Isotonitazene is a synthetic
opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
drug from the
nitazene class and structural homolog of
etonitazene
Etonitazene, also known as EA-4941 or CS-4640, is a List of benzimidazole opioids, benzimidazole opioid, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency (pharmacology), potency of morphine in anim ...
,
which has been sold as a
designer drug
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. ...
.
It has only around half the potency of etonitazene in animal studies,
but it is likely even less
potent in humans as was seen with etonitazene (1000 times as potent as
morphine
Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
in animal models yet only 60 times as potent in humans).
Isotonitazene (obtained from an online vendor) was fully characterized in November 2019 in a paper where the authors performed a full analytical structure elucidation in addition to determination of the potency at the μ-opioid receptor using a biological functional assay ''in vitro''. While isotonitazene was not compared directly to morphine in this assay, it was found to be around 2.5 times more potent than
hydromorphone
Hydromorphone, also known as dihydromorphinone, and sold under the brand name Dilaudid among others, is a morphinan opioid used to treat moderate to severe pain. Typically, long-term use is only recommended for pain due to cancer. It may b ...
and slightly more potent than
fentanyl
Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...
.
Side effects
Side effects of benzimidazole derived opioids are likely to be similar to those of fentanyl, which include
itching
An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...
,
nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. It can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the throat.
Over 30 d ...
and potentially serious
respiratory depression
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...
, which can be life-threatening.
Isotonitazene has been detected in multiple fatalities in Europe since March 2019 and in the U.S. since August 2019, as reported by NPS Discovery, the Center for Forensic Science Research and Education, and NMS Labs.
Legal status
The US Drug Enforcement Administration issued a notice of intent to publish a temporary order to schedule isotonitazene in Schedule I of the Controlled Substances Act, which came into effect on 20 August 2020.
See also
*
BIM-018
BIM-018 is a synthetic cannabinoid that is the benzimidazole analog of JWH-018. It is presumed to be a potent agonist of the CB2 receptor and has been sold online as a designer drug.
Related benzimidazole derivatives have been reported to be ...
*
Clonitazene
*
Etonitazene
Etonitazene, also known as EA-4941 or CS-4640, is a List of benzimidazole opioids, benzimidazole opioid, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency (pharmacology), potency of morphine in anim ...
*
Etonitazepyne
*
Etazen
*
Metonitazene
*
Protonitazene
Protonitazene is a benzimidazole derivative with potent opioid effects which has been sold over the internet as a designer drug since 2019, and has been identified in various European countries, as well as Canada, the US and Australia. It has bee ...
*
Secbutonitazene
References
{{Opioids
Analgesics
Abandoned drugs
Designer drugs
Benzimidazole opioids
Diethylamino compounds