Tianeptine, indicated as a thymoleptic, reduces the effects of serotonin in the limbic system and the pre-frontal cortex, giving rise to a mood elevation, unlike the mood blunting associated with SSRIs.
Suggested dosage is three times daily, due to its short duration of action. Tianeptine is synergistic and has been used in conjunction with other drugs such as modafinil.
Tianeptine has a strong antidepressant and anxiolytic properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, thus suggesting it is particularly suitable for use in elderly patients and in those following alcohol withdrawal; such patients can be more sensitive to the adverse effects of psychotropic drugs.
Uses
Approved:
Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with fewer side effects. It was shown to be more effective than maprotiline in a group of patients 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 (Paxil) or tianeptine (Stablon) therapy showed equivalent panic-blocking effects.
Contraindications
According to Servier International, tianeptine is contraindicated in children under 15 years of age, people taking MAOIs, and pregnant or lactating women. However, as of 2005, there are no studies published showing increased risk of birth defects.
Side effects
Side effects are as follows:
dry mouth
constipation
dizziness/syncope
drowsiness
postural hypotension
Insomnia and vivid dreams
Interestingly, tianeptine along with its two metabolites does not affect the reuptake of monoamines (DA, 5-HT, and noradrenaline) in vitro. Results from in vivo studies confirm that serotonin reuptake is enhanced -while dopamine and noradrenaline are unaffected- suggesting a mechanism independent of SERT. No data is available regarding effects of the drug on postsynaptic receptors.
Drug interactions
No sufficient data available at present date.
Usual doses
Although Servier's official recommendation is 12.5 mg three times per day before the main meals of the day, lower or higher doses may be used as determined by your prescribing physician.