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Cefuroxime Axetil (Ceftin)


Basic information
  • Generic name: Cefuroxime Axetil
  • Brand/Trade names: Ceftin
  • Dosages:
    Tablets 125 mg, 250 mg, 500 mg
    Suspension 125 mg/5 mL, 250 mg/5 mL
  • Pharmacologic category: Cephalosporin antibiotic (Second Generation)
  • FDA approved: December 1987
  • Manufacturer: GlaxoWellcome
  • Habit forming? No
  • Pregnancy risk factor: B
Medical uses

Cefuroxime Axetil is a semi-synthetic cephalosporin antibiotic developed by Glaxo.

Cefuroxime Axetil is used to treat infections, including:

  • 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

Most frequent side effects include: diarrhea, nausea, vomiting, eosinophilia, headache.

Cefuroxime for Ear Infection (Otitis Media)

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 amoxicillin/clavulanate potassium.

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, moxicillin, or amoxicillin and clavulanate potassium. In published studies, the overall clinical response rate to a 10-day regimen of oral cefuroxime axetil in pediatric patients with AOM has ranged from 62–94%.

Cefuroxime axetil also appears to be effective for the treatment of otitis media in children when administered in a 5-day regimen. 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 amoxicillin/clavulanate potassium (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 amoxicillin and clavulanate potassium (Augmentin)1. 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 patients with underlying disease, recurrent or persistent otitis media, or perforated tympanic membranes and spontaneous purulent drainage.

Cefuroxime for Pharyngitis and Tonsillitis (Strep Throat)

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 at least as effective as a 10-day regimen of penicillin V 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) 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.

Pharmacological characteristics
  • 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.
Benefits
  • 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.
Concerns
  • Antibiotics, including cefuroxime axetil (Ceftin) can alter the colon's normal bacteria, leading to overgrowth of a bacterium called Clostridium difficile. Overgrowth of this bacterium leads to the release of toxins that contribute to the development of Clostridium difficile–associated diarrhea, which may range in severity from mild diarrhea to fatal colitis
Mechanism of action

Cefuroxime, a beta-lactam antibiotic similar to penicillins, inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) that are located inside the bacterial cell wall.

References
  • 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: results of a randomized multicenter comparison with amoxicillin/clavulanate. 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. Food and Drug Administration. Cefuroxime axetil (Ceftin) U.S. Prescribing Information. Available at (PDF format): Prescribing Information

 

Interesting facts


Cefuroxime facts
  • Absorption of the Cefuroxime tablet is greater when medication taken after food.
  • Cefuroxime axetil may be considered a second-line agent for the treatment of urinary tract infections.

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