eMedExpert Home > Medications Facts > Cefuroxime Axetil (Ceftin)

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.

• Pharyngitis/Tonsillitis (strep throat)
• 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.
• 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 Acute Otitis Media
Cefuroxime is not considered a drug of first choice for initial treatment of otitis media. It is recommended as an alternative to amoxicillin or amoxicillin/clavulanate potassium when these drugs are ineffective or cannot be used (e.g., in persons with a history 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 as effective or more effective than a 10-day regimen of cefaclor, amoxicillin, or amoxicillin/clavulanate potassium3. According to the studies, the overall symptoms improvement rate to a 10-day course of oral cefuroxime axetil in children with otitis media ranges from 62–94%.

Cefuroxime axetil is used for the treatment of acute otitis media caused by S. pneumoniae, H. influenzae (including beta-lactamase-producing strains), M. catarrhalis (including beta-lactamase-producing strains), or S. pyogenes.

Cefuroxime for Pharyngitis and Tonsillitis (Strep Throat)
Cefuroxime axetil is used for the treatment of pharyngitis and tonsillitis caused by S. pyogenes (group A beta-hemolytic streptococci).

A 10-day regimen of cefuroxime is at least as effective as a 10-day regimen of penicillin V for the treatment of streptococcal pharyngitis and tonsillitis4. In addition, results of a prospective, randomized study in children 2–15 years of age indicate that a 4-day regimen of cefuroxime axetil (20 mg/kg of cefuroxime in 2 divided doses daily) is as effective as a 10-day regimen of penicillin V (45 mg/kg daily in 3 divided doses). The symptoms improvement rate was 94.8% in those who received the 4-day cefuroxime and 96.1% in those who received the 10-day penicillin. 30 days after treatment, the infection relapse rate was 2.8 and 2.3%, respectively.

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 the treatment of uncomplicated rectal gonorrhea in women. However, cefuroxime is not considered a preferred medication for the treatment of gonococcal infections.

In a study5 comparing efficacy of a single 1g oral dose of cefuroxime or a single 500mg oral dose of ciprofloxacin in adults with uncomplicated gonorrhea, both regimens appeared to be equally effective in eradicating urethral, endocervical, and rectal infections in women (eradication rate: 97–99%). However, the eradication rate in men with uncomplicated urethral infections was 93% in those who received cefuroxime axetil and 100% in those who received ciprofloxacin. While only a limited number of patients in the study had pharyngeal gonococcal infections, the single-dose oral cefuroxime axetil regimen appeared to be slightly less effective than the single-dose oral ciprofloxacin. In a study in women with uncomplicated gonorrhea who received a single 1g oral dose of cefuroxime, the cure rate ranged from 96–99% in those with urethral, endocervical, or rectal infections; in those with pharyngeal gonorrhea, the cure rate with cefuroxime was 60%.

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 oral doxycycline, oral amoxicillin, or oral cefuroxime axetil as first-line therapy for the treatment of early Lyme disease associated with erythema migrans, in the absence of specific neurologic involvement or advanced atrioventricular (AV) heart block.

Advantages:

• Broad-spectrum antibiotic. Cefuroxime has bactericidal activity against a wide range of common pathogens, including many beta-lactamase-producing strains6.
  Cefuroxime has good stability to bacterial beta-lactamase, and consequently is active against many ampicillin-resistant or amoxicillin-resistant strains.
• Less gastrointestinal side effects. Cefuroxime axetil produces fewer gastrointestinal side effects than some other widely used antibiotics (e.g. amoxicillin/clavulanate8, 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.
• 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 of cefuroxime 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.
• 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 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.

Cefuroxime is bactericidal antibiotic. Cefuroxime 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 penicillin-resistant or ampicillin and amoxicillin-resistant strains of susceptible species.

Cefuroxime half-life is 1.2 -1.3 h for tablets and 1.4-1.9 h for suspension.

• Cefuroxime (Ceftin) versus Other Medications

• 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. Drug Intelligence & Clinical Pharmacy: Vol. 19, No. 3, pp. 188-198.
• 3. Pichichero M, Aronovitz GH, Gooch WM, McLinn SE, Maddern B, Johnson C, Darden PM. Abstract Comparison of cefuroxime axetil, cefaclor, and amoxicillin-clavulanate potassium suspensions in acute otitis media in infants and children. South Med J. 1990 Oct;83(10):1174-7. PubMed
• 4. Gooch WM 3rd, Swenson E, Higbee MD, Cocchetto DM, Evans EC. Cefuroxime axetil and penicillin V compared in the treatment of group A beta-hemolytic streptococcal pharyngitis. Clin Ther. 1987;9(6):670-7. PubMed
• 5. Thorpe EM, Schwebke JR, Hook EW 3rd, Rompalo A, McCormack WM, Mussari KL, Giguere GC, Collins JJ. Comparison of single-dose cefuroxime axetil with ciprofloxacin in treatment of uncomplicated gonorrhea caused by penicillinase-producing and non-penicillinase-producing Neisseria gonorrhoeae strains. Antimicrob Agents Chemother. 1996 Dec;40(12):2775-80. PubMed
• 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. Short course therapy with cefuroxime axetil for acute otitis media: results of a randomized multicenter comparison with amoxicillin/clavulanate. PubMed