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Resources for Recovery
Published in Sandra Rasmussen, Developing Competencies for Recovery, 2023
The Drug Enforcement Administration is a United States federal law enforcement agency under the U.S. Department of Justice tasked with combating drug trafficking and distribution within the U.S. It is the lead agency for domestic enforcement of the Controlled Substances Act, sharing concurrent jurisdiction with the Federal Bureau of Investigation, the U.S. Immigration and Customs Enforcement, and U.S. Customs and Border Protection. The DEA has sole responsibility for coordinating and pursuing U.S. drug investigations both domestically and abroad. Check out its useful Drug Fact Sheets from amphetamines to U-47700 (“U4,” “pink,” or “pinky,” a highly potent synthetic opioid).
Misuse, Recreational Use, and Addiction in Relation to Prescription Medicines
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Francesco S. Bersani, Claudio Imperatori
In relation to synthetic opioids, special concerns arise from the diffusion of substances of such classes which were originally developed as pharmaceutical products but are nowadays used exclusively for recreational purposes. U-47700 is a potent μ-opioid receptor agonist (approximately 7.5 times more potent than morphine) developed by Upjohn in the 1970s and never studied in humans (Coopman & Cordonnier, 2018). Sold online as a ‘research chemical’ or hidden among spice-like herbal incenses (Coopman & Cordonnier, 2018), U-47700 is increasingly used recreationally, and several cases of fatal intoxication related to it have been recorded since 2016 (Coopman, Blanckaert, Van Parys, Van Calenbergh, & Cordonnier, 2016; Elliott, Brandt, & Smith, 2016; McIntyre, Gary, Joseph, & Stabley, 2017).
New synthetic opioid cyclopropylfentanyl together with other novel synthetic opioids in respiratory insufficient comatose patients detected by toxicological analysis
Published in Clinical Toxicology, 2019
Dieter Müller, Hartmud Neurath, Merja A. Neukamm, Maurice Wilde, Caroline Despicht, Sabine Blaschke, Marcel Grapp
In comparison with the typical therapeutic serum concentration of fentanyl and post-mortem concentrations, the concentration of cyclopropylfentanyl of 51 ng/ml found in case 1 is likely to be in the lethal range. The opioid U-47700 has been developed after AH-7921 in the 1970s and is known for a 7.5 times higher antinociceptive activity than morphine [21]. Numerous overdose reports describe acute intoxications and fatalities due to the misuse of U-47700 [14,22–28]. The serum concentration of U-47700 (7.2 ng/ml) is lower compared with findings of Coopman et al. (13.8 ng/ml-subclavian blood) [23], and much lower than in other fatal cases described by Dziadosz et al. (525 and 819 ng/ml-femoral blood) [25] or Lehmann et al. (1.520 ng/mL-femoral blood) [27]. Higher concentrations of N-desmethyl- and N,N-didesmethyl metabolites may indicate rapid metabolisation or a consumption some time ago. The concentrations of 2-fluoroiso- or 4-fluoroiso-butyrfentanyl and butyrfentanyl might also be in the active range.
The role of take-home naloxone in the epidemic of opioid overdose involving illicitly manufactured fentanyl and its analogs
Published in Expert Opinion on Drug Safety, 2019
Hong K. Kim, Nicholas J. Connors, Maryann E. Mazer-Amirshahi
U-47700 is a structural isomer of AH-7921 that was synthesized by Upjohn pharmaceuticals (‘U’) in the 1970s. It was investigated as an analgesic in animal models but was never further considered for human use because of its addictive properties [61]. It is commonly referred to as ‘Pink’ and ‘U4’ and is approximately 7.5 times as potent as morphine (Table 1) [78,79]. It is reported to provide intense but brief feelings of euphoria that cause users to seek repeated administration [80]. Like AH-7921, U-47700 is also commonly sold on the Internet, by itself or as other drugs such as heroin and counterfeit tablets [78]. Since 2015, dozens of deaths have been associated with U-47700 in the United States. The compound was made a Schedule I controlled substance in 2016 [81]. Little is known about its metabolism. In one in vitro study using human liver microsomes, U-47700 was metabolized by N-demethylation and produced four metabolites, including N-desmethyl-U-47700 and N,N-didesmethyl-U-47700 [82].
Scene Safety and Force Protection in the Era of Ultra-Potent Opioids
Published in Prehospital Emergency Care, 2018
Michael J. Lynch, Joe Suyama, Francis X. Guyette
Overdose deaths from opioids have reached epidemic proportions in the United States. According to the Centers of Disease Control and Prevention (CDC), there were 52,404 drug overdose deaths in 2015 with 33,091 from opioids.1 More than 500,000 Americans died from unintentional drug overdose since 1999 making overdose the leading cause of accidental injury death in the United States.2 This trend was initially driven by prescription opioid misuse, but has since been supplanted by inexpensive and potent heroin and illicit synthetic opioids.1 While prescription opioid deaths have remained relatively stable since 2011, deaths related to heroin and illicit synthetic opioids (including fentanyl, carfentanil, and its derivatives) rose by 20.6% and 72.2%, respectively, with 2015 representing the first year in which illicit opioid overdose deaths surpassed prescription opioid deaths.2 Representative of many communities in the United States, Pennsylvania's Allegheny County, reported fentanyl related deaths surpassing heroin deaths for the first time in 20163 (Figure 1). The 2016 DEA Emerging Threat Report identified 15 synthetic opioid and fentanyl analogues including carfentanil and U-47700. Of those 15, nine were reported for the first time in 2016.4 These findings demonstrate the rapid evolution of available opioids and the surge of potent fentanyl analogues with an associated increase in mortality (Figure 2).