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Cefuroxime

Cefuroxime: A Comprehensive Review of the Second-Generation Cephalosporin

Cefuroxime is a broad-spectrum, second-generation cephalosporin antibiotic that plays a vital role in treating bacterial infections across a range of clinical scenarios. Introduced in the 1970s, it has proven its utility against both Gram-positive and Gram-negative organisms, especially those responsible for respiratory tract infections, skin infections, urinary tract infections, and early Lyme disease.

1. Introduction to Cefuroxime

Cefuroxime belongs to the beta-lactam class of antibiotics and is categorized under second-generation cephalosporins. It is available in two formulations:

  • Cefuroxime sodium – for intravenous or intramuscular injection

  • Cefuroxime axetil – an orally administered prodrug

Due to its enhanced stability against beta-lactamases compared to first-generation cephalosporins, Cefuroxime has become a preferred agent for infections involving resistant bacteria.

2. Chemical and Structural Characteristics

Cefuroxime’s structure contains:

  • A beta-lactam ring, essential for antibacterial activity

  • A syn-oxime methoxyimino group, which provides resistance to many beta-lactamases

  • A carbamoyl group at the 7-position, enhancing its spectrum against Gram-negative organisms

Its prodrug, cefuroxime axetil, is lipophilic and designed for better gastrointestinal absorption. Upon oral administration, it is hydrolyzed to the active form, cefuroxime.

3. Mechanism of Action

Like all beta-lactams, Cefuroxime targets bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs), which are crucial for peptidoglycan cross-linking. This interference causes structural instability in the bacterial cell wall, leading to cell lysis and death. Cefuroxime exhibits bactericidal activity, making it highly effective in eradicating susceptible pathogens.

4. Antibacterial Spectrum

Cefuroxime has a broad spectrum of activity:

Gram-Positive Bacteria

  • Streptococcus pneumoniae

  • Streptococcus pyogenes

  • Staphylococcus aureus (methicillin-sensitive)

Gram-Negative Bacteria

  • Haemophilus influenzae (including beta-lactamase producers)

  • Moraxella catarrhalis

  • Escherichia coli

  • Klebsiella pneumoniae

  • Neisseria gonorrhoeae

Limitations

  • Ineffective against Pseudomonas aeruginosa

  • Limited efficacy against organisms producing extended-spectrum beta-lactamases (ESBLs) or carbapenemases

5. Pharmacokinetics

Absorption

  • Cefuroxime axetil has about 30-50% bioavailability.

  • Food enhances absorption, and it is recommended to take it with meals.

Distribution

  • Well-distributed into body fluids and tissues: lungs, tonsils, middle ear, sinuses, bones, and soft tissues

  • Penetrates the cerebrospinal fluid (CSF) when meninges are inflamed

Metabolism and Elimination

  • Not extensively metabolized

  • Excreted unchanged in urine

  • Half-life: approximately 1–1.5 hours

  • Renal elimination necessitates dose adjustments in renal impairment

6. Formulations and Dosage

Form Strengths Typical Adult Dose
Cefuroxime Axetil (oral) 125 mg, 250 mg, 500 mg tablets 250–500 mg twice daily
Cefuroxime Sodium (IV/IM) 750 mg, 1.5 g 750 mg–1.5 g every 8 hours

Pediatric Dosing

  • Oral: 20–30 mg/kg/day divided twice daily

  • Parenteral: 50–100 mg/kg/day in divided doses

7. Clinical Applications

7.1 Respiratory Tract Infections

Cefuroxime is commonly prescribed for:

  • Acute bronchitis

  • Chronic obstructive pulmonary disease (COPD) exacerbations

  • Community-acquired pneumonia

  • Pharyngitis and tonsillitis

  • Acute bacterial sinusitis

Its excellent activity against H. influenzae and S. pneumoniae makes it ideal in outpatient respiratory infections.

7.2 Skin and Soft Tissue Infections

  • Treats cellulitis, impetigo, and infected wounds

  • Used where beta-lactamase–producing Staph. aureus or Streptococcus spp. are suspected

7.3 Urinary Tract Infections

  • Effective in cystitis and pyelonephritis caused by E. coli and other Gram-negative bacilli

7.4 Lyme Disease

  • Recommended by IDSA as second-line oral treatment in early Lyme disease caused by Borrelia burgdorferi

  • Also used for Lyme-associated arthritis

7.5 Gonorrhea

  • Cefuroxime has historical use in uncomplicated Neisseria gonorrhoeae infections, although newer resistance patterns limit its role today

8. Adverse Effects

Most side effects are mild and reversible:

Common

  • Diarrhea

  • Nausea

  • Vomiting

  • Abdominal pain

Less Common

  • Headache

  • Dizziness

  • Rash

  • Vaginal candidiasis (yeast infection)

Serious (Rare)

  • Anaphylaxis

  • Stevens-Johnson syndrome

  • Clostridioides difficile–associated diarrhea

  • Seizures (especially with renal impairment or high doses)

9. Drug Interactions

  • Antacids and H2 blockers: reduce absorption of cefuroxime axetil

  • Probenecid: decreases renal excretion, increasing serum levels

  • Oral contraceptives: may reduce contraceptive efficacy (a theoretical risk common to many antibiotics)

10. Resistance Mechanisms

Cefuroxime, like all antibiotics, faces growing resistance:

Mechanisms

  • Beta-lactamase production: especially extended-spectrum beta-lactamases (ESBLs)

  • Altered PBPs: reduced binding affinity

  • Efflux pumps: reduce intracellular drug concentrations

  • Porin channel mutations: limit cell wall permeability

Resistance Trends

  • Resistance is rising among Enterobacteriaceae, especially in nosocomial settings

  • Community-acquired S. pneumoniae and H. influenzae remain largely susceptible, but monitoring is essential

11. Special Populations

Pregnancy and Lactation

  • Classified as Category B

  • No known teratogenic effects

  • Safe during breastfeeding; minimal excretion into breast milk

Renal Impairment

  • Dose adjustment is necessary

  • Risk of neurotoxicity (seizures) in patients with severe renal dysfunction

Pediatric Use

  • Widely used in children over 3 months

  • Well-tolerated and safe with proper dosing

12. Cefuroxime vs. Other Cephalosporins

Feature Cefuroxime Ceftriaxone Cefixime
Generation 2nd 3rd 3rd
Route Oral/IV/IM IV/IM Oral
CNS Penetration Moderate Excellent Moderate
Half-life 1–1.5 hrs ~8 hrs ~3–4 hrs
Dosing Frequency BID Once daily Once or twice daily
Best Use RTIs, Lyme Meningitis, Sepsis URTI, UTI

13. Emerging Role and Future Trends

As antibiotic resistance continues to rise, Cefuroxime remains useful in outpatient settings, particularly for respiratory and skin infections. However, stewardship is essential to preserve its efficacy.

Areas of Ongoing Research

  • New prodrugs for enhanced oral bioavailability

  • Combination therapies with beta-lactamase inhibitors

  • Role in COVID-19–related secondary bacterial infections (limited data)

14. Conclusion

Cefuroxime remains a cornerstone antibiotic in the management of community-acquired infections due to its reliability, broad-spectrum efficacy, and favorable safety profile. While its role in severe nosocomial infections is limited by resistance, it continues to be invaluable in outpatient and pediatric care. Proper antibiotic stewardship, susceptibility testing, and rational prescribing will ensure that Cefuroxime remains a key player in combating bacterial infections in the years ahead.