Brand names: Ceftin, Zinacef
Drug class: Second Generation Cephalosporins
Chemical name: [6R-[6α,7β(Z)]]-3-[[(2-Aminocarbonyl)oxy]methyl]-7-[2-furanyl(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monosodium salt
Molecular formula: C₁₆H₁₆N₄O₈S
CAS number: 56238-63-2

Medically reviewed by Drugs.com on Oct 1, 2024. Written by ASHP.

Introduction

Antibacterial; β-lactam antibiotic; second generation cephalosporin.

Uses for Cefuroxime

Acute Otitis Media (AOM)

Treatment of AOM caused by Streptococcus pneumoniae, Haemophilus influenzae (including β-lactamase-producing strains), Moraxella catarrhalis (including β-lactamase-producing strains), or S. pyogenes.

When anti-infectives indicated, AAP recommends high-dose amoxicillin or amoxicillin and clavulanate as drugs of choice for initial treatment of AOM; certain cephalosporins (cefdinir, cefpodoxime, cefuroxime, ceftriaxone) recommended as alternatives for initial treatment in penicillin-allergic patients without a history of severe and/or recent penicillin-allergic reactions.

Pharyngitis and Tonsillitis

Treatment of pharyngitis and tonsillitis caused by S. pyogenes (group A β-hemolytic streptococci). Generally effective in eradicating S. pyogenes from nasopharynx; efficacy in prevention of subsequent rheumatic fever not established.

AAP, IDSA, AHA, and others recommend a penicillin regimen (10 days of oral penicillin V or oral amoxicillin or single dose of IM penicillin G benzathine) as treatments of choice for S. pyogenes pharyngitis and tonsillitis; other anti-infectives (oral cephalosporins, oral macrolides, oral clindamycin) recommended as alternatives in penicillin-allergic patients.

If an oral cephalosporin used, 10 day regimen of first generation cephalosporin (cefadroxil, cephalexin) preferred instead of other cephalosporins with broader spectrums of activity (e.g., cefaclor, cefdinir, cefixime, cefpodoxime, cefuroxime).

Bone and Joint Infections

Parenteral treatment of bone and joint infections caused by susceptible Staphylococcus aureus (including penicillinase-producing strains).

Meningitis

Parenteral treatment of meningitis caused by susceptible S. pneumoniae, H. influenzae (including ampicillin-resistant strains), Neisseria meningitidis, or S. aureus (including penicillinase-producing strains).

Not a drug of choice for meningitis; treatment failures have been reported, especially in meningitis caused by H. influenzae. In addition, bacteriologic response to cefuroxime appears to be slower than that reported with ceftriaxone, which may increase the risk for hearing loss and neurologic sequelae. When a cephalosporin is indicated for the treatment of bacterial meningitis, a parenteral third generation cephalosporin (usually ceftriaxone or cefotaxime) generally recommended.

Respiratory Tract Infections

Treatment of acute maxillary sinusitis caused by susceptible S. pneumoniae or H. influenzae (non-β-lactamase-producing strains only). Data insufficient to date to establish efficacy for treatment of acute maxillary sinusitis known or suspected to be caused by β-lactamase-producing strains of H. influenzae or M. catarrhalis. Because of variable activity against S. pneumoniae and H. influenzae, IDSA no longer recommends second or third generation oral cephalosporins for empiric monotherapy of acute bacterial sinusitis. Oral amoxicillin or amoxicillin and clavulanate usually recommended for empiric treatment. If an oral cephalosporin used as an alternative in children (e.g., in penicillin-allergic individuals), combination regimen that includes a third generation cephalosporin (cefixime or cefpodoxime) and clindamycin (or linezolid) recommended.

Treatment of secondary bacterial infections of acute bronchitis caused by susceptible S. pneumoniae, H. influenzae (non-β-lactamase-producing strains only), or H. parainfluenzae (non-β-lactamase-producing strains only).

Treatment of acute exacerbations of chronic bronchitis caused by susceptible S. pneumoniae, H. influenzae (non-β-lactamase-producing strains only), or H. parainfluenzae (non-β-lactamase-producing strains only).

Parenteral treatment of lower respiratory tract infections (including pneumonia) caused by susceptible S. pneumoniae, S. aureus (including penicillinase-producing strains), S. pyogenes (group A β-hemolytic streptococci), H. influenzae (including ampicillin-resistant strains), Escherichia coli, or Klebsiella.

