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Cefuroxime: Drug information

Cefuroxime: Drug information
(For additional information see "Cefuroxime: Patient drug information" and see "Cefuroxime: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: Canada
  • APO-Cefuroxime;
  • Auro-Cefuroxime;
  • Ceftin;
  • PRO-Cefuroxime-500 [DSC];
  • RATIO-Cefuroxime [DSC]
Pharmacologic Category
  • Antibiotic, Cephalosporin (Second Generation)
Dosing: Adult

Note: IM is an FDA-approved route and can be given at the same dose as IV. Ceftin oral suspension has been discontinued in the United States for more than 1 year.

Bite wound infection, prophylaxis or treatment

Bite wound infection, prophylaxis or treatment (animal or human bite) (alternative agent) (off-label use): Oral: 500 mg twice daily, in combination with an agent appropriate for anaerobes (Ref). Duration of prophylaxis is 3 to 5 days (Ref). Duration of treatment for established infection typically ranges from 5 to 14 days and varies based on clinical response and patient-specific factors (Ref).

Chronic obstructive pulmonary disease, acute exacerbation

Chronic obstructive pulmonary disease, acute exacerbation: Note: Avoid use in patients with risk factors for Pseudomonas infection or poor outcomes (eg, ≥65 years of age with major comorbidities, FEV1 <50% predicted, frequent exacerbations) (Ref).

Oral: 500 mg twice daily for 5 to 7 days (Ref).

Intra-abdominal infection, mild to moderate, community acquired in patients without risk factors for resistance or treatment failure

Intra-abdominal infection, mild to moderate, community acquired in patients without risk factors for resistance or treatment failure (off-label use):

Cholecystitis, acute: IV: 1.5 g every 8 hours; continue for 1 day after gallbladder removal or until clinical resolution in patients managed nonoperatively (Ref). Note: The addition of anaerobic therapy (eg, metronidazole) is recommended if biliary-enteric anastomosis is present (Ref).

Other intra-abdominal infections (eg, perforated appendix, diverticulitis, intra-abdominal abscess): IV: 1.5 g every 8 hours in combination with metronidazole. Total duration of therapy (which may include transition to oral antibiotics) is 4 to 5 days following adequate source control (Ref); for diverticulitis or uncomplicated appendicitis managed without intervention, duration is 7 to 10 days (Ref).

Lyme disease

Lyme disease (Borrelia spp. infection):

Erythema migrans: Oral: 500 mg twice daily for 14 days (Ref).

Carditis (initial therapy for mild disease [first-degree atrioventricular block with PR interval <300 msec] or step-down therapy after initial parenteral treatment for more severe disease once PR interval <300 msec): Oral: 500 mg twice daily for 14 to 21 days (Ref).

Arthritis without neurologic involvement (alternative agent) (off-label use): Oral: 500 mg twice daily for 28 days (Ref).

Odontogenic soft tissue infection, pyogenic

Odontogenic soft tissue infection, pyogenic (initial therapy for mild infection or step-down therapy after parenteral treatment) (alternative agent) (off-label use):

Note: For patients unable to take penicillin (Ref).

Oral: 500 mg twice daily in combination with metronidazole; continue until clinical resolution, typically for 7 to 14 days. Use in addition to appropriate surgical management (eg, drainage and/or extraction) (Ref).

Otitis media, acute

Otitis media, acute (alternative agent for mild [nonanaphylactic] penicillin allergy) (off-label): Oral: 500 mg twice daily; duration of therapy is 5 to 7 days (mild to moderate infection) or 10 days (severe infection) (Ref).

Pneumonia, community-acquired, outpatient empiric therapy

Pneumonia, community-acquired, outpatient empiric therapy (patients with comorbidities): Oral: 500 mg twice daily as part of an appropriate combination regimen. Duration is for a minimum of 5 days; patients should be clinically stable with normal vital signs before discontinuing therapy (Ref).

Streptococcal pharyngitis, group A

Streptococcal pharyngitis, group A (alternative agent for mild, nonanaphylactic penicillin allergy):

Note: Cephalosporin selection depends on the type of hypersensitivity reaction to penicillin. To avoid the development of resistance, narrower spectrum cephalosporins (eg, cephalexin or cefadroxil) are preferred when possible (Ref).

Oral: 250 mg twice daily for 10 days (Ref).

