Efficacy and ocular penetration of sparfloxacin in experimental streptococcal endophthalmitis.
Gram-positive cocci are the most common pathogens in severe human eye infections. Streptococcal endophthalmitis is a devastating infection, and intravitreal antibiotic therapy is limited by retinal toxicity. Because few systemic antistreptococcal antibiotics penetrate into the vitreous, sparfloxacin, a newer quinolone with improved antistreptococcal activity, might be of interest. We therefore assessed its efficacy by the intravitreal route in a rabbit model of streptococcal endophthalmitis. The vitreal bacterial count (mean +/- standard deviation log10 CFU per milliliter) was significantly reduced after an intravitreal injection of 800 micrograms of sprafloxacin (4.9 +/- 0.7) relative to the counts in untreated control (7.1 +/- 0.7) and pefloxacin-treated (7.8 +/- 1.2) eyes. After systemic administration to rabbits, the maximum concentration of sparfloxacin in serum was 5.6 micrograms.ml-1 and the half-life was 7.5 h. Sparfloxacin exhibited very good penetration ratios in the vitreous (54%), cornea (76%), and lens (36%). In the vitreous, the levels of sparfloxacin remained greater than the MICs for most gram-positive cocci for up to 18 h. Further experimental studies are warranted to determine the efficacy of systemic sparfloxacin as adjuvant therapy in the treatment of human endophthalmitis.
Institut National de la Santé et de la Recherche Médicale U13, Hôpital Claude Bernard, Paris, France.
I
I
Cochereau-Massin
J
J
Bauchet
S
S
Marrakchi-Benjaafar
A
A
Saleh-Mghir
F
F
Faurisson
J M
JM
Vallois
E
E
Vallee
J J
JJ
Pocidalo
D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D009877:Endophthalmitis / Q000188:drug therapy* / Q000382:microbiology; D005123:Eye / Q000378:metabolism*; D024841:Fluoroquinolones; D006207:Half-Life; D007267:Injections; D007273:Injections, Intramuscular; D015366:Pefloxacin / Q000627:therapeutic use; D015363:Quinolones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011817:Rabbits; D013203:Staphylococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D014822:Vitreous Body
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D015366:Pefloxacin; C061363:sparfloxacin