Metabolic interaction between morphine and naloxone in human liver. A common pathway of glucuronidation?
Metabolic interaction between naloxone and morphine has been studied in vitro in human liver microsomes. Morphine and naloxone are metabolized by an UDP-glucuronyl transferase to their 3-glucuronides. There is a very good correlation between the rates of formation of morphine-3-glucuronide and of naloxone-3-glucuronide. Naloxone seems to have a 10-fold higher affinity for the enzyme binding site than does morphine. Morphine and naloxone show bisubstrate kinetic patterns which appear very similar.
Wahlström
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A
Division of Clinical Pharmacology, University Hospital, Uppsala, Sweden.
Persson
K
K
Rane
A
A
D002851:Chromatography, High Pressure Liquid; D014453:Glucuronosyltransferase / Q000378:metabolism; D006801:Humans; D008862:Microsomes, Liver / Q000201:enzymology / Q000378:metabolism*; D009020:Morphine / Q000378:metabolism*; D009270:Naloxone / Q000378:metabolism*; D014535:Uridine Diphosphate Glucuronic Acid / Q000378:metabolism
D014535:Uridine Diphosphate Glucuronic Acid; D009270:Naloxone; D009020:Morphine; D014453:Glucuronosyltransferase