Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function

European Journal of Clinical Pharmacology
A JönssonA Melander

Abstract

Glibenclamide (Gb) may provoke long-lasting hypoglycaemic reactions, and one of the known risk factors is impaired renal function. We have demonstrated Gb to have a terminal elimination half-life of 15 h, and the main metabolites have a hypoglycaemic effect. With few exceptions, detailed studies on second generation sulphonylureas in diabetics with impaired renal function are lacking. Therefore, we analysed the pharmacokinetics of Gb and its active metabolites, 4-trans-hydroxyglibenclamide (M1) and 3-cis-hydroxy-glibenclamide (M2) in this patient group. Two groups of 11 diabetic patients with impaired renal function (IRF, iohexol clearance range 7-42 ml.min(-1) . 1.73 m(-2)) or normal renal function (NRF, iohexol clearance range 75-140 ml.min(-1) . 1.73 m(-2)) were compared. A single oral 7-mg dose of Gb was administered after overnight fasting. Serum samples and urine collections were obtained over 48 h and 24 h, respectively. Concentrations of Gb, M1 and M2 were determined by a sensitive and selective high-performance liquid chromatography assay. Peak serum values of M1 (24-85 ng.ml(-1) vs 16-57 ng.ml(-1)), M2 (7-22 ng.ml(-1) vs <5-18 ng.ml(-1)) and M1 + M2 (32-100 ng.ml(-1) vs 23-76 ng.ml(-1)) were higher in the IRF group. A...Continue Reading

Citations

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