Sulfonylureas: Basic Aspects and Clinical Uses
H.E. Lebovitz, A. Melander,
A. Melander
The NEPI Foundation, Medical Research Centre, University Hospital, Malmö, Sweden
Search for more papers by this authorH.E. Lebovitz, A. Melander,
A. Melander
The NEPI Foundation, Medical Research Centre, University Hospital, Malmö, Sweden
Search for more papers by this authorAbstract
This chapter describes the chemistry, mechanism of action, pharmacodynamics, pharmacokinetics, kinetics–effect relations, clinically beneficial and adverse effects of sulfonylurea drugs, as well as the efficacy of these agents in randomized-controlled clinical trials and other studies. It also compares the different sulfonylurea compounds, especially in terms of differences in potency, rate of onset, and duration of action, and how such differences may contribute to different clinical profiles of the various compounds. In addition, some important interactions with other drugs are listed. Their appropriate place in the therapeutic armamentarium concerning type 2 diabetes is thoroughly discussed.
References
- 1 Kennedy DL, Piper JM, Baum C. Trends in the use of oral hypoglycemic agents. Diabetes Care 1988; 11: 558–62.
- 2 Boccuzzi SJ, Sung JCY, Wogen J, Shah AB, Fox J, Kim J. Utilization of oral hypoglycemic agents in a drug-insured U.S. population. Diabetes Care 2001; 24: 1411–5.
- 3 Melander A, Bitzén P-O, Faber O, Groop L. Sulphonylurea antidiabetic drugs: an update of their clinical pharmacology and rational therapeutic use. Drugs 1989; 37: 58–72.
- 4 Ribes G, Trimble ER, Blayac JP, Wollheim CB, Puech R, Loubatières-Mariani MM. Effect of a new hypoglycaemic agent (HB 699) on the in vivo secretion of pancreatic hormones in the dog. Diabetologia 1981; 20: 501–5.
- 5 Garrino M-G, Meissner H-P, Henquin J-C. The non-sulphonylurea moiety of gliquidone mimics the effects of the parent molecule on pancreatic B-cells. Eur J Pharmacol 1986; 124: 309–16.
- 6 Proks P, Reimann F, Green N, Gribble F, Ashcroft F. Sulfonylurea stimulation of insulin secretion. Diabetes 2002; 51 (suppl 1): S 368–76.
- 7 Hansen AM, Christensen IT, Hansen JB, Carr RD, Ashcroft FM, Wahl P. Differential interactions of nateglinide and repaglinide on the human beta-cell sulphonylurea receptor 1. Diabetes 2002; 51: 2789–95.
- 8 Hellman B, Sehlin J, Täljedal I-B. The pancreatic B-cell recognition of insulin secretagogues, II: sites of action of tolbutamide. Biochem Biophys Res Comm 1971; 45: 1384–8.
- 9 Aguilar-Bryan L, Bryan J. Molecular biology of adenosine triphosphate-sensitive potassium channels. Endocr Rev 1999; 20: 101–35.
- 10 Cook DL, Satin LS, Ashford MLJ, Hales CN. ATP-sensitive K+ channels in pancreatic B-cells. Spare channel hypothesis. Diabetes 1988; 37: 49 5–8.
- 11 Boyd AE III. Sulfonylurea receptors, ion channels, and fruit flies. Diabetes 1988; 37: 847–50.
- 12 Levine R. Sulfonylureas: background development of the field. Diabetes Care 1984; 7 (suppl 1): 3–7.
- 13 Loubatières A. Analyse du mécanisme de l'action hypoglycemiante du p-aminobenzène-sulfamidothiodiazol. Compt Rend Soc Biol 1944; 138: 766–7.
- 14 Mirsky IA, Perisutti G, Jinks R. Ineffectiveness of sulfonylureas in alloxan diabetic rats. Proc Soc Exp Biol Med 1956; 91: 475–7.
- 15 Parker ML, Pildes RS, Chao K, Cornblath M, Kipnis DM. Juvenile diabetes mellitus. A deficiency in insulin. Diabetes 1968; 17: 27–32.
- 16 Joffe BI, Jackson WPU, Bank S, Vinik AI. Effect of oral hypoglycemic agents on glucose tolerance in pancreatic diabetes. Gut 1972; 13: 285–7.
- 17 Yalow RS, Black H, Villazon M, Berson SA. Comparison of plasma insulin levels following administration of tolbutamide and glucose. Diabetes 1960; 9: 356–62.
- 18 Hellman B, Täljedal I-B. Effects of sulphonylurea derivatives on pancreatic beta cells. In E Dorzbach (ed), Insulin, Part 2. Berlin: Springer, 1975: pp 175–94.
- 19 Malaisse WJ, Lebrun P. Mechanisms of sulfonylurea-induced insulin release. Diabetes Care 1990; 13 (suppl 3): 9–17.
- 20 Wick AN, Britton B, Gabowski R. The action of a sulfonylurea hypoglycemic agent (Orinase) in extrahepatic tissues. Metabolism 1956; 5: 739–43.
- 21 Bowen V, Lazarus NR. Insulin release from the perfused rat pancreas. Biochem J 1974; 142: 385–9.
- 22 Schmid-Antomarchi H, De Weille J, Fosset M, Lazdunski M. The receptor for antidiabetic sulphonylureas controls the activity of the ATP-modulated K+ channel in insulin secreting cells. J Biol Chem 1987; 262: 15840–4.
- 23 Siconolfi-Baez L, Banerji MA, Lebovitz HE. Characterization and significance of sulfonylurea receptors. Diabetes Care 1990; 13 (suppl 3): 2–8.
- 24 Aguilar-Bryan L, Nichols CG, Wechsler SW, Clement IV JP, Boyd AE III, Gonzalez G, Herrera-Sosa H, Nguy K, Bryan J, Nelson DA. Cloning of the B-cell high affinity sulfonylurea receptor: a regulator of insulin secretion. Science 1995; 268: 423–6.
