WARNINGDANGER OF DEATH
High doses alone or ordinary doses in combination with other depressants can fatally stop breathing.
Tianeptine
Tianeptine is an atypical tricyclic antidepressant of the dibenzothiazepine class.citation needed Unlike typical tricyclics, it is thought to act primarily through glutamatergic modulation rather than direct monoaminergic regulation. Clinically prescribed for depression and anxiety, it also exhibits anxiolytic and purported nootropic properties. At supratherapeutic doses, tianeptine produces opioid-like effects, contributing to its recreational misuse potential. It is considered habit-forming and is most commonly available in its sodium salt form.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Tianeptine occurs commonly in 2 salts, sodium and sulfate. The duration of sulfate is much longer.
Duration
Subjective Effects
Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.
Effects vary widely by individual, dose, and context.
Physical
Cognitive
Visual
Pharmacology
Pharmacodynamics
Tianeptine acts primarily as a full agonist of the μ-opioid receptor (MOR) and may function as a biased agonist at this site.citation needed It also shows full agonism at the δ-opioid receptor with approximately 200-fold lower potency, while κ-opioid receptor activity is clinically negligible. Tianeptine indirectly modulates glutamatergic neurotransmission through effects on AMPA and NMDA receptors and promotes the release of brain-derived neurotrophic factor (BDNF), influencing neuroplasticity. Additional actions include allosteric modulation of the serotonin transporter (SERT) that enhances rather than inhibits serotonin reuptake, modest enhancement of mesolimbic dopamine release with indirect potentiation of D2 and D3 receptor signaling (without direct receptor affinity), and high-efficacy agonism at the nuclear receptor PPAR-δ.
Pharmacokinetics
Tianeptine has an oral bioavailability of approximately 99% and reaches peak plasma concentrations within about one hour, with approximately 95% plasma protein binding.1 Metabolism is hepatic via β-oxidation, and CYP enzymes are not involved, limiting the potential for drug-drug interactions.citation needed The elimination half-life is 2.5 to 3 hours, increasing to 4 to 9 hours in elderly individuals. Two active metabolites are produced: MC5, which retains μ-opioid but not δ-opioid agonist activity and has a longer half-life of approximately 7.6 hours, and MC3, which is a much weaker μ-opioid agonist. MC5 takes about one week to reach steady-state under daily dosing. Approximately 65% of tianeptine is excreted renally and 15% in feces.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Opioids, Tricyclic antidepressants
Harm Potential
Addiction & Dependence
Psychological
ModerateTianeptine has moderate abuse potential, particularly at doses exceeding the therapeutic range. Its short duration of action may compel frequent redosing, and the opioid-like euphoria at high doses (above 100mg) can drive compulsive use patterns.citation needed Between 1989 and 2004, France identified 141 cases of recreational use, representing 1 to 3 cases per 1000 treated patients.
Physical
ModeratePhysical dependence develops with chronic use at high doses. Withdrawal symptoms resemble those of typical opioids including agitation, nausea, vomiting, tachycardia, hypertension, diarrhea, tremor, and diaphoresis, along with emotional instability.citation needed Withdrawal severity correlates with daily dosage and duration of use, with high doses described as extremely difficult to quit.
Toxicity
Unlike other tricyclic antidepressants, tianeptine produces significantly fewer cardiovascular effects and does not appear to affect heart function at therapeutic doses.citation needed
Intravenous injection of crushed tablets can cause thrombosis and severe necrosis due to silica and other undissolved particles blocking capillaries; this harm is associated with improper administration of oral formulations rather than inherent compound toxicity.
Seizure Risk
Research indicates possible anticonvulsant activity via downstream modulation of adenosine A1 receptors, suggesting tianeptine may have seizure-protective rather than seizure-promoting properties.
