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. 2007 Mar 12;51(5):1661–1665. doi: 10.1128/AAC.00744-06

TABLE 2.

Pharmacokinetic parameters and activities of amoxicillin, linezolid, and vancomycin in the prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant E. faecalis strainsa

Prophylactic regimenb Cmax (mg/liter) Tmax (h) Cmin (mg/liter) T/MIC (h) No. of infected rats/total no. of rats
VansE. faecalis strain JH2-2 inoculated with ID90 VanrE. faecalis strain UCN41 inoculated with:
ID90 10 × ID90
None 9/9 10/10 12/12
AMX 29.4 ± 6.59 2 0.52 ± 0.08 12 0/10d 0/10d,e 0/9d,e,f
LNZ-1 17.5 ± 5.13 1 3.81 ± 0.61 12 2/9d 8/11 9/9
LNZ-2 18.6 ± 4.47 1 4.57 ± 1.10 24 ND 4/10d 7/9
LNZ-4 19.3 ± 5.34 1 5.93 ± 1.69 48 ND 0/12d 3/11d
VAN 37.8 ± 3.29 0.5 5.57 ± 0.56 12c 0/9d 3/3 ND
a

Cmax, peak concentration of drug in serum; Tmax, time to maximum concentration of drug in serum; Cmin, trough concentration of drug in serum; T/MIC, time above MIC; ND, not determined; Vans, vancomycin susceptible; Vanr, vancomycin resistant. Values represent means ± standard deviations.

b

AMX, human simulation of a single oral dose of 2 to 3 g amoxicillin; LNZ-1, human simulation of a single oral dose of 600 mg linezolid; LNZ-2, human simulation of two consecutive oral doses of 600 mg linezolid every 12 h; LNZ-4, human simulation of four consecutive oral doses of 600 mg linezolid every 12 h; VAN, human simulation of a single i.v. dose of 1 g vancomycin.

c

Time above the MIC for the susceptible strain.

d

P < 0.05 versus no treatment.

e

P < 0.05 versus treatment with LNZ-1.

f

P < 0.05 versus treatment with LNZ-2.