PMID: 3923453Mar 1, 1985

Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects

Pharmacotherapy
J M Feldman

Abstract

Glyburide, a second-generation hypoglycemic sulfonylurea, is 200 times as potent as tolbutamide. This increase is due to greater intrinsic hypoglycemic potency of the molecule rather than to a prolonged biologic half-life. Glyburide is inactivated by the liver to 4-trans-hydroxyglyburide and 3-cis-hydroxyglyburide; 50% of these compounds is excreted in the urine and 50% in the bile. Although the serum concentration of glyburide can be measured by radioimmunoassay and high-performance liquid chromatography, the importance of its serum concentration in the reduction of hyperglycemia is not yet established. Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects. To date it has a low frequency of clinically significant interactions with other drugs. Glyburide should not be prescribed for patients with liver disease or significant renal disease. Because glyburide is a potent hypoglycemic agent, it should be prescribed in small initial doses, particularly for elderly patients with diabetes. At the present time there is no definite evidence that it modifies the increased risk of cardiovascular disease of diabetic patients. A...Continue Reading

References

Mar 1, 1979·Diabetes·K KawashimaA Matsuda
Apr 30, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·H G Joost, A Hasselblatt
Jan 1, 1977·Drugs·J M Hansen, L K Christensen
Jan 1, 1977·European Journal of Clinical Pharmacology·L BalantJ Fabre
Jan 21, 1978·British Medical Journal·A MelanderP O Bitzén
Jan 1, 1975·European Journal of Clinical Pharmacology·L BalantG R Zahnd
Jan 10, 1970·Lancet·M DavidsonP Beaconsfield
Jul 1, 1972·Biochemical Pharmacology·J D Teale, A H Love
Apr 1, 1973·Annals of Internal Medicine·A M MosesM Miller
Jul 1, 1969·The American Journal of the Medical Sciences·R M KaterF L Iber
Sep 1, 1972·Clinical Pharmacology and Therapeutics·J A Taylor
Sep 1, 1971·European Journal of Clinical Investigation·N CarulliG F Salvioli
Dec 1, 1971·European Journal of Clinical Pharmacology·E SotaniemiO Koivisto
Jan 14, 1971·The New England Journal of Medicine·P N WeissmanR I Gregerman
Nov 1, 1968·Diabetes·H Podgainy, R Bressler
Oct 26, 1967·The New England Journal of Medicine·J B FieldA Remer
Jan 1, 1983·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·K ShimaY Kumahara
Nov 30, 1983·The American Journal of Medicine·H E Lebovitz, M N Feinglos
Jan 17, 1983·The American Journal of Medicine·D H LockwoodM L McCaleb
May 1, 1983·The American Journal of Medicine·S A Blumenthal
Jun 1, 1983·Diabetologia·K AsplundF Lithner
Dec 1, 1983·The Journal of Clinical Endocrinology and Metabolism·E HjøllundO Pedersen
Sep 1, 1983·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·A MatsudaK Kawashima
Nov 30, 1983·The American Journal of Medicine·J A ColwellP V Halushka
Sep 1, 1983·Diabetes Care·T KadowakiS Yoshida
Dec 22, 1983·The New England Journal of Medicine·R A Camerini-DavalosJ M Bloodworth
Sep 1, 1980·The Journal of Clinical Investigation·M J Prince, J M Olefsky
Jan 1, 1980·Acta Medica Scandinavica·G SartorE Wåhlin-Boll
Feb 1, 1981·The American Journal of Medicine·T G Skillman, J M Feldman
Jan 1, 1982·European Journal of Clinical Pharmacology·G SartorE Wåhlin-Boll
Oct 22, 1982·Deutsche medizinische Wochenschrift·H HamelbeckK Schöffling
Jan 1, 1983·Diabetes Care·L J MeltonC P Chu
Oct 1, 1980·European Journal of Clinical Pharmacology·E Wåhlin-BollB Scherstén
Apr 1, 1981·The Journal of Clinical Investigation·W S PutnamH E Lebovitz
Jan 1, 1982·European Journal of Clinical Pharmacology·E Wåhlin-BollB Scherstén
Aug 1, 1980·European Journal of Clinical Pharmacology·U Bergman Ostman
Feb 1, 1964·Metabolism: Clinical and Experimental·O LOZANO CASTANEDAA MARBLE

Citations

Sep 24, 2009·Radiation Research·Jianfei JiangJoel S Greenberger
Nov 17, 2011·Assay and Drug Development Technologies·Timothy J HaggertyJames T Kurnick
Apr 5, 2012·Evidence-based Complementary and Alternative Medicine : ECAM·Ji-Yin ZhouYan He
Nov 3, 2012·Expert Opinion on Pharmacotherapy·Elizabeth Mary LamosStephen N Davis
Dec 11, 2013·Nephrology, Dialysis, Transplantation : Official Publication of the European Dialysis and Transplant Association - European Renal Association·Paul ArnoutsWim van Biesen
Apr 26, 2017·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Rui LiManthena V S Varma
Jun 1, 1990·British Journal of Clinical Pharmacology·S W CoppackA V Rodgers
Dec 30, 2017·ELife·Kenneth Pak Kin LeeRoderick MacKinnon
Oct 17, 2012·Biomedical Chromatography : BMC·Selvan RavindranNavya Sloka
May 4, 2010·Biopharmaceutics & Drug Disposition·Lin ZhouQingcheng Mao
May 11, 2016·Expert Opinion on Drug Metabolism & Toxicology·Rana Malek, Stephen N Davis
May 30, 2019·Acta Neurologica Scandinavica·Kaibin HuangSuyue Pan
Jun 11, 1992·The Annals of Pharmacotherapy·J G GumsL R Reynolds
Mar 29, 2014·Expert Opinion on Drug Metabolism & Toxicology·André J Scheen
Jul 22, 2014·Phytotherapy Research : PTR·Prasad NeeratiAnil Kumar Gangi
Dec 15, 2015·Physiological Reviews·Monique N Foster, William A Coetzee
Jan 2, 2001·Endocrine Reviews·S MatthaeiH U Häring
Feb 27, 2003·The International Journal of Artificial Organs·C M NzerueT Edeki
Mar 10, 2015·International Journal of Molecular Sciences·Nicholas CaffesJ Marc Simard
Sep 2, 2014·Biomedical Chromatography : BMC·Selvan RavindranBidyut Nanda
Dec 1, 2020·World Neurosurgery·Michael J ArmahizerNicholas A Morris
Aug 1, 1986·The American Journal of Physiology·T B Patel

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