Zisuva 375/Zisuva 625/Zisuva 1G/Zisuva DS/Zisuva 600/Zisuva 1200 Mechanism of Action

Pharmacology: Zisuva 375/Zisuva 625/Zisuva 1G/Zisuva DS: Amoxicillin and Potassium Clavulanate is an oral antibacterial combination consisting of the semisynthetic antibiotic amoxicillin and the β-lactamase inhibitor, Potassium Clavulanate (the potassium salt of clavulanic acid).
Clavulanic acid binds and inhibits beta-lactamases that inactivate amoxicillin resulting in amoxicillin having an expanded spectrum of activity. Amoxicillin inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
Zisuva 600/Zisuva 1200: Mechanism of action: Amoxicillin is a semisynthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes (often referred to as penicillin-binding proteins, PBPs) in the biosynthetic pathway of bacterial peptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to weakening of the cell wall which is usually followed by cell lysis and death.
Amoxicillin is susceptible to degradation by beta-lactamases produced by resistant bacteria and therefore the spectrum of activity at amoxicillin alone does not include organisms which produce these enzymes.
Clavulanic acid is a beta-lactam structurally related to penicillins. It inactivates some beta-lactamase enzymes thereby preventing inactivation of amoxicillin. Clavulanic acid alone does not exert a clinically useful antibacterial effect.
Pharmacokinetics: Zisuva 375/Zisuva 625/Zisuva 1G/Zisuva DS: Amoxicillin and Potassium Clavulanate are well absorbed from the gastrointestinal tract after oral administration of amoxicillin and potassium clavulanate. Dosing in the fasted or fed state has minimal effect on the pharmacokinetics of amoxicillin. While amoxicillin and potassium clavulanate can be given without regard to meals, absorption of potassium clavulanate when taken with food is greater relative to the fasted state. In 1 study, the relative bioavailability of clavulanate was reduced when amoxicillin 1 potassium clavulanate was dosed at 30 and 150 minutes after the start of a high - fat breakfast. The safety and efficacy of amoxicillin and potassium clavulanate was taken without regard to meals.
Amoxicillin serum concentration achieved with amoxicillin and potassium clavulanate are similar to those produced by the oral administration of equivalent doses of amoxicillin alone. The half-life of amoxicillin after the oral administration of amoxicillin and potassium clavulanate is 1.3 hours and that of clavulanic acid is 1.0 hour. Approximately 50% to 70% of the amoxicillin and approximately 25% to 40% of the clavulanic acid are excreted unchanged in urine during the first 6 hours after administration of a single 250 mg or 500 mg tablet of amoxicillin and potassium clavulanate.
Concurrent administration of Probenecid delays amoxicillin excretion but does not delay renal excretion of clavulanic acid.
Neither component in amoxicillin and potassium clavulanate is highly protein - bound: clavulanic acid has been found to be approximately 25% bound to human serum and amoxicillin approximately 18% bound.
Amoxicillin diffuses readily into most body tissues and fluids with the exception of the brain and spinal fluid. The results of experiments involving the administration of clavulanic acid to animals suggest that this compound, like amoxicillin, is well distributed in body tissues.