CEROXIM Tablet, Suspension Ref.[50620] Active ingredients: Cefuroxime

Source: Health Products Regulatory Authority (ZA)  Revision Year: 2015  Publisher: RANBAXY PHARMACEUTICALS (PTY) LTD, 14 Lautre Road, Stormill, Ext.1, Roodepoort, 1724, South Africa

5.1. Pharmacodynamic properties

Pharmacological classification: A 20.1.1 Broad and medium spectrum antibiotics

Cefuroxime is a bactericidal second-generation cephalosporin. The antibacterial action of cefuroxime results from inhibition of bacterial cell wall synthesis by binding to essential target proteins in bacterial cytoplasmic membranes. Cefuroxime has bactericidal activity against a wide range of bacterial organisms, including beta-lactamase producing strains.

Microbiological susceptibility

The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is such that the utility of cefuroxime axetil in at least some types of infections is questionable.

Cefuroxime is usually active against the following microorganisms in vitro.

Microorganisms for which acquired resistance may be a problem

Gram-positive aerobes:

Streptococcus pneumonia

Gram-negative aerobes:

Citrobacter freundii
Enterobacter aerogenes
Enterobacter cloacae
Escherichia coli
Klebsiella pneumoniae
Proteus mirabilis
Proteus spp. (other than P. vulgaris)
Providencia spp.

Gram-positive anaerobes:

Peptostreptococcus spp.
Propionibacterium spp.

Gram-negative anaerobes:

Fusobacterium spp.
Bacteroides spp.
Inherently resistant microorganisms

Gram-positive aerobes:

Enterococcus faecalis
Enterococcus faecium

Gram-negative aerobes:

Acinetobacter spp.
Campylobacter spp.
Morganella morganii
Proteus vulgaris
Pseudomonas aeruginosa
Serratia marcescens

Gram-negative anaerobes:

Bacteroides fragilis

Others:

Chlamydia spp.
Mycoplasma spp.
Legionella spp.

* All methicillin-resistant S. aureus are resistant to cefuroxime.

5.2. Pharmacokinetic properties

Cefuroxime axetil is an oral prodrug of cefuroxime. After oral absorption, cefuroxime axetil is hydrolysed in the intestinal mucosa and blood to release cefuroxime into the plasma. Oral absorption is optimal when administered with food. Peak serum levels of cefuroxime occur approximately two to three hours after oral dosing when taken with food. Protein binding is approximately 33% to 50%. Cefuroxime is not metabolised and is excreted unchanged in the urine by glomerular filtration and tubular secretion. The elimination half-life is between 1 and 1,5 hours after oral dosing. The elimination half-life is prolonged with renal impairment and in neonates. Serum levels of cefuroxime are reduced by dialysis.

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