Sulfonylureas and their use in clinical practice

Daniele Sola, Luca Rossi, Gian Piero Carnevale Schianca, Pamela Maffioli, Marcello Bigliocca, Roberto Mella, Francesca Corlianò, Gian Paolo Fra, Ettore Bartoli, Giuseppe Derosa, Daniele Sola, Luca Rossi, Gian Piero Carnevale Schianca, Pamela Maffioli, Marcello Bigliocca, Roberto Mella, Francesca Corlianò, Gian Paolo Fra, Ettore Bartoli, Giuseppe Derosa

Abstract

Many anti-diabetic drugs with different mechanisms of action are now available for treatment of type 2 diabetes mellitus. Sulfonylureas have been extensively used for treatment of type 2 diabetes for nearly 50 years and, even in our times, are widely used for treatment of this devastating chronic illness. Here, we review some of the available data on sulfonylureas, evaluating their mechanism of action and their effects on glycemic control. We can conclude that sulfonylureas are still the most used anti-diabetic agents: maybe this is due to their lower cost, to the possibility of mono-dosing and to the presence of an association with metformin in the same tablet. However, sulfonylureas, especially the older ones, are linked to a greater prevalence of hypoglycemia, and cardiovascular risk; newer prolonged-release preparations of sulfonylureas are undoubtedly safer, mainly due to reducing hypoglycemia, and for this reason should be preferred.

Keywords: glycemic control; hypoglycemia; sulfonylureas.

Figures

Figure 1
Figure 1
Mechanism of action of sulfonylureas On the top right corner is represented the SUR, while octagon is sulfonylurea (SU). When the SU binds SUR, the flow of K (arrows) stopped, so the cell membrane is depolarized. An increased flow of calcium cause the contraction of the filaments of actomyosin responsible for the exocytosis of insulin.

