ABSTRACT
Objective: This study used Monte Carlo simulations
to assess the potential for attainment of pharmacody-
namic targets with the fluoroquinolones garenoxacin,
gemifloxacin, and moxifloxacin against Streptococcus
pneumoniae in serum and epithelial lining fluid (ELF)
from hospitalized patients with community-acquired
pneumonia (CAP).
Methods: Data on the free AUC over 24 hours
(ƒAUC
0–24
), a measure of drug exposure, were derived
from previously described population pharmacokinetic
models for therapeutic doses of the 3 fluoroquinolones.
MIC distribution data for S pneumoniae were obtained
from the Canadian Respiratory Organism Suscep-
tibility Study. These data were used to produce the ratio
of ƒAUC
0–24
to the MIC
90
(ƒAUC
0–24
/MIC
90
), a phar-
macodynamic predictor of bacterial eradication. Monte
Carlo simulations were used to analyze the potential for
garenoxacin 400 mg QD, gemifloxacin 320 mg QD,
and moxifloxacin 400 mg QD to achieve target
ƒAUC
0–24
/MIC
90
ratios of 30, 40, 100, and 120 against
S pneumoniae in serum and ELF from hospitalized pa-
tients with CAP. Target ratios of 30 and 40 were used
to assess the probability of bacterial eradication, while
ratios of 100 and 120 were used to assess the probabili-
ty of preventing development of resistance.
Results: Monte Carlo simulations indicated that all
3 fluoroquinolones had a high probability (>90%) of
attaining target ƒAUC
0–24
/MIC
90
ratios of 30 and 40
against S pneumoniae in both serum and ELF. Garen-
oxacin 400 mg QD was associated with a >95% prob-
ability of achieving target ƒAUC
0–24
/MIC
90
ratios of
100 and 120 in both serum and ELF. Both gemifloxacin
320 mg QD and moxifloxacin 400 mg QD were asso-
ciated with high probabilities of attaining ƒAUC
0–24
/
MIC
90
ratios of 100 and 120 in ELF (>95%); the prob-
ability of gemifloxacin and moxifloxacin attaining these
targets in serum ranged from 78.3% to 88.0%.
Conclusion: Based on these simulations, garenoxacin
400 mg QD, gemifloxacin 320 mg QD, and moxi-
floxacin 400 mg QD appeared likely to achieve target
serum and ELF concentrations against S pneumoniae in
hospitalized patients with CAP, with a low potential to
select for resistance. (Clin Ther. 2007;29:2685–2689)
Copyright © 2007 Excerpta Medica, Inc.
Key words: target attainment, fluoroquinolones,
community-acquired pneumonia, Monte Carlo analysis.
INTRODUCTION
Community-acquired pneumonia (CAP) is a common
respiratory illness that is frequently life threatening in
the elderly.
1
CAP is a significant cause of both mor-
bidity and mortality worldwide.
1
Streptococcus pneu-
moniae accounts for 9% to 55% of cases of CAP
requiring hospitalization
1–5
and is the most common
cause of fatal CAP.
6
Treatment of lower respiratory
infections, particularly CAP, commonly includes the
use of the newer respiratory fluoroquinolones.
7
Several authorities, including the Infectious Diseases
December 2007 2685
Comparative Pharmacodynamics of Garenoxacin,
Gemifloxacin, and Moxifloxacin in Community-Acquired
Pneumonia Caused by Streptococcus pneumoniae:
A Monte Carlo Simulation Analysis
Ayman M. Noreddin, PhD
1,2
; Angela A. Reese, PharmD
1
; Melissa Ostroski, PharmD
1
;
Daryl J. Hoban PhD
2,3
; and George G. Zhanel, PharmD, PhD
2,3
1
Department of Pharmacy Practice and Pharmaceutical Sciences, College of Pharmacy, University of
Minnesota, Duluth, Minnesota;
2
Department of Medical Microbiology, Faculty of Medicine, University of
Manitoba, Winnipeg, Canada; and
3
Department of Clinical Microbiology, Health Sciences Centre,
Winnipeg, Canada
Accepted for publication October 2, 2007.
doi:10.1016/j.clinthera.2007.12.019
0149-2918/$32.00
Printed in the USA. Reproduction in whole or part is not permitted.
Copyright © 2007 Excerpta Medica, Inc.