CHANGES IN CONCENTRATION OF CEFOTETAN IN BLOOD AND LUNG TISSUE AFTER INTRAVENOUS ADMINISTRATION

Cefotetan (CTT), a newly-developed cephamycin antibiotic, has been used widely for the treatment of various infectious diseases because of its excellent antibacterial potency and dynamic transport in vivo. Although the drug transfer to almost every organ, tissue, and body fluid has been studied, only a few reports are available regarding the transfer to lung tissue. In the present study, 1g of CTT was intravenously injected in a single dose to each of 22 patients subjected to pulmonary resection. Subsequently, its concentrations in blood and lung tissue were measured in sequence. The degree of transfer of the drug to the lung tissue was calculated to evaluate the pharmacodynamics of CTT in vivo. The following results were obtained in this analysis. 1. The T 1/2(β) of the concentration in blood was 4.18 hours, and AUC0-∞ was 478.7 μg·hr/ml. 2. Cmax in the lung tissue was 31.5 μg/g, and Tmax was 0.83 hour, and tissue concentrations decreased in parallel to blood concentrations. CTT was transferred to the lung tissue to achieve high concentrations following an intravenous administration. Since high concentrations are maintained for a long period of time, this antibiotic is expected to exert an excellent effect in the prevention and the treatment of respiratory infections.