Cefuroxime in Brief
- Active ingredient: Cefuroxime Axetil
- Common brand names: Ceftin, Zinacef
- Drug class: Antibiotic, Cephalosporin, Second-generation
- FDA Approved: December 28, 1987
- Pregnancy Category: B
- Originally discovered: 1970s, Glaxo, UK
Cefuroxime is a second-generation cephalosporin antibiotic, developed
by Glaxo in the 1970s. Cefuroxime is the subject of U.S. Patent No.
3,974,153. Cefuroxime required intravenous or intramuscular injection
because of bioabsorption difficulties and was therefore of limited usefulness.
Glaxo then synthesized a family of cefuroxime esters that were suitable
for oral administration and obtained U.S. Patent No. 4,267,320, issued
May 12, 19811.
FDA approved uses
- Otitis media (middle ear infection)
- Sinusitis (sinus infection)
- Acute bronchitis, chronic bronchitis
- Uncomplicated skin and skin-structure infections - such as folliculitis,
impetigo, erysipelas, cellulitis, furuncles, carbuncles, and non-perirectal
abscesses. Most uncomplicated skin and skin-structure infections are
caused by Staphylococcus aureus and Streptococcus pyogenes.
- Uncomplicated urinary tract infections (UTI) - uncomplicated urinary
tract infection is a bladder infection (cystitis) or kidney infection
(pyelonephritis) that is not caused by a structural problem, obstruction
within the urinary tract (such as a kidney stone or an enlarged prostate),
or other medical condition that affects kidney and bladder function.
- Early Lyme Disease (erythema migrans) - a tick-borne spirochetal
disease. In the US, Lyme disease is caused by the spirochete Borrelia
burgdorferi, which is transmitted by the bite of Ioxodes scapularis
or I. pacificus ticks.
Cefuroxime for Otitis Media
Cefuroxime is not considered a first choice for initial treatment
of otitis media. It is recommended as an alternative to amoxicillin
or Augmentin when these drugs are ineffective or cannot be used (e.g., in persons with a history of hypersensitivity
reactions to penicillins).
Results of clinical studies in children 3 months to 12 years of age
with acute otitis media show that a 10-day regimen of cefuroxime axetil
is quite effective3. The overall symptoms improvement rate is 62–94%.
Cefuroxime axetil is used for the treatment of acute otitis media
caused by S. pneumoniae, S. pyogenes, H. influenzae, and M. catarrhalis, including beta-lactamase-producing strains.
Cefuroxime for Pharyngitis and Tonsillitis
A 10-day regimen of cefuroxime axetil is effective for the
treatment of streptococcal pharyngitis and tonsillitis.
In addition, results of a prospective, randomized study in children 2–15 years of age indicate that a 4-day regimen
of cefuroxime axetil is also sufficiently
effective4. The symptoms improvement rate was 94.8%;
the infection relapse rate was 2.8%.
Cefuroxime for Respiratory Tract Infections
Cefuroxime axetil is used orally for the treatment of mild to moderate
respiratory tract infections, including acute maxillary sinusitis and
acute exacerbations of chronic bronchitis and secondary infections of
Cefuroxime sodium is used parenterally for the treatment of lower respiratory
tract infections, including pneumonia, caused by susceptible S. pneumoniae,
Staphylococcus aureus (penicillinase- and nonpenicillinase-producing
strains), S. pyogenes (group A beta-hemolytic streptococci), H. influenzae
(including ampicillin-resistant strains), Escherichia coli, and Klebsiella.
Cefuroxime axetil is used orally for the treatment of uncomplicated
urethral and endocervical gonorrhea and for uncomplicated
rectal gonorrhea in women5. However, cefuroxime is not considered a preferred
treatment for gonococcal infections. Also, it appears ineffective against pharyngeal gonococcal infection.
Cefuroxime may be an acceptable therapy in geographical areas where quinolone-resistant gonorrhea is prevalent.
Early Lyme Disease
Cefuroxime axetil is used for the treatment of early Lyme disease manifested
as erythema migrans. The Infectious Diseases Society of America (IDSA),
American Academy of Pediatrics (AAP), and other clinicians recommend cefuroxime axetil as first-line
therapy for early Lyme disease associated with erythema migrans, in the absence of specific neurologic
involvement or advanced atrioventricular (AV) heart block.
