Tianeptine
Atypical antidepressant, μ-opioid modulator, EU/Russian prescription.
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WHAT IS TIANEPTINE?
Detailed overview
Tianeptine (Coaxil, Stablon) is a French (Servier, 1989) atypical antidepressant. Its original SSRE (serotonin reuptake enhancer) theory was revised by the 2014 Gassaway et al. work (PMID 25049078), which described a **μ-opioid receptor (MOR) partial agonist** profile at therapeutic doses (EC50 ~194 nM) + lower δ-opioid affinity. At clinically relevant doses (12.5-37.5 mg/day) the antidepressant effect dominates with minimal euphoria, but at high doses (>50 mg) classic opioid-like side effects emerge, **causing opioid tolerance and dependence**. **Glutamatergic modulation**: inhibits stress-induced hippocampal glutamate overproduction + BDNF up-regulation → a structural antidepressant effect. Banned OTC in the USA (controlled substance in several states – "gas station heroin" abuse epidemic), strictly prescription-only in the EU (including Hungary).
Mechanism
μ-opioid partial agonist
Half-life
~2.5 h
Legal status
EU Rx / USA banned
Safety
Side effects, stop signs, contraindications
Side effects · 7
- Nausea, dry mouth and constipation (common GI complaints)
- Dizziness, headache and drowsiness
- Sleep disturbance, irritability and vivid dreams
- At high doses opioid-like euphoria, then tolerance development
- Physical dependence and opioid withdrawal on cessation (craving, sweating, anxiety)
- Rarely hepatotoxicity (hepatitis) with elevated liver enzymes
- Respiratory depression in overdose, heightened with other opioids or sedatives
Contraindications · 6
- History of substance use disorder or opioid dependence (high abuse and dependence potential)
- Concomitant use with MAO inhibitors (washout required before and after)
- Concurrent opioids or CNS depressants, alcohol (respiratory depression, overdose risk)
- Pregnancy and breastfeeding (not recommended, limited safety data)
- Severe hepatic or renal impairment and elderly age (dose reduction required)
- Avoid abrupt discontinuation (withdrawal syndrome); gradual tapering required
Related Nootropics
Same therapeutic category
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The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.