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 mug 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 mug of cephaloglycin per ml. Klebsiella-Aerobacter species were more resistant to cephaloglycin and 12.5 mug 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 mug 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.

Bacteria↗

PubMed1968

Hemophilus influenzae pneumonia in adults. Report of five cases and review of the literature.

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Adult↗

PubMed1968

Antibacterial activity of human urine.

The fate of bacteria in human urine was studied after inoculation of small numbers of Escherichia coli and other bacterial strains commonly implicated in urinary tract infection. Urine from normal individuals was often inhibitory and sometimes bactericidal for growth of these organisms. Antibacterial activity of urine was not related to lack of nutrient material as addition of broth did not decrease inhibitory activity. Antibacterial activity was correlated with osmolality, urea concentration and ammonium concentration, but not with organic acid, sodium, or potassium concentration. Between a pH range of 5.0-6.5 antibacterial activity of urine was greater at lower pH. Ultrafiltration and column chromatography to remove protein did not decrease antibacterial activity. Urea concentration was a more important determinant of antibacterial activity than osmolality or ammonium concentration. Increasing the urea of a noninhibitory urine to equal that of an inhibitory urine made the urine inhibitory. However, increasing osmolality (with sodium chloride) or increasing ammonium to equal the osmolality or ammonium of an inhibitory urine did not increase antibacterial activity. Similarly, dialysis to decrease osmolality or ammonium but preserve urea did not decrease inhibitory activity. Decreasing urea with preservation of ammonium and osmolality decreased antibacterial activity. Removal of ammonium with an ion exchanger did not decrease antibacterial activity, whereas conversion of urea to ammonium with urease and subsequent removal of the ammonium decreased antibacterial activity. Urine collected from volunteers after ingestion of urea demonstrated a marked increase in antibacterial activity, as compared with urine collected before ingestion of urea.

Dialysis↗

PubMed1968