Pharmacology: Cefixime is an antibacterial agent of the cephalosporin class. Like other cephalosporins, Cefixime inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs); which in turn inhibit 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.
Pharmacokinetics: Absorption: The absolute oral bioavailability of Cefixime is in the range of 22-54%. Absorption is not significantly modified by the presence of food. Cefixime may therefore be given without regard to meals.
Distribution: The mean volume of distribution of Cefixime is 0.1 L/kg. Penetration into tissue fluid is slow (mean tmax=6.7h) but peak concentration similar to those of plasma has been achieved. Lower levels are found in palatine tonsil, maxillary sinus mucosa, sputum and middle ear discharge. Very high concentrations occur in bile. After single oral dose of 100 mg, mean biliary concentrations is 135 mg/ml. Cefixime is almost exclusively bound to the albumin fraction, the mean free fraction being approximately 30%. Protein binding of Cefixime is only concentration dependent in human serum at very high concentrations which are not seen following clinical dosing.
Elimination: Cefixime is predominantly eliminated as unchanged drug in the urine. Glomerular filtration is considered the predominant mechanism. Metabolites of Cefixime have not been isolated from human serum or urine.
Half life: Half life of Cefixime in adults with normal renal function is 2.4-4 hours. In patients with renal impairment, half-life averages 6-11.5 hours.
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