Following IV doses of 750 mg and 1.5 g, serum concentrations were approximately 50 and 100 mcg/mL, respectively, at 15 minutes. Therapeutic serum concentrations of approximately 2 mcg/mL or more were maintained for 5.3 hours and 8 hours or more, respectively. There was no evidence of accumulation of cefuroxime (cefuroxime (cefuroxime injection) injection) in the serum following IV administration of 1.5 g doses every 8 hours to normal volunteers. The serum half-life after IV injection is approximately 80 minutes.

Approximately 89% of a dose of cefuroxime (cefuroxime (cefuroxime injection) injection) is excreted by the kidneys over an 8 hour period, resulting in high urinary concentrations.

Intravenous doses of 750 mg and 1.5 g produced urinary levels averaging 1,150 and 2,500 mcg/mL, respectively, during the first 8 hour period.

The concomitant oral administration of probenecid with cefuroxime (cefuroxime (cefuroxime injection) injection) slows tubular secretion, decreases renal clearance by approximately 40%, increases the peak serum level by approximately 30%, and increases the serum half-life by approximately 30%. Cefuroxime (cefuroxime (cefuroxime injection) injection) is detectable in therapeutic concentrations in pleural fluid, joint fluid, bile, sputum, bone, cerebrospinal fluid (in patients with meningitis), and aqueous humor.

Cefuroxime (cefuroxime (cefuroxime injection) injection) is detectable in therapeutic concentrations in cerebrospinal fluid (CSF) of adults and pediatric patients with meningitis. The following table shows the concentrations of cefuroxime (cefuroxime (cefuroxime injection) injection) achieved in cerebrospinal fluid during multiple dosing of patients with meningitis.

Table 1. Concentrations of Cefuroxime (cefuroxime (cefuroxime injection) injection) Achieved in Cerebrospinal Fluid During Multiple Dosing of Patients with Meningitis

Cefuroxime (cefuroxime (cefuroxime injection) injection) is approximately 50% bound to serum protein.

Microbiology: Cefuroxime (cefuroxime (cefuroxime injection) injection) has in vitro activity against a wide range of gram-positive and gram-negative organisms, and it is highly stable in the presence of beta-lactamases of certain gram-negative bacteria. The bactericidal action of cefuroxime (cefuroxime (cefuroxime injection) injection) results from inhibition of cell-wall synthesis.

Cefuroxime (cefuroxime (cefuroxime injection) injection) is usually active against the following organisms in vitro.

Aerobes, Gram-positive

Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus pneumoniae, and
Streptococcus pyogenes (and other streptococci)

NOTE: Most strains of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to cefuroxime (cefuroxime (cefuroxime injection) injection) . Methicillin-resistant staphylococci and Listeria monocytogenes are resistant to cefuroxime (cefuroxime (cefuroxime injection) injection) .

Aerobes, Gram-negative

Citrobacter spp.
Enterobacter spp.
Escherichia coli
Haemophilus influenzae (including ampicillin-resistant strains)
Haemophilus parainfluenzae
Klebsiella spp. (including Klebsiella pneumoniae)
Moraxella (Branhamella) catarrhalis (including ampicillin- and cephalothin-resistant strains)
Morganella morganii (formerly Proteus morganii)
Neisseria gonorrhoeae (including penicillinase- and non-penicillinase-producing strains)
Neisseria meningitidis
Proteus mirabilis
Providencia rettgeri (formerly Proteus rettgeri)
Salmonella spp., and Shigella spp.

NOTE: Some strains of Morganella morganii, Enterobacter cloacae, and Citrobacter spp. have been shown by in vitro tests to be resistant to cefuroxime (cefuroxime (cefuroxime injection) injection) and other cephalosporins. Pseudomonas and Campylobacter spp., Acinetobacter calcoaceticus, and most strains of Serratia spp. and Proteus vulgaris are resistant to most first- and second-generation cephalosporins.

Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp.), gram-positive bacilli (including Clostridium spp.), and gram-negative bacilli (including Bacteroides and Fusobacterium spp.).

NOTE: Clostridium difficile and most strains of Bacteroides fragilis are resistant to cefuroxime (cefuroxime (cefuroxime injection) injection) .

Susceptibility Tests

Diffusion Techniques

Quantitative methods that require measurement of zone diameters give an estimate of antibiotic susceptibility. One such standard procedure¹ that has been recommended for use with disks to test susceptibility of organisms to cefuroxime (cefuroxime injection) uses the 30 mcg cefuroxime (cefuroxime (cefuroxime injection) injection) disk. Interpretation involves the correlation of the diameters obtained in the disk test with the minimum inhibitory concentration (MIC) for cefuroxime (cefuroxime (cefuroxime injection) injection) .

A report of &lequo;Susceptible” indicates that the pathogen is likely to be inhibited by generally achievable blood levels. A report of “Moderately Susceptible” suggests that the organism would be susceptible if high dosage is used or if the infection is confined to tissues and fluids in which high antibiotic levels are attained. A report of “ Intermediate” suggests an equivocable or indeterminate result. A report of “ Resistant” indicates that achievable concentrations of the antibiotic are unlikely to be inhibitory and other therapy should be selected.

Reports from the laboratory giving results of the standard single-disk susceptibility test for organisms other than Haemophilus spp. and Neisseria gonorrhoeae with a 30 mcg cefuroxime (cefuroxime (cefuroxime injection) injection) disk should be interpreted according to the following criteria:

Results for Haemophilus spp. should be interpreted according to the following criteria:

Results for Neisseria gonorrhoeae should be interpreted according to the following criteria:

Organisms should be tested with the cefuroxime (cefuroxime injection) disk since cefuroxime (cefuroxime (cefuroxime injection) injection) has been shown by in vitro tests to be active against certain strains found resistant when other beta-lactam disks are used. The cefuroxime (cefuroxime (cefuroxime injection) injection) disk should not be used for testing susceptibility to other cephalosporins.

Standardized procedures require the use of laboratory control organisms. The 30 mcg cefuroxime (cefuroxime (cefuroxime injection) injection) disk should give the following zone diameters.

1.Testing for organisms other than Haemophilus spp. and Neisseria gonorrhoeae:

2. Testing for Haemophilus spp.:

3. Testing for Neisseria gonorrhoeae:

Dilution Techniques

Use a standardized dilution method¹ (broth, agar, microdilution) or equivalent with cefuroxime (cefuroxime (cefuroxime injection) injection) powder. The MIC values obtained for bacterial isolates other than Haemophilus spp. and Neisseria gonorrhoeae should be interpreted according to the following criteria:

MIC values obtained for Haemophilus spp. should be interpreted according to the following criteria:

MIC values obtained for Neisseria gonorrhoeae should be interpreted according to the following criteria:

As with standard diffusion techniques, dilution methods require the use of laboratory control organisms. Standard cefuroxime (cefuroxime (cefuroxime injection) injection) powder should provide the following MIC values.

1. For organisms other than Haemophilus spp. and Neisseria gonorrhoeae:

2. For Haemophilus spp.:

3. For Neisseria gonorrhoeae:

REFERENCES

1. National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Susceptibility Testing. Third Informational Supplement. NCCLS Document M100-S3, Vol. 11, No. 17, Villanova, PA: NCCLS; 1991.

Last reviewed on RxList: 4/10/2008
This monograph has been modified to include the generic and brand name in many instances.