Tianeptine Stats - Substance Search

Pharmacology

DrugBank

Half-life Approximately 2.5 h Protein binding 95% bound to plasma protein . State Solid Vd 0.8 L/kg (0.77 +/- 0.31 L/kg) Clearance Rapidly cleared by the kidneys .

Description

Tianeptine is a drug used primarily in the treatment of major depressive disorder and has been studied in the treatment of irritable bowel syndrome (IBS) . Structurally, it is classified as a tricyclic antidepressant (TCA), however, it possesses different pharmacological properties than typical tricyclic antidepressants . Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s . Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in several other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S.

Mechanism of Action

Recent studies suggest that tianeptine acts as a full agonist at the mu-type opioid receptor (MOR) , . The mu opioid receptors are currently being studied as effective targets for antidepressant therapies . It is believed that the clinical effects of tianeptine are owed to its modulation of these receptors . In addition to its actions on the opioid receptor, previous studies have owed its action to its effect on the serotonin receptor , , dopamine (D2/3) receptors , and glutamate receptors , , as discussed below: Tianeptine has challenged the monoaminergic hypothesis of depression, as well as the widely supported monoaminergic mechanisms whereby the action of most known antidepressants have been explained . Specifically, this drug is thought to persistently alter glutamate receptor bursting of the hippocampal CA3 commissural associational synapse . Current research suggests that tianeptine produces its antidepressant effects through the modulation of glutamate receptor activity (for example, AMPA receptors and NMDA receptors) and affect the release of brain-derived neurotrophic factor (BDNF), which impacts neural plasticity . More recent studies by support the role of tianeptine in the modulation of glutaminergic activity in the amygdala, the emotional region of the brain associated with memories .

Pharmacodynamics

Analyses in large-scale epidemiologic surveys have shown that the anxiety disorders are widely comorbid with major depression. This makes antidepressant with anxiolytic properties particularly unique and attractive . Tianeptine is effective in reducing depressive symptoms in mild to severe major depressive disorder and also alleviates anxious symptoms associated with depression without the need for coadministration of an anti-anxiety medication . These findings, however, are met with controversial data. In a study of healthy volunteers, Tianeptine-treated subjects were less accurate at identifying facial expressions, suggesting a lack of improvement in the psychomotor symptoms of depression. The tianeptine group also showed reduced memory and reduced attentional vigilance to various stimuli .

Metabolism

Tianeptine is metabolized primarily by beta-oxidation of its heptanoic side chain . The metabolism of tianeptine was studied after a one-time oral administration of radioisotopically (14C) labeled compound to healthy male volunteers. After 1 week, approximately 66% of the dose was eliminated by the kidneys (55% elimination during the first 24 hr). After 24h, unchanged drug 3% of the drug was found unchanged in the urine. Three major metabolites result from beta-oxidation of Tianeptine. The metabolite profiles of tianeptine in feces and plasma were found to be qualitatively similar to that in urine .

Absorption

Well absorbed, approximately 99% bioavailability .

Toxicity

There are several published case reports of tianeptine intoxication and death . An overdose of tianeptine can lead to opiod-like effects and lead to respiratory failure and death, due to its direct effect on the _mu_ opioid receptor . In addition, cardiotoxicity can result from an overdose of this medication .

Indication

Used primarily in the treatment of major depressive disorder and anxiety . It is currently being studied for fibromyalgia pain treatment .

Elimination

Eliminated with bile as glucuronide and glutamine conjugates .

Receptor Profile

Receptor Actions

Agonists

μ-opioid receptor agonist (full)

Inhibitors

Previously classified as serotonin reuptake enhancer (now questioned)

Modulators

Glutamate receptor modulator (NMDA receptor

Other

AMPA receptor)

Modulates neuroplasticity via BDNF release

History & Culture

1960s–1983

Tianeptine was developed and patented by the French Society of Medical Research during the 1960s. Following clinical development, it was introduced for therapeutic use in France in 1983, becoming available through Laboratories Servier SA. The drug subsequently gained approval across numerous European countries under the trade name Coaxil, and expanded into Asian markets including Singapore as well as Latin American countries where it was marketed as Stablon and Tatinol.

2001–2020

Following its widespread availability as a prescription antidepressant, tianeptine's potential for recreational misuse began attracting regulatory attention in the early 2000s. In 2001, Singapore's Ministry of Health implemented restrictions limiting tianeptine prescribing exclusively to psychiatrists. French pharmacovigilance monitoring identified 141 cases of recreational use between 1989 and 2004, representing approximately 1 to 3 cases per 1000 individuals treated with the medication, with an additional 45 cases documented between 2006 and 2011. Abuse patterns in Russia proved particularly concerning, with some individuals dissolving and injecting tianeptine tablets intravenously to achieve opioid-like effects or mitigate opioid withdrawal symptoms. Because the tablets contain silica that does not fully dissolve, inadequately filtered injections frequently resulted in blocked capillaries, leading to thrombosis and severe tissue necrosis. These complications prompted Russia to classify tianeptine as a Schedule III controlled substance. In March 2020, Italy became the first European country to prohibit tianeptine entirely, classifying it as a Class I controlled substance by ministerial decree.

