CEC06-05 Fentanyloïds

IF 2.9 3区 医学 Q2 TOXICOLOGY
C. Lyphout
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引用次数: 0

Abstract

Fentanyl analogs – structurally related synthetic opioids within the 4-anilidopiperidine class – have become increasingly implicated in the rising incidence of opioid-related overdose deaths. These compounds, which include acetylfentanyl, butyrylfentanyl, and furanylfentanyl, are illicitly manufactured and trafficked, often sold as heroin or counterfeit prescription pills, leading to unintentional and frequently fatal exposures.
Fentanyl analogs exhibit high potency and rapid central nervous system penetration due to their lipophilicity. While they share core structural features with fentanyl, even minor chemical modifications can lead to substantial changes in receptor binding affinity, potency, and duration of action. These compounds produce classic opioid toxidromes, including respiratory depression, bradycardia, and miosis, which can be reversed with naloxone. However, due to their high potency, standard naloxone dosing may be insufficient, and higher initial doses (≥2 mg) are recommended. Law enforcement data show increasing seizure rates of various analogs, reflecting both high demand and the ease with which these compounds are synthesized and distributed. The clandestine nature of their production, coupled with a lack of clinical data, complicates diagnosis, treatment, and regulation.
Fentanyl analogs represent a relevant component of the opioid epidemic, distinguished by their high potency, rapid onset, and potential to cause fatal overdose at low doses. Their presence in the illicit drug supply steers the need for improved detection methods, targeted public health responses, and the development of effective harm-reduction and regulatory strategies.
CEC06-05 Fentanyloïds
芬太尼类似物-结构上与4-苯胺多哌啶类合成阿片类药物相关-越来越多地与阿片类药物过量死亡发生率上升有关。这些化合物包括乙酰芬太尼、丁基芬太尼和呋喃基芬太尼,它们是非法制造和贩运的,通常作为海洛因或假冒处方药出售,导致意外和经常致命的暴露。芬太尼类似物由于其亲脂性而表现出高效力和快速的中枢神经系统渗透。虽然它们与芬太尼具有相同的核心结构特征,但即使是微小的化学修饰也会导致受体结合亲和力、效力和作用持续时间的实质性变化。这些化合物会产生典型的阿片类药物毒副反应,包括呼吸抑制、心动过缓和瞳孔缩小,这些症状可以用纳洛酮逆转。然而,由于其效力高,标准纳洛酮剂量可能不足,建议使用更高的初始剂量(≥2mg)。执法数据显示,各种类似物的缉获率不断上升,反映出这些化合物的高需求和易于合成和分发。它们生产的秘密性质,加上缺乏临床数据,使诊断、治疗和监管复杂化。芬太尼类似物是阿片类药物流行的一个相关组成部分,其特点是效力高、起效快,并且在低剂量下可能导致致命的过量。它们存在于非法药物供应中,因此需要改进检测方法、有针对性的公共卫生对策以及制定有效的减少危害和管制战略。
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来源期刊
Toxicology letters
Toxicology letters 医学-毒理学
CiteScore
7.10
自引率
2.90%
发文量
897
审稿时长
33 days
期刊介绍: An international journal for the rapid publication of novel reports on a range of aspects of toxicology, especially mechanisms of toxicity.
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