CEFUROXIME
Clinical safety rating: safe
Human studies have proved safety
Cefuroxime is a second-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), disrupting peptidoglycan cross-linking and leading to cell lysis.
| Metabolism | Cefuroxime is not metabolized significantly; it is excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Renal excretion of unchanged drug accounts for 80-90% of elimination via glomerular filtration and tubular secretion; biliary/fecal excretion is minimal (<10%). |
| Half-life | Terminal elimination half-life is 1.2 hours in adults with normal renal function (increased to 15-22 hours in severe renal impairment [CrCl <10 mL/min], requiring dose adjustment). |
| Protein binding | 50% bound to serum albumin. |
| Volume of Distribution | 0.2-0.3 L/kg, reflecting distribution primarily into extracellular fluid; low intracellular penetration. |
| Bioavailability | Oral (cefuroxime axetil): 30-50% (increased to 60-70% with food). Intramuscular: 100%. |
| Onset of Action | Intravenous: Immediate (within minutes). Intramuscular: 15-30 minutes. Oral: 1-2 hours (due to conversion to active form). |
| Duration of Action | Intravenous/Intramuscular: 6-8 hours (dose-dependent, sufficient for 8-hour dosing intervals). Oral: 8-12 hours (based on twice-daily dosing for most infections). |
| Molecular Weight | 424.38 |
250-500 mg orally twice daily; 750 mg-1.5 g IV/IM every 8 hours for moderate infections; 1.5 g IV/IM every 8 hours for severe infections.
| Dosage form | Injectable |
| Renal impairment | CrCl 30-50 mL/min: same dose every 12 hours; CrCl 15-29 mL/min: same dose every 24 hours; CrCl <15 mL/min: 250-500 mg orally every 24 hours or 750 mg IV every 24 hours; hemodialysis: 750 mg IV after each dialysis. |
| Liver impairment | No adjustment required for mild to moderate hepatic impairment. Not studied in severe impairment; use with caution. |
| Pediatric use | Oral: 125-250 mg twice daily for 10 days for pharyngitis; IV/IM: 50-100 mg/kg/day divided every 6-8 hours, max 1.5 g every 8 hours. |
| Geriatric use | Elderly patients may have reduced renal function; adjust dose based on creatinine clearance. No specific age-related dose adjustment beyond renal considerations. |
| 1st trimester | Cefuroxime crosses the placenta. Animal studies do not indicate teratogenic effects. Human data from a large number of pregnancies have not shown an increased risk of major malformations. Use if clearly needed. |
| 2nd trimester | Similar to T1. No evidence of fetal harm. Considered safe for use in treating maternal infections. |
| 3rd trimester | Similar to T1. Use if clinically indicated. No known adverse fetal effects. |
Clinical note
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
| Placental transfer | Cefuroxime crosses the placenta readily. Detectable levels in fetal blood and amniotic fluid have been reported, approximately 30-50% of maternal serum concentrations. |
| Breastfeeding | Cefuroxime is excreted into breast milk in low concentrations. It is generally considered compatible with breastfeeding. The small amount ingested is unlikely to cause adverse effects in the infant. Monitor for potential gastrointestinal disturbances (e.g., diarrhea, thrush). |
■ FDA Black Box Warning
No FDA black box warning is issued for cefuroxime.
| Common Effects | Diarrhea |
| Serious Effects |
Hypersensitivity to cefuroxime or any cephalosporinImmediate-type hypersensitivity reaction to penicillins (severe anaphylaxis)
| Precautions | Hypersensitivity reactions including anaphylaxis, especially in patients with penicillin or cephalosporin allergy., Clostridioides difficile-associated diarrhea (CDAD) ranging from mild diarrhea to fatal colitis., Seizures may occur with high doses or in patients with renal impairment., Increased risk of bleeding due to interference with vitamin K synthesis (rare)., Prolonged use may result in superinfection with resistant organisms. |
| Food/Dietary | Cefuroxime axetil absorption is enhanced by food; take with meals or a snack. Avoid alcohol during therapy and for 72 hours after completion to reduce risk of disulfiram-like reaction (though less common with cephalosporins). |
Loading safety data…
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | In first trimester, no increased risk of major malformations observed in human studies; animal studies show no teratogenicity. Second and third trimesters, no known fetal harm, but use only if clearly needed. |
| Fetal Monitoring | Monitor maternal renal function, signs of hypersensitivity, and superinfection. For prolonged use, monitor fetal growth if used in pregnancy. |
| Fertility Effects | No adverse effects on fertility reported in animal studies; human data not available. |
| Clinical Pearls | Administer cefuroxime axetil with food to enhance absorption; avoid IM injection in neonates due to risk of sterile abscess formation; monitor renal function in elderly and adjust dosing if CrCl <30 mL/min; cefuroxime can cause false positive urine glucose tests with Clinitest but not with glucose oxidase methods; use with caution in penicillin-allergic patients due to cross-sensitivity (~10%). |
| Patient Advice | Take this medication exactly as prescribed, even if symptoms improve. · For the oral tablet (cefuroxime axetil), take with food to improve absorption. · Do not crush or chew the oral suspension; shake well before use. · Complete the full course of treatment to prevent bacterial resistance. · Contact your healthcare provider if you develop severe diarrhea, rash, or signs of an allergic reaction. |