Clinical pharmacokinetics of cefotaxime and penetration in sputum, bone, and prostatic tissue

Cefotaxime is a new powerful methoxycephalosporin with a broad anti-microbial spectrum, suitable for parenteral administration. In the present study, the concentrations of cefotaxime in serum and in bronchial secretion were determined after intramuscular injection of 1 gm every eight hours for seven days. Subjects were patients suffering from an exacerbation of chronic bronchitis. Serum levels versus time curve were interpreted in terms of a one-compartment open model. Pharmacokinetic parameters after single and multiple doses were investigated. No evidence of significant accumulation was found. Furthermore, a type of in vivo rate of killing with cefotaxime was investigated by evaluating the decrease in the number of colonies in bronchial mucus cultures daily for seven days. In two groups of volunteers who had to undergo surgery, bone and prostatic concentrations of cefotaxime were determined and correlated with serum levels.