Usage
Cefuroxime is a second-generation cephalosporin antibiotic prescribed for various bacterial infections. These include:
- Respiratory tract infections: Pharyngitis, tonsillitis, acute bacterial maxillary sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
- Urinary tract infections: Uncomplicated and complicated cystitis and pyelonephritis.
- Skin and soft tissue infections: Impetigo, uncomplicated skin and skin structure infections.
- Other infections: Gonorrhea, Lyme disease, early Lyme disease, otitis media, and meningitis.
- Surgical prophylaxis: Prevention of infections following surgical procedures such as cardiovascular, esophageal, gastrointestinal, gynecological, and orthopedic operations.
Pharmacological Classification: Antibiotic.
Mechanism of Action: Cefuroxime inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs). This binding disrupts the cross-linking of peptidoglycans, essential components of the bacterial cell wall, ultimately leading to bacterial cell lysis and death.
Alternate Names
Cefuroxime axetil (oral formulation)
Brand names: Ceftin, Zinacef, Zinnat.
How It Works
Pharmacodynamics: Cefuroxime exerts its bactericidal action by interfering with bacterial cell wall synthesis. It has a broad spectrum of activity against both gram-positive and gram-negative bacteria.
Pharmacokinetics:
- Absorption: Cefuroxime axetil, the oral prodrug, is absorbed from the gastrointestinal tract and hydrolyzed to active cefuroxime. Absorption is enhanced when taken with food.
- Distribution: Cefuroxime is widely distributed in the body, achieving therapeutic concentrations in various tissues and fluids, including bone, pleural fluid, sputum, and cerebrospinal fluid. Protein binding is approximately 33% to 50%.
- Metabolism: Cefuroxime axetil is metabolized to the active compound cefuroxime.
- Elimination: Cefuroxime is primarily eliminated by the kidneys via glomerular filtration and tubular secretion. The elimination half-life is approximately 1 to 2 hours in adults with normal renal function.
Mode of Action: Cefuroxime inhibits bacterial cell wall synthesis by binding to and inactivating PBPs, leading to cell lysis.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Cefuroxime acts by binding to PBPs, not receptors, enzymes, or neurotransmitters.
Elimination Pathways: Primarily renal excretion.
Dosage
Standard Dosage
Adults:
- Oral: 250 to 500 mg twice daily.
- IV/IM: 750 mg to 1.5 g every 8 hours.
Children:
- Oral: 10 to 15 mg/kg twice daily (maximum 1 g/day).
- IV/IM: 30 to 100 mg/kg/day divided every 6 to 8 hours (maximum 6 g/day). Neonates: 30 to 100 mg/kg/day divided every 12 hours
Special Cases:
- Elderly Patients: No dosage adjustment is generally necessary unless renal impairment is present.
- Patients with Renal Impairment: Dosage adjustment is necessary based on creatinine clearance.
- Patients with Hepatic Dysfunction: No dosage adjustment is usually required.
- Patients with Comorbid Conditions: Dosage adjustments may be needed in patients with severe infections, diabetes, or other comorbid conditions. Consider consulting an infectious disease specialist or a clinical pharmacist specialized in infectious diseases.
Clinical Use Cases
- Intubation/Surgical Procedures/Mechanical Ventilation/ICU Use: 1.5 g IV at induction of anesthesia, followed by 750 mg every 8 hours.
- Emergency Situations: Higher doses (up to 3 g every 8 hours for meningitis) may be required depending on the severity of the infection.
Dosage Adjustments
Dosage adjustments are primarily required in patients with renal impairment. See above, under “Standard Dosage/Special Cases/Patients with Renal Impairment.”
Side Effects
Common Side Effects:
- Diarrhea
- Nausea
- Vomiting
- Rash
- Pain at injection site
Rare but Serious Side Effects:
- Clostridium difficile -associated diarrhea (pseudomembranous colitis)
- Seizures (with high doses or renal impairment)
- Anaphylaxis (rare)
- Serum sickness
- Stevens-Johnson syndrome
- Thrombocytopenia
Long-Term Effects: Potential long-term effects primarily relate to Clostridium difficile infection or antibiotic-associated colitis.
