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2004 OMIG, Abstract 19

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Comparison of the Penetration into Aqueous Humor in Humans of Two 4th Generation Fluoroquinolones
JP McCulley, W Shine. University of Texas Southwestern Medical School, Dallas, Texas

Purpose: To compare directly the penetration of two commercial 4th generation fluoroquinolones (FQ) [moxifloxacin and gatifloxacin], into aqueous humor (AH) in humans after q.i.d. topical application and to compare to published levels for 2nd and 3rd generation FQs.
Methods: Patients who were otherwise without ocular disease and scheduled for routine phacoemulsification were given, in a double masked fashion, either commercial moxifloxacin 0.5% (Vigamox™) or gatifloxacin 0.3% (Zymar™) to use q.i.d. the day before surgery and on the day of surgery one hour prior to the surgical entry into the anterior chamber. AH samples were taken and chromatographically analyzed by HPLC. AH FQ concentration was calculated by peak comparison to a known concentration peak for ciprofloxacin which was run as an internal standard. These were compared to published concentrations after similar q.i.d. dosing of other available FQs.
Results: Moxifloxacin concentration was 1.88±0.52ug/ml and for gatifloxacin 1.06±0.36 ug/ml. Published values after q.i.d. dosing for ciprofloxacin are 0.07 ug/ml, levofloxacin 0.5% are 0.28 ug/ml but are unavailable for ofloxacin with q.i.d. dosing.
Conclusion: AH antibiotic concentrations after loading regiments are of little clinical relevance. Concentrations achieved at cataract surgery can serve as surrogates for what can be achieved with post-operative topical dosing, e.g. q.i.d. Both 4th generation FQs achieved adequate concentrations with moxifloxacin achieving a far superior (clinically significant) concentration compared to gatifloxacin.

Supported in part by an unrestricted grant from RPB and Alcon Labs
Disclosure code: F C, R

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