EC Pharmacology and Toxicology

Tianeptine, also known as “gas station heroin”, is an opioid agonist and an antidepressant. In some countries, tianeptine is used as an oral antidepressant at a typical labeled dose of 12.5 mg three times daily. Tianeptine has been shown to be a moderately potent agonist for the mu-opioid receptor (MOR) and to a lesser extent the delta-opioid receptor (DOR). The antidepressant efficacy of tianeptine appears to be related to its MOR activity and its action on glutamate-mediated pathways of neuroplasticity. Because it is an opioid agonist with significant potential for abuse, high doses of tianeptine can produce opioid-like euphoria, tolerance, dependence, and withdrawal symptoms consistent with other opioid agonists. In the United States, tianeptine is an unapproved drug sold unlawfully as an unregulated dietary supplement. Despite explicit warnings from the FDA against its sale and distribution, tianeptine is frequently available at convenience stores, gas stations, vape shops, and online retailers. Tianeptine is often used recreationally, but it has also been used by some consumers to self-treat a variety of conditions or disorders. In recent years, case reports of recreational abuse of tianeptine have increased significantly. Reports of tianeptine abuse describe consumers ingesting high daily doses of tianeptine (from 50 mg to 10 g), leading to either withdrawal, intoxication, or death from an overdose. Due to the increase in tianeptine abuse, which can lead to serious harm, including death, several States have banned products containing tianeptine and have designated tianeptine as a controlled substance. The FDA has also been working on protecting the public from tianeptine products, including warning consumers and health care professionals about the serious adverse events that are associated with tianeptine abuse and helping detain tianeptine shipments at the U.S. borders. Health care professionals need to be proactive in understanding and addressing the recreational abuse of tianeptine as a growing threat to public health. Health care providers must encourage patients and consumers to avoid all products containing tianeptine, including those claiming to treat a medical condition or disorder. Health care professionals must also provide patients and the public with accurate and reliable information about tianeptine products and the underlying dangers of tianeptine abuse.

 Keywords: Tianeptine; Gas Station Heroin; Supplement; Dietary Supplement; Nootropic Supplement; Opioid; Opioid Agonist; MOR Agonist; Abuse; Withdrawal; Dependence; Respiratory Depression; Overdose; Opioid Use Disorder; Naloxone; Buprenorphine

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