Cefoperazone (sodium salt)

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Background

Cefoperazone is a new semisynthetic cephalosporin with a broad spectrum of antibacterial activity. Cefoperazone shows high activity against gram-positive bacteria and gram-negative bacilli, such as Escherichia coli, Klebsiella pneumoniae, and Proteus species [1].
In vitro: There was only a small spread between the minimum inhibitory concentrations and the minimum bactericidal concentrations of cefoperazone and a significant decrease in activity with an increase in inoculum size. Cefoperazone is relatively stable to hydrolysis to β-lactamases produced by gram-negative bacteria. Relative rates of hydrolysis of cefoperazone by cephalosporinases were 7.0 to 0.01[1]. In 50 strains of N. gonorrhoeae, the MIC50 of cefoperazone was ≤ 0.004-0.06 μg/ml [2].
In vivo: In four patients with cholelithiasis and one patient with carcinoma of the head of the pancreas, all of whom had normal renal functions, cefoperazone was intravenously administrated. In common duct bile, the maximum concentrations of cefoperazone ranged from 373.4 to 3,100 μg/ml while the concentrations ranged from 6.8 to 680 μg/ml in gall bladder bile. Cefoperazone concentrations of the gall bladder wall ranged from 16.8 to 48.0 μg/g [3].

[1] Matsubara N, Minami S, Muraoka T, et al. In vitro antibacterial activity of cefoperazone (T-1551), a new semisynthetic cephalosporin[J]. Antimicrobial agents and chemotherapy, 1979, 16(6): 731-735.
[2] Baker C N, Thornsberry C, Jones R N. In vitro antimicrobial activity of cefoperazone, cefotaxime, moxalactam (LY127935), azlocillin, mezlocillin, and other beta-lactam antibiotics against Neisseria gonorrhoeae and Haemophilus influenzae, including beta-lactamase-producing strains[J]. Antimicrobial agents and chemotherapy, 1980, 17(4): 757-761.
[3] Nakamura T, Hashimoto I, Sawada Y, et al. Cefoperazone concentrations in bile and gall bladder wall after intravenous administration[J]. Antimicrobial agents and chemotherapy, 1980, 18(6): 980-982.