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Nitazenes: New Synthetic Opioids besides Fentanyl

by Cedric Dent

August 26, 2022
Paramedics and Firefighters respond to an overdose on synthetic opioids, not fentanyl but multiple Nitazenes.

The U.S. Drug Enforcement Administration (DEA) considers nitazenes to be a newly up-trending threat. Also known as benzimidazole-opioids, nitazenes are a class of synthetic opioids now being heavily trafficked. The leader among them in fatal overdose connections is fentanyl. However, the DEA reports that new data suggests fentanyl’s the tip of the iceberg. These drugs are so powerful that physicians will not prescribe them due to the high risk of overdose. Law enforcement officials attribute the increase in nitazene pedaling to the similarity between nitazenes’ effects and those of real opioids. Opioids are drugs naturally found in the opium poppy plant that impact the brain to provide pain relief and relaxation. The DEA tracks the uptrend back to 2019.

Nitazenes and the Opioid Epidemic

The DEA has seen a steady uptick in adverse health effects and even deaths correlating with nitazene use, based on toxicology reports. This is an established way to track the impact that other synthetic opioids are having on a population, too. A prime example would be fentanyl. 

Fentanyl is another synthetic opioid that authorities have been watching over the course of the last several years as it has skyrocketed to unprecedented mortality rates in the last three years. The DEA has even reported that about 40% of fatal overdoses in the U.S. are due, at least in part, to fentanyl. That’s also been the focus for harm reduction groups nationwide, too.

Nitazene, and its analogs (etonitazene, metonitazene and isotonitazene) can be 40 times more potent than fentanyl and 50 times greater than morphine, according to the Emergency and Mobile Medicine Learning Network.

A report on nitazenes from the DEA’s diversion control division pointed out that the current opioid epidemic is negatively affected by nitazene use. Right now, fentanyl is the best known example of the increase in the trafficking and misuse of new, deadly synthetic opioids. In particular, this suggests that nitazenes might rise to a future threat level comparable to that of fentanyl today. Nitazenes are synthetic opioids “with no approved medical use,” according to the DEA.

The Trafficking of NitazenesMore and more drug seizures are finding synthetic opioids and not just fentanyl but other Nitazenes.

On the street, the DEA reports that nitazenes are showing up more and more in confiscated drugs. These benzimidazole-opioids get reported to the National Forensic Laboratory Information System (NFLIS-Drug), which began recording nitazenes in significant amounts from drug seizures beginning in 2019. This actually constitutes a resurgence from the trend that persisted from 1999-2004. 

“With no approved medical use, the positive identification of these substances in toxicology cases underscore the public health threat associated with their presence on the illicit drug market,” said the DEA report.

In the last three years, NFLIS-Drug has registered 1,660 reports of nitazenes from law enforcement. Beyond that, the data correlates these nitazenes with psychoactive substances due to both being commonly confiscated together. The psychoactive drugs in question include other illegal opioids but also benzodiazepines. Some of these reports come not just from confiscations but from toxicology reports of bodily fluids of individuals who were drug screened.

Identifying the New Class

The term, nitazene, is related to the analgesic drug, etonitazene, which is a mu-opioid receptor agonist. It was first reported in 1957. It’s since been measured in animal trials as bearing well over a thousand times the potency of morphine. Etonitazene has also been the focus of illicit production and trafficking in the past.

A long list of nitazenes are now similarly being measured the same way — relative to morphine. Pre-clinical trials have recently shown that the drugs on that list are comparable to etonitazene. The DEA identifies them as butonitazene, etodesnitazene, etonitazepipne, etonitazepyne, flunitazene, metodesnitazene, metonitazene and protonitazene. All of them produced analgesic effects of varying strengths according to the data from those pre-clinical studies.

Flunitazene and metodesnitazene are the least powerful drugs on that list according to the DEA, yet they produce effects equal to morphine. The others proved far more powerful. Like fentanyl, they bind to and activate the mu-opioid receptor and mimic the operations of mu-opioid receptor agonists. 

If any of these drugs are substances you’ve tried, know that they are a quick route to fatal overdose. If you or someone you know has a habit that you think may have mortal consequences sooner or later, visit Landmark Recovery or call 888-448-0302 ASAP!

DEA Profile of Average Users

Those who typically abuse prescription opioid analgesics consistently prove to be the ones switching to nitazenes. Heroin users comprise a significant chunk of the nitazene user populace, too. The agency bases these conjectures on the types of drugs commonly found with nitazenes when confiscated in drug seizures. This also matches their findings from toxicology and coroner reports in fatal overdose cases.

In general, so-called tock-screens show benzimidazole-opioids in users’ systems alongside not only other opioids but also stimulants and benzodiazepines, too. The DEA also warns that these drugs represent serious health risks because they vary widely in potency. The variability comes from the fact that most users acquire these drugs from unregulated sources. It’s entirely possible that some users don’t even know what these drugs are when they use them.

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