Propofol inhibits enzymatic degradation of alfentanil and sufentanil by isolated liver microsomes in vitro

P. K. Janicki, M. F.M. James, W. A.R. Erskine

Research output: Contribution to journalArticle

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Abstract

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.

Original languageEnglish (US)
Pages (from-to)311-312
Number of pages2
JournalBritish Journal of Anaesthesia
Volume68
Issue number3
DOIs
StatePublished - Mar 1992

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Sufentanil
Alfentanil
Liver Microsomes
Propofol
Swine
Tissue Donors
Liver
Inhibitory Concentration 50
In Vitro Techniques
Transplants

All Science Journal Classification (ASJC) codes

  • Anesthesiology and Pain Medicine

Cite this

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abstract = "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.",
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Propofol inhibits enzymatic degradation of alfentanil and sufentanil by isolated liver microsomes in vitro. / Janicki, P. K.; James, M. F.M.; Erskine, W. A.R.

In: British Journal of Anaesthesia, Vol. 68, No. 3, 03.1992, p. 311-312.

Research output: Contribution to journalArticle

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