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). |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
| Breastfeeding | Cefuroxime is excreted in human milk in small amounts (M/P ratio ~0.03–0.05); considered compatible with breastfeeding due to low oral bioavailability in infants. Monitor infant for diarrhea or rash. |
| 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 |
■ FDA Black Box Warning
No FDA black box warning is issued for cefuroxime.
| Common Effects | Diarrhea |
| Serious Effects |
["Hypersensitivity to cefuroxime or any cephalosporin antibiotic.","Contraindicated in patients with known anaphylactic reaction to penicillins (cross-sensitivity may occur)."]
| 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 |
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| 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. |
| 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). |
| 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. |