tianeptine tianeptine tianeptine, sold under the brand names stablon, tatinol, and coaxil among others, is an atypical tricyclic antidepressant which is used mainly in the treatment of major depressive disorder, although it may also be used to treat anxiety, asthma, and irritable bowel syndrome. tianeptineclinical datatrade namesstablon, coaxil, othersother namess-1574; jnj-39823277; tpi-1062ahfs/drugs.cominternational drug namesroutes ofadministrationby mouthatc coden06ax14 (who) legal statuslegal status in general: rx-onlyus: unapproved "new drug" (as defined by 21 u.s. code § 321(p)(1)). use in dietary supplements, food, or medicine is unlawful; otherwise uncontrolled. au: s4others: controlled in fr, bh, sg) pharmacokinetic databioavailability99%protein binding95%metabolismhepatic by β-oxidationelimination half-life2.5–3 hours4–9 hours (elderly)excretionurine: 65%feces: 15%identifiers iupac name 7-benzothiazepin-11-yl)amino]heptanoic acid cas number72797-41-2 y 30123-17-2 (sodium)1224690-84-9 (sulfate) 2231739-19-6 (hemioxalate)pubchem cid68870iuphar/bps7558chemspider62102 yunii0t493yfu8okeggd02575 ychebichebi:91749chemblchembl1289110 ncomptox dashboard (epa)dtxsid7048295 echa infocard100.131.750 100.069.844, 100.131.750 chemical and physical dataformulac21h25cln2o4smolar mass436.95 g·mol−13d model (jsmol)interactive image smiles clc1cc2c(cc1)c(c3c(n(c)s2(=o)=o)cccc3)nccccccc(=o)o inchi inchi=1s/c21h24cln2nao4s/c1-24-18-9-6-5-8-16(18)21(23-13-7-3-2-4-10-20(25)26)17-12-11-15(22)14-19(17)29(24,27)28/h5-6,8-9,11-12,14,21,23h,2-4,7,10,13h2,1h3,(h,25,26) ykey:jicjbgpomzqubb-uhfffaoysa-n y ny (what is this?) (verify) tianeptine has antidepressant and anxiolytic effects with a relative lack of sedative, anticholinergic, and cardiovascular side effects. it has been found to act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. this may explain part of its antidepressant and anxiolytic effects, however, it is thought that tianeptine also modulates glutamate receptors, and this may also explain tianeptine’s antidepressant/anxiolytic effects. 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, or the united kingdom. medical uses depression and anxiety 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. a 2005 study in egypt showed tianeptine to be effective in men with depression and erectile dysfunction. tianeptine has been found to be effective in depression, in people with parkinson's disease, and with post-traumatic stress disorder for which it was as safe and effective as fluoxetine and moclobemide. other uses a clinical trial comparing its efficacy and tolerability with amitriptyline in the treatment of irritable bowel syndrome showed that tianeptine was at least as effective as amitriptyline and produced fewer 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 who 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 an under-25,000 person open-label study lasting over seven years, both showing effectiveness. 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. tianeptine has been shown to have efficacy with minimal side effects in the treatment of attention-deficit hyperactivity disorder. contraindications known contraindications include the following: hypersensitivity to tianeptine or any of the tablet's excipients. side effects compared to other tricyclic antidepressants, it produces significantly fewer cardiovascular, anticholinergic (like dry mouth or constipation), sedative and appetite-stimulating effects. a recent review found that it was amongst the antidepressants most prone to causing hepatotoxicity (liver damage), although the evidence to support this concern was of limited quality. unlike other tricyclic antidepressants, tianeptine does not affect heart function. μ-opioid receptor agonists can sometimes induce euphoria, as does tianeptine, occasionally, at high doses, well above the normal therapeutic range. tianeptine can also cause severe withdrawal symptoms after prolonged use at high doses which should prompt extreme caution. by frequency sources: common (>1% frequency) headache (up to 18%) dizziness (up to 10%) insomnia/nightmares (up to 20%) drowsiness (up to 10%) dry mouth (up to 20%) constipation (up to 15%) nausea abdominal pain weight gain (~3%) agitation anxiety/irritability uncommon (0.1-1% frequency) bitter taste flatulence gastralgia blurred vision muscle aches premature ventricular contractions micturition disturbances palpitations orthostatic hypotension hot flushes tremor rare (<0.1% frequency) hepatitis hypomania euphoria ecg changes pruritus/allergic-type skin reactions protracted muscle aches general fatigue pharmacology pharmacodynamics