title: Effect of probenecid on the pharmacokinetics of DQ-2556, a new 3-quaternary ammonium cephalosporin antibiotic, in humans.
abstract: 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.
authors.affiliation: Second Department of Internal Medicine, Jikei University, School of Medicine, Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Shiba
authors.forename: M
authors.initials: M
authors.lastname: Yoshida
authors.forename: J
authors.initials: J
authors.lastname: Shimada
authors.forename: A
authors.initials: A
authors.lastname: Saito
authors.forename: K
authors.initials: K
authors.lastname: Matsubayashi
authors.forename: S
authors.initials: S
authors.lastname: Hashimoto
authors.forename: K
authors.initials: K
authors.lastname: Yoshida
authors.forename: Y
authors.initials: Y
authors.lastname: Osada
authors.forename: O
authors.initials: O
authors.lastname: Sakai
mesh_terms: 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*
chemical_list: D002511:Cephalosporins; C050465:DQ 2556; D011339:Probenecid