Ophthalmic use of fosfomycin calcium

Abstract

The results of laboratory and clinical experiments for ophthalmic use of fosfomycin (FOM) were summarized as follows. 1. The minimum growth inhibitory concentrations of FOM against organisms caused ocular infections were 25∼50, μg/ml for KOCH-WEEKS bacillus, 1.56∼6.25, μg/ml for MORAX-AXENFELD diplobacillus, 6.25∼>100gg/ml for Diplo. pneumoniae, >100, μg/ml for Strept. viridans, 6.25∼25μg/ml for Strept. hemolyticus, >100, μg/ml for Cory. diphtheriae, 6.25, μg/ml for N. gonorrhoeae and 1.56, μg/ml for Staph. aureus FDA 209 P. 2. The sensitivity of Ps. aeruginosa and Staph. aureus isolated from eye patients: The distribution of the sensitivity for 11 strains of Ps. aeruginosa was in the range of 3.13∼>100μg/ml, 6strains (54.9%) were inhibited under 12.5μg/ml. Twelve strains of Staph. aureus were sensitive in 1.56∼>100μg/ml, 6 strains (50%) were in 6.25μg/ml. 3. Serum level: After oral administration of 500mg FOM-Ca in a single dose, the peak level was attained 2 hours (4. 33 μg/ml), then decreased gradually up to 8 hours (1.0 μg/ml). 4. Ocular penetration: Ocular penetrations after oral application of 50mg/kg FOM-Ca were examined with rabbit eye. The aqueous humor levels revealed from 1/4 to 6 hours, the peak level was 1 hour (14.6 μg/ml). The high ocular tissue concentrations were recognized in both outer and inner parts of the eye at 2 hours after oral administration. 5. Clinical effects: Twenty-one cases of ocular infections, such as external hordeolum, lid abscess, acute and chronic dacryocystitis, tenonitis, corneal ulcer, infection of socket and perforating injury, were treated with oral administration of FOM-Ca 250mg or 500mg 4 times daily. Good clinical effects were obtained in 13 cases. 6. Side effects: One case of diarrhoea and 2 cases of anorexia were observed, but no cessation of application was needed. No other severe side effects were noticed. © 1975, Japanese Society of Chemotherapy. All rights reserved.