Cefdinir is a broad-spectrum, third-generation cephalosporin resistant to many β-lactamase enzymes. It is structurally similar to Cefixime and was patented in 1979 by Fujisawa Pharmaceutical. Cefdinir is an inhibitor of neutrophil myeloperoxidases and can also interact with the dipeptide transporters PEPT1 and PEPT2.
| Mechanism of Action | 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, however, Cefdinir is not typically inactivated by this mechanism. |
| Spectrum | Cefdinir targets both Gram-positive and Gram-negative bacteria, including those responsible for ear, sinus and skin infections. |
| Microbiology Applications | Cefdinir is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive and Gram-negative microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options . Representative MIC values include:
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| Eukaryotic Cell Culture Applications | Cefdinir inhibits the luminol-amplified chemiluminescence (LACL) response of human neutrophils stimulated by PMA (but not opsonized zymosan) in a concentration-dependent manner. Cefdinir also inhibited LACL generation in cell-free systems consisting of H2O2, NaI, and either horseradish peroxidase or a myeloperoxidase-containing neutrophil extract (Labro et al, 1994).
Cefdinir inhibits the activity of myeloperoxidase-containing neutrophil extract released into the extracellular medium during neutrophil stimulation by soluble mediators, but has no effect on that released into the phagolysosome during phagocytosis. This unusual property could be of interest in modulating the exaggerated inflammatory process associated with infectious diseases (Labro et al, 1994). |
| Molecular Formula | C14H13N5O5S2 |
| Impurities | Impurity G: ≤0.7% Single Impurity: ≤0.2% Total Impurities: ≤3.0% |
| References |
Cefdinir (TOKU-E) Kaul M et al (2016) Combining the FtsZ-targeting prodrug TXA709 and the cephalosporin Cefdinir confers synergy and reduces the frequency of resistance in Methicillin-resistant Staphylococcus aureus. Antimicrob. Agents Chemother. 60(7):4290-4296 Link to article General: Inamoto, Y et al (1988) FK 482, a new orally active cephalosporin synthesis and biological properties. J. Antibiotic. 41(6):828-830 PMID 3255303 |
| MIC | Bacillus cereus| 6|| Bacteroides fragilis| ≤0.05 － >16|| Bordetella pertussis | 32 － 128|| Burkholderia cepacia| 2 － 128|| Citrobacter amalonaticus| 8.5|| Citrobacter diversus| 0.06 － 1|| Citrobacter freundii| 0.12 － >128|| Corynebacterium jeikeium| 0.06 － >16|| Edwardsiella hoshinae | ≤0.03|| Edwardsiella ictaluri | ≤0.03 － 0.13|| Edwardsiella tarda| ≤0.03 － 0.5|| Enterobacter aerogenes| 0.25 － >16|| Enterobacter agglomerans| 0.06 － 1|| Enterobacter cloacae| 0.063 － >100|| Enterobacter sakazakii| 1.03|| Enterobacter taylorae| 16|| Enterococcus faecalis| 0.5 － >128|| Enterococcus faecium| 16 － >128|| Enterococcus spp.| 1 － >16|| Escherichia coli| 0.06 － 16|| Flavobacterium spp.| >16|| Haemophilus influenzae| 0.05 － 4|| Hafnia alvei| 6|| Klebsiella ozaenae| 0.06|| Klebsiella pneumonia| ≤0.063 － 128|| Klebsiella spp.| ≤0.03 － 8|| Legionella pneumophila| 0.25 － 8|| Listeria monocytogenes| 12|| Moraxella catarrhalis| 0.013 － 12.5|| Morganella morganii| 0.25 － 128|| Neisseria spp.| ≤0.015 － 0.25|| Proteus mirabilis| ≤0.03 － 12.5|| Proteus vulgaris| 0.1 － 64|| Providencia rettgeri| ≤0.004 － 128|| Providencia stuartii| ≤0.03 － >16|| Pseudomonas aeruginosa| >16 － >128|| Pseudomonas cepacia| >16|| Pseudomonas flourescens| >16|| Pseudomonas putida| >16|| Salmonella enteritidis| 0.06 － 0.5|| Salmonella typhi| 0.09|| Serratia liquefaciens| 2|| Serratia marcescens| 1－ >128|| Shigella spp.| 0.12 － 0.5|| Staphylococcus aureus (5)| 0.013 － >128|| Staphylococcus epidermidis| ≤0.03 － >128|| Staphylococcus spp. (coagulase-negative)| ≤0.03 － >16|| Stenotrophomonas maltophilia| 100 - >128|| Streptococcus agalactiae| 0.032 － 0.063|| Streptococcus bovis| ≤0.03|| Streptococcus pneumonia| 0.006 － 64|| Streptococcus pyogenes| ≤0.004 － 2|| Streptococcus spp.| ≤0.015 － 0.5|| Xanthomonas maltophilia| 0.12 － >16|| Yersinia enterocolitica| 0.12 － 2|| |