Yates R A, Adam H K, Donnelly R J, Houghton H L, Charlesworth E A, Laws E A
J Antimicrob Chemother. 1983 Jan;11 Suppl:185-91. doi: 10.1093/jac/11.suppl_a.185.
Cefotetan, a third generation cephalosporin, in doses of 0.25, 0.5, 1.0 and 2.0 g was administered intravenously as the disodium salt to ten healthy male Caucasian volunteers and its pharmacokinetics and tolerance determined. The elimination half-life was 3.3 h. The drug was 88% plasma protein bound and 67% was recovered unchanged in the urine. HPLC and bioassay techniques for cefotetan plasma-concentration determinations gave virtually identical results. Cefotetan was well tolerated although half of the volunteers experienced transient mild to moderate diarrhoea. It is concluded that the pharmacokinetic disposition of cefotetan is similar in Caucasian and Japanese subjects and that the long elimination half-life, lack of detectable metabolism and high urinary excretion will result in plasma and urine concentrations in excess of the MIC of sensitive bacteria on a twice daily dosing regime.
头孢替坦是一种第三代头孢菌素，以0.25克、0.5克、1.0克和2.0克的剂量作为二钠盐静脉注射给10名健康的白种男性志愿者，并测定其药代动力学和耐受性。消除半衰期为3.3小时。该药物与血浆蛋白的结合率为88%，67%以原形从尿液中回收。用于测定头孢替坦血浆浓度的高效液相色谱法和生物测定技术得出了几乎相同的结果。尽管一半的志愿者经历了短暂的轻度至中度腹泻，但头孢替坦耐受性良好。得出的结论是，头孢替坦在白种人和日本受试者中的药代动力学特征相似，并且其长消除半衰期、缺乏可检测到的代谢以及高尿排泄量将导致在每日两次给药方案下血浆和尿液浓度超过敏感细菌的最低抑菌浓度。
