In countries where tianeptine is prescribed to treat depression, 25 to 50-mg daily doses are standard. Tianeptine is an antidepressant drug approved for the treatment of major depressive disorder in countries other than the US. It is classified as an atypical tricyclic antidepressant and has shown potential benefits in addressing anxiety and irritable bowel disease. However, it is important to note that tianeptine is not approved for any use by the United States Federal Drug Administration (FDA). Despite its lack of approval by the FDA, tianeptine has been distributed online and at small retail locations.
The term “gas station drugs” refers to a wide range of substances typically available for purchase from gas stations, corner stores, bodegas, mini marts, smoke shops, and the Internet. These substances may be produced commercially by drug manufacturers or in clandestine laboratories to mimic the effects of more well-known illicit/controlled substances such as marijuana, cocaine, opioids, etc. Tianeptine has made its way to convenience stores and gas station shelves, branded as “Zaza” and “Tianna Red.” It can also be obtained online from independent vendors without a prescription. Misuse of tianeptine can lead to euphoric, opioid-like highs with the potential for chronic users to develop dependence and tolerance.
- Despite lacking FDA approval for any purpose in the United States, tianeptine can still be found in certain convenience stores and gas stations 6.
- AK reports funding from the National Institute of Justice, U.S. Department of Justice, for sample analysis and salary.
- At high doses or in combination with other substances, tianeptine can be dangerous.
- Another case of tianeptine misuse was reported in late 2018, in which a 44-year-old male presented for suicidal ideation and progressively worsening depression for the previous 2 weeks.
Cannabis use in first trimester has ‘significant’ harmful effects on a fetus
In contrast, the SSRIs fluoxetine and fluvoxamine were ineffective in preventing the stress-induced changes in CA3 morphology 105, suggesting that the effects of tianeptine and SSRIs may be mediated, at least in part, by different cellular and molecular mechanisms. Additional work has shown that tianeptine also prevents the effects of chronic stress on hippocampus-dependent learning and memory 30,104,212. Investigators have yet to determine whether or not tianeptine prevents the effects of chronic stress on prefrontal cortex morphology. Considering tianeptine’s ability to block the effects of chronic stress on hippocampal structure and function, it is likely that tianeptine would exert positive effects on the prefrontal cortex, as well. Tianeptine also blocks the effects of chronic stress on hypertrophy of amygdala dendritic arbors, as well as the concurrent enhancement of anxiety-like behavior accompanying chronic stress 144. These findings may be relevant to other work reporting that chronic tianeptine treatment reduced the expression of auditory fear conditioning, an amygdala-dependent task 23.
- For instance, traditional antidepressants ameliorate depressive symptoms only in a subset of patients, despite their low levels of monoamines 12, and are largely ineffective for people with severe forms of depression 113,137.
- “Its unregulated status in the US also increases the potential for abuse or misuse, as there are no standard dosing recommendations here for this drug,” says Johnson-Arbor.
- This increases the risk of an unintentional overdose, along with other adverse side effects like lethargy, elevated blood pressure and heart rate, agitation, abdominal pain, tremors, and hallucinations.
- The clinical effects of tianeptine abuse and withdrawal can mimic opioid toxicity and withdrawal, according to the Centers for Disease Control and Prevention.
- Complex suicide involving the above combination appears unusual, and the use of tianeptine is rare 29.
Publication types
In other states, it is technically legal since it sits in a gray area – it is not FDA-approved but neither is it a controlled substance. Just because the FDA is unable to control the sale of tianeptine, does not mean that it is safe. Benzodiazepine tapers may assist in controlled withdrawal if the patient experiences difficulty completing a tianeptine taper. Lauhan et al. reported successfully using an inpatient benzodiazepine taper in a 44-year-old man who had previously failed outpatient tianeptine taper. The patient was initially administered 0.5 mg of oral lorazepam before being switched to diazepam and received 30 mg of diazepam over the 2 days of inpatient care 23.
