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Have You Heard of “Gas Station Heroin?”

A gas station with an associated Food Mart. It's a bright, sunny day and two date trees are in the background.

Another unregulated drug is lurking around the shelves of energy drinks and beef jerky at your local convenience store. It is an antidepressant called tianeptine but has been dubbed “gas station heroin” because of its opioid-like effects at high doses. Calls to poison centers are on the rise and area hospitals are describing cases of overdose and withdrawal. 

Tianeptine is available online or at gas stations, convenience stores, and smoke shops under many names including ZaZa Red, Tianna Red, and Neptune’s Fix, to name a few. It is not approved for use by the US Food and Drug Administration but it has been approved by other countries to treat depression. In the US, it has made its way into dietary supplements and illicit substances that evade regulatory oversight. Individuals have reported taking tianeptine for recreational abuse, improved mood, cognitive enhancement, or self-treatment of withdrawal symptoms from opioid use disorder. Since abuse has increased, a few states have passed specific regulations or prohibitions on tianeptine sales. 

PHARMACOLOGY

Tianeptine was developed decades ago and classified as an atypical tricyclic antidepressant because of its similarities with the basic TCA structure (see below). However, its mechanism of action has been found to be different from TCAs. At low doses, tianeptine functions as an antidepressant by modulating glutamate, but at high doses it has the potential for abuse as a full mu- and weak delta-opioid receptor agonist.

Tianeptine
Amitriptyline

 

Heroin

 

PHARMACOKINETICS

Tianeptine is rapidly absorbed and is highly protein bound. It is quickly distributed before being metabolized in the liver and then eliminated by the kidneys. The half-life of tianeptine is 2.5 hours. 

DOSING & ADVERSE EFFECTS

In countries where it is used therapeutically as an antidepressant, the usual dose is 12.5 mg tablets three times daily with meals or a range of 25 to 50 mg per day. Much higher doses are needed to agonize mu opioid receptors and achieve the intended euphoria. Recreational doses have reached into the thousands of mg, sometimes exceeding 100 times the therapeutic range. 

In clinical trials and post marketing evaluation outside of the US, side effects reported include:

  • CNS: somnolence, headache, dizziness, nightmares, insomnia, tremor, extrapyramidal disorder, dyskinesia, suicidal thoughts
  • GI: anorexia, dry mouth, nausea, abdominal pain and constipation
  • CV: tachycardia, chest pain
  • Other: hyponatremia, increased liver enzymes and hepatitis

MISUSE, ABUSE, AND OVERDOSE

Tianeptine is misused or abused for its CNS effects including euphoria and an opioid-like high. Individuals often require increasing doses to achieve the same high and may experience withdrawal upon cessation. Overdose can be fatal and may occur following escalating doses or as deliberate self-harm. Based on case reports in the literature, overdose symptoms include nausea, vomiting, drowsiness, agitation, confusion, sweating, tachycardia, hypertension, restlessness, CNS and respiratory depression, and coma. One case demonstrated psychosis in a female with preexisting psychiatric history; her psychosis resolved 2 days after discontinuing tianeptine. Some cases are complicated by adulterants found in the tianeptine samples such as synthetic cannabinoids, barbiturates, and other illicit substances. Other cases have shown EKG changes (prolonged QT and QRS intervals), seizures, hypotension, and cardiac arrest, although it is not clear if tianeptine was the sole cause of these symptoms. Adding to the complexity of the clinical picture, individuals will often abuse other substances with tianeptine to enhance the pleasurable effects. 

MANAGEMENT OF OVERDOSE & WITHDRAWAL

Because of its similarities to opioid overdose, naloxone has been effective in treating tianeptine overdose. Follow the usual naloxone protocol:

  • The typical initial dose of IV, IM, or Sub-Q naloxone is 0.4 mg. However, 2 to 4 mg initial dose is often given if fentanyl or another highly potent agent is suspected, as in emergency rooms or by EMS. Repeat doses every 2 to 3 minutes as needed. Response should be rapid if the diagnosis is correct and the naloxone dose is adequate. If no response after 10 mg total, consider other cause of respiratory depression.

Withdrawal symptoms include anxiety, agitation, nausea, vomiting, diaphoresis, lacrimation, and yawning. Case reports have demonstrated treatment of withdrawal symptoms with benzodiazepines, antipsychotics, and clonidine. As with opioid use disorder, buprenorphine/naloxone may help taper individuals off tianeptine use and case reports have shown success following similar protocols.

Routine urine drug screens do not detect tianeptine. Accurate analysis for clinical purposes can be done by large clinical labs using GC-MS; this is typically a “send out.”  Urine drug screen tests for tianeptine can be found on the internet but none are FDA-approved and their reliability is uncertain. 

The Missouri Poison Center is here to help 24/7 by calling 1-800-222-1222. Our specially trained nurses, pharmacists, and toxicologist can offer information on tianeptine and provide the most up-to-date information regarding exposures and treatment.

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