- 25 Inagaki N, Gonoi T, Clement IV JP, Namba N, Inazawa J, Gonzalez G, Aguilar-Bryan L, Seino S, Bryan J. Reconstition of IKATP an inward rectifier subunit plus the sulfonylurea receptor. Science 1995; 270: 1166–70.
- 26 Ashcroft FM, Gribble FM. ATP-sensitive K+ channels and insulin secretion: their role in health and disease. Diabetologia 1999; 42: 903–19.
- 27 Inagaki N, Gonoi T, Clement JP, Wang CZ, Aguilar-Bryan L, Bryan J, Seino S. A family of sulfonylurea receptors determines the properties of ATP-sensitive channel K+ channels. Neuron 1996; 16: 1011–7.
- 28 Gylfe E, Hellman B, Sehlin J, Täljedal I-B. Interaction of sulphonylurea with the pancreatic B-cell. Experientia 1984; 40: 1126–34.
- 29 Boyd AE III, Hill RS, Oberwetter JM, Berg M. Calcium dependency and free calcium concentrations during insulin secretion in a hamster beta cell line. J Clin Invest 1986; 77: 774–81.
- 30 Hellman B, Sehlin J, Täljedal I-B. Glibenclamide is exceptional among hypoglycaemic sulphonylureas in accumulating progressively in B-cell rich pancreatic islets. Acta Endocrinol 1984; 105: 385–90.
- 31 Carpentier J-L, Sawano F, Ravazzola M, Malaisse WJ. Internalization of [3H] glibenclamide in pancreatic islet cells. Diabetologia 1986; 29: 259–61.
- 32 Renstrom E, Barg S, Thevenod F, Rorsman P. Sulfonylurea-mediated stimulation of insulin exocytosis via an ATP-sensitive K+ channel-independent action. Diabetes 2002; 51 (suppl 1): S 33–6.
- 33 Reaven G, Dray J. Effect of chlorpropamide on serum glucose and immunoreactive insulin concentrations in patients with maturity-onset diabetes mellitus. Diabetes 1967; 16: 487–92.
- 34 Feldman JM, Lebovitz HE. Endocrine and metabolic effects of glibenclamide: evidence for an extra-pancreatic mechanism of action. Diabetes 1971; 20: 745–51.
- 35 Pfeifer MA, Halter JB, Graf R, Porte D Jr. Potentiation of insulin secretion to non-glucose stimuli in normal man by tolbutamide. Diabetes 1980; 29: 335–40.
- 36 Judzewitsch RG, Pfeifer MA, Best JD, Beard JC, Halter JB, Porte D Jr. Chronic chlorpropamide therapy of non-insulin-dependent diabetes augments basal and stimulated insulin secretion by increasing islet sensitivity to glucose. J Clin Endocrinol Metab 1982; 55: 321–7.
- 37 Sumi S, Ichihara K, Nonaka K, Tauri S. Effect of the discontinuation of long-term sulfonylurea treatment on blood glucose and insulin secretion in non-insulin-dependent diabetes mellitus. Endocrinol Jpn 1982; 29: 41–7.
- 38 DeFronzo RA. The triumvirate: B-cell, muscle, liver. A collusion responsible for NIDDM. Diabetes 1988; 37: 667–87.
- 39 Kosaka K, Kuzuya T, Akanuma Y, Hagura R. Increase in insulin response after treatment of overt maturity onset diabetes mellitus is independent of the mode of treatment. Diabetologia 1980; 18: 23–8.
- 40 Unger RH, Grundy S. Hyperglycaemia as an inducer as well as a consequence of impaired islet cell function and insulin resistance: implication for the management of diabetes. Diabetologia 1985; 28: 119–21.
- 41 Karam JH, Sanz N, Salamon E, Nolte MS. Selective unresponsiveness of pancreatic B-cells to acute sulfonylurea stimulation during sulfonylurea therapy in NIDDM. Diabetes 1986; 35: 1314–20.
- 42 Kawaki J, Nagashima K, Tanaka J, Miki T, Miyazaki M, Gonio T, Mitsuhashi N, Nakajima N, Iwanaga T, Yano H, Seino S. Unresponsiveness to glibenclamide during chronic treatment induced by reduction of ATP-sensitive K+ channel activity. Diabetes 1999; 48: 2001–6.
- 43 Davies MJ, Metcalf J, Day JL, Greenfell A, Hales CN, Gray IP. Effect of sulphonylurea therapy on plasma insulin, intact and 32/33 split proinsulin in subjects with type 2 diabetes mellitus. Diabet Med 1994; 11: 293–8.
- 44 Prigeon RL, Jacobson RK, Porte D Jr, Kahn SE. Effect of sulfonylurea withdrawal on proinsulin levels, B cell function, and glucose disposal in subjects with noninsulin-dependent diabetes mellitus. J Clin Endocrinol Metab 1996; 81: 329 5–8.
- 45 Levy J, Malaisse WJ. The stimulus–secretion coupling of glucose-induced insulin release, XVII: effects of sulfonylureas and diazoxide on insular biosynthetic activity. Biochem Pharmacol 1975; 24: 235–9.
- 46 Duckworth WC, Solomon SS, Kitabchi AE. Effect of chronic sulfonylurea therapy on plasma insulin and proinsulin levels. J Clin Endocrinol Metab 1972; 35: 585–91.
- 47 Quesada I, Nadal A, Soria B. Different effects of tolbutamide and diazoxide in (α-, (β-, (δ-cells within intact islets of Langerhans induces impairment of glucagon and growth hormone responses during mild insulin-induced hypoglycemia. Diabetes 1999; 48: 2390–7.
- 48 Landstedt-Hallin L, Adamson U, Lins P-E. Oral glibenclamide suppresses glucagon secretion during insulin-induced hypoglycemia in patients with type 2 diabetes. J Clin Endocrinol Metab 1999; 84: 3140–5.
- 49 Ter Braak EW, Appelman, van der Tweel I, Erkelens DW, van Haeften TW. The sulfonylurea glyburide induces impairment of glucagon and growth hormone responses during mild insulin-induced hypoglycemia. Diabetes Care 2002; 25: 107–12.
