Tianeptine is an atypical tricyclic antidepressant primarily used to treat major depressive disorder. Marketed under brand names like Stablon, Tatinol, and Coaxil, it has also been prescribed for anxiety, asthma, and irritable bowel syndrome. As an antidepressant, Tianeptine distinguishes itself from other tricyclics with its unique pharmacological profile and mechanism of action, making it a subject of interest in the treatment of mood disorders.
Tianeptine, dubbed 'gas station heroin,' is legally ambiguous and widely accessible raising concerns. Health experts are sounding alarms about the unapproved drug's potential health risks and addictive qualities sold in gas stations and convenience stores across the US.
In 1983, Tianeptine was introduced for medical use in France under the brand name Stablon.
In 1983, Tianeptine was introduced for medical use in France.
Between 1989 and 2004, in France 141 cases of recreational use of Tianeptine were identified, correlating to an incidence of 1 to 3 cases per 1000 persons treated with tianeptine.
In August 1998, Dr. Fuad Lechin and colleagues published the results of a 52-week randomized controlled trial of asthmatic children that showed the children in the groups who received tianeptine had a sharp decrease in clinical rating and increased lung function.
In 2001, Singapore's Ministry of Health restricted tianeptine prescribing to psychiatrists due to its recreational potential.
In 2003, Bahrain classified tianeptine a controlled substance due to increasing reports of misuse and recreational use.
By November 2004, two double-blind placebo-controlled crossover trials and an under-25,000 person open-label study lasting over seven years, both showing effectiveness of Tianeptine for Asthma.
Between 1989 and 2004, in France 141 cases of recreational use of Tianeptine were identified, correlating to an incidence of 1 to 3 cases per 1000 persons treated with tianeptine.
A 2005 study in Egypt showed Tianeptine to be effective in men with depression and erectile dysfunction.
Between 2006 and 2011, 45 cases of recreational use of Tianeptine were identified in France.
In January 2007, a clinical trial in Spain showed that tianeptine is effective in treating pain due to fibromyalgia.
In 2007, Tianeptine's manufacturer Servier agreed to modify the drug's label, following problems with dependency, according to French Health Products Safety Agency.
In June 2009, Phase I clinical trials of tianeptine for the treatment of major depressive disorder were completed in the United States.
Between 2006 and 2011, 45 cases of recreational use of Tianeptine were identified in France.
In January 2012, development of tianeptine for the treatment of major depressive disorder was discontinued in both the United States and Belgium for unclear reasons.
In 2012, Janssen patented tianeptine sulfate, a slower-releasing formulation of Tianeptine.
In 2014, The U.S. National Poison Data System showed a nationwide increase in tianeptine exposure calls.
In 2014, tianeptine was found to be a μ-opioid receptor (MOR) full agonist using human proteins. It was also found to act as a full agonist of the δ-opioid receptor (DOR), although with approximately 200-fold lower potency.
In 2017, The U.S. National Poison Data System data showed a nationwide increase in calls related to abuse and misuse of Tianeptine.
On 6 April 2018, Michigan became the first US state to outlaw tianeptine sodium, classifying it as a schedule II controlled substance.
The scheduling of tianeptine sodium in Michigan as a schedule II controlled substance became effective on July 4, 2018.
A literature review conducted in 2018 found 25 articles involving 65 patients with tianeptine abuse or dependence.
On March 13, 2020, Italy became the first European country to outlaw tianeptine considering it a Class I controlled substance.
On March 15, 2021, Alabama outlawed tianeptine, initially classifying it as a schedule II controlled substance.
On July 1, 2022, Tennessee outlawed tianeptine, classifying it as a schedule II controlled substance.
On December 22, 2022, Ohio outlawed tianeptine, classifying it as a schedule I controlled substance.
In 2022, Tonix Pharmaceuticals received permission from the US FDA to conduct phase II clinical trials on tianeptine hemioxalate extended-release tablets designed for once-daily use.
On March 23, 2023, Kentucky outlawed tianeptine, classifying it as a schedule I substance.
On September 20, 2023, Florida outlawed tianeptine, classifying it as a schedule I substance.
In October 2023, Tonix Pharmaceuticals announced that it had discontinued its development of tianeptine as a monotherapy for major depressive disorder after disappointing phase-2 clinical trial results.
In late 2023, Tonix Pharmaceuticals discontinued phase II clinical trials on tianeptine hemioxalate extended-release tablets designed for once-daily use because of disappointing results in clinical trials.
As recently as January 2024, the Food and Drug Administration (FDA) has issued warnings about the dangers of recreational tianeptine use and the risks posed by adulterated dietary supplements containing undeclared tianeptine.
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