Cefuroxime

Pronunciation

(se fyoor OKS eem)

U.S. Brand Names

Ceftin®; Zinacef®

Synonyms

Cefuroxime Axetil; Cefuroxime Sodium

Generic Available

Yes

Canadian Brand Names

Apo-Cefuroxime®; Ceftin®; Kefurox®; ratio-Cefuroxime; Zinacef®

Use

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

Pregnancy Risk Factor

Lactation

Enters breast milk/use caution

Contraindications

Hypersensitivity to cefuroxime, any component of the formulation, or other cephalosporins

Warnings/Precautions

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 . May be associated with increased INR, especially in nutritionally-deficient patients, prolonged treatment, hepatic or renal disease. Tablets and oral suspension are not bioequivalent (do not substitute on a mg-per-mg basis).

Adverse Reactions

1% to 10%:

Endocrine & metabolic: Alkaline phosphatase increased (2%)

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

Hepatic: Transaminases increased (4%)

Local: Thrombophlebitis (2%)

<1%: Anaphylaxis, angioedema, cholestasis, colitis, diarrhea, dizziness, erythema multiforme, fever, GI bleeding, headache, hemolytic anemia, increased BUN, increased creatinine, interstitial nephritis, leukopenia, nausea, neutropenia, pain at injection site, pancytopenia, prolonged PT/INR, pseudomembranous colitis, rash, seizure, stomach cramps, thrombocytopenia, toxic epidermal necrolysis, vaginitis, vomiting

Reactions reported with other cephalosporins include agranulocytosis, aplastic anemia, asterixis, encephalopathy, hemorrhage, neuromuscular excitability, serum-sickness reactions, superinfection, toxic nephropathy

Overdosage/Toxicology

Symptoms of overdose include neuromuscular hypersensitivity and convulsions. Many beta-lactam containing antibiotics have the potential to cause neuromuscular hyperirritability or convulsive seizures. Hemodialysis may be helpful to aid in removal of the drug from blood; otherwise, treatment is supportive or symptom-directed.

Drug Interactions

Increased effect: High-dose probenecid decreases clearance

Increased toxicity: Aminoglycosides increase nephrotoxic potential

Ethanol/Nutrition/Herb Interactions

Food: Bioavailability is increased with food; cefuroxime serum levels may be increased if taken with food or dairy products.

Stability

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

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; crosses placenta; enters breast milk

Protein binding: 33% to 50%

Bioavailability: Tablet: Fasting: 37%; Following food: 52%

Half-life elimination: Adults: 1-2 hours; prolonged with renal impairment

Time to peak, serum: I.M.: ~15-60 minutes; I.V.: 2-3 minutes

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

Children 3 months to 12 years:

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

Acute otitis media, impetigo: Oral:

Suspension: 30 mg/kg/day (maximum: 1 g/day) in 2 divided doses for 10 days

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

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

Acute bacterial maxillary sinusitis:

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

Children 13 years and Adults:

Oral: 250-500 mg twice daily for 10 days (5 days in selected patients with acute bronchitis)

Uncomplicated urinary tract infection: 125-250 mg every 12 hours for 7-10 days

Uncomplicated gonorrhea: 1 g as a single dose

Early Lyme disease: 500 mg twice daily for 20 days

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:

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

Clcr<10 mL/minute: Administer every 24 hours

Hemodialysis: Dialyzable (25%)

Continuous arteriovenous or venovenous hemodiafiltration effects: Dose as for Clcr 10-20 mL/minute

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.

I.M.: Inject deep I.M. into large muscle mass.

I.V.: Inject direct I.V. over 3-5 minutes. Infuse intermittent infusion over 15-30 minutes.

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-positive serum or urine creatinine with Jaffé reaction

Dietary Considerations

May be taken with food.

Zinacef®: Sodium content: 4.8 mEq (111 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

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. 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 suspension should be taken as directed, at regular intervals around-the-clock (with or without food); complete full course of medication, even if you feel better. Chilling suspension improves flavor (do not freeze). 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 unusual bruising or bleeding; or opportunistic infection (vaginal itching or drainage, sores in mouth, blood in urine or stool).

Breast-feeding precaution: Consult prescriber if breast-feeding.

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

Dosage Forms

[DSC] = Discontinued product

Infusion, as sodium [premixed] (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 (Zinacef®): 750 mg, 1.5 g, 7.5 g [contains sodium 4.8 mEq (111 mg) per 750 mg]

Powder for oral suspension, as axetil (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

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.

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.

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.

