Suppr超能文献

在娱乐场所用1,4-丁二醇环醚替代γ-羟基丁酸:化学性行为中的新趋势。

Replacing GHB with GBL in Recreational Settings: A New Trend in Chemsex.

作者信息

Busardò Francesco Paolo, Gottardi Massimo, Tini Anastasio, Minutillo Adele, Sirignano Ascanio, Marinelli Enrico, Zaami Simona

机构信息

Section of Legal Medicine, Department of Excellence - Biomedical Sciences and Public Health. University "Politecnica delle Marche" of Ancona, Italy.

Comedical Srl., Trento, Italy.

出版信息

Curr Drug Metab. 2018;19(13):1080-1085. doi: 10.2174/1389200219666180925090834.

Abstract

BACKGROUND

Recently, Gamma-hydroxybutyrate (GHB) consumption in the recreational setting has been replaced by that of its prodrug Gamma-butyrolactone (GBL), cheaper and easier to obtain due to several legal industrial applications.

OBJECTIVE

The aim of the present paper was to report the most authoritative literature on the pharmacology and toxicology of GBL, dependence and abuse potential and the related public health issues together with the results of the analyses of several illicit liquid preparations containing GHB/GBL generally sold as "G".

METHOD

International literature concerning "Gamma-butyrolactone", "GBL" "toxicology", "pharmacology", "abuse", "dependence" and "GHB has been reviewed and liquid preparations containing GHB/GBL analysed by ultra-high performance liquid chromatography coupled to the tandem mass spectrometry validated methodology.

RESULTS

GBL for recreational purposes is orally administered in liquid form and rapidly transformed into GHB by lactonase enzymes present in the blood. As GBL shows a higher lipophilicity than GHB, it is absorbed more quickly, its bioavailability is higher and its effects are faster than those of GHB. Studies on rodents have shown that GBL has a low acute toxicity and only central nervous system depression has been highlighted. GBL abuse potential broadly mimics that of GHB, taking into account that it exerts its effects on the only after conversion into GHB. The analysis of 30 illicit preparations generally sold as "G" highlighted the presence of GBL in all of them at a mean concentration of 760.7 ±91.46 mg/mL (range: 588.5 - 899.3 mg/mL).

CONCLUSION

GBL currently represents a growing public health issue since the substance is relatively cheaper and easier to obtain than GHB. Improvement and implementation of laws and policies to place GBL under control are needed to limit its diffusion, the eventual health threat for users and its non -negligible abuse liability and dependence risk.

摘要

背景

近来,在娱乐场所中,γ-羟基丁酸(GHB)的使用已被其前体药物γ-丁内酯(GBL)所取代,GBL因在多个合法工业应用中使用,价格更低且更易获取。

目的

本文旨在报告关于GBL药理学和毒理学、依赖和滥用潜力以及相关公共卫生问题的最具权威性的文献,同时报告对几种通常作为“G”出售的含GHB/GBL非法液体制剂的分析结果。

方法

查阅了有关“γ-丁内酯”“GBL”“毒理学”“药理学”“滥用”“依赖”和“GHB”的国际文献,并采用超高效液相色谱-串联质谱验证方法对含GHB/GBL的液体制剂进行了分析。

结果

用于娱乐目的的GBL以液体形式口服给药,并通过血液中存在的内酯酶迅速转化为GHB。由于GBL的亲脂性高于GHB,其吸收更快,生物利用度更高,作用也比GHB更快。对啮齿动物的研究表明,GBL急性毒性较低,仅突出显示有中枢神经系统抑制作用。考虑到GBL仅在转化为GHB后才发挥作用,其滥用潜力与GHB大致相似。对30种通常作为“G”出售的非法制剂的分析表明,所有制剂中均含有GBL,平均浓度为760.7±91.46 mg/mL(范围:588.5 - 899.3 mg/mL)。

结论

GBL目前构成了一个日益严重的公共卫生问题,因为该物质比GHB相对更便宜且更易获取。需要改进和实施法律及政策以管控GBL,从而限制其传播、对使用者最终的健康威胁以及其不可忽视的滥用倾向和依赖风险。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验