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British Journal of Anaesthesia, 2002, Vol. 88, No. 5 653-658
© 2002 The Board of Management and Trustees of the British Journal of Anaesthesia

Clinical Investigations

Propofol metabolites in man following propofol induction and maintenance

P. Favetta1, C.-S. Degoute2, J.-P. Perdrix2, C. Dufresne1, R. Boulieu1,3 and J. Guitton*,4,5

1Département de Pharmacie Clinique, de Pharmacocinétique et d’Evaluation du Médicament, Institut des Sciences Pharmaceutiques et Biologiques de Lyon, 8 avenue Rockefeller, F-69373 Lyon Cedex 08, France. 2Service d’Anesthésie et réanimation, Centre Hospitalier Universitaire Lyon-Sud, 165 chemin du grand Revoyet, F-69495 Pierre Bénite Cedex, France. 3Service Pharmaceutique, Hôpital Neuro-cardiologique, 59 Bd Pinel, F-69393 Lyon, France. 4Fédération de Biochimie, Laboratoire C, Hôpital E. Herriot, 3 place d’Arsonval, F-69437 Lyon Cedex 03, France. 5Laboratoire de Physiologie Rénale et Métabolique, INSERM U499, Faculté de Médecine Laennec, 8 rue G. Paradin, F-69008 Lyon, France*Corresponding author: Fédération de Biochimie, Laboratoire C, Hôpital E. Herriot, 3 place d’Arsonval, F-69437 Lyon Cedex 03, France

Background. The pharmacokinetics of propofol in man is characterized by a rapid metabolic clearance linked to glucuronidation of the parent drug to form the propofol-glucuronide (PG) and sulfo- and glucuro-conjugation of hydroxylated metabolite via cytochrome P450 to produce three other conjugates. The purpose of this study was to assess the urine metabolite profile of propofol following i.v. propofol anaesthesia in a Caucasian population.

Methods. The extent of phase I and phase II metabolism of propofol was studied in 18 female and 17 male patients after an anaesthesia induced and maintained for at least 4 h with propofol. The infusion rates (mg kg–1 h–1) of propofol were (mean (SD)) 4.1 (1.0) and 4.5 (1.3) for males and females, respectively. Urine was collected from each patient for the periods 0–4, 4–8, 8–12, and 12–24 h after the start of propofol administration. In a preliminary study, the three main glucuro-conjugated metabolites were isolated from urine and characterized by magnetic resonance spectroscopy. The quantification of these metabolites for the different collection periods was then performed by a HPLC–UV assay.

Results. Total recovery of propofol in the metabolites studied amounts to 38%, of which 62% was via the PG metabolite and 38% via cytochrome P-450. This percentage is significantly higher than that previously reported from patients after a bolus dose of propofol. Extreme values for PG (0–24 h period) were included from 73 to 49%. There was no significant difference between female and male patients in the metabolite ratio.

Conclusions. We conclude that the extent of hydroxylation in propofol metabolism was higher than in previous findings after administration of anaesthetic doses of propofol. Moreover, the ratio between hydroxylation and glucuronidation of propofol is subject to an inter-patient variability but this does not correlate with the dose of propofol. However, the variation of the metabolite profile observed in the present report does not seem to indicate an extended role of metabolism in pharmacokinetic variability.

Br J Anaesth 2002; 88: 653–8


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