Ceftin (Cefuroxime Axetil) for Bacterial Infections
Direct Answer
Ceftin (cefuroxime axetil) is a second-generation oral cephalosporin used at 250-500 mg twice daily for 5-10 days to treat community-acquired respiratory tract infections (including acute bacterial sinusitis, acute otitis media, pharyngitis, bronchitis, and pneumonia), urinary tract infections, and skin/soft tissue infections caused by susceptible bacteria including Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. 1, 2
Primary Clinical Indications
Respiratory Tract Infections
- Upper respiratory infections: Cefuroxime axetil is recommended as first-line therapy for acute bacterial sinusitis (maxillary, frontal, fronto-ethmoidal, and sphenoidal) at 250-500 mg twice daily 1, 2
- Lower respiratory infections: Effective for community-acquired pneumonia and acute exacerbations of chronic bronchitis, with 500 mg twice daily recommended for pneumonia or severe infections 3, 4
- Acute otitis media: 5-day courses are as effective as 10-day courses in clinical trials 4
- Pharyngitis/tonsillitis: At least as effective as penicillin V for group A beta-hemolytic streptococcal infections 5
Other Infections
- Urinary tract infections: 125-250 mg twice daily for uncomplicated cystitis; higher doses for pyelonephritis 3, 4
- Skin and soft tissue infections: 250-500 mg twice daily for furunculosis, pyoderma, and impetigo 3, 6
- Uncomplicated gonorrhea: Single 1-gram dose for acute uncomplicated gonococcal urethritis and cervicitis 3
- Early Lyme disease: Effective for erythema migrans 5, 4
Bacterial Spectrum of Activity
Gram-Positive Coverage
- Streptococcus pneumoniae: Achieves 75-85% coverage for penicillin-susceptible and intermediate strains based on pharmacokinetic/pharmacodynamic breakpoints 2, 7
- Critical limitation: No clinically significant activity against drug-resistant S. pneumoniae (DRSP)—this is a major treatment failure risk 1, 2, 7
- Other gram-positive organisms: Active against methicillin-susceptible Staphylococcus aureus, group A beta-hemolytic streptococci, and Streptococcus pyogenes 2, 3
Gram-Negative Coverage
- Haemophilus influenzae: Achieves 70-85% coverage, including beta-lactamase-producing strains, though less active than cefpodoxime 1, 2, 7
- Moraxella catarrhalis: Approximately 50% coverage—significantly inferior to third-generation cephalosporins 2
- Enterobacteriaceae: Active against E. coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella/Shigella species 3
Organisms Without Coverage
- No activity against Pseudomonas aeruginosa, enterococci, or anaerobes like Bacteroides fragilis 2
- No activity against methicillin-resistant Staphylococcus aureus (MRSA) 3
Dosing Recommendations
Standard Adult Dosing
- Most infections: 250 mg twice daily 3, 4
- Severe lower respiratory infections or pneumonia: 500 mg twice daily 3, 4
- Uncomplicated UTI: 125 mg twice daily may be sufficient 3
- Gonorrhea: Single 1-gram dose 3
Treatment Duration
- Standard course: 5-10 days for most infections 4
- Short-course therapy: 5-day courses are as effective as 10-day courses for acute otitis media and acute bronchitis 5, 4
Sequential IV-to-Oral Therapy
- Parenteral cefuroxime 750 mg 2-3 times daily for 2-5 days, followed by oral cefuroxime axetil 500 mg twice daily for 3-8 days is effective for community-acquired pneumonia requiring initial hospitalization 4
Mechanism of Action and Pharmacokinetics
- Mechanism: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), triggering bacterial autolysis 8
- Bioavailability: 68% (range 63-73%) after oral administration of 500 mg with food 3
- Peak plasma concentration: 4.6 mg/L after 250 mg and 7.9 mg/L after 500 mg when taken with meals 3
- Protein binding: 33% 3
- Tissue penetration: Achieves therapeutic concentrations in interstitial fluid, bronchial mucosa, tonsils, and bronchial secretions 3
Critical Clinical Pitfalls and Caveats
When NOT to Use Cefuroxime
- Drug-resistant S. pneumoniae suspected: Cefuroxime has no activity against DRSP—use high-dose amoxicillin (80-100 mg/kg/day) or respiratory fluoroquinolones instead 1, 2, 7
- H. influenzae as primary pathogen: Consider cefpodoxime instead, which has markedly superior activity 1, 7
- Severe M. catarrhalis infections: Only 50% coverage makes cefuroxime suboptimal 2
Comparative Positioning
- Middle-tier oral cephalosporin: Superior to cefaclor and loracarbef but inferior to cefpodoxime for H. influenzae coverage 1, 7
- Equivalent to cefdinir and cefprozil for S. pneumoniae activity 1, 2
- Preferred second-line agent: When high-dose amoxicillin or amoxicillin-clavulanate fails or is intolerable, cefpodoxime is generally preferred over cefuroxime due to superior H. influenzae coverage 1, 7
Pediatric Considerations
- Palatability issue: Cefuroxime axetil suspension is notably unpalatable, which significantly limits adherence in children—this is a major practical limitation 7
- Acute bronchiolitis in children: First-line antibiotic therapy is generally not indicated; if needed, use only for fever >38.5°C persisting >3 days, purulent otitis media, or confirmed pneumonia 1
Safety Profile and Monitoring
Common Adverse Effects
- Gastrointestinal disturbances: Diarrhea, nausea, and vomiting are most common but generally mild to moderate 3, 5, 4
- Overall incidence: Low adverse event rate with <1% serious events 5, 4
Special Populations
- Pregnancy: Listed on the 2015 US FDA list of drugs that can be used safely during pregnancy 6
- Nursing mothers: Excreted in human milk; use with caution 9
- Renal impairment: Reduce total daily dose in patients with renal insufficiency to prevent drug accumulation 9
- Pediatric patients: Safety not established in children <3 months of age 9
Drug Interactions and Monitoring
- Prothrombin time monitoring: Required in patients at risk (renal/hepatic impairment, poor nutritional state, prolonged therapy, concurrent anticoagulation) due to potential fall in prothrombin activity 9
- Nephrotoxicity risk: Use caution with concurrent aminoglycosides 9
- Laboratory interference: False-positive urine glucose with copper reduction tests (use enzyme-based tests instead); false-negative ferricyanide test for blood glucose 9
Resistance Considerations
Geographic Variability in Europe
- Penicillin non-susceptible S. pneumoniae (PNSP) rates vary widely: <5% in northern Europe, but >25% in southern/eastern Europe (Cyprus 43%, Malta 47%, Turkey 34%, France 30%) 1
- Clinical implication: In high-resistance areas, cefuroxime may have unacceptably high failure rates for pneumococcal infections 1