cefuroxime axetil
Ceftin

cefuroxime sodium
Kefurox, Zinacef

Available forms
Available by prescription only
cefuroxime axetil
Suspension: 125 mg/5 ml, 250 mg/5 ml
Tablets (film-coated): 125 mg, 250 mg, 500 mg
cefuroxime sodium
Infusion: 750 mg, 1.5-g infusion packets
Injection: 750 mg, 1.5 g, 7.5 g

Indications and dosages
 Serious lower respiratory, urinary tract, skin, and skin-structure infections; bone and joint infections; septicemia; meningitis caused by susceptible organisms. Adults: Usual dosage is 750 mg to 1.5 g I.M. or I.V. q 8 hours for 5 to 10 days. For life-threatening infections and infections caused by less susceptible organisms, 1.5 g I.M. or I.V. q 6 hours; for bacterial meningitis, up to 3 g I.V. q 8 hours.
Children and infants older than age 3 months: 50 to 100 mg/kg I.M. or I.V. daily in divided doses q 6 to 8 hours. Some clinicians give 100 to 150 mg/kg daily. For meningitis, the usual starting dosage is 200 to 240 mg/kg I.V. daily in divided doses q 6 to 8 hours, reduced to 100 mg/kg daily when clinical improvement occurs. However, some clinicians prefer other agents for meningitis.
 Total daily dose is same for I.M. and I.V. administration and depends on susceptibility of organism and severity of infection. Inject cefuroxime deep I.M. into a large muscle mass, such as the gluteus or lateral aspect of the thigh.
 Pharyngitis, tonsillitis, lower respiratory tract infection, urinary tract infection. Adults and children older than age 12: 125 to 500 mg P.O. b.i.d. for 10 days.
Children younger than age 12 who can swallow pills: 125 to 250 mg P.O. b.i.d. (tablets) for 10 days.
Children ages 3 months to 12 years: 20 mg/kg P.O. daily in divided doses b.i.d. (oral suspension) to maximum dose of 500 mg for 10 days.
 Otitis media, impetigo. Children ages 3 months to 12 years: 30 mg/kg P.O. oral suspension daily divided into two doses (maximum dose is 1 g) for 10 days.
Children who can swallow pills: 250 mg P.O. b.i.d. for 10 days.
 Perioperative prophylaxis. Adults: 1.5 g I.V. 30 to 60 minutes before surgery; then 750 mg I.M. or I.V. q 8 hours intraoperatively for a prolonged procedure. Open-heart surgery patients can receive 1.5 g I.V. at induction, then q 12 hours for a total of 6 g.
 Gonorrhea (urethral, endocervical, rectal). Adults: 1.5 g I.M. as a single dose, alone or with other antibiotics.
 Lyme disease (erythema migrans) caused by Adults and children age 13 and older: 500 mg P.O. b.i.d. for 20 days.
≡ Dosage adjustment. Safety of drug in patients with renal impairment hasn’t been established. In patients with impaired renal function, dose or frequency of administration must be modified based on degree of renal impairment, severity of infection, and susceptibility of organism. To prevent toxic accumulation, reduced I.M. or I.V. dosage may be required. For patients with creatinine clearance of 10 to 20 ml/ minute, give 750 mg q 12 hours. For those with creatinine clearance below 10 ml/minute, give 750 mg q 24 hours. For hemodialysis patients, give 750 mg at end of each dialysis period in addition to regular dose.

Pharmacodynamics
Antibacterial action: Cefuroxime is primarily bactericidal; it also may be bacteriostatic. Activity depends on the organism, tissue penetration, dosage, and rate of organism multiplication. It acts by adhering to bacterial penicillin-binding proteins, thereby inhibiting cell wall synthesis.
  Cefuroxime is active against many gram-positive organisms and enteric gram-negative bacilli, including Streptococcus pneumoniae and S. pyogenes, Haemophilus influenzae, Klebsiella species, Staphylococcusaureus, Escherichia coli, Enterobacter, and Neisseria gonorrhoeae; Bacteroides fragilis, Pseudomonas, and Acinetobacter species are resistant to cefuroxime.

