Pharmacokinetics and protein binding of propofol in patients with cirrhosis

Anesthesiology. 1988 Dec;69(6):887-91. doi: 10.1097/00000542-198812000-00014.

Abstract

The pharmacokinetics and protein binding of propofol were studied in ten patients with cirrhosis and in ten control patients undergoing elective surgery. All patients received 2.5 mg.kg-1 propofol as an intravenous bolus injection for the induction of anesthesia. Whole blood propofol concentrations were measured at intervals up to 12 h, using a high-performance liquid chromatography (HPLC) technique. Propofol protein binding was estimated by equilibrium dialysis 10 min after injection of propofol. Individual propofol profiles for all patients were best described by a three-compartment open mammillary model. Rapid and slow propofol distribution half-times were observed, followed by an elimination phase with a half-time of 4-5 h. Propofol total body clearance was reduced (1.99 +/- 0.68 l.min-1) in the patients with cirrhosis but did not differ significantly from that in the control patients (2.30 +/- 0.61 l.min-1). The apparent volume of distribution at steady state (Vdss) was similar in the two groups. No significant difference in elimination half-life was observed between the two groups. Propofol was extensively bound (mean: 97-98%) to the plasma protein of both cirrhotic and control groups. This study shows that propofol pharmacokinetics and protein binding of propofol following a single intravenous bolus dose were not markedly affected by uncomplicated cirrhosis of the liver.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anesthetics / blood
  • Anesthetics / pharmacokinetics*
  • Blood Proteins / metabolism
  • Body Weight
  • Female
  • Half-Life
  • Humans
  • Liver / metabolism
  • Liver Cirrhosis / blood*
  • Male
  • Middle Aged
  • Phenols / blood
  • Phenols / pharmacokinetics*
  • Propofol

Substances

  • Anesthetics
  • Blood Proteins
  • Phenols
  • Propofol