- 50 Lebovitz HE. Oral hypoglycemic agents. In H Rifkin, D Porte (eds), Diabetes Mellitus: Theory and Practice, 4th edn. New York: Excerpta Medica, 1990; pp 554–75.
- 51 Lebovitz HE, Feinglos MN. Sulfonylurea drugs: mechanism of antidiabetic action and therapeutic usefulness. Diabetes Care 1978; 1: 189–97.
- 52 Lebovitz HE. Oral hypoglycemic agents. In KGMM Alberti, Krall LP (eds), Diabetes Annual 3. Amsterdam: Elsevier, 1987; pp 72–93.
- 53 Haupt A, Kausch C, Dahl D, Bachmann O. Stumvoll M, Haring H-U, Matthaei S. Effect of glimepiride on insulin-stimulated glycogen synthesis in cultured human skeletal muscle cells. Diabetes Care 2002; 25: 2129–32.
- 54 Overkamp D, Volk A, Maerker E, Heide PE, Wahl HG, Rett K, Haring H-U. Acute effect of glimepiride on insulin-stimulated glucose metabolism in glucose-intolerant insulin-resistant offspring of patients with type 2 diabetes. Diabetes Care 2002; 25: 2065–73.
- 55 Hribal ML, D'Alfonso R, Giovannone B, Lauro D, Liu YY, Borboni P, Federici M, Lauro R, Sesti G. The sulfonylurea glimepiride regulates intracellular routing of the insulin-receptor complexes through their interaction with specific protein kinase C isoforms. Mol Pharmacol 2001; 59: 322–30.
- 56 Lebovitz HE. Cellular loci of sulfonylurea actions. Diabetes Care 1984; 7 (suppl 1): 67–71.
- 57 Jacobs DB, Hayes GR, Lockwood DH. In vitro effects of sulfonylurea on glucose transport and translocation of glucose transporters in adipocytes from streptozotocin-induced diabetic rats. Diabetes 1989; 38: 205–10.
- 58 Putnam WS, Andersen DK, Jones RS, Lebovitz HE. Selective potentiation of insulin-mediated glucose disposal in normal dogs by the sulfonylurea, glipizide. J Clin Invest 1981; 67: 1016–23.
- 59 Firth RG, Bell PM, Rizza RA. Effects of tolazamide and exogenous insulin on insulin action in patients with non-insulin-dependent diabetes mellitus. N Engl J Med 1986; 314: 1280–6.
- 60 Simonson DC, Delprato S, Castellino P, Groop L, DeFronzo RA. Effect of glyburide on glycemic control, insulin requirement, and glucose metabolism in insulin-treated diabetic patients. Diabetes 1987; 36: 136–46.
- 61 Sartor G, Ursing D, Nilsson-Ehle P, Wåhlin-Boll E, Melander A. Lack of primary effect of sulphonylurea (glipizide) on plasma lipoproteins and insulin action in former type 2 diabetics with attenuated insulin secretion. Eur J Clin Pharmacol 1987; 33: 279–82.
- 62 Lebovitz HL, Feinglos MN, Bucholtz HK, Lebovitz FL. Potentiation of insulin action: a probable mechanism for the antidiabetic action of sulfonylurea drugs. J Clin Endocrinol Metab 1977; 45: 601–4.
- 63 Kolterman OG, Gray RS, Shapiro G, Scarlett JA, Griffin J, Olefsky JM. The acute and chronic effects of sulfonylurea therapy in type II diabetic subjects. Diabetes 1984; 33: 346–54.
- 64 Ward G, Harrison LC, Proietto J, Aitken P, Nankervis A. Gliclazide therapy is associated with potentiation of postbinding insulin action in obese, non-insulin-dependent diabetic subjects. Diabetes 1985; 34: 241–5.
- 65 Faber OK, Beck-Nielsen H, Binder C, Butzer P, Damsgaard EM, Froland F, Hjollund E, Lindskov HO, Melander A, Pedersen O, Petersen P, Schwarts Sorensen N, Wâhlin-Boll E. Acute actions of sulfonylurea drugs during long-term treatment of NIDDM. Diabetes Care 1990; 13 (suppl 3): 26–31.
- 66 Lebovitz HE. Oral hypoglycemic sulfonylureas: pancreatic vs extrapancreatic actions. In Y Shigeta, HE Lebovitz, JE Gerich, WJ Malaisse (eds), Best Approach to Ideal Therapy of Diabetes Mellitus. Amsterdam: Excerpta Medica, 1987; pp 21–6.
- 67 Beck-Nielsen H, Hother-Hielsen O, Pedersen O. Mechanism of action of sulphonylureas with special reference to the extrapancreatic effect: an overview. Diabet Med 1988; 5: 613–20.
- 68 Wang PH, Beguinot F, Smith RJ. Augmentation of the effects of insulin and insulin-like growth factors I and II on glucose uptake in cultured rat skeletal muscle cells by sulfonylureas. Diabetologia 1987; 30: 797–803.
- 69 Mirsky IA, Perisutti G, Diengatt D. The inhibition of insulinase by hypoglycemic sulfonamides. Metabolism 1956; 5: 138–43.
- 70 Almér L-O, Johansson E, Melander A, Wåhlin-Boll E. Influence of sulphonylureas on the secretion, disposal and effect of insulin. Eur J Clin Pharmacol 1982; 22: 27–32.
- 71 Scheen AJ, Lefebvre PJ, Luyckx AS. Glipizide increases plasma insulin but not C-peptide level after a standardized breakfast in type 2 diabetic patients. Eur J Clin Pharmacol 1984; 26: 471–4.
- 72 Groop L, Groop P-H, Stenman S, Saloranta C, Tötterman K-J, Fyhrquist F, Melander A. Comparison of pharmacokinetics, metabolic effects and mechanisms of action of glyburide and glipizide during long-term treatment. Diabetes Care 1987; 10: 671–8.
