Clinical Insight – Tianeptine

Use of the “gas station drug” tianeptine has been increasing nationwide, despite a public warning from the Food and Drug Administration regarding unproven medical claims on product packaging and adverse effects. This edition of Clinical Insight provides information about what this drug is, its legality, and both its desired and adverse effects.

What is tianeptine and is it legal in the US?

• • Tianeptine is an antidepressant medication that, while approved in various European and Asian countries, is not approved for any use in the United States.
  • Currently, it has not been placed on the list of federally controlled substances. However, sale of this drug has been restricted or banned in several states.
  • Marketed as a dietary supplement, tianeptine can be easily purchased online or in gas stations, smoke shops or convenience stores.

How is tianeptine supplied?

• • Tianeptine is available in various forms (e.g., liquid, tablet, and powder), and is largely taken orally, although some users report injecting or inhaling it.
  • Common brand names include Neptune’s Fix, Tianna Red, Pegasus and ZaZa. It is also referred to as “gas station heroin”. 
  • As an unregulated product, dosages may be inconsistent and can contain unsafe amounts of tianeptine or other dangerous unlisted contaminants.
  • Counterfeit pills designed to look like prescription opioids, such as hydrocodone or oxycodone, have been found to include tianeptine.

What are the uses and desired effects of tianeptine?

• • Marketed uses of tianeptine include treatment of depression and anxiety; improved memory and energy; pain relief; and alleviation of opioid withdrawal symptoms. The FDA has not found tianeptine to be safe or effective for any of these conditions.
  • In addition to its antidepressant effects at prescribed doses, tianeptine works on opioid receptors in the body. Users report that high-dose tianeptine produces opioid-like effects, such as euphoria, pain relief, improved mood, and increased energy.
  • Recreational users have reported doses of up to 7500mg, which far exceed the prescribed dose of 25 to 50 mg for depression or anxiety.
  • Tolerance to the effects of tianeptine can build quickly, leading users to increase doses rapidly. It is often used in combination with other substances, such as alcohol.

Does tianeptine cause adverse effects?

• • Adverse effects are generally associated with high doses of tianeptine. Common adverse effects from misuse of this drug include agitation, tremor, increased heart rate, excessive sweating, high blood pressure, sedation, changes in mental state and gastrointestinal distress (e.g., nausea, vomiting).
  • In more serious cases, respiratory depression, coma, or even death have been reported.
  • Tianeptine misuse can lead to tolerance and dependency. It has also been associated with withdrawal symptoms when discontinued. These symptoms can mimic the symptoms of opioid overdose or withdrawal.
  • Naloxone, the opioid rescue medication, may be effective in a tianeptine overdose due to the activity of tianeptine at the opioid mu receptors. However, tianeptine products may contain other dangerous substances that may not respond effectively to naloxone.