Aqueous humor levels of topically applied levofloxacin, norfloxacin, and lomefloxacin in the same human eyes.
OBJECTIVE
To assess the relative penetration of topical eyedrops of 3 fluoroquinolones into the aqueous humor in human eyes.


METHODS
Department of Ophthalmology, Sano-Kosei Hospital, Sano, Japan.


METHODS
Fifty-nine cataract patients (36 women, 23 men) received 3 drops each of levofloxacin 0.5%, norfloxacin 0.3%, and lomefloxacin 0.3% in the same eye at 15-minute intervals beginning 90 minutes before cataract surgery. At the beginning of surgery, 50 microL of aqueous humor was aspirated from the anterior chamber and stored at -80 degrees C until analyzed. The drug concentrations in the samples were analyzed using high-performance liquid chromatography.


RESULTS
Five patients were excluded from the study because their sample volumes were insufficient. Norfloxacin was detected in 3 patients; the mean aqueous humor level was 0.10 microg/mL +/- 0.02 (SD). Levofloxacin was detected in all cases; the mean aqueous humor level was 0.60 +/- 0.28 microg/mL (n = 54). Lomefloxacin was not detected in 10 patients; the mean aqueous humor level was 0.23 +/- 0.11 microg/mL (n = 44).


CONCLUSIONS
Topically applied levofloxacin had better penetration into the aqueous humor than lomefloxacin and norfloxacin.
Yamada
Masakazu
M
Departments of Ophthalmology, Keio University School of Medicine, Tokyo, Japan. yamadam@sc.itc.keio.ac.jp
Mochizuki
Hiroshi
H
Yamada
Kyoko
K
Kawai
Masataka
M
Mashima
Yukihiko
Y
D000368:Aged; D000369:Aged, 80 and over; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D000892:Anti-Infective Agents, Urinary / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D024841:Fluoroquinolones / Q000493:pharmacokinetics*; D006801:Humans; D064704:Levofloxacin; D008297:Male; D009643:Norfloxacin / Q000493:pharmacokinetics*; D015242:Ofloxacin / Q000493:pharmacokinetics*; D015363:Quinolones / Q000493:pharmacokinetics*
D000890:Anti-Infective Agents; D000892:Anti-Infective Agents, Urinary; D024841:Fluoroquinolones; D015363:Quinolones; D064704:Levofloxacin; D015242:Ofloxacin; C053091:lomefloxacin; D009643:Norfloxacin