Intraoperative ceforanide pharmacokinetics and protein binding

Area of Science:

• Pharmacology
• Clinical Pharmacy
• Drug Metabolism

Background:

• Understanding the pharmacokinetics and protein binding of antibiotics is crucial for optimizing therapeutic efficacy.
• Ceforanide is a cephalosporin antibiotic used in surgical prophylaxis.
• Limited data exists on ceforanide's in vivo protein binding and pharmacokinetic parameters.

Purpose of the Study:

• To determine the pharmacokinetics and protein binding of ceforanide in patients undergoing cholecystectomies.
• To compare intraoperative ceforanide concentrations with those of other cephalosporins.

Main Methods:

• 15 patients undergoing cholecystectomies received intravenous ceforanide (20 mg/kg).
• Serial blood samples were collected to measure total and free ceforanide concentrations using high-pressure liquid chromatography.
• Pharmacokinetic parameters (elimination rate constants, volume of distribution, systemic clearance) were calculated.

Main Results:

• Mean elimination rate constants were 0.41 h-1 (total) and 0.50 h-1 (free) ceforanide.
• Ceforanide exhibited a mean protein binding of 87.9%.
• Mean volume of distribution was 100 ml/kg and systemic clearance was 45.9 ml/min per 1.73 m2.
• Intraoperative ceforanide concentrations were higher than those of cefazolin and cefoxitin.

Conclusions:

• Ceforanide demonstrates predictable pharmacokinetics and significant protein binding in surgical patients.
• The drug's pharmacokinetic profile and higher intraoperative concentrations suggest potential advantages over cefazolin and cefoxitin.