Cefuroxime (Ceftin / Zinacef)
cefuroxime axetil (oral) · cefuroxime sodium (IV/IM)
Indications
| Indication | Approved Population | Formulation | Status |
|---|---|---|---|
| Pharyngitis / tonsillitis (S. pyogenes) | Adults & peds (tablets ≥13 y; suspension ≥3 mo) | Oral | FDA Approved |
| Acute otitis media (S. pneumoniae, H. influenzae, M. catarrhalis, S. pyogenes) | Pediatric ≥3 months | Oral (suspension) | FDA Approved |
| Acute bacterial sinusitis (S. pneumoniae, H. influenzae) | Adults & peds (tablets ≥13 y; suspension ≥3 mo) | Oral | FDA Approved |
| Acute exacerbation of chronic bronchitis (S. pneumoniae, H. influenzae, H. parainfluenzae) | Adults & peds ≥13 years | Oral | FDA Approved |
| Uncomplicated skin & skin structure infections (S. aureus [MSSA], S. pyogenes) | Adults & peds ≥13 years | Oral | FDA Approved |
| Uncomplicated UTI (E. coli, K. pneumoniae) | Adults & peds ≥13 years | Oral | FDA Approved |
| Uncomplicated gonorrhea (N. gonorrhoeae) | Adults & peds ≥13 years | Oral (single dose) | FDA Approved |
| Early Lyme disease (Borrelia burgdorferi) | Adults & peds ≥13 years | Oral | FDA Approved |
| Lower respiratory tract infections (pneumonia) | Adults & peds ≥3 months | IV/IM | FDA Approved |
| Septicemia, meningitis, bone/joint infections, perioperative prophylaxis | Adults & peds ≥3 months (Zinacef) | IV/IM | FDA Approved |
Cefuroxime is a versatile second-generation cephalosporin available in both oral (as the prodrug cefuroxime axetil) and parenteral (as cefuroxime sodium) formulations. Compared with first-generation agents, cefuroxime offers enhanced activity against beta-lactamase-producing H. influenzae and M. catarrhalis while retaining useful gram-positive coverage. It is one of the few oral cephalosporins with an FDA-approved indication for early Lyme disease and is recommended as an alternative to doxycycline by IDSA/AAN guidelines. The parenteral formulation achieves adequate CSF penetration in bacterial meningitis, which is unique among second-generation cephalosporins.
Community-acquired pneumonia — IV-to-oral step-down: Commonly used as sequential IV cefuroxime → oral cefuroxime axetil for hospitalised patients with CAP. ATS/IDSA CAP guidelines list cefuroxime as an option for non-ICU inpatients. Evidence quality: Moderate.
Intracameral injection — post-cataract endophthalmitis prophylaxis: Cefuroxime 1 mg intracameral injection at the end of cataract surgery is supported by high-quality evidence (ESCRS trial) and is standard practice in Europe and increasingly in the US. Evidence quality: High.
Dosing
Adult Oral Dosing by Clinical Scenario (Cefuroxime Axetil Tablets)
| Clinical Scenario | Starting Dose | Maintenance Dose | Maximum Dose | Notes |
|---|---|---|---|---|
| Pharyngitis / tonsillitis (GAS) | 250 mg PO BID | 250 mg PO BID | 500 mg/day | 10 days; alternative to penicillin |
| Acute bacterial sinusitis | 250 mg PO BID | 250 mg PO BID | 500 mg/day | 10 days |
| Acute exacerbation of chronic bronchitis | 250–500 mg PO BID | 250–500 mg PO BID | 1 g/day | 10 days Use 500 mg for more severe exacerbations |
| Uncomplicated skin/soft tissue infection | 250–500 mg PO BID | 250–500 mg PO BID | 1 g/day | 10 days |
| Uncomplicated UTI | 250 mg PO BID | 250 mg PO BID | 500 mg/day | 7–10 days |
| Uncomplicated gonorrhea | 1 g PO single dose | N/A | 1 g | Single dose; not preferred per current CDC guidelines |
| Early Lyme disease (erythema migrans) | 500 mg PO BID | 500 mg PO BID | 1 g/day | 20 days; IDSA/AAN recommended alternative to doxycycline Jarisch-Herxheimer reaction may occur |
Adult IV/IM Dosing by Clinical Scenario (Cefuroxime Sodium — Zinacef)
| Clinical Scenario | Starting Dose | Maintenance Dose | Maximum Dose | Notes |
|---|---|---|---|---|
| Uncomplicated infection (UTI, SSSI, pneumonia) | 750 mg IV/IM Q8H | 750 mg IV/IM Q8H | 2.25 g/day | 5–10 days; step down to oral when able |
| Severe / complicated infection | 1.5 g IV Q8H | 1.5 g IV Q8H | 4.5 g/day | 5–10 days |
| Bone & joint infections | 1.5 g IV Q8H | 1.5 g IV Q8H | 4.5 g/day | May follow with oral step-down |
| Life-threatening / less susceptible organisms | 1.5 g IV Q6H | 1.5 g IV Q6H | 6 g/day | Maximum IV dose |