Surgical prophylaxis

Surgical prophylaxis (eg, cardiac surgery, head and neck surgery) (alternative agent): IV: 1.5 g within 60 minutes prior to surgical incision; use in combination with metronidazole for select head and neck procedures. Cefuroxime dose may be repeated intraoperatively in 4 hours if procedure is lengthy or if there is excessive blood loss (Ref). In cases where an extension of prophylaxis is warranted postoperatively, total duration should be ≤24 hours (Ref). Postoperative prophylaxis is not recommended in clean and clean-contaminated surgeries (Ref).

Urinary tract infection, cystitis, acute uncomplicated or acute simple cystitis

Urinary tract infection, cystitis, acute uncomplicated or acute simple cystitis (infection limited to the bladder without signs/symptoms of upper tract, prostate, or systemic infection) (alternative agent):

Note: Use only when first-line agents cannot be used; limited evidence suggests inferior efficacy of oral beta-lactams (Ref).

Oral: 250 mg twice daily for 5 to 7 days (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function:

Cefuroxime Dose Adjustments in Altered Kidney Function

CrCl (mL/minute)

IV

Oral

If usual recommended dose is 750 mg to 1.5 g every 8 hours

If usual recommended dose is 250 to 500 mg every 12 hours

aExpert opinion derived from concentrations observed in Konishi 1993.

≥30

No dosage adjustment necessary

No dosage adjustment necessary

10 to 30

750 mg to 1.5 g every 12 hours

250 mg every 12 hours (preferred)a or 250 to 500 mg every 24 hours

<10

750 mg to 1.5 g every 24 hours

250 mg every 24 hours (preferred)a or 250 to 500 mg every 48 hours

Augmented renal clearance (measured urinary CrCl ≥130 mL/minute/1.73 m2): Augmented renal clearance (ARC) is a condition that occurs in certain critically ill patients without organ dysfunction and with normal serum creatinine concentrations. Young patients (<55 years of age) admitted post-trauma or major surgery are at highest risk for ARC, as well as those with sepsis, burns, or hematologic malignancies. An 8- to 24-hour measured urinary CrCl is necessary to identify these patients (Ref).

IV:

Extended infusion: 1.5 g infused over 3 hours every 6 hours (Ref).

Continuous infusion: 1.5 g loading dose, followed by 6 g infused over 24 hours every 24 hours (Ref).

Hemodialysis, intermittent (thrice weekly): Dialyzable (enhances plasma clearance by at least 30% (Ref)):

IV, Oral: Dose as for patients with CrCl <10 mL/minute; when scheduled dose falls on a dialysis day, administer after dialysis (Ref).

Peritoneal dialysis:

IV, Oral: Dose as for patients with CrCl <10 mL/minute (Ref).

CRRT: Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement. Recommendations are based on high-flux dialyzers and effluent flow rates of 20 to 25 mL/kg/hour (or ~1,500 to 3,000 mL/hour) unless otherwise noted. Appropriate dosing requires consideration of adequate drug concentrations (eg, site of infection) and consideration of initial loading doses. Close monitoring of response and adverse reactions (eg, neurotoxicity) due to drug accumulation is important.

IV: 1.5 g every 12 hours (Ref).

PIRRT (eg, sustained, low-efficiency diafiltration): Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement. Appropriate dosing requires consideration of adequate drug concentrations (eg, site of infection) and consideration of initial loading doses. Close monitoring of response and adverse reactions (eg, neurotoxicity) due to drug accumulation is important.

IV: 1.5 g every 12 hours (Ref).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Pediatric

(For additional information see "Cefuroxime: Pediatric drug information")

Note: Ceftin oral suspension has been discontinued in the US for >1 year.

General dosing, susceptible infection (Ref): Infants, Children, and Adolescents:

Mild to moderate infection:

Oral: 20 to 30 mg/kg/day divided twice daily; maximum dose: 500 mg/dose.

IM, IV: 75 to 100 mg/kg/day divided in 3 doses; maximum dose: 1,500 mg/dose.

Severe infection: IM, IV: 100 to 200 mg/kg/day divided in 3 to 4 doses; maximum dose: 1,500 mg/dose.

Bone and joint infection

Bone and joint infection: Infants ≥3 months, Children, and Adolescents: IM, IV: 50 mg/kg/dose every 8 hours; maximum dose: 1,500 mg/dose. Note: Upon completion of parenteral therapy follow with oral antibiotic therapy if indicated.

Bronchitis, chronic; acute exacerbations

Bronchitis, chronic; acute exacerbations: Adolescents: Oral tablets: 250 to 500 mg every 12 hours for 10 days.

