Effects of a rifampicin pre-treatment on linezolid pharmacokinetics

Fumiyasu Okazaki; Yasuhiro Tsuji; Yoshihiro Seto; Chika Ogami; Yoshihiro Yamamoto; Hideto To

doi:10.1371/journal.pone.0214037

Effects of a rifampicin pre-treatment on linezolid pharmacokinetics

Fumiyasu Okazaki, Yasuhiro Tsuji, Yoshihiro Seto, Chika Ogami, Yoshihiro Yamamoto, Hideto To

Research output: Contribution to journal › Article › peer-review

19 Scopus citations

Abstract

Linezolid is an oxazolidinone antibiotic that effectively treats methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). Since rifampicin induces other antibiotic effects, it is combined with linezolid in therapeutic regimes. However, linezolid blood concentrations are reduced by this combination, which increases the risk of the emergence of antibiotic-resistant bacteria. We herein demonstrated that the combination of linezolid with rifampicin inhibited its absorption and promoted its elimination, but not through microsomal enzymes. Our results indicate that the combination of linezolid with rifampicin reduces linezolid blood concentrations via metabolic enzymes.

Original language	English
Article number	e0214037
Journal	PLoS ONE
Volume	14
Issue number	9
DOIs	https://doi.org/10.1371/journal.pone.0214037
State	Published - 2019/09/01

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title = "Effects of a rifampicin pre-treatment on linezolid pharmacokinetics",

abstract = "Linezolid is an oxazolidinone antibiotic that effectively treats methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). Since rifampicin induces other antibiotic effects, it is combined with linezolid in therapeutic regimes. However, linezolid blood concentrations are reduced by this combination, which increases the risk of the emergence of antibiotic-resistant bacteria. We herein demonstrated that the combination of linezolid with rifampicin inhibited its absorption and promoted its elimination, but not through microsomal enzymes. Our results indicate that the combination of linezolid with rifampicin reduces linezolid blood concentrations via metabolic enzymes.",

author = "Fumiyasu Okazaki and Yasuhiro Tsuji and Yoshihiro Seto and Chika Ogami and Yoshihiro Yamamoto and Hideto To",

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T1 - Effects of a rifampicin pre-treatment on linezolid pharmacokinetics

AU - Okazaki, Fumiyasu

AU - Tsuji, Yasuhiro

AU - Seto, Yoshihiro

AU - Ogami, Chika

AU - Yamamoto, Yoshihiro

AU - To, Hideto

PY - 2019/9/1

Y1 - 2019/9/1

N2 - Linezolid is an oxazolidinone antibiotic that effectively treats methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). Since rifampicin induces other antibiotic effects, it is combined with linezolid in therapeutic regimes. However, linezolid blood concentrations are reduced by this combination, which increases the risk of the emergence of antibiotic-resistant bacteria. We herein demonstrated that the combination of linezolid with rifampicin inhibited its absorption and promoted its elimination, but not through microsomal enzymes. Our results indicate that the combination of linezolid with rifampicin reduces linezolid blood concentrations via metabolic enzymes.

AB - Linezolid is an oxazolidinone antibiotic that effectively treats methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). Since rifampicin induces other antibiotic effects, it is combined with linezolid in therapeutic regimes. However, linezolid blood concentrations are reduced by this combination, which increases the risk of the emergence of antibiotic-resistant bacteria. We herein demonstrated that the combination of linezolid with rifampicin inhibited its absorption and promoted its elimination, but not through microsomal enzymes. Our results indicate that the combination of linezolid with rifampicin reduces linezolid blood concentrations via metabolic enzymes.

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Effects of a rifampicin pre-treatment on linezolid pharmacokinetics

Abstract

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