| Bacterial meningitis | 1.5 g IV Q6–8H | 1.5 g IV Q6–8H | 6 g/day | Adequate CSF penetration with inflamed meninges Pediatric: 200–240 mg/kg/day divided Q6–8H (max 9 g/day) |
| Surgical prophylaxis | 1.5 g IV | 750 mg IV/IM Q8H × 24–48 h | 1.5 g preop | Give ½–1 h before incision Open-heart: 1.5 g Q12H × 4 total doses |
Renal Dose Adjustment
| CrCl (mL/min) | Oral | IV/IM | Source |
|---|---|---|---|
| ≥30 | No adjustment | No adjustment | FDA PI |
| 10–29 | Standard dose Q24H | 750 mg IV Q12H | FDA PI / StatPearls |
| <10 | Standard dose Q48H | 750 mg IV Q24H | FDA PI / StatPearls |
| Hemodialysis | Additional dose after each session | FDA PI | |
Cefuroxime axetil tablets and oral suspension are NOT bioequivalent and must not be substituted on a milligram-per-milligram basis. The suspension achieves approximately 91% of the AUC and 71% of the Cmax compared with the tablet formulation. Each formulation has independently established safety and efficacy data. Tablets can be taken with or without food (food increases absorption), while the suspension must always be administered with food (FDA PI). Avoid concurrent use of antacids, H2-receptor antagonists, or proton pump inhibitors, as these can significantly reduce oral cefuroxime bioavailability.
Pharmacology
Mechanism of Action
Cefuroxime is a bactericidal beta-lactam antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), disrupting the final transpeptidation step of peptidoglycan cross-linking. This leads to osmotic instability and cell lysis. As a second-generation cephalosporin, cefuroxime has enhanced stability against beta-lactamases produced by common respiratory pathogens such as H. influenzae and M. catarrhalis, while retaining activity against MSSA and streptococci. Its bactericidal activity is time-dependent (% fT > MIC). The oral formulation (cefuroxime axetil) is an acetoxyethyl ester prodrug that is rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to release active cefuroxime.
ADME Profile
| Parameter | Value | Clinical Implication |
|---|---|---|
| Absorption | Oral: prodrug hydrolyzed to cefuroxime; bioavailability ~37–52% (increases with food); Tmax ~2–3 h. IV: Cmax ~100 mcg/mL after 1.5 g | Food significantly enhances oral absorption; suspension MUST be given with food; tablets may be taken with or without food but food improves absorption; avoid acid-suppressing drugs |
| Distribution | Distributed throughout extracellular fluids; ~50% protein bound; penetrates CSF (especially inflamed meninges), bone, synovial fluid, sputum, bile | CSF penetration supports meningitis use (IV formulation only); adequate bone penetration for osteomyelitis |
| Metabolism | Axetil ester hydrolyzed to cefuroxime + acetaldehyde + acetic acid; cefuroxime itself undergoes no hepatic metabolism; no CYP involvement | Minimal drug-drug interaction potential via metabolic pathways; no hepatic dose adjustment |
| Elimination | t½ ~1.2–1.3 h (normal renal function); ~3.5 h in elderly (CrCl ~35); oral: ~50% unchanged in urine within 12 h; IV: ~89% unchanged in urine within 8 h | Dose reduction required when CrCl <30 mL/min; removed by hemodialysis — give supplemental dose post-dialysis |
Side Effects
| Adverse Effect | Incidence | Clinical Note |
|---|---|---|
| Diarrhea / loose stools | 3.7% | Most common GI reaction; taking with food may reduce; distinguish from C. difficile |
| Nausea / vomiting | 3.0% | Usually self-limiting; more common with suspension |
| Jarisch-Herxheimer reaction | 5.6% | Occurs in early Lyme disease treatment only; fever, myalgia within 24 h of starting; self-limiting |
| Vaginitis | 5.1% | Reported primarily in Lyme disease trials (20-day course); disruption of vaginal flora |
| Adverse Effect | Incidence | Clinical Note |
|---|---|---|
| Thrombophlebitis (IV) | 1.7% (1 in 60) | IV administration; rotate infusion sites |
| Transient eosinophilia | ~1% | Usually not clinically significant |
| Elevated liver enzymes | ~1% | Transient AST/ALT elevations; monitor if prolonged therapy |
| Positive Coombs’ test | ~1% | Usually without hemolysis; inform blood bank |
| Adverse Effect | Estimated Frequency | Typical Onset | Required Action |
|---|---|---|---|
