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Tianeptine (brand names Stablon, Coaxil, Tatinol, Tianeurax and Salymbra) is a drug used primarily in the treatment of major depressive disorder, although it may also be used to treat asthma or irritable bowel syndrome. Chemically it is a tricyclic antidepressant (TCA), but it has different pharmacological properties than typical TCAs as recent research suggests that tianeptine produces its antidepressant effects through indirect alteration of glutamate receptor activity (i.e., s and s) and release of , in turn affecting neural plasticity. Tianeptine has antidepressant and anxiolytic (anti-anxiety) properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, thus suggesting it is particularly suitable for use in the elderly and in those following alcohol withdrawal; such persons can be more sensitive to the adverse effects of psychotropic drugs.〔〔 Recent results indicate possible anticonvulsant (anti-seizure) and analgesic (painkilling) activity of tianeptine via immediate or downstream modulation of adenosine A1 receptors (as the effects could be experimentally blocked by antagonists of this receptor).〔 Tianeptine is a full agonist at the μ-opioid and δ-opioid receptors with negligible effect at the κ-opioid receptors.〔 Selective μ-opioid agonists typically induce euphoria, which may contribute to tianeptine's antidepressant effect. Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s. Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in a number of other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S.. ==Medical uses== Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with significantly fewer side effects. It was shown to be more effective than maprotiline in a group of people with co-existing 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 (carbogen) on paroxetine or tianeptine therapy showed equivalent panic-blocking effects. Like many antidepressants (including bupropion, the selective serotonin reuptake inhibitors, the serotonin-norepinephrine reuptake inhibitors, moclobemide and numerous others) it may also have a beneficial effect on cognition in people with depression-induced cognitive dysfunction. Tianeptine has been found to be effective in depression in Parkinson's disease and in post-traumatic stress disorder of which it was as safe and effective as fluoxetine and moclobemide. A clinical trial has been conducted to compare its efficacy and tolerability with amitriptyline in the treatment of irritable bowel syndrome. The results of this trial showed that tianeptine was at least as effective as amitriptyline and produced less prominent adverse effects such as dry mouth and constipation. Tianeptine has been reported to be very effective for asthma. In August 1998, 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 earlier, they had found a close, positive association between free serotonin in plasma and severity of asthma in symptomatic persons.〔 As tianeptine was the only agent known to both reduce 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 2004, there had been two double-blind placebo-controlled crossover trials and a >25,000 person open-label 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. Tianeptine also has anticonvulsant and analgesic effects, and a clinical trial in Spain that ended in January 2007 has shown that tianeptine is effective in treating pain due to fibromyalgia.〔(【引用サイトリンク】title=ISRCTN16400909 - Tianeptine for the treatment of fibromyalgia: a prospective double-blind, randomised, single-centre, placebo-controlled, parallel group study )〕 Tianeptine has been shown to have efficacy with minimal side effects in the treatment of attention-deficit hyperactivity disorder. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「tianeptine」の詳細全文を読む スポンサード リンク
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