ZINACEF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZINACEF (ZINACEF).
Cefuroxime, a second-generation cephalosporin, inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), disrupting peptidoglycan cross-linking.
| Metabolism | Cefuroxime is not metabolized; eliminated renally as unchanged drug via glomerular filtration and tubular secretion. |
| Excretion | Renal: 80-95% unchanged via glomerular filtration and tubular secretion; biliary: 5-10% excreted in feces; fecal: negligible. |
| Half-life | Terminal elimination half-life: 1.5-2 hours in adults with normal renal function; prolonged to 2.5-3.5 hours in elderly and up to 48 hours in end-stage renal disease. |
| Protein binding | 33-50%, primarily to serum albumin. |
| Volume of Distribution | 0.3-0.7 L/kg, indicating distribution primarily into extracellular fluid; Vd increases in neonates and critically ill patients. |
| Bioavailability | Intramuscular: approximately 98% bioavailable; oral: not applicable (no oral formulation). |
| Onset of Action | Intravenous (IV): immediate (within minutes). Intramuscular (IM): 15-30 minutes after injection. |
| Duration of Action | Duration: 6-8 hours for IM/IV administration, allowing twice-daily dosing for most infections; prolonged in renal impairment. |
750 mg IV/IM every 8 hours; for severe infections: 1.5 g IV every 8 hours; for life-threatening infections: 1.5 g IV every 6 hours
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 10-30 mL/min: 750 mg every 12 hours; CrCl <10 mL/min: 750 mg every 24 hours; hemodialysis: 750 mg after each dialysis session |
| Liver impairment | No specific Child-Pugh based adjustments; no dose adjustment required in hepatic impairment |
| Pediatric use | 3 months to 12 years: 50-100 mg/kg/day IV/IM divided every 6-8 hours; maximum 6 g/day; for meningitis: 200-240 mg/kg/day IV divided every 6-8 hours |
| Geriatric use | Dose adjustment based on renal function; no age-specific adjustments except for renal impairment |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZINACEF (ZINACEF).
| Breastfeeding | Cefuroxime is excreted into breast milk in small amounts (M/P ratio approximately 0.25-0.4). Infant dose is <1% of therapeutic dose. Considered compatible with breastfeeding; monitor infant for diarrhea, candidiasis, or allergic reaction. |
| Teratogenic Risk | ZINACEF (cefuroxime) is classified as FDA Pregnancy Category B. No evidence of teratogenicity in animal studies. Inadequate human studies; however, cephalosporins are generally considered low risk. Risk to fetus cannot be ruled out, but potential benefits may warrant use in pregnant women when clinically indicated. First trimester use is not associated with major malformations; caution in second and third trimesters due to theoretical risk of kernicterus. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Known hypersensitivity to cefuroxime or any component of the formulation","Hypersensitivity to other cephalosporins","Severe immediate hypersensitivity reaction (e.g., anaphylaxis) to penicillins or other beta-lactam antibiotics"]
| Precautions | ["Hypersensitivity reactions (including anaphylaxis) in patients with penicillin or other beta-lactam allergies","Clostridioides difficile-associated diarrhea (CDAD) ranging from mild diarrhea to fatal colitis","Potential for superinfection with prolonged use","Seizures may occur with high doses or renal impairment","Hematologic effects (e.g., neutropenia, agranulocytosis, thrombocytopenia) with prolonged therapy","Renal function monitoring in patients with pre-existing renal impairment or receiving nephrotoxic drugs"] |
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| Fetal Monitoring | Monitor maternal renal function and complete blood count during prolonged therapy. Fetal monitoring as per standard obstetric care; no specific fetal monitoring required beyond routine antenatal surveillance. |
| Fertility Effects | No known adverse effects on fertility in animal studies. No human data on fertility impairment. |