| Anaphylaxis / severe hypersensitivity | Rare | Minutes to hours | Discontinue; epinephrine; emergency care |
| C. difficile-associated diarrhea | Uncommon | During or up to 2 months post-therapy | Test for toxin; discontinue cefuroxime; treat with vancomycin or fidaxomicin |
| Seizures | Rare (postmarketing) | Variable; higher risk with renal impairment | Discontinue; anticonvulsant therapy; dose-adjust for renal function |
| Hepatitis / cholestasis | Rare (postmarketing) | Days to weeks | Discontinue; evaluate hepatic function |
| Hearing loss (IV, pediatric meningitis) | Uncommon | During therapy | Audiometric monitoring in meningitis; usually mild-to-moderate |
| Stevens-Johnson syndrome | Very rare | 1–3 weeks | Discontinue immediately; dermatology referral |
Up to 5.6% of patients treated for early Lyme disease may experience a Jarisch-Herxheimer reaction — an acute febrile response with myalgia, headache, and temporary worsening of symptoms — typically within the first 24 hours of antibiotic initiation. This reaction reflects spirochaetal lysis and should not be confused with drug allergy. It is self-limiting, resolves within 24–48 hours, and should not prompt discontinuation of therapy. Symptomatic management with antipyretics is appropriate (FDA PI).
Drug Interactions
Cefuroxime itself undergoes no CYP-mediated metabolism, but the oral prodrug (cefuroxime axetil) is significantly affected by gastric pH, making acid-suppressing drugs a clinically important interaction.
Monitoring
- Renal FunctionBaseline; periodically
RoutineAssess CrCl before and during therapy. Dose adjustment required when CrCl <30 mL/min. Elderly patients likely to have impaired renal function; mean t½ increases to 3.5 h. - Clinical Response48–72 h
RoutineEvaluate for clinical improvement. For Lyme disease, assess resolution of erythema migrans. If no response, consider cultures and alternative therapy. - GI Symptoms / StoolIf diarrhea develops
Trigger-basedTest for C. difficile toxin if diarrhea is persistent, watery, or bloody, during or up to 2 months after therapy. - CBCIf therapy >14 days
Trigger-basedMonitor for eosinophilia, leukopenia, thrombocytopenia. Particularly relevant for prolonged Lyme disease courses (20 days). - Hearing (Pediatric Meningitis)During and after IV therapy
Trigger-basedMild-to-moderate hearing loss reported in pediatric meningitis patients treated with cefuroxime. Audiometric assessment recommended. - IV SiteEach dose
RoutineMonitor for thrombophlebitis (~1.7% incidence); rotate infusion sites as needed.
Contraindications & Cautions
Absolute Contraindications
- Known hypersensitivity to cefuroxime or any member of the cephalosporin class
Relative Contraindications (Specialist Input Recommended)
- History of penicillin allergy — cross-hypersensitivity among beta-lactams may occur in up to 10% of penicillin-allergic patients
- MRSA infection — cefuroxime has no activity; confirm susceptibility
Use with Caution
- Renal impairment (CrCl <30 mL/min) — dose adjustment required; risk of accumulation and seizures
- Concurrent acid-suppressing therapy — PPIs, H2 blockers, and antacids significantly reduce oral bioavailability
- Elderly patients — impaired renal function prolongs half-life (mean 3.5 h when CrCl ~35)
- History of GI disease (especially colitis) — increased risk of C. difficile
- Pediatric meningitis (IV) — risk of hearing loss; audiometric monitoring recommended
- Pediatric patients <3 months — safety and effectiveness not established
Cross-hypersensitivity among beta-lactam antibacterial drugs may occur in up to 10% of patients with a history of penicillin allergy. Before initiating cefuroxime therapy, inquire about previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. If an allergic reaction occurs, discontinue the drug immediately and institute appropriate treatment (FDA PI).
Patient Counselling
Purpose of Therapy
Cefuroxime is a prescription antibiotic used to treat bacterial infections of the ears, sinuses, throat, lungs, skin, urinary tract, and for early Lyme disease. The oral form (tablets or liquid) is taken at home, while the injectable form is given by a healthcare professional in a hospital or clinic. Cefuroxime does not work against viral infections.
