Pharmacokinetics and pharmacodynamics of a single bolus of propofol 2% in healthy volunteers

J Clin Pharmacol. 2003 Apr;43(4):397-405. doi: 10.1177/0091270003251391.

Abstract

This study was undertaken to assess the bioequivalence between a new formulation of propofol 2% and the commercially available product Diprivan. Secondary objectives were to compare the times to onset of and emergence from hypnosis, the hemodynamic effects, and the safety profiles. Twelve healthy male volunteers were included in a randomized crossover study. Subjects were administered a 2-mg/kg single bolus injection of each formulation separated by a 7- to 10-day washout period. Plasma propofol was determined by reversed-phase liquid chromatography with fluorescence detection. Eleven subjects completed the study, and both formulations were considered bioequivalent. There were no serious or severe adverse events. The concentration-time profiles of all the subjects could adequately be described using a three-compartment model. The mean times to cessation of counting out loud (17 vs. 18 s) and to eye opening (245 vs. 244 s) were not statistically different between treatment groups. Moreover, they seem to show some degree of pharmacodynamic bioequivalence, although a higher number of subjects are necessary to unequivocally demonstrate it.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Anesthetics, Intravenous / adverse effects
  • Anesthetics, Intravenous / pharmacokinetics*
  • Anesthetics, Intravenous / pharmacology*
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Humans
  • Male
  • Propofol / adverse effects
  • Propofol / pharmacokinetics*
  • Propofol / pharmacology*
  • Therapeutic Equivalency
  • Time Factors

Substances

  • Anesthetics, Intravenous
  • Propofol