What is Tianeptine?

From 2014 through 2017, there was an increase in U.S. poison control calls related to tianeptine. Indeed, this surge possibly suggests an emerging public health risk. Recreational use of this drug can cause many side effects. Deaths following the misuse of this substance have been reported. So, what is tianeptine?

Tianeptine is a prescription antidepressant in Latin America, Asia, and Europe. It is marketed as Stablon or Coaxil. It belongs to the class of medications known as tricyclic antidepressants (TCAs).

In the U.S., it has no medical approval. It is, however, purchased online by people who misuse it. This substance is available as tablets, capsules, and powder.

According to reports, this drug was first discovered by the French Society of Medical Research back in the 1960s. In addition to its effects on depression, it has also been shown to help with other conditions. There are reports of efficacy for anxiety, asthma, and irritable bowel syndrome.

The clinical effects of tianeptine abuse and withdrawal can mimic opioids. Studies show that it is an opioid receptor agonist. Hence, the similarities in withdrawal symptoms.

 

How Does Tianeptine Work?

This drug works by increasing the uptake of serotonin in the brain. As a result, it is similar in a way to a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs).

Even though tianeptine is a tricyclic antidepressant, it is somewhat atypical. Because of this, it does not have some of the side effects of most other tricyclic antidepressants. Even though it has a low propensity for abuse, this can happen.

Tianeptine helps with the treatment of depression, dysthymia, and adjustment disorder. In terms of efficacy, this drug is similar to other TCAs like amitriptyline, clomipramine, and imipramine. It is also equivalent to SSRIs like sertraline, paroxetine, and fluoxetine. For this reason, some people self medicate with this substance.

Even though this drug has beneficial uses, it can also cause adverse effects. Tolerance and withdrawal can also occur. Dependence on tianeptine during pregnancy can cause neonatal abstinence syndrome. This condition is similar to opioid neonatal abstinence syndrome. Given this, it is advisable to avoid tianeptine during pregnancy.

 

Side Effects of Tianeptine

The adverse effects of tianeptine are more similar to SSRIs and less so to TCAs. In the U.S., this drug does not have approval for medical use by the Food and Drug Administration (FDA).

The most common side effects of this drug are:

  • Abdominal pain
  • Constipation
  • Nausea
  • Dizziness
  • Headaches
  • Confusion
  • Rapid heartbeat (tachycardia)
  • High blood pressure
  • Depression
  • Difficulty sleeping
  • Nightmares
  • Weight gain
  • Agitation
  • Anxiety
  • Dry mouth

Some uncommon side effects are:

  • Blurred vision
  • Muscle aches
  • Problems with urination
  • Hot flushes
  • Tremors
  • Liver inflammation
  • Allergic skin reactions
  • Kidney failure
  • Respiratory depression
  • Coma
  • Death

 

Withdrawal Symptoms

The withdrawal symptoms of this substance are similar to those of opioids. Many people who abuse this drug tend to use high doses, hence making withdrawals worse. Withdrawal symptoms include:

  • Nausea
  • Vomiting
  • Mood swings
  • Muscle aches
  • Tearing (lacrimation)
  • Runny nose (rhinorrhea)
  • Dilatation of the pupils
  • Sweating
  • Diarrhea
  • Yawning
  • Fever
  • Difficulty sleeping

 

Who Abuses Tianeptine?

The Centers for Diseases Control and Prevention (CDC) analyzed calls related to tianeptine poisoning. The report showed most tianeptine exposures occurred amongst persons aged 21 – 40 years. About 80% of the users were males. Many of the effects of this drug were similar to opioids.

In some online forums, users of this substance describe getting a “high” from using. This experience is known as euphoria. Also, combining tianeptine with other illicit drugs seems rife. The commonest coexposure drugs are opioids, benzodiazepines, alcohol, and phenibut. Because of the clinical similarity to opioids, tianeptine has an abuse potential in former opiate drug users. Some countries have put in place bans and tighter regulations on this drug as a result.

For these reasons and more, this drug is not FDA approved in the United States. It is, however, readily available online as a dietary supplement.

The standard tianeptine dose is 12.5 mg three times a day. On the streets, however, people take as much as 500 mg to 3,000 mg daily. Thus, the risk of toxicity and overdose is high.

 

Why Do People Abuse This Drug?

Tianeptine is similar in effect to opioids. This similarity is an attractive reason for people who abuse opioids.

In recent times, there has been a tightening of the prescription of opioids. Despite this, the opioid crisis remains an issue. The recent uptick in tianeptine abuse may be related to the crackdown in opioids.

