This page describes pharmacological agents that may have legal restrictions, side effects, and drug interactions in your jurisdiction. Information is for educational research only — consult a clinician before considering any compound.
Surface here is educational only; do not use without medical supervision. Our editorial verdict is SKIP-PERMANENT — risk:benefit fails for the canonical archetype.
Tianeptine
Functionally a μ-opioid agonist sold as an "antidepressant nootropic" — at biohacker doses it produces opioid-tier euphoria, opioid-class…
Aliases (11)
Overview
What is Tianeptine?
Tianeptine is an atypical antidepressant approved in France, Russia, and other countries (not US) marketed as Stablon or Coaxil. Originally classified as a "serotonin reuptake enhancer," it is now understood to act primarily as a mu-opioid receptor partial agonist — a mechanism that explains both its efficacy and its abuse liability.
Key Benefits
Antidepressant and anxiolytic effects with rapid onset, particularly in anxious or somatically-tinged depression; appears to enhance neuroplasticity and mood without typical SSRI sexual or sedative side effects. Significant abuse and dependence risk at supratherapeutic doses (gas-station "ZaZa").
Mechanism of Action
Tianeptine is a full mu-opioid receptor agonist at therapeutic doses (recently confirmed) and a partial delta-opioid agonist. It also modulates glutamatergic transmission, restoring hippocampal LTP/synaptic plasticity disrupted by stress, and influences BDNF expression. The opioid mechanism underlies efficacy and the steep abuse-liability gradient at high doses.
▸Brand options8 known
StatusRx in France/EU/Asia (Stablon 12.5mg); Schedule I or controlled in 15+ US states (MI, AL, MN, TN, GA, IN, KY, OH, FL, MS, NC, LA, VA, DE, TX as of 2026); FDA Class I warning letter 2024 + reissued 2025; not federally scheduled in US (regulatory gap that fueled the gas-station epidemic)
Research Indications
Full μ-opioid receptor (MOR) agonist
Ki ~383 nM, EC50 ~194 nM for G-protein activation. Same target as morphine, heroin, fentanyl, oxycodone, hydrocodone. Lower affinity than…
Peptide Interactions
All "synergies" amount to "stacking opioids with other CNS depressants" → respiratory depression risk multiplies.
mitragynine + 7-OH-mitragynine are also μ-opioid agonists. Co-use is the most common pattern in tianeptine fatality case series. Stacking μ-agonists is how p…
GABA-B agonist + μ-opioid agonist = compounded sedation, respiratory depression, and two simultaneous severe withdrawals if both are run chronically. This is…
additive μ-agonism, additive respiratory depression.
additive respiratory depression. The CDC respiratory-depression-death warning for opioid + benzo applies fully.
historically contraindicated; risk of serotonin/hypertensive interaction unclear given the corrected mechanism, but the warning stands.
both have opioid + monoamine effects; stacking is doubly bad.
Quality Indicators
Pharmacy-dispensed, intact packaging
Prescription tablets in original sealed packaging from a licensed pharmacy.
Generic vs branded
Generics are usually fine but bioavailability can vary slightly; track if you switch.
Unbranded blister or counterfeit risk
Counterfeit pharmaceuticals are a known issue; verify pharmacy and lot if buying internationally.
What to Expect
- Day 1PK-driven acute peak per administration. Verify dose tolerated.
- Week 1Steady-state reached for most daily-dosed pharma.
- Week 2-4Therapeutic effect established; titration window if needed.
- Long-termPeriodic monitoring per drug class (labs, BP, ECG as applicable).
