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Absorption and Metabolism
After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime. Cefuroxime is subsequently distributed throughout the extracellular fluids. The axetil moiety is metabolized to acetaldehyde and acetic acid.
Approximately 50% of serum cefuroxime is bound to protein. Serum pharmacokinetic parameters for CEFTIN (cefuroxime axetil) Tablets and CEFTIN (cefuroxime axetil) for Oral Suspension are shown in Tables 1 and 2.
Table 1. Postprandial Pharmacokinetics of Cefuroxime Administered as CEFTIN (cefuroxime axetil) Tablets to Adults*
|Time of Peak
|*Mean values of 12 healthy adult volunteers. †Drug administered immediately after a meal.|
Table 2. Postprandial Pharmacokinetics of Cefuroxime Administered as CEFTIN (cefuroxime axetil) for Oral Suspension to Pediatric Patients*
|Time of Peak
| *Mean age = 23 months.
†Drug administered with milk or milk products.
Comparative Pharmacokinetic Properties
A 250 mg/5 mL-dose of CEFTIN (cefuroxime axetil) Suspension is bioequivalent to 2 times 125 mg/5 mL-dose of CEFTIN (cefuroxime axetil) Suspension when administered with food (see Table 3). CEFTIN (cefuroxime axetil) for Oral Suspension was not bioequivalent to CEFTIN (cefuroxime axetil) Tablets when tested in healthy adults. The tablet and powder for oral suspension formulations are NOT substitutable on a milligram-per-milligram basis. The area under the curve for the suspension averaged 91% of that for the tablet, and the peak plasma concentration for the suspension averaged 71% of the peak plasma concentration of the tablets. Therefore, the safety and effectiveness of both the tablet and oral suspension formulations had to be established in separate clinical trials.
Table 3. Pharmacokinetics of Cefuroxime Administered as 250 mg/5 mL or 2 x 125 mg/5 mL CEFTIN (cefuroxime axetil) for Oral Suspension to Adults* With Food
|Time of Peak
|250 mg/5 mL||2.23||3||1.40||8.92|
|2 x 125 mg/5 mL||2.37||3||1.44||9.75|
|*Mean values of 18 healthy adult volunteers.|
Food Effect on Pharmacokinetics
Absorption of the tablet is greater when taken after food (absolute bioavailability of CEFTIN (cefuroxime axetil) Tablets increases from 37% to 52%). Despite this difference in absorption, the clinical and bacteriologic responses of patients were independent of food intake at the time of tablet administration in 2 studies where this was assessed.
All pharmacokinetic and clinical effectiveness and safety studies in pediatric patients using the suspension formulation were conducted in the fed state. No data are available on the absorption kinetics of the suspension formulation when administered to fasted pediatric patients.
Cefuroxime is excreted unchanged in the urine; in adults, approximately 50% of the administered dose is recovered in the urine within 12 hours. The pharmacokinetics of cefuroxime in the urine of pediatric patients have not been studied at this time. Until further data are available, the renal pharmacokinetic properties of cefuroxime axetil established in adults should not be extrapolated to pediatric patients.
Because cefuroxime is renally excreted, the serum half-life is prolonged in patients with reduced renal function. In a study of 20 elderly patients (mean age = 83.9 years) having a mean creatinine clearance of 34.9 mL/min, the mean serum elimination half-life was 3.5 hours. Despite the lower elimination of cefuroxime in geriatric patients, dosage adjustment based on age is not necessary (see PRECAUTIONS: Geriatric Use).
The in vivo bactericidal activity of cefuroxime axetil is due to cefuroxime's binding to essential target proteins and the resultant inhibition of cell-wall synthesis.
Cefuroxime has bactericidal activity against a wide range of common pathogens, including many beta-lactamase-producing strains. Cefuroxime is stable to many bacterial beta-lactamases, especially plasmid-mediated enzymes that are commonly found in enterobacteriaceae.
Cefuroxime has been demonstrated to be active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section (see INDICATIONS AND USAGE section).
