Cefuroxime

Mechanism of action and antimicrobial spectrum

Like all beta-lactam antibiotics, cefuroxime disrupts bacterial cell wall synthesis, exerting a bactericidal effect. A crucial evolutionary feature of the second generation is that they are more resistant to $eta$-lactamases than first-generation drugs.

Features of the activity spectrum:

• Gram-negative flora: Activity is significantly higher than that of the first generation. The spectrum is expanded to include Haemophilus influenzae (cefuroxime is the group leader in efficacy against this pathogen), Neisseria spp., certain strains of Enterobacter aerogenes, and enteric bacteria (E. coli, Proteus, Salmonella, Shigella).
• Gram-positive flora: Efficacy is somewhat lower compared to first-generation cephalosporins.
• Spectrum limitations: The drug is inactive against Pseudomonas aeruginosa (P. aeruginosa). Also, unlike the other subgroup of its generation (cefotetan, cefoxitin), cefuroxime lacks anti-anaerobic activity (inactive against Bacteroides).

Pharmacokinetics

The pharmacokinetic profile depends on the route of administration. Cefuroxime penetrates well into organs and tissues, and is eliminated predominantly by the kidneys.

Parenteral form (Cefuroxime / Ketocef):

• Administered intramuscularly (IM) or intravenously (IV).
• The half-life requires administration every 8 hours (3–4 times daily).
• BBB penetration: Crosses the blood-brain barrier only in the presence of meningeal inflammation.

Oral form (Cefuroxime axetil / Zinnat):

• Is a prodrug — a cefuroxime derivative adapted for gastrointestinal absorption.
• Features a more convenient dosing regimen: prescribed twice daily.

Clinical indications

Due to its activity against Haemophilus influenzae and pneumococcus, cefuroxime is frequently used to treat community-acquired pneumonia and other bacterial infections of the upper and lower respiratory tract.

Other indications include:

• Urinary tract infections.
• Skin and soft tissue infections.
• Bone and joint infections.
• Perioperative antibiotic prophylaxis in surgery (a general indication for the group).

Side effects

The drug possesses a safety profile typical of cephalosporins.

• Common reactions: diarrhea, transient elevation of hepatic transaminases, allergic reactions (hypersensitivity, cross-allergy with penicillins is possible).
• Rare but severe reactions: agranulocytosis, interstitial nephritis.

Dosage forms and regimen

The drug is available for both enteral and parenteral use.

1. For oral administration (tablets):

• Dosages: 0.125 g, 0.25 g, and 0.5 g.
• Regimen: 0.125–0.5 g twice daily.

2. For injection (powder in vials):

• Dosages: 0.75 g and 1.5 g.
• Administration regimen: intramuscularly or intravenously 0.75–1.5 g 3–4 times daily (every 8 hours).

Class and exam questions

What else to study on this topic

• Comparative characteristics of 1st and 2nd generation cephalosporins
• Cephalosporins with anti-anaerobic activity (cefotetan, cefoxitin)
• Mechanisms of Gram-negative bacterial resistance to beta-lactams
• Principles of perioperative antibiotic prophylaxis
• The concept of prodrugs in pharmacology using cefuroxime axetil as an example

Other topics in the «Drugs and Prescriptions» section

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