TIANEPTINE: "Gas Station Heroin"

The FDA and many state health agencies are raising the alarm about tianeptine, also called “gas station heroin.”[1]  It is illegally marketed in smoke shops, convenience stores, gas stations and online as a dietary supplement, research chemical or brain enhancer. Some of the more common brand names include ZaZa, Pegasus, Neptune’s Fix and Tianna Red.

Unsupported claims have been made that it improves brain function and relieves depression and anxiety. Some people use it for its opioid-like effects to lessen physical and emotional pain. In addition, false claims have been made that it can treat Opioid Use Disorder (e.g., heroin and fentanyl addiction).

Some people using these products have experienced seizures, psychosis and loss of consciousness winding up in hospital emergency rooms. Calls to poison control are also on the rise and several deaths have been reported.[2],[3]

What is Tianeptine?

Tianeptine is a lab-made chemical that was first discovered in the 1960’s by the French Society of Medical Search. As a prescription labeled under brand names like Stablon, Coaxil and Tatinol, it is marketed as an antidepressant in other countries as a way to treat depression.  It is also being evaluated as a potential treatment for persistent depressive disorder, bipolar disorder and adjustment disorders.[4]

In countries where it is legally prescribed (outside the United States), the typical dose of tianeptine is 25mg to 50 mg per day.  When taken as prescribed, the side effects can include an upset stomach or stomach pain, constipation, headaches, dizziness, nightmares and dry mouth.

In the United States, Tonix Pharmaceuticals has just completed a phase 2 study using tianeptine to treat Major Depressive Disorder (MDD).[5] They report that, unlike other forms of the medication available in other countries, which require three doses a day, their version is a once-a-day pill. It also appears to have fewer sexual, sleep and weight gain side effects. Additional work must be completed before they can present it to the FDA for approval.

How is it misused and what are the side effects?

People misusing the substance often take very high doses of it – reportedly up to 7500mg dose as compared to a standard dose of 25mg to 50 mg used to treat depression. At higher doses, it mimics the effects of opioids (i.e., heroin, prescription pain killers).

According to researchers who combed Reddit for posts on tianeptine, the positive effects of using the substance included improved mood, contentment, more energy and pain relief.[6] Some people also noted that it was helpful as a substitute for buprenorphine and to deal with withdrawal symptoms from opioids. It is important to note that many of these posts discussed using tianeptine as part of a “stack,” which refers to an individual’s preferred combination of substances. Stacks typically included kratom, phenibut and racetams.

Here is one positive post:

“Super clear-headed. A bit more sustained euphoria than usual but not a tweaked out high (that can a be fun feeling, but not my goal as it’s counterproductive for me). Amazing focus and enhanced critical thinking. This isn’t your Daddy’s focus…we’re talking Ferrari-like mental performance and more importantly, I still have effective task prioritization with limited sidetracks. Better and faster strategic problem-solving. I negotiate in often tense environments for my job so this is huge for me. I feel I have the upper hand.”

When it came to negative effects, posts highlighted the rapid development of their tolerance to tianeptine. This means a person needs to take more of the substance to get the same effect that lower amounts used to provide. For example:

Pretty intense rush but less than 30 minutes later and you’re mixing another shot. My tolerance rose 3x fold in one day. I used 500mg the first day then 1.5g the next before my 2g was gone. Never bought more because I realized just how dangerous this one could be. I believe this is literally the worst thing you could be dependent on.”

Others stated that the substance was addictive and that it led them to relapse on opioids.  There were also mentions of overdosing. Several opioid-like withdrawal symptoms were noted, including pain, stomach upset, vomiting, diarrhea, sleep problems and lack of pleasure in anything, as well as increased depression and anxiety. One Reddit user reported:

“I was told the withdrawals were that of less than opiate withdrawal and that is not the case at all. Constantly crawling out of my skin, RLS but all over my body, horrible [IBS], sweating, nose running, hot and cold, in bed rolling around crying and screaming, in the most pain I’ve ever felt in my entire life.”

It is illegal and not approved by the FDA

Tianeptine is not legal in the United States. It has not been approved by the Food and Drug Administration (FDA) for medical use, and it is not available as a prescription medication. Regardless, products containing tianeptine are being illegally sold despite FDA warnings.[7]

Reports have noted that illegally produced tianeptine may have other ingredients mixed in, ranging from substances like barbiturates to brown sugar. One Reddit user wrote:

I bought a bottle of TD red. I opened the bottle and the smell was weird so I opened up a capsule onto paper and it was brown sugar. I buy from the same shop and they know me and I know them personally. I went back in, opened up a capsule in front of the owner and showed him. It was brown sugar. Now I am scared to even take this crap ever again because now I know you could be getting God knows what…” [8]

Safety measures

Given that tianeptine is not regulated and it’s very difficult to know what is actually in the product, the safest course of action is not to use it.  There are many approved treatment options for depression, anxiety, substance use and other health issues; consider reaching out to your healthcare provider to explore them.

Because tianeptine attaches to the same receptors in the brain as opioids, naloxone (i.e., Narcan, which can reverse an opioid overdose) may be able to reverse an overdose from tianeptine if used in time. Learn more about how to get and use naloxone.

Buprenorphine, a medication to treat opioid use disorder (MOUD), may help treat tianeptine dependence.[9] Learn more about MOUD.

If you have more questions or need help with a loved one using tianeptine, you can connect to our support services, including our helpline, here.