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Pharmacokinetics and disposition of the lipid‐lowering drug acifran in normal subjects and in patients with renal failure
Author(s) -
Cayen Mitchell N,
Ferdinandi Eckhardt S,
Hicks David R,
Gonzalez Ramona,
Cosyns Luc,
Dubuc Jean,
Kraml Michael,
Edwards K David G
Publication year - 1990
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1990.7
Subject(s) - pharmacokinetics , volume of distribution , urine , drug , distribution (mathematics) , dosing , half life , pharmacology , disposition , medicine , urinary system , oral administration , endocrinology , chemistry , psychology , mathematical analysis , social psychology , mathematics
The pharmacokinetics and metabolic fate of the antihyperlipidemic drug acifran were assessed after a single oral dose of the 14 C‐labeled drug to healthy male volunteers. Peak serum acifran and radioactivity concentrations were attained 1 to 2 hours after dosing, and the drug was eliminated with a half‐life of 1.6 hours. Virtually all of the recovered dose was excreted in the urine. All of the serum and urinary radioactivity was caused by unconjugated acifran. In patients with moderate chronic renal failure, the binding of acifran to plasma proteins was decreased, and the plasma concentrations of total and unbound drug were greater than those of healthy subjects. Renal failure substantially reduced the plasma and renal clearance of total and particularly of unbound acifran, moderately reduced its volume of distribution, and increased its elimination half‐life from 1.4 to 1.7 hours to 5.7 hours. The results show that acifran is very well absorbed, is rapidly eliminated, is excreted in the urine, and does not undergo any detectable biotransformation in healthy human subjects. Clinical Pharmacology and Therapeutics (1990) 47, 50–56; doi: 10.1038/clpt.1990.7