Effect of probenecid on the pharmacokinetics of DQ-2556, a new 3-quaternary ammonium cephalosporin antibiotic, in humans.
A total of 5 healthy volunteers were enrolled in a crossover study on the dose dependency and the effect of probenecid on pharmacokinetics of DQ-2556. They were administered intravenously 0.5 and 1.0 g of DQ-2556, and 1.0 g of DQ-2556 with oral administration of probenecid. The linearity in pharmacokinetics of DQ-2556 was confirmed up to the dose of 1.0 g. In the case of 1.0 g of DQ-2556 with probenecid treatment, the area under the serum concentration-time curve was larger, and total and renal clearances were less than those in the case of 1.0 g of DQ-2556 alone (by approximately 15% for each parameter, p < 0.01). These results demonstrated that DQ-2556 is secreted in the renal tubule, although it is excreted mainly by the glomerular filtration.
Shiba
K
K
Second Department of Internal Medicine, Jikei University, School of Medicine, Tokyo, Japan.
Yoshida
M
M
Shimada
J
J
Saito
A
A
Matsubayashi
K
K
Hashimoto
S
S
Yoshida
K
K
Osada
Y
Y
Sakai
O
O
D000284:Administration, Oral; D000328:Adult; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006801:Humans; D007275:Injections, Intravenous; D007668:Kidney / Q000187:drug effects / Q000378:metabolism; D008297:Male; D011339:Probenecid / Q000494:pharmacology*
D002511:Cephalosporins; C050465:DQ 2556; D011339:Probenecid