ABSTRACT:
Ceftazidime is a semi synthetic, broad-spectrum, beta-lactam, third-generation cephalosporin antibiotic useful for the treatment of many bacterial infections like joint infections, meningitis, pneumonia, sepsis, urinary tract infections, malignant otitis externa, and vibrio infection. It is synthesized chemically using ethyl acetoacetate, sodium nitrite and hydrochloric acid. The Structural analogues of Ceftazidime are better in terms of activity, potency and stability. Cefmenoxime has increased stability to beta-lactamases, the syn isomer of Ceftizoxime is more potent, Moxalactam has enhanced activity against Pseudomonas, Ceftriaxone has higher serum peak level and a prolonged half-life. Ceftazidime acts by inhibiting bacterial transpeptidases and preventing the synthesis of bacterial cell wall. It is assayed by Infrared spectroscopy. Stability studies showed that the drug degrades extensively on reconstitution in aqueous solution on exposures to heating at 45ºC and UV/Visible radiation, while the drug in solid state is stable. The drug is identified by carbonate or sodium tests and tested for its pH, clarity of solution, loss on drying and bacterial endotoxins. In 2015, USFDA approved a combination of Ceftazidime with Avibactam, a non-ß-lactam ß-lactamase inhibitor which protects ceftazidime from hydrolysis by a wide range of serine ß-lactamases and expands its spectrum of activity to Enterobacteriaceae resistant to ceftazidime, and is used for the treatment of complicated urinary tract infections and intra-abdominal infections. Five new ceftazidime derivatives have improved acid stability and increased spectrum of ceftazidime. All the Schiff bases showed good antimicrobial activity especially against G(+) bacteria. Compounds 2 and 3 showed broader antibacterial spectrum against both G(+) and G(-) bacteria.