Pills and powders containing a substance known as tianeptine are being marketed as supplements that claim to provide an “intense mood boost” and “mental clarity.” The “supplement,” which commonly goes by the brand names ZaZa or Tianna Red, are instead bringing deadly outcomes.
“The kind of scary side to it… is its availability in convenience stores or gas stations or things of that sort,” says Jessica Rivera, PharmD, DABAT, a clinical pharmacist and clinical toxicologist at the University of Alabama at Birmingham. “It’s readily accessible without regulations.”
Tianeptine, commonly known as Coaxil or Stablon in its prescribed form, is an atypical antidepressant, meaning it doesn’t quite fit under any of the other umbrellas of antidepressants. These drugs are mostly outdated and have been replaced with their more modern, less side-effect producing counterparts, like selective serotonin reuptake inhibitors, or SSRIs. While tianeptine is looped in with antidepressants by doctors around the globe, its effects go beyond mood boosting.
“Its true mechanism of action is not completely or well understood,” says Rivera. “What we’ve seen is it does have activity at the Mu opioid receptor, which is where a lot of our opioid agents work and activate.”
Opioids are typically prescribed for pain relief, most notably under the brand names OxyContin and Vicodin. Other opioids, like heroin and fentanyl, are illegal. They are known to create a morphine-like state of consciousness, producing a relaxed and happy feeling, contributing to its addictive quality. According to the National Library of Medicine, nearly three million Americans are addicted to opioids.
Tianeptine attaches to the same receptors in the brain as an opioid, typically producing a similar effect, which is part of what makes the drug so appealing. However, so much about the drug is still yet to be discovered.
Is Tianeptine Legal?
Tianeptine is not approved by the FDA for prescription regulation in America, but is used as medicine in other countries in Europe, Asia, and Latin America. The approval process is rigorous, and research surrounding tianeptine has not yet met FDA regulatory requirements.
When used through a prescription in foreign countries, dosages run around 30 to 50 milligrams per day. In cases of recreational usage in the United States, users have reported taking an upward of 3,000 milligrams per day, according to the Journal of Analytical Toxicology.
Rivera and her colleagues recently performed a study where they tapped into the back pages of Reddit to better understand why tianeptine users seek the drug.
“What we found fascinating is that a lot of them would use the phrase ‘just kind of chasing the okayness’,” says Rivera. “So not necessarily looking for particularly a high, but maybe trying to negate the negative effects of withdrawal.”
Is Tianeptine Dangerous?
The drug has a very short half-life, which means its effects don’t last very long in the system. This leads users to increasing dosages and using more often. Users plunge into deep downward spiral, needing more and thus using more. This spiral makes it nearly impossible to give up the drug, especially when withdrawal symptoms overpower the desire to quit, says Rivera.
Overuse has led to many hospitalizations, and even deaths. In most of these cases, the deaths were ultimately the result of respiratory depression, when breathing slows to an inefficient state.
“If you dig into the sporadic cases of death, a lot of them resulted from respiratory depression, which you wouldn’t necessarily think about with a kind of run-of-the-mill antidepressant,” says Rivera. “And so with increasing doses you can definitely see a pretty significant opioid-like picture with lethargy and shallow breathing.”
Hospitalized tianeptine users exhibit similar symptoms to that of opioid withdrawal, including decreasing heart rate and even severe agitation. Narcan, a quick acting injection most utilized to reverse opioid overdose symptoms, has been seen to be an effective treatment for a tianeptine overdose.
Michigan headed the fight for regulation of tianeptine by passing Public Act 107 in 2018, adding the drug to its list of controlled substances. Several states, including Alabama, Tennessee, Minnesota, and Georgia have since followed suit.
Case numbers in these states have “precipitously declined” with state regulation, says Rivera. Its popularity in these states have, luckily, led to quicker regulation. Most states, however, are just now seeing an uptick in usage.
“We are aware of other states that are either just now starting to see some of these trends or have been seeing continued increasing trends given its lack of regulation,” says Rivera. Until more states achieve this regulation, it is important to remember that just because it’s available, doesn’t mean it’s safe.
Cori Ritchey, NASM-CPT is an Associate Health & Fitness Editor at Men’s Health and a certified personal trainer and group fitness instructor. You can find more of her work in HealthCentral, Livestrong, Self, and others.
