Abstract
Using an experimental endocarditis model, we studied the activity of daptomycin used alone or in combination with gentamicin against an Enterococcus faecium strain that was highly resistant to glycopeptides and susceptible to gentamicin. In vitro, the MIC of daptomycin was 1 micrograms/ml. In vivo, daptomycin appeared to be effective only when it was used in a high-dose regimen, i.e., 12 mg/kg of body weight every 8 h (-2.5 log10 CFU/g versus controls; P < 0.05), particularly when it was combined with gentamicin (-5.0 log10 CFU/g versus controls; P < 0.01). Since the distribution of daptomycin into cardiac vegetations, as evaluated by autoradiography, appeared to be homogeneous, the poor in vivo activity of daptomycin was considered to be related to its high degree of protein binding, as suggested by killing curves studies. Since the MIC of teicoplanin for the vancomycin-resistant E. faecium strain used in the study was only 64 micrograms/ml and since an in vitro synergy between teicoplanin at high dose and gentamicin was observed, a high-dose regimen of teicoplanin, i.e., 40 mg/kg every 12 h, was also assessed in vivo. This treatment provided marginal activity only when it was combined with gentamicin (-2.3 log10 CFU/g versus controls; P < 0.05). These results suggest that the levels of daptomycin or teicoplanin in serum required to cure experimental endocarditis caused by a highly glycopeptide-resistant strain of E. faecium would not be achievable in humans.
MeSH Terms
Animals
Daptomycin
Diffusion
Drug Resistance, Microbial
Drug Synergism
Drug Therapy, Combination/pharmacokinetics,therapeutic use
Endocarditis, Bacterial/drug therapy,metabolism,microbiology
Enterococcus/drug effects
Female
Gentamicins/pharmacokinetics,therapeutic use
Glycopeptides/pharmacology
Humans
Microbial Sensitivity Tests
Peptides/pharmacokinetics,therapeutic use
Rabbits
Teicoplanin/pharmacokinetics,therapeutic use
Chemicals
Gentamicins
Glycopeptides
Peptides
Teicoplanin
Daptomycin
Authors & Affiliations
9 authors, click to expand affiliations / ORCID
Caron F
Groupe de Recherche en Infections Expérimentales, Hôpital Charles Nicolle, Rouen, France.
Kitzis M D
Gutmann L
Cremieux A C
Maziere B
Vallois J M
Saleh-Mghir A
Lemeland J F
Carbon C
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