Zinnat Mechanism of Action





Zuellig Pharma
Full Prescribing Info
Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β-lactamases and is active against a wide range of gram-positive and gram-negative organisms.
Microbiology: Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound cefuroxime.
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.
Microbiology: Cefuroxime is usually active against the following organisms in vitro:
Gram-Negative Aerobes: Haemophilus influenzae (including ampicillin-resistant strains); Haemophilus parainfluenzae; Moraxella (Branhamella) catarrhalis; Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains); Escherichia coli; Klebsiella sp; Proteus mirabilis; Providencia sp; Proteus rettgeri.
Gram-Positive Aerobes: Staphylococcus aureus and Staphylococcus epidermidis (including penicillinase-producing strains but excluding methicillin-resistant strains); Streptococcus pyogenes (and other β-haemolytic streptococci); Streptococcus pneumoniae; Streptococcus Group B (Streptococcus agalactiae).
Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus sp); gram-positive bacilli (including Clostridium sp) and gram-negative bacilli (including Bacteroides and Fusobacterium sp); Propionibacterium sp.
Other Organisms: Borrelia burgdorferi.
The following organisms are not susceptible to cefuroxime: Clostridium difficile; Pseudomonas and Campylobacter sp; Acinetobacter calcoaceticus; Listeria monocytogenes; methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis; Legionella sp.
Some strains of the following genera are not susceptible to cefuroxime: Enterococcus (Streptococcus) faecalis; Morganella morganii; Proteus vulgaris; Enterobacter sp, Citrobacter sp and Serratia sp; Bacteroides fragilis.
Pharmacokinetics: After oral administration, cefuroxime axetil is slowly absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation.
Optimum absorption occurs when it is administered shortly after a meal.
Following administration of cefuroxime axetil tablets, peak serum levels (2.9 mg/L for a 125-mg dose, 4.4 mg/L for a 250-mg dose, 7.7 mg/L for a 500-mg dose and 13.6 mg/L for a 1-g dose) occur approximately 2.4 hrs after dosing when taken with food.
Peak serum levels (2-3 mg/L for a 125-mg dose, 4-6 mg/L for a 250-mg dose, 5-8 mg/L for a 500-mg dose and 9-14 mg/L for a 1-g dose) occur approximately 2-3 hrs after dosing when taken after food, unlike IV dosing which peaks immediately.
The absorption of cefuroxime is enhanced in the presence of food. The rate of absorption of cefuroxime from the suspension compared with the tablets is reduced, leading to later, lower peak serum levels and reduced systemic bioavailability (4-17% less).
The serum half-life is between 1 and 1.5 hrs. Protein-binding has been variously stated as 33-50% depending on the methodology used.
Cefuroxime is not metabolised and is excreted by glomerular filtration and tubular secretion. Concurrent administration of probenecid increases the area under the mean serum concentrations time curve by 50%.
Serum levels of cefuroxime are reduced by dialysis.
Toxicology: Preclinical Safety Data: Animal toxicity studies indicated that cefuroxime axetil is of low toxicity with no significant findings.
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