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Opioids and Related Agents
Published in Frank A. Barile, Barile’s Clinical Toxicology, 2019
In the 1990s, fentanyl enjoyed increasing popularity as the narcotic of choice among illicit drug users, principally because of its enhanced potency (China white). At 200 times and 7000 times greater potency than morphine, respectively, α-methylfentanyl and 3-methylfentanyl also display greater potential for toxicity. The median lethal dose is about 145 µg for the former and 5 µg for the latter.* Therapeutically, fentanyl is marketed in the form of medicated patches (Duragesic Transdermal System®) for the management of chronic pain. Depending on the size of the patch and the amount of fentanyl delivered (10–40 cm2 containing 2.5–20 mg total per patch), the transdermal system can release up to 200 μg per hour.
Fentanyl and Related Opioids
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Esther Papaseit, Magí Farré, Clara Pérez-Mañá, Adriana Farré, Francina Fonseca, Marta Torrens
Regarding misuse and abuse, in the mid-70s, misuse of prescription fentanyl (pharmaceutical fentanyl, PF) was first described in clinicians and pharmacists. Shortly after, fentanyl and synthetic analogues appeared mixed with heroin or in pure form (alpha-methylfentanyl or China White, 3-methylfentanyl or Tango & Cash, synthetic heroin) whilst in the 1980s and ’90s, illicitly manufactured fentanyl (non-pharmaceutical fentanyl, NPF) appeared on the black market. Between 2005 and 2007, more than 1,000 fentanyl analogues were used as adulterants in street heroin or as heroin substitutes. At that moment, some of these derivatives formed part of the so-called ‘designer drugs’.
Licit and illicit drugs
Published in Jason Payne-James, Richard Jones, Simpson's Forensic Medicine, 2019
Jason Payne-James, Richard Jones
Some opioids are much more potent than others. Novel synthetic opioids have recently emerged on the recreational drug market. They include fentanyl (a potent narcotic analgesic) and its analogues (e.g., acetylfentanyl, acryloylfentanyl, carfentanil, α-methylfentanyl, 3-methylfentanyl, furanylfentanyl, 4-fluorobutyrylfentanyl, 4-methoxybutyrylfentanyl, 4-chloroisobutyrylfentanyl, 4-fluoroisobutyrylfentanyl, tetrahydrofuranylfentanyl, cyclopentylfentanyl and ocfentanil) and compounds with different chemical structures, such as AH-7921, MT-45 and U-47700. Fentanyl, for example, is more than 100 times more powerful than morphine, because it is a better fit for the μ1 receptor than morphine. The molecular structure of the opiate can also have an effect on routine drug screening tests. Routine drug screening tests (including the various test kits used in most casualty wards) are antibody based. The antibodies used have usually been designed to attach to morphine and will not react at all in the presence of synthetic opioids such as fentanyl. More worryingly, carfentanil – a synthetic fentanyl analogue approved for veterinary use, with an estimated analgesic potency approximately 10,000 times that of morphine and 20–30 times that of fentanyl, based on animal studies – has become available. Since 2016, an increasing number of reports describe detection of carfentanil in the illicit drug supply. Little is known about the pharmacology of carfentanil in humans. Its high potency and presumed high lipophilicity, large volume of distribution, and potential active metabolites have raised concerns about the management of people exposed to carfentanil as well as the safety of first responders. It has been associated with a number of deaths in association with other illicitly used drugs.
Underreporting of drug use among electronic dance music party attendees
Published in Clinical Toxicology, 2021
Joseph J. Palamar, Alberto Salomone, Katherine M. Keyes
Specimens were tested via published methods using ultra-high performance liquid chromatography–tandem mass spectrometry [41–43]. We tested for common drugs including cannabis (THC), amphetamine, methamphetamine, cocaine, MDMA, ketamine, PCP, heroin (6-MAM), and prescription opioids including morphine, codeine, oxycodone, hydrocodone, hydromorphine, and oxymorphone. We also tested for a variety of uncommon drugs and NPS including 19 synthetic cathinones (i.e. mephedrone, 4-MEC, methylone, 3,4-MDPV, pentedrone, 3-MMC, ethylcathinone, alpha-PVP, butylone, buphedrone, mexedrone, amfepramone, pentylone, methedrone, ethylone, naphyrone, 4-F-methylcathinone, 3,4-DMMC, alpha-PHiP) and 7 psychedelic phenethylamines (i.e. 2 C-B, 2 C-P, 25B-NBOMe, 25 C-NBOMe, 25H-NBOMe, 25I-NBOMe, 4-EA-NBOMe). We also tested for 5 other euphoric stimulants (i.e. 4-FA, 5/6-APB, 5-MAPB, PMA, PMMA) and 3 dissociative NPS (i.e. MXE, 4-MeO-PCP, diphenidine). In addition, we tested for fentanyl, 8 fentanyl analogs (i.e. carfentanyl, acetylfentanyl, furanylfentanyl, butyrfentanyl, acryloylfentanil, 4-fluorofentanyl, 3-methylfentanyl, ocfentanyl), and for 5 other opioid NPS (i.e. U-47,700, U-49900, AH-7921, MT-45, U-51,754).