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慢性肾衰竭患者持续非卧床腹膜透析时头孢地尼的药代动力学及其向透析液中的转移

Pharmacokinetics of cefdinir and its transfer to dialysate in patients with chronic renal failure undergoing continuous ambulatory peritoneal dialysis.

作者信息

Tomino Y, Fukui M, Hamada C, Inoue S, Osada S

机构信息

Department of Medicine, Juntendo University School of Medicine, Tokyo, Japan.

出版信息

Arzneimittelforschung. 1998 Aug;48(8):862-7.

PMID:9748717
Abstract

Cefdinir (CAS 91832-40-5) was administered orally as a 100-mg capsule (Cefzon) to a total of 12 patients with chronic renal failure undergoing continuous ambulatory peritoneal dialysis (CAPD) to investigate changes in the serum concentrations, excretion rate into the dialysate and serum-protein binding of cefdinir. Cmax values were 1.64-4.34 micrograms/ml, t1/2 values were 10.8-21.9 h., and AUC values were 31.1-73.1 micrograms.h/ml (0-30 h) in four patients given a single oral dose of 100 mg of cefdinir as a capsule. About 1 microgram/ml of cefdinir had still remained in the blood of all the patients 24 h after administration. The serum concentrations of cefdinir were dose-dependent in four patients of each group who were given an oral daily dose of 100 mg for 3 to 8 days and 200 mg (2 capsules) for 4 to 14 consecutive days. No marked change in laboratory test values or clinical symptoms before and after administration were observed in these dose regimes. Protein levels of 5.17-5.71 g/day were eliminated from the peritoneal dialysate and urine. Cefdinir inhibited 90 to 100% of the clinical isolates such as Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and other enteric bacteria causing catheter infection and peritonitis, and its antibacterial activity was stronger than that of amoxicillin (CAS 26787-78-0) or cefaclor (CAS 53944-73-3) against these clinical isolates.

摘要

头孢地尼(化学物质登记号91832 - 40 - 5)以100毫克胶囊(头孢zon)的形式口服给药,共12例接受持续性非卧床腹膜透析(CAPD)的慢性肾衰竭患者,以研究头孢地尼的血清浓度变化、向透析液中的排泄率以及血清蛋白结合情况。4例单次口服100毫克胶囊头孢地尼的患者,其Cmax值为1.64 - 4.34微克/毫升,t1/2值为10.8 - 21.9小时,AUC值(0 - 30小时)为31.1 - 73.1微克·小时/毫升。给药24小时后,所有患者血液中仍残留约1微克/毫升的头孢地尼。每组各4例患者,分别口服每日剂量100毫克,持续3至8天,以及连续4至14天口服200毫克(2粒胶囊),头孢地尼的血清浓度呈剂量依赖性。在这些剂量方案下,给药前后实验室检查值或临床症状均未观察到明显变化。从腹膜透析液和尿液中清除的蛋白水平为5.17 - 5.71克/天。头孢地尼对金黄色葡萄球菌、表皮葡萄球菌、大肠杆菌和其他引起导管感染和腹膜炎的肠道细菌等临床分离株的抑制率为90%至100%,其抗菌活性强于阿莫西林(化学物质登记号26787 - 78 - 0)或头孢克洛(化学物质登记号53944 - 73 - 3)对这些临床分离株的抗菌活性。

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