- 73 Groop L, Groop P-H, Stenman S, Saloranta C, Tötterman K-J, Fyhrquist F, Melander A. Do sulfonylureas influence hepatic insulin clearance? Diabetes Care 1988; 11: 689–90.
- 74 Beck-Nielsen H, Hother Nielsen O, Andersen PH, Pedersen O, Schmitz O. In vivo action of glibenclamide. Diabetologia 1986; 29: 515A (abstract 26).
- 75 Wåhlin-Boll E, Sartor G, Melander A, Scherstén B. Impaired effect of sulphonylurea following increased dosage. Eur J Clin Pharmacol 1982; 22: 21–5.
- 76 Stenman S, Melander A, Groop P-H, Groop L. What is the benefit of increasing the sulphonylurea dose? Ann Int Med 1993; 118: 169–72.
- 77 Kuo BS, Korner G, Bjornsson TD. Effects of sulfonylureas on the synthesis and secretion of plasminogen activator from bovine aortic endothelial cells. J Clin Invest 1988; 81: 730–7.
- 78 Moses AM, Numann P, Miller M. Mechanism of chlorpropamide-induced antidiuretics in man. Evidence for release of ADH and enhancement of peripheral action. Metabolism 1973; 22: 59–66.
- 79 Lebovitz HE. Oral therapies for diabetic hyperglycemia. Endocrinol Metab Clin North Am 2001; 30: 909–33.
- 80 Lebovitz HE. Insulin secretogogues: old and new. Diabetes Rev 1999; 7: 139–53.
- 81 Lindblad U, Melander A. Sulphonylurea dose–response relationships: relation to clinical practice. Diabetes Obes Metab 2000; 2: 25–31.
- 82 Greenfield MS, Doberne L, Rosenthal M, Schulz B, Widström A, Reaven GM. Effect of sulfonylurea treatment on in vivo insulin secretion and action in patients with non-insulin-dependent diabetes mellitus. Diabetes 1982; 31: 307–12.
- 83 Best JD, Judzewitsch RG, Pfeifer MA, Beard JC, Halter JB, Porte D Jr. The effect of chronic sulfonylurea therapy on hepatic glucose production in non-insulin-dependent diabetes mellitus. Diabetes 1982; 31: 333–8.
- 84 Lebovitz HE, Feinglos MN. Mechanism of action of the second generation sulfonylurea glipizide. Am J Med 1983; 75 (suppl 5B): 46–54.
- 85 Camerini-Davalos R, Lozano-Castaneda O, Marble A. Five years experience with tolbutamide. Diabetes 1962; 11 (suppl): 74–80.
- 86 Cervantes-Amezeua A, Naldjian S, Camerini-Davalos R, Marble A. Long-term use of chlorpropamide in diabetes. JAMA 1965; 193: 759–62.
- 87 Muller R, Bauer G, Schroder R, Saito S. Summary report of clinical investigation of the oral antidiabetic drug HB 419 (glibenclamide). Horm Metab Res 1969; 1 (suppl): 88–92.
- 88 Emanueli A, Molari E, Colombo A, Pirola L, Caputo G. Glipizide, a new sulfonylurea in the treatment of diabetes mellitus. Arzneim Forsch (Drug Res) 1972; 22: 1881–5.
- 89 Rizza RA. Is secondary failure inevitable? In D Cameron, S Colagiuri, L Heding, C Kuhl, A Ma, Mortimer R (eds), Non-insulin-dependent Diabetes Mellitus. Hong Kong: Excerpta Medica, 1989; pp 57–61.
- 90 Balodimos MC, Camerini-Davalos R, Marble A. Nine years experience with tolbutamide in the treatment of diabetes. Metabolism 1966; 11: 957–70.
- 91 Turner RC, Holman RR, Matthews DR. Sulfonylurea failure and inadequacy. In D Cameron, S Colagiuri, L Heding, C Kuhl, A Ma, R Mortimer (eds), Non-insulin-dependent Diabetes Mellitus. Hong Kong: Excerpta Medica, 1989; pp 52–6.
- 92 Simonson DC, Kourides IA, Feinglos M, Shamoon, Fishette CT. Efficacy, safety, and dose–response characteristics of glipizide gastrointestinal therapeutic system on glycemic control and insulin secretion in NIDDM. Diabetes Care 1997; 20: 597–606.
- 93 Rosenstock J, Samols E, Muchmore DB, Schneider J. Glimepiride, a new once-daily sulfonylurea. Diabetes Care 1996; 19: 1194–9.
- 94 Garber AJ, Larsen J, Schneider SH, Piper BA, Henry D. Simultaneous glyburide/metformin therapy is superior to component monotherapy as an initial pharmacological treatment for type 2 diabetes. Diabetes Obes Metab 2002; 4: 201–8.
- 95 Singer DL, Hurwitz D. Long-term experience with sulfonylureas and placebo. N Engl J Med 1967; 277: 450–6.
- 96 Lev-Ran A. Trial of placebo in long-term chlorpropamide-treated diabetics. Diabetologia 1974; 10: 197–200.
- 97 University Group Diabetes Program. Effects of hypoglycemic agents on vascular complication in patients with adult-onset diabetes, III: clinical implications of UGDP results. JAMA 1971; 218: 1400–10.
- 98 The United Kingdom Prospective Diabetes Study (UKPDS) Group. UK Prospective Study of Therapies of Maturity-onset Diabetes, I: effect of diet, sulphonylurea, insulin or biguanide therapy on fasting plasma glucose and body weight over one year. Diabetologia 1983; 24: 404–11.
- 99 The United Kingdom Prospective Diabetes Study (UKPDS) Group. UK Prospective Diabetes Study, II: reduction in HbA1c with basal insulin supplement, sulfonylurea or biguanide therapy in maturity-onset diabetes. Diabetes 1985; 34: 793–8.
- 100 The United Kingdom Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998; 352: 837–53.
- 101 Turner RC, Cull CA, Frighi V, Holman RR. Glycemic control with diet, sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus. Progressive requirement for multiple therapies (UKPDS 49). JAMA 1999; 281: 2005–12.
