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头孢替安和头孢唑林对小鼠奇异变形杆菌所致尿路感染的比较活性

Comparative activities of cefotiam and cefazolin against urinary tract infections with Proteus mirabilis in mice.

作者信息

Iwahi T, Tsuchiya K

出版信息

Antimicrob Agents Chemother. 1980 Aug;18(2):257-63. doi: 10.1128/AAC.18.2.257.

DOI:10.1128/AAC.18.2.257
PMID:7004338
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC283980/
Abstract

The therapeutic effect of cefotiam on experimental urinary tract infections with Proteus mirabilis IFO 3849 in mice was compared with that of cefazolin. The minimal inhibitory concentrations of cefotiam and cefazolin against the test organism were 1.56 and 25 micrograms/ml, respectively. Beginning 3 days after infection, various doses of each cephalosporin were given subcutaneously twice a day for 5 days. Doses of 100 mg of cefotiam per kg or more sterilized the urine within 3 days and effected a marked reduction or complete eradication of bacteria in the bladder walls and kidneys of mice sacrificed the day after treatment was terminated. A dose of cefazolin greater than 800 mg/kg was required for equivalent therapeutic results. Clearance of bacteria from urinary tract organs was as rapid or more rapid with 50-mg/kg doses of cefotiam as with 200-mg/kg doses of cefazolin. Much more rapid clearance was attained with 200-mg/kg doses of cefotiam. The concentrations of cefotiam attained in plasma, kidney, and urine were lower than the cefazolin levels achieved at an equivalent dose. The superiority of cefotiam over cefazolin in treatment of experimental urinary tract infections appears to be due to its greater activity against the test organism.

摘要

将头孢替安与头孢唑林对小鼠奇异变形杆菌IFO 3849所致实验性尿路感染的治疗效果进行了比较。头孢替安和头孢唑林对受试菌的最低抑菌浓度分别为1.56微克/毫升和25微克/毫升。感染后3天开始,每天两次皮下注射不同剂量的每种头孢菌素,持续5天。每千克100毫克或更高剂量的头孢替安在3天内使尿液无菌,并使在治疗结束后次日处死的小鼠膀胱壁和肾脏中的细菌显著减少或完全根除。需要大于800毫克/千克剂量的头孢唑林才能取得同等治疗效果。50毫克/千克剂量的头孢替安与200毫克/千克剂量的头孢唑林相比,尿路器官中细菌的清除速度相同或更快。200毫克/千克剂量的头孢替安清除速度更快。头孢替安在血浆、肾脏和尿液中达到的浓度低于同等剂量头孢唑林的水平。头孢替安在治疗实验性尿路感染方面优于头孢唑林,这似乎是由于其对受试菌的活性更高。

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Pharmacokinetics of cefotiam in normal humans.
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本文引用的文献

1
The effective concentrations of penicillin in vitro and in vivo for streptococci, pneumococci, and Treponema pallidum.青霉素在体外和体内对链球菌、肺炎球菌及梅毒螺旋体的有效浓度。
J Bacteriol. 1950 May;59(5):625-43. doi: 10.1128/jb.59.5.625-643.1950.
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Effect of schedule of administration on the therapeutic efficacy of penicillin; importance of the aggregate time penicillin remains at effectively bactericidal levels.给药方案对青霉素治疗效果的影响;青霉素维持有效杀菌水平的累计时间的重要性。
Am J Med. 1950 Sep;9(3):280-99. doi: 10.1016/0002-9343(50)90425-6.
3
"Continuous" vs. "discontinuous" therapy with penicillin; the effect of the interval between injections on therapeutic efficacy.青霉素的“连续”与“间断”疗法;注射间隔时间对治疗效果的影响。
N Engl J Med. 1953 Mar 19;248(12):481-8. doi: 10.1056/NEJM195303192481201.
4
Absorption, distribution and excretion of SCE-963, a new broad-spectrum cephalosporin, in mice, rats, rabbits and dogs.新型广谱头孢菌素SCE - 963在小鼠、大鼠、兔子和狗体内的吸收、分布及排泄情况。
J Antibiot (Tokyo). 1978 Dec;31(12):1272-82. doi: 10.7164/antibiotics.31.1272.
5
SCE-963, a new broad-spectrum cephalosporin: in vitro and in vivo antibacterial activities.SCE - 963,一种新型广谱头孢菌素:体外及体内抗菌活性
Antimicrob Agents Chemother. 1978 Oct;14(4):557-68. doi: 10.1128/AAC.14.4.557.
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Cefazolin and cephradine: relationship between antibacterial activity in vitro and in mice experimentally infected with Escherichia coli.
J Infect Dis. 1978 Apr;137(4):391-402. doi: 10.1093/infdis/137.4.391.
7
Experimental urinary tract infection with Pseudomonas aeruginosa in mice.小鼠铜绿假单胞菌实验性尿路感染
Infect Immun. 1978 Nov;22(2):508-15. doi: 10.1128/iai.22.2.508-515.1978.