Impetigo

Impetigo: Infants ≥3 months and Children: Oral suspension: 15 mg/kg/dose twice daily for 10 days; maximum dose: 500 mg/dose.

Intra-abdominal infection complicated, community-acquired

Intra-abdominal infection complicated, community-acquired: Infants, Children, and Adolescents: IV: 150 mg/kg/day in divided doses every 6 to 8 hours; maximum dose: 1,500 mg/dose (Ref).

Lyme disease

Lyme disease ( Borrelia spp. infection): Infants, Children, and Adolescents: Oral: 15 mg/kg/dose every 12 hours; maximum dose: 500 mg/dose. Duration of therapy depends on clinical syndrome; treat erythema migrans and borrelial lymphocytoma for 14 days, carditis for 14 to 21 days, arthritis (initial, recurrent, or refractory) for 28 days, and acrodermatitis chronica atrophicans for 21 to 28 days (Ref).

Otitis media, acute

Otitis media, acute (AOM) (alternative agent for nonanaphylactic penicillin allergy):

Infants ≥3 months, Children, and Adolescents: Oral: 15 mg/kg/dose every 12 hours; maximum dose: 500 mg/dose (Ref). For patients with severe or recurrent AOM, tympanic membrane perforation, or who are <2 years of age, treat for 10 days; for patients ≥2 years of age with mild to moderate, nonrecurrent disease without tympanic membrane perforation, shorter durations of 5 to 7 days may be sufficient (Ref).

Pneumonia, bacterial, HIV-exposed/-infected

Pneumonia, bacterial, HIV-exposed/-infected: Infants and Children: IV: 35 to 50 mg/kg/dose 3 times daily; maximum dose: 2,000 mg/dose (Ref).

Sinusitis

Sinusitis:

Infants ≥3 months and Children:

Oral suspension: 15 mg/kg/dose twice daily for 10 days; maximum dose: 500 mg/dose.

Oral tablet (for patients able to swallow tablet whole): 250 mg twice daily for 10 days.

Adolescents: Oral tablet: 250 mg twice daily for 10 days.

Skin and skin structure infections, uncomplicated

Skin and skin structure infections, uncomplicated: Adolescents: Oral tablet: 250 to 500 mg twice daily for 10 days.

Streptococcus, group A; pharyngitis/tonsillitis

Streptococcus, group A; pharyngitis/tonsillitis (alternative agent for nonanaphylactic penicillin allergy): Note: Narrow-spectrum cephalosporins (eg, cephalexin) are preferred over broad-spectrum cephalosporins such as cefuroxime (Ref).

Infants ≥3 months, Children, and Adolescents: Oral: 10 mg/kg/dose every 12 hours for 10 days; maximum dose: 250 mg/dose (Ref).

Surgical prophylaxis

Surgical prophylaxis: Children and Adolescents: IV: 50 mg/kg within 60 minutes prior to procedure; may repeat dose in 4 hours if procedure is lengthy or if there is excessive blood loss; maximum dose: 1,500 mg/dose (Ref).

Urinary tract infection, uncomplicated

Urinary tract infection, uncomplicated:

Infants and Children 2 to 24 months: Oral suspension: 10 to 15 mg/kg/dose twice daily (Ref).

Children >24 months: Moderate to severe disease (possible pyelonephritis): Oral suspension: 20 to 30 mg/kg/day divided twice daily; maximum dose: 500 mg/dose (Ref).

Adolescents: Oral tablet: 250 mg twice daily for 7 to 10 days.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Infants, Children, and Adolescents:

Oral: There are no dosage adjustments provided in the manufacturer's labeling; however, the following adjustments have been reported in the literature (Ref): Note: Renally adjusted dose recommendations are based on doses of 30 mg/kg/day divided every 12 hours:

GFR ≥30 mL/minute/1.73 m2: No adjustment required

GFR 10 to 29 mL/minute/1.73 m2: Administer 15 mg/kg/dose every 12 hours

GFR <10 mL/minute/1.73 m2: Administer 15 mg/kg/dose every 24 hours

Intermittent hemodialysis: Administer 15 mg/kg/dose every 24 hours

Peritoneal dialysis (PD): Administer 15 mg/kg/dose every 24 hours

IV: The manufacturer's labeling recommends decreasing the frequency similar to adult recommendations. The following guidelines have been used by some clinicians (Ref). Note: Renally adjusted dose recommendations are based on doses of 75 to 150 mg/kg/day divided every 8 hours.

