Ishikawa M, Akiba N, Kawashima N, Arase T, Sakurai K
First Department of Surgery, Jikei University School of Medicine.
Jpn J Antibiot. 1988 Mar;41(3):331-7.
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, 1 g 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 T1/2(beta) of the concentration in blood was 4.18 hours, and AUC0-infinity was 478.7 micrograms.hr/ml. 2. Cmax in the lung tissue was 31.5 micrograms/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.
头孢替坦（CTT）是一种新开发的头孢霉素类抗生素，因其出色的抗菌效力和体内动态转运而被广泛用于治疗各种传染病。尽管已经对该药物向几乎每个器官、组织和体液的转运进行了研究，但关于其向肺组织转运的报道却很少。在本研究中，对22例接受肺切除术的患者每人单次静脉注射1g头孢替坦。随后，依次测量其在血液和肺组织中的浓度。计算药物向肺组织的转运程度，以评估头孢替坦在体内的药效学。本次分析得出以下结果。1. 血液中浓度的T1/2（β）为4.18小时，AUC0-无穷大为478.7微克·小时/毫升。2. 肺组织中的Cmax为31.5微克/克，Tmax为0.83小时，组织浓度与血液浓度平行下降。静脉给药后，头孢替坦转运至肺组织并达到高浓度。由于高浓度能维持较长时间，预计这种抗生素在预防和治疗呼吸道感染方面将发挥出色的效果。
