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Medication Safety Issues
Sound-alike/look-alike issues:
Cefuroxime may be confused with cefotaxime, cefprozil, ceftizoxime, deferoxamine
Ceftin® may be confused with Cefzil®, Cipro®
Zinacef® may be confused with Zithromax®
International issues:
Ceftin® may be confused with Cefiton® which is a brand name for cefixime in Portugal
Ceftin® may be confused with Ceftina® which is a brand name for cefalotin in Mexico
Ceftin® may be confused with Ceftim® which is a brand name for ceftazidime in Italy
Pronunciation
(se fyoor OKS eem)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
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 upper and lower respiratory tract, otitis media, urinary tract, uncomplicated skin and soft tissue, bone and joint, sepsis, uncomplicated gonorrhea, and early Lyme disease; preoperative prophylaxis of susceptible infections
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events were not observed in animal studies; therefore, cefuroxime is classified as pregnancy category B. Cefuroxime crosses the placenta and reaches the cord serum and amniotic fluid. Placental transfer is decreased in the presence of oligohydraminios. Several studies have failed to identify a teratogenic risk to the fetus from maternal cefuroxime use. During pregnancy, mean plasma concentrations of cefuroxime are 50% lower, the AUC is 25% lower, and the plasma half-life is shorter than nonpregnant values. At term, plasma half-life is similar to nonpregnant values and peak maternal concentrations after I.M. administration are slightly decreased. Pregnancy does not alter the volume of distribution.
Lactation
Enters breast milk/use caution
Breast-Feeding Considerations
Cefuroxime is excreted in breast milk. Manufacturer recommendations vary; caution is recommended if cefuroxime I.V. is given to a nursing woman and it is recommended to consider discontinuing nursing temporarily during treatment following oral cefuroxime. Nondose-related effects could include modification of bowel flora.
Contraindications
Hypersensitivity to cefuroxime, any component of the formulation, or other cephalosporins
Warnings/Precautions
Concerns related to adverse effects:
• Elevated INR: May be associated with increased INR, especially in nutritionally-deficient patients, prolonged treatment, hepatic or renal disease.
• Penicillin allergy: Use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria).
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Renal impairment: Use with caution in patients with renal impairment; modify dosage in severe impairment.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
• Suspension/tablet bioequivalence: Tablets and oral suspension are not bioequivalent; do not substitute on a mg-per-mg basis.
Adverse Reactions
>10%: Gastrointestinal: Diarrhea (4% to 11%, duration-dependent)
1% to 10%:
Dermatologic: Diaper rash (3%)
Endocrine & metabolic: Alkaline phosphatase increased (2%), lactate dehydrogenase increased (1%)
Gastrointestinal: Nausea/vomiting (3% to 7%)
Genitourinary: Vaginitis (?5%)
Hematologic: Eosinophilia (7%), hemoglobin and hematocrit decreased (10%)
Hepatic: Transaminases increased (2% to 4%)
Local: Thrombophlebitis (2%)
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Anaphylaxis, angioedema, BUN increased, chest pain, cholestasis, colitis, creatinine increased, dyspnea, erythema multiforme, fever, GI bleeding, hemolytic anemia, hepatitis, hives, hyperbilirubinemia, hypersensitivity, interstitial nephritis, jaundice, leukopenia, neutropenia, pain at injection site, pancytopenia, positive Coombs test, prolonged PT/INR, pseudomembranous colitis, rash, renal dysfunction, seizure, Stevens-Johnson syndrome, stomach cramps, tachycardia, thrombocytopenia (rare), tongue swelling, toxic epidermal necrolysis, urticaria
Reactions reported with other cephalosporins: Agranulocytosis, aplastic anemia, asterixis, encephalopathy, hemorrhage, neuromuscular excitability, serum-sickness reactions, superinfection, toxic nephropathy
Drug Interactions
Antacids: May decrease the serum concentration of Cefuroxime. Risk C: Monitor therapy
H2-Antagonists: May decrease the absorption of Cefuroxime. Separate oral doses by at least 2 hours. Risk C: Monitor therapy
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Risk D: Consider therapy modification
Uricosuric Agents: May decrease the excretion of Cephalosporins. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Food: Bioavailability is increased with food; cefuroxime serum levels may be increased if taken with food or dairy products.
Storage
Injection: 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.
Oral suspension: Prior to reconstitution, store at 2°C to 30°C (36°F to 86°F). Reconstituted suspension is stable for 10 days at 2°C to 8°C (36°F to 46°F).
Tablet: Store at 15°C to 30°C (59°F to 86°F).
Compatibility
Stable in D51/4NS, D51/2NS, D5NS, D5W, D10W, LR, NS.
