Disposition of gamma-hydroxybutyric acid in conventional and nonconventional biologic fluids after single drug administration:: Issues in methodology and drug monitoring
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作者:
Abanades, Sergio
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Abanades, Sergio
Farre, Magi
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Farre, Magi
Segura, Mireia
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Segura, Mireia
Pichini, Simona
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Pichini, Simona
Pastor, Antoni
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Pastor, Antoni
Pacifici, Roberta
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Pacifici, Roberta
Pellegrini, Manuela
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
Pellegrini, Manuela
de la Torre, Rafael
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机构:IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
de la Torre, Rafael
机构:
[1] IMIM, Pharmacol Res Unit, Human Pharmacol & Clin Neurosci Res Grp, Barcelona, Spain
[2] Ist Super Sanita, Drug Res & Evaluat Dept, I-00161 Rome, Italy
[3] Univ Autonoma Barcelona, E-08193 Barcelona, Spain
Little controlled drug administration data are available to aid in the interpretation of gamma-hydroxybutyric acid (GHB) distribution in conventional and nonconventional fluids and the potential correlation between the pharmacokinetics of GHB and drug effects. Single oral sodium GHB doses of 50 mg/kg were administered to five volunteers. Plasma, oral fluid, urine, and sweat were analyzed for GHB by gas chromatography mass spectrometry. GHB stability in plasma was studied at different storage temperatures. Subjective effects were measured using a set of 13 different visual analog scales. Mean peak GHB plasma concentrations at 30 minutes were 83.1 mu g/mL. After the absorption phase, concentrations declined to mean values of 0.9 mu g/mL at 6 hours. GHB was found in oral fluid at peak value concentrations equivalent to one third to one fourth of those found in plasma. The oral fluid-to-plasma ratio varied two fold in the 1- to 6-hour time range but always was lower than unit. The mean half-life (t(1/2)) of GHB was approximately 0.7 hour in plasma and approximately 1.2 hours in oral fluid. GHB urinary excretion is less than 2% of the dose administered. GHB was also detected in sweat at low concentrations. GHB showed a mixed sedative-stimulant pattern with subjective effects peaking between 1 and 1.5 hours after drug administration and lasting for 2 hours. Oral fluid and sweat appeared not to be suitable biologic matrices for monitoring GHB consumption. GHB -mediated subjective effects are related to GHB plasma concentrations.
机构:
Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USAVirginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA
Nicholson, KL
Balster, RL
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Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USAVirginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA
机构:
Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USAVirginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA
Nicholson, KL
Balster, RL
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Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USAVirginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA