KEFUROX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KEFUROX (KEFUROX).
Cefuroxime inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting the final transpeptidation step of peptidoglycan synthesis, leading to cell lysis.
| Metabolism | Cefuroxime is not metabolized and is excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Primarily renal (80-90% unchanged via glomerular filtration and tubular secretion); biliary/fecal <10%. |
| Half-life | 1.2-1.6 hours in adults with normal renal function (Clcr >80 mL/min); prolonged to 10-20 hours in end-stage renal disease (Clcr <10 mL/min). |
| Protein binding | 50-60% (primarily to albumin). |
| Volume of Distribution | 0.16-0.23 L/kg (low Vd, consistent with limited extravascular distribution; primarily remains in extracellular fluid). |
| Bioavailability | IM: 100%; Oral: Not available (parenteral administration only). |
| Onset of Action | IV: Immediate (peak concentration at end of infusion); IM: 15-30 minutes; Oral: Not applicable (parenteral only). |
| Duration of Action | 6-8 hours for susceptible organisms; prolonged in renal impairment. Clinical effect persists ~12-24 hours in severe renal failure. |
| Molecular Weight | 424.39 |
750 mg to 1.5 g intramuscularly or intravenously every 8 hours; for severe infections, 1.5 g intravenously every 6 to 8 hours.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 50-20 mL/min: 750 mg every 12 hours; GFR 20-10 mL/min: 750 mg every 24 hours; GFR <10 mL/min: 750 mg every 48 hours; hemodialysis: 750 mg after each dialysis session. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment; Child-Pugh class C: no specific data, use with caution. |
| Pediatric use | Children 3 months to 18 years: 30-100 mg/kg/day intravenously divided every 6 to 8 hours; maximum 6 g/day. Neonates: 30-50 mg/kg/day intravenously divided every 8 to 12 hours based on gestational and postnatal age. |
| Geriatric use | Elderly patients: no specific dose adjustment, but dose selection should be cautious based on renal function; monitor renal function and adjust per renal adjustment guidelines. |
| 1st trimester | Category B: No evidence of risk in humans; animal studies show no fetal harm. Use only if clearly needed. |
| 2nd trimester | Category B: Similar to t1; caution advised. Cefuroxime crosses placenta with measurable fetal serum levels. |
| 3rd trimester | Category B: Use near term may lead to kernicterus in neonates due to bilirubin displacement; avoid if alternative available. |
Clinical note
Comprehensive clinical and safety monograph for KEFUROX (KEFUROX).
| Placental transfer | Crosses placenta; fetal serum concentrations reach 50-100% of maternal levels. |
| Breastfeeding | Cefuroxime is excreted into breast milk in small amounts (less than 1% of maternal dose). No adverse effects in nursing infants reported; considered compatible with breastfeeding. Monitor for diarrhea or rash in infant. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to cephalosporinsPrevious anaphylactic reaction to penicillins (risk of cross-sensitivity)
| Precautions | Serious hypersensitivity reactions (anaphylaxis) may occur, especially in patients with penicillin allergy., Clostridioides difficile-associated diarrhea (CDAD) can occur and may range from mild diarrhea to fatal colitis., Seizures may occur, especially in patients with renal impairment when doses are not reduced., Prolonged use may result in overgrowth of non-susceptible organisms. |
| Food/Dietary | Cefuroxime absorption is enhanced when taken with food. Avoid alcohol during treatment and for 48 hours after completing therapy to prevent disulfiram-like reaction (though rare with cephalosporins, caution is advised). No specific dietary restrictions; maintain adequate hydration. |
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| Lactation Rating |
| L1 (Safe) |
| Teratogenic Risk | No evidence of teratogenicity in animal studies. Insufficient human data; risk cannot be excluded. Use only if clearly needed during pregnancy. |
| Fetal Monitoring | No specific fetal monitoring required. Standard maternal monitoring for adverse effects (e.g., hypersensitivity, diarrhea). |
| Fertility Effects | No known adverse effects on fertility in animal or human studies. |
| Clinical Pearls | KEFUROX (cefuroxime) is a second-generation cephalosporin with activity against Gram-positive cocci (except MRSA and enterococci) and some Gram-negative bacilli including Haemophilus influenzae and Neisseria gonorrhoeae. It is renally eliminated; adjust dose in CrCl <30 mL/min. Administer with food to reduce GI upset. For serious infections, consider IV formulation due to incomplete oral absorption. Monitor for hypersensitivity reactions, especially in penicillin-allergic patients (cross-reactivity ~10%). Use with caution in patients with history of colitis. |
| Patient Advice | Take this medication exactly as prescribed; do not skip doses or stop early even if you feel better. · You may take cefuroxime with food to decrease stomach upset. · Complete the full course of therapy to prevent resistance. · Contact your healthcare provider if you experience severe diarrhea, rash, or difficulty breathing. · Inform your doctor if you have a penicillin allergy, kidney disease, or a history of colitis. · This medication may cause dizziness; avoid driving until you know how it affects you. |