Position of tianeptine among
antidepressive chemotherapies

Loo H, Deniker P
Service Hospitalo-Universitaire
de Sante Mentale et de Therapeutique,
Hopital Sainte Anne, Paris, France.
Clin Neuropharmacol 1988; 11 Suppl 2:S97-102


The advent of a new antidepressant is always received with both interest and scepticism by clinicians. No new compound has yet been shown to be more efficient than imipramine in the treatment of depression. In determining the position of a compound among the antidepressants, four levels are to be considered: (a) Chemical family: Tianeptine is a tricyclic compound of dibenzothiazepine type. It is the only representative of this subgroup. (b) Biochemical activities: Tianeptine increases the presynaptic uptake of serotonin after single as well as repeated administration; but this action is not linked to any effect on the 5-HT post-synaptic systems. Electrophysiological modifications are observed in the locus coeruleus (noradrenergic) at 2.5 times higher doses; nevertheless, the essential action involves the serotoninergic systems. Tianeptine has no affinity for alpha 1 adrenergic and H1 antihistaminic receptors; this affinity is responsible in a large part for the sedative anxiolytic properties of antidepressants. Tianeptine has no affinity for the muscarinic receptors. It has secured its place among the non-anticholinergic antidepressants. The mechanism of action or the therapeutic profile cannot be inferred from this original biochemical profile. (c) In clinical trials, the double-blind trials confirm the antidepressant efficacy in essentially neurotic depressive syndromes, similar to that of imipramine, nomifensine, amitriptyline. They do not show a shorter onset time of antidepressant activity. The therapeutic profile appears to be neither stimulating nor sedative. Some arguments are in favor of an anxiolytic activity. Others favor a more psychotonic profile. Tianeptine can be classified among the mid-position antidepressants. (d) With respect to clinical acceptability, tianeptine has no anticholinergic effect and no cardiovascular effect.
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