30 Jan FDA Warns Against Gas Station Heroin
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.
- In countries where tianeptine is prescribed to treat depression, 25 to 50-mg daily doses are standard.
- The work reported in this manuscript was supported by a VA Merit Review Award and a grant from I.R.I. Servier.
- We became aware of a cluster of 34 patients in New Jersey who became ill following ingestion of the tianeptine containing-product Neptune’s Fix, the rate of which (4.6 cases per month) far exceeded the background rate for this substance of 0.5 cases per year.
- Researchers have also hypothesized that depression involves a disruption of long-term synaptic plasticity 36,121.
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“Higher doses can produce euphoria, and some countries have restricted how tianeptine is prescribed and dispensed or revised the drug label to warn of possible addiction,” Makary said. “FDA recommends that health care professionals encourage patients to avoid all products containing tianeptine, including those claiming to treat an ailment or disorder.” Tianeptine’s actions do not appear to involve the modulation of stress-induced changes in HPA activity. We previously reported that tianeptine blocked the stress-induced impairment of spatial memory without affecting the stress-induced increase in glucocorticoid levels.
- From June 2023– February 2024 we prospectively surveilled tianeptine exposures reported to NJPIES, recorded demographic and clinical information, and recruited samples for testing.
- This case series describes an outbreak of 41 cases of tianeptine exposure reported to NJPIES from June 2023– February 2024, a marked increase compared with the poison center’s historical average.
- Worldwide, it is responsible for the most significant proportion of disease burden related to disability, measured as years lost to disability (YLD) 2.
- The most commonly administered therapies included fluids (35.1%), benzodiazepines (27.2%), and oxygen (10.5%) (Table 2).
Environment
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.
Chronic Use and Withdrawal
In the case of tianeptine-containing substances, they are commonly advertised as nootropics that provide cognitive enhancement 21. The manufacturers have even gone so far as to claim that they can reduce the symptoms of opioid withdrawal. However, the drugs can also be addictive, trading one addiction for another 17, 19. Glutamate has been implicated in neural mechanisms related to the pathophysiology of MDD 12.
FDA Issues New Warning on Tianeptine
One patient abruptly ceased tianeptine use, and developed a withdrawal syndrome consistent with opioid withdrawal, characterized by piloerection, vomiting, diarrhea, and dilated pupils. Six bottles, a mix of open and sealed, labeled “Neptune’s Fix Elixir,” were collected from patients in two reported cases. All six bottles contained a dark liquid and were labeled with an ingredients list containing tianeptine, kava (Piper methysticum), magnesium, solvents (propylene glycol, vegetable glycerin, and/or water), and flavoring. Four were cherry flavored (with three different label types) and two were tropical flavored. The samples were sent to the Center for Forensic Science Research and Education (Horsham, PA) for comprehensive chemical analysis of drugs and toxicants. Samples were prepared and dual analyzed using an Agilent Technologies gas chromatograph mass spectrometer (GC-MS) and a SCIEX liquid chromatograph quadrupole time-of-flight mass spectrometer (LC-QTOF-MS).
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.
Peek inside new convenience stores to uncover the best in retail store design across North America. Become a CSP member today and unlock exclusive benefits, including unlimited access to all of our content. The authors declare that they have no conflicts of interest nor financial disclosures relevant to this study. Data analyzed in this study were from the National Poison Data System, which is owned and managed by America’s Poison Centers. Department of Health and Human Services.Use of trade names and commercial sources is for identification only and does not imply endorsement by the U.S.
Study Population and Data Collection
Working standard solutions of both drugs in methanol were created, and tianeptine was mixed with 250 µg/ml vilazodone to form a tianeptine concentration of 10–100 ng/ml. A 1000 µg/ml concentration of tianeptine in methanol was created from 12.5-mg tablets to be tested against the standard via spectrofluorimetry. The authors reported success in determining and quantitating tianeptine concentrations from the sample with high fidelity.
Quantitation was performed through liquid chromatography-tandem mass spectrometry (LC-MS-MS) using a binary gradient of 0.1% formic acid in water and 0.1% formic acid tianeptine products linked to serious harm, overdoses, death in acetonitrile. The authors noted the difficulty in recovering tianeptine because it comprises both active acidic and basic groups. However, fragmentation was not impeded, and two ion transitions were successfully acquired.
Tianeptine: a review of its use in depressive disorders
Medical journals and reports to the FDA suggest that bad effects may occur when tianeptine is taken at doses higher than those prescribed in the countries where the drug has been approved. These reports describe U.S. consumers taking daily doses between 1.3 and 250 times the daily tianeptine dose typically recommended in products approved in other countries. Tianeptine is a non-prescription antidepressant that has become a popular method of getting high in the US in the past decade. It’s even been found in powder form in counterfeit pills of hydrocodone and oxycodone. Some products market dietary supplements containing tianeptine under the brand names Tianaa, Tianna Green, Tianna Red, Tianna White, and ZaZa.
Additionally, the same chronic stress that leads to hypertrophy of cells in the amygdala increases the expression of anxiety-like behaviors in rats tested in the elevated plus maze 197,198. In general, studies have reported significant reductions of hippocampal and prefrontal cortex volumes in depressed patients 74,111,194. The hippocampus is a medial temporal lobe structure which is important for declarative memory in humans 49,182 and spatial working memory in rodents 20,21,79,128,129,207. The prefrontal cortex is located in the anterior portion of the frontal lobe and plays an important role in complex cognitive processes, such as planning, decision-making and behavioral flexibility 13. Depressed individuals exhibit impaired performance on hippocampus- and prefrontal cortex-dependent cognitive tasks, which corresponds with reduced or abnormal activity in each of these brain regions when depressed patients engage in such tasks 47,126.