Tianeptine - A review of its use in depressive disorders

Tianeptine is an antidepressant agent with a novel neurochemical profile. I t increases serotonin (5-hydroxytryptamine: 5-HT) uptake in the brain tin c ontrast with most antidepressant agents) and reduces stress-induced atrophy of neuronal dendrites. Like the selective serotonin reuptake inhibitors (S SRIs) and in contrast with most tricyclic antidepressant agents, tianeptine does not appear to be associated with adverse cognitive, psychomotor, slee p, cardiovascular or bodyweight effects and has a low propensity for abuse. Tianeptine has a comparatively favourable pharmacokinetic profile. It is no t subject to first-pass hepatic metabolism. has high bioavailability and li mited distribution, and is rapidly eliminated. While this offers advantages for tianeptine over the tricyclic antidepressant agents in terms of dose t itration, treatment changes and potential drug interactions, its rapid elim ination makes adherence to dosage schedules more important. Tianeptine diff ers from most antidepressants in that it is not primarily metabolised by th e hepatic cytochrome P450 system, indicating less likelihood of drug-drug i nteractions: this is of particular interest for elderly patients. Tianeptine. in dosages of 25 to 50 mg/day, has been investigated in patient s with major depression, depressed bipolar disorder, dysthymia or adjustmen t disorder. It has equivalent antidepressant efficacy to several classical antidepressant agents (amitriptyline, clomipramine, imipramine, mianserin) and the SSRIs fluoxetine tin most patients), paroxetine and sertraline. Com parison with maprotiline indicated superior efficacy for tianeptine but dot hiepin appeared superior in another study, Extended treatment with tianepti ne decreases the incidence of relapse/ recurrence of depression. Tianeptine appears to be as effective as fluoxetine, sertraline, amitriptyl ine, clomipramine and mianserin and more effective than maprotiline in impr oving associated anxiety in patients with depressive disorders. Depression and anxiety symptoms in alcohol dependant patients also respond well to tia neptine. The adverse effects associated with tianeptine are similar in many respects to those of the SSRIs and minimal in comparison with the tricyclic antidep ressants. The most common adverse effects are nausea, constipation, abdomin al pain, headache, dizziness and changes in dreaming. Anticholinergic effec ts occur less often with tianeptine than with tricyclic agents. Hepatoxicit y is rare. The dosage should be decreased in elderly patients and those wit h severe renal failure, but adjustment is not necessary in patients with al coholism or hepatic impairment, or those undergoing haemodialysis. Conclusions: The antidepressant efficacy and favourable tolerability and ph armacokinetic profiles of tianeptine in patients with depression, including those with associated anxiety, have been proven: the data indicate that it may have additional potential in specific subgroups of depressed patients such as the elderly and those with chronic alcoholism.