PMID: 3383987Jan 1, 1988Paper

Effect of probenecid on the elimination and protein binding of ceftriaxone

European Journal of Clinical Pharmacology
K StoeckelP J McNamara

Abstract

The kinetics and binding parameters of ceftriaxone have been characterized in eight normal subjects who received, in sequence, 1.0 g ceftriaxone and 1.0 g ceftriaxone together with 250 and 500 mg probenecid q.i.d. Probenecid increased the total systemic clearance (CLTS) from 0.244 to 0.312 ml/min/kg, whereas the terminal half-life (t1/2T (beta)) fell from 8.1 to 6.5 h. In contrast, the renal clearance of free ceftriaxone (CLFR) was decreased from 2.09 to 1.67 ml/min/kg, confirming a small but significant contribution of tubular secretion to the renal elimination of ceftriaxone. The final value of CLFR was attained with the lower dose probenecid, whereas the non-renal clearance of free ceftriaxone (CLFNR) fell progressively from 2.78 to 1.90 ml/min/kg with the increasing probenecid dose. The total decrease in the systemic clearance of free ceftriaxone (CLFS) after the higher dose of probenecid was about 30% (4.87 to 3.57 ml/min/kg). As a consequence of a decreased affinity constant (KA), the average free fraction in plasma (f) was increased by 54% after the low dose and by 74% after the high dose of probenecid. The protein binding interaction between probenecid and ceftriaxone appears to be unique. The results are of limited cli...Continue Reading

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Citations

May 1, 1990·Journal of Clinical Pharmacology·I H PatelG A Gibson
Jan 1, 1992·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·L Pérez-GallardoJ F Escanero
Sep 1, 1996·The Journal of Emergency Medicine·G BrownA Clarke
Jul 1, 1991·British Journal of Clinical Pharmacology·A HedmanR Dahlqvist
Jun 1, 1989·Antimicrobial Agents and Chemotherapy·G L JungbluthW J Jusko
Apr 12, 2005·Annual Review of Pharmacology and Toxicology·Yoshihisa ShitaraYuichi Sugiyama
Oct 16, 1992·Pharmaceutisch Weekblad. Scientific Edition·T B VreeY A Hekster
May 1, 1988·Journal of Pharmaceutical Sciences·P J McNamaraK Stoeckel
May 15, 2015·Pharmaceutical Research·Robert GharaviHazem E Hassan
Feb 19, 2004·The Annals of Pharmacotherapy·Victoria C Cox, Peter J Zed
Feb 18, 2017·Clinical Pharmacokinetics·Anton IvanyukThierry Buclin
Jul 1, 1989·DICP : the Annals of Pharmacotherapy·R T Scheife
Dec 5, 2018·European Journal of Drug Metabolism and Pharmacokinetics·Qian ZhangJinao Duan
Sep 15, 1990·Biochemical Pharmacology·P J McNamaraK Stoeckel
Jul 28, 2021·Journal of Veterinary Pharmacology and Therapeutics·Gul CetinKamil Uney
Oct 1, 1989·Journal of Pharmaceutical Sciences·G L JungbluthW J Jusko

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