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Naloxone Use in the Opioid Epidemic
Published in Sahar Swidan, Matthew Bennett, Advanced Therapeutics in Pain Medicine, 2020
According to the U.S. Centers for Disease Control and Prevention,4 the rise in opioid overdose deaths can be outlined in three distinct waves (Figure 24.1): The first wave began when opioid prescribing increased in the 1990s, with overdose deaths involving prescription opioids (natural and semi-synthetic opioids and methadone) increasing since at least 1999.The second wave began in 2010, with rapid increases in overdose deaths involving heroin.The third wave began in 2013, with significant increases in overdose deaths involving synthetic opioids—particularly those involving illicitly manufactured fentanyl. The illicit fentanyl market continues to change, and fentanyl can be found in combination with heroin, counterfeit pills, and cocaine. Carfentanil, a synthetic opioid used to tranquilize large animals, is also becoming more popular on the illicit market, used to “cut” heroin and increase profits for dealers. Carfentanil is estimated to be 100 times more potent than fentanyl and 10,000 times more potent than morphine. It has a quick onset and is short-acting.
Toxicology
Published in Christoph Schroth, Peter Phillips, 100 Cases in UK Paramedic Practice, 2018
Christoph Schroth, Peter Phillips
Fentanyl is a potent opioid analgesic that is approximately 80–100 times more potent than morphine, so very small doses are likely to have significant effects. Two other variations currently available are carfentanil and acrylfentanil. Carfentanil is said to be about 100 times more potent than fentanyl, about 50 times more potent than heroin and roughly 10 000 times more potent than morphine. Acrylfentanil is only about 50 times as potent as morphine, but according to some sources it is supposedly resistant to naloxone hydrochloride. This is not supported by many sources, but should be kept in mind when treating fentanyl-related overdose patients.
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.
A potential paradigm shift in opioid crisis management: The role of pharmacogenomics
Published in The World Journal of Biological Psychiatry, 2022
David Eapen-John, Ayeshah G. Mohiuddin, James L. Kennedy
Carfentanil is another synthetic opioid often compared to fentanyl. It is traditionally used as part of tranquiliser medications for large animals and has essentially no indications for human use. It is a very specific MOR agonist and follows the same major metabolic pathway as fentanyl (CYP3A4) but is noted to have a potency 20 times higher than that of fentanyl and 10,000 times more powerful than morphine (Leen and Juurlink 2019). Carfentanil is often cheaper and easier to manufacture than other types of opioids or other drugs that are distributed in a similar form (cocaine, methamphetamine, etc.) so there have been many instances where illicit drug manufacturers lace their products with carfentanil to reduce costs while increasing potency (Leen and Juurlink 2019). It has been suggested that a significant portion of modern drug-related mortality is due to overdose or other adverse reactions to illicit drugs laced with carfentanil (Leen and Juurlink 2019). As the studies on fentanyl largely focus on clinical settings and specific populations (e.g. cancer patients from one ethnic group), future research is necessary to investigate carfentanil specifically and connections between demographic factors (such as socioeconomic status), and illicit use with the demonstrated impact of the polymorphisms discussed.
Detection of carfentanil in a cluster of patients without associated mortality: Response to Chhabra et al.
Published in The American Journal of Drug and Alcohol Abuse, 2021
Laura M. Szczesniak, Gregory A. Hobbs, Ross W. Sullivan
An analysis of fentanyl analog exposures in Cook County, Illinois recently published in this journal by Chhabra et al. found that more than half of urine drug screens detected at least one fentanyl analog or synthetic opioid (1). The relative ease of manufacturing and cost-cutting measures in the illicit drug industry has caused a flooding of the market with synthetic opioids, which is reflected in reported overdose deaths, as synthetic opioid-involved deaths increased 1040% from 2013 to 2019 (2). Use and overdose of carfentanil specifically has increased rapidly around the United States since it was first identified in patient samples in 2016 (3). Given the high potency of the drug (approximately 10,000 times as potent as morphine), most cases of carfentanil use have been identified postmortem, which poses a serious threat to patients with opioid use disorder.
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
Carfentanil is an ultrapotent fentanyl analog that was developed in 1974 and was used in the past primarily as a large animal tranquilizer. It is approximately 10,000 times as potent as morphine and 100 times as potent as fentanyl (Table 1) [7,49]. It is estimated that as little as 20 μg can be fatal to a human [50]. Until March 2017, pharmaceutical companies in China legally manufactured carfentanil and sold it in North America, Europe, and Australia for as little as $2,750/kg [49]. Illicit manufacturing is easy and inexpensive using the Ugi reaction, which consists of two chemical steps that produce carfentanil with a high yield [51]. Carfentanil has been found as an adulterant in heroin and cocaine and in counterfeit pills [49]. The first reports of fatalities associated with carfentanil came from Ohio and Florida in 2016 [17]. Carfentanil was responsible for 7.6% of the 5,152 opioid overdose deaths reported from 10 states in the United States during the latter half of 2016 [3]. In 2017, carfentanil was the second most commonly reported fentanyl analog (6,213 reports [3.52%]) to the NFLIS [35].