cefuroxime
Brand: Zinacef, Ceftin
Prototype Drug
Drug Class: second-generation cephalosporin
Drug Family: antibiotic
Subclass: oral and parenteral second-generation cephalosporin
Organ Systems: infectious-disease
Mechanism of Action
Inhibits cell wall synthesis by binding PBPs; offers enhanced gram-negative spectrum over first-generation cephalosporins including H. influenzae and M. catarrhalis, while maintaining gram-positive activity.
penicillin-binding proteins (PBPs)
Indications
- community-acquired pneumonia
- sinusitis
- otitis media
- skin and soft tissue infections
- UTI
- Lyme disease (early)
- surgical prophylaxis
Contraindications
- cephalosporin hypersensitivity
Adverse Effects
Common
- diarrhea
- nausea
- metallic taste (oral)
Serious
- anaphylaxis
- C. difficile colitis
- hemolytic anemia
Pharmacokinetics (ADME)
| Absorption | oral axetil prodrug: 37–52% bioavailability, increased with food; IV/IM: complete absorption |
| Distribution | widely distributed; poor CSF penetration (unless inflamed meninges) |
| Metabolism | axetil prodrug hydrolyzed to active cefuroxime in intestinal mucosa |
| Excretion | renal (unchanged) |
| Half-life | 1–2 hours |
| Onset | rapid |
| Peak | 2–3 hours (oral), 30 min (IV/IM) |
| Duration | 8–12 hours |
| Protein Binding | 33–50% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| probenecid | reduces renal tubular secretion, increases cefuroxime levels | minor |
| antacids/H2 blockers | reduced oral absorption of cefuroxime axetil prodrug | moderate |
Nursing Considerations
- Administer oral cefuroxime axetil with food to improve bioavailability and reduce GI upset.
- IV infusion: administer over 15–60 minutes; monitor for phlebitis at infusion site.
- Reduce dose in severe renal impairment (CrCl <20 mL/min).
- For early Lyme disease, 500 mg twice daily for 14–21 days is the standard regimen; counsel patient to complete the full course.
Clinical Pearls
- Cefuroxime is one of the few second-generation cephalosporins available in both oral and IV formulations, allowing convenient oral step-down therapy.
- Its prodrug formulation (cefuroxime axetil) is activated by intestinal esterases; reduced gastric pH from antacids or H2 blockers can impair this activation.
Safety Profile
Pregnancy generally-safe
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.