Treatment of community-acquired pneumonia (CAP). Recommended by ATS and IDSA as an alternative for treatment of CAP caused by penicillin-susceptible S. pneumoniae. Also recommended as an alternative in certain combination regimens used for empiric treatment of CAP. Select regimen for empiric treatment of CAP based on most likely pathogens and local susceptibility patterns; after pathogen is identified, modify to provide more specific therapy (pathogen-directed therapy).

For empiric outpatient treatment of CAP when risk factors for drug-resistant S. pneumoniae are present (e.g., comorbidities such as chronic heart, lung, liver, or renal disease, diabetes, alcoholism, malignancies, asplenia, immunosuppression; use of anti-infectives within the last 3 months), ATS and IDSA recommend monotherapy with a fluoroquinolone active against S. pneumoniae (moxifloxacin, gemifloxacin, levofloxacin) or, alternatively, a combination regimen that includes a β-lactam active against S. pneumoniae (high-dose amoxicillin or fixed combination of amoxicillin and clavulanic acid or, alternatively, ceftriaxone, cefpodoxime, or cefuroxime) given in conjunction with a macrolide (azithromycin, clarithromycin, erythromycin) or doxycycline. Cefuroxime and cefpodoxime may be less active against S. pneumoniae than amoxicillin or ceftriaxone.

If a parenteral cephalosporin is used as an alternative to penicillin G or amoxicillin for treatment of CAP caused by penicillin-susceptible S. pneumoniae, ATS and IDSA recommend ceftriaxone, cefotaxime or cefuroxime; if an oral cephalosporin is used for treatment of these infections, ATS and IDSA recommend cefpodoxime, cefprozil, cefuroxime, cefdinir, or cefditoren.

Septicemia

Parenteral treatment of septicemia caused by susceptible S. aureus (including penicillinase-producing strains), S. pneumoniae, E. coli, H. influenzae (including ampicillin-resistant strains), or Klebsiella.

In the treatment of known or suspected sepsis or the treatment of other serious infections when the causative organism is unknown, concomitant therapy with an aminoglycoside may be indicated pending results of in vitro susceptibility tests.

Skin and Skin Structure Infections

Oral treatment of uncomplicated skin and skin structure infections caused by susceptible S. aureus (including β-lactamase-producing strains) or S. pyogenes.

Parenteral treatment of skin and skin structure infections caused by susceptible S. aureus (including β-lactamase-producing strains), S. pyogenes, E. coli, Klebsiella, or Enterobacter.

Urinary Tract Infections (UTIs)

Oral treatment of uncomplicated UTIs caused by susceptible E. coli or K. pneumoniae.

Parenteral treatment of UTIs caused by susceptible E. coli or K. pneumoniae.

Gonorrhea and Associated Infections

Has been used orally or parenterally for treatment of uncomplicated urethral, endocervical, or rectal gonorrhea caused by susceptible Neisseria gonorrhoeae.

Has been used parenterally for treatment of disseminated gonococcal infections caused by susceptible N. gonorrhoeae.

Not included in current CDC recommendations for gonococcal infections.

Because of concerns related to recent reports of N. gonorrhoeae with reduced susceptibility to cephalosporins, CDC states that oral cephalosporins no longer recommended as first-line treatment for uncomplicated gonorrhea. For treatment of uncomplicated urogenital, anorectal, or pharyngeal gonorrhea, CDC recommends a combination regimen that includes a single dose of IM ceftriaxone and either a single dose of oral azithromycin or 7-day regimen of oral doxycycline.

Lyme Disease

Treatment of early Lyme disease manifested as erythema migrans. IDSA, AAP, and other clinicians recommend oral doxycycline, oral amoxicillin, or oral cefuroxime axetil as first-line therapy for treatment of early localized or early disseminated Lyme disease associated with erythema migrans, in the absence of specific neurologic involvement or advanced atrioventricular (AV) heart block.

Treatment of early neurologic Lyme disease^{† [off-label]} in patients with cranial nerve palsy alone without evidence of meningitis (i.e., those with normal CSF examinations or those for whom CSF examination is deemed unnecessary because there are no clinical signs of meningitis). Parenteral anti-infectives (IV ceftriaxone, IV penicillin G sodium, or IV cefotaxime) recommended for treatment of early Lyme disease when there are acute neurologic manifestations such as meningitis or radiculopathy.

Treatment of Lyme carditis^{† [off-label]}. IDSA and others state that patients with AV heart block and/or myopericarditis associated with early Lyme disease may be treated with an oral regimen (doxycycline, amoxicillin, or cefuroxime axetil) or a parenteral regimen (IV ceftriaxone or, alternatively, IV cefotaxime or IV penicillin G sodium). A parenteral regimen usually recommended for initial treatment of hospitalized patients; an oral regimen can be used to complete therapy and for the treatment of outpatients.

