Basic and clinical studies on cefluprenam in ophthalmology

• Published in: Japanese Journal of Chemotherapy Vol. 43; no. Supplement4; pp. 242 - 252
• Main Authors: Motoyama, Mariko, Tazawa, Hiroshi, Hotta, Akihiro, Ooishi, Masao, Abe, Tatsuya, Suzuki, Akiko, Chiba, Kagari, Takahasi, Kuniko, Hara, Jiro, Miyagawa, Shinichi, Yasuda, Fuyuko, Imai, Akira, Tamai, Makoto, Yoshino, Kei, Kamata, Ryuji, Miyao, Masuya, Tazawa, Yutaka, Sasagawa, Tomoyuki, Katoh, Keiichi, Nomura, Yoshiko, Fujiwara, Takaaki, Okamura, Ryoichi, Okura, Fumiko
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 1995; 公益社団法人 日本化学療法学会
• Subjects: cefluprenam; 眼組織内移行; 細菌性眼科感染症
• ISSN: 1340-7007; 1884-5886
• DOI: 10.11250/chemotherapy1995.43.Supplement4_242

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.