Aqueous and vitreous penetration of linezolid and levofloxacin after oral administration.
OBJECTIVE
To evaluate the time course of drug concentrations achieved in aqueous (AQ), vitreous (V), and serum (S) compartments after oral administration of linezolid and levofloxacin.


METHODS
Randomized, clinical trial.


METHODS



METHODS
Clinical practice.


METHODS
Sixteen patients (16 eyes) undergoing vitrectomy who had not had a prior pars plana vitrectomy in the study eye were randomly assigned to one of 4 groups.


METHODS
AQ, V, and S samples were obtained from all subjects after single concomitant doses of linezolid 600 mg and levofloxacin 750 mg between 1 and 12 h before the procedure: group A = 1-3 h; group B = 3-6 h; group C = 6-9 h; group D = 9-12 h.


METHODS
AQ, V, and S concentrations of linezolid and levofloxacin.


RESULTS
Overall mean concentrations ± standard deviation (μg/mL) achieved by linezolid in AQ, V, and S compartments were 3.32 ± 2.06, 2.98 ± 1.87, and 7.91 ± 3.94, respectively. Overall mean concentrations ±standard deviation (μg/mL) achieved by levofloxacin in AQ, V, and S compartments were 2.19 ± 1.92, 1.95 ± 1.27, and 7.38 ± 3.47, respectively.


CONCLUSIONS
Single concomitant doses of linezolid and levofloxacin achieved AQ and V concentrations above the minimum inhibitory concentration for 90% of common ocular gram-positive and gram-negative pathogens up to 12 h after administration. The combination of linezolid and levofloxacin represents a viable option for the prophylaxis and management of endophthalmitis.
Department of Pharmacy Practice, University of the Sciences in Philadelphia, Philadelphia, PA 19104, USA. j.george@usp.edu
Jomy M
JM
George
Richard
R
Fiscella
Michael
M
Blair
Keith
K
Rodvold
Lawrence
L
Ulanski
John
J
Stokes
Norman
N
Blair
Laura
L
Pontiggia
D000081:Acetamides / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D001082:Aqueous Humor / Q000378:metabolism; D004359:Drug Therapy, Combination; D009877:Endophthalmitis / Q000517:prevention & control; D005260:Female; D006801:Humans; D064704:Levofloxacin; D000069349:Linezolid; D008297:Male; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D015242:Ofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D023303:Oxazolidinones / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D013997:Time Factors; D014018:Tissue Distribution; D014821:Vitrectomy / Q000379:methods; D014822:Vitreous Body / Q000378:metabolism
D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D064704:Levofloxacin; D015242:Ofloxacin; D000069349:Linezolid