GFR ≥30 mL/minute/1.73 m2: No adjustment required

GFR 10 to 29 mL/minute/1.73 m2: Administer 25 to 50 mg/kg/dose every 12 hours

GFR <10 mL/minute/1.73 m2: Administer 25 to 50 mg/kg/dose every 24 hours

Intermittent hemodialysis: Administer 25 to 50 mg/kg/dose every 24 hours

Peritoneal dialysis (PD): Administer 25 to 50 mg/kg/dose every 24 hours

Continuous renal replacement therapy (CRRT): Administer 25 to 50 mg/kg/dose every 8 hours

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Reconstituted, Injection, as sodium [strength expressed as base, preservative free]:

Generic: 750 mg (1 ea); 7.5 g (1 ea [DSC])

Solution Reconstituted, Intravenous, as sodium [strength expressed as base, preservative free]:

Generic: 1.5 g (1 ea)

Tablet, Oral, as axetil [strength expressed as base]:

Generic: 250 mg, 500 mg

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Reconstituted, Intravenous, as sodium [strength expressed as base]:

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 (70 mL, 100 mL) [contains aspartame]

Tablet, Oral, as axetil [strength expressed as base]:

Ceftin: 250 mg [DSC], 500 mg [DSC] [contains methylparaben, propylparaben, sodium benzoate]

Generic: 250 mg, 500 mg

Product Availability

Ceftin oral suspension has been discontinued in the US for more than 1 year.

Administration: Adult

Oral suspension: Administer with food. Shake well before use.

Oral tablet: May administer with or without food (absorption improved with food). Swallow tablet whole (crushed tablet has strong, persistent, bitter taste).

IM: Inject deep IM into large muscle mass.

IV: Inject direct IV over 3 to 5 minutes. Infuse intermittent infusion over 15 to 30 minutes.

Administration: Pediatric

Oral: Cefuroxime axetil suspension must be administered with food; shake suspension well before use; tablets may be administered with or without food; administer with food to decrease GI upset; avoid crushing the tablet due to its bitter taste

Parenteral:

IM: Inject deep IM into large muscle mass, such as gluteus or lateral part of thigh

Intermittent IV infusion: Administer over 15 to 30 minutes

IV Push: Administer over 3 to 5 minutes

Use: Labeled Indications

Bone and joint infections (injection only): Treatment of bone and joint infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).

Chronic obstructive pulmonary disease, acute exacerbation (tablets only): Treatment of mild to moderate acute bacterial exacerbations of chronic bronchitis in adults and adolescents ≥13 years of age caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains), or Haemophilus parainfluenzae (beta-lactamase negative strains).

Lower respiratory tract infections (injection only): Treatment of lower respiratory tract infections, including pneumonia, caused by S. pneumoniae, H. influenzae (including ampicillin-resistant strains), Klebsiella spp., S. aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, and Escherichia coli.

Lyme disease (early) (tablets only): Treatment of adults and adolescents ≥13 years of age with early Lyme disease (eg, erythema migrans, carditis) caused by Borrelia burgdorferi.

Otitis media, acute (tablets and oral suspension only): Treatment of pediatric patients ≥3 months of age with acute bacterial otitis media caused by S. pneumoniae, H. influenzae (including beta-lactamase-producing strains), Moraxella catarrhalis (including beta-lactamase-producing strains), or S. pyogenes.

Septicemia (injection only): Treatment of septicemia caused by S. aureus (penicillinase- and non-penicillinase-producing strains), S. pneumoniae, E. coli, H. influenzae (including ampicillin-resistant strains), and Klebsiella spp.

Sinusitis, acute bacterial (tablets and oral suspension only): Treatment of mild to moderate acute bacterial maxillary sinusitis caused by S. pneumoniae or H. influenzae (non-beta-lactamase-producing strains only).

Limitations of use: Effectiveness for sinus infections caused by beta-lactamase-producing H. influenzae or M. catarrhalis in patients with acute bacterial maxillary sinusitis has not been established. Note: According to the IDSA guidelines for acute bacterial rhinosinusitis, cefuroxime is no longer recommended as monotherapy for initial empiric treatment (IDSA [Chow 2012]).

Skin and skin-structure infections (impetigo) (oral suspension only): Treatment of pediatric patients 3 months to 12 years of age with skin or skin-structure infections (impetigo) caused by S. aureus (including beta-lactamase-producing strains) or S. pyogenes.