Aerobic Gram-Positive Microorganisms
Staphylococcus aureus (including beta-lactamase-producing strains)
Aerobic Gram-Negative Microorganisms
Haemophilus influenzae (including beta-lactamase-producing strains)
Moraxella catarrhalis (including beta-lactamase-producing strains)
Neisseria gonorrhoeae (including beta-lactamase-producing strains)
Cefuroxime has been shown to be active in vitro against most strains of the following microorganisms; however, the clinical significance of these findings is unknown.
Cefuroxime exhibits in vitro minimum inhibitory concentrations (MICs) of 4.0 mcg/mL or less (systemic susceptible breakpoint) against most (≥ 90%) strains of the following microorganisms; however, the safety and effectiveness of cefuroxime in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled trials.
Aerobic Gram-Positive Microorganisms
NOTE: Listeria monocytogenes and certain strains of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to cefuroxime. Methicillin-resistant staphylococci are resistant to cefuroxime.
Aerobic Gram-Negative Microorganisms
NOTE: Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Legionella spp., and most strains of Serratia spp. and Proteus vulgaris are resistant to most first- and second-generation cephalosporins. Some strains of Morganella morganii, Enterobacter cloacae, and Citrobacter spp. have been shown by in vitro tests to be resistant to cefuroxime and other cephalosporins.
NOTE: Most strains of Clostridium difficile and Bacteroides fragilis are resistant to cefuroxime.
Quantitative methods that are used to determine MICs provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. One such standardized procedure uses a standardized dilution method1 (broth, agar, or microdilution) or equivalent with cefuroxime powder. The MIC values obtained should be interpreted according to the following criteria:
|≤ 4||(S) Susceptible|
|≥ 32||(R) Resistant|
A report of “Susceptible” indicates that the pathogen, if in the blood, is likely to be inhibited by usually achievable concentrations of the antimicrobial compound in blood. A report of “Intermediate” indicates that inhibitory concentrations of the antibiotic may be achieved if high dosage is used or if the infection is confined to tissues or fluids in which high antibiotic concentrations are attained. This category also provides a buffer zone that prevents small, uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that usually achievable concentrations of the antimicrobial compound in the blood are unlikely to be inhibitory and that other therapy should be selected.
Standardized susceptibility test procedures require the use of laboratory control microorganisms. Standard cefuroxime powder should give the following MIC values:
|Escherichia coli ATCC 25922||2-8|
|Staphylococcus aureus ATCC 29213||0.5-2|
Quantitative methods that require measurement of zone diameters provide estimates of the susceptibility of bacteria to antimicrobial compounds. One such standardized procedure2 that has been recommended (for use with disks) to test the susceptibility of microorganisms to cefuroxime uses the 30-mcg cefuroxime disk. Interpretation involves correlation of the diameter obtained in the disk test with the MIC for cefuroxime.
Reports from the laboratory providing results of the standard single-disk susceptibility test with a 30-mcg cefuroxime disk should be interpreted according to the following criteria:
|Zone Diameter (mm)||Interpretation|
|≥ 23||(S) Susceptible|
|≤ 14||(R) Resistant|
Interpretation should be as stated above for results using dilution techniques.
As with standard dilution techniques, diffusion methods require the use of laboratory control microorganisms. The 30-mcg cefuroxime disk provides the following zone diameters in these laboratory test quality control strains:
|Microorganism||Zone Diameter (mm)|
|Escherichia coli ATCC 25922||20-26|
|Staphylococcus aureus ATCC 25923||27-35|
Ceftin (cefuroxime axetil) Tablets
Acute Bacterial Maxillary Sinusitis: One adequate and well-controlled study was performed in patients with acute bacterial maxillary sinusitis. In this study each patient had a maxillary sinus aspirate collected by sinus puncture before treatment was initiated for presumptive acute bacterial sinusitis. All patients had to have radiographic and clinical evidence of acute maxillary sinusitis. As shown in the following summary of the study, the general clinical effectiveness of CEFTIN (cefuroxime axetil) Tablets was comparable to an oral antimicrobial agent that contained a specific beta-lactamase inhibitor in treating acute maxillary sinusitis. However, sufficient microbiology data were obtained to demonstrate the effectiveness of CEFTIN (cefuroxime axetil) Tablets in treating acute bacterial maxillary sinusitis due only to Streptococcus pneumoniae or non-beta-lactamase-producing Haemophilus influenzae. An insufficient number of beta-lactamase-producing Haemophilus influenzae and Moraxella catarrhalis isolates were obtained in this trial to adequately evaluate the effectiveness of CEFTIN (cefuroxime axetil) Tablets in the treatment of acute bacterial maxillary sinusitis due to these 2 organisms.
