh:

Oups started going off-topic here, sorry couldn't resist. :D So yeah basically the only way to access tianeptine is ordering it from shady online pharmacies and it's quite pricey so as a long-term (if you're in North America) drug it's not so convenient.

Now more details about my experiences with tianeptine.

Basically tianeptine feels very 'clean', actually seems to improve mental clarity and cognition, and increases emotions while significantly reducing anxiety. This is quite unlike the mood-blunting effect of SSRIs that often leave you feeling dumb, apathetic, and emotion-less.

The 'increased emotions' effect was interesting in that it would increase empathy towards people. Also even while watching a movie I could feel emotions including sadness with more intensity. This is great for those of us who generally feel emotionally-blunted and SSRIs make things worst. ADHD medications also tend to cause emotional-blunting and tianeptine does reverses this. It made me feel more alive and human. :) SSRIs are a joke compared to tianeptine. tianeptine also actually can increase sex drive unlike SSRIs'.

On the other hand, I would NOT recommend tianeptine for those who tend to have large mood-swings daily or bipolar types.



Any questions? :D

sarahsweets
05-15-13, 04:14 AM
wow dark sanity that sounds really promising, makes you wonder why the us and canada are not doing more with it.