[Basic and clinical studies on cefotaxime]

The most frequently encountered infectious disease in the field of internal medicine is respiratory tract infections. One of the most important requirements for an antibiotic in the treatment of infections is that it must be efficiently transferred to the infected site to attain a high concentration there. In the case of respiratory tract infections, it is desirable for the drug concentration in the sputum to be higher than the MIC for the causative bacterium. Cefotaxime (CTX) expresses potent antibacterial activity against Haemophilus influenzae, Klebsiella pneumoniae and Streptococcus pneumoniae, which are the major causative bacteria of respiratory tract infections. CTX also exerts antibacterial effects against a wide range of other bacteria. We administered CTX to patients with respiratory tract infections, then measured and compared the drug concentrations in the serum and sputum. The results are described below. When 2 g of CTX was drip-infused, the drug concentration in the serum was 113.0 micrograms/ml at 5 minutes after the completion of infusion, 64.9 micrograms/ml at 30 minutes, 38.7 micrograms/ml at 1 hour, 19.0 micrograms/ml at 2 hours, 8.9 micrograms/ml at 4 hours and 3.8 micrograms/ml at 6 hours. The drug concentration in the sputum was 1.29 micrograms/ml at 5 minutes after completion of infusion, 1.54 micrograms/ml at 5 to 30 minutes, 1.36 micrograms/ml at 30 minutes to 1 hour, 1.47 micrograms/ml at 1 to 2 hours, 1.12 micrograms/ml at 2 to 4 hours and 1.35 micrograms/ml at 4 to 6 hours. The drug concentration in the serum was the highest at 5 minutes after completion of the drip-infusion, and then it gradually decreased.(ABSTRACT TRUNCATED AT 250 WORDS)