No

Antibiotic, Cephalosporin (Second Generation)

Treatment of infections caused by staphylococci, group B streptococci, H. influenzae (type A and B), E. coli, Enterobacter, Salmonella, and Klebsiella; treatment of susceptible infections of the lower respiratory tract, otitis media, urinary tract, skin and soft tissue, bone and joint, sepsis and gonorrhea

B

Hypersensitivity to cefuroxime, any component, or cephalosporins

Modify dosage in patients with severe renal impairment, prolonged use may result in superinfection; use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, urticaria); may cause antibiotic-associated colitis or colitis secondary to C. difficile

1% to 10%:

Hematologic: Eosinophilia (7%), decreased hemoglobin and hematocrit (10%)

Hepatic: Increased transaminases (4%), increased alkaline phosphatase (2%)

Local: Thrombophlebitis (1.7%)

<1%: Anaphylaxis, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, interstitial nephritis, dizziness, fever, headache, rash, nausea, vomiting, diarrhea, stomach cramps, GI bleeding, colitis, neutropenia, leukopenia, increased creatinine, increased BUN, pain at injection site, vaginitis, seizures, angioedema, pseudomembranous colitis

Other reactions with cephalosporins include toxic nephropathy, cholestasis, agranulocytosis, colitis, pancytopenia, aplastic anemia, hemolytic anemia, hemorrhage, prolonged PT, encephalopathy, asterixis, neuromuscular excitability, serum-sickness reactions, superinfection

After acute overdose, most agents cause only nausea, vomiting, and diarrhea, although neuromuscular hypersensitivity and seizures are possible, especially in patients with renal insufficiency; many beta-lactam antibiotics have the potential to cause neuromuscular hyperirritability or seizures

Hemodialysis may be helpful to aid in the removal of the drug from the blood but not usually indicated, otherwise most treatment is supportive or symptom directed following GI decontamination

Increased effect: High-dose probenecid decreases clearance

Increased toxicity: Aminoglycosides increase nephrotoxic potential

Reconstituted solution is stable for 24 hours at room temperature and 48 hours when refrigerated; I.V. infusion in NS or D₅W solution is stable for 24 hours at room temperature, 7 days when refrigerated, or 26 weeks when frozen; after freezing, thawed solution is stable for 24 hours at room temperature or 21 days when refrigerated

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

Absorption: Oral (cefuroxime axetil): Increased when given with or shortly after food or infant formula (37% to 52%)

Distribution: Widely distributed to body tissues and fluids; crosses blood-brain barrier; therapeutic concentrations achieved in CSF even when meninges are not inflamed; crosses placenta and reaches breast milk

Protein binding: 33% to 50%

Bioavailability, axetil: Oral: 37% to 52%

Half-life:

Neonates: less than or equal to 3 days: 5.1-5.8 hours; 6-14 days: 2-4.2 hours; 3-4 weeks: 1-1.5 hours

Adults: 1-2 hours (prolonged in renal impairment)

Time to peak serum concentration: I.M.: Within 15-60 minutes

Elimination: Primarily excreted 66% to 100% as unchanged drug in urine by both glomerular filtration and tubular secretion

Children:

Pharyngitis, tonsillitis: Oral:

Suspension: 20 mg/kg/day (maximum: 500 mg/day) in 2 divided doses

Tablet: 125 mg every 12 hours

Acute otitis media, impetigo: Oral:

Suspension: 30 mg/kg/day (maximum: 1 g/day) in 2 divided doses

Tablet: 250 mg every 12 hours

I.M., I.V.: 75-150 mg/kg/day divided every 8 hours; maximum dose: 6 g/day

Meningitis: Not recommended (doses of 200-240 mg/kg/day divided every 6-8 hours have been used); maximum dose: 9 g/day

Adults:

Oral: 250-500 mg twice daily; uncomplicated urinary tract infection: 125-250 mg every 12 hours

I.M., I.V.: 750 mg to 1.5 g/dose every 8 hours or 100-150 mg/kg/day in divided doses every 6-8 hours; maximum: 6 g/24 hours

Dosing adjustment in renal impairment:

