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British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1995 Jul;40(1):83–86. doi: 10.1111/j.1365-2125.1995.tb04540.x

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

E Sampol 1, B Lacarelle 1, J F Rajaonarison 1, J Catalin 1, A Durand 1
PMCID: PMC1365033  PMID: 8527274

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).

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Selected References

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