Kefsyn/Kefsyn 750 Mechanism of Action

Kefsyn FC tab: Pharmacotherapeutic group: Antibacterials for systemic use, second-generation cephalosporins.
Pharmacology: In vivo bactericidal activity of Cefuroxime is due to Cefuroxime's binding to essential target proteins and the resultant inhibition of cell wall synthesis.
Cefuroxime has bactericidal activity against a wide range of common pathogens, including many beta-lactamase-producing strains. Cefuroxime is stable to many bacterial beta-lactamases, especially plasmid-mediated enzymes that are commonly found in enterobacteriaceae.
Pharmacodynamics: Mechanism of action: 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 amoxicillin-resistant strains.
The bactericidal action of Cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.
Pharmacokinetics: Cefuroxime is absorbed from the gastrointestinal tract and is rapidly hydrolysed in the intestinal mucosa and blood to release Cefuroxime; absorption is enhanced in the presence of food. Peak plasma concentrations are reported about 2 to 3 hours after an oral dose.
The sodium salt is given by intramuscular or intravenous injection. Peak plasma concentrations of about 27 micrograms/mL have been achieved 45 minutes after an intramuscular dose of 750 mg with measurable amounts present 8 hours after a dose. Up to 50% of Cefuroxime in the circulation is bound to plasma proteins.
The plasma half-life is about 70 minutes and is prolonged in patients with renal impairment and in neonates. Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid, and aqueous humour, but only achieves therapeutic concentrations in the CSF when the meninges are inflamed. It crosses the placenta and has been detected in breast milk.
Cefuroxime is excreted unchanged, by glomerular filtration and renal tubular secretion, and high concentrations are achieved in the urine. On injection, most of the dose of Cefuroxime is excreted within 24 hours, the majority within 6 hours. Probenecid competes for renal tubular secretion with Cefuroxime resulting in higher and more prolonged plasma concentrations of Cefuroxime.
Small amounts of cefuroxime are excreted in bile.
Plasma concentrations are reduced by dialysis.
Kefsyn granules for oral susp: Pharmacology: Pharmacodynamics: Bacteriology: Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound, cefuroxime. Cefuroxime is a well-characterized and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including beta-lactamase producing strains. Cefuroxime has good stability to bacterial beta-lactamase, and consequently is active against many ampicillin-resistant or amoxicillin-resistant strains. The bactericidal action of cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.
Cefuroxime is usually active against the following organisms in vitro: Aerobes Gram-negative: Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains), Escherichia coli, Klebsiella spp, Proteus mirabilis, Providencia spp, Proteus rettgeri.
Aerobes Gram-positive: Staphylococcus aureus (including penicillinase producing strains, excluding methicillin-resistant strains), Staphylococcus epidermidis (including penicillinase producing strains, excluding methicillin-resistant strains), Streptococcus pyogenes (and other beta-hemolytic streptococci), Streptococcus pneumoniae, Streptococcus Group B (Streptococcus agalactiae).
Anaerobes: Gram-positive cocci and Gram-negative cocci (including Peptococcus and Peptostreptococcus species), Gram-positive bacilli (including Clostridium species), Gram-negative bacilli (including Bacteroides and Fusobacterium species), Propionibacterium spp.
Other organisms: Borrelia burgdorferi.
The following organisms are not susceptible to cefuroxime: Clostridium difficile, Pseudomonas spp, Campylobacter spp, Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp.
Some strains of the following genera are not susceptible to cefuroxime: Enterococcus (Streptococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp, Citrobacter spp, Serratia spp, Bacteroides fragilis.
Pharmacokinetics: After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed in the intestinal mucosa and blood to release cefuroxime into the circulation. Optimum absorption occurs when it is administered shortly after 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 hours after the dosing when taken with food. Absorption of cefuroxime axetil suspension 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 slightly reduced systemic bioavailability (4%-17% less). The serum half-life is between 1 and 1.5 hours. Protein-binding has been variously stated as 33%-50% depending on the methodology used. Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion. Concurrent administration of probenecid increases the area under the mean serum concentration-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.
Kefsyn 750: Pharmacotherapeutic group: Antibacterials for systemic use, second-generation cephalosporins.
Pharmacology: Mechanism of action: Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin-binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
Pharmacokinetics: The sodium salt is given by intramuscular or intravenous injection. Peak plasma concentrations of about 27 micrograms/mL have been achieved 45 minutes after an intramuscular dose of 750 mg with measurable amounts present 8 hours after a dose. Up to 50% of Cefuroxime in the circulation is bound to plasma proteins. The plasma half-life is about 70 minutes and is prolonged in patients with renal impairment and in neonates.
Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid, and aqueous humour, but only achieves therapeutic concentrations in the CSF when the meninges are inflamed. It crosses the placenta and has been detected in breast milk.
Cefuroxime is excreted unchanged, by glomerular filtration and renal tubular secretion, and high concentrations are achieved in the urine. On injection, most of the dose of Cefuroxime is excreted within 24 hours, the majority within 6 hours. Probenecid competes for renal tubular secretion with Cefuroxime resulting in higher and more prolonged plasma concentrations of Cefuroxime. Small amounts of cefuroxime are excreted in bile.
Plasma concentrations are reduced by dialysis.