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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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
Issue number3
Publication statusPublished - 1992


  • γ-Hydroxybutyric acid
  • Alcohol dependence
  • Pharmacokinetics

ASJC Scopus subject areas

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

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