International Brand Names

Aksef® (TR); Apo-Cefuroxime® (CA); Axetine® (BE, BG, CZ, RO, RU, SG, SK, TH, VN); Axetin® (RU); Axurocef® (TH); Biociclin® (IT); Biofuroksym® (PL); Bioracef® (PL); Cefaks® (TR); Cefamar® (RO, TH); Cefatin® (TR); Ceflux® (AR); Cefofix® (NL); Cefogen-750® (RO); Cefogram® (AR); Cefoprim® (IT); Ceftin® (CA); cefudura® (DE); Cefuhexal® (DE); Cefuracet® (MX); Cefurax® (DE); Cefurex® (IT); Cefurim® (TH); Cefurin® (IT); Cefuro-Puren® (DE); Cefurox® (AR, ID); Cefuroxima Biochemie® (CO); Cefuroxima Chiesi® (ES); Cefuroxima Combino Pharm® (ES); Cefuroxima Fabra® (AR); Cefuroxima Fada® (AR); Cefuroxima Ges® (ES); Cefuroxima IPS Farma® (ES); Cefuroxima K24® (IT); Cefuroxima Klonal® (AR); Cefuroxima Klonal® [inj.] (AR); Cefuroxim AL® (DE); Cefuroxima Normon® (ES); Cefuroxima Northia® (AR); Cefuroxima Richet® (AR); Cefuroxima® (RO); Cefuroxim AZU® (DE); Cefuroxim beta® (DE); Cefuroxim-Biochemie® (CH); Cefuroxim curasan® (DE); Cefuroxime Biochemie® (RO, TH); Cefuroxime® (GB, NZ); Cefuroxime Orion Pharma® (FI); Céfuroxime Panpharma® (FR); Cefuroxime Panpharma® (RO); Cefuroxime Sodium® (NZ); Cefuroxime-Teva® (IL); Cefuroxim Fresenius® (DE); Cefuroxim Heumann® (DE); Cefuroxim Hexal® (DE); Cefuroxim Inno Pharm® (DE); Cefuroxim Lilly® (AT, DE); Cefuroxim® (NO, RO); Cefuroxim-ratiopharm® (DE); Cefuroxim-saar® (DE); Cefuroxim Sandoz® (DE); Cefuroxim Stada® (DE); Cefuroxim Stragen® (DK); cefuroxim von ct® (DE); Cefurox-Wolff® (DE); Cefu TAD® (DE); Cépazine® (FR); Ceroxim® (HU, PL, ZA); Cethixim® (ID); Cetoxil® [inj.] (MX); Cetoxil® [tabs] (MX); Cexim® (HU); Cipofix® (ZA); Colifossim® (IT); Curocef® (AT); Curocef Inyectable® (CL); Curocef Oral® (CL); Curoxima® (ES); Curoxime® (PT); Curoxim® (IT); Deltacef® (IT); Deltrox® (AR); Duxima® (IT); Elobact® (DE); Froxal® [inj.] (MX); Froxime® (HK, JO, KW, LB, MT, MY, RO); Furoxim® (AT); Furoxime® (TH); Ipacef® (IT); Itorex® (IT); Kalcef® [caps] (ID); Kalcef® [inj.] (ID); Kefox® (IT); Kefurim® (IL); Kefurox® (BE, CA, LU); Kenacef® (ID); Kesint® (IT); Ketocef® (HR, RO, RU, SI); Lafurex® (IT); Lifurom® (ZA); Lifurox® (ES, NO, RO); Magnaspor® (TH); Maxil® (EG, JO, KW, LB, SY); Medoxem® (GR); Multisef® (RO, TR); Naroxit® (ID); Nilacef® (YU); Nivador® (ES); Novocef® (HR, SI); Oraceftin® (TR); Oraxim® (IT); Pharmacare-Cefuroxime® (ZA); Plixym® (PL); ratio-Cefuroxime (CA); Roxbi® (ID); Sefuroks® (TR); Selan® (ES); Sharox® (ID); Shincef® (SG); Supacef® (IN); Supero® (IT); Tarsime® (PL); Tilexim® (IT); Tvindal® (SI); Vekfazolin® (RO); Xorim® (HU); Zilisten® (RO); Zinacef® (BD, BE, BG, BR, CA, CH, CO, DE, DK, FI, GB, HK, HU, ID, IE, IL, KW, LU, NL, NO, NZ, PL, RO, RU, SE, SG, SI, TH, YU, ZA); Zinat® (CH); Zinnat® (AT, AU, BD, BE, BG, BR, CO, CR, DE, DK, DO, EC, ES, FI, FR, GB, GT, HK, HN, HR, HU, ID, IE, IL, IT, KW, LU, MX, NL, NZ, PA, PL, RO, RU, SE, SG, SI, SV, TH, TR, ZA); Zinnat® [inj.] (EC, FR, MX, SI, TR); Zinocep® (IT); Zipos® (PT); Zoref® (IT, PT)

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