Skin and skin-structure infections (injection; tablets [uncomplicated infections only]): Treatment of adults and pediatric patients >3 months of age with skin and skin-structure infections (including impetigo) caused by S. aureus (penicillinase- and non-penicillinase-producing strains), S. pyogenes, E. coli, Klebsiella spp., and Enterobacter spp.

Streptococcal pharyngitis, group A (tablets and oral suspension only): Treatment of mild to moderate pharyngitis/tonsillitis caused by S. pyogenes in adults and pediatric patients ≥3 months of age.

Limitations of use: Efficacy in the prevention of rheumatic fever has not been established in clinical trials. Efficacy in the treatment of penicillin-resistant strains of S. pyogenes has not been demonstrated.

Surgical prophylaxis (injection only): Prophylaxis of infection in patients undergoing surgical procedures that are classified as clean-contaminated or potentially contaminated procedures.

Urinary tract infection (tablets and injection only): Treatment of adults and pediatric patients >3 months of age with urinary tract infection caused by E. coli and Klebsiella spp.

Use: Off-Label: Adult

Bite wound, prophylaxis or treatment (animal or human bite); Intra-abdominal infection, mild to moderate, community acquired in patients without risk factors for resistance or treatment failure; Lyme disease (Borrelia spp. infection), arthritis without neurologic involvement; Odontogenic soft tissue infection, pyogenic

Medication Safety Issues
Sound-alike/look-alike issues:

Cefuroxime may be confused with cefotaxime, cefprozil, deferoxamine, sulfaSALAzine

Ceftin may be confused with Cefzil, Cipro

Zinacef may be confused with Zithromax

International issues:

Ceftin [US, Canada] may be confused with Cefiton brand name for cefixime [Portugal]; Ceftim brand name for ceftazidime [Portugal]; Ceftime brand name for ceftazidime [Thailand]

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Gastrointestinal: Diarrhea (4% to 11%; duration dependent)

1% to 10%:

Cardiovascular: Local thrombophlebitis (2%)

Dermatologic: Diaper rash (children: 3%)

Endocrine & metabolic: Increased lactate dehydrogenase (1%)

Gastrointestinal: Nausea and vomiting (3% to 7%), unpleasant taste (children: 5%)

Genitourinary: Vaginitis (≤5%)

Hematologic & oncologic: Decreased hematocrit (≤10%), decreased hemoglobin (≤10%), eosinophilia (1% to 7%)

Hepatic: Increased serum alanine aminotransferase (2%), increased serum alkaline phosphatase (2%), increased serum aspartate aminotransferase (2%)

Immunologic: Jarisch-Herxheimer reaction (6%)

<1%:

Cardiovascular: Chest pain, chest tightness, tachycardia

Dermatologic: Erythema of skin, pruritus, skin rash, urticaria

Endocrine & metabolic: Increased thirst

Gastrointestinal: Abdominal pain, anorexia, dyspepsia, flatulence, gastrointestinal infection, oral mucosa ulcer, sialorrhea, stomach cramps, swollen tongue

Genitourinary: Dysuria, urethral bleeding, urethral pain, urinary tract infection, vaginal discharge, vaginal irritation, vulvovaginal candidiasis, vulvovaginal pruritus

Hematologic & oncologic: Neutropenia, positive direct Coombs test

Hepatic: Hyperbilirubinemia

Infection: Candidiasis, viral infection

Nervous system: Chills, dizziness, drowsiness, drug fever, headache, hyperactive behavior, irritability, trismus

Neuromuscular & skeletal: Arthralgia, joint swelling, muscle cramps, muscle rigidity, muscle spasm (neck)

Otic: Hearing loss

Renal: Renal pain

Respiratory: Cough, dyspnea, sinusitis, upper respiratory tract infection

Miscellaneous: Fever

Postmarketing:

Cardiovascular: Hypersensitivity angiitis

Dermatologic: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis

Gastrointestinal: Cholestasis, Clostridioides difficile-associated diarrhea, Clostridioides difficile colitis, colitis

Hematologic & oncologic: Hemolytic anemia, leukopenia, pancytopenia, prolonged prothrombin time, thrombocytopenia

Hepatic: Hepatitis, jaundice

Hypersensitivity: Anaphylaxis, angioedema, hypersensitivity reaction (may include ischemic heart disease with or without acute myocardial infarction)

Immunologic: Serum sickness-like reaction

Nervous system: Encephalopathy, seizure

Renal: Decreased creatinine clearance, increased blood urea nitrogen, increased serum creatinine, interstitial nephritis, renal insufficiency

Contraindications

Hypersensitivity to cefuroxime, any component of the formulation, or other beta-lactam antibacterial drugs (eg, penicillins and 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.

• Hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving beta-lactam drugs. Before initiating therapy, carefully investigate previous penicillin, cephalosporin, or other allergen hypersensitivity. Use caution if given to a patient with a penicillin or other beta-lactam allergy because cross sensitivity among beta-lactam antibacterial drugs has been established. If an allergic reaction occurs, discontinue and institute appropriate therapy.

• 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:

• Gastrointestinal disease: Use with caution in patients with a history of colitis.

• Renal impairment: Use with caution in patients with renal impairment; modify dosage in severe impairment.

• Seizure disorders: Use with caution in patients with a history of seizure disorder; cephalosporins have been associated with seizure activity, particularly in patients with renal impairment not receiving dose adjustments. Discontinue if seizures occur.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

• Phenylalanine: Some products may contain phenylalanine.

• Tablets: Should not be crushed or chewed due to a strong, persistent bitter taste.

Metabolism/Transport Effects

Substrate of OAT1/3

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Aminoglycosides: Cephalosporins may enhance the nephrotoxic effect of Aminoglycosides. Cephalosporins may decrease the serum concentration of Aminoglycosides. Risk C: Monitor therapy

Antacids: May decrease the serum concentration of Cefuroxime. Management: Administer cefuroxime axetil at least 1 hour before or 2 hours after the administration of short-acting antacids. Risk D: Consider therapy modification

Bacillus clausii: Antibiotics may diminish the therapeutic effect of Bacillus clausii. Management: Bacillus clausii should be taken in between antibiotic doses during concomitant therapy. Risk D: Consider therapy modification

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Risk C: Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Risk X: Avoid combination

Furosemide: May enhance the nephrotoxic effect of Cephalosporins. Risk C: Monitor therapy

Histamine H2 Receptor Antagonists: May decrease the absorption of Cefuroxime. Separate oral doses by at least 2 hours. Risk X: Avoid combination

Immune Checkpoint Inhibitors: Antibiotics may diminish the therapeutic effect of Immune Checkpoint Inhibitors. Risk C: Monitor therapy

Inhibitors of the Proton Pump (PPIs and PCABs): May decrease the absorption of Cefuroxime. Risk X: Avoid combination

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. 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: Avoid use of live attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid starting antibiotics within 3 days of last vaccine dose. 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

Bioavailability is increased with food; cefuroxime serum levels may be increased if taken with food or dairy products. Clinical and bacteriologic responses were independent of food intake in clinical trials. Management: Administer tablet without regard to meals; suspension must be administered with food.

Pregnancy Considerations

Cefuroxime crosses the placenta (Dallmann 2017; Lalic-Popovic 2016).

An increased risk of major birth defects or other adverse fetal or maternal outcomes has generally not been observed following maternal use of cephalosporin antibiotics, including cefuroxime.

Due to pregnancy-induced physiologic changes, some pharmacokinetic properties of cefuroxime may be altered (Dallmann 2017; Lalic-Popovic 2016).

Cefuroxime is one of the antibiotics effective for prophylactic use prior to cesarean delivery (ACOG 2018). Cefuroxime is used for the treatment of Lyme disease. Vertical transmission from mother to fetus is not well documented; it is unclear if infection increases the risk of adverse pregnancy outcomes. When treatment for Lyme disease in pregnancy is needed, the indications and dosing of cefuroxime are the same as in nonpregnant patients (IDSA/AAN/ACR [Lantos 2021]; Lambert 2020; SOGC [Smith 2020]).

Breastfeeding Considerations

Cefuroxime is present in breast milk.

The relative infant dose (RID) of cefuroxime is 0.5% when calculated using the highest breast milk concentration located and compared to an oral infant therapeutic dose of 30 mg/kg/day.

In general, breastfeeding is considered acceptable when the RID is <10% (Anderson 2016; Ito 2000).

The RID of cefuroxime was calculated using the highest milk concentration located (1.05 mcg/mL), providing an estimated daily infant dose via breast milk of 0.158 mg/kg/day. This milk concentration was obtained 0.5 to 1.5 hours following maternal administration of oral cefuroxime axetil 500 mg (Vree 1990).

