Laboratory and clinical studies on cefluprenam

Cefluprenam (CFLP) a new injectable cephem with a broad antibacterial spectrum and potent antibacterial activity, was evaluated in vitro and in vivo antibacterial activities in comparison with those of ceftazidime (CAZ) and cefzonam (CZON). The results were as follows: 1. Antimicrobial activities: Minimal inhibitory concentrations (MICs) against 483 clinical isolated strains including 16 different species were determined by the microbroth dilution method. CFLP showed excellent antimicrobial activities against gram-positive and gram-negative bacteria. The MIC values of CFLP for gram-positive bacteria were almost same as that of CZON, and superior to CAZ. Against gram-negative bacteria, CFLP showed the best antimicrobial activities among the antibiotics tested. 2. The concentrations of CFLP in serum and sputum: CFLP was intravenously administered in a single dose of 1g to a patient with bronchiectasis, and its concentrations in serum and sputum were measured at various intervals by bioassay. The peak concentration of CFLP in serum was 48.4μg/ml at one hour after the administration. The peak concentration in sputum was 6.57μg/ml at 1.5 hours after the administration. The penetration ratio into sputum was 13.6%. 3. Clinical efficacy and adverse reaction: Fifteen patients with respiratory tract infection were treated with CFLP, and overall efficacy rate was 93.3% (excellent in 1 case, good in 13, poor in 1). As to adverse reactions, fever and urticaria were observed in each one patient, and fever, eruption and drug induced pneumonitis in one patient. Whereas, although abnormal laboratory findings were observed in 6 cases, all were mild and transient. From these data, we can conclude that CFLP is a very useful antibiotics for the treatment of respiratory infectious diseases.