Hi-Perazone Mechanism of Action

Therapeutic Classification: Antibacterial.
Pharmacology: Pharmacodynamics: The antibacterial component of Cefoperazone + Sulbactam is cefoperazone, a third generation cephalosporin, which acts against sensitive organisms during the stage of active multiplication by inhibiting the biosynthesis of cell wall mucopeptide. Sulbactam does not possess any useful antibacterial activity, except against Neisseriaceae and Acinetobacter. As sulbactam also binds with some penicillin-binding proteins, sensitive strains are also often rendered more susceptible to Cefoperazone + Sulbactam than to Cefoperazone alone. The combination of Sulbactam and Cefoperazone is active against all organisms sensitive to cefoperazone. In addition, it demonstrates synergistic activity (up to 4-fold reduction in the minimum inhibitory concentrations for the combination versus those for each component) in a variety of organisms.
Pharmacokinetics: Absorption: The mean serum concentration obtained at 30 mins. after 1 g I.V. Cefoperazone is 114 mcg/mL. The mean serum concentration obtained at 15 mins. after 500 mg and 1000 mg IV Sulbactam are 21-40 mcg/mL and 48-88 mcg/mL respectively. The average peak plasma concentration at 5 minutes after intravenous dose of 1 g is 81 mg/litre.
Distribution: The protein binding of Cefoperazone is 82-93% and that of Sulbactam is 38%.
Metabolism and Excretion: No significant quantity of metabolites of Cefoperazone has been found in the urine. Cefoperazone is excreted mainly in the bile. About 75-85% of Sulbactam is excreted in the urine during the first eight hours of administration.
Pharmacokinetics in Special Groups: Renal Insufficiency in Patients: No significant changes observed compared to normal patients.
Hepatic Insufficiency Patients: In patients with hepatic dysfunction, the serum half-life is prolonged and urinary excretion is increased. In patients combined with renal and hepatic insufficiency, Cefoperazone may accumulate in the serum.