Cefetamet Pivoxil Hydrochloride is the hydrochloride salt form of Cefetamet Pivoxil, a pivalate ester prodrug that is hydrolysed to form the active agent, cefetamet. It is a third-generation cephalosporin with broad-spectrum activity. It is active against bacteria causing respiratory and urinary tract infections.
Cefetamet Pivoxil Hydrochloride is soluble in DMSO and ethanol but insoluble in water.
| Mechanism of Action | Cefetamet Pivoxil Hydrochloride exerts its bactericidal action by inhibition the final transpeptidation step of peptidoglycan synthesis in the bacterial cell wall by binding to one or more of the penicillin-binding proteins (PBPs).
Cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases. |
| Spectrum | Cefetamet displays high in vitro activity against both Gram-positive and Gram-negative bacteria. |
| Microbiology Applications | Cefetamet has excellent in vitro activity against the major respiratory pathogens including Streptococcus pneumonia and Haemophilus influenza. However, it has poor activity against penicillin-resistant S. pneumonia. The in vitro activity of cefetamet is unaffected by the composition of the agar medium, agar pH or the addition of serum to the agar. In vivo, cefetamet demonstrated antibacterial activity consistent with its in vitro activity in animal models of septicaemia, pyelonephritis, respiratory tract infection and syphilis. |
| Molecular Formula | C20H25N5O7S2 · HCl |
| References |
Harriet Bryson H and Rex Brogden R (1993) Cefetamet Pivoxil: A Review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 45(4):589–621 PMID: 7684677 Hoh P, von Graevenitz A and Zollinger-Iten J (1988) Cefetamet Pivoxil: Bacteriostatic and bactericidal activity of the free acid against 355 gram-negative rods. Infection 16:194–198 Speciale A et al (1996) Cefetamet Pivoxil: Comparable evaluation with other orally available antibiotics against selected species of respiratory pathogens. Chemother. 42(1):1-10 |
