Short Communication Effects of ketamine on human UDP-glucuronosyltransferases in vitro predict potential drug- drug interactions arising from ketamine inhibition of codeine and morphine glucuronidation
نویسندگان
چکیده
Department of Clinical Pharmacology, Flinders University School of Medicine, Adelaide, Australia (VU, PR, NC, JOM) Faculty of Pharmaceutical Science, Khon Kaen University, Khon Kaen, Thailand (VU) Department of Biomedical Sciences, Prince of Songkla University, Hat Yai, Thailand (PR, BJ) School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, Australia (AME) DMD Fast Forward. Published on May 6, 2011 as doi:10.1124/dmd.111.039727
منابع مشابه
Short Communication Effects of Ketamine on Human UDP-Glucuronosyltransferases In Vitro Predict Potential Drug-Drug Interactions Arising from Ketamine Inhibition of Codeine and Morphine Glucuronidation
In this study, the selectivity of UDP-glucuronosyltransferase (UGT) enzyme inhibition by ketamine (KTM) and the kinetics of KTM inhibition of human liver microsomal morphine (MOR) and codeine (COD) glucuronidation were characterized to explore a pharmacokinetic basis for the KTM-opioid interaction. With the exception of UGT1A4, KTM inhibited the activities of recombinant human UGT enzymes in a ...
متن کاملEffects of ketamine on human UDP-glucuronosyltransferases in vitro predict potential drug-drug interactions arising from ketamine inhibition of codeine and morphine glucuronidation.
In this study, the selectivity of UDP-glucuronosyltransferase (UGT) enzyme inhibition by ketamine (KTM) and the kinetics of KTM inhibition of human liver microsomal morphine (MOR) and codeine (COD) glucuronidation were characterized to explore a pharmacokinetic basis for the KTM-opioid interaction. With the exception of UGT1A4, KTM inhibited the activities of recombinant human UGT enzymes in a ...
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The widely used hypnosedative-anxiolytic agent R,S-lorazepam is cleared predominantly by conjugation with glucuronic acid in humans, but the enantioselective glucuronidation of lorazepam has received little attention. The present study characterized the kinetics of the separate R and S enantiomers of lorazepam by human liver microsomes (HLMs) and by a panel of recombinant human UDP-glucuronosyl...
متن کاملIn vitro-in vivo extrapolation predicts drug-drug interactions arising from inhibition of codeine glucuronidation by dextropropoxyphene, fluconazole, ketoconazole, and methadone in humans.
Because codeine (COD) is eliminated primarily via glucuronidation, factors that alter COD glucuronide formation potentially affect the proportion of the dose converted to the pharmacologically active metabolite morphine. Thus, in vitro-in vivo extrapolation approaches were used to identify potential drug-drug interactions arising from inhibition of COD glucuronidation in humans. Initial studies...
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