Comparative Effects of Antifungal Agents on Zidovudine Glucuronidation by Human Liver Microsomes
Overview
Affiliations
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).
Bennani Y, Ben Hassine K, Gencaslan M, Boudal-Khoshbeen M, Samer C, Ansari M Pharmacol Res Perspect. 2024; 12(6):e70011.
PMID: 39611692 PMC: 11605732. DOI: 10.1002/prp2.70011.
Wang Y, Wang S, Nie X, Yang K, Xu P, Wang X J Biol Chem. 2019; 294(33):12415-12431.
PMID: 31243100 PMC: 6699835. DOI: 10.1074/jbc.RA119.007505.
Effects of oral clotrimazole troches on the pharmacokinetics of oral and intravenous midazolam.
Shord S, Chan L, Camp J, Vasquez E, Jeong H, Molokie R Br J Clin Pharmacol. 2010; 69(2):160-6.
PMID: 20233179 PMC: 2824477. DOI: 10.1111/j.1365-2125.2009.03559.x.
In vitro and in vivo glucuronidation of midazolam in humans.
Hyland R, Osborne T, Payne A, Kempshall S, Logan Y, Ezzeddine K Br J Clin Pharmacol. 2009; 67(4):445-54.
PMID: 19371318 PMC: 2679108. DOI: 10.1111/j.1365-2125.2009.03386.x.
Effects of the antifungal agents on oxidative drug metabolism: clinical relevance.
Venkatakrishnan K, von Moltke L, Greenblatt D Clin Pharmacokinet. 2000; 38(2):111-80.
PMID: 10709776 DOI: 10.2165/00003088-200038020-00002.