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
- Marketed legally in Europe as an Antidepressant and Anxiolytic
- 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. Pharmacokinetics
- Rapid oral absorption
- Half-Life: 2.5 hours
IV. Adverse Effects: Toxic Doses
-
General
- Diaphoresis
- Neurologic
- Cardiovascular
- Gastrointestinal
V. Labs
VI. 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
VII. References
- Tomaszewski (2024) Crit Dec Emerg Med 38(2): 34