Comparison of the behavioral effects of gamma-hydroxybutyric acid (GHB) and its 4-methyl-substituted analog, gamma-hydroxyvaleric acid (GHV)

Carter, Lawrence P.; Chen, Weibin; Wu, Huifang; Mehta, Abhishek; Hernandez, R. Jason; Ticku, Maharaj K.; Coop, Andrew; Koek, Wouter

doi:10.1016/j.drugalcdep.2004.10.002

Cited by 57 publications

(39 citation statements)

References 42 publications

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“…NMP (Reisch, 2008), and similar molecules, including GHV (Brunt et al, 2013;Carter et al, 2005), phenibut (O'Connell et al, 2014;Samokhvalov et al, 2013;Schmitt et al, 2013) and baclofen (Franchitto et al, 2014;Gahr et al, 2014;Weißhaar et al, 2012) are now starting to emerge as substitutes for GHB/GBL. Some internet sites that formerly offered GHB and GBL for sale to assist sleep, as an aid in bodybuilding, for energy boosts, as an antidepressant, etc.…”

Section: Discussionmentioning

confidence: 99%

“…NMP is sometimes used as a substitute for GBL (Reisch, 2008), and has been found in some GHB solutions (DEA, 2004). Also of interest is that a related substance GVL (gamma-valerolactone) is being used recreationally in Europe; it has similar effects to GHB and its pro-drugs, and is metabolised by a lactonase to GVC (gamma-hydroxy valeric acid, 4-methyl-GHB, gamma-methyl-GHB) (Carter et al, 2005). It is a legal substance but has a two-fold lower affinity for the GHB receptor (Andresen-Streichert et al, 2013).…”

Section: Non-medical Uses Of Ghb and Its Precursorsmentioning

confidence: 99%

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Gamma hydroxybutyrate (GHB), gamma butyrolactone (GBL) and 1,4-butanediol (1,4-BD; BDO): A literature review with a focus on UK fatalities related to non-medical use

Corkery

Loi

Claridge

et al. 2015

Neuroscience & Biobehavioral Reviews

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Misuse of gamma hydroxybutrate (GHB) and gamma butyrolactone (GBL) has increased greatly since the early 1990s, being implicated in a rising number of deaths. This paper reviews knowledge on GHB and derivatives, and explores the largest series of deaths associated with their non-medical use. Descriptive analyses of cases associated with GHB/GBL and 1,4-butanediol (1,4-BD) use extracted from the UK's National Programme on Substance Abuse Deaths database. From 1995 to September 2013, 159 GHB/GBL-associated fatalities were reported. Typical victims: White (92%); young (mean age 32 years); male (82%); with a drug misuse history (70%). Most deaths (79%) were accidental or related to drug use, the remainder (potential) suicides. GHB/GBL alone was implicated in 37%; alcohol 14%; other drugs 28%; other drugs and alcohol 15%. Its endogenous nature and rapid elimination limit toxicological detection. Post-mortem blood levels: mean 482 (range 0-6500; SD 758)mg/L. Results suggest significant caution is needed when ingesting GHB/GBL, particularly with alcohol, benzodiazepines, opiates, stimulants, and ketamine. More awareness is needed about risks associated with consumption.

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Section: Discussionmentioning

confidence: 99%

Section: Non-medical Uses Of Ghb and Its Precursorsmentioning

confidence: 99%

Gamma hydroxybutyrate (GHB), gamma butyrolactone (GBL) and 1,4-butanediol (1,4-BD; BDO): A literature review with a focus on UK fatalities related to non-medical use

Corkery

Loi

Claridge

et al. 2015

Neuroscience & Biobehavioral Reviews

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“…Some studies have stated, in contrast, that pretreatment with NCS-382 potentiated, rather than antagonized, a GHB-induced sedative hypnotic effect [59], which was offset by others who questioned the antagonistic properties of NCS-382 on GHBR since it failed to block the effect of GHB on hypomotility and sedation/hypnosis [60,61,62]. The involvement of GHBR was confirmed when the specific GHBR agonist c-hydroxyvaleric acid was proved to mimic the sedative effects of GHB without binding to the GABA B R [58,63]. Higher supraphysiological concentrations (such as ExGHB) downregulate the GHBR and eliminate the tonic inhibitory control of GHBR on the GABA presynaptic element.…”

