Chapter 35
Oral Glucose-Lowering Agents
Clifford J. Bailey,
Andrew J. Krentz,
Clifford J. Bailey
School of Life and Health Sciences, Aston University, Birmingham, UK
Search for more papers by this authorAndrew J. Krentz
Institute for Cardiovascular and Metabolic Research, University of Reading, Reading, UK
Department of Population Health Sciences, King's College London, London, UK
Search for more papers by this authorClifford J. Bailey,
Andrew J. Krentz,
Clifford J. Bailey
School of Life and Health Sciences, Aston University, Birmingham, UK
Search for more papers by this authorAndrew J. Krentz
Institute for Cardiovascular and Metabolic Research, University of Reading, Reading, UK
Department of Population Health Sciences, King's College London, London, UK
Search for more papers by this authorBook Editor(s):Richard I.G. Holt MA, MB BChir, PhD, FRCP, FHEA,
Allan Flyvbjerg MD, DMSc,
Richard I.G. Holt MA, MB BChir, PhD, FRCP, FHEA
Professor in Diabetes & Endocrinology Faculty of Medicine Honorary Consultant Physician
Human Development and Health
University of Southampton, Southampton, UK
Southampton National Institute for Health Research Biomedical Research Centre, University Hospital Southampton NHS Foundation Trust, Southampton, UK
Search for more papers by this authorAllan Flyvbjerg MD, DMSc
Former CEO at Steno Diabetes Center Copenhagen (SDCC) Professor of Clinical Endocrinology
The Capital Region of Denmark
Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark
Search for more papers by this authorFirst published: 12 January 2024
Summary
Treatment of hyperglycaemia is fundamental to the management of type 2 diabetes. It is required to prevent and relieve acute symptoms and complications of hyperglycaemia; prevent, defer, and reduce the severity of microvascular complications; and afford some benefits against macrovascular complications. This chapter focuses on the role of oral blood glucose-lowering agents in the treatment of type 2 diabetes. The interdependent multiplicity of genetic and environmental factors underlying type 2 diabetes gives rise to a highly heterogeneous and progressive natural history. The pathophysiology typically involves defects of insulin secretion and insulin action. Metformin (dimethylbiguanide) is the only biguanide currently used in most countries. The history of biguanides stems from a guanidine-rich herb, Galega officinalis, which was used as a traditional treatment in Europe. Since their introduction in the 1950s, sulfonylureas have been used extensively as insulin secretagogues for the treatment of type 2 diabetes.
References
- American Diabetes Association ( 2021 ). Diab. Care 44 ( Suppl 1 ): S1 – S212 .
-
Bailey , C.J.
(
2020
).
Glucose-lowering drugs other than insulin
. In:
Encyclopedia of Molecular Pharmacology
(ed.
S. Offermanns
and
W. Rosenthal
).
Berlin
:
Springer
https://doi.org/10.1007/978-3-030-21573-6_109-1
.
10.1007/978-3-030-21573-6_109-1 Google Scholar
- Buse , J. , Wexler , D.J. , Tsapas , A. et al. ( 2020 ). Diabetologia 63 : 221 – 228 .
- Garber , A.J. , Handelsman , Y. , Grunberger , G. et al. ( 2020 ). Endocr. Pract. 26 : 107 – 139 .
- Tahrani , A. , Barnett , A.H. , and Bailey , C.J. ( 2016 ). Nat. Rev. Endocrinol. 12 : 566 – 592 .
- DeFronzo , R.A. , Ferrannini , E. , Groop , L. et al. ( 2015 ). Nat. Rev. Dis. Primers. 1 : 15019 .
- Kahn , S.E. , Cooper , M.E. , and Del Prato , S. ( 2014 ). Lancet 383 : 1068 – 1083 .
- UK Prospective Study (UKPDS) Group ( 1998 ). Lancet 352 : 837 – 853 .
- Stratton , I.M. , Adler , A.I. , Neil , H.A. et al. ( 2000 ). BMJ 321 : 405 – 412 .
- Holman , R.R. , Paul , S.K. , Bethel , M.A. et al. ( 2008 ). N. Engl. J. Med. 359 : 1577 – 1589 .
