Acetylfentanyl (acetyl fentanyl) is an opioidanalgesic drug that is an analog of fentanyl.[4] Studies have estimated acetylfentanyl to be 15 times more potent than morphine,[5][6] which would mean that despite being somewhat weaker than fentanyl, it is nevertheless still several times stronger than pure heroin. It has never been licensed for medical use and instead has only been sold on the illicit drug market. Acetylfentanyl was discovered at the same time as fentanyl itself and had only rarely been encountered on the illicit market in the late 1980s. However, in 2013, Canadian police seized 3 kilograms of acetylfentanyl.[7] As a μ-opioid receptor agonist, acetylfentanyl may serve as a direct substitute for oxycodone, heroin or other opioids. Common side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea, and potentially fatal respiratory depression. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.[8][9][10]
Deaths
Europe
Acetylfentanyl has been analytically confirmed in 32 fatalities in four European member states between 2013 and August 2015, Germany (2), Poland (1), Sweden (27), and the United Kingdom (2).[3]
Russia
Twelve deaths have been associated with acetylfentanyl in Russia since 2012.[3][11]
United States
The Centers for Disease Control and Prevention (CDC) issued a health alert to report that between March 2013 and May 2013, 14 overdose deaths related to injected acetylfentanyl had occurred among intravenous drug users (ages between 19 and 57 years) in Rhode Island. After confirming five overdoses in one county, including a fatality, Pennsylvania asked coroners and medical examiners across the state to screen for acetylfentanyl. As a result of this investigation, Pennsylvania confirmed at least one acetylfentanyl overdose death and attributed at least 50 fatalities to either fentanyl or acetylfentanyl during the first half of 2013.[12][13] In July 2015, the DEA informed about 52 confirmed fatalities involving acetylfentanyl in the United States between 2013 and 2015.[14]
As an analog of fentanyl, acetylfentanyl is a Schedule I controlled drug.[1]
China
As of October 2015, acetylfentanyl is a controlled substance in China.[16]
United States
Acetylfentanyl is a Schedule I controlled substance as of May 2015.[17]
Switzerland
As of March 2023[update], acetylfentanyl is a controlled substance in Switzerland.[18]
United Kingdom
Acetylfentanyl was made a class A drug as an analogue of fentanyl in 1986.[19]
Overdose
Acetylfentanyl overdosage has been reported to closely resemble heroin overdosage clinically. Additionally, while naloxone (Narcan) is effective in treating acetylfentanyl overdose, larger than normal doses of the antidote may be required.[5]
Detection in body fluids
Acetylfentanyl may be quantitated in blood, plasma, or urine by liquid chromatography-mass spectrometry to confirm a diagnosis of poisoning in hospitalized patients or to provide evidence in a medicolegal death investigation. Postmortem peripheral blood acetylfentanyl concentrations have been in a range of 89–945 μg/L in victims of acute overdosage.[20][21]
^Helander A, Bäckberg M, Beck O (20 April 2016). "Intoxications involving the fentanyl analogs acetylfentanyl, 4-methoxybutyrfentanyl and furanylfentanyl: results from the Swedish STRIDA project". Clinical Toxicology. 54 (4): 324–32. doi:10.3109/15563650.2016.1139715. PMID26850293. S2CID41668288.
^ abHigashikawa Y, Suzuki S (June 2008). "Studies on 1-(2-phenethyl)-4-(N-propionylanilino)piperidine (fentanyl) and its related compounds. VI. Structure-analgesic activity relationship for fentanyl, methyl-substituted fentanyls and other analogues". Forensic Toxicology. 26 (1): 1–5. doi:10.1007/s11419-007-0039-1. ISSN1860-8965. S2CID22092512.
^Mounteney J, Giraudon I, Denissov G, Griffiths P (July 2015). "Fentanyls: Are we missing the signs? Highly potent and on the rise in Europe". The International Journal on Drug Policy. 26 (7): 626–31. doi:10.1016/j.drugpo.2015.04.003. PMID25976511.
^Ruangyuttikarn W, Law MY, Rollins DE, Moody DE (May–June 1990). "Detection of fentanyl and its analogs by enzyme-linked immunosorbent assay". Journal of Analytical Toxicology. 14 (3): 160–4. doi:10.1093/jat/14.3.160. PMID2374405.
^Drug Enforcement Administration (July 2015). "Acetyl fentanyl"(PDF). Drug Enforcement Administration Office of Diversion Control.
^Yonemitsu K, Sasao A, Mishima S, Ohtsu Y, Nishitani Y (October 2016). "A fatal poisoning case by intravenous injection of "bath salts" containing acetyl fentanyl and 4-methoxy PV8". Forensic Science International. 267: e6–e9. doi:10.1016/j.forsciint.2016.08.025. PMID27591912.
^关于印发《非药用类麻醉药品和精神药品列管办法》的通知 [Notice on Printing and Distributing the "Measures for the Scheduling of Non-Pharmaceutical Narcotic Drugs and Psychotropic Substances"]. sfda.gov.cn (in Chinese). 29 September 2015. Archived from the original on 1 October 2015. Retrieved 1 October 2015.
^Patton AL, Seely KA, Pulla S, Rusch NJ, Moran CL, Fantegrossi WE, et al. (February 2014). "Quantitative measurement of acetyl fentanyl and acetyl norfentanyl in human urine by LC-MS/MS". Analytical Chemistry. 86 (3): 1760–6. doi:10.1021/ac4036197. PMID24354295.
^Baselt RC (2017). "Acetylfentanyl"(PDF). Disposition of toxic drugs and chemicals in man. Seal Beach, Ca.: Biomedical Publications. ISBN978-0-692-77499-1.
Further reading
Stogner JM (December 2014). "The potential threat of acetyl fentanyl: legal issues, contaminated heroin, and acetyl fentanyl "disguised" as other opioids". Annals of Emergency Medicine. 64 (6): 637–9. doi:10.1016/j.annemergmed.2014.07.017. PMID25153008.
