The role of nateglinide and repaglinide, derivatives of meglitinide, in the treatment of type 2 diabetes mellitus

Archives of Medical Science

Volumn 9, Issue 5, 2013, Pages 936-943

  Guardado Mendoza, Rodolfo ^a   Prioletta, Annamaria ^b   Jiménez Ceja, Lilia M ^a   Sosale, Aravind ^c   Folli, Franco ^d  

^a UNIVERSITY OF GUANAJUATO   (Mexico)

^b Diabetes Center   (Italy)

^c Diacon Hospital   (India)

^d Mays Cancer Center at UT Health San Antonio   (United States)

Author keywords

Glycemic control; Hypoglycemia; Meglitinide; Nateglinide; Post prandial glucose excursion; Repaglinide

Indexed keywords

ADENOSINE TRIPHOSPHATE SENSITIVE POTASSIUM CHANNEL; BARBITURIC ACID DERIVATIVE; CARBAMAZEPINE; CYCLOSPORIN; CYTOCHROME P450; GLIBENCLAMIDE; GLIBENCLAMIDE PLUS METFORMIN; GLICLAZIDE; GLUCOSE; HEMOGLOBIN A1C; INCRETIN; INSULIN; INSULIN ASPART; ISOPHANE INSULIN; KETOCONAZOLE; MEGLITINIDE; METFORMIN; METFORMIN PLUS REPAGLINIDE; NATEGLINIDE; REPAGLINIDE; RIFAMPICIN; SHORT ACTING INSULIN; STEROID; SULFONYLUREA; SULFONYLUREA RECEPTOR; TRIACYLGLYCEROL; VOLTAGE GATED CALCIUM CHANNEL;

APOPTOSIS; ARTICLE; CALORIC INTAKE; CARDIOVASCULAR RISK; DIET RESTRICTION; DIETARY COMPLIANCE; DRUG ABSORPTION; DRUG ACCUMULATION; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; EXOCYTOSIS; GLUCAGON RELEASE; GLUCOSE BLOOD LEVEL; GLUCOSE METABOLISM; GLYCEMIC CONTROL; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; IMPAIRED GLUCOSE TOLERANCE; IN VITRO STUDY; INSULIN RELEASE; INSULIN RESISTANCE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; MORBIDITY; MORTALITY; MULTICENTER STUDY (TOPIC); NON INSULIN DEPENDENT DIABETES MELLITUS; OXIDATIVE STRESS; PATIENT COMPLIANCE; POSTPRANDIAL STATE; RANDOMIZED CONTROLLED TRIAL (TOPIC); WEIGHT CHANGE;

EID: 84888091849     PISSN: 17341922     EISSN: None     Source Type: Journal    
DOI: 10.5114/aoms.2013.34991     Document Type: Article

References (82)

