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头孢甘氨酸及其生物活性代谢物去乙酰头孢甘氨酸。

Cephaloglycin and its biologically active metabolite desacetylcephaloglycin.

作者信息

Wick W E, Wright W E, Kuder H V

出版信息

Appl Microbiol. 1971 Mar;21(3):426-34. doi: 10.1128/am.21.3.426-434.1971.

DOI:10.1128/am.21.3.426-434.1971
PMID:4994901
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC377197/
Abstract

Chromatographic studies and microbiological assays show that, after oral administration, cephaloglycin is partially converted in man to a biologically active metabolite desacetylcephaloglycin. The antibacterial activity of this metabolite compared to that of cephaloglycin is equivalent against gram-positive organisms but is lower against gram-negative bacilli. Successful therapy of urinary tract infections with cephaloglycin must be mainly attributed to the antibacterial activity of this metabolite. At the present time, it is not possible to assess what influence low amounts of unaltered cephaloglycin have on the outcome of therapy.

摘要

色谱研究和微生物测定表明,口服后,头孢甘氨酸在人体内部分转化为具有生物活性的代谢产物去乙酰头孢甘氨酸。与头孢甘氨酸相比,这种代谢产物对革兰氏阳性菌的抗菌活性相当,但对革兰氏阴性杆菌的抗菌活性较低。头孢甘氨酸成功治疗尿路感染主要归因于这种代谢产物的抗菌活性。目前,尚无法评估少量未改变的头孢甘氨酸对治疗结果有何影响。

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1
Cephaloglycin and its biologically active metabolite desacetylcephaloglycin.头孢甘氨酸及其生物活性代谢物去乙酰头孢甘氨酸。
Appl Microbiol. 1971 Mar;21(3):426-34. doi: 10.1128/am.21.3.426-434.1971.
2
Problems in the bio-assay of orally administered cephaloglycin in biological fluids and method for the detection of its metabolite, desacetylcephaloglycin.生物流体中口服头孢甘氨酸生物测定的问题及其代谢物去乙酰头孢甘氨酸的检测方法。
J Antibiot (Tokyo). 1970 Apr;23(4):216-22. doi: 10.7164/antibiotics.23.216.
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In vitro antimicrobial activity and human pharmacology of cephaloglycin.头孢甘氨酸的体外抗菌活性及人体药理学
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Cephaloglycin. Clinical and laboratory experience with an orally administered cephalosporin.头孢甘氨酸。口服头孢菌素的临床及实验室经验。
JAMA. 1968 Dec 16;206(12):2698-702. doi: 10.1001/jama.206.12.2698.
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Method for the detection and quantitative assay of cephaloglycin and its biologically active metabolites.头孢甘氨酸及其生物活性代谢物的检测和定量测定方法。
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Antimicrob Agents Chemother. 1972 Feb;1(2):90-3. doi: 10.1128/AAC.1.2.90.
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Pharmacologically active drug metabolites: therapeutic and toxic activities, plasma and urine data in man, accumulation in renal failure.药理活性药物代谢物:治疗及毒性活性、人体血浆及尿液数据、肾衰竭时的蓄积情况
Clin Pharmacokinet. 1976 Nov-Dec;1(6):426-43. doi: 10.2165/00003088-197601060-00003.

本文引用的文献

1
Pharmacological and toxicological studies on cephalotin.头孢噻吩的药理与毒理学研究
Clin Med (Northfield). 1963 Jun;70:1123-38.
2
IN VITRO AND IN VIVO LABORATORY EVALUATION OF CEPHALOGLYCIN AND CEPHALORIDINE.头孢甘氨酸和头孢噻啶的体外及体内实验室评估
Appl Microbiol. 1965 Mar;13(2):248-53. doi: 10.1128/am.13.2.248-253.1965.
3
In vitro and in vivo laboratory evaluation of cephalothin, a new broad spectrum antibiotic.新型广谱抗生素头孢噻吩的体外和体内实验室评估
J Bacteriol. 1962 Dec;84(6):1292-6. doi: 10.1128/jb.84.6.1292-1296.1962.
4
Guide to antibiotic therapy of experimental bacterial infections in mice.小鼠实验性细菌感染的抗生素治疗指南。
J Bacteriol. 1961 Feb;81(2):233-5. doi: 10.1128/jb.81.2.233-235.1961.
5
Factors influencing in vitro susceptibility to the cephalosporins and clinical trial of an oral cephalosporin, cephaloglycin.影响头孢菌素体外敏感性的因素及口服头孢菌素头孢甘氨酸的临床试验
Antimicrob Agents Chemother (Bethesda). 1966;6:82-7.
6
In vitro and in vivo laboratory comparison of cephalothin and desacetylcephalothin.头孢噻吩与去乙酰头孢噻吩的体外和体内实验室比较
Antimicrob Agents Chemother (Bethesda). 1965;5:870-5.
7
Delineation of the differences of various bacterial susceptibility tests with cephalexin.头孢氨苄对各种细菌药敏试验差异的描述。
Antimicrob Agents Chemother (Bethesda). 1968;8:435-41.
8
Chemistry of cephalosporin antibiotics. XI. Preparation and properties of desacetylcephaloglycin and its lactone.头孢菌素抗生素的化学。十一。去乙酰头孢甘氨酸及其内酯的制备与性质
J Med Chem. 1968 Sep;11(5):1067-9. doi: 10.1021/jm00311a035.
9
Method for the detection and quantitative assay of cephaloglycin and its biologically active metabolites.头孢甘氨酸及其生物活性代谢物的检测和定量测定方法。
Appl Microbiol. 1968 Aug;16(8):1132-3. doi: 10.1128/am.16.8.1132-1133.1968.
10
Clinical experience with cephaloglycin.头孢甘氨酸的临床经验。
Antimicrob Agents Chemother (Bethesda). 1967;7:624-9.