- Action to Control Cardiovascular Risk in Diabetes Study Group ( 2008 ). N. Engl. J. Med. 358 : 2545 – 2559 .
- ADVANCE Collaborative Group ( 2008 ). N. Engl. J. Med. 358 : 2560 – 2572 .
- Duckworth , W. , Abraira , C. , Moritz , T. et al. ( 2009 ). N. Engl. J. Med. 360 : 129 – 139 .
- Riddle , M.C. , Ambrosius , W.T. , Brillon , D.J. et al. ( 2010 ). Diab. Care 33 : 983 – 990 .
- Kosiborod , M. , Inzucchi , S.E. , Krumholz , H.M. et al. ( 2008 ). Circulation 117 : 1018 – 1027 .
- Bonora , E. , Calcaterra , F. , Lombardi , S. et al. ( 2001 ). Diab. Care 24 : 2023 – 2029 .
- Ceriello , A. and Genovese , S. ( 2016 ). Revs. Endocr. Metab. Dis. 17 : 111 – 116 .
- Scheen , A.J. and van Gaal , L.F. ( 2015 ). Lancet Diab. Endocrinol. 2 : 911 – 922 .
- Home , P. , Riddle , M. , Cefalu , W.T. et al. ( 2014 ). Diab. Care 37 : 1499 – 1506 .
- Lascar , N. , Brown , J. , Pattison , H. et al. ( 2018 ). Lancet Diab. Endocrinol. 6 : 69 – 80 .
- Bellary , S. , Kyrou , I. , Brown , J.E. , and Bailey , C.J. ( 2021 ). Nat. Rev. Endocrinol. 17 : 534 – 548 .
- Bailey , C.J. ( 2017 ). Diabetologia 60 : 1566 – 1576 .
- Bailey , C.J. and Turner , R.C. ( 1996 ). N. Engl. J. Med. 334 : 574 – 579 .
- Campbell , I.W. , Howlett , H.C. , Holman , R.R. , and Bailey , C.J. ( 2017 ). Metformin: 60 Years of Clinical Experience . Weinheim : Wiley-VCH .
- Bailey , C.J. ( 2008 ). Cardiovasc. Drugs Ther. 22 : 215 – 224 .
- Han , Y. , Xie , H. , Liu , Y. et al. ( 2019 ). Cardiovasc. Diabetol. 18 : 96 .
- Bailey , C.J. ( 2012 ). Nat Rev Endocrinol 8 : 449 – 450 .
- LaMoia , T.E. and Shulman , G.I. ( 2021 ). Endocr. Rev. 42 : 77 : – 96 .
- Scheen , A.J. ( 1996 ). Clin. Pharmacokinet. 30 : 359 – 371 .
- Bailey , C.J. ( 2014 ). Metformin . In: Therapy for Diabetes Mellitus and Related Disorders , 6e (ed. G.E. Umpierrez ), 341 – 358 . Alexandria, VA : American Diabetes Association .
- Sharpe , A. , Morley , L.C. , Tang , T. et al. ( 2019 ). Cochrane Database Syst. Rev. ( 12 ): CD013505 .
- UK Prospective Diabetes Study Group ( 1998 ). Lancet 352 : 854 – 865 .
- Diabetes Prevention Program Research Group ( 2002 ). N. Engl. J. Med. 346 : 393 – 403 .
- Hostalek , U. , Gwilt , M. , and Hildemann , S. ( 2015 ). Drugs 75 : 1071 – 1094 .
- Inzucchi , S.E. , Lipska , K.J. , Mayo , H. et al. ( 2014 ). JAMA 312 : 2668 – 2675 .
- Henquin , J.C. ( 1992 ). Diabetologia 35 : 907 – 912 .
- Proks , P. , Reimann , F. , Green , N. et al. ( 2002 ). Diabetes 51 ( Suppl 3 ): S368 – S376 .
- Rorsman , P. and Renstrom , E. ( 2003 ). Diabetologia 46 : 1029 – 1045 .
- Ball , A.J. , Flatt , P.R. , and McClenaghan , N.H. ( 2000 ). Eur. J. Pharmacol. 408 : 327 – 333 .
