COMPARATIVE EFFECTS OF ANTIFUNGAL AGENTS ON ZIDOVUDINE GLUCURONIDATION BY HUMAN LIVER-MICROSOMES

Authors
SAMPOL E LACARELLE B RAJAONARISON JF CATALIN J DURAND A
Citation
E. Sampol et al., COMPARATIVE EFFECTS OF ANTIFUNGAL AGENTS ON ZIDOVUDINE GLUCURONIDATION BY HUMAN LIVER-MICROSOMES, British journal of clinical pharmacology, 40(1), 1995, pp. 83-86
Citations number
19
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
British journal of clinical pharmacology → ACNP
ISSN journal
03065251
Volume
40
Issue
1
Year of publication
1995
Pages
83 - 86
Database
ISI
SICI code
0306-5251(1995)40:1<83:CEOAAO>2.0.ZU;2-Q
Abstract
Zidovudine (ZDV) is extensively metabolised by the liver to an inactiv e 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-fluorocy tosine and itraconazole had no inhibitory effect whereas amphotericine B, ketoconazole, miconazole and fluconazole inhibited in vitro GZDV f ormation (K-i values were 0.13, 0.08, 0.18 and 1.4 mM respectively).