EXIME 750 INJECTION

Indications

• Bacterial infections due to susceptible organisms
• Complicated urinary tract infections
• Pyelonephritis
• Cellulitis
• Erysipelas
• Prophylaxis of infection from human bites
• Acute diverticulitis
• Superficial bacterial eye infections
• Endophthalmitis prophylaxis after cataract surgery

Mechanism of action

Cefuroxime, like other beta-lactam antibiotics, binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. This binding inhibits the third and final stage of bacterial cell wall synthesis. The resultant disruption leads to cell lysis, aided by bacterial cell wall autolytic enzymes such as autolysins. Cefuroxime may also interfere with an autolysin inhibitor, enhancing its bactericidal effect.

Pharmacodynamics

Cefuroxime is a bactericidal agent that works by inhibiting the synthesis of peptidoglycan, an essential component of the bacterial cell wall. This inhibition occurs through the blockade of the transpeptidation process, which is required for cross-linking of the cell wall structure. Cefuroxime is effective against various organisms, including aerobic Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pneumoniae, as well as Gram-negative bacteria like Escherichia coli and Haemophilus influenzae, including strains that produce beta-lactamase.

Pharmacokinetics

Cefuroxime is well-absorbed after oral administration, with its bioavailability being enhanced when taken with food. The drug exhibits a volume of distribution indicating good tissue penetration. Cefuroxime is primarily eliminated by the kidneys, with renal clearance contributing significantly to its overall elimination. Dosage adjustments may be necessary in patients with renal impairment to prevent accumulation and toxicity.

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Allergic reactions
• Thrombophlebitis at the injection site
• Renal impairment

Interactions

• Probenecid may increase cefuroxime levels
• Other nephrotoxic drugs may enhance renal toxicity
• Anticoagulants may have increased effects

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of superinfection
• May cause allergic reactions in sensitive individuals
• Caution in patients with a history of gastrointestinal disease

Pregnancy

Not known to be harmful, but should be used only if clearly needed.

Breast-feeding

Present in low concentrations in breast milk; generally considered appropriate to use.

Storage

Store in a cool, dry place away from direct light. Reconstituted solutions should be used immediately or stored at 2–8°C for a short time.

Formulations

• Intravenous injection solution
• Powder for solution for injection
• Oral suspension
• Tablets

Mechanism of action

Cefuroxime, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefuroxime interferes with an autolysin inhibitor.

Pharmacodynamics

Cefuroxime is a &beta;-lactam type antibiotic. More specifically, it is a second-generation cephalosporin. Cephalosporins work the same way as penicillins: they interfere with the peptidoglycan synthesis of the bacterial wall by inhibiting the final transpeptidation needed for the cross-links. This effect is bactericidal. Cefuroxime is effective against the following organisms: Aerobic Gram-positive Microorganisms: <i>Staphylococcus aureus</i>, <i>Streptococcus pneumoniae</i>, <i>Streptococcus pyogenes</i>. Aerobic Gram-negative Microorganisms: <i>Escherichia coli</i>, <i>Haemophilus influenzae</i> (including beta-lactamase-producing strains), <i>Haemophilus parainfluenzae</i>, <i>Klebsiella pneumoniae</i>, <i>Moraxella catarrhalis</i> (including beta-lactamase-producing strains), <i>Neisseria gonorrhoeae</i> (including beta-lactamase-producing strains). Spirochetes: <i>Borrelia burgdorferi</i>. Cefuroxime axetil is the prodrug