Treatment of borrelial lymphocytoma^{† [off-label]}. Although experience is limited, IDSA states that available data indicate that borrelial lymphocytoma may be treated with an oral regimen (doxycycline, amoxicillin, or cefuroxime axetil).

Treatment of uncomplicated Lyme arthritis^{† [off-label]} without clinical evidence of neurologic disease. An oral regimen (doxycycline, amoxicillin, or cefuroxime axetil) can be used, but a parenteral regimen (IV ceftriaxone or, alternatively, IV cefotaxime or IV penicillin G sodium) should be used in those with Lyme arthritis and concomitant neurologic disease. Patients with persistent or recurrent joint swelling after a recommended oral regimen should receive retreatment with the oral regimen or a switch to a parenteral regimen. Some clinicians prefer retreatment with an oral regimen for those whose arthritis substantively improved but did not completely resolve; these clinicians reserve parenteral regimens for those patients whose arthritis failed to improve or worsened. Allow several months for joint inflammation to resolve after initial treatment before an additional course of anti-infectives is given.

Perioperative Prophylaxis

Perioperative prophylaxis in patients undergoing cardiac surgery; a drug of choice for cardiac procedures (e.g., coronary artery bypass, pacemaker or other cardiac device insertion, ventricular assist devices).

Perioperative prophylaxis in patients undergoing clean head and neck surgery involving placement of prosthesis (excluding tympanostomy); perioperative prophylaxis in conjunction with metronidazole in patients undergoing clean-contaminated cancer surgery of the head and neck or other clean-contaminated head and neck procedures (excluding tonsillectomy and functional endoscopic sinus procedures). A drug of choice.

Has been used for perioperative prophylaxis in patients undergoing noncardiac thoracic surgery, GI or biliary tract surgery, gynecologic or obstetric surgery (e.g., vaginal hysterectomy), orthopedic procedures, or heart transplantation. Other anti-infectives (e.g., cefazolin) usually preferred.

Cefuroxime Dosage and Administration

Administration

Administer cefuroxime axetil orally. Administer cefuroxime sodium by IV injection or infusion or deep IM injection.

IV route preferred in patients with septicemia or other severe or life-threatening infections or in patients with lowered resistance, particularly if shock is present.

Cefuroxime ADD-Vantage (TwistVial) vials, Duplex drug delivery system containing cefuroxime and dextrose injection in separate chambers, and the commercially available premixed cefuroxime injection (frozen) should be used only for IV infusion.

Oral Administration

Oral suspension must be administered with food.

Tablets may be given orally without regard to meals, but administration with food maximizes bioavailability.

Children 3 months to 12 years of age unable to swallow tablets should receive the oral suspension. Although the tablets have been crushed and mixed with food (e.g., applesauce, ice cream), the crushed tablets have a strong, persistent taste and the manufacturers state that the drug should not be administered in this manner.

Reconstitution

Reconstitute powder for oral suspension at the time of dispensing by adding the amount of water specified on the bottle to provide a suspension containing 125 or 250 mg of cefuroxime per 5 mL of suspension.

Tap the bottle to thoroughly loosen the powder; add the water in a single portion and shake vigorously. Shake suspension well just prior to each use and replace the cap securely after each opening.

IV Injection

Reconstitution

Reconstitute vials containing 750 mg or 1.5 g of cefuroxime with 8 or 16 mL of sterile water for injection, respectively, to provide solutions containing approximately 90 mg/mL.

Rate of Administration

Inject appropriate dose of reconstituted solution directly into a vein over a period of 3–5 minutes or slowly into the tubing of a freely flowing compatible IV solution.

IV Infusion

Other IV solutions flowing through a common administration tubing or site should be discontinued while cefuroxime is being infused unless the solutions are known to be compatible and the flow rate is adequately controlled. If an aminoglycoside is administered concomitantly with cefuroxime, the drugs should be administered at separate sites.

Reconstitution and Dilution

Reconstitute 7.5-g pharmacy bulk vial according to the manufacturer’s directions and then further dilute in a compatible IV infusion solution.

Reconstitute ADD-Vantage (TwistVial) vials containing 750 mg or 1.5 g according to the manufacturer’s directions.

Reconstitute (activate) commercially available Duplex drug delivery system containing 750 mg or 1.5 g of crystalline cefuroxime and 50 mL of dextrose injection in separate chambers according to the manufacturer’s directions.