Cefuroxime "pros" and "cons"
- Broad-spectrum antibiotic. Cefuroxime has bactericidal activity
against a wide range of common pathogens, including many beta-lactamase-producing
It has good stability to bacterial beta-lactamase, and consequently
is active against many
strains resistant to penicillins.
- Less gastrointestinal side effects. Cefuroxime axetil produces
fewer gastrointestinal side effects than some other widely used antibiotics
- Safe for use in children. Safety and effectiveness of cefuroxime
axetil have been established for children aged 3 months to 12 years.
- Pregnancy category B. There is no experimental evidence of
embryopathic or teratogenic effects associated with cefuroxime axetil.
- Absorption is increased with food. Cefuroxime serum levels
may be increased if taken with food or dairy products (from 37% to 52%).
- Ease of use - twice daily dosing.
- Available in oral and I.V. formulations. One of the major
advantages over other cephalosporins is that it is available
in I.V. and oral preparations. Therefore, doctors can change the route
of drug administration without altering the spectrum of antibacterial
- Most active cephalosporin for beta-lactamase-producing Haemophilus
influenzae, organism that causes respiratory tract infections
such as otitis media, bronchitis and sinusitis.
- Wide tissue distribution. Widely distributed in the body
into most tissues and fluids including gallbladder, liver, kidney,
bone, uterus, ovary, sputum, bile, and peritoneal, pleural, and synovial
- Clostridium difficile-associated colitis. Cefuroxime axetil
(like other antibiotics) is associated with a risk for Clostridium
difficile-associated diarrhea ranging from mild diarrhea to fatal
colitis. Some cases have been reported more than 2 months after the
end of antibiotic therapy.
- More expensive than penicillins.
Mode of action
Cefuroxime is a bactericidal antibiotic, which exerts antibacterial
activity by inhibition of bacterial cell wall synthesis in susceptible
species. Cefuroxime has good stability to several bacterial beta-lactamase
enzymes and, consequently, is active against many resistant
strains of susceptible species.
Time to clear out of the system
Cefuroxime half-life is 1.2 -1.3 h for tablets and 1.4-1.9 h for suspension.
- 1. United
States Court of Appeals for the Federal Circuit
- 2. TA Tartaglione, RE Polk. Review of the new
second-generation cephalosporins: cefonicid, ceforanide, and cefuroxime.
The Annals Vol. 19, No. 3,
- 3. Gooch WM 3rd, Blair E, Puopolo A, Paster Z, Schwartz RH, Miller HC, Smyre HL,
Giguere GC, Collins JJ. Cefuroxime axetil suspension in pediatric patients with acute otitis media with effusion.
Clin Ther. 1995 Sep-Oct;17(5):838-51.
- 4. Aujard Y, Boucot I, Brahimi N, Chiche D, Bingen E.
Pediatr Infect Dis J. 1995 Apr;14(4):295-300.
- 5. Reichman RC, Nolte FS, Wolinsky SM, Greisberger CA, Trupei MA, Nitzkin J. Single-dose cefuroxime axetil in the treatment of uncomplicated gonorrhea: a controlled trial. Sex Transm Dis. 1985 Oct-Dec;12(4):184-7.
- 6. Perry CM, Brogden RN. Cefuroxime axetil. A
review of its antibacterial activity, pharmacokinetic properties and
therapeutic efficacy. Drugs. 1996 Jul;52(1):125-58. PubMed
- 7. Arthur M, McAdoo M, Guerra J, Maloney R, McCluskey
D, Giguere G, Gomez G, Collins JJ. Clinical Comparison of Cefuroxime
Axetil with Cefixime in the Treatment of Acute Bronchitis. Am J Ther.
1996 Sep;3(9):622-629. PubMed
- 8. Pessey JJ, Gehanno P, Thoroddsen E, Dagan
R, Leibovitz E, Machac J, Pimentel JM, Marr C, Leblanc F. Pediatr Infect Dis J. 1999 Oct;18(10):854-9.
Published: July 01, 2008
Last updated: April 09, 2012
- Absorption of the Cefuroxime is greater when taken after
- Cefuroxime axetil suspension is not bioequivalent
to Cefuroxime axetil tablets. The tablet and powder for oral suspension
formulations are NOT substitutable on a milligram-per-milligram