Premedication medicines do not cause drug metabolic interaction with propofol using human liver microsomes in vitro

European Journal of Clinical Pharmacology
Einosuke TanakaKatsuya Honda

Abstract

Propofol (2,6-diisopropylphenol) is widely used for anesthetic induction as well as for chronic sedation in intensive care units. In this study, we investigated the interaction between propofol and premedications, i.e., psychotropic and antianxiety agents (diazepam, midazolam), hypnotics (thiamylal), local anesthetics (lidocaine), depolarizing muscular relaxants (vecuronium), an antihypertensive (clonidine) and an H2-receptor antagonist (cimetidine) using human liver microsomes in vitro. The interaction effects between propofol and premedications were examined using human liver microsomal preparation in vitro. The concentration of propofol was determined by HPLC with UV detection. The apparent Michaelis-Menten constant (Km) and the maximal velocity of total metabolic formation (Vmax) of propofol in human liver microsomes were 123 microM and 26.1 micromol/min per milligram of mg protein, respectively. Seven premedications (diazepam, midazolam, thiamylal, lidocaine, cimetidine, vecuronium, and clonidine) did not inhibit propofol metabolism in human liver microsomes at concentrations within the therapeutic range. These results showed no interactions between propofol and seven premedication drugs within the therapeutic range of pro...Continue Reading

References

Apr 1, 1988·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·P J SimonsM Rowland
Jan 1, 1995·Pharmacology & Therapeutics·H Vanden BosscheH Moereels
Jun 1, 1995·The Annals of Pharmacotherapy·J S MarkowitzW H Carson
May 1, 1995·British Journal of Anaesthesia·T L ChenC C Liu
Oct 1, 1994·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·J R SneydB Wright
Apr 1, 1993·Anesthesia and Analgesia·M T BakerW C Ronnenberg
Jul 1, 1997·Clinical and Experimental Pharmacology & Physiology·M Murray
Oct 9, 1998·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·D McKillopC Simcock
Feb 27, 1999·Journal of Clinical Pharmacy and Therapeutics·E Tanaka
Aug 25, 1999·Clinical Pharmacology and Therapeutics·N HamaokaA Asada
Apr 12, 2001·British Journal of Clinical Pharmacology·Y OdaA Asada
Apr 16, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·James M RaeZeruesenay Desta

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Citations

Jan 20, 2006·Journal of Anesthesia·Yoshiko OsakaMakoto Tanaka
Jul 11, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·N MurayamaH Yamazaki
Jun 30, 2009·Biopharmaceutics & Drug Disposition·Sara Asimus, Michael Ashton
Apr 18, 2009·Anesthesia and Analgesia·Jaap VuykAlbert Dahan
Aug 10, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Hiroshi YamazakiNorie Murayama

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