Is there a concentration-effect relationship for sulphonylureas?

Clinical Pharmacokinetics
Arne MelanderT Rydberg

Abstract

Sulphonylureas have remained the mainstay of oral therapy for type 2 (non-insulin-dependent) diabetes mellitus (NIDDM). They stimulate insulin release from pancreatic beta cells. Pharmacokinetic differences between the various sulphonylureas are of clinical importance in terms of the time to onset of action, timing of drug administration in relation to food intake, magnitude and duration of the glucose-lowering effect and the risk of serious hypoglycaemia. Recent studies with improved analytical sensitivity have shown that the elimination half-life of glibenclamide is longer than previously thought and that 2 metabolites of glibenclamide have significant hypoglycaemic activity. Furthermore, single dose studies in healthy volunteers using an integrated pharmacokinetic-pharmacodynamic model have identified clear concentration-effect relationships for both glibenclamide and its metabolites after oral and intravenous administration. Under multiple dose conditions, kinetic-dynamic relations have been identified with shorter-acting drugs in dosages that give discontinuous sulphonylurea exposure. However, at continuous exposure, i.e. sustained 24-hour therapeutic concentrations in plasma, there is evidence indicating the development o...Continue Reading

Citations

Feb 22, 2011·European Journal of Clinical Pharmacology·A SurendiranC Adithan
Jun 16, 2000·European Journal of Pharmacology·Y UwaiK Inui
Dec 17, 2002·Diabetes Research and Clinical Practice·Tsvetalina TankovaGeorgi Kirilov
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May 16, 2007·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·F Lee Cantrell, Richard F Clark
Jun 27, 2008·The American Journal of Medicine·Joseph Tibaldi
Nov 1, 2005·Nitric Oxide : Biology and Chemistry·Malek Moien Ansar, Mohammad Ansari
Dec 22, 2005·Diabetes, Obesity & Metabolism·M KvapilM Shestakova
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