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High serum and bile levels of CEFOBID (sterile cefoperazone) are attained after a single dose of the drug. Table 1 demonstrates the serum concentrations of CEFOBID (sterile cefoperazone) in normal volunteers following either a single 15-minute constant rate intravenous infusion of 1, 2, 3 or 4 grams of the drug, or a single intramuscular injection of 1 or 2 grams of the drug.
TABLE 1. Cefoperazone Serum Concentrations
|Mean Serum Concentrations (mcg/mL)|
|Dose/Route||0*||0.5 hr||1 hr||2 hr||4 hr||8 hr||12 hr|
|1 g IV||153||114||73||38||16||4||0.5|
|2 g IV||252||153||114||70||32||8||2|
|3 g IV||340||210||142||89||41||9||2|
|4 g IV||506||325||251||161||71||19||6|
|1 g IM||32**||52||65||57||33||7||1|
|2 g IM||40**||69||93||97||58||14||4|
|* Hours post-administration, with 0 time being the end of
** Values obtained 15 minutes post-injection.
The mean serum half-life of CEFOBID (sterile cefoperazone) is approximately 2.0 hours, independent of the route of administration.
In vitro studies with human serum indicate that the degree of CEFOBID (sterile cefoperazone) reversible protein binding varies with the serum concentration from 93% at 25 mcg/mL of CEFOBID (sterile cefoperazone) to 90% at 250 mcg/mL and 82% at 500 mcg/mL.
CEFOBID (sterile cefoperazone) achieves therapeutic concentrations in the following body tissues and fluids:
|Tissue or Fluid||Dose||Concentration|
|Ascitic Fluid||2 g||64 mcg/mL|
|Cerebrospinal Fluid (in patients with inflamed meninges)||50 mg/kg||1.8 mcg/mL to 8.0 mcg/mL|
|Urine||2 g||3,286 mcg/mL|
|Sputum||3 g||6.0 mcg/mL|
|Endometrium||2 g||74 mcg/g|
|Myometrium||2 g||54 mcg/g|
|Palatine Tonsil||1 g||8 mcg/g|
|Sinus Mucous Membrane||1 g||8 mcg/g|
|Umbilical Cord Blood||1 g||25 mcg/mL|
|Amniotic Fluid||1 g||4.8 mcg/mL|
|Lung||1 g||28 mcg/g|
|Bone||2 g||40 mcg/g|
CEFOBID (sterile cefoperazone) is excreted mainly in the bile. Maximum bile concentrations are generally obtained between one and three hours following drug administration and exceed concurrent serum concentrations by up to 100 times. Reported biliary concentrations of CEFOBID (sterile cefoperazone) range from 66 mcg/mL at 30 minutes to as high as 6000 mcg/mL at 3 hours after an intravenous bolus injection of 2 grams.
Following a single intramuscular or intravenous dose, the urinary recovery of CEFOBID (sterile cefoperazone) over a 12-hour period averages 20–30%. No significant quantity of metabolites has been found in the urine. Urinary concentrations greater than 2200 mcg/mL have been obtained following a 15-minute infusion of a 2 g dose. After an IM injection of 2 g, peak urine concentrations of almost 1000 mcg/mL have been obtained, and therapeutic levels are maintained for 12 hours.
Repeated administration of CEFOBID (sterile cefoperazone) at 12-hour intervals does not result in accumulation of the drug in normal subjects. Peak serum concentrations, areas under the curve (AUC's), and serum half-lives in patients with severe renal insufficiency are not significantly different from those in normal volunteers. In patients with hepatic dysfunction, the serum half-life is prolonged and urinary excretion is increased. In patients with combined renal and hepatic insufficiencies, CEFOBID (sterile cefoperazone) may accumulate in the serum.
CEFOBID (sterile cefoperazone) has been used in pediatrics, but the safety and effectiveness in children have not been established. The half-life of CEFOBID (sterile cefoperazone) in serum is 6–10 hours in low birth-weight neonates.