Thaw the commercially available premixed cefuroxime injection (frozen) at room temperature (25°C) or in a refrigerator (5°C); do not force thaw by immersion in a water bath or by exposure to microwave radiation. A precipitate may have formed in the frozen injection, but should dissolve with little or no agitation after reaching room temperature. Discard thawed injection if an insoluble precipitate is present or if container seals or outlet ports are not intact or leaks are found. Do not use in series connections with other plastic containers; such use could result in air embolism from residual air being drawn from the primary container before administration of fluid from the secondary container is complete.

Rate of Administration

Intermittent IV infusions generally infused over 15–60 minutes.

IM Injection

Administer IM injections deeply into a large muscle mass such as the gluteus or lateral aspect of the thigh. Use aspiration to ensure needle is not in a blood vessel.

Reconstitution

Prepare IM injections by reconstituting vial containing 750 mg of cefuroxime with 3 mL of sterile water for injection to provide a suspension containing approximately 220 mg/mL.

Shake IM suspension gently prior to administration.

Dosage

Available as cefuroxime axetil or cefuroxime sodium ; dosage expressed in terms of cefuroxime.

Tablets and oral suspension are not bioequivalent and are not substitutable on a mg/mg basis.

Pediatric Patients

General Pediatric Dosage

Neonates

IV or IM

Neonates ≤7 days of age: 50 mg/kg every 12 hours, regardless of weight.

Neonates 8–28 days of age: 50 mg/kg every 8–12 hours for those weighing ≤2 kg or 50 mg/kg every 8 hours for those weighing >2 kg.

Mild to Moderate Infections

Oral

Children beyond neonatal period: AAP recommends 20–30 mg/kg daily given in 2 divided doses.

IV or IM

Children beyond neonatal period: AAP recommends 75–100 mg/kg daily given in 3 divided doses.

Children ≥3 months of age: Manufacturer states 50–100 mg/kg daily given in 3 or 4 equally divided doses has been effective for most infections in children .

Severe Infections

Oral

Oral route inappropriate for severe infections per AAP.

IV or IM

Children beyond neonatal period: AAP recommends 100–200 mg/kg daily given in 3 or 4 divided doses.

Children ≥3 months of age: Manufacturer recommends 100 mg/kg daily given in 3 or 4 equally divided doses.

Acute Otitis Media (AOM)

Children 3 Months to 12 Years of Age

Oral

Tablets (for children able to swallow tablets whole): 250 mg twice daily for 10 days.

Oral suspension: 30 mg/kg daily (maximum 1 g daily) given in 2 divided doses for 10 days.

Has been given in a 5-day regimen^{† [off-label]}. AAP does not recommend oral anti-infective regimens of <10 days’ duration in children <2 years of age or in patients with severe symptoms.

Pharyngitis and Tonsillitis

Children 3 Months to 12 Years of Age

Oral

Oral suspension: 20 mg/kg daily (maximum 500 mg daily) in 2 divided doses for 10 days.

Adolescents ≥13 Years of Age

Oral

Tablets: 250 mg twice daily for 10 days.

Bone and Joint Infections

Children 3 Months to 12 Years of Age

IV or IM

150 mg/kg daily given in equally divided doses every 8 hours.

Meningitis

Children 3 Months to 12 Years of Age

IV or IM

200–240 mg/kg daily given in equally divided doses every 6–8 hours.

Respiratory Tract Infections

Acute Sinusitis in Children 3 Months to 12 Years of Age

Oral

Tablets (for children able to swallow tablets whole): 250 mg twice daily for 10 days.

Oral suspension: 30 mg/kg daily (maximum 1 g daily) given in 2 divided doses for 10 days.

Acute Sinusitis in Adolescents ≥13 Years of Age

Oral

Tablets: 250 mg twice daily for 10 days.

Secondary Bacterial Infections of Acute Bronchitis in Adolescents ≥13 Years of Age

Oral

Tablets: 250 or 500 mg twice daily for 5–10 days.

Acute Exacerbations of Chronic Bronchitis in Adolescents ≥13 Years of Age

Oral

Tablets: 250 or 500 mg twice daily for 10 days. Efficacy of regimens <10 days has not been established.

Skin and Skin Structure Infections

Impetigo in Children 3 Months to 12 Years of Age

Oral

Oral suspension: 30 mg/kg daily (maximum 1 g daily) in 2 divided doses for 10 days.

Uncomplicated Infections in Adolescents ≥13 Years of Age

Oral

Tablets: 250 or 500 mg twice daily for 10 days.

