Tianeptine is a novel
antidepressant agent, both structurally (modified tricyclic) and in terms of its pharmacodynamic profile. Unlike other
antidepressant agents,
tianeptine stimulates the uptake of
serotonin (
5-hydroxytryptamine; 5-HT) in rat brain synaptosomes and rat and human platelets, increases 5-hydroxyindoleacetic
acid (5-HIAA) levels in cerebral tissue and plasma, and reduces serotonergic-induced behaviour.
Tianeptine reduces the hypothalamic-pituitary-adrenal response to stress, antagonises stress-induced behavioural deficits and prevents changes in cerebral morphology. The
antidepressant efficacy of
tianeptine, as shown in 2 trials of patients with major depression or depressed
bipolar disorder with or without
melancholia, is greater than that of placebo. In patients with major depression without
melancholia or psychotic features, depressed
bipolar disorder or
dysthymic disorder, the
antidepressant efficacy of short term (4 weeks to 3 months)
tianeptine therapy appears to be similar to that of
amitriptyline,
imipramine and
fluoxetine and may be superior to that of
maprotiline in patients with coexisting depression and anxiety. However, submaximal dosages of
amitriptyline and
maprotiline were used in these studies. Preliminary evidence suggests that
tianeptine may also be effective in patients with
endogenous depression. Progressive therapeutic improvements have been observed with up to 1 year of
tianeptine treatment, and long term
therapy may reduce the rate of relapse or recurrence.
Tianeptine is effective in the treatment of depression in elderly and post-alcohol-withdrawal patient subgroups.
Tianeptine was more effective in reducing psychic anxiety than placebo in patients with major depression or depressed
bipolar disorder with or without
melancholia. The overall
anxiolytic properties of
tianeptine in patients with coexisting depression and anxiety appear to be similar to those of
amitriptyline,
imipramine and
fluoxetine and may be superior to those of
maprotiline, although submaximal dosages of
amitriptyline and
maprotiline were used. Studies of
tianeptine in patients with primary anxiety have not been conducted.
Tianeptine is well tolerated in the short (3 months) and long (up to 1 year) term. The incidence of dry mouth (38 vs 20%),
constipation (19 vs 15%),
dizziness/
syncope (23 vs 13%), drowsiness (17 vs 10%) and
postural hypotension (8 vs 3%) are greater with
amitriptyline than with
tianeptine.
Insomnia and nightmares occur in more
tianeptine than
amitriptyline recipients (20 vs 7%). The relative lack of
sedative,
anticholinergic and cardiovascular adverse effects with
tianeptine makes it particularly suitable for use in the elderly and in patients following alcohol withdrawal; these patients are known to have increased sensitivity to the adverse effects associated with
psychotropic drugs.(ABSTRACT TRUNCATED AT 400 WORDS)