What is the use of Tianeptine?

October 6, 2025 •

4 min read

In countries across Europe, Asia, and Latin America, tianeptine has been used as a prescription medication to treat depression and anxiety. In stark contrast, it is not approved for any medical use by the U.S. Food and Drug Administration (FDA), which has issued multiple warnings about its significant health risks and high potential for abuse.

Quick Summary

Tianeptine is an atypical antidepressant used legally in some countries for mood and anxiety disorders, but it is unapproved and dangerous in the US, known for its opioid-like abuse potential and serious health risks. It modulates glutamate and agonizes mu-opioid receptors, leading to dependence and dangerous overdose potential at high, unregulated doses.

Key Points

International Therapeutic Use: Tianeptine is a legal prescription drug for major depression, anxiety, and IBS in many countries outside the U.S..
Unapproved in the U.S.: The FDA has not approved tianeptine for any medical use and warns against consuming products that contain it due to serious health risks.
Dual Mechanism of Action: It primarily modulates glutamate for its antidepressant effects but also acts as a mu-opioid receptor agonist, especially at higher doses.
High Abuse Potential: Due to its opioid agonist effects, high doses can cause euphoria, leading to misuse and a high potential for addiction.
Severe Withdrawal Syndrome: Abrupt cessation of high-dose tianeptine use can result in withdrawal symptoms that are similar to those of opioids.
Overdose Risk: High doses increase the risk of a fatal overdose, which can be reversed by naloxone due to its opioid properties.
Risk of Adulteration: Unregulated products sold in the U.S. may contain other harmful substances in addition to or instead of tianeptine.

Therapeutic Uses Outside the United States

In regions where it is a legal prescription drug, the use of tianeptine has been primarily focused on its therapeutic effects as an antidepressant.

Treatment of Major Depressive Disorder

For decades, tianeptine has been marketed and prescribed in countries like France, under brand names such as Stablon and Coaxil, for treating major depressive episodes. Clinical studies have suggested that tianeptine's effectiveness is comparable to that of conventional selective serotonin reuptake inhibitors (SSRIs), but with a potentially more favorable side effect profile. It has been noted to produce fewer anticholinergic, sedative, and cardiovascular side effects than traditional tricyclic antidepressants (TCAs).

Anxiety and Related Conditions

Tianeptine also exhibits significant anxiolytic (anxiety-reducing) properties. It has been used to manage co-existing depression and anxiety and has shown effectiveness for a spectrum of anxiety disorders.

Irritable Bowel Syndrome (IBS)

Limited clinical trials have explored the use of tianeptine for treating irritable bowel syndrome, with some finding it to be as effective as other medications but with fewer adverse effects.

Other Investigational Uses

Research has explored other potential uses, including for asthma, fibromyalgia, and cognitive dysfunction associated with depression. However, its opioid-like properties and abuse potential have complicated the drug's overall profile, even in countries where it is medically sanctioned.

Unapproved and High-Risk Status in the U.S.

In the United States, there are no approved medical uses for tianeptine, and the FDA considers it an unsafe food additive.

Illegal Marketing and Unregulated Products

Despite its unapproved status, products containing tianeptine are widely and illegally marketed as dietary supplements or nootropics (cognitive enhancers) and are sold online and in stores like gas stations. These unregulated products often carry misleading claims of improving mood, treating anxiety, or even alleviating opioid withdrawal symptoms. However, the products can be mislabeled, adulterated with other harmful substances, and sold at dangerously high doses.

The Rise of "Gas Station Heroin"

Due to its agonist activity at mu-opioid receptors, high doses of tianeptine can produce euphoric, opioid-like effects. This has led to its street name, "gas station heroin," and has resulted in a significant increase in reported misuse, dependence, and addiction in the U.S..

The Pharmacology of Tianeptine

Atypical Mechanism of Action

Unlike most antidepressants that primarily target monoamine neurotransmitters like serotonin, tianeptine's mechanism is unique and multifaceted.

Glutamatergic Modulation

At therapeutic doses, tianeptine primarily modulates glutamate signaling in the brain. This affects neural plasticity, the brain's ability to change and adapt, and helps stabilize glutaminergic signaling, which is thought to be the basis for its antidepressant and anxiolytic effects.

