II. Mechanism

  1. Antidepressant that increases brain uptake of Serotonin (5-HT) and increasing central Serotonin activity
    1. Unique to Tianeptine and in contrast with SSRIs that inhibit the synaptic reuptake of Serotonin
    2. Marketed legally in Europe as an Antidepressant and Anxiolytic
  2. Atypical and weak mu-Opioid receptor Agonist when used at high dose
    1. Available in the U.S. as a "dietary supplement", and often sold in gas station convenience stores
    2. Ilicit use for Opioid-like euphoria (typically at excessive doses that risk toxicity)
    3. Patients with addiction will use doses of 100 mg every 2 hours

III. Pharmacokinetics

  1. Rapid oral absorption
  2. Half-Life: 2.5 hours

IV. Adverse Effects: Toxic Doses

  1. General
    1. Diaphoresis
  2. Neurologic
    1. Agitation
    2. Lethargy
    3. Tremor
  3. Cardiovascular
    1. Tachycardia
    2. Hypertension
  4. Gastrointestinal
    1. Nausea or Vomiting
    2. Abdominal Pain

V. Labs

VI. Management

  1. ABC Management
  2. Activated Charcoal
    1. Consider if presentation within 1 hour of ingestion
  3. Respiratory depression or apnea
    1. Consider Naloxone (may be ineffective)
  4. Agitation
    1. Benzodiazepines
  5. Withdrawal
    1. Consider Buprenorphine
  6. Disposition
    1. Consider observation for CNS depression

VII. References

  1. Tomaszewski (2024) Crit Dec Emerg Med 38(2): 34

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