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Microbiology: The bactericidal action of cefuroxime results from the inhibition of the bacterial cell wall synthesis. To achieve this, the integrity of β-lactam group is essential. The presence of a methoxyimine group prevents cefuroxime from breakdown by endo-β-lactamases produced by gram-negative bacteria (Enterobacter spp and indole-positive Proteus). So, cefuroxime is active against other cephalosporin-resistant strains. Treatment of infections caused by strains susceptible to cefuroxime: Respiratory Tract Infections: Bronchitis, bronchopneumonia, bacterial pneumonia, lung abscess, empyema and bronchiectasis.
Ear, Nose and Throat Infections: Tonsillitis, laryngitis, sinusitis, otitis media, mastoiditis.
Genitourinary Tract Infections: Pyelitis, pyelonephritis, cystitis, prostatitis , epididymitis, gonococcal urethritis, metritis, parametritis and adnexitis.
Skin and Soft Tissue Infections: Ecpyesis, cellulitis, phlegmon gangrene, mastitis and wound infections.
Pharmacokinetics: Tablet: After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime; absorption is enhanced in the presence of food. Cefuroxime is subsequently distributed throughout the body including pleural fluid, sputum bone, synovial fluid, and aqueous humour, but only achieves therapeutic concentrations in the cerebrospinal fluid (CSF) when the meninges are inflamed. Cefuroxime crosses the placenta and has been detected in breast milk. Approximately 50% of serum cefuroxime is bound to protein. Serum pharmacokinetic parameters are as follows: (See Table.)
Click on icon to see table/diagram/imageCefuroxime is excreted unchanged by glomerular filtration and renal tubular secretion, and high concentrations are achieved in the urine. Small amounts are excreted in bile. Dialysis reduces plasma concentrations.
The axetil moiety is metabolized to acetaldehyde and acetic acid.
