Introduction

When it comes to recreational drugs, there are literally countless different chemicals that can be pleasurable and abusable. While there are certainly “main” ones that tend to flood the streets, with fentanyl being a good example in the last decade, chemistry shows no bounds: Federal and state laws in America have been playing catch-up with recreational chemicals and their scheduling for a very long time. A chemical subject to this scrutiny recently is an atypical French antidepressant called tianeptine.

What is Tianeptine?

Tianeptine (trade names: Stablon, Coaxil) is an atypical tricyclic antidepressant that was discovered in the 1960s by the French Society of Medical Research. Tricyclic antidepressants are somewhat different from SSRI antidepressants like Prozac and Lexapro, and have been around for much longer. Tianeptine has many mechanisms of action, but perhaps the most notable is that it can bind to μ-opioid receptors as a full agonist (similar to drugs like codeine and morphine.)

Tianeptine has been widely prescribed outside of the western world since around the mid-twentieth century. In these regions, it has long been available at the standard 12.5mg dose in order to treat things like depression, anxiety, asthma and irritable bowel syndrome. Tianeptine has negligible opioid activity (and is mostly serotonergic) when used at the standard therapeutic dose of 12.5mg. In the dose range of 50mg – 100mg, it becomes very recreational as essentially an opioid drug.

Tianeptine Abuse

Between 1989 and 2004, in France 141 cases of recreational use were identified, correlating to an incidence of 1 to 3 cases per 1000 persons treated with tianeptine and 45 between 2006 and 2011. The main reason for recreational use is to achieve an anxiolytic effect. According to Servier, stopping of treatment with tianeptine is difficult, due to the possibility of withdrawal symptoms in a person. The severity of the withdrawal is dependent on the daily dose, with high doses being extremely difficult to quit.

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The abuse of tianeptine has been documented since around the 1990s. In 2001, Singapore’s Ministry of Health restricted tianeptine access to psychiatrist-prescribed only after concerns of widespread abuse. Bahrain made it a controlled substance in 2003 for very similar concerns.

Furthermore, France began treating Stablon as a controlled substance in 2012 in response to widespread abuse. The manufacturer Servier had already modified the Stablon packaging in 2007 after being pressured to by the French Health Products Safety Agency over dependency fears.

In Russia

Tianeptine has been intravenously injected by drug users in Russia. This method of administration reportedly causes an opioid-like effect and is sometimes used in an attempt to lessen opioid withdrawal symptoms. Tianeptine tablets contain silica and do not dissolve completely. Often the solution is not filtered well thus particles in the injected fluid block capillaries, leading to thrombosis and then severe necrosis. Thus, in Russia tianeptine (sold under the brand name “Coaxil”) is a schedule III controlled substance in the same list as the majority of benzodiazepines and barbiturates.

(source)

Tianeptine in America

In places like the United States and Canada, tianeptine is mostly unrecognized as a drug. American users have access to bulk amounts of powder (by the gram) on the “clear web”, usually not treated as a consumable / dietary supplement in a commerce sense in order to please the FDA.

Many Americans might have seen tianeptine mentioned on the news when certain gas station / head-shop brands became popular and were getting users hooked. Some of these products have been marketed as being for research purposes and unapproved for human consumption- but others were sold as dietary supplements. Well known brands across the country include “ZA ZA” and “Tianna“. It is not usually advertised exactly how much tianeptine is in each of these product’s capsules, but many are certain that it must exceed a therapeutic 12.5mg dose.

Scheduled in Michigan

The Center for Disease Control in America became publicly concerned about tianeptine in 2018, when they released a paper regarding it’s spike in nationwide abuse and corresponding poison control calls. The CDC’s numbers show that said tianeptine-related calls spiked dramatically in 2015, from where they continued to become more frequent. During the same year, Michigan became the first state to schedule it (the sodium form) as a schedule II controlled substance.

Pending Scheduling in Alabama

In February of 2020, a bill was initially introduced in Alabama that would make tianeptine a schedule II controlled substance should it pass. As of June 2020, the bill has received 102 “Yea” votes and just 1 “Nay” and is only one step away from finalization. This comes after a local controversy surrounding the gas station brand “Tianna” and users becoming addicted to it.

Safety Profile & Excessive Dosing

While opioids tend to depress the respiratory system at high enough doses, leading to overdose; tianeptine tends not to have this effect. When a user exceeds the therapeutic dose range, the opioid-like effects become more prevalent without a ceiling. Though an overdose for an intolerant user would be dysphoric and involve vomiting, a “traditional” opioid overdose via respiratory depression seems to be incredibly rare (when taken alone).

The lack of ceiling on effects combined with tianeptine’s duration of effects being so short means that users develop tolerance rapidly, quickly reaching incredibly high doses that are sometimes in the gram amounts.

Sodium Salt and Sulfate Forms

Tianeptine occurs in a few forms, with the two main ones being two sodium salt and sulfate. When consumed, the sodium salt reportedly has much more recreational potential (“rush”) but shorter “legs”, so re-dosing becomes frequent for those dependent. The sulfate form is reported to have a much longer duration and less of a blunt onset. This means that the recreational potential is still there, but noticeably lesser so.

Tianeptine Addict Communities are Strong

The /r/QuittingTianeptine Subreddit is a fast-growing addiction support community that is full of dependency anecdotes serious enough to make one’s skin crawl. Users frequently tell of their sky-high tolerance causing other opioid drugs, even highly abused ones like oxycodone, to be rendered ineffective entirely. Many Alabamans have been flocking here lately: A crowd divided between those hopeful for the future under the new legislation, and those that are terrified and seeking support for the impending doom of tianeptine soon being inaccessible.

Tianeptine addicts have described treating their dependency with known maintenance therapies such as methadone and Suboxone. If they can get this treatment, due to the fact that many treatment centers will only accept someone that tests positive for recognized opioids, even then success is negligible. For those that were dependent and taking mega-doses, the amount of agonist activity in which their receptors have adapted to is competitive with what even high doses of buprenorphine and methadone can offer. Addicts often describe a drug-induced hell that no other opioids can touch.

Conclusion

In a country going through an opioid crisis, it’s almost impossible for many to believe that such a dangerous and potent drug is still legal in 49 states. This is partly what leads many to using it in the first place, given that it was formerly sold through well known storefronts like NootropicsDepot and Amazon, and especially because many users could grab it from the corner store.

With the voices of those affected becoming louder, and still very little action being taken by the States, there is no just telling how long tianeptine will be as regulated as Tylenol (and sometimes even as accessible). A scary thought for those with addictive and impulsive mindsets, and for those parents out there who are worried about their child’s teenage experimentation becoming fatal.

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