Open AccessEffects of a rifampicin pre-treatment on linezolid pharmacokinetics
Author(s) -
Fumiyasu Okazaki,
Yasuhiro Tsuji,
Yoshihiro Seto,
Chika Ogami,
Yoshihiro Yamamoto,
Hideto To
Publication year - 2019
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0214037
Subject(s) - linezolid , rifampicin , antibiotics , pharmacokinetics , vancomycin , pharmacology , staphylococcus aureus , microbiology and biotechnology , medicine , chemistry , bacteria , biology , genetics
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.