Comparative pharmacokinetics of cefoperazone and cefotaxime

The pharmacokinetics of cefoperazone and cefotaxime were compared in a crossover, randomized study in ten healthy volunteers (5 males, 5 females). Each subject received 2.0 gm of the study drug administered by an IV infusion over 30 minutes. Serum concentrations of cefoperazone and cefotaxime at the end of the infusion (zero time) were 254 mg/liter and 144 mg/liter, respectively. Comparative results at other times were the following: four hours, 20 mg/liter and 3 mg/liter; eight hours, 4.4 mg/liter and 0.3 mg/liter; and 12 hours, 1.2 mg/liter and 0.0 mg/liter. Twenty-one percent of the 2.0-gm single dose of cefoperazone was recovered in the urine during the first 24 hours following dosing, compared to 52% for cefotaxime. The renal clearance of cefoperazone was also determined in three patients during four hours. The results of the investigations will be discussed in view of the clinical relevance.