The rise of the ‘gas station heroin’ tianeptine


In late September of 2023, a significant development unfolded in the state of Florida as it joined the growing list of states to ban the drug tianeptine, often ominously referred to as the ‘gas station heroin’. This decision was prompted by a series of five tragic deaths recorded across the United States in a distressingly short span of time, shining a spotlight on the dangers associated with this substance.

In this blog, we embark on a journey to unravel the enigma of tianeptine, delving into its legal status, its impact on users, and, most importantly, exploring the unsettling rise in its misuse.

What is tianeptine?

Tianeptine is an antidepressant medication designed to alleviate the symptoms of depression. Unlike many other antidepressants, which belong to the selective serotonin reuptake inhibitor (SSRI) class, tianeptine works through a unique mechanism of action. It was once thought that its primary function was to enhance the reuptake of serotonin in the brain, leading to an increase in serotonin levels. Nowadays, studies suggest that Tianeptine works by helping the brain regain its balance. It does this by:

  • Restoring healthy brain changes in specific emotional regions.

 

  • Fixing problems with a key brain chemical called glutamate, which is essential for various functions affected during depression.

In essence, tianeptine could help the brain heal and improve its functioning in areas linked to depression. However, it can replicate the effects opioids, such as heroin, can have.

 

The legal status of tianeptine

Below, we show a list of the countries where tianeptine is legal, not available or available via prescription. Please note that these laws could change in the near future, especially after a recent ban in California.

 

 

Country

 

 

Tianeptine Legal Status

 

United States

 

Not approved by FDA; Schedule II controlled substance in some states

Canada Not approved for sale
 

United Kingdom        

Not approved for use
Australia

 

Not approved for use

 

Germany

 

Available by prescription

 

France

 

Available by prescription

 

India

 

Available by prescription

 

Russia

 

Available by prescription

 

Brazil

 

Available by prescription

 

Mexico

 

Available by prescription

 

Japan

 

Available by prescription

 

Controversy in the US

It’s important to note that in the United States, tianeptine is not approved by the Food and Drug Administration (FDA) for medical use. Its sale as a dietary supplement or research chemical is not regulated. This has led to a situation where tianeptine can be found in various forms and brand names, often in unconventional places, such as petrol stations. This is where the nickname ‘gas station heroin’ came from initially.

One of the commonly encountered brand names for tianeptine products in the US is “ZA ZA”.

These products are marketed as dietary supplements or nootropics and are sometimes labelled with impressive claims about their potency, such as containing up to 700mg of tianeptine per dose. It’s worth noting that such high doses are significantly greater than what is typically prescribed for depression in other countries, where doses are generally 12.5mg 3 times per day.

So, why are we focusing on how the US is controlling the drug? The absence of proper regulations for such a potent substance allows individuals to consume it without restrictions. Consequently, this has resulted in an increase in substance abuse and widely recognised cases of addiction.

Potential for misuse

Tianeptine carries a notable potential for misuse, primarily stemming from off-label use and its potential for abuse and dependence. When used off-label, outside the scope of its approved indications, tianeptine may pose health risks. Unsupervised or improper use can lead to adverse effects, including sedation, dizziness, and gastrointestinal issues.

Tianeptine has gained notoriety due to its potential for misuse and addiction. In some cases, individuals may take higher doses than prescribed, seeking euphoric effects, leading to addiction and withdrawal symptoms upon cessation. This misuse can result in severe health consequences and necessitate professional intervention.

 

Why are some abusing tianeptine?

Tianeptine has gained popularity as a recreational drug in some regions. There are several reasons why people might abuse tianeptine:

  • Euphoria and mood enhancement: Tianeptine can produce euphoric and mood-enhancing effects, especially when taken in higher doses than prescribed. Some individuals abuse it to experience these pleasurable sensations.

 

  • Opioid-like effects: At high doses, tianeptine can act on opioid receptors in the brain, leading to pain relief and feelings of relaxation. This similarity to opioids makes it appealing to some individuals, especially those with a history of opioid addiction.

 

  • Easy accessibility: Tianeptine is available without a prescription in some countries or can be obtained through online sources. This easy accessibility makes it more likely for people to misuse and abuse the drug.

 

  • Lack of regulation: Tianeptine is not regulated as strictly in some countries as many other substances with abuse potential, making it easier for individuals to acquire and misuse it.

 

  • Self-medication: Some individuals may turn to tianeptine as a form of self-medication for anxiety, depression, or pain without a prescription or proper medical guidance.

 

  • Lack of awareness: Some people may not be aware of the potential risks associated with tianeptine misuse or may underestimate its addictive potential.

 

Case study- Brandon

This is Brandon, a former tianeptine addict. He made an appearance on the US news show ‘The Doctors’ in February 2021 to talk with an investigative producer about his addiction to the drug.