Section: Endogenous and Exogenous Ghbmentioning

confidence: 78%

The Neurobiological Mechanisms of Gamma-Hydroxybutyrate Dependence and Withdrawal and Their Clinical Relevance: A Review

Kamal

Noorden²,

Franzek³

et al. 2016

Neuropsychobiology

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Objective: γ-Hydroxybutyrate (GHB) has gained popularity as a drug of abuse. In the Netherlands the number of patients in treatment for GHB dependence has increased sharply. Clinical presentation of GHB withdrawal can be life threatening. We aim, through this overview, to explore the neurobiological pathways causing GHB dependency and withdrawal, and their implications for treatment choices. Methods: In this work we review the literature discussing the findings from animal models to clinical studies focused on the neurobiological pathways of endogenous but mainly exogenous GHB. Results: Chronic abuse of GHB exerts multifarious neurotransmitter and neuromodulator effects on γ-aminobutyric acid (GABA), glutamate, dopamine, serotonin, norepinephrine and cholinergic systems. Moreover, important effects on neurosteroidogenesis and oxytocin release are wielded. GHB acts mainly via a bidirectional effect on GABA_B receptors (GABA_BR; subunits GABA_B1 and GABA_B2), depending on the subunit of the GIRK (G-protein-dependent ion inwardly rectifying potassium) channel involved, and an indirect effect of the cortical and limbic inputs outside the nucleus accumbens. GHB also activates a specific GHB receptor and β₁-subunits of α₄-GABA_AR. Reversing this complex interaction of neurobiological mechanisms by the abrupt cessation of GHB use results in a withdrawal syndrome with a diversity of symptoms of different intensity, depending on the pattern of GHB abuse. Conclusion: The GHB withdrawal symptoms cannot be related to a single mechanism or neurological pathway, which implies that different medication combinations are needed for treatment. A single drug class, such as benzodiazepines, gabapentin or antipsychotics, is unlikely to be sufficient to avoid life-threatening complications. Detoxification by means of titration and tapering of pharmaceutical GHB can be considered as a promising treatment that could make polypharmacy redundant.

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“…GBL was not banned at that time so that GBL remained a legal alternative to GHB as it is rapidly converted in the body to GHB following its ingestion; in fact, GBL is a legal pro-drug of illegal GHB. Other legal alternatives for GHB are 1,4-butanediol (BDO) and gamma-hydroxyvaleric acid (GHV) (Carter et al, 2005), which will be no further discussed here. That GHB can be substituted for by GBL has not escaped the attention of the WHO which is currently carrying out a risk assessment for GBL.…”

Section: Introductionmentioning

confidence: 99%

Risk assessment of GBL as a substitute for the illicit drug GHB in the Netherlands. A comparison of the risks of GBL versus GHB

Amsterdam

Brunt

Pennings

et al. 2014

Regulatory Toxicology and Pharmacology

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Comparison of the behavioral effects of gamma-hydroxybutyric acid (GHB) and its 4-methyl-substituted analog, gamma-hydroxyvaleric acid (GHV)

Cited by 57 publications

References 42 publications

Gamma hydroxybutyrate (GHB), gamma butyrolactone (GBL) and 1,4-butanediol (1,4-BD; BDO): A literature review with a focus on UK fatalities related to non-medical use

Gamma hydroxybutyrate (GHB), gamma butyrolactone (GBL) and 1,4-butanediol (1,4-BD; BDO): A literature review with a focus on UK fatalities related to non-medical use

The Neurobiological Mechanisms of Gamma-Hydroxybutyrate Dependence and Withdrawal and Their Clinical Relevance: A Review

Risk assessment of GBL as a substitute for the illicit drug GHB in the Netherlands. A comparison of the risks of GBL versus GHB

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