Something New: Tianeptine

tianeptine

 

 

One of my doctor friends called me to ask if I’d seen any patients addicted to tianeptine. No, I had not. This was a new one for me, so I did some internet research for my readers.

Tianeptine is a medication used to treat depression, though some sources say it can be used for asthma and irritable bowel syndrome. Though structurally similar to tricyclic antidepressants, it exerts its action in a different way, via glutamate receptors. Other antidepressants are thought to work because they increase serotonin and norepinephrine levels, so tianeptine is novel in this sense.

Scientists know depression causes structural and functional changes in the brain, and some articles about tianeptine say this medication can reverse some of the stress-induced changes seen in depressed brains. We don’t fully understand all aspects of neurotransmitters and mood, and this medication shows us that serotonin and norepinephrine are not the only determiners of mood. [1, 2]

It’s an interesting medication, but not available in the U.S., Canada, or the United Kingdom. It is sold in Europe under the brand names Coaxil and Stablon. It appears to be more toxic to the liver than traditional antidepressants. And of course, if you Google tianeptine, you will see websites offering to sell it, with the fine of print of “not for human consumption,” with a wink and a nod, to protect the sellers, I assume. Mostly sites sell it in a powder form.

But what about this medication’s addictive potential? Why would people take it compulsively?

When I want to know how people are using various drugs, I go to several websites, including erowid, bluelight, and drugs-forum (www.erowid.org , www.bluelight.org , drugs-forum.com) On these sites, people record their experiences with various medications used for euphoria, and occasionally for other reasons too.

On these sites, people described a euphoria similar to opioids, though the described dose was usually far in excess of the recommended 12.5mg three times daily. One person took 500mg and described euphoria. Other people mixed it with other drugs, so it’s hard to know what effect the tianeptine had. Other people described a difficult withdrawal from tianeptine.

Kesa et. al., 2007, says tianeptine has some stimulating activity at the mu opioid receptors, thought it has a low affinity for those receptors. Apparently it takes high doses to produce euphoria, moderated through those opioid receptors.

In the Annals of Internal Medicine, 2003, Leterme et al describe five cases of tianeptine abuse. Withdrawal was said to be difficult, due mostly to anxiety.

Bence et al, Pediatrics, 2016, published a case study about a pregnant woman who was taking tianeptine, more than 650mg per day. Unexpectedly, her newborn had a withdrawal syndrome indistinguishable from opioid withdrawal, which was when her doctors discovered her tianeptine use. The baby was treated with morphine, and no mention is made of treatment for the mother until her next pregnancy, when she was admitted to a residential detox unit in her seventh month of pregnancy. Other than low birth weight, her second infant was delivered at full term with no withdrawal. Both children appear to have normal development.

From the collective experiences I read, it seems tianeptine is a weak opioid agonist, but at high doses gives an opioid effect. It sounds like people describe a typical opioid addiction after using these high doses daily for more than a few weeks. They described classic signs and symptoms of opioid withdrawal.

The doctor friend who first called me about this drug worked at an opioid treatment program. The tianeptine-consuming patient he was seeing wanted to be started on buprenorphine or methadone to treat tianeptine withdrawal. I told my friend I didn’t know enough about the drug to feel it was OK to try buprenorphine or methadone.

Since then I’ve done more research, and I suspect buprenorphine or methadone could help treat these patients, but I didn’t see any studies about their use for this addiction.

Particularly with methadone, if we prescribe it to people without a clear indication, they could later get nasty and angry about being started on methadone, a difficult drug to taper off of.

I’d like a need for a study of tianeptine-addicted patients, to see if using classic opioid use disorder treatment medications work for these patients.

Tianeptine could become the latest fad drug. Some drugs fade in and out of popularity, like the latest style of dress or music. I think this one could be a harmful fad, and we have no research about treatment.

  1. Kasper et. al., “Neurobiological and clinical effects of the antidepressant tianeptine,” CNS Drugs, 2008;22(1);15-26.
  2. McEwen et. al., “The neurobiological properties of Tianeptine (Stablon): From hypothesis to glutamatergic modulation,” Molecular Psychiatry 2010 March;15(3): 237-249.
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6 responses to this post.

  1. Posted by Bernie Rearden on October 17, 2016 at 11:19 am

    Thank you for the information, and our patients look forward to your articles.

    Reply

  2. Posted by Linda on October 23, 2016 at 9:13 pm

    It has been a big problem in russia for years now! Coaxil is used there by former heroin users, it is alot cheaper and easier to come by.
    But it makes people lose their arms and legs.

    Reply

  3. Posted by Jim Dean on July 29, 2017 at 5:06 am

    Like to know where this detox doctor was from? Because I was treated in VA Beach for this drug and I was prescribed Suboxone and it did work. Doctor said he was going to write a paper on it. I still have flash back from my withdrawal episodes, when you detox from this stuff you get a real bad chemical smell the permeates from your skin and time to time I smell something that puts me flashbacks. Bad drug for addicts but could be useful for depression but most people who are depressed seemed to be addiction prone.

    Reply

  4. I can tell you that it doesn’t just feel likeopiates at high doses. It causes the full nod, with euphoria mimicking that of morphine. It’s easily the most difficult drug to withdrawal from. And, I’ve had to withdrawal from OxyContin and suboxone. The sodium form is so fast acting that you have to redose every two to three hours. Most addicts wake up in the middle of the night in full-blown withdrawal. I have read that it’s terrible for your kidneys and liver. This drug has rapidly consumed my life. I take anywhere from five to eight grams a day, which is insane. The half life is so short that tolerance builds rapidly. Physical addiction also occurs much more quickly than traditional opiates. This drug is definitely scary, and I have a feeling we will begin to see many health issues associated with it in the near future. It’s easy to buy online, but it can be very expensive. I’ve been spending upwards of $100 a day. Tonight I took my last dose. I have clonopin and loperamide to help with withdrawal. Using traditional opiates DOES NOT take away the windrawl. Not even a little. I imagine that’s because it’s affects different parts of your brain, along with the opiate receptors. If you’re reading this and wondering if you should try this drug, please do not. It’s a beast. I’m severely depressed and anxious. Coming off of it brings on full-blown opiate withdrawal symptoms but far stronger, along with a slew of other dopamine reuptake related symptoms such as severe anxiety, brain zaps, and terrible acid reflux. Not having it is unbearable. It’s only been four hours, and I’m ready to crawl out of my skin. The restless leg syndrome and insomnia are unbearable. I’ve been using it for eight months. So, it’s imperative that I quit now. Please, if you’re looking for something to help with depression or just to get high, stay away from this drug.

    Reply

  5. Posted by Want to be normal again on October 2, 2018 at 12:31 pm

    In this now , read it helped PTSD. Over several months, my dose became extreme. Now I am wanting off, but at times feeling normal again, never high. Please help set up some place to help

    Reply

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