- Lebovitz , H.E. ( 1999 ). Diab. Rev. 7 : 139 – 151 .
- Sola , D. , Rossi , L. , Schianca , G.P. et al. ( 2015 ). Arch. Med. Sci. 11 : 840 – 848 .
- Rendell , M. ( 2004 ). Drugs 64 : 1339 – 1358 .
- Schernthaner , G. , Grimaldi , A. , Di Mario , U. et al. ( 2004 ). Eur. J. Clin. Invest. 34 : 535 – 542 .
- Krentz , A.J. , Ferner , R.E. , and Bailey , C.J. ( 1994 ). Drug Saf. 11 : 223 – 241 .
- Wexler , D.J. ( 2019 ). JAMA 322 : 1147 – 1149 .
- Garrino , M.G. , Schmeer , W. , Nenquin , M. et al. ( 1985 ). Diabetologia 28 : 697 – 703 .
- Blickle , J.F. ( 2006 ). Diab. Metab. 32 : 113 – 120 .
- Yki-Jarvinen , H. ( 2004 ). N. Engl. J. Med. 351 : 1106 – 1118 .
- Nissen , S.E. and Wolski , K. ( 2007 ). N. Engl. J. Med. 356 : 2457 – 2471 .
- Dormandy , J.A. , Charbonnel , B. , Eckland , D.J. et al. ( 2005 ). Lancet 366 : 1279 – 1289 .
- Kernan , W.N. , Viscoli , C.M. , Furie , K.L. et al. ( 2016 ). N. Engl. J. Med. 374 : 1321 – 1331 .
- Dubois , V. , Eeckhoute , J. , Lefebvre , P. , and Staels , B. ( 2017 ). J. Clin. Invest. 127 : 1202 – 1214 .
- Lebovitz , H.E. ( 2019 ). Curr. Diab. Rep. 19 : 151 .
- Kahn , S.E. , Haffner , S.M. , Heise , M.A. et al. ( 2006 ). N. Engl. J. Med. 355 : 2427 – 2443 .
- Vaccaro , O. , Masulli , M. , Nicolucci , A. et al. ( 2017 ). Lancet Diab. Endocrinol. 5 : 887 – 897 .
- Holst , J.J. ( 2019 ). Metabolism 96 : 46 – 55 .
- Nauck , M.A. and Meier , J.J. ( 2018 ). Diabetes Obes. Metab. 20 ( Suppl 1 ): 5 – 21 .
- Drucker , D.J. ( 2018 ). Cell Metab. 27 : 740 – 756 .
- Nauck , M.A. , Vardarli , I. , Deacon , C.F. et al. ( 2011 ). Diabetologia 54 : 10 – 18 .
- Deacon , C.F. ( 2011 ). Diab. Obes. Metab. 13 : 7 – 18 .
- Deacon , C.F. ( 2019 ). Front. Endocrinol. 10 : 80 .
- Ling , J. , Cheng , P. , Ge , L. et al. ( 2019 ). Acta Diabetol. 56 : 249 – 272 .
- Gallwitz , B. ( 2019 ). Front. Endocrinol. 10 : 389 .
- Liu , D. , Jin , B. , Chen , W. , and Yun , P. ( 2019 ). BMC Pharmacol. Toxicol. 20 : 15 .
- Wright , E.M. , Loo , D.D. , and Hirayama , B.A. ( 2011 ). Physiol. Rev. 91 : 733 – 794 .
- Ghezzi , C. , Loo , D.D. , and Wright , E.M. ( 2018 ). Diabetologia 61 : 2087 – 2097 .
-
Bailey , C.J.
(
2015
).
New drugs for the treatment of diabetes mellitus
. In:
International Textbook of Diabetes Mellitus
,
4e
(ed.
R.A. DeFronzo
,
E. Ferrannini
,
P. Zimmet
and
G.M. Alberti
),
709
–
725
.
Chichester
:
Wiley
.
10.1002/9781118387658.ch47 Google Scholar
- DeFronzo , R.A. , Hompesch , M. , Kasichayanula , S. et al. ( 2013 ). Diab. Care 36 : 3169 – 3176 .
