Pharmacokinetics of Cefpiramide (SM-1652) in Humans

The pharmacokinetics of cefpiramide (SM-1652) were studied after the intravenous administration of single or multiple doses to 21 healthy volunteers. The cefpiramide concentration in plasma at time zero after a bolus intravenous injection of 500 or 1,000 mg was 152 or 303 micrograms/ml, respectively. The maximum cefpiramide level in plasma at the end of a 1-h infusion of 1,000 or 2,000 mg was 166 or 317 micrograms/ml, respectively. The mean plasma half-life of cefpiramide in 15 subjects who received a single dose of 500 or 1,000 mg was 4.44 h. There was no evidence of drug accumulation in plasma when 500 or 1,000 mg of cefpiramide was administered 11 times at 12-h intervals. Urinary excretion of cefpiramide over a 24-h period was ca. 22.5%, regardless of the intravenous administration technique and the dosage. Fecal recoveries of cefpiramide varied from 0 to 36.9% in different subjects.