We have studied the effect of propofol on the enzymatic degradation of alfentanii and sufentanii utilizing isolated liver microsomes obtained from pig and human liver. Propofol inhibited dose-dependently the oxidative metabolic degradation of alfentanii and sufentanii by both microsomal preparations. The calculated concentration of propofol causing 50% inhibition of metabolic degradation (IC50) was 32.6 μmol litre-1 for alfentanii and 22.1 pwnol litre-1 for sufentanii in pig liver microsomes. Similar values of inhibitory activity of propofol (IC values 62.8 and 52.9 μmol litre-1, respectively) were observed using human microsomes prepared from liver taken from an organ transplant donor. We suggest that propofol in clinically relevant concentrations interferes with oxidative metabolic degradation of alfentanii and sufentanii in the microsomal fraction of pig and human liver.
All Science Journal Classification (ASJC) codes
- Anesthesiology and Pain Medicine