Basic and clinical studies on cefozopran in respiratory infections

• Published in: CHEMOTHERAPY Vol. 41; no. Supplement4; pp. 261 - 268
• Main Authors: Fukuhara, Hiroshi, Inadome, Jun, Kakazu, Tomokazu, Nakamura, Hiroaki, Kaneshima, Hiroshi, Saito, Atsushi, Kusano, Nobuchika, Nakasone, Isamu, Furugen, Yoshiko, Taira, Shinko, Hokama, Seitetsu, Miyagi, Mamoru, Oyakawa, Tominori, Kitagawa, Daishirou
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1993
• Subjects: cefozopran
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.41.Supplement4_261

We performed basic and clinical studies on cefozopran (CZOP), a new parenteral cephalosporin antibiotic, following results were obtained. 1. Antimicrobial activity: The minimum inhibitory concentrations (MIC) of CZOP against a total of 321 clinically isolated strains of 13 species were measured and compared with those of three cephalosporins (ceftazidime, cefuzonam, ceftizoxime) and one carbapenem (imipenem/cilastatin) using the MIC-2000 System (Dynatech Laboratories). CZOP showed stronger bactericidal activity than other three cephalosporin antibiotics against Gram-positive bacteria, and than imipenem/cilastatin against Gram-negative bacteria. CZOP had wide bactericidal activity against these clinically isolated strains except Methicillin-resistant Staphylococcus aureus. 2. CZOP levels in serum and sputum Serum and sputum levels of CZOP (1g intravenous drip infusion for 30 minutes) were measured by the method of bioassay in a patient with chronic bronchitis. Peak serum levels were 50.7μg/ml at the end of drip infusion. Peak sputum levels were 4.1 μg/ml at 1-2 hour after infusion. This suggests that CZOP has rapid and good penetration into the lung. 3. Clinical study results: CZOP was given sixteen patients (pneumonia 11, chronic bronchitis 4, acute bronchitis 1) with respiratory infection. The overall efficacy rate was 87.5% (excellent 9, good 3, fair 1, no change 1). No adverse reaction was noted, though mild and transient elevations in GPT were obserbed in two patients. From the above results, we consider CZOP to be useful antibiotics for the treatment of bacterial respiratory tract infection.