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

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 itracona...

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Veröffentlicht in:	British journal of clinical pharmacology 1995-07, Vol.40 (1), p.83-86
Hauptverfasser:	Sampol, E, Lacarelle, B, Rajaonarison, JF, Catalin, J, Durand, A
Format:	Artikel
Sprache:	eng
Schlagworte:	Amphotericin B - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - pharmacology Antiviral agents Antiviral Agents - chemistry Antiviral Agents - metabolism Antiviral Agents - pharmacology Biological and medical sciences Chromatography, High Pressure Liquid Drugs fluconazole Fluconazole - pharmacology Flucytosine - pharmacology Glucuronates - chemistry Glucuronates - metabolism Humans Itraconazole Itraconazole - pharmacology Ketoconazole Ketoconazole - pharmacology Liver Medical sciences Miconazole Miconazole - pharmacology Microsomes Microsomes, Liver - drug effects Microsomes, Liver - metabolism Pharmacology. Drug treatments Zidovudine Zidovudine - chemistry Zidovudine - metabolism Zidovudine - pharmacology
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Zusammenfassung:	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).
ISSN:	0306-5251 1365-2125
DOI:	10.1111/j.1365-2125.1995.tb04540.x