States Rally To Ban “Gas Station Heroin” Tianeptine

What is tianeptine?

Tianeptine is an atypical tricyclic antidepressant used primarily to treat major depressive disorder (MDD) and studied in the treatment of irritable bowel syndrome (IBS). Although never approved in the United States, it’s legitimately prescribed for those purposes under the brand names Coaxil in Europe and Stablon and Tatinol in Asia and Latin America.^[1]

Tianeptine’s mechanism of action isn’t fully understood. Structurally, it’s similar to other tricyclic antidepressants such as amitriptyline and nortriptyline, an older generation of antidepressants that have largely been replaced by SSRIs for mental health conditions but are still prescribed, including in the U.S., for nerve pain and migraines, among other conditions.^[2] However, it’s been found to have very different effects, some of which have only been illuminated in the last decade.

In 2014, tianeptine was found to be an agonist of one type of opioid receptor (μ).^[3] That means at high doses (above those used therapeutically), it can induce euphoria similar to that induced by opioids like heroin and is liable for abuse and addiction.^[4] 

Although unapproved for medical use, tianeptine is not a federally controlled substance in the U.S., meaning it can be legally sold in many states, including in gas stations, convenience stores, and online. Tianeptine may be marketed as a mood enhancer or dietary supplement, under the names Zaza, Tianaa Red, and Pegasus.^[5] This availability has opened the door for abuse, especially among people with current or previous opioid addictions, lending it the street name “gas station heroin.” 

What are the dangers of tianeptine?

While tianeptine is a prescription drug in some countries, it can be very dangerous when abused and has been associated with addiction, overdose, and severe withdrawal symptoms.

Adverse effects of tianepentine include respiratory depression, coma, agitation, and seizures.^[6] In overdose, it can mimic opioid toxicity.^[7]

Tianeptine can also cause physical dependence and severe withdrawal symptoms, likened to opioid withdrawal but described by some users as worse.^[5] Commonly reported withdrawal symptoms include agitation, nausea, vomiting, and elevated heart rate and blood pressure.^[7]

In 2018, a literature review found 65 reports of tianeptine abuse and dependence in medical studies, with patients taking daily doses of between 50mg and 10g (therapeutic doses are 25-50mg) orally, intravenously, or through snorting. 15 cases of overdose were reported, eight in combination with another substance (usually alcohol, cocaine, or opioids), and nine total deaths were registered.^[8]

Tianeptine abuse has risen sharply

Tianeptine has increasingly been used as a substitute or enhancer of opioids, with abuse growing exponentially over the last few years. In 2018, the CDC noted that between 2001 and 2013, there were just 11 incidents of tianeptine exposure reported by poison control centers to the National Poison Data System (NPDS). However, between just 2014 and 2017, there were 217 reports, suggesting the drug is an “emerging public health threat.”^[7]

Since then, its use has further escalated. According to the FDA, in 2020 alone, there were 151 reports of tianeptine exposure made to poison control centers.^[9]

The FDA notes that people with a history of opioid use disorder or dependence are at particular risk for abusing tianeptine.^[9] They may seek it out as a cheaper, more readily available substitute to illicit opioids. Additionally, they may be exposed to it unwittingly: the Drug Enforcement Administration (DEA) reports that tianeptine may be present in counterfeit pills purporting to be the opioids hydrocodone or oxycodone.^[4]

States take action against tianeptine

Reacting to a string of overdoses in the state, Michigan made tianeptine a Schedule 2 controlled substance in 2018.^[10] It’s subsequently been made a controlled substance in Alabama, Georgia, Indiana, and Ohio. Most recently, in March 2023, both Kentucky and Mississippi tightened controls on the drug.

In Kentucky, Governor Andy Beshear signed an emergency regulation making tianeptine a Schedule 1 substance, banning the sale of all products containing it. 

“Today, Kentucky became a safer place,” said Beshear, signing the regulation. “Until now, someone looking for a heroin-like high could walk into certain places or buy this harmful product online. We’re committed to protecting Kentuckians from this kind of harm, and if someone is struggling with abuse, we’re here to help.”  

Meanwhile, in Mississippi, tianeptine will be classified as a Schedule 3 substance from June 30, 2023, after legislation was signed by Governor Tate Reeves.^[11] The state House of Representatives had initially passed a bill to make it a Schedule 1 substance but the legislation was amended in the Senate.^[12]

“This is the red ZaZa that's sold in convenience stores throughout our state that's causing so many problems,” said Mississippi State Representative Lee Yancey, chair of the Legislature’s Drug Policy Committee, "We have letters from family members begging for us to get it off the shelves.”^[12]

Tianeptine remains legal in 43 states and federally.