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头孢诺酮:正常人志愿者的体外抗菌活性及药理学研究

Cephanone: in vitro antibacterial activity and pharmacology in normal human volunteers.

作者信息

Meyers B R, Hirschman S Z, Nicholas P

出版信息

Antimicrob Agents Chemother. 1972 Oct;2(4):250-4. doi: 10.1128/AAC.2.4.250.

Abstract

Cephanone, a new 3-heterocyclic-thiomethyl cephalosporin antibiotic, was found to have an antibacterial spectrum similar to that of cephalothin. The compound was active in vitro against a variety of gram-positive and gram-negative bacteria. All strains of Staphylococcus aureus tested were inhibited by concentrations of 6.2 mug or less of cephanone per ml. Beta-hemolytic group A streptococci and pneumococci were exquisitely sensitive. Among strains of Escherichia coli and Klebsiella sp., 83 and 82%, respectively, were inhibited by 3.1 mug or less of cephanone per ml. Excellent serum concentrations of the antibiotic were obtained after parenteral administration. Peak concentrations of 38 and 81.2 mug/ml were achieved in the serum after intramuscular and intravenous doses of 1 g of cephanone, respectively. The serum concentrations of cephanone fell gradually during the 12 hr after administration. Very high concentrations of cephanone were found in the urine.

摘要

头孢诺酮是一种新型的3-杂环硫甲基头孢菌素抗生素,其抗菌谱与头孢噻吩相似。该化合物在体外对多种革兰氏阳性菌和革兰氏阴性菌具有活性。所有测试的金黄色葡萄球菌菌株均被每毫升6.2微克或更低浓度的头孢诺酮抑制。A组β溶血性链球菌和肺炎球菌极为敏感。在大肠杆菌和克雷伯菌属菌株中,分别有83%和82%被每毫升3.1微克或更低浓度的头孢诺酮抑制。经肠胃外给药后,该抗生素可在血清中达到良好的浓度。肌肉注射和静脉注射1克头孢诺酮后,血清中的峰值浓度分别达到38微克/毫升和81.2微克/毫升。给药后12小时内,头孢诺酮的血清浓度逐渐下降。在尿液中发现了非常高浓度的头孢诺酮。

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