Pharmacokinetics
Absorption: Cefuroxime sodium isn’t well absorbed from the GI tract and must be given parenterally. Cefuroxime axetil is better absorbed orally; between 37% and 52% of an oral dose is absorbed. Food appears to enhance absorption.
Distribution: Distributed widely into most body tissues and fluids, including the gallbladder, liver, kidneys, bone, bile, and pleural and synovial fluids; CSF penetration is greater than that of most first- and second-generation cephalosporins and achieves adequate therapeutic levels in inflamed meninges. Cefuroxime crosses the placental barrier and is 33% to 50% protein-bound.
Metabolism: Not metabolized.
Excretion: Primarily excreted in urine by renal tubular secretion and glomerular filtration; elimination half-life is 1 to 2 hours in patients with normal renal function; end-stage renal disease prolongs half-life 15 to 22 hours. Some drug appears in breast milk. Hemodialysis removes cefuroxime.

Contraindications and precautions
Contraindicated in patients hypersensitive to cefuroxime or other cephalosporins. Use cautiously in breast-feeding women and in patients with impaired renal function or penicillin allergy.

Interactions
Drug-drug. Aminoglycosides: Produces synergistic activity against some organisms; increases risk of nephrotoxicity. Monitor patient closely.
Diuretics: Increases risk of adverse effects. Monitor patient closely.
Probenecid: Competitively inhibits renal tubular secretion of cephalosporins, resulting in higher, prolonged serum levels of these drugs. Sometimes used for this effect.
Drug-food. Any food: Increases absorption. Advise patient to take drug with food.

Adverse reactions
CV: phlebitis, thrombophlebitiswith I.V. injection.
GI: pseudomembranous colitis, nausea, anorexia, vomiting, diarrhea.
Hematologic: transient neutropenia, eosinophilia, hemolytic anemia, thrombocytopenia, decreased hemoglobin and hematocrit.
Skin: maculopapular and erythematous rash, urticaria, pain, induration, sterile abscesses, temperature elevation, tissue sloughingat injection site.
Other: hypersensitivity reactions (serum sickness, anaphylaxis).

Effects on lab test results
• May increase ALT, AST, alkaline phosphatase, bilirubin, and LDH levels.
• May increase PT, INR, and eosinophil count. May decrease hemoglobin, hematocrit, and neutrophil and platelet counts.

Overdose and treatment
Overdose may cause neuromuscular hypersensitivity. Seizures may follow high CNS levels.
 Hemodialysis or peritoneal dialysis will remove cefuroxime.

Special considerations
 ALERT Names of some cephalosporins are similar. Use caution when prescribing.
• Tablets and suspension aren’t bioequivalent and can’t be substituted on a milligram-per-milligram basis.
• Compliance may be a problem when treating otitis media in children. Order suspension form if child is unable to swallow pills.
• For patients on sodium restriction, note that cefuroxime sodium contains 2.4 mEq of sodium per gram of drug.
• Check solutions for particulate matter and discoloration. Solution may range in color from light yellow to amber without affecting potency.
• Shake I.M. solution gently before administration to ensure complete drug dissolution. Give deep into a large muscle mass, preferably the gluteus area. Aspirate before injecting to prevent inadvertent injection into a blood vessel. Rotate injection sites to prevent tissue damage. Ice to injection site may relieve pain.
• For direct intermittent I.V., inject solution slowly into vein over 3 to 5 minutes or slowly through tubing of free-running, compatible I.V. solution.
• Reconstituted solution retains potency for 24 hours at room temperature or for 48 hours if refrigerated.
• Because drug is hemodialyzable, patients undergoing treatment with hemodialysis or peritoneal dialysis may require dosage adjustments.
• Reconstituted suspension can be stored at room temperature or in refrigerator. Discard unused portion after 10 days. Shake well before each dose.
• Drug causes false-positive results in urine glucose tests using cupric sulfate (Benedict’s reagent or Clinitest); use glucose oxidase tests (Chemstrip uG, Diastix, or glucose enzymatic test strip) instead. Cefuroxime also causes false elevations in serum or urine creatinine levels in tests using Jaffe reaction. Cefuroxime may cause positive Coombs’ test results.
• With large doses or prolonged therapy, monitor patient for superinfection, especially if high-risk.
• Monitor renal function during therapy, especially when maximum dose is used in a severely ill patient.
Breast-feeding patients
• Drug appears in breast milk; use cautiously in breast-feeding women.
Pediatric patients
• Safety in infants younger than age 3 months hasn’t been established.
Geriatric patients
• Use cautiously in elderly patients.

Patient education
• Inform patient of potential adverse reactions.
• Patient should report discomfort at I.V. site.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use