- 102
Matthews DR,
Cull CA,
Stratton IM,
Holman RR,
Turner RC.
UKPDS 26: Sulphonylurea failure in non-insulin dependent diabetic patients over six years.
Diabet Med
1998;
15:
297–303.
10.1002/(SICI)1096-9136(199804)15:4<297::AID-DIA572>3.0.CO;2-W CAS PubMed Web of Science® Google Scholar
- 103 The UKPDS Group. UKPDS, 16: Overview of 6 years' therapy of type 2 diabetes: a progressive disease. Diabetes 1995; 44: 1249–58.
- 104 Ferner RE, Chaplin S. The relationship between the pharmacokinetics and pharmacodynamic effects of oral hypoglycaemic drugs. Clin Pharmacokin 1987; 12: 379–401.
- 105 Melander A, Sartor G, Wåhlin E, Scherstén B, Bitzén P-O. Serum tolbutamide and chlorpropamide concentrations in patients with diabetes mellitus. Br Med J 1978; 1: 142–4.
- 106
Cerasi E,
Efendic S,
Luft R.
Dose response relation between insulin and blood glucose levels during oral glucose loads in prediabetic and diabetic subjects.
Lancet
1973; i:
794–7.
10.1016/S0140-6736(73)90599-0 Google Scholar
- 107 Luft R, Wajngot A, Efendic S. On the pathogenesis of maturity-onset diabetes. Diabetes Care 1981; 4: 58–63.
- 108 DeFronzo RA, Ferrannini E, Koivisto V. New concepts in the pathogenesis and treatment of noninsulin-dependent diabetes mellitus. Am J Med 1983; 74 (suppl 1A): 52–81.
- 109
Temple RC,
Carrington CA,
Luzio SD,
Owens DR,
Schneider AE,
Sobey WJ,
Hales CN.
Insulin deficiency in non-insulin-dependent diabetes.
Lancet
1989; i:
293–5.
10.1016/S0140-6736(89)91306-8 Google Scholar
- 110 Bitzén P-O, Melander A, Scherstén B, Wåhlin-Boll E. The influence of glipizide on early insulin release and glucose disposal before and after diet regulation in diabetic patients with different degrees of hyperglycaemia. Eur J Clin Pharmacol 1988; 35: 31–7.
- 111 Bitzén P-O. On the Early Detection and Treatment of Non-insulin-dependent Diabetes Mellitus in Primary Health Care, PhD Thesis. Sweden: University of Lund, 1988.
- 112 Hartling SG, Faber OK, Wegmann M-L, Wåhlin-Boll E, Melander A. Interaction of ethanol and glipizide in humans. Diabetes Care 1987; 10: 683–6.
- 113 Arnqvist HJ, Karlberg BE, Melander A. Pharmacokinetics and effects of glibenclamide in two formulations, HB419 and HB420, in type 2 diabetics. Ann Clin Res 1983; 15 (suppl 37): 21–5.
- 114 Groop L, Luzi L, Melander A, Groop P-H, Ratheiser K, Simonson DC, DeFronzo RA. Different effects of glyburide and glipizide on insulin secretion and hepatic glucose production in normal and NIDDM subjects. Diabetes 1987; 36: 1320–8.
- 115 Ikegawi H, Shima K, Tanaka A, Tahara Y, Hirota M, Kumahara Y. Interindividual variation in the absorption of glibenclamide in man. Acta Endocrinol 1986; 111: 528–32.
- 116 Campbell DB, Adriaenssens P, Hopkins YW, Gordon B, Williams JRB. Pharmacokinetics and metabolism of gliclazide: a review. In H Keen et al. (eds), Gliclazide and the Treatment of Diabetes. (International Congress and Symposium Series 20). London: Academic Press, 1980; pp 71–82.
- 117 Wåhlin-Boll E, Almér L-O, Melander A. Bioavailability, pharmacokinetics and effects of glipizide in type 2 diabetics. Clin Pharmacokinet 1982; 7: 363–72.
- 118 Eriksson J, Franssila-Kalluni A, Ekstrand A, Saloranta C, Widén E, Schalin C, Groop L. Early metabolic defects in persons at increased risk for non-insulin-dependent diabetes mellitus. N Engl J Med 1989; 321: 337–43.
- 119 Sartor G, Lundquist I, Melander A, Scherstén B, Wåhlin-Boll E. Improved effect of glibenclamide on administration before breakfast. Eur J Clin Pharmacol 1982; 21: 403–8.
- 120 Wåhlin-Boll E, Melander A, Sartor G, Scherstén B. Influence of food intake on the absorption and effect of glipizide in diabetics and in healthy subjects. Eur J Clin Pharmacol 1980; 18: 279–83.
- 121 Silins RA, Butcher MA, Marlin GE. Improved effect of tolbutamide when given before food in patients on long-term therapy [letter]. Br J Clin Pharmacol 1984; 18: 647–8.
- 122 Asplund K, Wiholm B-E, Lithner F. Glibenclamide-associated hypoglycaemia. A report on 57 cases. Diabetologia 1983; 24: 412–7.
- 123 Berger W, Cardiff F, Pasquel M, Rump A. Die relative Häufigkeit der schweren Sulfonylharnstoff-Hypoglykämie in den letzten 25 Jahren in der Schweiz. Schweiz Med Wschr 1986; 116: 145–51.
- 124 Seltzer HS. Severe drug-induced hypoglycemia. A review. Comp Ther 1979; 5: 21–9.
- 125 Jönsson A, Rydberg T, Ekberg G, Hallengren B, Melander A. Slow elimination of glyburide in NIDDM subjects. Diabetes Care 1994; 17: 142–5.
- 126 Statistics from the Department of Drugs. Uppsala, Sweden: Swedish Board of Health and Welfare, 1985.
- 127 Behrle M. Untersuchung zur Pharmakokinetik von Glibenclamid bei nierengesunden und niereninsuffizienten Diabetikern, Thesis. Heidelberg, Germany: Ruprecht-Karl-Universität, 1980.