Diarrhea has been reported in breastfeeding infants exposed to cefuroxime (Benyami 2005). In general, antibiotics that are present in breast milk may cause non-dose-related modification of bowel flora. Monitor infants for GI disturbances, such as thrush and diarrhea (WHO 2002).

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Beta-lactam antibiotics are generally considered compatible with breastfeeding when used in usual recommended doses; cefuroxime was not specifically included within this report (WHO 2002).

Dietary Considerations

Some products may contain phenylalanine and/or sodium.

Oral suspension: Should be taken with food.

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.

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

Absorption: Oral tablet: Increases with food.

Distribution: Widely to body tissues and fluids including bronchial secretions, synovial and pericardial fluid, kidneys, heart, liver, bone and bile; crosses blood-brain barrier.

Vd:

Infants and children ≤6 years of age: 0.65 L/kg (del Rio 1982).

Adults: 50 ± 28 L (Nix 1997).

Brain tissue:blood ratio, steady state (AUC): 33% (Hosman 2018).

Protein binding: 33% to 50%.

Metabolism: Cefuroxime axetil (oral) is hydrolyzed in the intestinal mucosa and blood to cefuroxime.

Bioavailability: Tablet: Fasting: 37%; Following food: 52%; Cefuroxime axetil suspension is less bioavailable than the tablet (91% of the AUC for tablets).

Half-life elimination:

Premature neonates:

PNA ≤3 days: Median: 5.8 hours (de Louvois 1982).

PNA ≥8 days: Median: 1.6 to 3.8 hours (de Louvois 1982).

Children and adolescents: 1.4 to 1.9 hours.

Adults: ~1 to 2 hours; prolonged with renal impairment.

Time to peak, serum: IM: ~15 to 60 minutes; IV: 2 to 3 minutes; Oral: Children: ~3 to 4 hours; Adults: ~2 to 3 hours.

Excretion: Urine (66% to 100% as unchanged drug).

Pharmacokinetics: Additional Considerations

Anti-infective considerations:

Parameters associated with efficacy:

Time dependent, associated with free time (fT) drug concentration > minimum inhibitory concentration (MIC); goal: ≥40% fT > MIC (Craig 1998; Nielsen 2011).

Expected drug exposure in patients with normal renal function:

Infants and children ≤6 years of age: Cmax (peak): IV, single dose:

50 mg/kg: 105 ± 36 mg/L (del Rio 1982).

Children 7 to 12 years of age: Cmax (peak): Oral (tablet), single dose:

500 mg (fed): 4.3 to 5.7 mg/L (Ginsburg 1985).

500 mg (fasting): 3.8 to 3.9 mg/L (Ginsburg 1985).

Adults: Cmax (peak):

IV: 1.5 g, single dose: 100 mg/L.

Oral (tablet), steady state:

250 mg (fed): 4.1 mg/L.

500 mg (fed): 7 mg/L.

500 mg (fasted): 4.9 mg/L.

Postantibiotic effect: H. influenzae: 0 to ~1.4 hours; M. catarrhalis: 0 to ~1.4 hours; S. pneumoniae: ~0.2 to 2.9 hours; S. pyogenes: 0 to ~1.75 hours; S. aureus: Not observed in most isolates (Craig 1993; Davies 2000; Dubois 2000).

Pricing: US

Solution (reconstituted) (Cefuroxime Sodium Injection)

750 mg (per each): $2.70 - $3.67

Solution (reconstituted) (Cefuroxime Sodium Intravenous)

1.5 g (per each): $5.40 - $7.01

Tablets (Cefuroxime Axetil Oral)

