Download Cefuroxime Basics

Cefuroxime
Basics
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Description
Formulation Details
[West-Ward Pharmaceutical Corp] (7.5 g)
Formulation Details
[West-Ward Pharmaceutical Corp] (1.5 g)
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[West-Ward Pharmaceutical Corp] (750 mg)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (750 mg)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (1.5 g)
Formulation Details
Ceftin® [GlaxoSmithKline] (250 mg)
Formulation Details
Ceftin® [GlaxoSmithKline] (500 mg)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (7.5 g)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (750 mg)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (1.5 g)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (750 mg)
Formulation Details
Zinacef® [Covis Pharmaceuticals] (1.5 g)
Formulation Details
Ceftin® [GlaxoSmithKline] (125 mg/5 mL)
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Ceftin® [GlaxoSmithKline] (250 mg/5 mL)
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[B Braun Medical Inc] (750 mg)
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[B Braun Medical Inc] (1.5 g)
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[Hospira] (1.5 g)
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[Hospira] (7.5 g)
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[Baxter Healthcare] (750 mg)
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[Baxter Healthcare] (1.5 g)
[Northstar Rx LLC] (250 mg)
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[Northstar Rx LLC] (500 mg)
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[Sagent Pharmaceuticals Inc] (750 mg)
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[Sagent Pharmaceuticals Inc] (1.5 g)
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[Sagent Pharmaceuticals Inc] (7.5 g)
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[Greenstone Ltd] (250 mg)
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[Greenstone Ltd] (500 mg)
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Description
[Apotex Corp] (500 mg)
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[Apotex Corp] (250 mg)
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[Apotex Corp] (250 mg)
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[Apotex Corp] (500 mg)
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[Ranbaxy Pharmaceuticals Inc] (250 mg)
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[Ranbaxy Pharmaceuticals Inc] (500 mg)
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[Ranbaxy Pharmaceuticals Inc] (125 mg/5 mL)
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[Ranbaxy Pharmaceuticals Inc] (250 mg/5 mL)
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[APP Pharmaceutical] (750 mg)
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[APP Pharmaceutical] (1.5 g)
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[APP Pharmaceutical] (7.5 g)
[Wockhardt Americas Inc] (250 mg)
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[Wockhardt Americas Inc] (500 mg)
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Description
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[Aurobindo Pharma USA] (250 mg)
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[Aurobindo Pharma USA] (500 mg)
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[Samson Medical Technologies] (75 g)
[Lupin Pharmaceuticals Inc] (250 mg)
Formulation Details
[Lupin Pharmaceuticals Inc] (500 mg)
Formulation Details
U.S. Brand Names
Ceftin; Zinacef; Zinacef in D5W; Zinacef in Sterile Water
Canadian Brand Names
Apo-Cefuroxime®; Auro-Cefuroxime; Ceftin®; Cefuroxime For Injection; Cefuroxime For Injection, USP; PRO-Cefuroxime; ratio-Cefuroxime
Medication Safety Issues
Sound-alike/look-alike issues:
Cefuroxime may be confused with cefotaxime, cefprozil, deferoxamine
Ceftin® may be confused with Cefzil®, Cipro®
Zinacef® may be confused with Zithromax®
International issues:
Ceftin [U.S., Canada] may be confused with Cefiton brand name for cefixime [Portugal]; Ceftim brand name for ceftazidime [Portugal]; Ceftime
brand name for ceftazidime [Thailand]
Generic Available (U.S.)
May be product dependent
Therapeutic Category
Antibiotic, Cephalosporin (Second Generation)
Related Terms
Cefuroxime Axetil; Cefuroxime Sodium
Clinical Pharmacology
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.
Pharmacokinetics (Adult data unless noted)
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)
Indications & Usage
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 upper and lower respiratory tract, otitis media, urinary tract, uncomplicated skin and soft tissue, bone and joint,
sepsis, uncomplicated gonorrhea, and early Lyme disease; surgical prophylaxis
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.
Pregnancy & Lactation
Pregnancy Risk Factor
B
Pregnancy Implications
Adverse events were not observed in animal reproduction studies. Cefuroxime crosses the placenta and reaches the cord serum and amniotic fluid.
