PMID: 9549643Apr 29, 1998Paper

Pharmacokinetics and protein binding of eprosartan in healthy volunteers and in patients with varying degrees of renal impairment

Journal of Clinical Pharmacology
D MartinD Jorkasky

Abstract

This was an open-label, parallel group study to compare the pharmacokinetics of multiple oral doses of eprosartan in subjects with normal renal function (Clcr > 80 mL/min; n = 8) and patients with mild (Clcr 60-80 mL/min; n = 8), moderate (Clcr 30-59 mL/min; n = 15), or severe (Clcr < 30 mL/min; n = 3) renal insufficiency. Each subject received oral eprosartan 200 mg twice daily for 6 days and a single dose on day 7. Mean total maximum concentration (Cmax) and area under the concentration-time curve from 0 to 12 hours (AUC0-12) were similar for healthy subjects and those with mild renal impairment, but were an average of 25% to 35% and 51% to 55% greater for patients with moderate and severe renal impairment, respectively, compared with healthy subjects. Mean renal clearance (Clr), which was similar for healthy subjects and patients with mild renal impairment, was decreased an average of 41% and 95% in the groups with moderate and severe renal impairment, respectively, compared with normal subjects. Eprosartan was highly bound to plasma proteins in all groups; however, the unbound fraction was increased approximately two-fold in the group with severe renal impairment. Mean unbound Cmax and AUC0-12 were an average of 53% to 61% ...Continue Reading

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Citations

Jul 8, 2003·Current Hypertension Reports·Domenic A Sica
Sep 29, 2012·Clinical Pharmacokinetics·Dmytro KhadzhynovHarm Peters
Jun 5, 2003·European Journal of Pharmacology·Alexander NapPieter A van Zwieten
May 25, 2005·Clinical Pharmacokinetics·Arthur J BergmanAnup Majumdar
Mar 3, 2007·Clinical Pharmacokinetics·Jaakko PuttonenPertti J Pentikäinen
Nov 4, 2005·Drugs·Gayle W Robins, Lesley J Scott
Nov 17, 2009·Drugs·Greg L Plosker
Jan 9, 2003·Expert Opinion on Pharmacotherapy·Luis Ruilope, Bodo Jäger
Jul 16, 2009·Drug Metabolism Reviews·Italo PoggesiJean-Baptiste Watelet
Aug 9, 2005·Pharmacology & Therapeutics·Hong SunLeslie Z Benet
Apr 23, 1999·Pharmacotherapy·D A Sica, N K Hollenberg
Feb 14, 2003·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Domenic A Sica, Todd W B Gehr
Jun 21, 2001·The Journal of Clinical Hypertension·D A Sica
Jun 1, 2000·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·D A SicaA Fernandez
Jun 20, 2002·Journal of Cardiovascular Pharmacology·Jippe C BaltPieter A van Zwieten
May 30, 2003·Journal of Medicinal Chemistry·Boris Schmidt, Bernhard Schieffer

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