- 128 Rydberg T, Jönsson A, Röder M, Melander A. Hypoglycemic activity of glyburide (glibenclamide) metabolites in man. Diabetes Care 1994; 17: 1026–30.
- 129 Ferner R, Rawlins MD, Alberti KGMM. Impaired B-cell responses improve when fasting blood glucose concentration is reduced in non-insulin-dependent diabetes. Q J Med 1988; 66: 137–46.
- 130 Olson SC, Ayres JW, Antal EJ, Albert KS. Effect of food and tablet age on relative bioavailability and pharmacodynamics of two tolbutamide products. J Pharm Sci 1985; 74: 735–9.
- 131 Scott J, Poffenbarger PL. Pharmacodynamics of tolbutamide metabolism in humans. Diabetes 1979; 28: 41–51.
- 132 Neuvonen PJ, Kärkkäinen S. Effects of charcoal, sodium bicarbonate and ammonium chloride on chlorpropamide kinetics. Clin Pharmacol Ther 1983; 33: 386–93.
- 133 Groop L, Wåhlin-Boll E, Groop P-H, Tötterman K-J, Melander A, Tolppanen E-M, Fyhrqvist F. Pharmacokinetics and metabolic effects of glibenclamide and glipizide in Type 2 diabetics. Eur J Clin Pharmacol 1985; 28: 697–704.
- 134 Taylor R, Isles TE, MacLaren S, Stevenson IH, Newton RW. Comparison of metabolic profiles in non-obese non-insulin-dependent diabetics receiving glipizide and glibenclamide. Diabetologia Croatica 1983; 12: 279–92.
- 135 Cabrera-Rode E, Perich P, Diaz-Horta O, Tiberti C, Molina G, Arranz C, Martin JM, Licea M, DeLeiva AD, Puig-Domingo M, Dimario U. Slowly progressing type 1 diabetes: persistence of islet cell autoantibodies is related to glibenclamide treatmenr. Autoimmunity 2002; 35: 469–74.
- 136 Blomgren KB, Sundstrom A, Steineck G, Wiholm BE. Obesity and treatment of diabetes with glyburide may both be risk factors for acute pancreatitis. Diabetes Care 2002; 25: 298–302.
- 137 Langer O, Conway DL, Berkus MD, Xenakis EMJ. Gonzales O. A comparison of glyburide and insulin in women with gestational diabetes mellitus. New Engl J Med 2000; 343: 1134–8.
- 138 Forette B, Rolland A, Hopkins Y, Gordon B, Campbell B. Gliclazide kinetics in the elderly. In KGMM Alberti, T Ogada, JA Aluoch, EN Mngola (eds), 11th Congress of the International Diabetes Federation. Amsterdam: Excerpta Medica, 1982; p 9.
- 139 Holmes B, Heel RC, Brogden RN, Speight TM, Avery GS. Gliclazide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy in diabetes mellitus. Drugs 1984; 27: 301–27.
- 140 Kradjian W, Kobayashi KA, Bauer LA, Horn JR, Opheim K, Wood F Jr. Glipizide pharmacokinetics: effects of age, diabetes and multiple dosing (in press).
- 141 Wåhlin-Boll E, Groop L, Karhumaa S, Groop P-H, Tötterman K-J, Melander A. Therapeutic equivalence of once- and thrice-daily glipizide. Eur J Clin Pharmacol 1986; 31: 95–9.
- 142 Berelowitz M, Fischette C, Cefalu W, Shade DS, Sutfin T, Kourides IA. Comparative efficacy of a once daily contolled-release type 2 diabetes. Formulation of glipizide and immediate-release glipizide in patients with NIDDM. Diabetes Care 1994; 17: 1460–4.
- 143 Campbell RK. Glimepiride: role of a new sulfonylurea in the treatment of type 2 diabetes mellitus. Ann Pharmacother 1998; 32: 1044–52.
- 144 Holstein A, Plaschke A, Egberts EH. Lower incidence of severe hypoglycaemia in patients with type 2 diabetes treated with glimepiride versus glibenclamide. Diabetes Metab Res Rev 2001; 17: 467–73.
- 145 Tsunekawa T, Hayashi T, Suzuki Y, Matsui-Hirai H, Kano H, Fukatsu A, Nomura N, Miyazaki A, Iguchi A. Plasma adiponectin plays an important role in improving insulin resistance with glimepiride in elderly type 2 diabetic subjects. Diabetes Care 2003; 26: 285–9.
- 146 Klepzig H, Kober G, Matter C, Luus H, Schneider H, Boedekert KH, Klowski W, Amann FW, Gruber D, Harris S, Burger W. Sulphonylureas and ischemic preconditioning. A double-blind, placebo-controlled evaluation of glimepiride and glibenclamide. Eur Heart J 1999; 20: 439–46.
- 147 Lee T-M, Chou T-F. Impairment of myocardial protection in type 2 diabetic patients. J Clin Endocrinol Metab 2003; 88: 531–7.
- 148 Korytkowski M, Thomas A, Reid L, Tedesco MB, Gooding WE, Gerich J. Glimepiride improves both first and second phases of insulin secretion in type 2 diabetes. Diabetes Care 2002; 25: 1607–11.
- 149 Alberti KGMM. A desktop guide to type 2 diabetes mellitus. European Diabetes Policy Group 1998–1999 International Diabetes Federation European Region. Exp Clin Endocrinol Diabetes 1999; 107: 390–420.
- 150 Lebovitz HE. Treating hyperglycemia in type 2 diabetes: new goals and strategies. Cleve Clin J Med 2002; 69: 809–20.
- 151 Rendell M, Slevin D, Meltz G, Simpson J, Barquet A. A case of maturity-onset diabetes mellitus resistant to insulin but responsive to tolbutamide. Arch Int Med 1979; 90: 195–7.
- 152 Persson G. Cardiovascular complications in diabetics and subjects with reduced glucose tolerance. Acta Med Scand 1977; (suppl 605).
- 153 Donahue RP, Abbott RD, Reed DM, Katsuhiko Y. Postchallenge glucose concentration and coronary heart disease in men of Japanese ancestry. Honolulu Heart Program. Diabetes 1987; 36: 689–92.
