Rouan M C, Lecaillon J B, Guibert J, Modai J, Schoeller J P
Antimicrob Agents Chemother. 1985 Feb;27(2):177-80. doi: 10.1128/AAC.27.2.177.
After intravenous bolus injections of 0.5, 1, and 2 g of cefotiam to three healthy volunteers, the mean (+/- standard deviation) total plasma clearances measured for each dose were, respectively, 26.8 +/- 2.7, 22.8 +/- 0.8, and 17.8 +/- 0.9 liters/h; the terminal elimination half-lives were 54.0 +/- 0.1, 68 +/- 15, and 98 +/- 36 min; and the renal clearances were 16.0 +/- 2.9, 13.3 +/- 1.4, and 11.3 +/- 2.6 liters/h. The 24-h urinary recovery was independent of the dose and averaged 53% of the dose. After intramuscular administration of 1 g of cefotiam to three healthy volunteers, a mean (+/- standard deviation) peak concentration of 16.6 +/- 5.1 micrograms/ml was reached at 0.75 to 1 h post dosing. The concurrent intramuscular administration of lidocaine and cefotiam did not modify the kinetics of cefotiam. During a constant-rate infusion, the steady-state plasma clearance decreased slightly when the infusion rate was increased. There was no trend towards accumulation of cefotiam in plasma during chronic treatment with 1 g intravenously every 12 h for 10 days.
对三名健康志愿者静脉推注0.5克、1克和2克头孢替安后，各剂量测得的平均（±标准差）总血浆清除率分别为26.8±2.7、22.8±0.8和17.8±0.9升/小时；终末消除半衰期分别为54.0±0.1、68±15和98±36分钟；肾清除率分别为16.0±2.9、13.3±1.4和11.3±2.6升/小时。24小时尿液回收率与剂量无关，平均为剂量的53%。对三名健康志愿者肌肉注射1克头孢替安后，给药后0.75至1小时达到的平均（±标准差）峰值浓度为16.6±5.1微克/毫升。同时肌肉注射利多卡因和头孢替安并未改变头孢替安的动力学。在恒速输注期间，当输注速率增加时，稳态血浆清除率略有下降。每12小时静脉注射1克，持续10天进行慢性治疗期间，血浆中头孢替安没有蓄积趋势。