This study enrolled 317 adult patients, 132 patients in the United States and 185 patients in South America. Patients were randomized in a 1:1 ratio to cefuroxime axetil 250 mg twice daily or an oral antimicrobial agent that contained a specific beta-lactamase inhibitor. An intent-to-treat analysis of the submitted clinical data yielded the following results:
Table 10. Clinical Effectiveness of CEFTIN (cefuroxime axetil) Tablets Compared
Inhibitor-Containing Control Drug in the Treatment of Acute Bacterial Maxillary Sinusitis
|US Patients*||South American Patients†|
(n = 49)
(n = 43)
(n = 87)
(n = 89)
|Clinical success (cure + improvement)||65%||53%||77%||74%|
| *95% Confidence interval around the success difference
†95% Confidence interval around the success difference [-0.10, +0.16].
In this trial and in a supporting maxillary puncture trial, 15 evaluable patients had non-beta-lactamase-producing Haemophilus influenzae as the identified pathogen. Ten (10) of these 15 patients (67%) had their pathogen (non-beta-lactamase-producing Haemophilus influenzae) eradicated. Eighteen (18) evaluable patients had Streptococcus pneumoniae as the identified pathogen. Fifteen (15) of these 18 patients (83%) had their pathogen (Streptococcus pneumoniae) eradicated.
Safety: The incidence of drug-related gastrointestinal adverse events was statistically significantly higher in the control arm (an oral antimicrobial agent that contained a specific beta-lactamase inhibitor) versus the cefuroxime axetil arm (12% versus 1%, respectively; P< .001), particularly drug-related diarrhea (8% versus 1%, respectively; P = .001).
Early Lyme Disease: Two adequate and well-controlled studies were performed in patients with early Lyme disease. In these studies all patients had to present with physician-documented erythema migrans, with or without systemic manifestations of infection. Patients were randomized in a 1:1 ratio to a 20-day course of treatment with cefuroxime axetil 500 mg twice daily or doxycycline 100 mg 3 times daily. Patients were assessed at 1 month posttreatment for success in treating early Lyme disease (Part I) and at 1 year posttreatment for success in preventing the progression to the sequelae of late Lyme disease (Part II).
A total of 355 adult patients (181 treated with cefuroxime axetil and 174 treated with doxycycline) were enrolled in the 2 studies. In order to objectively validate the clinical diagnosis of early Lyme disease in these patients, 2 approaches were used: 1) blinded expert reading of photographs, when available, of the pretreatment erythema migrans skin lesion; and 2) serologic confirmation (using enzyme-linked immunosorbent assay [ELISA] and immunoblot assay ["Western" blot]) of the presence of antibodies specific to Borrelia burgdorferi, the etiologic agent of Lyme disease. By these procedures, it was possible to confirm the physician diagnosis of early Lyme disease in 281 (79%) of the 355 study patients. The efficacy data summarized below are specific to this "validated" patient subset, while the safety data summarized below reflect the entire patient population for the 2 studies.
Analysis of the submitted clinical data for evaluable patients in the "validated" patient subset yielded the following results:
Table 11. Clinical Effectiveness of CEFTIN (cefuroxime axetil) Tablets Compared to Doxycycline in the Treatment of Early Lyme Disease
(1 MonthPost treatment)*
(1 YearPost treatment)†
(n = 125)
(n = 108)
|CEFTIN (cefuroxime axetil)
(n = 105‡)
(n = 83‡)
|Satisfactory clinical outcome§||91%||93%||84%||87%|
| *95% confidence interval around the satisfactory difference
for Part I (-0.08, +0.05).
