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S.M. Hariprasad, K.J. Blinder, G.K. Shah, R.S. Apte, B. Rosenblatt, M.G. Grand, M.A. Thomas, N.M. Holekamp, W.F. Mieler, R.A. Prince; Determination of Vitreous and Aqueous Concentration of Topically Administered Moxifloxacin 0.5% in Humans . Invest. Ophthalmol. Vis. Sci. 2004;45(13):525.
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Purpose:To investigate the penetration of moxifloxacin 0.5%, a novel fourth–generation fluoroquinolone antibiotic, into the vitreous and aqueous humor after topical administration in humans. Methods:A prospective, non–randomized clinical study of ten consecutive patients scheduled for vitrectomy surgery between September 2003 and October 2003 at the Barnes Retina Institute. Aqueous and vitreous samples were obtained and later analyzed from ten patients after topical administration of moxifloxacin 0.5% every two hours for three days prior to surgery. Assays were performed using high–performance liquid chromatography. Results:Mean moxifloxacin concentrations in vitreous (n=10) and aqueous (n=9) were 0.11 + 0.05 µg/ml and 2.28 + 1.23 µg/ml, respectively. MIC90 levels were far exceeded in the aqueous for a wide spectrum of pathogens including Staphylococcus epidermidis, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Propionibacterium acnes, Haemophilus influenzae, Escherichia coli, Bacillus cereus, Neisseria gonorrhoeae, Proteus mirabilis, and other organisms. Concentration of moxifloxacin in the vitreous did not exceed the MIC90 for several organisms; however, the MIC50 was exceeded for Staphylococcus epidermidis, Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Bacillus cereus, and other gram negatives. Conclusions:The Endophthalmitis Vitrectomy Study revealed that 94.2% of isolates from post–operative endophthalmitis are gram positive bacteria (70% due to Staphylococcus epidermidis). Moxifloxacin has a spectrum of coverage that appropriately encompasses the most common causative organisms in endophthalmitis. The pharmacokinetic findings of this investigation reveal that topically administered moxifloxacin can achieve relatively high aqueous levels. Although vitreous concentrations are lower, the levels achieved may be adequate for prophylaxis. Potential uses for topical moxifloxacin include surgical prophylaxis against post–operative endophthalmitis, treatment of localized filtering bleb infection or blebitis, and adjunctive therapy for the current treatment of endophthalmitis.
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