How to Take (Oral)
Take tablets twice daily with or without food, though taking with food improves absorption. The liquid suspension must always be taken with food. Shake the liquid well before each dose. Swallow tablets whole; do not crush — crushed tablets have a strong bitter taste. Complete the full course even if symptoms improve. Store the liquid in the refrigerator and discard after 10 days.
Sources
- CEFTIN (cefuroxime axetil) tablets and oral suspension prescribing information. Revised 2021. FDA LabelPrimary source for oral formulation indications, dosing, adverse reactions (including Lyme disease-specific data), PK, and drug interactions.
- ZINACEF (cefuroxime for injection) prescribing information. Revised 2021. FDA LabelPrimary source for IV/IM formulation indications (including meningitis, septicemia, surgical prophylaxis), dosing, PK (t½ ~80 min, ~89% renal excretion), and CSF penetration data.
- Cefuroxime axetil tablets prescribing information (generic). Aurobindo Pharma. DailyMedUpdated generic tablet label confirming identical clinical information to branded Ceftin product.
- Nadelman RB, Luger SW, Frank E, et al. Comparison of cefuroxime axetil and doxycycline in the treatment of early Lyme disease. Ann Intern Med. 1992;117(4):273-280. doi:10.7326/0003-4819-117-4-273Pivotal RCT establishing cefuroxime axetil 500 mg BID × 20 days as effective alternative to doxycycline for early Lyme disease.
- Luger SW, Paparone P, Wormser GP, et al. Comparison of cefuroxime axetil and doxycycline in treatment of patients with early Lyme disease associated with erythema migrans. Antimicrob Agents Chemother. 1995;39(3):661-667. doi:10.1128/AAC.39.3.661Second pivotal Lyme disease trial confirming comparable efficacy of cefuroxime axetil vs doxycycline; safety data for 20-day course.
- Wormser GP, Dattwyler RJ, Shapiro ED, et al. The clinical assessment, treatment, and prevention of Lyme disease, human granulocytic anaplasmosis, and babesiosis: clinical practice guidelines by the IDSA. Clin Infect Dis. 2006;43(9):1089-1134. doi:10.1086/508667IDSA guideline recommending cefuroxime axetil 500 mg BID × 14–21 days as first-line alternative to doxycycline for early Lyme disease.
- Bratzler DW, Dellinger EP, Olsen KM, et al. Clinical practice guidelines for antimicrobial prophylaxis in surgery. Am J Health Syst Pharm. 2013;70(3):195-283. doi:10.2146/ajhp120568ASHP/IDSA/SIS/SHEA guideline recommending cefuroxime as alternative to cefazolin for surgical prophylaxis in head/neck, cardiac, and thoracic procedures.
- Chow AW, Benninger MS, Brook I, et al. IDSA clinical practice guideline for acute bacterial rhinosinusitis in children and adults. Clin Infect Dis. 2012;54(8):e72-e112. doi:10.1093/cid/cis370IDSA sinusitis guideline listing cefuroxime as alternative for acute bacterial sinusitis in penicillin-allergic patients.
- Neu HC, Fu KP. Cefuroxime, a beta-lactamase-resistant cephalosporin with a broad spectrum of gram-positive and -negative activity. Antimicrob Agents Chemother. 1978;13(4):657-664. doi:10.1128/AAC.13.4.657Original characterisation of cefuroxime’s in vitro activity against 604 isolates demonstrating enhanced beta-lactamase stability vs first-generation cephalosporins.
- Sommers DK, Van Wyk M, Moncrieff J, Schoeman HS. Influence of food and reduced gastric acidity on the bioavailability of cefuroxime axetil. Br J Clin Pharmacol. 1984;18(4):535-539. doi:10.1111/j.1365-2125.1984.tb02501.xKey PK study demonstrating food-enhanced absorption and negative impact of reduced gastric acidity on cefuroxime axetil bioavailability.
- Scott LJ, Ormrod D, Goa KL. Cefuroxime axetil: an updated review of its use in the management of bacterial infections. Drugs. 2001;61(10):1455-1500. doi:10.2165/00003495-200161100-00008Comprehensive PK and clinical review covering oral and IV cefuroxime formulations, bioavailability data, and clinical trial efficacy across all approved indications.
- Foord RD. Cefuroxime: human pharmacokinetics. Antimicrob Agents Chemother. 1976;9(5):741-747. doi:10.1128/AAC.9.5.741Foundational human PK study in 44 volunteers establishing cefuroxime serum half-life (~70 min), protein binding (33%), and urinary recovery (≥95%) after IM and IV doses.