†95% confidence interval around the satisfactory difference for Part II (-0.13, +0.07).
‡n's include patients assessed as unsatisfactory clinical outcomes (failure + recurrence) in Part I (CEFTIN (cefuroxime axetil) - 11 [5 failure, 6 recurrence]; doxycycline - 8 [6 failure, 2 recurrence]).
§ Satisfactory clinical outcome includes cure + improvement (Part I) and success + improvement (Part II).
CEFTIN (cefuroxime axetil) and doxycycline were effective in prevention of the development of sequelae of late Lyme disease.
Safety: Drug-related adverse events affecting the skin were reported significantly more frequently by patients treated with doxycycline than by patients treated with cefuroxime axetil (12% versus 3%, respectively; P = .002), primarily reflecting the statistically significantly higher incidence of drug-related photosensitivity reactions in the doxycycline arm versus the cefuroxime axetil arm (9% versus 0%, respectively; P< .001). While the incidence of drug-related gastrointestinal adverse events was similar in the 2 treatment groups (cefuroxime axetil - 13%; doxycycline - 11%), the incidence of drug-related diarrhea was statistically significantly higher in the cefuroxime axetil arm versus the doxycycline arm (11% versus 3%, respectively; P = .005).
Secondary Bacterial Infections of Acute Bronchitis: Four randomized, controlled clinical studies were performed comparing 5 days versus 10 days of CEFTIN (cefuroxime axetil) for the treatment of patients with secondary bacterial infections of acute bronchitis. These studies enrolled a total of 1,253 patients (CAE-516 n = 360; CAE-517 n = 177; CAEA4001 n = 362; CAEA4002 n = 354). The protocols for CAE-516 and CAE-517 were identical and compared CEFTIN (cefuroxime axetil) 250 mg twice daily for 5 days, CEFTIN (cefuroxime axetil) 250 mg twice daily for 10 days, and AUGMENTIN® 500 mg 3 times daily for 10 days. These 2 studies were conducted simultaneously. CAEA4001 and CAEA4002 compared CEFTIN (cefuroxime axetil) 250 mg twice daily for 5 days, CEFTIN (cefuroxime axetil) 250 mg twice daily for 10 days, and CECLOR® 250 mg 3 times daily for 10 days. They were otherwise identical to CAE-516 and CAE-517 and were conducted over the following 2 years. Patients were required to have polymorphonuclear cells present on the Gram stain of their screening sputum specimen, but isolation of a bacterial pathogen from the sputum culture was not required for inclusion. The following table demonstrates the results of the clinical outcome analysis of the pooled studies CAE-516/CAE-517 and CAEA4001/CAEA4002, respectively:
Table 12. Clinical Effectiveness of CEFTIN (cefuroxime axetil) Tablets 250 mg Twice Daily in Secondary Bacterial Infections of Acute Bronchitis: Comparison of 5 Versus 10 Days' Treatment Duration
|CAE-516 and CAE-517*||CAEA4001 and CAEA4002†|
(n = 127)
(n = 139)
(n = 173)
(n = 192)
|Clinical success (cure + improvement)||80%||87%||84%||82%|
| *95% Confidence interval around the success difference
†95% Confidence interval around the success difference [-0.061, +0.103].
The response rates for patients who were both clinically and bacteriologically evaluable were consistent with those reported for the clinically evaluable patients.
Safety: In these clinical trials, 399 patients were treated with CEFTIN (cefuroxime axetil) for 5 days and 402 patients with CEFTIN (cefuroxime axetil) for 10 days. No difference in the occurrence of adverse events was observed between the 2 regimens.
1.National Committee for Clinical Laboratory Standards. Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically. 3rd ed. Approved Standard NCCLS Document M7-A3, Vol. 13, No. 25. Villanova, Pa: NCCLS; 1993.
2.National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Disk Susceptibility Tests. 4th ed. Approved Standard NCCLS Document M2-A4, Vol. 10, No. 7. Villanova, Pa: NCCLS; 1990.
Last reviewed on RxList: 10/4/2010
This monograph has been modified to include the generic and brand name in many instances.
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