250 mg (per each): $4.39 - $5.66

500 mg (per each): $8.02 - $11.11

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Actixim (VN);
  • Adrox (BD);
  • Aksef (UA);
  • Alporin (KR);
  • Altacef (PH);
  • Altamax (PH);
  • Anbacim (ID);
  • Aprok (IE);
  • Aprokam (BE, DE, FR, GB);
  • Axet (PH);
  • Axetine (BH, CN, NZ, PH, SG);
  • Axim (BD, HK);
  • Bacticef (IN);
  • C-Tri T (TH);
  • Carvixime (PH);
  • Cef2 (TZ);
  • Cefabiot (MX);
  • Cefasun (IN);
  • Cefero (LK);
  • Cefmono (PH);
  • Cefora (LB);
  • Cefosan (PH);
  • Ceftil (KR);
  • Cefudura (DE);
  • Cefuhexal (DE);
  • Cefumax (EG, LB, PH);
  • Cefuracet (MX);
  • Cefurax (DE);
  • Cefuro-Puren (DE);
  • Cefurocos (ZW);
  • Cefurox (TH);
  • Cefurox-wolff (DE);
  • Cefutil (AE, CY, ET, IQ, IR, JO, KW, LY, OM, SA, SY, YE);
  • Cefutin (KR);
  • Cefuxime (HK, KR);
  • Cefuzime (BH);
  • Cefxin (SG, TW);
  • Cefzime (PH);
  • Celocid (ID);
  • Ceprosim (KR);
  • Cerox A (BD);
  • Ceroxim (ZA, ZW);
  • Cethixim (ID);
  • Cetil (ET, IN, PE);
  • Cetoxil (MX);
  • Cexil (KR);
  • Cexim (HU);
  • CMaxid (HK);
  • Cortum (PH);
  • Curocef (AT, CL);
  • Curoxime (PT);
  • Daliroxim (LK);
  • Daroxime (LB, QA);
  • Daroxine (BH);
  • Deltrox (AR);
  • Efox (HR);
  • Efurox (MY);
  • Elobact (DE);
  • Eroxmit (PH);
  • Famicef (BD);
  • Farmacef (TH);
  • Fornax (PE);
  • Froxime (AE, CY, IQ, IR, JO, KW, LY, OM, SA, SY, YE);
  • Furacam (EC);
  • Furobioxin (MX);
  • Furoxim (PH);
  • Furoxime (TH);
  • Gifro (TW);
  • Glanax (VN);
  • Gomcef (KR);
  • Jectocef (PH);
  • Keef-250 (PH);
  • Kefezy (PH);
  • Kefloxa (ZW);
  • Kefrox (LK);
  • Kefstar (PH);
  • Kefurox (LU);
  • Ketocef (HR);
  • Kimatcef (UA);
  • Magnaspor (TH);
  • Maxil (BH, JO, QA);
  • Medaxetine (VN);
  • Medxime (PH);
  • Milcef (LK);
  • Neurox-250 (TH);
  • Novador (MX);
  • Novocef (HR);
  • Olcef (KR);
  • Oratil (ZW);
  • Oraxim (AE, CY, IQ, IR, JO, KW, LY, OM, SA, SY, YE);
  • Oxtercid (ID);
  • Profurex (PH);
  • Rucef (PH);
  • Sefuxim (HK);
  • Sharox-500 (ID);
  • Shincef (KR);
  • Situroxime (ID);
  • Teikeden (HK);
  • Theoroxime (PH);
  • U-Cef (BH);
  • Unoximed (PH);
  • Uroxime (TW);
  • Vekfazolin (GR);
  • Vexuro (LK);
  • Xorim (QA);
  • Xorimax (HK, MY, PH, QA, SG, VN);
  • Xorufec (MX);
  • Zamur (QA, TT);
  • Zefu (MY);
  • Zegen (PH);
  • Zenon (BH, QA);
  • Zicef (PH);
  • Zilisten (MT);
  • Zinacef (AE, BB, BE, CH, CN, CO, CY, CZ, DK, EE, EG, ES, ET, FI, GB, GR, HU, IE, IS, JO, KW, LB, LK, LT, LU, MT, NL, NO, NZ, PH, PL, PT, QA, RU, SA, SE, SK, TR, UA, VN, ZW);
  • Zinat (CH);
  • Zincef (KR);
  • Zinnat (AE, AT, AU, BB, BE, BF, BH, BJ, BM, BR, BS, BZ, CH, CI, CO, CR, CY, CZ, DE, DK, DO, EC, EE, EG, ES, ET, FI, FR, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IE, IL, IQ, IR, IS, IT, JM, JO, KE, KR, KW, LB, LK, LR, LT, LU, LV, LY, MA, ML, MR, MT, MU, MW, MX, MY, NE, NG, NI, NL, NZ, OM, PA, PE, PH, PK, PL, PR, PY, QA, RO, SA, SC, SD, SG, SK, SL, SN, SR, SV, SY, TH, TN, TR, TW, TZ, UG, UY, VE, VN, YE, ZA, ZM, ZW);
  • Zinoximor (BH);
  • Zocef (TH, TZ);
  • Zoref (PT)


For country code abbreviations (show table)
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