Francesco Paolo Busardò 1 , Massimo Gottardi 2 , Anastasio Tini 3 , Adele Minutillo 4 , Ascanio Sirignano 5 , Enrico Marinelli 3 , Simona Zaami 3 Show Affiliations »
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BACKGROUND: Recently, Gamma-hydroxybutyrate (GHB) consumption in the recreational setting has been replaced by that of its prodrug Gamma-butyrolactone (GBL), cheaper and easier to obtain due to several legal industrial applications.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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
BACKGROUND: Recently, Gamma-hydroxybutyrate (GHB ) consumption in the recreational setting has been replaced by that of its prodrug Gamma-butyrolactone (GBL ), cheaper and easier to obtain due to several legal industrial applications.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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities: Chemical
Disease
Keywords:
abuse; chemsex; dependence; liquid G; γ-butyrolactone (GBL); γ-hydroxybutyrate (GHB).
Mesh： See more »
Substances： See more »
Year: 2018
PMID： 30251602 DOI： 10.2174/1389200219666180925090834
Source DB: PubMed Journal: Curr Drug Metab ISSN： 1389-2002 Impact factor: 3.731