- Abdul-Ghani , M.A. , Norton , L. , and DeFronzo , R.A. ( 2015 ). Am. J. Physiol. Renal. Physiol. 309 : F889 – F900 .
- Mudaliar , S. , Polidori , D. , Zambrowicz , B. , and Henry , R.R. ( 2015 ). Diab. Care 38 : 2344 – 2353 .
- Nauck , M.A. ( 2014 ). Drug Des. Dev. Ther. 8 : 1335 – 1380 .
-
Alves , C.
,
Penedones , A.
,
Mendes , D.
, and
Marques , F.B.
(
2015
).
Clin. Ther.
37
:
e123
.
10.1016/j.clinthera.2015.05.352 Google Scholar
- Li , J. , Gong , Y. , Li , C. et al. ( 2017 ). Medicine 96 : e7201 .
- Scheen , A.J. ( 2015 ). Clin. Pharmacokinet. 54 : 691 – 708 .
- Scheen , A.J. ( 2020 ). Nat. Rev. Endocrinol. 16 : 556 – 577 .
- Monami , M. , Nardini , C. , and Mannucci , E. ( 2014 ). Diab. Obes. Metab. 16 : 457 – 466 .
- Bailey , C.J. and Day , C. ( 2019 ). Diab. Res. Clin. Pract. 155 : 107785 .
- McGuire , D.K. , Shih , W.J. , Cosentino , F. et al. ( 2021 ). JAMA Cardiol. 6 : 148 – 158 .
- Zannad , F. , Ferreira , J.P. , Pocock , S.J. et al. ( 2020 ). Lancet 396 : 819 – 829 .
- Bailey , C.J. and Marx , N. ( 2019 ). Diab. Obes. Metab. 21 : 3 – 14 .
- Heerspink , H.J. , Kosiborod , M. , Inzucchi , S.E. , and Cherney , D.Z. ( 2018 ). Kidney Int. 94 : 26 – 39 .
- Taylor , S. , Blau , J.E. , and Rother , K.I. ( 2015 ). J. Clin. Endocrinol. Metab. 100 : 2849 – 2852 .
- Thethi , T.K. , Pratley , R. , and Meier , J.J. ( 2020 ). Diab. Obes. Metab. 22 : 1263 – 1277 .
- Lebovitz , H.E. ( 1998 ). Diab. Rev. 6 : 132 – 145 .
- Hedrington , M.S. and Davis , S.N. ( 2019 ). Expert Opin. Pharmacother. 20 : 2229 – 2235 .
- Chiasson , J.L. , Josse , R.G. , Gomis , R. et al. ( 2002 ). Lancet 359 : 2072 – 2077 .
- Holman , R.R. , Coleman , R.L. , Chan , J.C.N. et al. ( 2017 ). Lancet Diab. Endocrinol. 5 : 877 – 886 .
- Chiasson , J.-L. , Josse , R.G. , Gomis , R. et al. ( 2003 ). JAMA 290 : 486 – 494 .
- Holt , R.I.G. , Barnett , A.H. , and Bailey , C.J. ( 2010 ). Diab. Obes. Metab. 12 : 1048 – 1057 .
- DeFronzo , R.A. ( 2011 ). Diab. Care 34 : 789 – 794 .
- Handelsman , Y. ( 2011 ). Diab. Care 34 ( Suppl 2 ): S244 – S250 .
- Bailey , C.J. ( 2011 ). BMJ 342 : d1996 .
- Taylor , R. and Barnes , A.C. ( 2018 ). Diabetologia 61 : 273 – 283 .
- Van Gaal , L. and Scheen , A. ( 2015 ). Diab. Care 38 : 1161 – 1172 .
- Bailey , C.J. and Day , C. ( 2009 ). Diab. Obes. Metab. 11 : 527 – 533 .
- Abdul-Ghani , M. , Puckett , C. , Adams , J. et al. ( 2020 ). Diab. Care 44 : 433 – 439 .
- Food and Drug Administration ( 2019 ). New drug application 2020/212614Orig1s000. TRIJARDY XR. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212614Orig1s000MedR.pdf (accessed 6 February 2023).
