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芬太尼及其衍生物:止痛药还是杀人凶手?

Fentanyl and its derivatives: Pain-killers or man-killers?

作者信息

Patocka Jiri, Wu Wenda, Oleksak Patrik, Jelinkova Romana, Nepovimova Eugenie, Spicanova Lenka, Springerova Pavlina, Alomar Suliman, Long Miao, Kuca Kamil

机构信息

Department of Chemistry, Faculty of Science, University of Hradec Kralove, 50003 Hradec Kralove, Czech Republic.

School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China.

出版信息

Heliyon. 2024 Mar 28;10(8):e28795. doi: 10.1016/j.heliyon.2024.e28795. eCollection 2024 Apr 30.

DOI:10.1016/j.heliyon.2024.e28795
PMID:38644874
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11031787/
Abstract

Fentanyl is a synthetic μ-opioid receptor agonist approved to treat severe to moderate pain with faster onset of action and about 100 times more potent than morphine. Over last two decades, abuse of fentanyl and its derivatives has an increased trend, globally. Currently, the United States (US) faces the most serious situation related to fentanyl overdose, commonly referred to as the opioid epidemic. Nowadays, fentanyl is considered as the number one cause of death for adults aged 18-45 in the US. Synthesis and derivatization of fentanyl is inexpensive to manufacture and easily achievable. Indeed, more than 1400 fentanyl derivatives have been described in the scientific literature and patents. In addition, accessibility and efficacy of fentanyl and its derivatives can play a potential role in misuse of these compounds as a chemical weapon. In this review, the properties, general pharmacology, and overdose death cases associated with fentanyl and selected derivatives are presented. Moreover, current opioid epidemic in the US, Moscow theatre hostage crisis, and potential misuse of fentanyl and its derivatives as a chemical weapon are disclosed.

摘要

芬太尼是一种合成的μ阿片受体激动剂,被批准用于治疗中重度疼痛,起效更快,效力约为吗啡的100倍。在过去二十年中,芬太尼及其衍生物的滥用在全球呈上升趋势。目前,美国面临与芬太尼过量使用相关的最严峻形势,通常被称为阿片类药物流行。如今,芬太尼被认为是美国18至45岁成年人的首要死因。芬太尼的合成和衍生化生产成本低廉且易于实现。事实上,科学文献和专利中已描述了1400多种芬太尼衍生物。此外,芬太尼及其衍生物的可获得性和有效性可能在这些化合物被滥用作化学武器方面发挥潜在作用。在本综述中,介绍了与芬太尼及选定衍生物相关的性质、一般药理学和过量死亡案例。此外,还披露了美国当前的阿片类药物流行、莫斯科剧院人质危机以及芬太尼及其衍生物被滥用作化学武器的可能性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/42ed5f4b7c81/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/3fb67e50417a/gr1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/ec64672cb48a/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/42ed5f4b7c81/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/3fb67e50417a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/4e8fe007e0db/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/969c3fe375a2/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/c9e3c03eb1f8/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/ec64672cb48a/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36e8/11031787/42ed5f4b7c81/gr6.jpg

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Neuropharmacology. 2023 Apr 1;227:109442. doi: 10.1016/j.neuropharm.2023.109442. Epub 2023 Jan 30.
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