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A.R. Watts, J.I. Prydal, K. Tambe, D.R. Jenkins; Linezolid, a New Antibiotic for the Treatment of Post-operative Endophthalmitis . Invest. Ophthalmol. Vis. Sci. 2003;44(13):1451.
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Purpose: post-operative endophthalmitis is most frequently due to infection with gram positive bacteria, particularly coagulase negative Staphylococci. In the past, direct intra-ocular injection of antibiotics was necessary as penetration into the eye from the bloodstream was restricted by the blood-ocular barrier. The few antibiotics that may have achieved therapeutic intra-ocular concentrations following systemic administration had largely gram negative activity. An antibiotic with broad spectrum gram positive activity, which reaches therapeutic levels in the eye following intravenous or oral administration, would offer a significant advance in the treatment of endophthalmitis. Linezolid is the first licensed representative of a new class of antibiotics, the oxazolidinones. Its spectrum of activity is primarily against gram positive bacteria. Our aim was to establish pharmacokinetic curves for intraocular penetration of Linezolid following oral administration. Methods: a single oral dose of 600mg Linezolid was given to patients before routine cataract surgery, at different intervals from 30 to 240 minutes preceding surgery. A sample of 100µl aqueous was taken through a paracentesis at the beginning of the operation, and 5ml of venous blood taken at the same time. Linezolid assays were performed by high performance liquid chromatography, and mean pharmacokinetic curves of Linezolid in aqueous and blood were produced by grouping the results from these patients. Results: Linezolid showed significant penetration into the aqueous humour, and pharmacokinetic curves are presented. Conclusions: Linezolid showed good penetration into these non-inflamed human eyes, despite the intact blood-ocular barrier. In the post-operative endophthalmitis, the blood-ocular barrier is breached, and hence higher levels may be expected. Linezolid has excellent activity against the gram positive bacteria commonly implicated in post-operative endophthalmitis, and these results suggest that Linezolid will be a useful oral treatment for endophthalmitis, and may obviate the need for intraocular injection of antibiotics.
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