Cefuroxime Axetil (Ceftin)

• Generic name: Cefuroxime Axetil
• Brand names: Ceftin, Zinacef, Zinnat
• Dosages:
  Tablets 125 mg, 250 mg, 500 mg
  Suspension 125 mg/5 mL, 250 mg/5 mL
• Pharmacologic category: Cephalosporin antibiotic (Second Generation), β-lactam
• FDA approved: December 1987
• Manufacturer: GlaxoWellcome
• Pregnancy risk factor: B

Cefuroxime Axetil is a semi-synthetic cephalosporin antibiotic developed by Glaxo. It is resistant to beta-lactamase.

Cefuroxime (Ceftin, Zinnat) is used to treat:

• Respiratory tract infections - acute and chronic bronchitis
• Urinary tract infections - pyelonephritis, cystitis
• Skin and skin structures infections - cellulitis, erysipelas, peritonitis and wound infections
• Uncomplicated gonorrhea
• Otitis media (ear infection)
• Pharyngitis
• Tonsillitis
• Lyme disease

Cefuroxime is not a drug of first choice for treatment of otitis media (middle ear infection), but is recommended as an alternative to amoxicillin or Augmentin.

Studies in children 3 months to 12 years of age demonstrate that a 10-day regimen of cefuroxime axetil is as effective or more effective than a 10-day regimen of cefaclor, amoxicillin, or Augmentin. In published studies, the overall clinical response rate to a 10-day regimen of oral cefuroxime axetil in children with AOM has ranged from 62–94%.

Cefuroxime axetil also appears to be effective for the treatment of otitis media in children when administered for 5days. In a randomized study in children 3 months to 12 years of age with acute otitis media, a satisfactory bacteriologic response (cure or presumed cure) was obtained in 92% of those who received a 5-day regimen of cefuroxime axetil (30 mg/kg daily given in 2 divided doses), 84% of those who received a 10-day regimen or cefuroxime axetil (30 mg/kg daily given in 2 divided doses), or 95% of those who received a 10-day regimen of Augmentin (40 mg/kg daily given in 3 divided doses).

There is evidence from a randomized study in children 6–36 months of age with acute otitis media that a 5-day regimen of cefuroxime axetil is as effective as and may be better tolerated than an 8- or 10-day regimen of Augmentin1. Some doctors caution that short-term antibiotic regimens (i.e., 5 days or less) may not be appropriate for the treatment of otitis media in children younger than 2 years of age or for those with underlying disease, recurrent or persistent otitis media, or perforated tympanic membranes and spontaneous purulent drainage.

Cefuroxime axetil is used for the treatment of pharyngitis and tonsillitis caused by streptococcal pharyngitis (group A beta-hemolytic streptococci).

A 10-day course of cefuroxime is highly 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 (20 mg/kg of cefuroxime in 2 divided doses daily) also provides successful treatment. The symptoms improvement rate was 94.8% in children who received the 4-day cefuroxime. 30 days after treatment, the infection relapse rate was 2.8%.

• Elimination half-life: 1.2 - 1.3 h (tablets), 1.4 - 1.9 h (suspension), and about 80 min (IV/IM). (tablets/suspension) and about 89% over 8 h (IV/IM).
• Excretion: About 50% is excreted unchanged in the urine within 12 h.

• May be taken with food.
• Fewer gastrointestinal side effects
• Convenient BID (twice daily) dosing schedule.
• Generally well tolerated and side effects are usually transient.
• Cefuroxime is more active against gram-negative bacteria than are the first-generation cephalosporins (e.g. cephalexin).
• Except for ceftriaxone, cefuroxime is more active against Haemophilus influenzae, including beta-lactamase-producing strains, than are other cephalosporins.
• It is distributed into most body tissues and fluids including gallbladder, liver, kidney, bone, uterus, ovary, sputum, bile, and peritoneal, pleural, and synovial fluids.
• Improved activity against common beta-lactamase­producing respiratory pathogens such as H. influenzae and M. catarrhalis2.

Cefuroxime is a bactericidal beta-lactam antimicrobial. It inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific proteins (PBPs) that are located inside the bacterial cell wall. After antibiotic has bound to these receptors, the transpeptidation reaction is inhibited and peptidoglycan synthesis is blocked. Finally, it results in bacterial lysis.

• 1. 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: a randomized multicenter comparison. PubMed
• 2. Kayser FH, Bille J. In-vitro activity of cefuroxime-axetil against pathogens of bacterial infections of the respiratory tract. Schweiz Rundsch Med Prax. 1990 Nov 6;79(45):1383-6. PubMed
• 3. U.S. FDA. Cefuroxime axetil (Ceftin) Prescribing Information