Pharmacology: Pharmacodynamics: Cefuroxime is a well characterised and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including β-lactamase producing strains. Cefuroxime has good stability to bacterial β-lactamase, and consequently is active against many ampicillin-resistant or amoxycillin-resistant strains.
The bactericidal action of cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.
The prevalence of acquired resistance is geographically and time dependent and for select species may be very high. Local information on resistance is desirable, particularly when treating severe infections. (See Table 1.)
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Pharmacokinetics: Peak levels of cefuroxime are achieved within 30 to 45 minutes after i.m. administration.
Protein binding has been variously stated as 33-50% depending on the methodology used.
Concentrations of cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in bone, synovial fluid and aqueous humour. Cefuroxime passes the blood-brain barrier when the meninges are inflamed.
Cefuroxime is not metabolised and is excreted by glomerular filtration and tubular secretion.
The serum half-life after either i.m. or i.v. injection is approximately 70 minutes.
In the first weeks of life the serum half-life of cefuroxime can be 3 to 5 times that in the adult.
Concurrent administration of probenecid prolongs the excretion of the antibiotic and produces an elevated peak serum level. There is an almost complete recovery (85 to 90%) of unchanged cefuroxime in urine within 24 hours of administration. The major part is excreted in the first 6 hours.
Serum levels of cefuroxime are reduced by dialysis.
Toxicology: Pre-clinical Safety Data: No additional data of relevance.