Y-site administration: Compatible: Acyclovir, allopurinol, amifostine, atracurium, aztreonam, cyclophosphamide, diltiazem, docetaxel, etoposide, famotidine, fludarabine, foscarnet, gemcitabine, granisetron, hydromorphone, linezolid, melphalan, meperidine, morphine, ondansetron, pancuronium, perphenazine, propofol, remifentanil, sargramostim, tacrolimus, teniposide, thiotepa, vecuronium. Incompatible: Clarithromycin, filgrastim, fluconazole, midazolam, vinorelbine. Variable (consult detailed reference): Cisatracurium, vancomycin.
Compatibility in syringe: Incompatible: Doxapram.
Compatibility when admixed: Compatible: Clindamycin, floxacillin, furosemide, heparin, metronidazole, potassium chloride. Incompatible: Aminoglycosides, sodium bicarbonate. Variable (consult detailed reference): Gentamicin, ranitidine.
Mechanism of Action
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.
Pharmacodynamics/Kinetics
Absorption: Oral (cefuroxime axetil): Increases with food
Distribution: Widely to body tissues and fluids; crosses blood-brain barrier; therapeutic concentrations achieved in CSF even when meninges are not inflamed
Protein binding: 33% to 50%
Bioavailability: Tablet: Fasting: 37%; Following food: 52%
Half-life elimination: Children 1-2 hours; Adults: 1-2 hours; prolonged with renal impairment
Time to peak, serum: I.M.: ?15-60 minutes; I.V.: 2-3 minutes; Oral: Children: 3-4 hours; Adults: 2-3 hours
Excretion: Urine (66% to 100% as unchanged drug)
Dosage
Note: Cefuroxime axetil film-coated tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis
Usual dosage range:
Children 3 months to 12 years:
Oral: 20-30 mg/kg/day in 2 divided doses
I.M., I.V.: 75-150 mg/kg/day divided every 8 hours (maximum dose: 6 g/day)
Children ?13 years and Adults:
Oral: 250-500 mg twice daily
I.M., I.V.: 750 mg to 1.5 g every 6-8 hours or 100-150 mg/kg/day in divided doses every 6-8 hours (maximum: 6 g/day)
Indication-specific dosing:
Children ?3 months to 12 years:
Acute bacterial maxillary sinusitis, acute otitis media, and impetigo:
Oral: Suspension: 30 mg/kg/day in 2 divided doses for 10 days (maximum dose: 1 g/day); tablet: 250 mg twice daily for 10 days
I.M., I.V.: 75-150 mg/kg/day divided every 8 hours (maximum dose: 6 g/day)
Epiglottitis: Oral: 150 mg/kg/day in 3 divided doses for 7-10 days
Pharyngitis/tonsillitis:
Oral: Suspension: 20 mg/kg/day (maximum: 500 mg/day) in 2 divided doses for 10 days; tablet: 125 mg every 12 hours for 10 days
I.M., I.V.: 75-150 mg/kg day divided every 8 hours (maximum: 6 g/day)
Children ?13 years and Adults (all oral doses listed are for tablet formulation):
Bronchitis (acute and exacerbations of chronic bronchitis):
Oral: 250-500 mg every 12 hours for 10 days
I.V.: 500-750 mg every 8 hours (complete therapy with oral dosing)
Cellulitis, orbital: I.V.: 1.5 g every 8 hours
Gonorrhea:
Disseminated: I.M., I.V.: 750 mg every 8 hours
Uncomplicated:
Oral: 1 g as a single dose
I.M.: 1.5 g as single dose (administer in 2 different sites with probenecid)
Lyme disease (early): Oral: 500 mg twice daily for 20 days
Pharyngitis/tonsillitis and sinusitis: Oral: 250 mg twice daily for 10 days
Pneumonia (uncomplicated): I.V.: 750 mg every 8 hours
Severe or complicated infections: I.M., I.V.: 1.5 g every 8 hours (up to 1.5 g every 6 hours in life-threatening infections)
Skin/skin structure infection (uncomplicated):
Oral: 250-500 mg every 12 hours for 10 days
I.M., I.V.: 750 mg every 8 hours
Surgical prophylaxis:
I.V.: 1.5 g 30 minutes to 1 hour prior to procedure (if procedure is prolonged can give 750 mg every 8 hours I.M.)
Open heart: I.V.: 1.5 g every 12 hours to a total of 6 g
Urinary tract infection (uncomplicated):
Oral: 125-250 mg every 12 hours for 7-10 days
I.M., I.V.: 750 mg every 8 hours
Dosing adjustment in renal impairment:
Clcr 10-20 mL/minute: Administer every 12 hours
Clcr <10 mL/minute: Administer every 24 hours
Hemodialysis: Dialyzable (25%)
Peritoneal dialysis: Dose every 24 hours
Continuous renal replacement therapy (CRRT): 1 g every 12 hours
Administration: Oral
Administer around-the-clock to promote less variation in peak and trough serum levels. Oral suspension: Administer with food. Shake well before use.
Administration: I.M.
Inject deep I.M. into large muscle mass.
Administration: I.V.
Inject direct I.V. over 3-5 minutes. Infuse intermittent infusion over 15-30 minutes.
