Pharmacokinetics of γ-hydroxybutyric acid in alcohol dependent patients after single and repeated oral doses

S. D. Ferrara, S. Zotti, L. Tedeschi, G. Frison, F. Castagna, L. Gallimberti, G. L. Gessa, P. Palatini

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Abstract

1. The pharmacokinetics of γ-hydroxybutyric acid (GHB) were studied in 10 alcohol dependent subjects after single and repeated therapeutic oral doses (25 mg kg-1 every 12 h for 7 days). 2. GHB was readily absorbed and rapidly eliminated (t(max) = 20-45 min; mean t( 1/2 Z) 27 ± 5 s.d. min). Urinary recovery of unchanged GHB was negligible (<1% of the dose). γ-butyrolactone was not detected in either plasma or urine, indicating that lactonization of GHB does not occur in vivo. 3. The multiple-dose regimen resulted neither in accumulation of GHB nor in time-dependent modification of its pharmacokinetics. 4. In five subjects, the data were consistent with nonlinear elimination kinetics of GHB. Administration of a 50 mg kg-1 dose to these subjects resulted in significant increases in dose-normalized AUC, t( 1/2 Z) and mean residence time. 5. Doubling of the dose also resulted in a significant increase t(max) with little change in C(max). 6. At the administered doses, GHB did not accumulate in the plasma and caused no serious side effects.

Original languageEnglish
Pages (from-to)231-235
Number of pages5
JournalBritish Journal of Clinical Pharmacology
Volume34
Issue number3
Publication statusPublished - 1992

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Hydroxybutyrates
Pharmacokinetics
Alcohols
Area Under Curve
Urine
Therapeutics

Keywords

  • γ-Hydroxybutyric acid
  • Alcohol dependence
  • Pharmacokinetics

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Ferrara, S. D., Zotti, S., Tedeschi, L., Frison, G., Castagna, F., Gallimberti, L., ... Palatini, P. (1992). Pharmacokinetics of γ-hydroxybutyric acid in alcohol dependent patients after single and repeated oral doses. British Journal of Clinical Pharmacology, 34(3), 231-235.

Pharmacokinetics of γ-hydroxybutyric acid in alcohol dependent patients after single and repeated oral doses. / Ferrara, S. D.; Zotti, S.; Tedeschi, L.; Frison, G.; Castagna, F.; Gallimberti, L.; Gessa, G. L.; Palatini, P.

In: British Journal of Clinical Pharmacology, Vol. 34, No. 3, 1992, p. 231-235.

Research output: Contribution to journalArticle

Ferrara, SD, Zotti, S, Tedeschi, L, Frison, G, Castagna, F, Gallimberti, L, Gessa, GL & Palatini, P 1992, 'Pharmacokinetics of γ-hydroxybutyric acid in alcohol dependent patients after single and repeated oral doses', British Journal of Clinical Pharmacology, vol. 34, no. 3, pp. 231-235.
Ferrara, S. D. ; Zotti, S. ; Tedeschi, L. ; Frison, G. ; Castagna, F. ; Gallimberti, L. ; Gessa, G. L. ; Palatini, P. / Pharmacokinetics of γ-hydroxybutyric acid in alcohol dependent patients after single and repeated oral doses. In: British Journal of Clinical Pharmacology. 1992 ; Vol. 34, No. 3. pp. 231-235.
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