The Kinetics of Anterior Chamber Ofloxacin Penetration

Ciprofloxacin and ofloxacin aqueous humor concentrations after topical administration in dogs undergoing cataract surgery

“…We acknowledge, however, that we did not test this in a randomized concurrent trial. The higher aqueous humor ofloxacin concentrations compared to ciprofloxacin are consistent with the drug properties and findings for humans 14,16,17,24,25 . In humans, one large‐scale study of over 9000 cataract surgery patients showed that postoperative septic endophthalmitis rates are lower with the prophylactic use of ofloxacin (1 per 1000 cases) than ciprofloxacin (3.7 per 1000 cases) 39…”

“…In one human study, peak aqueous humor concentration of ofloxacin (after topical administration of 1 drop every 2 h for five doses, and then 1 drop every 5 min for five doses) was obtained after 100–150 min 13 . The point of maximum drug concentration may not have been reached or detected in our 157–239‐min long studies.…”

“…Ciprofloxacin and ofloxacin reach high tear film concentrations in rabbits and humans respectively 11,12 . Topical ofloxacin and ciprofloxacin cross the corneal barrier and penetrate into the aqueous humor of preoperative human cataract patients after various therapy protocols, with levels exceeding the MIC 90 for most potential intraocular bacterial contaminants 13–17 . Ofloxacin reaches higher aqueous humor concentrations than ciprofloxacin and norfloxacin in humans 16,17 .…”

Meta-analysis of six clinical phase III studies comparing lomefloxacin 0.3% eye drops twice daily to five standard antibiotics in patients with acute bacterial conjunctivitis

“…A long tear retention time of several hours at levels above MIC 90 of many ocular pathogens has been observed after instillation of one or two drops of the ophthalmic lomefloxacin 0.3% solution (Okacin). Okacin has an excellent transcorneal penetration in rabbits [9,29] and in humans [21] which compares favorably with other ophthalmic fluoroquinolones [4,8]. Lomefloxacin 0.3% was found to be highly efficacious in bacterial conjunctivitis, bacterial keratitis or endophthalmitis in animal studies [14,23,28].…”

Aqueous Humour Ofloxacin Concentration after Topical Instillation in Patients with Dry Eye Disease

“…Confined systemic exposure leads to reduced risk of side effects that may result from administration through other common routes (per os, intravitreally), reduced risk of resistance, and the achievement of high concentrations on the ocular surface. Bouchard et al reported that AqH aspiration within one hour of the last ofloxacin dose led to diminished AqH concentration in comparison to sampling afterward [31]. Nevertheless, the cornea comprises a complicated barrier in intraocular penetration, mainly subject to its unique anatomy and the physicochemical properties of the antimicrobial agent.…”