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European Journal of Drug Metabolism and Pharmacokinetics

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01-03-2011 | Original Paper

Effect of blood decrease on micafungin disposition in rats

Authors: Hiroki Konishi, Keizo Fukushima, Masatomo Sudo, Masaki Sumi, Tokuzo Minouchi, Ikumi Iga, Nobuhito Shibata, Akira Yamaji

Published in: European Journal of Drug Metabolism and Pharmacokinetics | Issue 1/2011

Abstract

Micafungin (MCFG) is a novel echinocandin-class antifungal agent that extensively undergoes metabolic removal in the liver. In the present study, the influence of decreased blood volume on pharmacokinetic disposition of MCFG was examined using a rat model prepared by phlebotomy. In phlebotomized rats, hematocrit level and plasma albumin concentration were decreased by 50 and 15%, respectively. Regarding the pharmacokinetic parameters of MCFG, there were no significant differences in the total body clearance (CL_tot) and elimination rate constant (k _e) between control and phlebotomized rat groups. A slight increase was observed in the apparent volume of distribution at steady-state (Vd_ss), but the degree of change was minimal. These findings demonstrate that the elimination capacity for MCFG is only slightly affected by severe anemia and moderate hypoalbuminemia, and provide experimental evidence for the preceding clinical studies suggesting that neither hematocrit level nor serum albumin concentration is a contributory factor for the metabolic clearance of MCFG.

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Title: Effect of blood decrease on micafungin disposition in rats
Authors: Hiroki Konishi
Keizo Fukushima
Masatomo Sudo
Masaki Sumi
Tokuzo Minouchi
Ikumi Iga
Nobuhito Shibata
Akira Yamaji
Publication date: 01-03-2011
Publisher: Springer-Verlag
Published in: European Journal of Drug Metabolism and Pharmacokinetics / Issue 1/2011
Print ISSN: 0378-7966
Electronic ISSN: 2107-0180
DOI: https://doi.org/10.1007/s13318-011-0023-3

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Effect of blood decrease on micafungin disposition in rats

Abstract

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Abstract

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