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F. A. Bucci, Jr., R. Evans, L. Amico, P. G. Ambrose, B. L. Schwam; The Pharmacokinetics and Aqueous Humor Penetration of Levofloxacin 1.5% and Moxifloxacin 0.5% in Patients Undergoing Cataract Surgery. Invest. Ophthalmol. Vis. Sci. 2009;50(13):304.
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To compare the aqueous penetration and pharmacokinetics of levofloxacin 1.5% (LEVO) and moxifloxacin 0.5% (MOXI) in the aqueous humor of patients undergoing phacoemulsification.
Ninety-seven phacoemulsification patients participated in a 4-day, single-center, single-masked, randomized, active comparator, parallel group study comparing LEVO and MOXI concentrations in the aqueous humor. Patients were randomized in a 1:1 ratio to receive either levofloxacin (n=49) or moxifloxacin (n=48) to 1 of 4 sub-groups. These sub-groups indicated the time between the last drop of study medication and the sample collection at surgery. Each patient was instructed to take 1 drop 4 x day for 3 days prior to their scheduled surgery. On the day of surgery, patients were instructed to use their study drop at 1 of 4 prearranged times. Aqueous samples were taken at 1, 2, 4 or 6 hours (± 5 minutes) following the last drop. The aqueous samples were collected with a 30 gauge needle on a TB syringe through peripheral clear cornea. Drug concentrations were determined by a validated LC-MS/MS.
Aqueous concentrations were higher for LEVO when compared to MOXI at all time periods. The mean aqueous penetration levels at ONE hour after the last study drop was given were LEVO 1.34/ MOXI 0.83 µg/ml significant at p=0.036 with LEVO 61% > MOXI. The TWO hour levels were LEVO 1.43/ MOXI 0.87 µg/ml significant at p=0.008 with LEVO 65% > MOXI. At FOUR hours the levels were LEVO 0.82 / MOXI 0.54 µg/ml trended toward significance p=0.10 with LEVO 52% > MOXI. At SIX hours following the last study drops the levels were LEVO 0.70 / MOXI 0.40 µg/ml and again reached statistical significance p=0.13 with LEVO 75% > MOXI. The mean AUC 1-6 (area under the curve) for LEVO was significantly higher than MOXI (p<0.001). The highest median concentration of LEVO was 1.60µg/ml vs. 0.83 µg/ml for MOXI (p<0.001).
LEVO 1.5% demonstrated significantly greater aqueous penetration vs. MOXI 0.5% at three of the four time intervals following the last drop administered prior to cataract surgery. LEVO 1.5% achieved at least 50% more aqueous absorption at all time periods evaluated. The AUC 1-6 for LEVO 1.5% was significantly greater than MOXI 0.5%, and the highest median conc. of LEVO was almost 2X compared to MOXI. These results suggest that LEVO 1.5% could be an effective agent in the prophylaxis of endophthalmitis at the time of cataract surgery.
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