Adverse Drug Reactions (ADR): Anaphylaxis, severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis), hematological adverse effects.
Contraindications
- Hypersensitivity to cefuroxime or other cephalosporins.
- History of severe allergic reaction (anaphylaxis) to any beta-lactam antibiotic.
Drug Interactions
- Probenecid: Reduces renal excretion of cefuroxime, increasing serum levels.
- Oral anticoagulants: May potentiate the anticoagulant effect.
- Aminoglycosides and loop diuretics: Increased risk of nephrotoxicity when used concurrently.
- Antacids: May decrease cefuroxime absorption.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: B.
- Fetal Risks: No demonstrated teratogenic effects in animal studies. Use with caution during pregnancy, especially in the first trimester.
- Breastfeeding: Cefuroxime is excreted in breast milk. Use with caution in breastfeeding mothers. Monitor the infant for potential side effects, such as diarrhea or rash.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis by binding to PBPs.
- Side Effects: Diarrhea, nausea, vomiting, rash, pain at injection site (common); C. difficile infection, seizures, anaphylaxis (rare).
- Contraindications: Hypersensitivity to cephalosporins; history of severe hypersensitivity to beta-lactams.
- Drug Interactions: Probenecid, oral anticoagulants, aminoglycosides, loop diuretics.
- Pregnancy & Breastfeeding: Caution advised. Category B.
- Dosage: See detailed dosage guidelines above.
- Monitoring Parameters: Renal function (creatinine clearance), signs of superinfection (C. difficile), prothrombin time (if co-administered with warfarin), liver function tests, complete blood counts.
Popular Combinations
Cefuroxime is often used alone. When part of a combination therapy, other drugs included might depend on the infection treated.
Precautions
- Renal function monitoring is important, especially in patients with pre-existing renal impairment.
- Caution is advised in patients with a history of penicillin allergy, as cross-reactivity may occur.
- Monitor for signs and symptoms of superinfection, including C. difficile infection.
- Advise patients to avoid alcohol during treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cefuroxime?
A: See detailed dosage guidelines above. Dosing depends on various factors such as age, the infection being treated, severity, and renal function.
Q2: What are the common side effects of Cefuroxime?
A: Common side effects include diarrhea, nausea, vomiting, and skin rash.
Q3: Is Cefuroxime safe during pregnancy?
A: Cefuroxime is Pregnancy Category B, meaning animal studies have not demonstrated fetal harm. However, it should be used with caution during pregnancy, especially in the first trimester, and only if the potential benefit outweighs the potential risk to the fetus.
Q4: Can Cefuroxime be used in patients with penicillin allergy?
A: Cefuroxime should be used with caution in patients with a history of penicillin allergy, as cross-reactivity may occur, although it is less common than with other cephalosporins. Patients with a history of severe reactions to penicillin should avoid cefuroxime.
Q5: How is Cefuroxime administered?
A: Cefuroxime can be administered orally (as cefuroxime axetil) or parenterally (IV or IM).
Q6: What should be monitored in patients receiving Cefuroxime?
A: Renal function, signs of superinfection, prothrombin time (if on warfarin), and complete blood count should be monitored.
Q7: Does Cefuroxime interact with other medications?
A: Yes, Cefuroxime may interact with probenecid, anticoagulants, aminoglycosides, and loop diuretics.
Q8: What are the signs of a serious allergic reaction to Cefuroxime?
A: Signs of a severe allergic reaction (anaphylaxis) may include difficulty breathing, swelling of the face or throat, hives, and a rapid heartbeat. Seek immediate medical attention if these occur.
Q9: Can I take Cefuroxime with food?
A: Cefuroxime axetil (oral) is better absorbed when taken with food.
Q10: What if I miss a dose of Cefuroxime?
A: Take the missed dose as soon as you remember, unless it is almost time for your next dose. Do not take two doses at the same time to make up for a missed dose.
