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.
Advertisements

2 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

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out / Change )

Twitter picture

You are commenting using your Twitter account. Log Out / Change )

Facebook photo

You are commenting using your Facebook account. Log Out / Change )

Google+ photo

You are commenting using your Google+ account. Log Out / Change )

Connecting to %s

%d bloggers like this: