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In Vitro Antimicrobial Activity and Human Pharmacology of Cephaloglycin

机译:头霉素的体外抗菌活性和人体药理作用

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Serum and urine concentrations of cephaloglycin (an orally absorbed derivative of cephalosporin C) were determined in normal volunteers and in patients. The in vitro activity of cephaloglycin was also studied. All strains of group A streptococci (Streptococcus pyogenes) and Diplococcus pneumoniae were inhibited by 0.4 μg of cephaloglycin per ml. Eighty per cent of the Staphylococcus aureus strains and about 50% of the Escherichia coli and Proteus mirabilis strains were inhibited by 1.6 μg of cephaloglycin per ml. Klebsiella-Aerobacter species were more resistant to cephaloglycin and 12.5 μg per ml was required to inhibit 70% of these strains. When single doses of 250, 500, or 1,000 mg of cephaloglycin were administered to fasting volunteers, a peak serum concentration of at least 0.5 μg per ml was achieved. A full breakfast did not interfere with absorption of cephaloglycin. Probenecid enhanced both the peak serum concentration and the duration of antibiotic activity in the serum. Serum concentrations of cephaloglycin were even higher in patients who were receiving repeated doses. The peak serum concentrations of cephaloglycin in all volunteers and patients were adequate to inhibit all strains of group A streptococci and D. pneumoniae. Many of the peak serum concentrations were adequate to inhibit some strains of S. aureus, E. coli, and P. mirabilis. Urine levels of cephaloglycin were high enough in all volunteers and patients to inhibit more than 90% of the E. coli and P. mirabilis strains and over 70% of the strains of Klebsiella-Aerobacter.
机译:在正常志愿者和患者中测定了血清和尿液中的头孢菌素浓度(头孢菌素C的口服吸收衍生物)。还研究了头甘氨酸的体外活性。每毫升A组链球菌(化脓性链球菌)和肺炎双球菌的所有菌株均被0.4μg头孢菌素抑制。每毫升1.6μg头孢菌素抑制了80%的金黄色葡萄球菌菌株以及约50%的大肠杆菌和奇异变形杆菌菌株。克雷伯杆菌属土壤杆菌对头孢菌素的耐药性更高,需要每毫升12.5μg抑制70%的这些菌株。当向空腹志愿者服用250、500或1,000 mg的单剂量头孢菌素时,血清峰值浓度至少为0.5μg/ ml。一份丰盛的早餐没有干扰头糖的吸收。丙磺舒可提高血清峰值浓度和血清中抗生素活性的持续时间。接受重复剂量治疗的患者血清中的脑甘油糖浓度甚至更高。在所有志愿者和患者中,血清脑白蛋白的峰值浓度足以抑制所有A组链球菌和肺炎D.菌株。许多峰值血清浓度足以抑制某些金黄色葡萄球菌,大肠杆菌和奇异假单胞菌菌株。在所有志愿者和患者中,尿中的脑白蛋白水平都足够高,可以抑制90%以上的大肠杆菌和奇异毕赤酵母菌株以及70%以上的克雷伯菌-土壤杆菌菌株。

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