Tianeptine
Atypical antidepressant / From Wikipedia, the free encyclopedia
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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.[3][4][5]
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Trade names | Stablon, Coaxil, Tatinol |
Other names | Tia;[1] ZaZa;[2] S-1574;[3][4][5] JNJ-39823277; TPI-1062[6] |
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Routes of administration | By mouth |
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Bioavailability | 99%[9][10] |
Protein binding | 95%[10] |
Metabolism | Hepatic[10] by β-oxidation[11] |
Elimination half-life | 2.5–3 hours[9][10] 4–9 hours (elderly)[10][12] |
Excretion | Urine: 65%[9] Feces: 15%[10] |
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ECHA InfoCard | 100.131.750 100.069.844, 100.131.750 |
Chemical and physical data | |
Formula | C21H25ClN2O4S |
Molar mass | 436.95 g·mol−1 |
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Tianeptine has antidepressant and anxiolytic effects[13] with a relative lack of sedative, anticholinergic, and cardiovascular side effects.[10][14] 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.[15][16][17] 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.[18][19] In the US, it is an unregulated drug sold under several names and some of these products have been found to be adulterated with other recreational drugs.[20]