Usage
Cefuroxime axetil is a second-generation cephalosporin antibiotic prescribed for various bacterial infections. It is effective against a broad range of gram-positive and gram-negative bacteria. It is commonly used to treat:
- Respiratory tract infections: Pharyngitis, tonsillitis, acute bronchitis, acute bacterial exacerbations of chronic bronchitis, and pneumonia.
- Ear infections: Acute otitis media.
- Skin and soft tissue infections: Such as cellulitis, impetigo, and wound infections.
- Urinary tract infections: Including cystitis and pyelonephritis.
- Gonorrhea: Uncomplicated gonococcal infections.
- Lyme disease: Early stages of Lyme disease (erythema migrans).
Pharmacological Classification: Antibiotic, specifically a second-generation cephalosporin.
Mechanism of Action: Cefuroxime inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to cell lysis and bacterial death.
Alternate Names
International and Regional Variations: Cefuroxime (axetil refers to the specific ester form).
Brand Names: Ceftin, Zinacef.
How It Works
Pharmacodynamics: Cefuroxime exerts its bactericidal effect by disrupting the synthesis of the peptidoglycan layer in bacterial cell walls, eventually leading to cell death. It is active against many Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Staphylococcus aureus (including some methicillin-susceptible strains), Escherichia coli, Proteus mirabilis, and Klebsiella spp. strains.
Pharmacokinetics:
- Absorption: Cefuroxime axetil is an orally administered prodrug that is hydrolyzed to cefuroxime upon absorption in the gastrointestinal tract. Absorption is enhanced when taken with food.
- Distribution: Cefuroxime is widely distributed throughout the body, reaching therapeutic concentrations in various tissues and fluids.
- Metabolism: Cefuroxime axetil is metabolized to cefuroxime. Cefuroxime is not extensively metabolized further.
- Elimination: Primarily eliminated by the kidneys via glomerular filtration and tubular secretion. The elimination half-life is approximately 1-2 hours in individuals with normal renal function.
Mode of Action: Cefuroxime exerts its antibacterial effect by binding to and inactivating penicillin-binding proteins (PBPs). These proteins play a crucial role in the final stages of peptidoglycan synthesis, a key component of the bacterial cell wall. By inhibiting PBPs, cefuroxime disrupts cell wall integrity, leading to cell lysis and bacterial death.
Elimination Pathways: Primarily renal excretion, both glomerular filtration and tubular secretion.
Dosage
Standard Dosage
Adults: 250-500 mg orally every 12 hours for 7-10 days for most infections. A single 1 g dose is used for uncomplicated gonorrhea.
Children (3 months to 12 years): Oral suspension: 10-15 mg/kg twice daily for 5-10 days for most infections (maximum 1,000 mg/day for suspension). For children who can swallow tablets: 250 mg twice daily for 10 days. Cefuroxime should not be used in infants younger than 3 months.
Special Cases:
- Elderly Patients: No specific dose adjustment needed based solely on age, however, dose adjustment is crucial in the presence of renal impairment.
- Patients with Renal Impairment: Dose reduction based on creatinine clearance is necessary.
- Patients with Hepatic Dysfunction: No dosage adjustment typically required.
- Patients with Comorbid Conditions: Consider drug interactions and disease states when determining appropriate dosage.
Clinical Use Cases
Cefuroxime axetil is generally not indicated for the specific clinical scenarios mentioned (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations). For these cases, intravenous cefuroxime (cefuroxime sodium) is generally preferred for optimal drug levels.
Dosage Adjustments
Dose adjustments are necessary for patients with impaired renal function. See the special cases section above.
Side Effects
Common Side Effects:
- Diarrhea
- Nausea
- Vomiting
- Abdominal pain
- Vaginal itching or discharge
- Headache
- Rash
Rare but Serious Side Effects:
- Severe allergic reactions (anaphylaxis)
- Pseudomembranous colitis (Clostridium difficile-associated diarrhea)
- Seizures
- Serum sickness
- Hemolytic anemia
- Thrombocytopenia
- Stevens-Johnson syndrome
Long-Term Effects:
Generally, no significant long-term effects are associated with short-term cefuroxime use. Long-term use may increase the risk of antibiotic resistance and Clostridium difficile infection.
