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. |
| Molecular Weight | 446.37 |
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 | Generally considered safe; no evidence of teratogenicity in animal studies; use only if clearly needed. |
| 2nd trimester | Safe; similar to t1; no known risk. |
| 3rd trimester | Safe; no known risk. |
Clinical note
Comprehensive clinical and safety monograph for ZINACEF (ZINACEF).
| Placental transfer | Crosses placenta; achieves therapeutic levels in fetal serum. |
| Breastfeeding | Excreted in human milk in small amounts; unlikely to cause adverse effects in infant; use with caution. |
| Lactation Rating | L2 |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to cefuroxime or any cephalosporinPrevious immediate hypersensitivity reaction to penicillins
| 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 |
| Food/Dietary | Take with food or milk to increase absorption and minimize GI side effects. Avoid alcohol: may cause disulfiram-like reaction (flushing, headache, nausea). No significant interactions with specific foods. |
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| 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. |
| 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. |
| Clinical Pearls | ZINACEF (cefuroxime axetil) is a second-generation cephalosporin with activity against β-lactamase-producing strains. Administer with food to enhance absorption. For acute otitis media, use higher dose (500 mg BID) in children. In suspected penicillin allergy, cross-reactivity risk is low (<5%) but caution advised. Do not use in patients with cephalosporin anaphylaxis. Monitor renal function in elderly; adjust dose if CrCl <30 mL/min. |
| Patient Advice | Take this medication exactly as prescribed, with food to improve absorption and reduce stomach upset. · Complete the full course even if you feel better to prevent antibiotic resistance. · Notify your doctor if you develop severe diarrhea, rash, or signs of allergic reaction (difficulty breathing, swelling). · Avoid alcohol during treatment and for 48 hours after finishing to prevent disulfiram-like reactions. · Do not chew or crush tablets; swallow whole. |