Cl_cr 10-20 mL/minute: Administer every 12 hours

Cl_cr <10 mL/minute: Administer every 24 hours

Hemodialysis: Dialyzable (25%)

Note: Cefuroxime axetil film-coated tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose as for Cl_cr 10-20 mL/minute

May be taken with food, however, bioavailability is increased with food

Observe for signs and symptoms of anaphylaxis during first dose; with prolonged therapy, monitor renal, hepatic, and hematologic function periodically

Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution), false-positive serum or urine creatinine with Jaffé reaction

May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins

May rarely cause neutropenia; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Take as directed, at regular intervals around-the-clock (with or without food). Chilling oral suspension improves flavor (do not freeze). Complete full course of medication, even if you feel better. Drink 2-3 L fluid/day. If diarrhea occurs, yogurt or buttermilk may help. May cause false-positive test with Clinitest®; use another form of testing. May interfere with oral contraceptives; additional contraceptive measures are necessary. Report severe, unresolved diarrhea; vaginal itching or drainage; sores in mouth; blood, pus, or mucus in stool or urine; easy bleeding or bruising; unusual fever or chills; rash; or respiratory difficulty. Breast-feeding precautions: Consult prescriber if breast-feeding.

Do not admix with aminoglycosides in same bottle/bag; obtain specimens for culture and sensitivity prior to the first dose

Infusion, as sodium, premixed (frozen) (Zinacef®): 750 mg (50 mL); 1.5 g (50 mL)

Powder for injection, as sodium: 750 mg, 1.5 g, 7.5 g

Powder for injection, as sodium (Kefurox®, Zinacef®): 750 mg, 1.5 g, 7.5 g

Powder for oral suspension, as axetil (tutti-frutti flavor) (Ceftin®): 125 mg/5 mL (50 mL, 100 mL, 200 mL); 250 mg/5 mL (50 mL, 100 mL)

Tablet, as axetil (Ceftin®): 125 mg, 250 mg, 500 mg

American Thoracic Society, "Guidelines for the Initial Management of Adults With Community-Acquired Pneumonia: Diagnosis Assessment of Severity and Initial Antimicrobial Therapy," Am Rev Respir Dis, 1993, 148(5):1418-26.

"Antimicrobial Prophylaxis in Surgery," Med Lett Drugs Ther, 1993, 35(906):91-4.

Broekhuysen J, Deger F, Douchamps J, et al, "Pharmacokinetic Study of Cefuroxime in the Elderly," Br J Clin Pharmacol, 1981, 21(6):801-5.

de Louvois J, Mulhall A, and Hurley R, "Cefuroxime in the Treatment of Neonates," Arch Dis Child, 1982, 57(1):59-62.

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Douglas JG, Bax RP, and Munro JF, "The Pharmacokinetics of Cefuroxime in the Elderly," J Antimicrob Chemother, 1980, 6(4):543-9.

Gentry LO, Zeluff BJ, and Cooley DA, "Antibiotic Prophylaxis in Open-Heart Surgery: A Comparison of Cefamandole, Cefuroxime, and Cefazolin," Ann Thorac Surg, 1988, 46(2):167-71.

Gooch WM 3rd, Blair E, Puopolo A, et al, "Effectiveness of Five Days of Therapy With Cefuroxime Axetil Suspension for Treatment of Acute Otitis Media," Pediatr Infect Dis J, 1996, 15(2):157-64.

Marshall WF and Blair JE, "The Cephalosporins," Mayo Clin Proc, 1999, 74(2):187-95.

Nelson JD, "Cefuroxime: A Cephalosporin With Unique Applicability to Pediatric Practice," Pediatr Infect Dis, 1983, 2(5):394-6.

Perry CM and Brogden RN, "Cefuroxime Axetil. A Review of Its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Efficacy," Drugs, 1996, 52(1):125-58.

Peterson CD, Lake KD, Arom KV, et al, "Antibiotic Prophylaxis in Open-Heart Surgery Patients: Comparison of Cefamandole and Cefuroxime," Drug Intell Clin Pharm, 1987, 21(9):728-32.

Thoene DE and Johnson CE, "Pharmacotherapy of Otitis Media," Pharmacotherapy, 1991, 11(3):212-21.