Administration: I.V. Detail
pH: 6.0-8.5 (vials); 5.0-7.5 (frozen premixed solution)
Monitoring Parameters
Observe for signs and symptoms of anaphylaxis during first dose; with prolonged therapy, monitor renal, hepatic, and hematologic function periodically; monitor prothrombin time in patients at risk of prolongation during cephalosporin therapy (nutritionally-deficient, prolonged treatment, renal or hepatic disease)
Test Interactions
Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution); false-negative may occur with ferricyanide test. Glucose oxidase or hexokinase-based methods should be used.
Dietary Considerations
May be taken with food.
Zinacef®: Sodium content: 1.8 mEq (41 mg) per 750 mg
Ceftin®: Powder for oral suspension 125 mg/5 mL contains phenylalanine 11.8 mg/5 mL; 250 mg/5 mL contains phenylalanine 25.2 mg/5 mL.
Patient Education
Do not take any new medication during therapy unless approved by prescriber. If administered by injection or infusion, report immediately any swelling, redness, or pain at injection/infusion site; respiratory difficulty or swallowing; chest pain; or rash. Oral tablets or suspension should be taken as directed, at regular intervals around-the-clock (with or without food). Chilling oral suspension improves flavor (do not freeze); shake well before using. Complete full course of medication, even if you feel better. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. May cause false test results with Clinitest®; use of another type of glucose testing is preferable. Report rash; breathing or swallowing difficulty; persistent diarrhea, nausea, vomiting, or abdominal pain; changes in urinary pattern or pain on urination; opportunistic infection (eg, vaginal itching or drainage, sores in mouth, blood in stool or urine, unusual fever or chills); CNS changes (eg, irritability, agitation, nervousness, insomnia, hallucinations); or other adverse reactions. Breast-feeding precaution: Consult prescriber if breast-feeding.
Geriatric Considerations
Adjust dose for renal function in the elderly. Considered one of the drugs of choice for outpatient treatment of community-acquired pneumonia in the elderly.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins
Mental Health: Effects on Psychiatric Treatment
May rarely cause neutropenia; use caution with clozapine and carbamazepine
Nursing: Physical Assessment/Monitoring
Assess results of culture/sensitivity tests and patient's allergy history prior to therapy. Assess other pharmacological or herbal products patient may be taking for potential interactions (eg, nephrotoxicity). Assess results of laboratory tests (prothrombin times), therapeutic response, and adverse reactions (eg, hemolytic anemia, hypoprothrombinemia, and bleeding) regularly during therapy. Advise patients with diabetes about use of Clinitest® (may cause false-positive test). Teach patient possible side effects/appropriate interventions and adverse symptoms to report (eg, opportunistic infection, hypersensitivity reaction).
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Note: Strength expressed as base
Infusion, as sodium [premixed]: 750 mg (50 mL); 1.5 g (50 mL)
Zinacef®: 750 mg (50 mL); 1.5 g (50 mL) [contains sodium 4.8 mEq (111 mg) per 750 mg]
Injection, powder for reconstitution, as sodium: 750 mg, 1.5 g, 7.5 g, 75 g, 225 g
Zinacef®: 750 mg, 1.5 g, 7.5 g [contains sodium 1.8 mEq (41 mg) per 750 mg]
Powder for suspension, oral, as axetil: 125 mg/5 mL (100 mL); 250 mg/5 mL (50 mL, 100 mL)
Ceftin®: 125 mg/5 mL (100 mL) [contains phenylalanine 11.8 mg/5 mL; tutti-frutti flavor]; 250 mg/5 mL (50 mL, 100 mL) [contains phenylalanine 25.2 mg/5 mL; tutti-frutti flavor]
Tablet, as axetil: 250 mg, 500 mg
Ceftin®: 250 mg, 500 mg
Pricing: U.S. (www.drugstore.com)
Suspension (reconstituted) (Cefuroxime Axetil)
250 mg/5 mL (100): $89.99
Tablets (Ceftin)
250 mg (20): $177.24
500 mg (20): $308.62
Tablets (Cefuroxime Axetil)
250 mg (20): $70.99
500 mg (20): $73.98
References
Abramowicz M, “Antimicrobial Prophylaxis in Surgery,” Medical Letter on Drugs and Therapeutics, Handbook of Antimicrobial Therapy, 16th ed, New York, NY: Medical Letter, 2002.
Aronoff GR, Bennett WM, Berns JS, et al, Drug Prescribing in Renal Failure: Dosing Guidelines for Adults and Children, 5th ed. Philadelphia, PA: American College of Physicians; 2007.
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.
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.
Mandell LA, Wunderink RG, Anzueto A, et al, “Infectious Diseases Society of America/American Thoracic Society Consensus Guidelines on the Management of Community-Acquired Pneumonia in Adults,” Clin Infect Dis, 2007, 44(Suppl 2):27-72.
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.
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.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
Content last modified August 2008
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