Opioid Receptor Activation

At higher doses, tianeptine acts as a full agonist at the mu-opioid receptors, which explains its pain-relieving and euphoric effects. Activation of these receptors is responsible for its high potential for abuse and physical dependence.

The Serious Dangers of Misuse

The misuse of unregulated tianeptine products carries severe health risks.

High Potential for Dependence: Because of its mu-opioid receptor activity, regular high-dose use can quickly lead to dependence and withdrawal symptoms.
Severe Withdrawal Symptoms: Abrupt cessation can trigger withdrawal symptoms that mimic those of opioids, including intense cravings, anxiety, muscle aches, insomnia, nausea, and vomiting.
Overdose Risk: Overdosing on tianeptine can be fatal. Severe overdose can lead to respiratory depression (slowed breathing), coma, and death. The opioid overdose reversal medication naloxone has been used to reverse the effects of tianeptine overdose.

Comparison of Tianeptine with Other Antidepressants


Feature	Tianeptine	SSRIs (e.g., Fluoxetine)	TCAs (e.g., Amitriptyline)
Mechanism	Modulates glutamate signaling; mu-opioid receptor agonist (at high doses).	Primarily inhibits serotonin reuptake.	Inhibits reuptake of serotonin and norepinephrine.
Effectiveness	Shown to be effective for depression and anxiety in international trials.	Widely proven effective for depression and anxiety.	Historically effective for depression.
Side Effects	Fewer anticholinergic/cardiovascular side effects than TCAs; potential for dependence at high doses.	Well-known for specific side effects like sexual dysfunction, weight changes, and insomnia.	Significant anticholinergic, sedative, and cardiovascular side effects.
Abuse Potential	Very high potential for abuse and dependence, especially in unregulated markets.	Minimal to none.	Minimal to none, but overdose potential exists.
FDA Status (U.S.)	Unapproved; considered an unsafe food additive.	FDA-approved for specific mental health conditions.	FDA-approved for specific mental health conditions.

Conclusion

While tianeptine serves as a legitimate prescription antidepressant in several parts of the world, its use in the United States is unapproved and extremely risky. Its dual mechanism of action—modulating glutamate at low, therapeutic doses and acting as a powerful opioid agonist at high doses—underpins its controversy. The illegal marketing and sale of unregulated tianeptine products, often misleadingly labeled as harmless supplements, has created a significant public health danger. Consumers face the risk of severe dependence, dangerous withdrawal, overdose, and exposure to harmful contaminants. Individuals struggling with mood disorders or addiction should seek medically approved treatments and avoid all unregulated products containing tianeptine. For anyone seeking help for substance use, a valuable resource is the Substance Abuse and Mental Health Services Administration (SAMHSA) national helpline.

Frequently Asked Questions

No, tianeptine is not approved by the U.S. Food and Drug Administration (FDA) for any medical purpose. While it is not a federally controlled substance, the FDA considers it an unsafe food additive, and its sale is illegal.

It is referred to as 'gas station heroin' because it is illegally sold in convenience stores and gas stations and, at high doses, acts on the same opioid receptors in the brain as heroin, producing a euphoric high.

In some countries in Europe, Asia, and Latin America, tianeptine is prescribed to treat major depressive disorder, generalized anxiety disorder, and irritable bowel syndrome.

Unlike common antidepressants like SSRIs that increase serotonin levels, tianeptine primarily works by modulating glutamate signaling and acting as a mu-opioid receptor agonist. This dual action gives it a distinct pharmacological profile.

Yes, tianeptine has a significant potential for dependence and addiction, especially when misused at high doses. Users can experience opioid-like withdrawal symptoms when they stop taking it.

Unregulated tianeptine products carry risks of mislabeling, inconsistent dosing, and contamination with other dangerous substances. These products are not held to any safety standards and pose severe health risks.

An overdose can lead to serious consequences, including respiratory depression, seizures, coma, and death. Because of its opioid-like effects, an overdose can be reversed with naloxone.