Placental transfer is decreased in the presence of oligohydramnios. Several studies have failed to identify an increased teratogenic risk to the fetus
following 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. Cefuroxime is one of the antibiotics recommended for prophylactic use prior to cesarean delivery.
Lactation
Enters breast milk
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
Interactions
Drug Interactions: Metabolism/Transport Effects
None known.
Drug Interactions
Aminoglycosides: Cephalosporins (2nd Generation) may enhance the nephrotoxic effect of Aminoglycosides. Risk C: Monitor therapy
Antacids: May decrease the serum concentration of Cefuroxime. Management: Consider administering antacids and cefuroxime at least 2 hours apart.
Risk D: Consider therapy modification
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
H2-Antagonists: May decrease the absorption of Cefuroxime. Separate oral doses by at least 2 hours. Risk C: Monitor therapy
Probenecid: May increase the serum concentration of Cephalosporins. Risk C: Monitor therapy
Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel
cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Risk D: Consider therapy modification
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management:
Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this
vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Cephalosporins may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Food Interactions
Food: Bioavailability is increased with food; cefuroxime serum levels may be increased if taken with food or dairy products.
Lab 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.
Dosing
Dosing: Adults
Note: Cefuroxime axetil film-coated tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis. 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
Cholecystitis, mild-to-moderate: I.V.: 1.5 g every 8 hours for 4-7 days (provided source controlled)
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 two different sites with probenecid)
Intra-abdominal infection, complicated, community-acquired, mild-to-moderate (in combination with metronidazole): I.V.: 1.5 g every 8
hours for 4-7 days (provided source controlled)
Lyme disease (early): Oral: 500 mg twice daily for 20 days
Pharyngitis/tonsillitis and sinusitis: Oral: 250 mg twice daily for 10 days
Skin/skin structure infection, uncomplicated:
Oral: 250-500 mg every 12 hours for 10 days
I.M., I.V.: 750 mg every 8 hours
Pneumonia, uncomplicated: I.M., 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)
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.)
Cholecystectomy: I.V.: 1.5 g every 8 hours, discontinue within 24 hours unless infection outside gallbladder suspected
Open heart: I.V.: 1.5 g every 12 hours to a total of 6 g
Urinary tract infection, uncomplicated:
Oral: 125-250 mg twice daily for 7-10 days
I.V., I.M.: 750 mg every 8 hours
Dosing: Elderly
Refer to adult dosing.
Dosing: Pediatric
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:
Epiglottitis:Oral: 150 mg/kg/day in 3 divided doses for 7-10 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 every 12 hours for 10 days
I.M., I.V.: 75-150 mg/kg/day divided every 8 hours (maximum dose: 6 g/day)
Acute bacterial maxillary sinusitis: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
Meningitis: NOT recommended (doses of 200-240 mg/kg/day divided every 6-8 hours have been used) (maximum dose: 9 g/day)
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 dose: 6 g/day
Children ≥13 years: Refer to adult dosing.
Dosing: 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
Note: Cefuroxime axetil film-coated tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis.
Dosing: Hepatic Impairment
No dosage adjustment provided in manufacturer’s labeling.
Available Products
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous, as sodium [strength expressed as base]:
Zinacef in D5W: 750 mg (50 mL)
Zinacef in Sterile Water: 1.5 g (50 mL)
Solution Reconstituted, Injection, as sodium [strength expressed as base]:
Zinacef: 750 mg (1 ea); 1.5 g (1 ea); 7.5 g (1 ea)
Generic: 750 mg (1 ea); 1.5 g (1 ea); 7.5 g (1 ea); 75 g (1 ea); 225 g (1 ea)
Solution Reconstituted, Intravenous, as sodium [strength expressed as base]:
Zinacef: 750 mg (1 ea); 1.5 g (1 ea)
Generic: 750 mg (1 ea); 1.5 g (1 ea); 7.5 g (1 ea)
Suspension Reconstituted, Oral, as axetil [strength expressed as base]:
Ceftin: 125 mg/5 mL (100 mL); 250 mg/5 mL (50 mL, 100 mL) [contains aspartame; tutti-frutti flavor]
Generic: 125 mg/5 mL (100 mL)
Tablet, Oral, as axetil [strength expressed as base]:
Ceftin: 250 mg, 500 mg
Generic: 250 mg, 500 mg
Administration
Administration, Oral
Administer with food. Shake oral suspension 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)
Storage & Compatibility
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).
