Cefoperazone is a third-generation cephalosporin antibiotic, marketed by

Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer ...

under the name Cefobid. It is one of few cephalosporin antibiotics effective in treating ''

Pseudomonas ''Pseudomonas'' is a genus of Gram-negative, Gammaproteobacteria, belonging to the family Pseudomonadaceae and containing 191 described species. The members of the genus demonstrate a great deal of metabolic diversity and consequently are able t ...

'' bacterial infections which are otherwise resistant to these antibiotics. It was patented in 1974 and approved for medical use in 1981.

Cefoperazone/sulbactam Cefoperazone/sulbactam is a combination drug used as an antibiotic. It is effective for the treatment of urinary tract infections. It contains cefoperazone, a β-lactam antibiotic, and sulbactam, a β-lactamase inhibitor Beta-lactamases ...

(Sulperazon) is a co-formulation with

sulbactam Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics. It was patented in 1977 and approved for medical use in ...

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 In organic chemistry and biochemistry, a side chain is a chemical group that is attached to a core part of the molecule called the "main chain" or backbone. The side chain is a hydrocarbon branching element of a molecule that is attached to a ...

. As the antibiotic is broken down in the body, it releases free NMTT, which can cause

hypoprothrombinemia Hypoprothrombinemia is a rare blood disorder in which a deficiency in immunoreactive prothrombin (Factor II), produced in the liver, results in an impaired blood clotting reaction, leading to an increased physiological risk for spontaneous bleedin ...

(likely due to

inhibition Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...

of the

enzyme Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products ...

vitamin K epoxide reductase) and a reaction with ethanol similar to that produced by

disulfiram Disulfiram is a medication used to support the treatment of chronic alcoholism by producing an acute sensitivity to ethanol (drinking alcohol). Disulfiram works by inhibiting the enzyme acetaldehyde dehydrogenase, causing many of the effects of ...

(Antabuse), due to inhibition of

aldehyde dehydrogenase Aldehyde dehydrogenases () are a group of enzymes that catalyse the oxidation of aldehydes. They convert aldehydes (R–C(=O)) to carboxylic acids (R–C(=O)). The oxygen comes from a water molecule. To date, nineteen ALDH genes have b ...

Mechanism of action

Cefoperazone exerts its bactericidal effect by inhibiting the

bacterial Bacteria (; singular: bacterium) are ubiquitous, mostly free-living organisms often consisting of one biological cell. They constitute a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria were amon ...

cell wall 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