Revision of AAPP Pharmacist Toolkit: Tianeptine from Wed, 06/03/2026 - 10:29

About AAPP Toolkits 

AAPP toolkits highlight both the evidence base available as well as strategies of clinical decision making used by expert psychiatric pharmacist clinicians. The content reflects the views and practice of the authors as substantiated with evidence-based facts as well as opinion and experience. Toolkits are peer reviewed by psychiatric pharmacists. Authors and AAPP review and update toolkits annually and strive to use up-to-date, non-stigmatizing language. Terminology does evolve rapidly and often regionally such that there may be differences between reader experiences and expectations and those of the author(s). AAPP members receive complimentary, continuous access to toolkits. Non-members can purchase for a fee for a period of 3 months.

Tianeptine is an atypical tricyclic antidepressant (TCA) approved for the treatment of major depressive disorder (MDD) in Europe, Asia, and Latin America, which is marketed under the brand names of Coaxil and Stablon.1,2,3 It is not FDA-approved for any indication in the United States.1

Despite lack of FDA approval, tianeptine has emerged as a significant drug of misuse in the U.S., marketed as "gas station heroin" and sold under brand names like "Zaza," "Tianna Red," and "Tianna" in convenience stores, gas stations, and smoke shops and through online vendors without a prescription.1,4

The primary public health concern stems from tianeptine’s activity as a full mu-opioid receptor (MOR) agonist. At supratherapeutic doses, this opioid agonist activity becomes the dominant pharmacologic effect, producing euphoria, dependence, tolerance, withdrawal syndromes, and overdose presentations like traditional opioids.1,2,5

Contents include:

  • Pharmacologic Classification and Therapeutic Mechanism of Action
  • Mechanism of Misuse
  • Pharmacokinetics
  • Epidemiology and Patterns of Use
  • Evaluation of the Patient
  • Clinical Presentation and Management of Acute Intoxication Syndrome
  • Clinical Presentation and Management of Withdrawal Syndrome
  • Key Clinical Pearls
  • References