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.
Cochereau-Massin
I
I
Institut National de la Santé et de la Recherche Médicale U13, Hôpital Claude Bernard, Paris, France.
Bauchet
J
J
Marrakchi-Benjaafar
S
S
Saleh-Mghir
A
A
Faurisson
F
F
Vallois
J M
JM
Vallee
E
E
Pocidalo
J J
JJ
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