Urinary Tract Infections (UTIs)

Uncomplicated Infections in Adolescents ≥13 Years of Age

Oral

Tablets: 250 mg twice daily for 7–10 days.

Gonorrhea and Associated Infections

Uncomplicated Urethral, Cervical, or Rectal Gonorrhea In Adolescents ≥13 Years of Age

Oral

Tablets: 1 g as a single dose recommended by manufacturer.

Not recommended by CDC as first-line treatment. (See Gonorrhea and Associated Infections under Uses.)

Lyme Disease

Early Localized or Early Disseminated Lyme Disease Manifested as Erythema Migrans

Oral

Tablets: 500 mg twice daily for 20 days in adolescents ≥13 years of age.

AAP, IDSA, and others recommend 30 mg/kg (maximum 500 mg) administered in 2 divided doses for 14 days (range 14–21 days) in children without specific neurologic involvement or advanced AV heart block.

Early Neurologic Lyme Disease†

Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA for children with cranial nerve palsy alone without clinical evidence of meningitis.

Lyme Carditis†

Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA.

Borrelial Lymphocytoma†

Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 14 days (range 14–21 days) recommended by IDSA.

Lyme Arthritis†

Oral

30 mg/kg daily in 2 equally divided doses (up to 500 mg per dose) for 28 days recommended by IDSA for children with uncomplicated Lyme arthritis without clinical evidence of neurologic disease.

Perioperative Prophylaxis

Cardiac, Cardiothoracic, or Noncardiac Thoracic Surgery

IV

50 mg/kg given within 1 hour prior to incision. If procedure is prolonged (>4 hours) or if major blood loss occurs, additional 50-mg/kg doses may be given. No evidence of benefit beyond 48 hours and no evidence to support continuing prophylaxis until all drains and indwelling catheters are removed.

Adults

General Adult Dosage

IV or IM

750–1.5 g every 8 hours for 5–10 days.

Life-threatening Infections or Those Caused by Less Susceptible Organisms

IV or IM

1.5 g every 6 hours.

Pharyngitis and Tonsillitis

Oral

Tablets: 250 mg twice daily for 10 days.

Bone and Joint Infections

IV or IM

1.5 g every 8 hours.

Meningitis

IV or IM

Up to 3 g every 8 hours.

Respiratory Tract Infections

Acute Sinusitis

Oral

Tablets: 250 mg twice daily for 10 days.

Secondary Bacterial Infections of Acute Bronchitis

Oral

Tablets: 250 or 500 mg twice daily for 5–10 days.

Acute Exacerbations of Chronic Bronchitis

Oral

Tablets: 250 or 500 mg twice daily for 10 days. Efficacy of regimens <10 days has not been established.

Pneumonia

Oral

500 mg twice daily recommended by ATS and IDSA for empiric treatment of community-acquired pneumonia^† (CAP). Must be used in conjunction with other anti-infectives for empiric treatment of CAP. (See Respiratory Tract Infections under Uses.)

IV or IM

750 mg every 8 hours. For severe or complicated infections, 1.5 g every 8 hours.

Skin and Skin Structure Infections

Uncomplicated Infections

Oral

Tablets: 250 or 500 mg twice daily for 10 days.

IV or IM

750 mg every 8 hours.

Severe or Complicated Infections

IV or IM

1.5 g every 8 hours.

Urinary Tract Infections (UTIs)

Uncomplicated Infections

Oral

Tablets: 250 mg twice daily for 7–10 days.

IV or IM

750 mg every 8 hours.

Severe or Complicated Infections

IV or IM

1.5 g every 8 hours.

Gonorrhea and Associated Infections

Uncomplicated Urethral, Cervical, or Rectal Gonorrhea

Oral

Tablets: 1 g as a single dose has been used.

Not recommended by CDC as first-line treatment. (See Gonorrhea and Associated Infections under Uses.)

IM

1.5 g as a single dose recommended by manufacturer; divide the dose, give at 2 different sites. Given in conjunction with 1 g of oral probenecid.

Not included in CDC recommendations. (See Uncomplicated Gonorrhea under Uses: Gonorrhea and Associated Infections.)

Disseminated Gonococcal Infections

IV or IM

750 mg every 8 hours recommended by manufacturer.

Not included in CDC recommendations. (See Gonorrhea and Associated Infections under Uses.)

Lyme Disease

Early Localized or Early Disseminated Lyme Disease Manifested as Erythema Migrans

Oral

Tablets: 500 mg twice daily for 20 days.

IDSA and others recommend 500 mg twice daily for 14 days (range 14–21 days) in adults without specific neurologic involvement or advanced AV heart block.

