Kinetics and tolerability of intravitreal pefloxacin in rabbits

In the treatment of patients with bacterial endophthalmitis, the intravitreal administration of antibiotics is suitable for induction therapy since it provides immediate high concentrations in the vitreous humor. Pefloxacin has been shown to have good intraocular penetration when given systemically....

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Bibliographic Details
Published in:Journal of antimicrobial chemotherapy 1994-02, Vol.33 (2), p.231-242
Main Authors: Cochereau-Massin, I., Marrakchi-Benjaafar, S., Bauchet, J., Vallois, J. M., Faurisson, F., D'Hermies, F., Pocidalo, J. J.
Format: Article
Language:English
Subjects:
Albinism, Ocular - metabolism
Animals
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Chromatography, High Pressure Liquid
Female
Half-Life
Lens, Crystalline - metabolism
Medical sciences
Pefloxacin - administration & dosage
Pefloxacin - pharmacokinetics
Pefloxacin - toxicity
Pharmacology. Drug treatments
Rabbits
Retina - metabolism
Retina - pathology
Vitreous Body - metabolism
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Summary:In the treatment of patients with bacterial endophthalmitis, the intravitreal administration of antibiotics is suitable for induction therapy since it provides immediate high concentrations in the vitreous humor. Pefloxacin has been shown to have good intraocular penetration when given systemically. In order to extend the potential routes of administration of this agent, we have assessed the kinetics and toxicity of pefloxacin in rabbit phakic eyes following intravitreal instillation. Kinetic parameters were determined for 12 albino and 12 pigmented rabbits after a single injection of 80 μg. Pefloxacin was undetectable in the aqueous humor but high concentrations were found in the chorioretina. The vitreal half-life was short (3 h). These results were consistent with posterior elimination via the chorioretina. Pefloxacin concentrations in the iris and chorioretina of pigmented rabbits were twofold greater than those in albino rabbits, probably because of binding to the pigmentary apparatus. Toxicity studies, including ophthalmological and histopatho-logical investigations, identified a maximum non-toxic dosage of 400 μg. Intravitreal pefloxacin may therefore be suitable for induction therapy in patients with endophthalmitis, although further studies in primates are required to confirm the efficacy and tolerability of this route of administration.
ISSN:0305-7453
1460-2091
DOI:10.1093/jac/33.2.231