II. Mechanism
-
Antidepressant that increases brain uptake of Serotonin (5-HT) and increasing central Serotonin activity
- Unique to Tianeptine and in contrast with SSRIs that inhibit the synaptic reuptake of Serotonin
- Also modulates Glutamate
- Marketed legally in Europe, Asia and Latin America as an Antidepressant and Anxiolytic
- Not FDA approved or regulated in the U.S.
- Atypical and weak mu-Opioid receptor Agonist when used at high dose
- Available in the U.S. as a "dietary supplement", and often sold in gas station convenience stores
- Ilicit use for Opioid-like euphoria (typically at excessive doses that risk toxicity)
- Patients with addiction will use doses of 100 mg every 2 hours
III. Precautions
- NOT recommended for any use in the U.S.
- Risk of Drug Dependence as well as life threatening events (especially in Overdose)
IV. Pharmacokinetics
- Rapid oral absorption
- Half-Life: 2.5 hours
V. Dosing
- Depression dosing: 37.5 mg/day
- Illicit dosing as a Opioid-like agent reaches doses as high as 10,000 mg/day
VI. Adverse Effects: Toxic Doses
-
General
- Diaphoresis
- Neurologic
- Respiratory
- Respiratory depression (deaths have occurred)
- Cardiovascular
- Gastrointestinal
VII. Drug Interactions
-
CNS Depressants (Benzodiazepines, Cannabinoids, Opioids)
- Potentiates effects of Tianeptine
-
Monoamine Oxidase Inhibitors
- Cardiovascular collapse and Seizure risk (may be fatal)
VIII. Labs
IX. Management
- ABC Management
-
Activated Charcoal
- Consider if presentation within 1 hour of ingestion
- Respiratory depression or apnea
- Consider Naloxone (may be ineffective)
- Agitation
- Withdrawal
- Consider Buprenorphine
- Disposition
- Consider observation for CNS depression
X. Complications
- Substance Abuse with dependence and withdrawal (similar to Opioid Toxicity and withdrawal)
XI. References
- (2025) Presc Lett 32(8): 48
- Tomaszewski (2024) Crit Dec Emerg Med 38(2): 34