γ‐Hydroxybutyrate (GHB) in Humans
Sergio Abanades, Magı́ Farré, Mireia Segura, Simona Pichini, Diego Barral, Roberta Pacifici, Manuela Pellegrini, Francina Fonseca, Klaus Langohr, Rafael de la Torre
Annals of the New York Academy of Sciences August 1, 2006 DOI: 10.1196/annals.1369.065 via OpenAlex
Summary
Gamma-hydroxybutyrate (GHB) produces dose-related changes in subjective effects, showing a mixed stimulant-sedative pattern: initial feelings of euphoria, high, and liking, followed by mild-to-moderate sedation with impaired performance and balance. Single oral doses of 40, 50, 60, and 72 mg/kg were given to eight volunteers. Mean peak plasma concentrations ranged from 79.1 to 130.1 μg/L. Physiological and subjective effects were dose-dependent and related to plasma concentrations. Urinary excretion was mainly related to dose. The results suggest high abuse liability at the doses typically consumed.
Study at a glance
| Characteristics | Randomized controlled trial, crossover Double-blind Peer reviewed |
|---|---|
| Sample size | 8 |
| Population | Volunteers |
| Intervention | Sodium GHB |
| Dose | 40, 50, 60, and 72 mg/kg |
| Keywords | Gamma hydroxybutyrate Sedative Euphoriant Pharmacokinetics Crossover study |
| Citations | 124 |
| Key finding | GHB produces dose-dependent subjective and physiological effects, with a mixed stimulant-sedative pattern and high abuse liability at typical doses. |
Abstract
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.