I.V. Compatibility
Stable in D51/4NS, D51/2NS, D5NS, D5W, D10W, LR, NS.
Y-site administration: Compatible: Acyclovir, allopurinol, amifostine, anidulafungin, atracurium, aztreonam, bivalirudin, cyclophosphamide,
cyclosporine, dexmedetomidine, diltiazem, docetaxel, etoposide phosphate, famotidine, fenoldopam, fentanyl, fludarabine, foscarnet, gemcitabine,
granisetron, hetastarch in lactate electrolyte injection (Hextend®), hydromorphone, linezolid, melphalan, meperidine, milrinone, morphine, ondansetron,
pancuronium, pemetrexed, propofol, remifentanil, sargramostim, tacrolimus, teniposide, thiotepa, vecuronium. Incompatible: Azithromycin, filgrastim,
fluconazole, midazolam, pantoprazole, vinorelbine. Variable (consult detailed reference): Amiodarone, cisatracurium, vancomycin.
Compatibility in syringe: Compatible: Dimenhydrinate. Incompatible: Doxapram, pantoprazole.
Monitoring
Monitoring Parameters
Monitor renal, hepatic, and hematologic function periodically with prolonged therapy. Monitor prothrombin time in patients at risk of prolongation during
cephalosporin therapy (nutritionally-deficient, prolonged treatment, renal or hepatic disease). Observe for signs and symptoms of anaphylaxis during first
dose.
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.
Patient Education
Discuss specific use of drug and side effects with patient as it relates to treatment. Patient may experience nausea, diarrhea, or vaginal yeast infection.
Have patient report immediately to prescriber ecchymosis or rash. Educate patient about signs of a significant reaction (eg, wheezing; chest tightness;
fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects.
Patient should consult prescriber for additional questions.
Dietary Implications
Some products may contain phenylalanine and/or sodium.
Oral suspension: May be taken with food.
View the Patient Handout: English | Spanish
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.
Bradley JS, Byington CL, Shah SS, et al. “The Management of Community-Acquired Pneumonia in Infants and Children Older Than 3 Months of Age:
Clinical Practice Guidelines by the Pediatric Infectious Diseases Society and the Infectious Diseases Society of America”, Clin Infect Dis, 2011, 53(7):e2576. [PMID: 21880587]
Bratzler DW, Dellinger EP, Olsen KM, et al, “Clinical Practice Guidelines for Antimicrobial Prophylaxis in Surgery,” Am J Health Syst Pharm, 2013,
70(3):195-283. [PMID: 23327981]
Bratzler DW and Houck PM (for the Surgical Infection Prevention Guidelines Writers Workgroup), “Antimicrobial Prophylaxis for Surgery: An Advisory
Statement From the National Surgical Infection Prevention Project,” Clin Infect Dis, 2004, 38(12):1706-15. [PMID: 15227616 ]
Broekhuysen J, Deger F, Douchamps J, et al, “Pharmacokinetic Study of Cefuroxime in the Elderly,” Br J Clin Pharmacol, 1981, 21(6):801-5. [PMID:
7340882]
de Louvois J, Mulhall A, and Hurley R, “Cefuroxime in the Treatment of Neonates,” Arch Dis Child, 1982, 57(1):59-62. [PMID: 7065695]
Douglas JG, Bax RP, and Munro JF, “The Pharmacokinetics of Cefuroxime in the Elderly,” J Antimicrob Chemother, 1980, 6(4):543-9. [PMID: 7430016]
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. [PMID: 3401076]
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. [PMID: 8822290]
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. [PMID: 17278083]
Marshall WF and Blair JE, “The Cephalosporins,” Mayo Clin Proc, 1999, 74(2):187-95. [PMID: 10069359]
Nelson JD, “Cefuroxime: A Cephalosporin With Unique Applicability to Pediatric Practice,” Pediatr Infect Dis, 1983, 2(5):394-6. [PMID: 6356062]
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. [PMID: 3498617]
Solomkin JS, Mazuski JE, Bradley JS, et al, “Diagnosis and Management of Complicated Intra-Abdominal Infections in Adults and Children: Guidelines by
the Surgical Infection Society and the Infectious Diseases Society of America,” Clin Infect Dis, 2010, 50(2):133-64. [PMID: 20034345]
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