Early Neurologic Lyme Disease†

Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA for adults with cranial nerve palsy alone without clinical evidence of meningitis.

Lyme Carditis†

Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA.

Borrelial Lymphocytoma†

Oral

500 mg twice daily for 14 days (range 14–21 days) recommended by IDSA.

Lyme Arthritis†

Oral

500 mg twice daily for 28 days recommended by IDSA for adults with uncomplicated Lyme arthritis without clinical evidence of neurologic disease.

Perioperative Prophylaxis

Cardiac Surgery

IV

For open-heart surgery, manufacturers recommend 1.5 g given at the time of induction of anesthesia and 1.5 g every 12 hours thereafter for a total dosage of 6 g.

For cardiac procedures, some experts recommend 1.5 g given within 1 hour prior to surgical incision and additional 1.5-g doses every 4 hours during prolonged procedures (>4 hours) or if major blood loss occurs.

Various data support a duration of perioperative prophylaxis ranging from a single preoperative dose to continuation for 24 hours postoperatively; no evidence of benefit beyond 48 hours and no evidence to support continuing prophylaxis until all drains and indwelling catheters are removed.

Other Surgery

IV or IM

Manufacturer recommends 1.5 g given IV just prior to surgery (approximately 0.5–1 hour prior to initial incision) and, in lengthy operations, 750 mg given IV or IM every 8 hours. Postoperative doses usually unnecessary and may increase risk of bacterial resistance.

Some experts recommend 1.5 g given within 1 hour prior to surgical incision and additional 1.5-g doses every 4 hours during prolonged procedures (>4 hours) or if major blood loss occurs.

Special Populations

Renal Impairment

Dosage adjustments of parenteral cefuroxime necessary in patients with Cl_cr ≤20 mL/minute.

Adults with impaired renal function: 750 mg IM or IV every 12 hours in those with Cl_cr 10–20 mL/minute or 750 mg IM or IV every 24 hours in those with Cl_cr <10 mL/minute.

Patients undergoing hemodialysis: Give a supplemental dose of parenteral cefuroxime after each dialysis period.

Children with impaired renal function: Make adjustments to dosing frequency for IM or IV cefuroxime similar to those recommended for adults with renal impairment.

Safety and efficacy of oral cefuroxime in patients with renal impairment not established.

Geriatric Patients

Cautious dosage selection because of age-related decreases in renal function. (See Renal Impairment under Dosage and Administration.)

Cautions for Cefuroxime

Contraindications

• Known hypersensitivity to cefuroxime or other cephalosporins.

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Possible emergence and overgrowth of nonsusceptible organisms with prolonged therapy. Careful observation of the patient is essential. Institute appropriate therapy if superinfection occurs.

Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile. C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all anti-infectives, including cefuroxime, and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.

Consider CDAD if diarrhea develops during or after therapy and manage accordingly. Obtain careful medical history since CDAD may occur as late as 2 months or longer after anti-infective therapy is discontinued.

If CDAD is suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.

Sensitivity Reactions

Hypersensitivity Reactions

Possible hypersensitivity reactions, including rash (maculopapular or erythematous), pruritus, fever, eosinophilia, urticaria, anaphylaxis, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

If an allergic reaction occurs, discontinue and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).

Cross-hypersensitivity

Partial cross-sensitivity among cephalosporins and other β-lactam antibiotics, including penicillins and cephamycins.

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. Cautious use recommended in individuals hypersensitive to penicillins: avoid use in those who have had an immediate-type (anaphylactic) hypersensitivity reaction and administer with caution in those who have had a delayed-type (e.g., rash, fever, eosinophilia) reaction.

General Precautions

History of GI Disease

Used with caution in patients with a history of GI disease, particularly colitis. (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis under Cautions.)

Prolonged PT

Prolonged PT reported with some cephalosporins.

Monitor PT in patients at risk, including those with renal or hepatic impairment, poor nutritional state, receiving prolonged therapy, or stabilized on anticoagulant therapy. Administer vitamin K when indicated.

Renal Effects

Periodically evaluate renal status during therapy, especially in seriously ill patients receiving maximum dosage.

Caution if used concomitantly with nephrotoxic drugs (e.g., aminoglycosides, potent diuretics). (See Interactions.)

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of cefuroxime and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.

Patients with Meningitis

Mild to moderate hearing loss reported rarely in pediatric patients who received cefuroxime for treatment of meningitis.

Persistence of positive CSF cultures at 18–36 hours reported; clinical importance unknown.

