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Cefuroxime

Pronunciation

Pronunciation: SEFF-yur-OX-eem
Class: Antibiotic, Cephalosporin

Trade Names

Ceftin
- Tablets 125 mg
- Tablets 250 mg
- Tablets 500 mg
- Suspension 125 mg/5 mL
- Suspension 250 mg/5 mL

Zinacef
- Powder for Injection 750 mg (2.4 mEq sodium/g)
- Powder for Injection 1.5 g (2.4 mEq sodium/g)
- Powder for Injection 7.5 g (2.4 mEq sodium/g)
- Injection 750 mg (2.4 mEq sodium/g)
- Injection 1.5 g (2.4 mEq sodium/g)

Apo-Cefuroxime (Canada)
ratio-Cefuroxime (Canada)

Pharmacology

Inhibits mucopeptide synthesis in bacterial cell wall.

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Pharmacokinetics

Absorption

Tablets

C max is 2.1 mcg/mL (125 mg dose) to 13.6 mcg/mL (1,000 mg dose). T max is 2.2 to 3 h. AUC is 6.7 mcg•h/mL (125 mg dose) to 50 mcg•h/mL (1,000 mg dose).

Suspension (10 to 20 mg/kg)

C max is 3.3 to 7 mcg/mL. T max is 2.7 to 3.6 h. AUC is 12.4 to 32.8 mcg•h/mL.

IM (750 mg dose)

C max is 27 mcg/mL. T max is about 45 min.

IV

C max is about 50 mcg/mL (750 mg dose) and about 100 mcg/mL (1.5 g dose). T max is 15 min.

Distribution

Cefuroxime is detectable in therapeutic concentrations in pleural and joint fluid, bile, sputum, bone, aqueous humor, and CSF (in those with meningitis). It is 50% protein bound.

Elimination

The t ½ is 1.2 to 1.3 h (tablets), 1.4 to 1.9 h (suspension), and about 80 min (IV/IM). About 50% is excreted unchanged in the urine within 12 h (tablets/suspension) and about 89% over 8 h (IV/IM).

Special Populations

Renal Function Impairment

The t ½ is prolonged. Dosage reduction is recommended.

Indications and Usage

Oral form

Treatment of infections of lower respiratory tract, urinary tract, skin and skin structures; treatment of uncomplicated gonorrhea, otitis media, pharyngitis, and tonsillitis caused by susceptible strains of specific microorganisms. Treatment of early Lyme disease, pharyngitis/tonsillitis, and impetigo.

Parenteral form

Treatment of infections of lower respiratory tract, urinary tract, skin and skin structures, bone and joint; preoperative prophylaxis; treatment of septicemia, gonorrhea, and meningitis caused by susceptible strains of specific microorganisms.

Contraindications

Hypersensitivity to cephalosporins.

Dosage and Administration

Infection
Adults and Children 12 yr of age and older

PO 125 to 500 mg twice daily. IV / IM 750 mg to 1.5 g every 8 h.

Children younger than 12 yr of age

PO 125 to 250 mg twice daily.

Infants and Children older than 3 mo of age

IV / IM 50 to 150 mg/kg/day (not to exceed adult dose) in equally divided doses every 6 to 8 h.

Bacterial Meningitis
Adults and Children 12 yr of age and older

IV / IM Up to 3 g every 8 h.

Infants and Children 3 mo to 12 yr of age

IV / IM 200 to 240 mg/kg/day in divided doses every 6 to 8 h.

Uncomplicated Gonorrhea
Adults and Children 12 yr of age and older

PO 1 g as single dose. IM 1.5 g as single dose.

Preoperative Prophylaxis
Adults

IV / IM 1.5 g 30 min to 1 h before surgery then 750 mg every 8 h for duration of surgery.

General Advice

  • Administer oral form with food to enhance absorption.
  • May crush and mix with food or beverages; however, crushed tablets have strong, persistent bitter taste. Consider alternative therapy if children cannot swallow whole tablets.
  • Reconstituted solution should be light yellow to amber. Do not administer if solution is cloudy or precipitate is present.
  • When giving by IM route, shake IM suspension gently before administration. Aspirate to prevent injection into blood vessel. Inject deeply into large muscle (eg, upper outer quadrant of gluteus muscle or lateral thigh); massage well. Rotate injection sites.
  • When giving by IV route, use direct intermittent infusion. Administer slowly over 3 to 5 min. Change IV sites every 48 to 72 h.
  • For intermittent IV infusion with Y-type administration set, administer over 30 min. and temporarily stop other solutions at Y-site.
  • For continuous infusion, reconstituted solution may be further diluted with D5W or sodium chloride 0.9%.

