Pharmacology: Pharmacodynamics: Mechanism of Action: 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.
Pharmacokinetics: Absorption: Cefazolin sodium is not appreciably absorbed from GI tract and must be administered parenterally.
Time to maximum plasma concentration (Tmax), IM: 0.5 to 2 hour.
Time to maximum plasma concentration (Tmax), IV: within 5 minutes.
Distribution: Widely into most body tissues and fluids including gallbladder, liver, kidneys, bone, sputum, bile, pleural, and synovial; CSF penetration is poor.
Protein binding: 74% to 86%.
Metabolism: Minimally hepatic.
Excretion: Renal: 80% to 100% unchanged in urine.
Elimination half-life: via IM or IV in neonates 3 to 5 hours, adult 90 to 150 minutes (prolonged with renal impairment).
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