Tianeptine Exposures Reported to United States Poison Centers, 2015–2023
Although tianeptine is not FDA approved in the United States, it is readily available for purchase online as a dietary supplement or research chemical. tianeptine products linked to serious harm, overdoses, death Several online discussion forums among users describe the euphoregenic effects of tianeptine. Users have also reported combining tianeptine with other drugs like phenibut for a potentiated effect.
Health Topic(s)
Although the mechanisms responsible for tianeptine’s clinical efficacy have only recently been elucidated, its basic pharmacokinetics have been established through decades of preclinical studies. With a half-life of only 2.5 h, tianeptine is quickly absorbed in the gastrointestinal tract. It becomes highly bound to albumin once in the bloodstream, thus having a low volume of distribution 4, 8. It is hepatically metabolized into MC3 and the biologically active MC5, which functions similarly to its parent compound 4, 7, 8. Since tianeptine is really cleared, its half-life is markedly increased in elderly patients and those with kidney disease.
Amber N. Edinoff, Saveen Sall, Eric D. Jackson, Danielle M. Wagner, Elyse M. Cornett. Kevin S. Murnane, Adam M. Kaye, and Alan D. Kaye was responsible for all revisions of the manuscript. No funding or sponsorship was received for this study or publication of this article.
Prepared Food is Your Growth Engine
A 2018 study published in Madrid reported that tianeptine use does not produce tolerance, dependence, or withdrawal, noting that the drug has a low potential for abuse. They further suggested that tianeptine could even be administered to patients who require prolonged use of morphine for its dependence-inhibiting effects 4. In partial agreement, an analysis by Bailey et al. that reviewed all accessible tianeptine clinical trial data reported that tianeptine is effective as an antidepressant, allowing for improved functionality compared to standard first-line antidepressant medications. However, it also acknowledged tianeptine’s potential for abuse and dependence when ingested at high doses due to its mu-opioid receptor agonist effects 8. While studies agree that tianeptine, at its therapeutic dose, is effective at treating depression, its opioid-like characteristics can induce euphoria at high enough doses 8.
Access this article
Tianeptine has been shown to block the stress-induced impairment of LTP in the hippocampus and prefrontal cortex, without interfering with the stress-induced enhancement of LTP in the basolateral amygdala (BLA) 72,164,173,196. Tianeptine blocked the inhibitory effects of stress on hippocampal LTP and primed burst potentiation (PBP), a low-threshold form of LTP, when it was administered before or after the stress experience 173,196. Other antidepressants, including some SSRIs, have also been reported to block the effects of stress on LTP in the hippocampus and prefrontal cortex, although these effects have been less significant and more transitory in nature 164. Tianeptine is not FDA-approved for any medical use and is commonly known as “gas station heroin” because of its availability in gas stations. Tianeptine products have been linked to serious harm, overdoses and death, the FDA said on its website. Some people may have difficulty stopping using tianeptine and may experience withdrawal symptoms.
In contrast to tianeptine, administration of the SSRI fluoxetine increased baseline and stress-induced levels of glutamate in the BLA and CeA 159. This finding may explain why SSRIs are anxiogenic early in the treatment phase and exert therapeutic antidepressant and anxiolytic effects only after a substantial delay 23,58. Moreover, investigators have shown that acute administration of the SSRI citalopram enhanced the acquisition of auditory fear conditioning, while chronic treatment with citalopram impaired the acquisition and expression of conditioned fear 23. Acute treatment with tianeptine, in contrast, had no effect on auditory fear conditioning, but when given chronically, exerted effects comparable to those of citalopram. Thus, tianeptine demonstrates long-lasting anxiolytic and antidepressant effects that are similar to SSRIs, without the adverse acute effects typically found with these agents. An alternative and well-established treatment for depression is tianeptine, an antidepressant which does not share pharmacological properties with TCAs, MAOIs or SSRIs 12,18,95,145,191.