Phenylketonuria

Ceftin oral suspensions containing 125 or 250 mg of cefuroxime/5 mL contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 11.8 or 25.2 mg of phenylalanine/5 mL, respectively.

Sodium Content

Cefuroxime sodium contains approximately 54.2 mg (2.4 mEq) of sodium per g of cefuroxime.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk; use with caution.

Pediatric Use

Safety and efficacy of oral or parenteral cefuroxime not established in children <3 months of age. Other cephalosporins accumulate in neonates resulting in prolonged serum half-life.

Safety and efficacy of oral cefuroxime for treatment of acute bacterial maxillary sinusitis in pediatric patients 3 months to 12 years of age have been established based on safety and efficacy of the drug in adults. In addition, use of oral cefuroxime in pediatric patients is supported by pharmacokinetic and safety data in adult and pediatric patients, clinical and microbiologic data from adequate and well-controlled studies of the treatment of acute bacterial maxillary sinusitis in adults and acute otitis media with effusion in pediatric patients, and postmarketing surveillance of adverse effects.

Tablets should not be crushed for pediatric administration since the drug has a strong, persistent, bitter taste; vomiting was induced aversively in some children who received crushed tablets. The oral suspension should be used in children who cannot swallow tablets whole.

To avoid overdosage, the commercially available Duplex drug delivery system containing 750 mg or 1.5 g of cefuroxime and 50 mL of dextrose injection in separate chambers should not be used in pediatric patients unless the entire 750-mg or 1.5-g dose is required.

Geriatric Use

No overall differences in safety and efficacy in those ≥65 years of age compared with younger adults, but the possibility of increased sensitivity in some geriatric individuals cannot be ruled out.

Substantially eliminated by kidneys; risk of toxicity may be greater in those with impaired renal function. Select dosage with caution; renal function monitoring may be useful because of age-related decreases in renal function. (See Renal Impairment under Dosage and Administration.)

Renal Impairment

Possible decreased clearance and increased serum half-life.

Dosage adjustments of parenteral cefuroxime necessary in patients with Cl_cr ≤20 mL/minute. (See Renal Impairment under Dosage and Administration.)

Safety and efficacy of oral cefuroxime in patients with renal impairment not established.

Common Adverse Effects

GI effects (nausea, vomiting, diarrhea/loose stools), hypersensitivity reactions, local reactions at IV injection sites.

Drug Interactions

Specific Drugs and Laboratory Tests

Cefuroxime Pharmacokinetics

Absorption

Bioavailability

Following oral administration of cefuroxime axetil, the drug is absorbed from the GI tract as the 1-(acetyloxy)ethyl ester and rapidly hydrolyzed to cefuroxime. Cefuroxime axetil has little, if any, microbiologic activity until hydrolyzed in vivo to cefuroxime.

Oral suspension is not bioequivalent to tablets.

In adults receiving film-coated tablets, peak serum concentrations attained approximately 2–3 hours after the dose.

Following oral administration of the oral suspension given with milk or milk products in children, peak serum concentrations attained within 2.7–3.6 hours.

Cefuroxime sodium not appreciably absorbed from the GI tract; must be given parenterally. Following IM administration in healthy adults, peak serum concentrations attained within 15–60 minutes.

In women, serum cefuroxime concentrations are lower when IM injections are given into the gluteus maximus rather than into the thigh.

Food

In adults, bioavailability following oral administration of film-coated tablets averages about 37% when given in the fasting state and 52% when given with or shortly after food.

Absorption increased when cefuroxime axetil given with milk or infant formula. The extent (but not rate) of absorption is substantially greater when administered concomitantly with milk compared with applesauce or fasting.

Distribution

Extent

Following IM or IV administration, widely distributed into body tissues and fluids including pleural fluid, joint fluid, bile, sputum, bone, and aqueous humor.

Therapeutic concentrations may be attained in CSF following IV administration in patients with inflamed meninges.

Readily crosses the placenta and is distributed into milk.

Plasma Protein Binding

33–50%.

Elimination

Metabolism

Following oral administration, cefuroxime axetil rapidly hydrolyzed to cefuroxime by nonspecific esterases in the intestinal mucosa and blood.

Cefuroxime not metabolized.

Elimination Route

Eliminated unchanged principally in urine.

Half-life

Adults: 1.2–1.6 hours following oral administration and 1–2 hours following IV or IM administration.

Neonates and children: Half-life inversely proportional to age.

Special Populations

Patients with renal impairment: Serum half-life prolonged and generally ranges from 1.9–16.1 hours depending on the degree of impairment. Serum half-life of 15–22 hours has been reported in anuric patients.