2018–present

Unlike most countries where tianeptine remained a prescription medication, in the United States the compound was never approved for medical use and remained unregulated at the federal level. This regulatory gap allowed tianeptine to be sold as a dietary supplement and through convenience stores, earning it the colloquial designation "gas station heroin" due to its ready availability and opioid-like effects at high doses. The Centers for Disease Control and Prevention characterized tianeptine as an "emerging public health risk," noting substantial increases in exposure-related calls to poison control centers. The Food and Drug Administration issued multiple warnings about the dangers of recreational tianeptine use, including a notice in January 2024, though the compound remains outside the Drug Enforcement Administration's controlled substance framework. Individual states began implementing their own controls starting with Michigan, which in April 2018 became the first to classify tianeptine sodium as a Schedule II controlled substance. Oklahoma followed in November 2019, Alabama in March 2021, Tennessee in July 2022, and Ohio in December 2022—with Ohio's governor specifically referencing its widespread availability as "gas-station heroin" when signing the legislation. Kentucky enacted restrictions in March 2023, followed by Florida in September 2023.

Effect Profile

Curated + 17 Reports

Opioid 5.0

Moderate euphoria and itching/nausea with mild sedation and pain relief

Euphoria / Warmth×3

6

Analgesia×2

4

Sedation / Relaxation×1

5

Itching / Nausea×1

6

Based on reports from:

Erowid Experience Reports PsychonautWiki Tianeptine

Tolerance & Pharmacokinetics

drugs.wiki

Tolerance Decay

Full tolerance 1d Half tolerance 21d Baseline ~35d

Experience Report Analysis

Erowid

17 Reports

2002–2024 Date Range

12 With Age Data

15 Effects Detected

Demographics

Gender Distribution

Age Distribution

Reports Over Time

Effect Analysis

Erowid

Effects aggregated from 17 experience reports (17 Erowid)

17 Reports

15 Effects Detected

10 Positive

2 Adverse

3 Neutral

Effect Sentiment Distribution

Confidence Distribution

Positive Effects 10

Euphoria 52.9% 70%

Sedation 47.1% 70%

Stimulation 47.1% 70%

Empathy 35.3% 70%

Anxiety Suppression 35.3% 70%

Color Enhancement 23.5% 70%

Music Enhancement 23.5% 70%

Tactile Enhancement 23.5% 70%

Focus Enhancement 23.5% 70%

Introspection 17.6% 70%

Adverse Effects 2

Nausea 23.5% 70%

Headache 17.6% 70%

Dosage Distribution

Dose distribution from experience reports

Median: 65.0 mg IQR: 45.0–187.5 mg n=10

Real-World Dose Distribution

62K Doses

From 21 individual dose entries

Oral (n=19)

Median: 62.5mg 25th: 47.5mg 75th: 193.75mg 90th: 366.8mg

mg/kg median: 0.893 mg/kg 75th: 2.549

Form / Preparation

Most common forms and preparations reported

Body-Weight Dosing

Dose relative to body weight from reports with weight data

Median: 0.895 mg/kg IQR: 0.763–2.507 mg/kg n=10

Redose Patterns

Redosing behavior across 11 reports

9.1% Redosed

1.1 Avg Doses

190m Median Interval

Legal Status

Country	Status	Notes
Canada	Uncontrolled	Legal to possess without any license or prescription. Not scheduled under federal controlled substances legislation.
Germany	Prescription medicine (Anlage 1 AMVV)	Classified as a prescription-only medicine under Anlage 1 of the Arzneimittelverschreibungsverordnung (AMVV). Not a controlled narcotic under the Betäubungsmittelgesetz, but requires a valid prescription for legal possession.
Russia	Schedule III	Classified as a Schedule III controlled substance since 2010. Possession, distribution, and production without authorization is prohibited.
Sweden	Controlled	Not approved as a prescription medicine in Sweden, and is therefore classified as a controlled substance. Possession without authorization is illegal.
Switzerland	Uncontrolled	Not listed under controlled substance categories Buchstabe A, B, C, or D. Generally considered legal to possess.
Turkey	Prescription only (green prescription)	Designated as a 'green prescription' substance, indicating controlled distribution through pharmacies. Illegal when sold or possessed without a valid prescription.
United Kingdom	Illegal (Psychoactive Substances Act)	Illegal to produce, supply, or import under the Psychoactive Substances Act 2016, which came into effect on May 26, 2016. The Act does not criminalize personal possession but prohibits all commercial activity.
United States	Federally uncontrolled (state restrictions apply)	Not scheduled at the federal level under the Controlled Substances Act. However, individual states have begun implementing controls. Michigan became the first state to classify tianeptine sodium salt as a Schedule II controlled substance in March 2018. Many nootropics vendors have voluntarily ceased distribution due to documented abuse potential.

Tianeptine Stats & Data