References

    1. Derosa G, Maffioli P. Thiazolidinediones plus metformin association on body weight in patients with type 2 diabetes. Diabetes Res Clin Pract. 2011;91:265–13.
    1. Derosa G, Tinelli C, Maffioli P. Effects of pioglitazone and rosiglitazone combined with metformin on body weight in people with diabetes. Diabetes Obes Metab. 2009;11:1091–9.
    1. Cicero AFG, Tartagni E, Ertek S. Metformin and its clinical use: new insights for an old drug in clinical practice. Arch Med Sci. 2012;8:907–17.
    1. Derosa G, Maffioli P. Efficacy and safety profile evaluation of acarbose alone and in association with other antidiabetic drugs: a systematic review. Clin Ther. 2012;34:1221–36.
    1. Derosa G, Maffioli P. Alpha-glucosidase inhibitors and their use in clinical practice. Arch Med Sci. 2012;8:899–906.
    1. Derosa G, Maffioli P. Dipeptidyl peptidase-4 inhibitors: 3 years of experience. Diabetes Technol Ther. 2012;14:350–64.
    1. Derosa G, Maffioli P. Patient considerations and clinical utility of a fixed dose combination of saxagliptin/metformin in the treatment of type 2 diabetes. Diabetes Metab Syndr Obes. 2011;4:263–71.
    1. Derosa G, Maffioli P. GLP-1 agonists exenatide and liraglutide: a review about their safety and efficacy. Curr Clin Pharmacol. 2012;7:214–28.
    1. Derosa G, Maffioli P. Optimizing glycemic control: clinical utility of exenatide prolonged release injection. Res Rep Endocr Disord. 2012;2:41–51.
    1. Bressler R, Johnson DG. Pharmacological regulation of blood glucose levels in non-insulin-dependent diabetes mellitus. Arch Intern Med. 1997;157:836–48.
    1. American Diabetes Association. Standards of Medical Care in Diabetes-2013. Diabetes Care. 2013;36(Suppl. 1):S11–66.
    1. Ramracheya R, Ward C, Shigeto M, et al. Membrane potential-dependent inactivation of voltage-gated ion channels in alpha-cells inhibits glucagon secretion from human islets. Diabetes. 2010;59:2198–208.
    1. Braun M, Ramracheya R, Amisten S, et al. Somatostatin release, electrical activity, membrane currents and exocytosis in human pancreatic delta cells. Diabetologia. 2009;52:1566–78.
    1. Olefsky JM, Reaven GM. Effects of sulphonylurea therapy on insulin binding to mononuclear leukocytes of diabetic patients. Am J Med. 1976;60:89–95.
    1. Blumenthal SA. Potentiation of the hepatic action of insulin by chlorpropamide. Diabetes. 1977;26:485–9.
    1. Shorr RI, Ray WA, Daugherty JR, Griffin MR. Individual sulfonylureas and serious hypoglycemia in older people. J Am Geriatr Soc. 1996;44:751–5.
    1. Lebovitz HE, Feinglos MN. Sulfonylurea drugs: mechanism of antidiabetic action and therapeutic usefulness. Diabetes Care. 1978;1:189–98.
    1. Stenman S, Melander A, Groop PH, Groop LC. What is the benefit of increasing the sulphonylurea dose? Ann Intern Med. 1993;118:169–72.
    1. Jönsson A, Rydberg T, Ekberg G, Hallengren B, Melander A. Slow elimination of glyburide in NIDDM subjects. Diabetes Care. 1994;17:142–5.
    1. Rydberg T, Jönsson A, Røder M, Melander A. Hypoglycemic activity of glyburide (glibenclamide) metabolites in humans. Diabetes Care. 1994;17:1026–30.
    1. Winkler G, Gerô L. Pharmacogenetics of insulin secretagogue antidiabetics. Orv Hetil. 2011;152:1651–60.
    1. Hermann LS, Scherstén B, Bitzén PO, Kjellström T, Lindgärde F, Melander A. Therapeutic comparison of metformin and sulphonylurea, alone and in various combinations. A double-blind controlled study. Diabetes Care. 1994;17:1100–9.
    1. Tessier D, Dawson K, Tétrault JP, Bravo G, Meneilly GS. Glibenclamide vs gliclazide in type 2 diabetes of the elderly. Diabet Med. 1994;11:974–80.
    1. Holstein A, Plaschke A, Egberts EH. Lower incidence of severe hypoglycemia in patients with type 2 diabetes treated with glimepiride versus glibenclamide. Diabetes Metab Res Rev. 2001;17:467–73.
    1. Gangji AS, Cukierman T, Gerstein HC, Goldsmith CH, Clase CM. A systematic review and meta-analysis of hypoglycemia and cardiovascular events: a comparison of glyburide with other secretagogues and with insulin. Diabetes Care. 2007;30:389–94.
    1. Shorr RI, Ray WA, Daugherty JR, Griffin MR. Incidence and risk factors for serious hypoglycemia in older persons using insulin or sulfonylureas. Arch Intern Med. 1997;157:1681–6.
    1. Bressler P, DeFronzo RA. Drugs and diabetes. Diabetes Rev. 1994;2:53–84.
    1. Shorr RI, Ray WA, Daugherty JR, Griffin MR. Incidence and risk factors for serious hypoglycemia in older persons using insulin or sulfonylureas. Arch Intern Med. 1997;157:1681–6.
    1. Lee YH, Lee BW, Chun SW, Cha BS, Lee HC. Predictive characteristics of patients achieving glycemic control with insulin after sulphonylurea failure. Int J Clin Pract. 2011;65:1076–84.
    1. Derosa G, Limas CP, Macías PC, Estrella A, Maffioli P. Dietary and nutraceutical approach to type 2 diabetes. Arch Med Sci. 2014;10:336–44.
    1. Groop L, Eriksson CJ, Huupponen R, Ylikahri R, Pelkonen R. Roles of chlorpropamide, alcohol and acetaldehyde in determining the chlorpropamide-alcohol flush. Diabetologia. 1984;26:34–8.
    1. Kadowaki T, Hagura R, Kajinuma H, Kuzuya N, Yoshida S. Chlorpropamide-induced hyponatremia: incidence and risk factors. Diabetes Care. 1983;6:468–71.
    1. Rao AD, Kuhadiya N, Reynolds K, Fonseca VA. Is the combination of sulfonylureas and metformin associated with an increased risk of cardiovascular disease or all-cause mortality? A meta-analysis of observational studies. Diabetes Care. 2008;31:1672–8.
