Grose W E, Bodey G P, Stewart D
Clin Pharmacol Ther. 1976 Nov;20(5):579-84. doi: 10.1002/cpt1976205579.
Comparative studies of cefamandole and cephalothin were carried out in 32 cancer patients. After rapid intravenous injection of 1 gm cefamandole or cephalothin, the peak mean serum concentrations in 11 patients achieved at 0.25 hr were 103.4 mcg/ml and 56.7 mcg/ml, respectively. Except at 6 hr, the serum concentration of cefamandole was higher (p less than 0.05) at all times. The terminal half-lives (t 1/2) were similar, being 1.2 hr for cefamandole and 1.0 hr for cephalothin. Cefamandole, 1 gm intramuscularly, induced a peak mean serum concentration of 26.6 mcg/ml at 1 hr, with a slow decay. Intermittent cefamandole (2 gm intravenously every 6 hr) induced very high mean serum concentrations (7 patients), but at 4 hr the concentrations were similar to those after 1 gm intravenously. Per cent of urinary excretion was similar for both drugs regardless of dose and mode of administration. Continuous-infusion cefamandole or cephalothin (2 gm loading followed by 2 gm every 6 hr) in 14 patients showed consistently higher serum concentrations for cefamandole (p less than 0.05) over a 5-day period. There was no evidence of drug accumulation in the multiple-dose studies. Both the single- and multiple-dose schedules were well tolerated.
对32例癌症患者进行了头孢孟多和头孢噻吩的对比研究。在快速静脉注射1克头孢孟多或头孢噻吩后,11例患者在0.25小时达到的平均血清峰值浓度分别为103.4微克/毫升和56.7微克/毫升。除6小时外,头孢孟多的血清浓度在所有时间均较高(p小于0.05)。终末半衰期(t1/2)相似,头孢孟多为1.2小时,头孢噻吩为1.0小时。肌肉注射1克头孢孟多在1小时时诱导的平均血清峰值浓度为26.6微克/毫升,且衰减缓慢。间歇性静脉注射头孢孟多(每6小时2克)诱导的平均血清浓度非常高(7例患者),但在4小时时浓度与静脉注射1克后相似。无论剂量和给药方式如何,两种药物的尿排泄百分比相似。14例患者持续输注头孢孟多或头孢噻吩(先负荷2克,然后每6小时2克),在5天期间头孢孟多的血清浓度始终较高(p小于0.05)。在多剂量研究中没有药物蓄积的证据。单剂量和多剂量方案的耐受性都很好。