Tianeptine

Stablon, Coaxil, Tatinol, ZaZa, Tianna Red

Psychoactive Class

Chemical Class

Dibenzothiazepine derivative Tricyclic compound

Tianeptine is an atypical tricyclic antidepressant of the dibenzothiazepine class.¹ 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

Threshold~3 mg

Light6-12 mg

Moderate12-35 mg

Strong35-100 mg

Heavy100+ mg

Bioavailability

~99%

Duration

Onset30-60 minutes

Come Up15-30 minutes

Peak1-1.5 hours

Offset0.5-1 hours

After Effects1-8 hours

Total2-3 hours

Half-life

2.5-3 hours

Subjective Effects

Effects vary widely by individual, dose, and context.

Physical

StimulationMuscle relaxation Headaches Dizziness Constipation Physical fatigue

Cognitive

Motivation enhancementThought acceleration or Thought decelerationRejuvenation

Visual

Forked from Subjective Effect Documentation

by Josie KinsJuly 2016.

Reagent Testing

Loading reagent data

Expected colorimetric results are being prepared.

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.²³ It also shows full agonism at the δ-opioid receptor with approximately 200-fold lower potency, while κ-opioid receptor activity is clinically negligible.² Tianeptine indirectly modulates glutamatergic neurotransmission through effects on AMPA and NMDA receptors and promotes the release of brain-derived neurotrophic factor (BDNF), influencing neuroplasticity.⁴ Additional actions include allosteric modulation of the serotonin transporter (SERT) that enhances rather than inhibits serotonin reuptake,⁴ 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.⁵

Pharmacokinetics

Tianeptine has an oral bioavailability of approximately 99% and reaches peak plasma concentrations within about one hour, with approximately 95% plasma protein binding.⁶ Metabolism is hepatic via β-oxidation, and CYP enzymes are not involved, limiting the potential for drug-drug interactions.¹⁷ The elimination half-life is 2.5 to 3 hours, increasing to 4 to 9 hours in elderly individuals.⁶ 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.⁶

Tolerance

Full Tolerance

Tolerance to many of tianeptine's effects develops with prolonged and repeated use, including its therapeutic benefits. This necessitates progressively larger doses to achieve equivalent effects. The compound's short duration of action may encourage frequent redosing, and the euphoric properties at high doses (above 100mg) can accelerate tolerance development.

Baseline Reset

1-2 weeks

Half Tolerance

3-7 days

Cross Tolerance

Opioids, Tricyclic antidepressants

Harm Potential

Addiction & Dependence

Psychological

Moderate

Tianeptine 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.⁸ Between 1989 and 2004, France identified 141 cases of recreational use, representing 1 to 3 cases per 1000 treated patients.

Physical

Moderate

Physical 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.⁹ Withdrawal severity correlates with daily dosage and duration of use, with high doses described as extremely difficult to quit.

Toxicity

Cardiovascular

Unlike other tricyclic antidepressants, tianeptine produces significantly fewer cardiovascular effects and does not appear to affect heart function at therapeutic doses.¹

Vascular

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.¹⁰ Following clinical development, it was introduced for therapeutic use in France in 1983, becoming available through Laboratories Servier…

Legality

By Country

United StatesFederally uncontrolled (state restrictions apply)

Not scheduled at the federal level under the Controlled Substances Act.¹¹ 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 2018.¹⁵ Many nootropics vendors have voluntarily ceased distribution due to documented abuse potential.

GermanyPrescription medicine (Anlage 1 AMVV)

Classified as a prescription-only medicine under Anlage 1 of the Arzneimittelverschreibungsverordnung (AMVV).¹⁶ Not a controlled narcotic under the Betäubungsmittelgesetz, but requires a valid prescription for legal possession.

SwedenControlled

Not approved as a prescription medicine in Sweden, and is therefore classified as a controlled substance. Possession without authorization is illegal.

TurkeyPrescription only (green prescription)

Designated as a 'green prescription' substance, indicating controlled distribution through pharmacies. Illegal when sold or possessed without a valid prescription.

CanadaUncontrolled

Legal to possess without any license or prescription. Not scheduled under federal controlled substances legislation.

RussiaSchedule III

Classified as a Schedule III controlled substance since 2010.¹¹ Possession, distribution, and production without authorization is prohibited.

SwitzerlandUncontrolled

Not listed under controlled substance categories Buchstabe A, B, C, or D. Generally considered legal to possess.

United KingdomIllegal (Psychoactive Substances Act)

Illegal to produce, supply, or import under the Psychoactive Substances Act 2016,¹⁷ which came into effect on May 26, 2016.¹⁷ The Act does not criminalize personal possession but prohibits all commercial activity.

References

Source Pages

Citations

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Tianeptine

Stablon, Coaxil, Tatinol, ZaZa, Tianna Red

Psychoactive Class

Opioid Antidepressant Depressant

Chemical Class

Dibenzothiazepine derivative Tricyclic compound