Cefoperazone Sodium: Injectable Cephalosporin Antibiotic

Cefoperazone sodium is a novel, third-generation, semi-synthetic cephalosporin for injection. It has a broad spectrum of antimicrobial activity and is effective against Pseudomonas aeruginosa; it also exhibits antimicrobial activity against Gram-negative bacteria, Gram-positive bacteria, and anaerobic bacteria. Unlike other cephalosporins, this drug is excreted primarily via extrarenal pathways. Following intravenous or intramuscular administration, cefoperazone sodium is effective against a wide range of infections caused by aerobic Gram-negative and Gram-positive bacteria, including biliary tract infections, and is also effective against most anaerobic infections.

Interaction of Cefoperazone Sodium with Bovine Transferrin and Bovine Serum Albumin

The interactions of cefoperazone sodium(CS) with bovine transferrin and bovine serum albumin were studied by multi-spectroscopic methods. Results showed that the intrinsic fluorescence of proteins was quenched by the CS with a static quenching procedure. The thermodynamics parameters indicated that electrostatic attraction played a major role in the interactions of drug and proteins. The results of synchronous fluorescence spectra demonstrated that the microenvironments of amino acid residues of the two proteins were disturbed by cefoperazone sodium and the binding site of CS to the bovine transferrin/bovine serum albumin was closer to tryptophan residues. Circular dichroism indicated that CS changed the secondary structures of the two proteins. Hill’s coefficient showed that there was negative cooperation in the interaction of subsequent cefoperazone sodium with bovine transferrin/bovine serum albumin. Moreover, the results showed that CS bound to bovine serum albumin with higher affinity. However, CS had larger influences on the microenvironment of bovine transferrin. The interaction between cefoperazone sodium and different proteins will be helpful for extracting the common features, applying the unique characteristic of drug-proteins systems.[1]

Multicenter Clinical Trial of Cefoperazone Sodium

A total of 187 physician investigators throughout the United States participated in a multicenter trial to evaluate the safety and efficacy of a twice daily dosage of Cefoperazone sodium; 91 percent of patients received a dosage of 4 g or less of cefoperazone per day. A total of 455 patients were included in the evaluation of efficacy: 100 patients with lower respiratory tract infection; 146 patients with skin and soft tissue infection; 14 patients with osteomyelitis;18 patients with obstetric and gynecologic infections; 84 patients with urinary tract infection; and 44 patients with bacteremia. Overall, treatment achieved a satisfactory clinical outcome in 95.3 percent of these patients. Side effects of cefoperazone were evaluated in 659 patients. Prothrombin time increased during therapy in 4 percent of patients, all but one of whom was more than 65 years old. Prothrombin time became normal with the administration of vitamin K. Diarrhea (4 or more loose stools a day) was observed in 3 percent of patients. Other adverse reactions including leukopenia, elevation of serum liver enzyme levels, and eosinophilia were mild, reversible, and typical of beta-lactam antibiotics. These results suggest that (1) twice daily administration of cefoperazone sodium can be used to treat a variety of bacterial infections caused by susceptible pathogens; (2) the adverse reactions associated with this agent at the dosage schedule employed in this trial (2 g twice a day) are predictable and limited; (3) multicenter trials of this type allow for rapid collection of data regarding safety and efficacy of new antibiotics.[2]

Therapeutic indications of cefoperazone

Cefoperazone sodium is a parenteral cephalosporin antibiotic that is pending approval by the U. S. Food and Drug Administration. Compared to most other cephalosporins cefoperazone has a greatly expanded spectrum of bactericidal activity that encompasses most aerobic gram-positive bacteria except enterococci, most aerobic gram-negative bacteria, including a majority of Pseudomonas aeruginosa strains, and a number of pathogenic anaerobic bacteria. Its long serum half-life, approximately two hours, permits a twelve hourly dosing schedule. No dosage modification is required in patients with renal insufficiency, and only minor modification is needed in patients with hepatic insufficiency or biliary obstruction. Clinical trials have established cefoperazone sodium's efficacy in lower respiratory tract infections, urinary tract infections, and a variety of other bacterial infections. Adverse reactions have been infrequent, and few serious reactions have been identified. Cefoperazone sodium is a promising new agent for the treatment of gram-negative bacillary and polymicrobial infections, especially in settings that require empiric therapy.[3]

References

[1]Duan, S., Liu, B.-S., Li, T., & Cui, M. (2017). The Interaction of Cefoperazone Sodium with Bovine Transferrin and Bovine Serum Albumin. 0. https://doi.org/10.11648/J.SJAC.20160406.14

[2]Cohen MS, Washton HE, Barranco SF. Multicenter clinical trial of cefoperazone sodium in the United States. Am J Med. 1984 Jul 31;77(1B):35-41. doi: 10.1016/s0002-9343(84)80094-7. PMID: 6380285.

[3]Funk EA, Strausbaugh LJ. Antimicrobial activity, pharmacokinetics, adverse reactions, and therapeutic indications of cefoperazone. Pharmacotherapy. 1982 Jul-Aug;2(4):185-96. doi: 10.1002/j.1875-9114.1982.tb03186.x. PMID: 6221236.

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