Cefuroxime is a broad spectrum 2nd generation cephalosporin antibiotic.
It is bactericidal.
It has less susceptibility to penicillinase inactivation than the first-generation cephalosporins.
Class:
2nd Generation Cephalosporin (β-lactam antibiotic)
Spectrum:
Broad-spectrum, bactericidal
Mechanism of Action
Cefuroxime inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs) . This disrupts the final transpeptidation step in peptidoglycan cross-linking, causing bacterial lysis and cell death.
- Resistant to many β-lactamases (penicillinases) compared to first-generation cephalosporins.
Susceptible Organisms
Effective against both Gram-positive and Gram-negative pathogens, including:
- Borrelia burgdorferi (Lyme disease)
- Escherichia coli
- Haemophilus influenzae
- Klebsiella spp.
- Moraxella catarrhalis
- Neisseria gonorrhoeae
- Proteus mirabilis
- Streptococcus pneumoniae
- Streptococcus pyogenes
Pharmacokinetics
- Absorption: Oral cefuroxime axetil is a prodrug, hydrolyzed to active cefuroxime after absorption.
- Distribution: Widely distributed in extracellular fluid.
- Metabolism: Minor metabolism to acetic acid and acetaldehyde.
- Protein Binding: ~50%
- Excretion: Renally excreted unchanged; ~50% recovered in urine within 12 hours.
- Half-life: ~1–1.5 hours
Indications
Cefuroxime is indicated for the treatment of various bacterial infections:
- Septicemia
- Meningitis
- Perioperative prophylaxis
- Bone and joint infections
- Respiratory tract infections
- Upper: Otitis media, sinusitis, tonsillitis, pharyngitis
- Lower: Acute/chronic bronchitis, pneumonia
- Skin and soft tissue infections (e.g., impetigo, furunculosis)
- Urinary tract infections (e.g., pyelonephritis, cystitis, urethritis)
- Gonorrhea (uncomplicated)
Contraindications
- Known hypersensitivity to cephalosporins or penicillins .
Adverse Reactions
Common (mild):
- GI: Nausea, vomiting, diarrhea
- Local: Pain at IM site
Severe (rare):
- Hypersensitivity: Anaphylaxis, angioedema, urticaria, serum sickness
- GI: Pseudomembranous colitis
- Hematologic: Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia
- Hepatic: Hepatitis, cholestasis, elevated liver enzymes, jaundice
- Dermatologic: Erythema multiforme, Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN)
- Neurologic: Headache, seizures (especially in overdose or renal impairment)
Precautions
- Caution in patients with β-lactam allergy .
- Risk of superinfection with prolonged use (e.g., C. difficile colitis).
- Tablets should not be crushed ; not recommended for children <5 years.
- Use with caution in renal impairment ; although no adjustment is usually necessary, monitoring is advised.
- Consider using glucose oxidase or hexokinase for accurate blood glucose monitoring.
Drug Interactions
- Probenecid: Increases serum cefuroxime levels (↓renal clearance).
- Antacids/PPIs: May reduce cefuroxime absorption (↓bioavailability).
- Anticoagulants: Potentiated effect (↑bleeding risk).
- Cholera vaccine, BCG vaccine: Reduced effectiveness.
- Ferricyanide test: May yield false-negative results.
Use in Pregnancy and Lactation
- Pregnancy: No known teratogenic risk. Use only if clearly indicated.
- Lactation: Excreted in breast milk. Consider temporary discontinuation of breastfeeding.
Dosage and Administration
| Indication | Dose (Adults) |
|---|---|
| Acute bronchitis | 250 mg PO BID |
| Pneumonia | 500 mg PO BID |
| Uncomplicated UTI | 125 mg PO BID |
| Pyelonephritis | 250 mg PO BID |
| Otitis media | 250 mg PO BID |
| Gonorrhea (uncomplicated) | 1000 mg PO single dose |
- Pediatrics (≥5 years): 125 mg PO BID if able to swallow tablets.
- Duration: Typically 7 days .
- Administration: Take after food to enhance absorption.
- Special populations: No dose adjustment usually required for elderly or renal impairment , but monitor closely.
Overdose Management
- Symptoms: Neurotoxicity, including seizures and cerebral irritation .
- Treatment: Supportive care. Hemodialysis or peritoneal dialysis can help eliminate the drug.
