Ocular pharmacokinetics, safety and efficacy of intracameral moxifloxacin 0.5% solution in a rabbit model.
OBJECTIVE
This study was carried out to determine the ocular pharmacokinetics, efficacy and potential endothelial toxicity of moxifloxacin (MF) after a single intracameral bolus injection of 500 µg/0.1 ml in a rabbit model.


METHODS
Forty-eight eyes of 24 New Zealand White Rabbits were separated into six groups, each including four rabbits. 0.1 ml of 0.5% intracameral moxifloxacin (500 µg) injection was injected to the right eyes and 0.1 ml of balanced salt solution to the left eyes (control). Aqueous humor (AH) and vitreous samples were collected at the 0.5th, 1st, 3rd, 6th, 12th and 24th hours from both eyes of group 1, 2, 3, 4, 5 and 6, respectively. MF concentrations were determined by high performance liquid chromatography. These were compared with the minimum inhibitory concentrations (MIC) and mutant prevention concentrations (MPC) for frequent endophthalmitis pathogens. Electron and light microscopical evaluation of the corneas were performed.


RESULTS
Moxifloxacin reaches higher concentration than the MIC of all common endophthalmitis pathogens in the AH and exceeds the mutant prevention concentration levels for Streptococcus pneumonia, Streptococcus viridans, flouroquinolone susceptible Coagulase-negative staphylococcus and flouroquinolone susceptible Staphylococcus aureus for 6 h. The half-life of moxifloxacin in the AH was 2.2 h. Electron and light microscopic evaluation revealed no noticeable sign of toxicity.


CONCLUSIONS
Peroperative intracameral moxifloxacin injection for endophthalmitis prophylaxis is a safe and effective method in uncomplicated phacoemulsification surgery.
Department of Ophthalmology, Faculty of Medicine, Baskent University, Ankara, Turkey.
Leyla
L
Asena
Yonca A
YA
Akova
Mustafa T
MT
Goktaş
Atilla
A
Bozkurt
Umit
U
Yaşar
Gülten
G
Karabay
Ebru
E
Demiralay
D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000633:toxicity; D001082:Aqueous Humor / Q000187:drug effects / Q000378:metabolism; D001372:Aza Compounds / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000633:toxicity; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D009877:Endophthalmitis / Q000188:drug therapy*; D019573:Epithelium, Corneal / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D015818:Eye Infections, Bacterial / Q000188:drug therapy*; D024841:Fluoroquinolones; D056965:Injections, Intraocular; D046529:Microscopy, Electron, Transmission; D000077266:Moxifloxacin; D018918:Phacoemulsification; D011804:Quinolines / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000633:toxicity; D011817:Rabbits; D013203:Staphylococcal Infections / Q000188:drug therapy; D013290:Streptococcal Infections / Q000188:drug therapy; D014822:Vitreous Body / Q000187:drug effects / Q000378:metabolism
D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D011804:Quinolines; D000077266:Moxifloxacin