Side Effects & Safety
Common (>10% even at therapeutic dose):
- Dry mouth, constipation, nausea (opioid GI signature)
- Drowsiness, dizziness
- Headache
- Insomnia (paradoxical — short half-life crash)
- At higher doses: itching, pinpoint pupils, sedation
Less common (1-10%):
- Hepatotoxicity (rare elevations in transaminases; cases of hepatitis reported)
- Mood swings on the post-dose crash
- Tachycardia, hypertension during withdrawal even at therapeutic-dose discontinuation
Rare-serious (<1% but clinically critical):
- Respiratory depression at high doses → ICU admission, mechanical ventilation, naloxone reversal documented
- Death — 6 fatalities NJ June 2023-March 2024; 2 fatalities TX with pulmonary edema; ongoing per FDA reporting; often co-detected with kratom (mitragynine), buprenorphine, benzodiazepines (multi-substance overdose physiology)
- Seizures at high doses (FDA Neptune's Fix advisory specifically lists seizures + loss of consciousness)
- Severe withdrawal — autonomic storm, suicidal ideation during PAWS, ICU-level detox in heavy users
- Full opioid use disorder by DSM-5 criteria
Specific watch periods:
- All of them. There is no safe biohacker window. Dependence physiology starts within days at supra-therapeutic doses.
References
The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist (Gassaway et al. 2014, Translational Psychiatry)
Original mechanism reversal paper. Ki ~383 nM at human MOR, full agonist at MOR + DOR.
View StudyThe Behavioral Effects of the Antidepressant Tianeptine Require the Mu-Opioid Receptor (Samuels et al. 2017, Neuropsychopharmacology)
MOR-knockout mice lose all antidepressant-like behavioral response.
View StudyMu opioid receptors on hippocampal GABAergic interneurons are critical for the antidepressant effects of tianeptine (2021)
Localizes the MOR-dependent mechanism to GABAergic interneurons.
View StudyTianeptine causes opioid-receptor-dependent beta oscillations in rat hippocampus (2025 bioRxiv preprint)
Replication of MOR-mediated effects in 2025.
View StudyTianeptine disinhibits hippocampal CA1 pyramidal neurons by reducing GABAergic neurotransmission (2025 bioRxiv preprint)
Mechanistic refinement: MOR on inhibitory interneurons → disinhibition → AMPA enhancement.
View StudyTianeptine, an Antidepressant with Opioid Agonist Effects: Pharmacology and Abuse Potential, a Narrative Review (2023, Pain and Therapy)
Review covering recreational doses (1645-1924 mg/day mean, up to 4000+ mg/day) and abuse pattern.
View StudyFDA: Do not use any tianeptine product
FDA Class I warning, reissued May 2025.
View StudyFDA: Gas Station Heroin / Tianeptine product trend
Product names: Tianaa, Zaza, Neptune's Fix, Pegasus, TD Red.
View StudyGas station heroin started out as tianeptine, an antidepressant (NPR, July 2024)
Public-facing summary of the epidemic.
View StudyStates That Have Banned or Restricted Tianeptine — LegalClarity
State-by-state ban tracker (15+ states as of 2026).
View StudyTianeptine Crackdown Continues — Buchanan Ingersoll & Rooney
Recent legislative summary including LA, VA, DE, TX 2024-2025.
View StudySevere tianeptine withdrawal symptoms managed with medications for opioid use disorder: case report (2023)
Buprenorphine taper protocol for tianeptine detox.
View StudyWhat is tianeptine, and recommendations for managing tianeptine misuse/withdrawal — UIC Drug Info Group, June 2024
Clinical management overview.
View StudyReported Adverse Effects, Withdrawal Symptoms, and Misuse Patterns — Rothman Opioid Foundation
Withdrawal symptom analysis.
View StudyTianeptine Sodium: Potentially Lethal? (Psychiatrist.com)
Case reports of fatalities.
View StudyManagement of Respiratory Depression from Tianeptine Overdose with Naloxone (American Thoracic Society)
Documented naloxone reversal.
View StudyClassics in Chemical Neuroscience: Tianeptine (ACS Chemical Neuroscience)
Comprehensive medicinal chemistry / pharmacology review.
View StudyStablon product information (Servier)
Original French Rx label, 12.5 mg TID.
View StudyTianeptine — Wikipedia
General overview, regulatory and historical context.
View StudyPsychonautWiki: Tianeptine
Subjective effects, sodium vs sulfate kinetics.
View StudyWhen an obscurity becomes a trend: Social-media descriptions of tianeptine use (2021)
How biohacker forums became the on-ramp to the gas-station epidemic.
View StudyHow was your experience with this compound?
Anonymous · one vote per session · results below at 5+ votes.
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