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EMCDDA states that withdrawal management/detox is the initial step, followed by drug-no cost Actual physical and social methods, like psychotherapy, geared to improving the individual’s wellbeing and independence.25
Controlled preclinical pharmacology and toxicology studies on acetylfentanyl are few, and such clinical studies are non-existent. Preclinically, acetylfentanyl has many characteristics of a mu opioid receptor agonist. It displaces 3H-etorphine binding (EC50 of 676 nM) at the mu opioid receptor, completely inhibits the mouse vas deferens stimulated twitch (EC50 of 4.42 x 10-7 M), and has antinociceptive effects in several rodent models. Acetylfentanyl can relieve signs of withdrawal in the morphine dependent rhesus monkey and thus demonstrating cross-dependency to morphine. Other preclinical tests directly pertinent to its abuse potential such as self-administration, drug discrimination, intra-cranial selfstimulation or conditioned place preference, appear not to have been reported if conducted.
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The actual dose needed to produce a behavioral effect is thought to be in the microgram range.18 One user website suggested, “If using iv then do 100-250 micros as starting iv, roughly 6-8mg of morphine IV.”19 A user at another site apparently had tried several routes of administration with acetylfentanyl.20 This user reported insufflating 10 mg and reporting, “Effects were not immediate and took a good 5-10 minutes to fully kick in. The effects were typical of this class of drugs, mildy sedating, nothing crazy. No real euphoria present, as is typical with Fentanyl itself, so this wasn’t surprising. All in all, 10mg produced a pleasant buzz that lasted around 90 minutes before a decline in effects was noticed.”20 The user subsequently apparently insufflated 15 mg of acetylfentanyl and reported that reminded him/her of heroin’s effects. This user also reported a lack of effect using 10 mg acetylfentanyl in his/her vaporizer. The user subsequently tried 10 mg acetylfentanyl intravenously and reported, “… 10mg produced very enjoyable, relaxing effects. And with the aid of two delicious beers (one chocolate stout and one pumpkin ale, both with slightly above average alcohol content) the effects could be felt the rest of the night without any inclination to redose.”
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It is clearly being non-medically used and abused, although the extent of its abuse cannot be accurately estimated given, in part, it is not routinely tested for in forensic toxicology. Controlled, clinical evidence of it inducing or maintaining physical dependence is not available, although user and treatment websites suggest that it should have much the dependence-related effects of the controlled substance, fentanyl, of which acetylfentanyl is found as an “impurity” during fentanyl’s synthesis and to which acetylfentanyl can be converted.
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Over the last few years, new synthetic opioids (NSOs), primarily fentanyl derivatives are increasingly implicated in overdose deaths, and have caused a global health concern. Among the 70,237 drug-related deaths estimated in 2017 in the US, the sharpest increase occurred among those related to fentanyl analogs with more than 28,400 overdose deaths which represents 45.2% increase from 2016 to 2017 [1, 2]. In Europe, their use appears to be geographically localized, but the number of synthetic opioids has grown rapidly since the first substance was reported in 2009. In fact, around 50 NSOs have been reported to the EU Early Warning System with 11 being reported for the first time in 2018 . From 2015 to early 2018, the European Monitoring Center for Drugs and Drug Addiction (EMCDDA) has conducted eight joint investigations with Europol on fentanyls that have caused serious concern at European level. The two agencies investigated acetylfentanyl, acryloylfentanyl and furanylfentanyl, 4-fluoroisobutyrylfentanyl (4F-iBF), tetrahydrofuranylfentanyl (THF-F), carfentanil, methoxyacetylfentanyl and cyclopropylfentanyl.
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