PMID: 8576296Oct 1, 1995Paper

Comparison of the kinetics of glyburide and its active metabolites in humans

Journal of Clinical Pharmacy and Therapeutics
T RydbergA Melander

Abstract

The pharmacokinetics of glyburide (Gb) and its active metabolites, 4-trans-hydroxyglibenclamide (M1) and 3-cis-hydroxyglibenclamide (M2), were compared in eight healthy subjects. After an overnight fast, each subject received a 3.5-mg single dose of Gb, M1 or M2 intravenously in random cross-over order. For comparison, a 3.5-mg oral dose of micronized formulation of Gb was also given in a test. The subjects continued to fast until standard meals were given at 0.5 and 5.5 h after each dose. Serum samples and urine fractions were collected for 10 h. Serum concentrations of Gb, M1 and M2, and urine concentrations of M1 and M2 were determined by a selective and sensitive liquid chromatographic method. The two metabolites had very similar pharmacokinetic profiles, except for volume of distribution and renal clearance. Estimated mean volume of distribution, total and renal clearance of M1 and M2 were 20.8 +/- 8.4 litres, 11.9 +/- 1.7 litres/h, 13.5 +/- 3.7 litres/h and 15.5 +/- 5.5 litres, 10.4 +/- 1.3 litres/h, 8.6 +/- 1.6 litres/h, respectively. Estimates of the volume of distribution and total clearance were significantly higher than those of Gb, which were 7.44 +/- 1.53 litres, 4.42 +/- 0.56 litres/h intravenously and 9.32 +/- 2....Continue Reading

References

Jan 1, 1977·European Journal of Clinical Pharmacology·L BalantJ Fabre
Jan 1, 1975·European Journal of Clinical Pharmacology·L BalantG R Zahnd
Jun 1, 1990·British Journal of Clinical Pharmacology·S W CoppackA V Rodgers
Sep 1, 1990·British Journal of Clinical Pharmacology·M L Dahl-PuustinenI Wikström
Mar 1, 1989·Clinical Pharmacology and Therapeutics·G F PeartG M Shenfield
Sep 1, 1988·Journal of Pharmaceutical Sciences·B P ImbimboG Bassotti
Mar 1, 1986·Clinical Pharmacology and Therapeutics·J G PearsonP G Welling
Apr 1, 1986·Acta Endocrinologica·H IkegamiY Kumahara
Nov 1, 1987·Diabetes Care·S G HartlingA Melander
Dec 1, 1985·Journal of Pharmacokinetics and Biopharmaceutics·K S Pang
Jan 1, 1985·European Journal of Clinical Pharmacology·L GroopF Fyhrqvist
Jan 1, 1985·European Journal of Clinical Pharmacology·D BrockmeierH Leonhardt
Apr 1, 1974·Journal of Pharmacokinetics and Biopharmaceutics·H G BoxenbaumR M Elashoff
Feb 1, 1973·The Journal of Clinical Pharmacology and New Drugs·L M FuccellaG Valzelli
Jan 1, 1981·Pharmacology & Therapeutics·J B Houston
Jan 1, 1993·European Journal of Clinical Pharmacology·L A JaberI R Welshman
Feb 1, 1994·Diabetes Care·A JönssonA Melander

Citations

Jul 27, 2007·Journal of Pharmacokinetics and Pharmacodynamics·Radojka M SavicMats O Karlsson
Oct 27, 2010·Nephrology, Dialysis, Transplantation : Official Publication of the European Dialysis and Transplant Association - European Renal Association·Matthew A WeirAmit X Garg
Jun 24, 1998·The Journal of Clinical Investigation·M H NathansonL Rios-Velez
Feb 12, 2004·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·J L C M DorneA G Renwick
Jun 12, 2009·Drug Metabolism Reviews·Shu-Feng ZhouBalram Chowbay
Apr 28, 2007·Biochemical Pharmacology·Olga L ZharikovaMahmoud S Ahmed
Sep 2, 2014·Biomedical Chromatography : BMC·Selvan RavindranBidyut Nanda
Oct 3, 2006·Biochemical Pharmacology·Selvan RavindranMahmoud S Ahmed
Jan 1, 1999·Nutritional Neuroscience·D S Roane, J K Bounds
Apr 26, 2017·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Rui LiManthena V S Varma

Related Concepts

High Pressure Liquid Chromatography Procedure
Neogluconin
Hypoglycemic Effect
Intravenous Injections
Molecular Stereochemistry
Cross-Over Studies

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Lipidomics & Rhinovirus Infection

Lipidomics can be used to examine the lipid species involved with pathogenic conditions, such as viral associated inflammation. Discovered the latest research on Lipidomics & Rhinovirus Infection.

Spatio-Temporal Regulation of DNA Repair

DNA repair is a complex process regulated by several different classes of enzymes, including ligases, endonucleases, and polymerases. This feed focuses on the spatial and temporal regulation that accompanies DNA damage signaling and repair enzymes and processes.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Torsion Dystonia

Torsion dystonia is a movement disorder characterized by loss of control of voluntary movements appearing as sustained muscle contractions and/or abnormal postures. Here is the latest research.

Archaeal RNA Polymerase

Archaeal RNA polymerases are most similar to eukaryotic RNA polymerase II but require the support of only two archaeal general transcription factors, TBP (TATA-box binding protein) and TFB (archaeal homologue of the eukaryotic general transcription factor TFIIB) to initiate basal transcription. Here is the latest research on archaeal RNA polymerases.

Alzheimer's Disease: MS4A

Variants within the membrane-spanning 4-domains subfamily A (MS4A) gene cluster have recently been implicated in Alzheimer's disease in genome-wide association studies. Here is the latest research on Alzheimer's disease and MS4A.

Central Pontine Myelinolysis

Central Pontine Myelinolysis is a neurologic disorder caused most frequently by rapid correction of hyponatremia and is characterized by demyelination that affects the central portion of the base of the pons. Here is the latest research on this disease.