The producer, Leslie Marcus, asked about why Brandon started to use tianeptine in the first place. Brandon stated he initially started them as an alternative to opiate replacement therapy.

Brandon: Wow, I got the relief that I wanted, but it was too good of a relief.

Leslie: How similar do they feel to opioids?

Brandon: Oh, it was every bit as good to me. I just didn’t know what was ahead of me.

Leslie: So let’s talk about what was ahead of you. So you’re going back to the same gas station and buying up pills; tell me about that.

Brandon: I would take five pills one time, seven pills, eight pills the next time. I was taking probably six bottles a day. (Shows bottles of tianeptine) I’ve just taken those in about six weeks. 100 to 120 pills a day.

When asked about the withdrawal symptoms from tianeptine, Brandon was able to recall his shocking experience:

Brandon: The withdrawal was so bad. I was not enjoying it (tianeptine) anymore. I’m just taking them not to get sick; it was terrifying. Stomach cramps, you’re burning up, you’re freezing, you’ll vomit, unpredictable body jerks.

So why was Brandon experiencing such strong withdrawals and such a strong desire to consume so many pills?

The science behind why tianeptine is so addictive

Tianeptine mainly affects how neurotransmitters work in the brain, especially serotonin. Unlike opioids, which mainly target specific receptors, tianeptine seems to involve changing how another chemical called glutamate works. Tianeptine helps increase the amount of serotonin available in the brain by making it stay in the gaps between nerve cells longer. This action is opposite to that of traditional SSRIs (Selective Serotonin Reuptake Inhibitors).

Tianeptine’s modulation of serotonin levels can lead to mood elevation and reduced symptoms of depression.

The science behind tianepetine’s withdrawals

These withdrawal symptoms can be severe and challenging to manage. The science behind tianeptine withdrawal involves both biological and psychological factors.

Withdrawal symptoms

Tianeptine withdrawal symptoms can include:

  • Depression and anxiety: Tianeptine is often used to treat depression and anxiety, so when it is withdrawn, individuals can experience a rebound effect, leading to increased depression and anxiety.

 

  • Flu-like symptoms: Withdrawal may manifest as flu-like symptoms, such as muscle aches, sweating, chills, and fatigue.

 

  • Mood swings: People going through tianeptine withdrawal can become irritable and experience mood swings.

 

  • Gastrointestinal distress: Nausea, vomiting, diarrhoea, and abdominal cramps are common withdrawal symptoms.

 

  • Insomnia: Difficulty sleeping is another common withdrawal symptom, contributing to the overall distress experienced during this process.

 

  • Cravings: There may be strong cravings for tianeptine, making it difficult for individuals to stay off the drug.

 

  • Death: There may be the possibility of the individual going into a coma, which could result in death.

 

So why do these types of withdrawals happen?

  • Issues with serotonin: Tianeptine affects the brain’s neurochemistry by modulating the reuptake of serotonin. When tianeptine is discontinued, the brain’s serotonin system can become dysregulated, leading to mood disturbances and other withdrawal symptoms.
  • Neuroadaptation: Prolonged use of tianeptine can lead to neuroadaptations in the brain. The brain becomes accustomed to the presence of the drug and adjusts its functioning accordingly. When the drug is removed, the brain’s functioning is disrupted, leading to withdrawal symptoms.
  • Psychological dependence: Tianeptine can be psychologically habit-forming. Individuals may develop a strong attachment to the drug, believing it is necessary for their well-being. This psychological dependence can amplify the severity of withdrawal symptoms as people struggle to cope without the drug.
  • Tolerance: Over time, individuals may develop tolerance to tianeptine, requiring higher doses to achieve the same therapeutic effect. This can lead to withdrawal symptoms when they attempt to reduce their dosage or quit.
  • Short half-life: Tianeptine has a relatively short half-life, meaning it leaves the body relatively quickly. This rapid clearance can contribute to the onset of withdrawal symptoms shortly after the last dose.

Final thoughts

It appears that the United States is currently facing a significant challenge with tianeptine misuse. While many individuals have experienced hardship due to its prevalence, numerous states have begun taking steps to prohibit the drug. It is disheartening to realise that some people unintentionally became addicted to tianeptine, enticed by its numerous promises. However, this situation serves as a stark reminder to the global community about the dangers associated with tianeptine. Hopefully, by learning from past mistakes, we can work towards reducing the occurrence of future ones.

Has recreational tianeptine use crept into your life?

If recreational tianeptine use has found its way into your life, reach out to UKAT’s trusted and respected addiction centre for immediate help. Your well-being is our top priority, and our experienced professionals are here to guide you on the path to recovery. Take the first step towards a healthier, happier future—contact UKAT today and let us support you on your journey to a life free from addiction. Your call can make all the difference.