1. Dornhorst A. Insulinotropic meglitinide analogues. Lancet 2001; 358: 1709-16. (Pubitemid 33124335)
2. Landgraf R. Meglitinide analogues in the treatment of type 2 diabetes mellitus. Drugs Aging 2000; 17: 411-25.
3. Culy CR, Jarvis B. Repaglinide: a review of its therapeutic use in type 2 diabetes mellitus. Drugs 2001; 61: 1625-60. (Pubitemid 32905281)
4. Aguilar-Bryan L, Bryan J. Molecular biology of adenosine triphosphate-sensitive potassium channels. Endocr Rev 1999; 20: 101-35. (Pubitemid 29339588)
5. Fuhlendorff J, Rorsman P, Kofod H, et al. Stimulation of insulin release by repaglinide and glibenclamide involves both common and distinct processes. Diabetes 1998; 47: 345-51. (Pubitemid 28104194)
6. Gromada J, Dissing S, Kofod H, Frokjaer-Jensen J. Effects of the hypoglycaemic drugs repaglinide and glibenclamide on ATP-sensitive potassium-channels and cytosolic calcium levels in beta TC3 cells and rat pancreatic beta cells. Diabetologia 1995; 38: 1025-32.
7. Hu S. Interaction of nateglinide with K(ATP) channel in beta-cells underlies its unique insulinotropic action. Eur J Pharmacol 2002; 442: 163-71. (Pubitemid 34521859)
8. Hu S, Wang S, Fanelli B, et al. Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: a comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther 2000; 293: 444-52. (Pubitemid 30244093)
9. Keilson L, Mather S, Walter YH, et al. Synergistic effects of nateglinide and meal administration on insulin secretion in patients with type 2 diabetes mellitus. J Clin Endocrinol Metab 2000; 85: 1081-6. (Pubitemid 32269353)
10. Hatorp V, Huang WC, Strange P. Repaglinide pharmacokinetics in healthy young adult and elderly subjects. Clin Ther 1999; 21: 702-10. (Pubitemid 29252092)
11. Hatorp V. Clinical pharmacokinetics and pharmacodynamics of repaglinide. Clin Pharmacokinet 2002; 41: 471-83. (Pubitemid 34804160)
12. Weaver ML, Orwig BA, Rodriguez LC, et al. Pharmacokinetics and metabolism of nateglinide in humans. Drug Metab Dispos 2001; 29: 415-21. (Pubitemid 32275555)
13. Luzio SD, Anderson DM, Owens DR. Effects of timing of administration and meal composition on the pharmacokinetic and pharmacodynamic characteristics of the short-acting oral hypoglycemic agent nateglinide in healthy subjects. J Clin Endocrinol Metab 2001; 86: 4874-80. (Pubitemid 33020535)
14. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). UK Prospective Diabetes Study (UKPDS) Group. Lancet 1998; 352: 837-53.
15. Standards of medical care in diabetes 2013. Diabetes Care 2013; 36: S1-99.
16. Cicero AF, 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.
17. Derosa G, Maffioli P. Alpha-Glucosidase inhibitors and their use in clinical practice. Arch Med Sci 2012; 8: 899-906.
18. Bastyr EJ 3rd, Stuart CA, Brodows RG, et al. Therapy focused on lowering postprandial glucose, not fasting glucose, may be superior for lowering HbA1c. IOEZ Study Group. Diabetes Care 2000; 23: 1236-41.
19. Cavalot F, Petrelli A, Traversa M, et al. Postprandial blood glucose is a stronger predictor of cardiovascular events than fasting blood glucose in type 2 diabetes mellitus, particularly in women: lessons from the San Luigi Gonzaga Diabetes Study. J Clin Endocrinol Metab 2006; 91: 813-9. (Pubitemid 43357744)
20. Folli F, Corradi D, Fanti P, et al. The role of oxidative stress in the pathogenesis of type 2 diabetes mellitus micro-and macrovascular complications: avenues for a mechanistic-based therapeutic approach. Curr Diabetes Rev 2011; 7: 313-24.
21. Folli F, Guzzi V, Perego L, et al. Proteomics reveals novel oxidative and glycolytic mechanisms in type 1 diabetic patients' skin which are normalized by kidney-pancreas transplantation. PLoS One 2010; 5: e9923.
22. Ihnat MA, Thorpe JE, Ceriello A. Hypothesis: the 'metabolic memory', the new challenge of diabetes. Diabet Med 2007; 24: 582-6. (Pubitemid 46808866)
23. Ihnat MA, Thorpe JE, Kamat CD, et al. Reactive oxygen species mediate a cellular 'memory' of high glucose stress signalling. Diabetologia 2007; 50: 1523-31. (Pubitemid 46879013)
24. Mannucci E, Monami M, Lamanna C, Adalsteinsson JE. Post-prandial glucose and diabetic complications: systematic review of observational studies. Acta Diabetol 2012; 49: 307-14.
25. Shiraiwa T, Kaneto H, Miyatsuka T, et al. Post-prandial hyperglycemia is an important predictor of the incidence of diabetic microangiopathy in Japanese type 2 diabetic patients. Biochem Biophys Res Commun 2005; 336: 339-45. (Pubitemid 41253439)
