CEFTIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CEFTIN (CEFTIN).
Ceftin (cefuroxime axetil) is a second-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), specifically transpeptidases, thereby disrupting peptidoglycan cross-linking. This leads to cell lysis and death primarily during active cell division.
| Metabolism | Cefuroxime axetil is a prodrug that is de-esterified to active cefuroxime during absorption. Cefuroxime undergoes minimal hepatic metabolism; the majority is excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Renal: 80-90% unchanged via glomerular filtration and tubular secretion; biliary/fecal: <5%. |
| Half-life | Terminal elimination half-life: 1-2 hours (normal renal function); prolonged to 15-20 hours in severe renal impairment (CrCl <10 mL/min). |
| Protein binding | 33-50% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 0.2-0.3 L/kg; indicating distribution primarily into extracellular fluid; penetrates well into pleural fluid and soft tissues. |
| Bioavailability | Oral: 30-50% (as cefuroxime axetil, enhanced by food); IM: ~100%. |
| Onset of Action | Intravenous: immediate; oral: variable, absorption fast with peak concentrations at 1-2 hours, clinical effect within 2-4 hours. |
| Duration of Action | Duration 8-12 hours after oral or intravenous administration; sustained levels in pleural fluid, bones, and soft tissues. |
| Action Class | Cephalosporins: 1st generation |
| Brand Substitutes | Sudrox 500mg Capsule, Nesdrox 500mg Capsule, Gadroxil 500mg Capsule, Kefloxin 500mg Capsule, PD Roxil 500mg Capsule, Cfd 250mg Capsule, Cefcare 250mg Capsule, Cefaxone 0.5gm Injection, Keftra 500mg Injection, Retel 500mg Injection, Trixon 500mg Injection, Oframax 500mg Injection, Xone Hospital 1000mg Injection, Ritecef 1000mg Injection, Cefaxone 1gm Injection, Trixon 1000mg Injection, Ceftrax 1000mg Injection, Ceftril 250mg Injection, Nosocef 250mg Injection, Trixon 250mg Injection, Ramcef 250mg Injection, Powercef 250mg Injection |
250-500 mg orally twice daily for 10 days; for community-acquired pneumonia, 500 mg twice daily for 10 days. Intravenous: 750-1500 mg every 8 hours.
| Dosage form | FOR SUSPENSION |
| Renal impairment | CrCl >30 mL/min: no adjustment. CrCl 10-30 mL/min: 250-500 mg every 24 hours. CrCl <10 mL/min: 250 mg every 24 hours. Hemodialysis: 250 mg every 24 hours, dose after dialysis. |
| Liver impairment | No dose adjustment required for hepatic impairment. No specific Child-Pugh guidelines exist. |
| Pediatric use | Children >3 months: 20-30 mg/kg/day orally divided every 12 hours (max 1 g/day). For acute otitis media: 30 mg/kg/day divided every 12 hours. Intravenous: 50-200 mg/kg/day divided every 6-8 hours (max 6 g/day). |
| Geriatric use | No specific adjustment based on age alone. Dose adjustment based on renal function; CrCl may be reduced in elderly. Consider lower end of dosing range and monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CEFTIN (CEFTIN).
| Breastfeeding | Excreted in breast milk in low concentrations (M/P ratio not reported; estimated 0.1-0.5). Considered compatible with breastfeeding by AAP. Monitor infant for diarrhea, rash, and candidiasis. |
| Teratogenic Risk | Pregnancy category B. No evidence of teratogenicity in animal studies; however, inadequate human data. Cefuroxime crosses the placenta. Use only if clearly needed, especially in first trimester. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to cefuroxime, any component of the formulation, or other cephalosporins.","Hypersensitivity to penicillins (potential cross-sensitivity); avoid in patients with immediate-type hypersensitivity reactions to penicillins.","Absolute contraindication: history of severe anaphylactic reaction to any beta-lactam antibiotic."]
| Precautions | ["Hypersensitivity reactions, including anaphylaxis, have been reported; cross-allergenicity with penicillins and other beta-lactams exists.","Clostridioides difficile-associated diarrhea (CDAD) may occur; consider if diarrhea develops during or after therapy.","Prolonged use may result in superinfection with non-susceptible organisms (e.g., Candida, Clostridium difficile).","Use with caution in patients with a history of gastrointestinal disease, particularly colitis.","Renal impairment requires dose adjustment; monitor renal function in elderly patients or those receiving high doses.","Direct Coombs test positivity has been reported (may interfere with crossmatching).","Seizures have been reported with cephalosporins, especially in patients with renal impairment or those receiving high doses.","Safety and efficacy in infants <3 months have not been established."] |
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| Standard prenatal monitoring; no specific fetal monitoring required. Monitor maternal renal function if prolonged therapy. Assess for hypersensitivity reactions. |
| Fertility Effects | No known adverse effects on human fertility based on limited data. Animal studies show no impairment of fertility at therapeutic doses. |
| Food/Dietary |
| Take with food or milk to enhance absorption (increases bioavailability by ~50%). Avoid alcohol during therapy and for 72 hours after completion to prevent disulfiram-like reaction. No other significant food interactions. |
| Clinical Pearls | Ceftin (cefuroxime axetil) is a second-generation cephalosporin with activity against many gram-positive and gram-negative organisms. It is prodrug; take with food to enhance absorption. Dose adjustment needed for CrCl <30 mL/min. Not active against MRSA, Enterococcus, or Pseudomonas. May cause false-positive urine glucose test with Clinitest but not with glucose oxidase methods. Disulfiram-like reaction possible if alcohol consumed within 72 hours. Use with caution in penicillin allergy (cross-reactivity ~5-10%). |
| Patient Advice | Take exactly as prescribed; complete full course even if you feel better. · Take with food to increase absorption and reduce stomach upset. · Shake oral suspension well before each use. Store reconstituted suspension in refrigerator; discard after 10 days. · Avoid alcohol during treatment and for at least 72 hours after last dose to prevent disulfiram-like reaction (nausea, vomiting, flushing). · Notify doctor if you experience severe diarrhea, rash, or signs of allergic reaction. · May cause false-positive urine glucose test; inform healthcare provider if you have diabetes. · If you miss a dose, take it as soon as remembered unless it's almost time for next dose; do not double dose. |