Basic and clinical studies on cefluprenam in ophthalmology

Abstract

We conducted a basic and clinical evaluation on a newly injectable cephalosporin, cefluprenam (CFLP) in the ophthalmological field and results were obtained as follows.
1) CFLP had broad spectrum against Gram-positive and negative bacteria. The susceptibility distribution of clinical isolates of Staphylococcus aureus (20 strains) stayed with in≤0.19-1.56μg/ml, showing the maximum distribution at 0.39μg/ml. The susceptibility distribution of clinical isolates of Pseudomonas aeruginosa (20 strains) stayed between 0.39-≥100μg/ml.
2) When CFLP was administered intravenously to matured white rabbits at a dose of 50mg/kg, the peak aqueous humor level was 4.1-4.2μg/ml after 15-30 minutes. At the time of 30 minutes after dosing, the ocular tissue levels were 6.8±0.1-53.4±0.4μg/g in extraocular tissues and 0.6-16.6±1.2μg/g in intraocular tissues.
3) Penetration of CFLP into human aqueous humor of anterio chamber were detected that the concentrations were 0.69-2.7μg/ml at 60-120 minutes after CFLP administration 1g dose d.i.v. High CFLP concentration in lacrimal sac of human was obtained as 15.6μg/g at 3 hours after CFLP administration 1g dose d.i.v.
4) CFLP was administered intravenously 1 g twice a day to 29 cases consisting of 1 blepharitis, 7 dacryosystitis, 13 corneal ulcer, 1 endophthalmitis, 4 panophthalmitis and 3 orbital cellulitis. Clinical responses were excellent in 11 cases, good in 13 cases, poor in 4 cases and unevaluable in 1 case showing the efficacy rate of 85.7%. Adverse drug reactions noted in 2 cases and abnormal laboratory findings recognized in 6 case.