BASIC AND CLINICAL STUDIES OF SPARFLOXACIN IN THE FIELD OF OPHTHALMOLOGY

• Published in: CHEMOTHERAPY Vol. 39; no. Supplement4; pp. 681 - 691
• Main Authors: Ooishi, Masao, Sakaue, Fujio, Tazawa, Hiroshi, Motoyama, Mariko, Miyao, Masuya, Oomomo, Akiko, Imai, Akira
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 1991
• Subjects: Sparfloxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.39.Supplement4_681

Sparfloxacin (SPFX) has a broad spectrum of antimicrobial activity against Gram-positive and negative bacteria similar to norfloxacin, ofloxacin, enoxacin and ciprofloxacin, but was found to exhibit stronger activity than the other quinolones. The sensitivity distribution for 20 clinically isolated strains of Staphylococcus aureus ranged from 0.02 to 0.09μg/ml, and that for 20 isolates of Pseudomonas aeruginosa ranged from 0.39 to 12.5μg/ml, in which the 5 isolates (25%) presented the distribution peak values of 1.56μg/ml. When SPFX was orally administered once to white adult rabbits at the dose of 50mg/kg, the peak value in the aqueous humor was 0.74μg/ml at 2 hours and the aqueous humor/serum concentration ratio was 0.224. The ocular tissue concentration at 2 hours ranged from 1.53 to 3.64μg/g in the extraocular tissues, and 0.12 to 3.08μg/g (or per ml) in inner ocular tissues. A clinical trial was conducted in a total of 45 patients with blepharitis (7), hordeolum (14), meibomianitis (6), lid abscess (2), chronic dacryocystitis (9), corneal infiltration (2), corneal ulcer (4) and conjunctival abscess (1). Their clinical response in a dosage regimen using SPFX tablets of 100 to 300mg once or twice daily, was excellent in 18 cases, good in 18, fair in 8 and poor in 1, the efficacy rate being 80.0%. The side effect of a rash was observed in one case (2.2%). When SPFX in a powder form was administered 1200mg) once to a total of 14 patients: 3 cases with blepharitis, 3 with external hordeolum, 3 with chronic dacryocystitis, 5 with corneal infiltration. The clinical response was excellent in 5, good in 7 and fair in 2 cases; the efficacy rate being 85.7% without side effects.