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

Research output: Contribution to journalArticlepeer-review

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

Keywords

  • γ-Hydroxybutyric acid
  • Alcohol dependence
  • Pharmacokinetics

ASJC Scopus subject areas

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

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