CEFOBID (sterile cefoperazone) is active in vitro against a wide range of aerobic and anaerobic, gram-positive and gram-negative pathogens. The bactericidal action of CEFOBID (sterile cefoperazone) results from the inhibition of bacterial cell wall synthesis. CEFOBID (sterile cefoperazone) has a high degree of stability in the presence of beta-lactamases produced by most gram-negative pathogens. CEFOBID (sterile cefoperazone) is usually active against organisms which are resistant to other beta-lactam antibiotics because of beta-lactamase production. CEFOBID (sterile cefoperazone) is usually active against the following organisms in vitro and in clinical infections:
- Staphylococcus aureus, penicillinase and non-penicillinase producing strains
- Staphylococcus epidermidis
- Streptococcus pneumoniae (formerly Diplococcus pneumoniae)
- Streptococcus pyogenes (Group A beta-hemolytic streptococci)
- Streptococcus agalactiae (Group B beta-hemolytic streptococci)
- Enterococcus (Streptococcus faecalis, S. faecium and S. durans)
- Escherichia coli
- Klebsiella species (including K. pneumoniae)
- Enterobacter species
- Citrobacter species
- Haemophilus influenzae
- Proteus mirabilis
- Proteus vulgaris
- Morganella morganii (formerly Proteus morganii)
- Providencia stuartii
- Providencia rettgeri (formerly Proteus rettgeri)
- Serratia marcescens
- Pseudomonas aeruginosa
- Pseudomonas species
- Some strains of Acinetobacter calcoaceticus
- Neisseria gonorrhoeae
- Gram-positive cocci (including Peptococcus and Peptostreptococcus)
- Clostridium species
- Bacteroides fragilis
- Other Bacteroides species
CEFOBID (sterile cefoperazone) is also active in vitro against a wide variety of other pathogens although the clinical significance is unknown. These organisms include: Salmonella and Shigella species, Serratia liquefaciens, N. meningitidis, Bordetella pertussis, Yersinia enterocolitica, Clostridium difficile, Fusobacterium species, Eubacterium species and beta-lactamase producing strains of H. influenzae and N. gonorrhoeae.
For the disk diffusion method of susceptibility testing, a 75 mcg CEFOBID (sterile cefoperazone) diffusion disk should be used. Organisms should be tested with the CEFOBID (sterile cefoperazone) 75 mcg disk since CEFOBID (sterile cefoperazone) has been shown in vitro to be active against organisms which are found to be resistant to other beta-lactam antibiotics.
Tests should be interpreted by the following criteria:
|Greater than or equal to 21 mm||Susceptible|
|16–20 mm||Moderately Susceptible|
|Less than or equal to 15 mm||Resistant|
Quantitative procedures that require measurement of zone diameters give the most precise estimate of susceptibility. One such method which has been recommended for use with the CEFOBID (sterile cefoperazone) 75 mcg disk is the NCCLS approved standard. (Performance Standards for
Antimicrobial Disk Susceptibility Tests. Second Information Supplement Vol. 2 No. 2 pp. 49– 69. Publisher–National Committee for Clinical Laboratory Standards, Villanova, Pennsylvania.)
A report of “susceptible” indicates that the infecting organism is likely to respond to CEFOBID (sterile cefoperazone) therapy and a report of “resistant” indicates that the infecting organism is not likely to respond to therapy. A “moderately susceptible” report suggests that the infecting organism will be susceptible to CEFOBID (sterile cefoperazone) if a higher than usual dosage is used or if the infection is confined to tissues and fluids (e.g., urine or bile) in which high antibiotic levels are attained.
Broth or agar dilution methods may be used to determine the minimal inhibitory concentration (MIC) of CEFOBID (sterile cefoperazone) . Serial twofold dilutions of CEFOBID (sterile cefoperazone) should be prepared in either broth or agar. Broth should be inoculated to contain 5 × 105 organisms/mL and agar “spotted” with 104 organisms.
MIC test results should be interpreted in light of serum, tissue, and body fluid concentrations of CEFOBID (sterile cefoperazone) . Organisms inhibited by CEFOBID (sterile cefoperazone) at 16 mcg/mL or less are considered susceptible, while organisms with MIC's of 17–63 mcg/mL are moderately susceptible. Organisms inhibited at CEFOBID (sterile cefoperazone) concentrations of greater than or equal to 64 mcg/mL are considered resistant, although clinical cures have been obtained in some patients infected by such organisms.
Last reviewed on RxList: 8/24/2009
This monograph has been modified to include the generic and brand name in many instances.
Additional Cefobid Information
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