History & Culture
Discovery and Medical Development
Tianeptine was developed and patented by the French Society of Medical Research during the 1960s.citation needed Following clinical development, it was introduced for therapeutic use in France in 1983, becoming available through Laboratories Servier SA. The drug subsequently…
Legality
By Country
References
Source Pages
Citations
- R J Royer, H Albin, D Barrucand, C Salvadori-Failler, & A Kamoun. (1988). Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors. Clinical Neuropharmacology, 11(Suppl 2), S90-6. https://pubmed.ncbi.nlm.nih.gov/3180120/1
- Drug Enforcement AdministrationDiversion Control DivisionDrug & Chemical Evaluation Section - Tianeptine. (n.d.). https://www.deadiversion.usdoj.gov/drug_chem_info/tianeptine.pdf1
- Novel Psychoactive Substances: Tianeptine (LAPPA Fact Sheet, March 2023). (n.d.). https://legislativeanalysis.org/wp-content/uploads/2023/03/Tianeptine-Fact-Sheet-FINAL.pdf12
- Controlled Drugs and Substances Act. canada.ca (n.d.). https://www.canada.ca/en/health-canada/services/publications/healthy-living/new-psychoactive-substances-canada-2024.html1
- Controlled Drugs and Substances Act. laws.justice.gc.ca (n.d.). https://laws.justice.gc.ca/eng/acts/C-38.8/FullText.html1
- Anlage 1 AMVV (Arzneimittelverschreibungsverordnung) — gesetze-im-internet.de. gesetze-im-internet.de (n.d.). https://www.gesetze-im-internet.de/amvv/anlage_1.html1
- Arzneimittelverschreibungsverordnung (AMVV). gesetze-im-internet.de (n.d.). https://www.gesetze-im-internet.de/amvv/__1.html1
- Arzneimittelverschreibungsverordnung (AMVV). gesetze-im-internet.de (n.d.). https://www.gesetze-im-internet.de/amvv/index.html1
- Characteristics of Tianeptine Exposures Reported to the National Poison Data System - United States, 2000-2017. (n.d.). https://www.cdc.gov/mmwr/volumes/67/wr/mm6730a2.htm1
- PubChem CID 68870 tianeptine chemical properties. pubchem.ncbi.nlm.nih.gov (n.d.). https://pubchem.ncbi.nlm.nih.gov/rest/pug/compound/cid/68870/property/IUPACName,MolecularFormula,CanonicalSMILES,IsomericSMILES/JSON1
Further Reading
Drugs-Forum: recreational use experiences (2012)
FDA consumer warning (2024)
IV toxicity case report (2017)
Mississippi withdrawal cases (2022)
Opioid-system mechanisms review (2023)
Pain Therapy narrative review (2023)
PBS NewsHour FDA warning coverage (2023)
Pharmacology and use review (ResearchGate 2018)
Reddit: community experiences (r/QuittingTianeptine)
Reddit: dosage discussion (r/researchchemicals 2023)
Reddit: high-dose habit report (r/QuittingTianeptine 2024)
Reddit: social media analysis (PMC 2021)
Severe withdrawal case management (2023)
UIC Pharmacy FAQ on tianeptine misuse (2024)
VICE article on Reddit withdrawal support
Article Status
Step 1 · Automated synthesisAn autonomous workflow built by Josie Kins compiled this article's foundation from information published across the web.
- Step 2 · First-pass review
A first pass manual review and edit of article prose and copy has been performed by subject-matter expert Lyrea. This does not guarantee factual accuracy. An additional human review for each of this article's citations is yet to be performed.
- Step 3 · Citation reviewPending
No one has reviewed this article's citations yet. That second pass checks each claim against the source it cites.
Recent changes8 human edits · latest
Times are UTCNewest first
16 August 2026
Lyrea · Edited in History & Culture › Sections 3 › Content
Lyrea · Reworded 10 words in Dosage & Duration › Routes 1 › Notes
Lyrea · Reworded 6 words in Dosage & Duration › Routes 1 › Notes
Lyrea · Changed a word in Dosage & Duration › Routes 1 › Dose ranges › Light
24 January 2026
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Suggest an edit
Spotted a mistake, an outdated claim, or something missing from the Tianeptine article? Send the editors a private note. Feedback lands in a moderation queue and is never shown on the site.
Wish to give generalised feedback? You can do so here.