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头孢霉素,一类新型β-内酰胺抗生素。IV. 体内研究。

Cephamycins, a new family of beta-lactam antibiotics. IV. In vivo studies.

作者信息

Miller A K, Celozzi E, Kong Y, Pelak B A, Kropp H, Stapley E O, Hendlin D

出版信息

Antimicrob Agents Chemother. 1972 Oct;2(4):287-90. doi: 10.1128/AAC.2.4.287.

Abstract

Cephamycin A was found to be more active in vivo than cephamycin B. In comparison with cephamycin C, cephamycin A was more active against gram-positive organisms but less active against gram-negative organisms. Given subcutaneously, cephamycin C had good in vivo gram-negative activity, comparing favorably with cephalothin and cephaloridine against cephalosporin-susceptible organisms. In general, against the gram-negative organisms, it was more active than cephalothin or cephalosporin C and about as active as cephaloridine. In addition, cephamycin C protected mice against beta-lactamase-producing Proteus cultures, including clinically isolated strains. The compound is remarkably nontoxic. Cephamycin C was detected in the serum and recovered from the urine of treated mice to about the same extent as cephaloridine. Like cephaloridine and cephalosporin C, cephamycin C must be excreted mainly by glomerular filtration, because the use of probenecid did not enhance the therapeutic effectiveness nor concentrations of these agents in the sera of treated mice.

摘要

已发现头孢西丁A在体内比头孢西丁B更具活性。与头孢西丁C相比,头孢西丁A对革兰氏阳性菌更具活性,但对革兰氏阴性菌活性较低。皮下给药时,头孢西丁C在体内对革兰氏阴性菌具有良好的活性,与头孢噻吩和头孢匹林相比,对头孢菌素敏感菌更具优势。一般来说,针对革兰氏阴性菌,它比头孢噻吩或头孢菌素C更具活性,与头孢匹林活性相当。此外,头孢西丁C可保护小鼠免受产β-内酰胺酶的变形杆菌培养物(包括临床分离菌株)的侵害。该化合物毒性极低。在治疗小鼠的血清中检测到了头孢西丁C,并且从尿液中回收的程度与头孢匹林大致相同。与头孢匹林和头孢菌素C一样,头孢西丁C必须主要通过肾小球滤过排泄,因为使用丙磺舒并未提高这些药物在治疗小鼠血清中的治疗效果和浓度。

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本文引用的文献

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Cephamycins, a new family of beta-lactam antibiotics. 3. In vitro studies.
Antimicrob Agents Chemother. 1972 Oct;2(4):281-6. doi: 10.1128/AAC.2.4.281.
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