Bryskier A, Procyk T, Tremblay D, Lenfant B, Fourtillan J B
Institut Roussel-Uclaf, Romainville, France.
J Antimicrob Chemother. 1990 Nov;26 Suppl C:65-70. doi: 10.1093/jac/26.suppl_c.65.
Cefodizime is a new third generation cephalosporin for parenteral use. The purpose of this study was to define the pharmacokinetic profile of cefodizime after intravenous dosing with 1.0 and 2.0 g in healthy adult volunteers. Concentrations in plasma were determined over a period of 34 h and in urine over 48 h, using high-pressure liquid chromatographic procedures. Cefodizime displays a long elimination half-life (3.5-3.7 h). Mean total clearance was 2.63 +/- 0.19 l/h and mean renal clearance was 1.37 +/- 0.15 l/h. Areas under the curve were 422 +/- 43 mg.h/l and 757 +/- 39 mg.h/l for 1.0 and 2.0 g respectively. The apparent volumes of distribution were 12.8 +/- 1.81 and 14.3 +/- 1.11. After 1.0 g administration the residual concentrations were 3.94 +/- 0.79 mg/l and 0.38 +/- 0.10 mg/l at 12 and 24 h, respectively; after 2.0 g administration the residual concentrations were 6.80 +/- 1.40 mg/l and 0.65 +/- 0.18 mg/l, at 12 h and 24 h. Cefodizime is mainly eliminated via the kidneys. This profile supports once-daily administration of cefodizime, when indicated in non-life-threatening infections.
头孢地嗪是一种新型的用于肠胃外给药的第三代头孢菌素。本研究的目的是确定健康成年志愿者静脉注射1.0克和2.0克头孢地嗪后的药代动力学特征。使用高压液相色谱法在34小时内测定血浆浓度,在48小时内测定尿液浓度。头孢地嗪显示出较长的消除半衰期(3.5 - 3.7小时)。平均总清除率为2.63±0.19升/小时,平均肾清除率为1.37±0.15升/小时。1.0克和2.0克剂量的曲线下面积分别为422±43毫克·小时/升和757±39毫克·小时/升。表观分布容积分别为12.8±1.81和14.3±1.11。给药1.0克后,12小时和24小时的残留浓度分别为3.94±0.79毫克/升和0.38±0.10毫克/升;给药2.0克后,12小时和24小时的残留浓度分别为6.80±1.40毫克/升和0.65±0.18毫克/升。头孢地嗪主要通过肾脏消除。该特征支持在非危及生命的感染中如有指征时每日一次给药头孢地嗪。