Penetration of Topically Applied Ciprofloxacin, Norfloxacin and Ofloxacin into the Aqueous Humor of the Uninflamed Human Eye

• Published in: Journal of chemotherapy (Florence) Vol. 9; no. 4; pp. 257 - 262
• Main Authors: Akkan, A.G., Mutlu, I., Ozyazgan, S., Gok, A., Yigit, U., Ozuner, Z., Senses, V., Pekel, H.
• Format: Journal Article
• Language: English
• Published: Firenze Taylor & Francis 1997; EIFT
• Subjects: Administration, Topical; Aged; Aged, 80 and over; Anti-Infective Agents - administration & dosage; Anti-Infective Agents - therapeutic use; Antibiotic Prophylaxis; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Aqueous Humor - drug effects; Aqueous Humor - metabolism; Biological and medical sciences; Cataract Extraction; Ciprofloxacin - administration & dosage; Ciprofloxacin - metabolism; Ciprofloxacin - therapeutic use; Eye Infections - prevention & control; Female; Humans; Male; Medical sciences; Middle Aged; Norfloxacin - administration & dosage; Norfloxacin - metabolism; Norfloxacin - therapeutic use; Ofloxacin - administration & dosage; Ofloxacin - metabolism; Ofloxacin - therapeutic use; Ophthalmic Solutions; Pharmacology. Drug treatments; Human; Cataract; Duration; Aqueous humor; Norfloxacin; Ofloxacin; Eye drop; Prevention; Eye disease; Chemotherapy; Fluoroquinolone derivatives; Lens disease; Absorption; Application method; Ciprofloxacin; Pharmacokinetics; Anterior segment disease; Comparative study; Quinolone derivatives; Topical administration
• ISSN: 1120-009X; 1973-9478
• DOI: 10.1179/joc.1997.9.4.257

This study was undertaken to compare aqueous humor penetration of topical 0.3% ciprofloxacin, 0.3% norfloxacin and 0.3% ofloxacin in 63 patients undergoing cataract surgery. The patients were divided into two groups. Group 1 (long-term treatment) involved 30 patients undergoing cataract extraction who received either 0.3% ciprofloxacin, 0.3% norfloxacin or 0.3% ofloxacin topical drops. Each patient was preoperatively given a single drop per hour six times. At the time of surgery, 0.1 ml aqueous fluid was aspirated from the anterior chamber and immediately stored at −70°C. Topically applied ciprofloxacin, ofloxacin and norfloxacin achieved mean aqueous humor levels of 2.80±1.07, 2.95± 1.19 and 1.50±0.48 μg/ml respectively. There was no statistically significant difference in intraocular mean aqueous levels of ciprofloxacin versus ofloxacin. Topical ciprofloxacin and ofloxacin achieved mean aqueous humor levels significantly higher than norfloxacin (p<0.001 and p<0.0008 respectively).
Group 2 (short-term treatment) involved 33 patients undergoing cataract extraction who received 0.3% ciprofloxacin, 0.3% ofloxacin and 0.3% norfloxacin topical drops. These patients were given one drop at 90 minutes and one drop 30 minutes preoperatively. At the time of surgery, 0.1 ml aqueous fluid was aspirated from the anterior chamber and immadiate-ly stored at −70°C. Topically applied ciprofloxacin, ofloxacin and norfloxacin achieved mean aqueous humor levels of 1.11±0.50, 1.50±0.62 and 1.20±0.43 μg/ml respectively. There was no statistically significant difference in intraocular mean aqueous humor levels of ofloxacin versus norfloxacin and ciprofloxacin versus norfloxacin. Topical ofloxacin achieved a significantly higher mean aqueous humor level than ciprofloxacin (p<0.03). All levels were above the minumum inhibitory concentrations of ciprofloxacin, ofloxacin and norfloxacin for most of the sensitive organisms.