    1. Morgan CL, Poole CD, Evans M, Barnett AH, Jenkins-Jones S, Currie CJ. What next after metformin? A retrospective evaluation of the outcome of second-line, glucose-lowering therapies in people with type 2 diabetes. J Clin Endocrinol Metab. 2012;97:4605–12.
    1. Kasznicki J, Drzewoski J. Heart failure in the diabetic population – pathophysiology, diagnosis and management. Arch Med Sci. 2014;10:546–56.
    1. A study of the effects of hypoglycemia agents on vascular complications in patients with adult-onset diabetes. VI. Supplementary report on nonfatal events in patients treated with tolbutamide. Diabetes. 1976;25:1129–53.
    1. Garratt KN, Brady PA, Hassinger NL, Grill DE, Terzic A, Holmes DR., Jr Sulphonylurea drugs increase early mortality in patients with diabetes mellitus after direct angioplasty for acute myocardial infarction. J Am Coll Cardiol. 1999;33:119–24.
    1. Malmberg K. Prospective randomised study of intensive insulin treatment on long term survival after acute myocardial infarction in patients with diabetes mellitus. DIGAMI (Diabetes Mellitus, Insulin Glucose Infusion in Acute Myocardial Infarction) Study Group. BMJ. 1997;314:1512–5.
    1. Simpson SH, Majumdar SR, Tsuyuki RT, Eurich DT, Johnson JA. Dose-response relation between sulphonylurea drugs and mortality in type 2 diabetes mellitus: a population-based cohort study. CMAJ. 2006;174:169–74.
    1. Abdelmoneim AS, Hasenbank SE, Seubert JM, Brocks DR, Light PE, Simpson SH. Variations in tissue selectivity amongst insulin secretagogues: a systematic review. Diabetes Obes Metab. 2012;14:130–8.
    1. Terao Y, Ayaori M, Ogura M, et al. Effect of sulphonylurea agents on reverse cholesterol transport in vitro and vivo. Diab Vasc Dis Res. 2011;18:513–30.
    1. Billman GE. The cardiac sarcolemmal ATP-sensitive potassium channel as a novel target for anti-arrhythmic therapy. Pharmacol Ther. 2008;120:54–70.
    1. Miki T, Liss B, Minami K, et al. ATP-sensitive K+ channels in the hypothalamus are essential for the maintenance of glucose homeostasis. Nat Neurosci. 2001;4:507–12.
    1. Zeller M, Danchin N, Simon D, et al. French Registry of Acute ST-Elevation and Non-ST-Elevation Myocardial Infarction investigators. Impact of type of preadmission sulfonylureas on mortality and cardiovascular outcomes in diabetic patients with acute myocardial infarction. J Clin Endocrinol Metab. 2010;95:4993–5002.
    1. Schramm TK, Gislason GH, Vaag A, et al. Mortality and cardiovascular risk associated with different insulin secretagogues compared with metformin in type 2 diabetes, with or without a previous myocardial infarction: a nationwide study. Eur Heart J. 2011;32:1900–8.
    1. ADVANCE Collaborative Group. Patel A, MacMahon S, Chalmers J, et al. Intensive blood glucose control and vascular outcomes in patients with type 2 diabetes. N Engl J Med. 2008;358:2560–72.
    1. Bowker SL, Majumdar SR, Veugelers P, Johnson JA. Increased cancer-related mortality for patients with type 2 diabetes who use sulfonylureas or insulin. Diabetes Care. 2006;29:254–8.
    1. Monami M, Balzi D, Lamanna C, et al. Are sulfonylureas all the same? A cohort study on cardiovascular and cancer-related mortality. Diabetes Metab Res Rev. 2007;23:479–84.
    1. Gerich J, Raskin P, Jean-Louis L, Purkayastha D, Baron MA. PRESERVE-beta: two-year efficacy and safety of initial combination therapy with nateglinide or glyburide plus metformin. Diabetes Care. 2005;28:2093–9.
    1. Nestler JE. Metformin in the treatment of infertility in polycystic ovarian syndrome: an alternative perspective. Fertil Steril. 2008;90:14–6.
    1. Derosa G, Putignano P, Bossi AC, et al. Exenatide or glimepiride added to metformin on metabolic control and on insulin resistance in type 2 diabetic patients. Eur J Pharmacol. 2011;666:251–6.
    1. Derosa G, Maffioli P, Salvadeo SA, et al. Exenatide versus glibenclamide in patients with diabetes. Diabetes Technol Ther. 2010;12:233–40.
    1. Hirst JA, Farmer AJ, Dyar A, Lung TW, Stevens RJ. Estimating the effect of sulfonylurea on HbA1c in diabetes: a systematic review and meta-analysis. Diabetologia. 2013;56:973–84.
    1. Derosa G, Cicero AF, Fogari E, D'Angelo A, Bianchi L, Maffioli P. Pioglitazone compared to glibenclamide on lipid profile and inflammation markers in type 2 diabetic patients during an oral fat load. Horm Metab Res. 2011;43:505–12.
    1. Derosa G, Maffioli P. Effects of thiazolidinediones and sulfonylureas in patients with diabetes. Diabetes Technol Ther. 2010;12:491–501.
    1. Derosa G. Pioglitazone plus glimepiride: a promising alternative in metabolic control. Int J Clin Pract Suppl. 2007;153:28–36.
    1. Derosa G, Cicero AF, D'Angelo A, et al. Effects of 1 year of treatment with pioglitazone or rosiglitazone added to glimepiride on lipoprotein (a) and homocysteine concentrations in patients with type 2 diabetes mellitus and metabolic syndrome: a multicenter, randomized, double-blind, controlled clinical trial. Clin Ther. 2006;28:679–88.
    1. Derosa G, Maffioli P, Ferrari I, et al. Effects of one year treatment of vildagliptin added to pioglitazone or glimepiride in poorly controlled type 2 diabetic patients. Horm Metab Res. 2010;42:663–9.
    1. Schernthaner G, Grimaldi A, Di Mario U, et al. GUIDE study: double-blind comparison of once-daily gliclazide MR and glimepiride in type 2 diabetic patients. Eur J Clin Invest. 2004;34:535–42.

Source: PubMed

Sponsor e collaboratori

Condizioni mediche

Interventi farmacologici

3
Sottoscrivi