Levexime-500 Mechanism of Action

Pharmacotherapeutic group: antibacterials for systemic use, second-generation cephalosporins.
Pharmacology: In vivo bactericidal activity of Cefuroxime axetil 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.
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 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.
Pharmacokinetics: Cefuroxime axetil 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 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.