Storage/Stability

  • Reconstituted solution is stable for 24 h at room temperature. When refrigerated, solution in vials is stable for 48 h; IV solution is stable for 7 days when refrigerated.
  • Completely thaw frozen solution at room temperature before use; do not refreeze.
  • Store sterile powder at room temperature and protect from light.
  • Store tablets at room temperature.

Drug Interactions

Aminoglycosides

Increased risk of nephrotoxicity with parenteral cefuroxime.

Probenecid

Inhibition of renal excretion of cefuroxime.

Incompatibility

Aminoglycosides

Do not add aminoglycosides to cefuroxime solutions because inactivation of both drugs may result; administer at separate sites if concurrent therapy is indicated.

Laboratory Test Interactions

May cause false-positive urine glucose test results with Benedict solution, Fehling solution, or Clinitest tablets but not with enzyme-based tests (eg, Clinistix , Tes-tape ); false-positive test results for proteinuria with acid and denaturization-precipitation tests; false-positive direct Coombs test results in certain patients (eg, those with azotemia); false elevations in urinary 17-ketosteroid values; false-negative reaction in ferricyanide test for blood glucose.

Adverse Reactions

GI

Nausea; vomiting; diarrhea; anorexia; abdominal pain or cramps; flatulence; colitis, including pseudomembranous colitis.

Genitourinary

Pyuria; renal dysfunction; dysuria; reversible interstitial nephritis; hematuria; toxic nephropathy.

Hematologic

Eosinophilia; neutropenia; lymphocytosis; leukocytosis; thrombocytopenia; decreased platelet function; anemia; aplastic anemia; hemorrhage.

Hepatic

Hepatic dysfunction; abnormal LFT results.

Miscellaneous

Hypersensitivity, including Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis; candidal overgrowth; serum sickness–like reactions (eg, skin rashes, polyarthritis, arthralgia, fever); phlebitis, thrombophlebitis, and pain at injection site.

Precautions

Monitor

Response to therapy

Monitor patient's response to therapy. Notify health care provider if infection does not appear to improve or worsens.

Adverse reactions

Monitor patient for GI, DERM, and general body adverse reactions, and signs of superinfection. Inform health care provider if noted and significant. Immediately report severe diarrhea, diarrhea containing blood or pus, or severe abdominal cramping.


Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Safety and efficacy in children younger than 3 mo of age not established.

Hypersensitivity

Reactions range from mild to life-threatening. Administer drug with caution to penicillin-sensitive patients because of possible cross-reactivity.

Renal Function

Use drug with caution in patients with renal function impairment. Dosage adjustment based on renal function may be required.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

Pseudomembranous colitis

Consider in patients in whom diarrhea develops.

Overdosage

Symptoms

Seizures.

Patient Information

  • Instruct patient to complete full course of therapy.
  • Advise patient to take with meals to enhance absorption. If tablet must be crushed, mix with food or beverage.
  • Advise parent to contact health care provider if child is unable to tolerate crushed tablet with food or beverage.
  • Remind patient to check body temperature daily. If fever persists for more than a few days or if high fever (higher than 102°F) or shaking chills are noted, notify health care provider immediately.
  • Advise patient to maintain normal fluid intake while using this medication.
  • Advise diabetic patient to use enzyme-based tests (eg, Clinistix , Testape ) for monitoring urine glucose because drug may give false results with other tests.
  • Instruct patient to report these symptoms to health care provider: nausea, vomiting, diarrhea, skin rash, sore throat, bruising, hives, muscle or joint pain.
  • Instruct patient to report signs of superinfection: black “furry” tongue, white patches in mouth, foul-smelling stools, vaginal itching or discharge.
  • Warn patient that diarrhea that contains blood or pus may be a sign of serious disorders. Tell patient to seek medical care and not to treat at home.
  • Instruct patient to seek emergency care immediately if wheezing or difficulty breathing occurs.

Copyright © 2009 Wolters Kluwer Health.

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