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Comparative effects of antifungal agents on zidovudine glucuronidation by human liver microsomes
E Sampol1, B Lacarelle, J F Rajaonarison
1Laboratoire de pharmacocinétique, Faculté de pharmacie, Marseille, France.
British Journal of Clinical Pharmacology
|July 1, 1995
Abstract:
Zidovudine (ZDV) is extensively metabolised by the liver to an inactive glucuronide (GZDV). Since ZDV is often administered with antimycotic drugs, we studied the effect of six systemic antifungal agents on the in vitro glucuronidation of ZDV by human liver microsomes. 5-fluorocytosine and itraconazole had no inhibitory effect whereas amphotericine B, ketoconazole, miconazole and fluconazole inhibited in vitro GZDV formation (Ki values were 0.13, 0.08, 0.18 and 1.4 mM respectively).