Pharmacokinetic and pharmacodynamic studies of glibenclamide in non-insulin dependent diabetes mellitus

British Journal of Clinical Pharmacology
S W CoppackA V Rodgers

Abstract

1. The pharmacokinetic and pharmacodynamic properties of oral glibenclamide have been studied in 31 hospitalised in-patients and 79 ambulant out-patients with diabetes mellitus. 2. Breakfast was found to have no significant influence on the kinetic behaviour of glibenclamide or on the effect of this drug on blood glucose utilisation. 3. The time course of glibenclamide kinetics after 20 mg dosing was adequately described by a two-compartment open model, yielding mean half-lives of 3.3 +/- 1.5 h (t1/2, lambda 1) and 9.7 +/- 1.2 (t1/2, z) for the initial and terminal elimination phases respectively. 4. No significant accumulation or change in kinetic profile occurred in patients who had normal renal and hepatic function, were treated continuously with glibenclamide, and then rechallenged after 8-12 weeks. 5. Despite inter-individual variations in drug absorption, peak plasma concentrations (Cmax) and the area under the plasma concentration-time curve (AUC(0-24] were dose-dependent over the dose range 5-20 mg. No significant dose-response behaviour was observed in respect of glucose utilisation, suggesting that there is little clinical benefit in using doses of glibenclamide above 5 mg day-1. 6. Comparison of plasma glibenclamide ...Continue Reading

References

Apr 16, 1979·Clinica Chimica Acta; International Journal of Clinical Chemistry·D Castoldi, O Tofanetti
Mar 1, 1979·Diabetes·K KawashimaA Matsuda
Jan 1, 1977·European Journal of Clinical Pharmacology·L BalantJ Fabre
Oct 1, 1979·British Journal of Clinical Pharmacology·C G SwiftI H Stevenson
Jan 21, 1978·British Medical Journal·A MelanderP O Bitzén
Jan 1, 1975·European Journal of Clinical Pharmacology·L BalantG R Zahnd
Mar 1, 1989·Clinical Pharmacology and Therapeutics·G F PeartG M Shenfield
Feb 1, 1989·Clinical Pharmacokinetics·P Marchetti, R Navalesi
Dec 1, 1989·British Journal of Clinical Pharmacology·P A Winstanley, M L Orme
Apr 8, 1989·British Dental Journal·J D Strahan
May 1, 1987·Diabetic Medicine : a Journal of the British Diabetic Association·S SjöbergJ Ostman
Mar 1, 1986·Clinical Pharmacology and Therapeutics·J G PearsonP G Welling
Apr 19, 1986·British Medical Journal·M Nattrass
Apr 1, 1986·Acta Endocrinologica·H IkegamiY Kumahara
May 10, 1986·British Medical Journal·J S Yudkin
Aug 1, 1986·British Journal of Clinical Pharmacology·C G SempleK R Paterson
Apr 2, 1988·British Medical Journal·R E Ferner, H A Neil
Apr 2, 1988·British Medical Journal·M OsbornD Gath
May 7, 1988·British Medical Journal·D W Ryan, J Oyston
Jan 1, 1985·European Journal of Clinical Pharmacology·L GroopF Fyhrqvist
Sep 1, 1984·Clinical Pharmacokinetics·P G Welling
Dec 1, 1984·Journal of Pharmaceutical Sciences·K KobayashiS Kaneko
Jun 1, 1983·Diabetologia·K AsplundF Lithner
Sep 1, 1983·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·A MatsudaK Kawashima
Oct 27, 1984·British Medical Journal·C F George
Oct 1, 1984·British Journal of Clinical Pharmacology·A SamantaI Shakir
May 1, 1983·Journal of Pharmacological Methods·A Johnston, R C Woollard
Jan 1, 1980·Acta Medica Scandinavica·G SartorE Wåhlin-Boll
Jan 1, 1982·European Journal of Clinical Pharmacology·G SartorE Wåhlin-Boll
Jan 1, 1982·European Journal of Clinical Pharmacology·E Wåhlin-BollB Scherstén

Citations

Mar 8, 2003·Journal of Diabetes and Its Complications·Fatima Z G A CyrinoEliete Bouskela
Aug 1, 1991·British Journal of Clinical Pharmacology·P J Neuvonen, K T Kivistö
Oct 1, 1995·Journal of Clinical Pharmacy and Therapeutics·T RydbergA Melander
Oct 23, 2013·PLoS Neglected Tropical Diseases·Gavin C K W KohW Joost Wiersinga
Jun 28, 2011·Journal of Pharmacology & Pharmacotherapeutics·S PrashanthJ Vidya Sagar
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
Mar 2, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·L M D GonçalvesP Mura
Nov 2, 2014·Clinical and Experimental Pharmacology & Physiology·Zhi-Xu HeShu-Feng Zhou
Feb 13, 2007·Trends in Cardiovascular Medicine·H M Omar Farouque, Ian T Meredith
Mar 8, 2012·British Journal of Pharmacology·Lei YuChun Jiang
May 4, 2010·Biopharmaceutics & Drug Disposition·Lin ZhouQingcheng Mao
Nov 14, 2006·Molecular and Cellular Endocrinology·Jens M BruunKarsten Buschard
Mar 18, 2005·Journal of Cardiovascular Pharmacology·Keiko UedaYukihito Higashi
Feb 18, 2003·Fundamental & Clinical Pharmacology·Denis RavelEliete Bouskela
Feb 8, 2003·The Journal of Clinical Endocrinology and Metabolism·Tsung-Ming Lee, Tsai-Fwu Chou
Aug 19, 2020·Cephalalgia : an International Journal of Headache·Mohammad Al-Mahdi Al-KaragholiMessoud Ashina
Jan 17, 2003·American Journal of Physiology. Heart and Circulatory Physiology·H M Omar Farouque, Ian T Meredith
Mar 20, 2009·Clinical Pharmacology and Therapeutics·M F HebertObstetric-Fetal Pharmacology Research Unit Network
Dec 1, 2017·PLoS Neglected Tropical Diseases·Julia A LoosAndrea C Cumino
Oct 9, 2020·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Mohammad Al-Mahdi Al-KaragholiMessoud Ashina

Related Concepts

Blood Glucose
Chromatography, Gas-Liquid
High Pressure Liquid Chromatography Procedure
Diabetes Mellitus, Non-Insulin-Dependent
Dose-Response Relationship, Drug
Nutrients
Neogluconin
Half-Life
Patient Non-Compliance

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.

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.

Pediculosis pubis

Pediculosis pubis is a disease caused by a parasitic insect known as Pthirus pubis, which infests human pubic hair, as well as other areas with hair including eye lashes. Here is the latest research.

Rh Isoimmunization

Rh isoimmunization is a potentially preventable condition that occasionally is associated with significant perinatal morbidity or mortality. Discover the latest research on Rh Isoimmunization here.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells. It also follows CRISPR-Cas9 approaches to generating genetic mutants as a means of understanding the effect of genetics on phenotype.

Enzyme Evolution

This feed focuses on molecular models of enzyme evolution and new approaches (such as adaptive laboratory evolution) to metabolic engineering of microorganisms. Here is the latest research.

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.

Pharmacology of Proteinopathies

This feed focuses on the pharmacology of proteinopathies - diseases in which proteins abnormally aggregate (i.e. Alzheimer’s, Parkinson’s, etc.). Discover the latest research in this field with this feed.

Alignment-free Sequence Analysis Tools

Alignment-free sequence analyses have been applied to problems ranging from whole-genome phylogeny to the classification of protein families, identification of horizontally transferred genes, and detection of recombined sequences. Here is the latest research.