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A. Arias–Puente, C. García–Saenz, M. Fresnadillo–Martinez, J. Bañuelos; Aqueous Humor Human Concentrations of Oral and Topical Fluoroquinolones . Invest. Ophthalmol. Vis. Sci. 2006;47(13):1920.
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To compare the intraocular concentrations of 3 different oral fluoroquinolones: ciprofloxacin, levofloxacin and moxifloxacin and 3 different topical ones: ciprofloxacin, ofloxacin and lomefloxacin after topical administration into the human eye.
A randomized clinical study was done with fluoroquinolones available in Europe. A total of 90 consecutive patients scheduled for cataract surgery were randomly divided into six groups the day before surgery. Treatment groups received either topical or oral fluoroquinolones. The first group received 2 oral 500 mg doses of ciprofloxacin at 12–hours interval. The second group received a single 500 mg dose of levofloxacin and the third group was assigned a single 400 mg dose of moxifloxacin. The fourth, fifth and sixth group received either topical ciprofloxacin or ofloxacin or lomefloxacin (instillation of one drop of ophthalmic solution every 10 minutes starting 40 minutes before surgery). At the time of surgery, 0.1 ml aqueous fluid was aspirated from the anterior chamber just before the operation, and immediately stored at –80ºC. Aqueous humor concentration of different fluoroquinolones were calculated using a two dimension diffusion biological assay, based on the determination of the level of antibiotic by a definable microbiologic response to a series of standard antibiotic concentrations by a strain of test organism
The mean aqueous levels or the oral antibiotics were as follows: ciprofloxacin 0.5 ± 0.25 µ g/ml, levofloxacin 1.5 ± 0.5 µ g/ml and moxifloxacin 2.4 ± 0.85 µ g/ml. On the other hand the mean aqueous levels of topical fluoroquinolones were: ciprofloxacin 0.4 ± 0.3 µ g/ml and ofloxacin 1.2 ± 0.5 µ g/ml. The test was not sensitive enough for lomefloxacin. Mean aqueous levels of oral levofloxacin, oral moxifloxacin and topical ofloxacin were above the 90% minimum inhibitory concentration for most of the common micro–organisms causing endophthalmitis
Therapeutic concentrations of fluoroquinolones after oral administration were found in all the aqueous human humor samples studied with better levels for levofloxacin and moxifloxacin. After topical administration, Ofloxacin achieves better intraocular levels than ciprofloxacin into the noninflamed eye. These fluoroquinolones could be considered as effective antibacterial agents in the prophylaxis of bacterial endophthalmitis.
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