Adverse Drug Reactions (ADR): See “Rare but Serious Side Effects.”
Contraindications
- Hypersensitivity to cefuroxime, other cephalosporins, or any component of the formulation.
Drug Interactions
- Antacids: May decrease the absorption of cefuroxime. Administer antacids at least 1 hour before or 2 hours after cefuroxime.
- H2 Receptor Antagonists and Proton Pump Inhibitors: May reduce the absorption of cefuroxime.
- Probenecid: Increases serum concentrations of cefuroxime by inhibiting renal tubular secretion.
- Oral Contraceptives: Cefuroxime may decrease the efficacy of oral contraceptives. Alternative or additional contraceptive methods should be considered.
- Anticoagulants: Cefuroxime may potentiate the anticoagulant effects of warfarin. Close monitoring of INR is recommended.
- Aminoglycosides and Loop Diuretics: Increased risk of nephrotoxicity when administered concurrently with cefuroxime, particularly in patients with pre-existing renal impairment.
Pregnancy and Breastfeeding
Cefuroxime is generally considered safe during pregnancy. Animal studies have not shown harm to the fetus, and human data have not revealed a clear link between cefuroxime use and adverse fetal outcomes. However, like all medications, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Cefuroxime is excreted in breast milk in small quantities. Although adverse effects in breastfed infants are unlikely, monitor for diarrhea, rash, or fungal infections (thrush).
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis.
- Side Effects: Diarrhea, nausea, vomiting, rash, allergic reactions.
- Contraindications: Hypersensitivity to cephalosporins.
- Drug Interactions: Antacids, H2 blockers, probenecid, anticoagulants.
- Pregnancy & Breastfeeding: Generally considered safe.
- Dosage: Adults: 250-500 mg twice daily; Children: 10-15 mg/kg twice daily.
- Monitoring Parameters: Renal function, signs of superinfection (e.g., thrush, C. difficile).
Popular Combinations
Not applicable for cefuroxime axetil.
Precautions
- Hypersensitivity reactions
- Renal impairment (dose adjustment needed)
- Clostridium difficile-associated diarrhea
- Use cautiously in patients with a history of penicillin allergy due to potential cross-reactivity.
- Alcohol consumption may be permissible; however, excessive intake may reduce the overall immune response to infections
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cefuroxime axetil?
A: Adults: 250-500 mg orally every 12 hours. Children (3 months-12 years): 10-15 mg/kg orally every 12 hours. Dose adjustments are needed for patients with renal impairment.
Q2: What are the common side effects of Cefuroxime axetil?
A: Common side effects include diarrhea, nausea, vomiting, rash, and abdominal pain.
Q3: Can Cefuroxime axetil be used in pregnant women?
A: Cefuroxime is generally considered safe to use during pregnancy; however, it should only be used if the potential benefit outweighs the potential risk to the fetus.
A: Cefuroxime axetil is metabolized to its active form, cefuroxime. Cefuroxime is primarily eliminated by the kidneys.
Q5: What are the contraindications to using Cefuroxime axetil?
A: A known hypersensitivity to cefuroxime, other cephalosporins, or any component of the formulation.
Q6: How does Cefuroxime axetil interact with other medications?
A: It can interact with antacids, H2 blockers, probenecid, and anticoagulants. Consult a comprehensive drug interaction resource for detailed information.
Q7: Can Cefuroxime axetil be used to treat viral infections?
A: No, cefuroxime axetil is only effective against bacterial infections. It has no activity against viral infections such as the common cold or flu.
Q8: What should be done if a patient develops diarrhea while taking Cefuroxime axetil?
A: Diarrhea can be a sign of Clostridium difficile-associated diarrhea, a serious complication of antibiotic use. If a patient develops diarrhea, it should be evaluated promptly, and the drug may need to be discontinued.
Q9: Is it safe to drink alcohol while taking Cefuroxime axetil?
A: Moderate alcohol consumption may not cause significant interactions. However, excessive alcohol use can weaken the immune system and impair the body’s ability to fight infections, which can reduce the drug’s effectiveness.
Q10: What is the difference between cefuroxime axetil and cefuroxime sodium?
A: Cefuroxime axetil is the oral prodrug, while cefuroxime sodium is administered intravenously or intramuscularly. They are not interchangeable on a milligram-per-milligram basis.