- 154
Fuller JH,
Shipley MJ,
Rose G,
Jarrett RJ,
Keen H.
Coronary-heart-disease risk and impaired glucose tolerance.
Lancet
1980; i:
1373–6.
10.1016/S0140-6736(80)92651-3 Google Scholar
- 155 Jarrett RJ, McCartney P, Keen H. The Bedford Survey. Ten year mortality rates in newly diagnosed diabetics, borderline diabetics and normoglycaemic controls and risk indices for coronary heart disease in borderline diabetics. Diabetologia 1982; 22: 79–84.
- 156 Eschwège E, Richard JL, Thibault N, et al. Coronary heart disease mortality in relation with diabetes, blood glucose and plasma insulin levels. The Paris prospective study, ten years later. Horm Metab Res 1985; 15 (suppl): 41–6.
- 157 The UKPDS Group. UKPDS 6: Complications in newly diagnosed type 2 diabetic patients and their association with different clinical and biochemical risk factors. Diabetes Res 1990; 13: 1–11.
- 158 Owens DR, Dolben J, Vora JP, et al. Retinopathy and nephropathy in relation to metabolic status in newly diagnosed NIDDM. In D Cameron, S Colagiuri, L Heding, C Kuhl, A Ma, R Mortimer (eds), Non-insulin-dependent Diabetes Mellitus. Hong Kong: Excerpta Medica, 1989; pp 11–9.
- 159 Bitzén P-O, Scherstén B. Assessment of laboratory methods for detection of unsuspected diabetes in primary health care. Scand J Prim Health Care 1986; 4: 85–95.
- 160 Sartor G, Scherstén B, Carlström S, Melander A, Nordén Å, Persson G. Ten-year follow-up of subjects with impaired glucose tolerance. Prevention of diabetes by tolbutamide and diet regulation. Diabetes 1980; 29: 41–9.
- 161 Knowler WC, Sartor G, Melander A, Scherstén B. Glucose tolerance and mortality, including a substudy of tolbutamide treatment. Diabetologia 1997; 40: 680–6.
- 162 Bailey TS, Lebovitz HE. Continuous sulfonylurea exposure desensitizes beta-cell insulin secretion at a distal site. Diabetes 1990; 39 (suppl 1): 137A (abstract 548).
- 163 Grodsky GM. A new phase of insulin secretion. How will it contribute to our understanding of B-cell function? Diabetes 1989; 38: 673–8.
- 164 Groop LC, Bottazzo GF, Doniach D. Islet cell antibodies identify latent type I diabetes in patients aged 35–75 years at diagnosis. Diabetes 1986; 35: 237–41.
- 165 Groop LC, Eriksson J, Schalin C, Ahola A. Does secondary oral failure represent slowly evolving type I diabetes? In D Cameron, S Colagiuri, L Heding, C Kuhl, A Ma, R Mortimer (eds), Non-insulin-dependent Diabetes Mellitus. Hong Kong: Excerpta Medica, 1989; pp 48–51.
- 166 Groop LC, Pelkonen R, Koskimies S, Bottazzo GF, Doniach D. Secondary failure to treatment with oral antidiabetic agents in non-insulin-dependent diabetes. Diabetes Care 1986; 9: 129–33.
- 167 Wright A, Burden AC, Paisey RB, Cull CA, Holman RR. Sulfonylurea inadequacy: efficacy of addition of insulin over 6 years in patients with type 2 diabetes in the UK Prospective Diabetes Study (UKPDS 57). Diabetes Care 2002; 25: 330–6.
- 168 Sinagra D, Greco D, Amato MC, D'Acquisto G, Galluzzo A. A 12-h intravenous insulin infusion restores the B-cell response torpidity to sulfonylureas in patients affected by type 2 diabetes. Diabetes Care 2000; 23: 1857–8.
- 169 Campbell IW, Howlett HCS. Worldwide experience of metformin as an effective glucose-lowering agent: a meta-analysis. Diabetes Metab Rev 1995; 11: S57.
- 170 The UKPDS Group. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998; 353: 854–65.
- 171 DeFronzo RA, Goodman AM. Efficacy of metformin in patients with non-insulin-dependent diabetes mellitus. New Engl J Med 1995; 333: 541–9.
- 172 Hermann LS, Scherstén B, Bitzén P-O, Kjellström T, Lindgärde F, Melander A. Therapeutic comparison of metformin and sulfonylurea, alone and in various combinations: a double-blind controlled study. Diabetes Care 1994; 17: 1100–9.
- 173 Hermann LS, Scherstén B, Melander A. Antihyperglycaemic efficacy, response prediction and dose–response relations of treatment with metformin and sulphonylurea, alone and in primary combination. Diabet Med 1994; 11: 953–60.
- 174 Yu JG, Kruszynska YT, Mulford MI, Olefsky JM. A comparison of troglitazone and metformin on insulin requirements in euglycemic intensively insulin-treated type 2 diabetic patients. Diabetes 1999; 48: 2414–21.
- 175 Lebovitz HE, Pasmantier RM. Combination insulin–sulfonylurea therapy. Diabetes Care 1990; 13: 667–75.
- 176 Groop LC, Groop P-H, Stenman S. Combined insulin–sulfonylurea therapy in treatment of NIDDM. Diabetes Care 1990; 13 (suppl 3): 47–52.
- 177 Yki-Järvinen H, Kauppila M, Kusansuu E, et al. Comparisons of insulin regimens in patients with non-insulin-dependent diabetes mellitus. N Engl J Med 1992; 327: 1426–33.
- 178 Pugh JA, Wagner ML, Sawyer J, Ramirez G, Tuley M, Friedberg SJ. Is combination sulfonylurea and insulin therapy useful in NIDDM patients? A meta-analysis. Diabetes Care 1992; 15: 953–8.
- 179 Sane T, Helve E, Yki-Järvinen H, Taskinen MR. One year response to evening insulin therapy in non-insulin dependent diabetes. J Int Med 1992; 231: 253–60.
