CEFUROXIME AXETIL
Clinical safety rating: safe
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
Cefuroxime axetil is a prodrug that is hydrolyzed to cefuroxime, a second-generation cephalosporin antibiotic. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation and disrupting peptidoglycan cross-linking.
| Metabolism | Cefuroxime axetil is de-esterified by nonspecific esterases in the intestinal mucosa and plasma to cefuroxime, which is not further metabolized. |
| Excretion | Renal: 70-90% unchanged by glomerular filtration and tubular secretion; biliary/fecal: <10% |
| Half-life | 1.2-1.6 hours (normal renal function); prolonged to 15-22 hours in end-stage renal disease (CrCl <10 mL/min). For oral cefuroxime axetil, consider absorption and conversion to active cefuroxime. |
| Protein binding | 33-50% (primarily albumin) |
| Volume of Distribution | 0.2-0.3 L/kg (suggests distribution primarily into extracellular fluid; clinical meaning: low Vd indicates limited tissue penetration, consistent with hydrophilic properties) |
| Bioavailability | Oral: 30-40% (cefuroxime axetil); absorption enhanced with food (up to 50-60%); IM: 100% (as cefuroxime sodium) |
| Onset of Action | Oral: 2-3 hours (time to peak serum concentration); IM: 1-2 hours (time to peak serum concentration); IV: immediate (peak concentration at end of infusion) |
| Duration of Action | Approximately 8-12 hours for susceptible pathogens (based on MIC and dosing interval); clinical duration depends on infection site and host factors. |
| Molecular Weight | 510.47 Da |
250–500 mg orally twice daily; for severe infections (e.g., pneumonia), 500 mg twice daily; for uncomplicated urinary tract infections, 250 mg twice daily; for Lyme disease, 500 mg twice daily for 20 days.
| Dosage form | TABLET |
| Renal impairment | CrCl >30 mL/min: no adjustment; CrCl 10–30 mL/min: 250 mg every 24 hours; CrCl <10 mL/min: 250 mg every 48 hours. |
| Liver impairment | No dosage adjustment required for hepatic impairment; no specific Child-Pugh based recommendations available. |
| Pediatric use | Children 3 months to 12 years: 20–30 mg/kg/day orally in two divided doses (max 500 mg per dose); for acute otitis media or pharyngitis, 30 mg/kg/day in two divided doses; for older children (>12 years), adult dosing applies. |
| Geriatric use | No specific dose adjustment based solely on age; adjust for renal function as per creatinine clearance; monitor for increased risk of adverse effects (e.g., diarrhea) due to age-related renal decline. |
| 1st trimester | Cefuroxime axetil crosses the placenta. Animal studies show no evidence of teratogenicity, but human data are limited. Use only if clearly needed. |
| 2nd trimester | Cephalosporins are considered safe in pregnancy. No known risk of fetal harm. |
| 3rd trimester | Cefuroxime axetil is safe to use in the third trimester. No known adverse effects on the fetus. |
Clinical note
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
| FDA category | Human |
| Placental transfer | Cefuroxime axetil crosses the placenta. Cord blood concentrations are approximately 20-30% of maternal serum levels. |
| Breastfeeding |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Diarrhea |
| Serious Effects |
Hypersensitivity to cefuroxime or any cephalosporin antibioticPrevious immediate hypersensitivity reaction to a penicillin (risk of cross-reactivity)
| Precautions | Hypersensitivity reactions (including anaphylaxis) in patients with penicillin or other beta-lactam allergy., Clostridioides difficile-associated diarrhea (CDAD)., Potential for superinfection with prolonged use., Caution in patients with renal impairment (dose adjustment required)., False-positive urine glucose test (Clinitest) and direct Coombs test. |
| Food/Dietary | Administration with food (especially a fatty meal) significantly increases bioavailability (up to 50% increase in AUC). Avoid grapefruit juice (moderate CYP3A4 interaction); separate by at least 4 hours. No specific restrictions with dairy. |
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| Cefuroxime is excreted into breast milk in low concentrations. It is generally considered compatible with breastfeeding due to minimal oral bioavailability in infants. However, monitor for possible diarrhea or rash in the infant. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | Cefuroxime axetil is FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects. There are no adequate and well-controlled studies in pregnant women. However, as a cephalosporin, it is generally considered low risk. No structural anomalies have been consistently associated with first trimester exposure. Second and third trimester use is not associated with fetal toxicity. Theoretical risk of disruption of fetal gut flora leading to diarrhea or candidiasis is minimal. |
| Fetal Monitoring | Monitor for signs of hypersensitivity (rash, urticaria, anaphylaxis) in the mother. No specific fetal monitoring is required for cefuroxime axetil use. However, if used for prolonged periods or for serious infections, standard maternal infection monitoring applies. Neonatal monitoring for diarrhea or candidiasis is not routinely needed but can be considered if maternal use is high dose or near term. |
| Fertility Effects | No adverse effects on fertility or reproduction have been reported in animal studies or human data. Cefuroxime axetil is not known to impair fertility in males or females. |
| Clinical Pearls | Cefuroxime axetil is a second-generation cephalosporin with beta-lactamase stability. Its ester prodrug formulation enhances oral absorption. Administer with food to increase bioavailability. Monitor for hypersensitivity reactions, especially in penicillin-allergic patients (cross-reactivity ~5-10%). Not effective against MRSA, Enterococcus, or Pseudomonas. Adjust dose in renal impairment (CrCl <30 mL/min: give every 24 hours). May cause false positive urine glucose test with copper-reducing methods (e.g., Clinitest). |
| Patient Advice | Take exactly as prescribed; complete the full course even if you feel better. · Take with food or milk to improve absorption and reduce stomach upset. · Shake the oral suspension well before each use; measure dose with the provided device. · Report any signs of allergy: rash, itching, swelling, or difficulty breathing. · Notify your doctor if you develop severe diarrhea, especially if watery or bloody, as this may indicate C. difficile infection. · Cefuroxime may interfere with certain lab tests (e.g., urine glucose); inform healthcare providers you are taking this medication. |