The higher prices on opiate prescriptions and stricter monitoring are causing people to seek alternatives. These reasons explain the increase in heroin addiction. There is a similar trend with kratom and tianeptine.

The ease of availability from the internet only makes this worse. Unfortunately, standard urine drug screens do not detect this drug. As a result, there is a need for specialized testing in cases of suspicion of use.

Nootropics are substances that may improve cognitive function. Other names for such compounds are smart drugs or cognitive enhancers. Tianeptine is usually sold online as a supplement that enhances mood and cognition. The effect on cognition and memory is, however, contrary to scientific studies.

 

Tianeptine Use in Foreign Countries

Prescriptions for this drug are available in several European countries, Asia and Latin America. On the other hand, prescribing is not available in Australia, New Zealand, United Kingdom, Canada, or the United States.

In 2001, Singapore put a restriction on psychiatrists prescribing tianeptine. This ban was due to the recreational potential of this drug. Also, in 2003, Bahrain classified it as a controlled substance due to misuse and abuse.

France identified many cases of recreational use in the 90s and early 2000s. As a result of this, the manufacturers of this substance modified the drug’s label. In 2012, however, France began to regard tianeptine as a controlled substance.

Interestingly, there have been reports of injecting this drug by users in Russia. Perhaps, this was done to quickly obtain the opioid-like effects or lessen the withdrawals from opioids. This drug is also now a controlled substance in Russia.

 

Control Status

In the U.S., tianeptine is not a controlled substance under the Controlled Substances Act. Except for Michigan.

In April 2018, Michigan passed Public Act 107 of 2018. This law adds tianeptine sodium to Michigan’s list of schedule II controlled substances. It was effective from July 4, 2018.

The Food and Drug Administration does not approve of this substance for medical use within the United States. So, despite the various internet claims, it is best to avoid it.

 

Treatment of Tianeptine Abuse

The treatment approach for tianeptine abuse is similar to that for opioid addiction.

Many people are turning to drugs like tianeptine due to the clampdown on opioids. The growing trend of abuse of this drug indicates the need to focus on the proper treatment of opioid use disorder.

Tianeptine has many similarities to opioids. Given this, naloxone (Narcan) is effective in reversing tianeptine overdose.

Medication-Assisted Treatment remains the gold-standard for the treatment of opioid addiction. Unfortunately, without proper treatment, people will continue to abuse alternative drugs. The main reason for this is that the cravings and withdrawals from opioids are intense.

There are two commonly used behavioral therapies for addiction to opioids. These also apply to tianeptine abuse. They are

  1. Cognitive-Behavioral Therapy
  2. Contingency Management

Cognitive-behavioral therapy helps to modify your tianeptine use expectations and behaviors. Contingency management provides rewards and incentives for positive behaviors. These therapies are, however, more effective when combined with medications. Support from family and friends is also vital.

In addition, treating the underlying cause of substance use goes a long way in addressing this addiction. Some people self-medicate with illicit drugs and supplements. They may do this because of their struggles with mental illness.  Depression, anxiety, and bipolar disorder are just a few of the issues that may need proper treatment. Thus, following up with a mental health provider is a vital component of treatment.

 

Tianeptine

Tianeptine

Conclusion

Tianeptine is a tricyclic antidepressant prescribed in Latin America, Asia, and Europe. In the U.S., it is, however, not approved for medical treatment by the FDA.

This drug is marketed as a smart drug, cognitive enhancer, or nootropic. Studies have, however, not shown this to be the case.

Tianeptine acts on opioid receptors in the brain. Tolerance and withdrawal can also occur with this substance. Due to its similarities to opioids, the withdrawal presentation and management are similar.

In the U.S., it has no medical approval. It is, however, purchased online by people who misuse it. This substance is available as tablets, capsules, and powder.

Some of the common side effects of this drug are constipation, nausea, headaches, nightmares, and dry mouth. Unfortunately, there are reports of death from using this substance.

In 2001, Singapore put a restriction on psychiatrists prescribing tianeptine. Also, in 2003, Bahrain classified it as a controlled substance due to misuse and abuse. In the U.S., tianeptine is not a controlled substance under the Controlled Substances Act, except in Michigan. It is, however, not approved by the FDA for medical use within the U.S.

The treatment approach for tianeptine abuse is similar to that for opioid addiction. Thus, naloxone (Narcan) is effective in reversing tianeptine overdose. Also, Medication-Assisted Treatment for opioids is helpful for this substance. In addition, behavioral therapies, social support, as well as treating underlying mental illness, are crucial.

Indeed, tianeptine abuse possibly suggests an emerging public health risk. It is, therefore, essential to address this issue on both public health and individual levels. Help is available, and it is crucial to get the treatment you need.