PMID: 8959645Nov 1, 1996Paper

Effects of erythromycin and roxithromycin on oxidation of testosterone and nifedipine catalyzed by CYP3A4 in human liver microsomes

The Journal of Toxicological Sciences
H YamazakiT Shimada

Abstract

Roxithromycin and erythromycin were incubated with rat and human liver microsomal or reconstituted cytochrome P450 (P450 or CYP) monooxygenase systems in the presence of an NADPH-generating system, and the effects of these chemicals on testosterone 6 beta-hydroxylation and nifedipine oxidation activities were compared with those of typical CYP3A4 inhibitors including ketoconazole, troleandomycin, and gestodene. Roxithromycin and erythromycin were found to be relatively weak inhibitors of testosterone 6 beta-hydroxylation and nifedipine oxidation activities by rat and human liver microsomes or by reconstituted systems containing CYP3A4/5. Formation of an inhibitory P450-metabolite complex was determined spectrally by incubating troleandomycin with human liver microsomes; the extents of the complex formation were lesser in liver microsomes of humans than those of rats treated with dexamethasone. Erythromycin and roxithromycin were also activated slightly by rat liver microsomes to form P450.Fe(II)-metabolite complex, although these chemicals caused very little or undetectable levels, respectively, of spectral changes by human liver microsomes even when a human sample which contained relatively high levels of CYP3A4 was used. Thes...Continue Reading

Citations

Jan 7, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Janvier Engelbert AgbokpontoLi Ding
Aug 4, 2016·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Yannick ParmentierBernard Walther
Dec 14, 2006·Therapeutic Drug Monitoring·Priska KaufmannStephan Krähenbühl
Jun 24, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Chuong PhamKen Korzekwa
Mar 17, 2019·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Ahmad SharanekAndré Guillouzo

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