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T. Bourcier, F. Jehl, A. Sauer, G. Prevost, C. Speeg-Schatz, M. Saleh; Vitreal Penetration of Linezolid After Oral Administration in Rabbits. Invest. Ophthalmol. Vis. Sci. 2008;49(13):843. doi: https://doi.org/.
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© ARVO (1962-2015); The Authors (2016-present)
The aim of this study was to evaluate the ocular distribution after oral administration in rabbits, of linezolid, which represents the first new class (oxazolidinone) of antimicrobial agent to be introduced into infectious disease practice in over two decades.
Twelve New Zealand rabbits were separated in 3 groups. Group 1 (n=4) received a single oral dose of linezolid (175 mg/kg), group 2 (n=6) received an oral dose of 120 mg of linezolid (35 mg/kg), and group 3 (n=2) an intravitreal injection of 120 mg of linezolid. All serum and vitreous samples were collected under general anesthesia (1ml ketamine) at 15, 30, 45 minutes, and 2,4,6,8 hours following administration. Drug concentrations in the serum and vitreous were measured by high-performance liquid chromatography. Animals were treated in compliance with the ARVO Statement for the Use of Animals in Ophthalmic and Vision Research.
Peak concentration after oral administration of linezolid was reached at 1 h in serum and 2 h in vitreous (Tmax). Mean concentrations at Tmax in group 1 (600mg) were 87, 32+/-6,7 mg/L in serum, and 25,23 +/- 3,23 mg/L in vitreous.In order to reach pharmacokinetic parameters close to those observed in human serum, the given dose was reduced in group 2 (120 mg). In consequence, concentrations were respectively, 11,87 +/- 3,45 mg/L in serum and 3,4 +/- 1,32 mg/L in vitreous.At last, direct intravitreal injection of linezolid produced peaks hundredfold higher than after oral administration.
Linezolid is the most effective antibiotic available against Gram positive bacterias. In this report, we show that linezolid passes the blood-ocular barrier and reaches concentrations 8 times higher than the minimal inhibitory concentration (MIC) for S.epidermidis after a single oral dose administration of 120 mg. Thus, this new antibiotic could play in the future a key role in the management of acute bacterial endophthalmitis.
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