Cefoperazone is a third-generation

cephalosporin The cephalosporins (sg. ) are a class of β-lactam antibiotics originally derived from the fungus ''Acremonium'', which was previously known as ''Cephalosporium''. Together with cephamycins, they constitute a subgroup of β-lactam antibiotics ...

antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...

, marketed by Pfizer under the name Cefobid. It is one of few cephalosporin antibiotics effective in treating '' Pseudomonas'' bacterial infections which are otherwise resistant to these antibiotics. It was patented in 1974 and approved for medical use in 1981. Cefoperazone/sulbactam (Sulperazon) is a co-formulation with sulbactam.

Spectrum of bacterial susceptibility

Cefoperazone has a broad spectrum of activity and has been used to target bacteria responsible for causing infections of the respiratory and urinary tract, skin, and the female genital tract. The following represents MIC susceptibility data for a few medically significant microorganisms. * ''Haemophilus influenzae'': 0.12 - 0.25 µg/ml * ''Staphylococcus aureus'': 0.125 - 32 µg/ml * ''Streptococcus pneumoniae'': ≤0.007 - 1 µg/ml

Adverse effects

Cefoperazone contains an ''N''-methylthiotetrazole (NMTT or 1-MTT) side chain. As the antibiotic is broken down in the body, it releases free NMTT, which can cause hypoprothrombinemia (likely due to inhibition of the enzyme

vitamin K epoxide reductase Vitamin K epoxide reductase (VKOR) is an enzyme () that reduces vitamin K after it has been oxidised in the carboxylation of glutamic acid residues in blood coagulation enzymes. VKOR is a member of a large family of predicted enzymes that are p ...

) and a reaction with ethanol similar to that produced by disulfiram (Antabuse), due to inhibition of aldehyde dehydrogenase.

Mechanism of action

Cefoperazone exerts its bactericidal effect by inhibiting the bacterial

cell wall A cell wall is a structural layer surrounding some types of cells, just outside the cell membrane. It can be tough, flexible, and sometimes rigid. It provides the cell with both structural support and protection, and also acts as a filtering mech ...

synthesis, and sulbactam acts as a beta-lactamase inhibitor, to increase the antibacterial activity of cefoperazone against beta-lactamase-producing organisms.

References

{{CephalosporinAntiBiotics Acetaldehyde dehydrogenase inhibitors Cephalosporin antibiotics Tetrazoles Piperazines Phenols Acetamides Lactams Pfizer brands