- 180 Yki-Jarvinen H, Dressler A, Zieman M. Study Group HOE 901/3002. Less nocturnal hypoglycemia and better post dinner glucose control with bedtime insulin glargine compared with bedtime NPH insulin during combination therapy in type 2 diabetes. Diabetes Care 2001; 23: 1130–6.
- 181 Yki-Jarvinen H, Ryysy L, Nikkila K, Tulokas T, Vanamo R, Heikkila M. Comparison of bedtime insulin regimens in patients with type 2 diabetes mellitus: a randomized, controlled trial. Ann Intern Med 1999; 130: 389–96.
- 182 Chiasson JL, Josse R, Hunt J, Palmason C, Rodger NW, Ross SA, et al. The efficacy of acarbose in the treatment of patients with non-insulin dependent diabetes mellitus. Ann Intern Med (USA) 1994; 121: 928–35.
- 183 Holman RR, Cull CA, Turner RC. A randomized double-blind trial of acarbose in type 2 diabetes shows improved glycemic control over 3 years. Diabetes Care 1999; 22: 960–4.
- 184 Raskin P, Rendell M, Riddle MC, Dole JF, Freed MI, Rosenstock J, for the Rosiglitazone Clinical Trials Study Group. A randomized trial of rosiglitazone therapy in patients with inadequately controlled insulin-treated type 2 diabetes. Diabetes Care 2001; 24: 1226–32.
- 185 Burge MR, Sood V, Sobhy TA, Rassam AG, Schade DS. Sulphonylurea-induced hypoglycaemia in type 2 diabetes melltus: a review. Diabetes Obes Metab 1999; 1: 199–206.
- 186 Shorr RI, Daugherty WA, Griffin MR. Incidence and risk factors for serious hypoglycemia in older persons using insulin or sulfonylureas. Arch Int Med 1997; 157: 1681–7.
- 187 van Staa T, Abenhaim L, Monette J. Rates of hypoglycemia in users of sulfonylureas. J Clin Epidemiol 1997; 50: 735–41.
- 188 Seltzer HS. Drug-induced hypoglycemia. Endocrinol Metab Clin North Am 1989; 18: 163–83.
- 189 Stahl M, Berger M. Higher incidence of severe hypoglycaemia leading to hospital admission in type 2 diabetic patients treated with long-acting versus short-acting sulphonylureas. Diabet Med 1999; 16: 586–90.
- 190 Shorr RI, Ray WA, Daugherty WA, Griffin MR. Individual sulfonylureas and serious hypoglycemia in older people. J Am Geriatr Soc 1996; 44: 751–5.
- 191 Krepinsky J, Ingram AJ, Clase CM. Prolonged sulfonylurea-induced hypoglycemia in diabetic patients with end stage renal disease. Am J Kidney Dis 2000; 35: 500–5.
- 192 Pearson ER, Liddle WG, Shepherd M, Corrall RJ, Hattersley AT. Sensitivity to sulphonylureas in patients with hepatic nuclear factor (HNF)-1 alpha gene mutations: evidence for pharmacogenetics in diabetes. Diabet Med 2000; 17: 543–5.
- 193 McLaughlin SA, Crandall CS, McKinney PE. Octreotide: an antidote for sulfonylurea-induced hypoglycemia. Ann Emerg Med 2001; 37: 417–8.
- 194 Nzerue CM, Thomas J, Volcy J, Edeki T. Use of octreotide to treat prolonged sulfonylurea-induced hypoglycemia in a patient with chronic renal failure. Int J Artif Organs 2003; 26: 86–9.
- 195 Boyle PJ, Justice K, Krentz AJ, Nagy RJ, Schade DS. Octreotide reverses hyperinsulinemia and prevents hypoglycemia induced by sulfonylurea overdoses. J Clin Endocrinol Metab 1993; 76: 752–6.
- 196 University Group Diabetes Program. A study of the effects of hypoglycemic agents on vascular complications in patients with adult-onset diabetes. Diabetes 1970; 19 (suppl 2).
- 197 Williamson JR, Kilo C. Effect of tolbutamide (TOLB) treatment on cardiovascular (CV) mortality in the University Group Diabetes Program (UGDP). In Abstracts of 10th Congress of the International Diabetes Federation No. 663F. Amsterdam: Exerpta Medica, 1979; p 255.
- 198 Hu S, Wang S, Dunning BE: Tissue selectivity of antidiabetic agent nateglinide: study on cardiovascular and beta-cell KATP channels. J Pharmacol Exp Ther 1999; 291: 1372–9.
- 199 Garratt KN, Brady PA, Hassinger NL, Grill DE, Terzic A, Holmes DR Jr. Sulfonylurea drugs increase early mortality in patients with diabetes mellitus after direct angioplasty for acute myocardial infarction. J Am Coll Cardiol 1999; 33: 119–24.
- 200 Scognamiglio R, Avogaro A, Vigili De Kreutzenberg S, Negut C, Palisi M, Bagolin E, Tiengo A. Effects of treatment with sulfonylurea drugs or insulin on ischemia-induced myocardial dysfunction in type 2 diabetes. Diabetes 2002; 51: 808–12.
- 201 Jollis JG, Simpson RJ, Cascio WE, Chowdhury MK, Crouse JR, Smith SC Jr. Relation between sulfonylurea therapy, complications and outcome for elderly patients with acute myocardial infarction. Am Heart J 1999; 138: S376–80.
- 202 Klamann A, Sarfert P, Launhardt V, Schulte G, Schmiegel WH, Nauck MA. Myocardial infarction in diabetic vs non-diabetic subjects. Survival and infarct size following therapy with sulfonylureas (glibenclamide). Eur Heart J 2000; 21: 220.
- 203 Riddle MC, Schneider J. Beginning insulin treatment of obese patients with evening 70/30 insulin plus glimepiride versus insulin alone. Diabetes Care 1998; 21: 1052–7.
- 204 Ashcroft FM, Gribble FM, J Diabetes Complications 2000; 14 (4): 192–6.
