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头孢克洛在正常志愿者和肾衰竭患者中的体外活性及药代动力学

In vitro activity and pharmacokinetics of cefaclor in normal volunteers and patients with renal failure.

作者信息

Levison M E, Santoro J, Agarwal B N

出版信息

Postgrad Med J. 1979;55 Suppl 4:12-6.

PMID:548939
Abstract

In both Mueller-Hinton agar (MHA) and antibiotic medium no. 1 (AB1) cefaclor was more active than cephalothin or cephalexin against Enterobacteriaceae. Its activity was equivalent to cephalexin against S. aureus in MHA. Cefaclor was particularly active against P. mirabilis. The activity of this antibiotic was greated in AB1 than in MHA. The inoculum effect was pronounced for cefaclor when compared with cephalothin, but cefaclor retained greater activity even against the higher inoculum. In volunteers with normal renal function, cefaclor produced slightly lower blood levels than those reported for cephalexin. Absorption after eating was decreased and delayed. Despite severe renal failure, substantial urine levels of antibiotic were still achieved. In contrast to cephalexin, plasma half-life for cefaclor was only moderately prolonged by renal failure (two-to-threefold) and only minimally shortened by haemodialysis. Adequate concentrations of cefaclor in sputum, active against common respiratory pathogens, could not be consistently demonstrated after the oral administration of a 1 gram dose of cefaclor.

摘要

在穆勒-欣顿琼脂(MHA)和1号抗生素培养基(AB1)中,头孢克洛对肠杆菌科细菌的活性均强于头孢噻吩或头孢氨苄。在MHA中,其对金黄色葡萄球菌的活性与头孢氨苄相当。头孢克洛对奇异变形杆菌特别有效。该抗生素在AB1中的活性高于MHA。与头孢噻吩相比,头孢克洛的接种物效应明显,但即使针对较高接种量,头孢克洛仍保持较高活性。在肾功能正常的志愿者中,头孢克洛产生的血药浓度略低于头孢氨苄报道的浓度。进食后吸收减少且延迟。尽管存在严重肾衰竭,但仍可达到相当高的尿液抗生素水平。与头孢氨苄不同,肾衰竭仅使头孢克洛的血浆半衰期适度延长(两到三倍),血液透析仅使其略微缩短。口服1克剂量的头孢克洛后,痰液中无法持续显示出对常见呼吸道病原体有效的足够浓度的头孢克洛。

相似文献

1
In vitro activity and pharmacokinetics of cefaclor in normal volunteers and patients with renal failure.头孢克洛在正常志愿者和肾衰竭患者中的体外活性及药代动力学
Postgrad Med J. 1979;55 Suppl 4:12-6.
2
Serum and sputum levels of cefaclor.
Postgrad Med J. 1979;55 Suppl 4:30-4.
3
Evaluation of cefaclor.头孢克洛的评估。
Am J Hosp Pharm. 1981 Jan;38(1):54-8.
4
Summary of laboratory studies on the antibacterial activity of cefaclor.头孢克洛抗菌活性的实验室研究总结。
Postgrad Med J. 1979;55 Suppl 4:22-9.
5
Comparative in vitro microbiological activity and stability of cefaclor.
Postgrad Med J. 1979;55 Suppl 4:9-11.
6
Variable in vitro activity of cefaclor, cephalothin and cefadroxil against Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis.头孢克洛、头孢噻吩和头孢羟氨苄对大肠杆菌、肺炎克雷伯菌和奇异变形杆菌的体外活性存在差异。
Scand J Infect Dis. 1988;20(4):421-4. doi: 10.3109/00365548809032479.
7
[Pharmacokinetics of cefaclor in subjects with normal renal function and in uraemic patients (author's transl)].
Therapie. 1981 Sep-Oct;36(5):533-40.
8
Summary of laboratory studies on the antibacterial activity of cefaclor.
Infection. 1979;7 Suppl 6:557-61. doi: 10.1007/BF01659735.
9
Reliability of cefaclor, cefazolin, cefamandole, and cephalothin disks to predict susceptibility of Enterobacteriaceae, Staphylococcus species, and Haemophilus influenzae.头孢克洛、头孢唑林、头孢孟多和头孢噻吩药敏纸片预测肠杆菌科细菌、葡萄球菌属细菌及流感嗜血杆菌药敏的可靠性。
Am J Clin Pathol. 1985 Nov;84(5):643-8. doi: 10.1093/ajcp/84.5.643.
10
The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.
Int J Clin Pharmacol Biopharm. 1979 Sep;17(9):397-400.

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