Stability

Storage

Oral

Tablets

20–25°C or 15–30°C, depending on manufacturer; store in tight container.

For Suspension

2–30°C. Following reconstitution, store immediately at 2–8°C; discard any unused suspension after 10 days.

Parenteral

Powder for Injection or Infusion

15–30°C; protect from light.

Powder for injection and solutions may darken; does not indicate loss of potency.

Reconstituted 750-mg or 1.5-g vials or 7.5-g pharmacy bulk vial are stable for 24 hours at room temperature or 48 hours (750-mg and 1.5-g vials) or 7 days (7.5-g pharmacy bulk vial) at 5°C. More dilute solutions (e.g., 750 mg or 1.5 g in 100 mL of sterile water for injection, 5% dextrose injection, or 0.9% sodium chloride injection) also stable for 24 hours at room temperature or 7 days when refrigerated.

IM suspensions containing 220 mg/mL prepared using sterile water for injection are stable for 24 hours at room temperature or 48 hours at 5°C.

For Injection, for IV Infusion

Reconstituted ADD-Vantage (TwistVial) vials prepared using 5% dextrose injection or 0.9 or 0.45% sodium chloride injection are stable for 24 hours at room temperature or 7 days under refrigeration; joined vials that have not been activated may be used within a 14-day period.

Store Duplex drug delivery system containing 750 mg or 1.5 g of cefuroxime and 50 mL of dextrose injection at 20–25°C (may be exposed to 15–30°C). Following reconstitution (activation), use within 24 hours if stored at room temperature or within 7 days if stored in refrigerator; do not freeze.

Injection (Frozen) for Infusion

-20°C or lower. After thawing, stable for up to 24 hours at room temperature (25°C) or up to 28 days under refrigeration (5°C).

Do not refreeze after thawing.

Compatibility

Parenteral

Solution CompatibilityHID

Sodium bicarbonate not recommended as a diluent.

Drug Compatibility

Actions and Spectrum

• Based on spectrum of activity, classified as a second generation cephalosporin. Generally no more active in vitro against susceptible gram-positive cocci than first generation cephalosporins, but has an expanded spectrum of activity against gram-negative bacteria compared with first generation drugs.

• Usually bactericidal.

• Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.

• Spectrum of activity includes many gram-positive aerobic bacteria, some gram-negative aerobic bacteria, and some anaerobic bacteria; inactive against Chlamydia, fungi, and viruses.

• Gram-positive aerobes: Active in vitro and in clinical infections against Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, S. pyogenes (group A β-hemolytic streptococci), and other streptococci. Oxacillin-resistant (methicillin-resistant) staphylococci, Listeria monocytogenes, and most enterococci (e.g., Enterococcus faecalis) are resistant.

• Strains of staphylococci resistant to penicillinase-resistant penicillins (oxacillin-resistant staphylococci) should be considered resistant to cefuroxime and cefuroxime axetil, although results of in vitro susceptibility tests may indicate that the organisms are susceptible to the drug. In addition, β-lactamase-negative, ampicillin-resistant (BLNAR) strains of H. influenzae should be considered resistant to cefuroxime and cefuroxime axetil despite the fact that results of in vitro susceptibility tests may indicate that the organisms are susceptible to the drug.

• Gram-negative aerobes: Active in vitro and in clinical infections against Citrobacter, Enterobacter, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), H. parainfluenzae, Klebsiella (including K. pneumoniae), Moraxella catarrhalis (including ampicillin-resistant strains), Morganella morganii, Neisseria gonorrhoeae, N. meningitidis, Proteus mirabilis, Providencia rettgeri, Salmonella, and Shigella. Some strains of Citrobacter, E. cloacae, and M. morganii are resistant. Acinetobacter calcoaceticus, Legionella, Campylobacter, Pseudomonas, P. vulgaris, Serratia usually are resistant.

• Anaerobes: Active in vitro against Bacteroides (except B. fragilis), Clostridium (except C. difficile), Fusobacterium, Peptococcus, and Peptostreptococcus.

Advice to Patients

• Advise patients that antibacterials (including cefuroxime) should only be used to treat bacterial infections; they do not treat viral infections (e.g., the common cold).

• Importance of completing full course of therapy, even if feeling better after a few days.

• Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with cefuroxime or other antibacterials in the future.

• Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued. Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.

• Advise individuals with phenylketonuria and other individuals who must restrict their intake of phenylalanine that Ceftin oral suspensions contain aspartame (NutraSweet), which is metabolized in the GI tract to phenylalanine.

• Importance of informing clinicians if an allergic reaction occurs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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