Cefuroxime (Ceftin®)

Based on "Antibiotic and Chemotherapy"
written by Roger G. Finch

History

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, 1981.

FDA approved uses

• Pharyngitis/Tonsillitis
• Otitis media (middle ear infection)
• Sinusitis (sinus infection)
• Acute/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.
• Gonorrhea
• 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 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 acute bronchitis.

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.

Gonorrhea
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.

Spectrum of activity

• Aerobic Gram-Positive Microorganisms: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes. Less active against Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae
• Aerobic Gram-Negative Microorganisms: E. coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrhoeae. Less active against Morganella morganii, Proteus inconstans, Proteus mirabilis, Providencia rettgeri.
• Spirochetes: Borrelia burgdorferi

Poor activity against most strains of:

• Enterobacter
• Citrobacter
• Serratia

Resistance

The following organisms are resistant to cefuroxime:

• Clostridium difficile
• Pseudomonas spp.
• Campylobacter spp.
• Acinetobacter calcoaceticus
• Listeria monocytogenes
• Methicillin resistant strains of Staphylococcus aureus
• Methicillin resistant strains of Staphylococcus epidermidis
• Legionella spp.

Cefuroxime "pros" and "cons"

Advantages:

• Broad-spectrum antibiotic. Cefuroxime is bactericidal against a wide range of common pathogens (disease-causing microbes), including many beta-lactamase-producing strains6.
  It has good stability to bacterial beta-lactamase, and consequently is active against many strains resistant to penicillins.
• Cefuroxime axetil is especially active against Haemophilus influenzae, including beta-lactamase-producing strains, and Moraxella catarrhalis.
• Less gastrointestinal side effects. Cefuroxime axetil produces fewer gastrointestinal side effects than some other widely used antibiotics (e.g. Augmentin8, cefixime7).
• 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. Cefuroxime has been recommended in the 2015 list of the US FDA list of drugs which can be used safely during pregnancy.
• Absorption is increased with food. Cefuroxime serum levels may be increased if it is 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 activity.
• The most active cephalosporin for beta-lactamase-producing Haemophilus influenzae (except for ceftriaxone), the 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 fluids.

Disadvantages:

• 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.

Further reading

• Cefuroxime (Ceftin) versus other medications
• Cefuroxime for Otitis Media
• Cefuroxime vs Amoxicillin
• Cefuroxime vs Ceftriaxone (Rocepin®)

References

• 1. CEFTIN (cefuroxime axetil) powder, for suspension CEFTIN (cefuroxime axetil) tablet, film coated Prescribing information
• 2. TA Tartaglione, RE Polk. Review of the new second-generation cephalosporins: cefonicid, ceforanide, and cefuroxime. The Annals Vol. 19, No. 3, pp. 188-198. PubMed
• 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. PubMed

Published: July 01, 2008
Last updated: October 27, 2017