Gamma-hydroxybutyrate (GHB) in humans: pharmacodynamics and pharmacokinetics.


Despite gamma-hydroxybutyrate (GHB) therapeutic uses and the increasing concern about its toxicity, few studies have addressed GHB dose-related effects under controlled administration and their relationship with its pharmacokinetics. The study design was double-blind, randomized, crossover, and controlled. As a pilot pharmacology phase I study, increasing doses of GHB were given. Single oral sodium GHB doses (40, 50, 60, and 72 mg/kg) were administered to eight volunteers. Plasma and urine were analyzed for GHB by gas chromatography-mass spectrometry. Physiological effects, psychomotor performance, and subjective effects were examined simultaneously. GHB produced dose-related changes in subjective effects as measured by questionnaires and VAS. GHB showed a mixed stimulant-sedative pattern, with initially increased scores in subjective feeling of euphoria, high, and liking followed by mild-moderate symptoms of sedation with impairment of performance and balance. Mean peak GHB plasma concentrations were 79.1, 83.1, 113.5, and 130.1 mug/L for 40, 50, 60, and 72 mg/kg, respectively. GHB-mediated physiological and subjective effects were dose dependent and related to GHB plasma concentrations. GHB urinary excretion was mainly related to administered doses. GHB-mediated subjective and physiological effects seem dose dependent and related to GHB plasma concentrations. Results suggest a high abuse liability of GHB in the range of dose usually consumed.

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@article{Abanades2006GammahydroxybutyrateI, title={Gamma-hydroxybutyrate (GHB) in humans: pharmacodynamics and pharmacokinetics.}, author={Sergio Abanades and Magi Farre and Mireia Segura and Simona Pichini and Diego Barral and Roberta Pacifici and Manuela Pellegrini and Francina Fonseca and Klaus Langohr and Rafael de la Torre}, journal={Annals of the New York Academy of Sciences}, year={2006}, volume={1074}, pages={559-76} }