The pharmacokinetics of linezolid in the non-inflamed human eye.

Abstract

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. 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. 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) microg/ml at 2-4 hours post-dose). An effective concentration is maintained for at least 12 hours, the standard interdose interval for this antimicrobial. 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.