Havard C W, Bax R P, Samanta T C, Pearson R M, Brumfitt W, Hamilton-Miller J M, Dash C H
Thorax. 1980 May;35(5):379-83. doi: 10.1136/thx.35.5.379.
A detailed pharmacokinetic study of cefuroxime has been carried out. Levels of cefuroxime were determined in the blood, sputum, saliva, and urine of 23 patients receiving parenteral cefuroxime eight hourly for chest infections. Profiles were obtained after the first dose and on the final (fifth) day of treatment. Antibiotic levels in the sputum reached 0.8 mg/l within one hour of the first injection, and were maintained close to this value for six hours. There was a build-up by the fifth day, mean cefuroxime concentrations at this time reaching 1.8 mg/l. This concentration was maintained for a prolonged period. Salivary concentrations were detectable but low (maximum mean value was 0.6 mg/l). Concentrations of antibiotic were significantly higher in the serum than those observed after the same doses in volunteers. In the patients there was no build-up in serum levels between the first and fifth days. The data obtained explain the clinical efficacy of cefuroxime in the treatment of lower respiratory infections, and suggest that a 12-hour schedule may be feasible.
已对头孢呋辛进行了详细的药代动力学研究。对23例因胸部感染每8小时接受一次头孢呋辛注射治疗的患者的血液、痰液、唾液和尿液中的头孢呋辛水平进行了测定。在首剂用药后以及治疗的最后（第五）天获取了药代动力学曲线。首次注射后1小时内，痰液中的抗生素水平达到0.8 mg/l，并在6小时内维持在该值附近。到第五天有所蓄积，此时头孢呋辛的平均浓度达到1.8 mg/l。该浓度维持了较长时间。唾液中的浓度可检测到，但较低（最大平均值为0.6 mg/l）。血清中的抗生素浓度显著高于志愿者接受相同剂量后观察到的浓度。在患者中，血清水平在第一天和第五天之间没有蓄积。所获得的数据解释了头孢呋辛治疗下呼吸道感染的临床疗效，并表明12小时给药方案可能是可行的。
