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The pharmacokinetics of linezolid in the non-inflamed human eye

¹ Department of Ophthalmic Surgery, University Hospitals of Leicester NHS Trust, Leicester LE1 5WW, UK
² Department of Clinical Microbiology, University Hospitals of Leicester NHS Trust, Leicester LE1 5WW, UK
³ Bristol Centre for Antimicrobial Research and Evaluation, Southmead Hospital, Bristol BS10 5NB, UK
⁴ Department of Ophthalmic Surgery, University Hospitals of Leicester NHS Trust, Leicester LE1 5WW, UK

Correspondence to:
Correspondence to:
Jeremy Prydal
Department of Ophthalmic Surgery, University Hospitals of Leicester NHS Trust, Infirmary Square, Leicester LE1 5WW, UK; jip{at}prydal.co.uk

ABSTRACT
Aim: This study describes the ocular pharmacokinetics of linezolid, an antibiotic with broad spectrum activity against those Gram positive bacteria that are the most frequent cause of postoperative endophthalmitis.

Method: Patients undergoing routine cataract surgery were given a single oral 600 mg dose of linezolid at a variable time before surgery. Aqueous and serum levels of linezolid were assayed by high performance liquid chromatography, and a pharmacokinetic curve constructed from the pooled results.

Results: Orally administered linezolid rapidly achieves levels in the aqueous of non-inflamed eyes that exceed the concentration required to kill Gram positive bacteria (maximum mean concentration 6.8 (SD 1.2) µg/ml at 2–4 hours post-dose). An effective concentration is maintained for at least 12 hours, the standard interdose interval for this antimicrobial.

Conclusion: Linezolid offers the possibility of a rapid, oral approach to effective treatment of most cases of postoperative endophthalmitis, with the potential of improving visual outcome.

Abbreviations: HPLC, high performance liquid chromatography; MIC, minimal inhibitory concentration; POE, postoperative endophthalmitis

Keywords: linezolid; pharmacokinetics; endophthalmitis