Tianeptine chemical structure
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Tianeptine

Tianeptine (INN) (Stablon®, Coaxil®, Tatinol®), is structurally similar to the tricyclic antidepressants. Unlike the tricyclics, however, it enhances the reuptake of serotonin instead of blocking it. No data is available regarding effects of the drug on postsynaptic receptors. more...

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Tianeptine has strong antidepressant and anxiolytic properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, making it particular suitable for use in elderly patients and in those following alcohol withdrawal as these patients are known to be more sensitive to the adverse effects of psychotropic drugs.

Currently, tianeptine is approved in France. The manufacturer there is Servier. It is also marketed to a host of countries in Europe, Asia and Latin America.

Uses

Approved

Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with fewer side effects. It was even more effective than maprotiline in a group of patients with coexisting depression and anxiety. Tianeptine also displays significant anxiolytic properties and is useful in treating a spectrum of anxiety disorders including panic disorder, as evidenced by a study in which those administered 35% CO2 gas on paroxetine (Paxil) or tianeptine (Stablon) therapy showed equivalent panic-blocking effects.

Investigational/Off-Label/Unapproved

Tianeptine has been reported to be very effective for asthma starting in August of 1998, when Dr. Fuad Lechin and colleagues at the Central University of Venezuela Institute of Experimental Medicine in Caracas published the results of a 52-week randomized controlled trial of asthmatic children; the children in the groups that received tianeptine had a sharp decrease in clinical rating and increased lung function. Two years ealier, they had found a close, positive association between free serotonin in plasma and severity of asthma in symptomatic patients. As tianeptine was the only agent known to reduce both free serotonin in plasma and enhance uptake in platelets, they decided to use it to see if reducing free serotonin levels in plasma would help. By November of 2004, there had been two double-blind placebo-controlled crossover trials, and a 25,000+ patient open-lable study lasting over seven years, all showing effectiveness.

A 2005 study in Egypt demonstrated tianeptine to be effective in men with depression and erectile dysfunction.

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Anti-depressant found to stop brain shrinkage
From Milwaukee Journal Sentinel, The, 10/2/01 by LAURAN NEERGAARD

Anti-depressant found to stop brain shrinkage

By LAURAN NEERGAARD

Associated Press

Tuesday, October 2, 2001

Washington -- Major depression makes an important part of the brain actually shrink. Stress seems to be a suspect, but no one knows how to stop or reverse the atrophy.

Now a new study of primates' brains says a European anti- depressant seems to counter the shrinkage -- raising calls for more research to see whether other medications might help people, too.

"These are impressive and important findings," said Robert Sapolsky of Stanford University, who reviewed the new research, published in today's Proceedings of the National Academy of Sciences.

But, "mind you, this is one anti-depressant and this is a fairly atypical one" compared with the anti-depressants most Americans use, Sapolsky cautioned.

German researchers tested a new anti-depressant sold only in Europe called tianeptine. The anti-depressants most popular in the United States -- Prozac and similar medications -- work by blocking the dissipation of a neurotransmitter called serotonin that is important for mood. Tianeptine does exactly the opposite, enhancing serotonin uptake.

Major, long-term depression can cause a brain region called the hippocampus to shrink, in some cases nearly 20%. The hippocampus is important for learning and memory, so that probably explains why memory loss often accompanies depression. And the region doesn't seem to bounce back after the depression is cured.

Nobody knows exactly why this atrophy occurs: Neurons may die or shrink, or ones that should have been born to replenish the region may not be. Whichever, it does seem linked to a stress hormone called cortisol, because about half of seriously depressed patients secrete too much cortisol.

To see if tianeptine could help, neurobiologist Eberhard Fuchs and colleagues at the German Primate Center tested tree shrews, which exhibit a classic model for human depression when exposed to social stress.

Over the 35-day study period, depressed shrews experienced excess cortisol, decreased amounts of brain chemicals important for healthy cells, a 33% decrease in new cell growth and a 7% decline in hippocampal volume. But shrews that were given oral tianeptine saw their brain chemical concentrations return to normal, cell growth restart and the hippocampus return to its pre-depression size.

"This increase produced by tianeptine suggests that hippocampal volume loss in depressed humans could possibly be prevented by anti- depressants," Fuchs concluded.

Copyright 2001 Journal Sentinel Inc. Note: This notice does not apply to those news items already copyrighted and received through wire services or other media
Provided by ProQuest Information and Learning Company. All rights Reserved.

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