Dear Doctor: What can you tell me about tianeptine, which a friend is buying online? All I know is that it's an antidepressant that people are taking instead of opioids.
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Dear Reader: Tianeptine, marketed as Coaxil or Stablon, is a prescription medication used to treat major depression in more than 60 countries in Europe, Asia and Latin America. It is also used to treat anxiety, asthma, Parkinson's disease and irritable bowel syndrome. The drug has not been approved for medical use by the U.S. Food and Drug Administration, which is why your friend is buying it online, where it is marketed as a dietary supplement or sold as a research chemical.
Human and animal studies show that tianeptine, which was patented in France in the 1960s and first marketed in 1989, is an opioid receptor agonist, as are codeine, fentanyl, hydrocodone and heroin. The drug stimulates opioid receptors in the brain, which leads to a cascade of chemical changes that, for some people, offer relief from symptoms of depression and anxiety.
However, as tianeptine came into wider use, it became evident that users were at risk of addiction, abuse and withdrawal, much as with opioids. Although even five years ago most people had never heard of the drug, statistics collected by poison control centers show that is rapidly changing. Between 2000 and 2013, there were a total of 11 calls regarding tianeptine exposure. In just the next three years, that number ballooned to 207 calls. Some addiction experts say it's no accident that tianeptine use is spiking just as new regulations are making it more difficult to obtain prescription opioids. According to the Centers for Disease Control and Prevention, the drug has "an abuse potential in former opiate drug users."
The exponential increase in tianeptine use, which epidemiologists warn is just the tip of the iceberg, has led the CDC to flag abuse of the drug as an emerging public health risk. In response, individual states are now taking steps to regulate it. At the end of 2018, Michigan became the first state to schedule the drug as illegal.
The negative effects of tianeptine are sometimes associated with abuse, but more often with withdrawal. The former occurs when users ingest significantly higher than the recommended dose, which they may do in pursuit of euphoric effects. The typical therapeutic dose is 25 mg to 30 mg. When taken in doses over 100 mg, tianeptine can mirror the effects of prescription opioids.
Many people report they seek out the drug for its calming, anti-anxiety effects. Taking too much tianeptine can cause nausea and vomiting. A tianeptine overdose can also cause slowed or irregular breathing or respiratory distress, as well as altered heart activity, all of which requires immediate emergency medical attention.
When it comes to abruptly stopping the drug, side effects can include insomnia, excitability, depression, anxiety and an inability to experience pleasure. In extreme cases, agitation, paranoia and physical outbursts have been reported. Withdrawal from the drug can be difficult and is best done with the help of addiction professionals.
(Send your questions to askthedoctors@mednet.ucla.edu, or write: Ask the Doctors, c/o UCLA Health Sciences Media Relations, 10880 Wilshire Blvd., Suite 1450, Los Angeles, CA, 90024. Owing to the volume of mail, personal replies cannot be provided.)