Cefoperazone

Cefoperazone (PDF Version)

Staphylococcus aureus (methicillin susceptible), Coagulase negative Staphylococci, Streptococcus pneumoniae (penicillin susceptible), Streptococcus spp., Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitides, Neisseria gonorrhoeae, Enterobacteriaceae, E. coli

Mechanism of Action:

Cephalosporins exert bactericidal activity by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan. The cephalosporins are also thought to play a role in the activation of bacterical cell autolysins which may contribute to bacterial cell lysis.

Pharmacodynamics:

Cephalosporins exhibit time-dependent killing (T > MIC)

Pharmacokinetics:

Dose of 1g: Cmax: 153mcg/L; Half-life: 2.1 hours; Volume of distribution: 11L; Table 11

Adverse Effects:

Hypersensitivity: Maculopapular rash, Urticaria, Pruritis, Anaphylaxis/angioedema, eosinophilia

Hematologic: Hypoprothrombinemia, Neutropenia, Leukopenia, Thrombocytopenia

GI: Diarrhea, C. difficile disease

Renal: Interstitial nephritis

Table 14

Dosage:

IV: 1g, 2g, 10g vials

Dosing in adults:

Skin and/or subcutaneous tissue infections: 2-4g/day divided IV q12h

Pelvic inflammatory disease: 2-4g/day divided IV/IM q12h

Respiratory tract infection: 2-4 g/day divided IV/IM q12h

Endometritis: 2-4 g/day divided IV/IM q12h

Dosing in pediatrics:

100-150mg/kg/day divided q8-12h

Table 12

Disease state based dosing:

Renal failure: No dosing changes recommended at this time.

Hepatic failure: No dosing changes recommended at this time.

Contraindications/Warnings/Precautions:

Precautions: hypersensitivity to penicillins, history of gastrointestinal disease, particularly colitis, renal impairment, dosage reduction may be necessary in patients with liver dysfunction, concomitant alcohol use (disulfiram-like reaction), patients with a poor nutritional status, malabsorption states (eg, cystic fibrosis), alcoholism, and patients on prolonged hyperalimentation regimens are at high risk for cefoperazone-induced vitamin K deficiency

Drug Interactions:

Heparin: an increased risk of bleeding

Live Typhoid Vaccine: decreased immunological response to the typhoid vaccine

Warfarin: an increased risk of bleeding

Pregnancy:

Category B: No evidence of risk in humans but studies inadequate.

Monitoring Requirements:

Therapeutic: Culture and sensitivities, serum levels, signs and symptoms of infection, white blood cell count

Toxic: Urinalysis, BUN, SCr, AST and ALT, skin rash, Neutropenia and leukopenia, Prothrombin time in patients with renal or hepatic impairment or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy.

Brand names/Manufacturer:

Cephobid®/Pfizer, Sulperazone®/Pfizer