6533b7d6fe1ef96bd126643a

RESEARCH PRODUCT

Renal and nonrenal clearances of ceftriaxone at the steady-state and its relation to plasma protein binding

Luis GraneroJesús Chesa-jiménezMercedes AlmelaJosé Esteban PerisMaría Pascual-arce

subject

Kidneymedicine.medical_specialtyChemistryPharmaceutical ScienceRenal functionmedicine.anatomical_structureEndocrinologyPharmacokineticsRenal physiologyInternal medicineBlood plasmamedicineCeftriaxoneSteady state (chemistry)medicine.drugAntibacterial agent

description

Abstract The effect of the saturable plasma protein binding of ceftriaxone on the elimination of this drug was studied under steady-state conditions in the rat. A concentration-dependent increase in the total, renal and nonrenal clearances of total drug (bound + unbound) was observed, and it was related to the increase in the ex vivo unbound fraction of ceftriaxone as the plasma concentration increased. The nonrenal clearance of the unbound ceftriaxone showed a statistically significant decrease as the plasma concentration of the unbound drug at the steady state increased, which indicates that the nonrenal elimination of the drug (mainly by biliary excretion) is a saturable process. Renal clearance of the unbound ceftriaxone was similar to the glomerular filtration rate, which indicates that glomerular filtration is the principal mechanism involved in the renal excretion of ceftriaxone in the rat.

https://doi.org/10.1016/0928-0987(95)00003-v