Comparative effects of antifungal agents on zidovudine glucuronidation by human liver microsomes.

Br J Clin Pharmacol

Laboratoire de pharmacocinétique, Faculté de pharmacie, Marseille, France.

Published: July 1995

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).

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1365033PMC
http://dx.doi.org/10.1111/j.1365-2125.1995.tb04540.xDOI Listing

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