Lenfant B, Namour F, Logeais C, Coussediere D, Rivault O, Bryskier A, Surjus A
Roussel Uclaf, Romainville, France.
Antimicrob Agents Chemother. 1995 Sep;39(9):2037-41. doi: 10.1128/AAC.39.9.2037.
Cefodizime is a new expanded-spectrum cephalosporin for parenteral use which possesses a broad antibacterial spectrum and potent antibacterial activity and is stable against most beta-lactamases. The aim of this study was to assess the pharmacokinetics of cefodizime, administered intravenously, over the dose range of 0.5 to 3.0 g in healthy volunteers. Concentrations of cefodizime in the serum and urine were determined by high-performance liquid chromatography. The area under the concentration-time curve from 0 h to infinity and the amount of drug excreted in urine from 0 to 34 h increased in a linear, dose-dependent manner with increasing doses of antibiotic from 0.5 to 3.0 g. Mean concentrations of cefodizime in plasma at the end of infusion increased from 97 to 440 mg liter-1 over the dose range 0.5 to 3.0 g and displayed a slight deviation from linearity at doses in excess of 2.0 g. Total plasma clearance (3.11 liters h-1), volume of distribution at steady state (10.5 liters), terminal elimination half-life (3.3 h), and renal clearance (1.91 liters h-1) remained constant over the doses administered. Cefodizime was well tolerated in this study.
头孢地嗪是一种新型的注射用广谱头孢菌素，具有抗菌谱广、抗菌活性强且对大多数β-内酰胺酶稳定的特点。本研究的目的是评估健康志愿者静脉注射剂量范围为0.5至3.0 g的头孢地嗪的药代动力学。通过高效液相色谱法测定血清和尿液中头孢地嗪的浓度。随着抗生素剂量从0.5 g增加到3.0 g，0小时至无穷大的浓度-时间曲线下面积以及0至34小时尿液中排出的药物量呈线性剂量依赖性增加。在0.5至3.0 g的剂量范围内，输注结束时血浆中头孢地嗪的平均浓度从97 mg/L升至440 mg/L，且在超过2.0 g的剂量时显示出与线性略有偏差。在所给予的剂量范围内，总血浆清除率（3.11 L/h）、稳态分布容积（10.5 L）、终末消除半衰期（3.3 h）和肾清除率（1.91 L/h）保持恒定。在本研究中，头孢地嗪耐受性良好。
