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对健康成年志愿者静脉单剂量(1.0克和2.0克)给药头孢地嗪的药代动力学。

Pharmacokinetics of cefodizime administered intravenously as a single-dose (1.0 and 2.0 g) to healthy adult volunteers.

作者信息

Bryskier A, Procyk T, Tremblay D, Lenfant B, Fourtillan J B

机构信息

Institut Roussel-Uclaf, Romainville, France.

出版信息

J Antimicrob Chemother. 1990 Nov;26 Suppl C:65-70. doi: 10.1093/jac/26.suppl_c.65.

DOI:10.1093/jac/26.suppl_c.65
PMID:2074253
Abstract

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.

摘要

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。

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引用本文的文献

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Pharmacokinetics of cefodizime following single doses of 0.5, 1.0, 2.0, and 3.0 grams administered intravenously to healthy volunteers.单次静脉注射0.5克、1.0克、2.0克和3.0克头孢地嗪后,健康志愿者体内的药代动力学情况。
Antimicrob Agents Chemother. 1995 Sep;39(9):2037-41. doi: 10.1128/AAC.39.9.2037.
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Clinical pharmacokinetics of antibiotics in patients with impaired renal function.肾功能受损患者抗生素的临床药代动力学
Clin Pharmacokinet. 1992 Mar;22(3):169-210. doi: 10.2165/00003088-199222030-00002.
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Cefodizime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.头孢地嗪:抗菌活性、药代动力学特性及治疗用途综述
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