Saptaz Mechanism of Action

Pharmacology: Cefepime is a fourth-generation cephalosporin and is active against a wide range of Gram-positive and Gram-negative aerobic organisms. Against Gram-positive cocci, its activity is similar to that of other cephalosporin and includes staphylococci (but not methicillin-resistant Staphylococcus aureus) and streptococci.
It is active against Enterobacteriaceae, it has a broader spectrum of activity than other cephalosporins, including activity against organisms producing chromosomally mediated beta-lactamases such as Enterobacter spp. and Proteus vulgaris, Pseudomonas aeruginosa. Tazobactam is a penicillanic acid sulfone derivative with beta-lactamases inhibitory properties. It has the potential to enhance the activity of beta-lactam antibacterials against beta-lactamases-producing bacteria.
Pharmacokinetics: Cefepime is almost completely absorbed following IM administration. In healthy adult males who received single 500 mg, 1 g or 2 g IM doses of cefepime, peak plasma concentrations of the drug were attained within 1.4-1.6 hours and averaged 13.9, 29.6 or 57.5 mcg/mL, respectively; plasma concentrations averaged 1.9, 4.5, or 8.7 mcg/mL, respectively.
Following IV infusion, over 30 minutes of a single 500 mg, 1 g or 2 g dose of cefepime in healthy adult males, peak plasma concentrations of the drug average 31.6-39.1, 65.9-81.7 or 126-163.9 mcg/mL respectively. Following parenteral administration, cefepime is widely distributed into tissues and fluids, including blister fluid, bronchial mucosa, sputum, bile, peritoneal fluid, appendix, gallbladder and prostate. Cefepime is distributed into cerebro-spinal fluid (CSF) following parenteral administration. Cefepime is distributed into human milk. Cefepime is approximately 20% bound to serum proteins.
After a 30 min infusion of 500 mg tazobactam alone, peak blister fluid levels of tazobactam are achieved at 0.94 h & mean maximum level of 6.4 mg/L is achieved. The plasma half-life of cefepime averages 2-2.3 hours.
Cefepime is partially metabolized in vivo to N-methylpyrrolidine (NMP) which is rapidly converted to the N-oxide (NMP-N-oxide). The drug is eliminated principally unchanged in urine by glomerular filtration, 80-82% of a single dose of cefepime is excreted unchanged in urine.
The elimination of tazobactam from plasma is rapid, with a mean half life of 0.35 to 0.67 h, the half-life increasing with dose.