26. Bech P, Moses R, Gomis R. The effect of prandial glucose regulation with repaglinide on treatment satisfaction, wellbeing and health status in patients with pharmacotherapy naive type 2 diabetes: a placebo-controlled, multicentre study. Qual Life Res 2003; 12: 413-25. (Pubitemid 36609886)
27. Inzucchi SE. Oral antihyperglycemic therapy for type 2 diabetes: scientific review. JAMA 2002; 287: 360-72. (Pubitemid 34256388)
28. Inzucchi SE, McGuire DK. New drugs for the treatment of diabetes: part II: Incretin-based therapy and beyond. Circulation 2008; 117: 574-84.
29. McGuire DK, Inzucchi SE. New drugs for the treatment of diabetes mellitus. Part I: thiazolidinediones and their evolving cardiovascular implications. Circulation 2008; 117: 440-9.
30. Marbury TC, Ruckle JL, Hatorp V, et al. Pharmacokinetics of repaglinide in subjects with renal impairment. Clin Pharmacol Ther 2000; 67: 7-15. (Pubitemid 30078382)
31. Goldberg RB, Einhorn D, Lucas CP, et al. A randomized placebo-controlled trial of repaglinide in the treatment of type 2 diabetes. Diabetes Care 1998; 21: 1897-903. (Pubitemid 28478290)
32. Hasslacher C. Safety and efficacy of repaglinide in type 2 diabetic patients with and without impaired renal function. Diabetes Care 2003; 26: 886-91. (Pubitemid 36929360)
33. Hollander PA, Schwartz SL, Gatlin MR, et al. Importance of early insulin secretion: comparison of nateglinide and glyburide in previously diet-treated patients with type 2 diabetes. Diabetes Care 2001; 24: 983-8. (Pubitemid 33716363)
34. Horton ES, Clinkingbeard C, Gatlin M, et al. Nateglinide alone and in combination with metformin improves glycemic control by reducing mealtime glucose levels in type 2 diabetes. Diabetes Care 2000; 23: 1660-5.
35. Rosenstock J, Shen SG, Gatlin MR, Foley JE. Combination therapy with nateglinide and a thiazolidinedione improves glycemic control in type 2 diabetes. Diabetes Care 2002; 25: 1529-33. (Pubitemid 41071106)
36. Horton ES, Foley JE, Shen SG, Baron MA. Efficacy and tolerability of initial combination therapy with nateglinide and metformin in treatment-naive patients with type 2 diabetes. Curr Med Res Opin 2004; 20: 883-9. (Pubitemid 38821527)
37. Rosenstock J, Hassman DR, Madder RD, et al. Repaglinide versus nateglinide monotherapy: a randomized, multi-center study. Diabetes Care 2004; 27: 1265-70. (Pubitemid 38679968)
38. Miwa S, Watada H, Ohmura C, et al. Efficacy and safety of once daily gliclazide (20 mg/day) compared with nateglinide. Endocr J 2004; 51: 393-8. (Pubitemid 39273449)
39. Zhang H, Bu P, Xie YH, et al. Effect of repaglinide and gliclazide on glycaemic control, early-phase insulin se cretion and lipid profiles in. Chin Med J (Engl) 2011; 124: 172-6.
40. Derosa G, Mugellini A, Ciccarelli L, et al. Comparison between repaglinide and glimepiride in patients with type 2 diabetes mellitus: a one-year, randomized, double-blind assessment of metabolic parameters and cardiovascular risk factors. Clin Ther 2003; 25: 472-84. (Pubitemid 36286914)
41. Lund SS, Tarnow L, Frandsen M, et al. Impact of metformin versus the prandial insulin secretagogue, repaglinide, on fasting and postprandial glucose and lipid responses in non-obese patients with type 2 diabetes. Eur J Endocrinol 2008; 158: 35-46. (Pubitemid 351211038)
42. Marre M, Van Gaal L, Usadel KH, et al. Nateglinide improves glycaemic control when added to metformin monotherapy: results of a randomized trial with type 2 diabetes patients. Diabetes Obes Metab 2002; 4: 177-86. (Pubitemid 34567674)
43. Weaver JU, Robertson D, Atkin SL. Nateglinide alone or with metformin safely improves glycaemia to target in patients up to an age of 84. Diabetes Obes Metab 2004; 6: 344-52. (Pubitemid 39172856)
44. Ristic S, Collober-Maugeais C, Cressier F, et al. Nateglinide or gliclazide in combination with metformin for treatment of patients with type 2 diabetes mellitus inadequately controlled on maximum doses of metformin alone: 1-year trial results. Diabetes Obes Metab 2007; 9: 506-11. (Pubitemid 47018514)
45. Ristic S, Collober-Maugeais C, Pecher E, Cressier F. Comparison of nateglinide and gliclazide in combination with metformin, for treatment of patients with type 2 diabetes mellitus inadequately controlled on maximum doses of metformin alone. Diabet Med 2006; 23: 757-62. (Pubitemid 44366074)
46. Derosa G, D'Angelo A, Fogari E, et al. Effects of nateglinide and glibenclamide on prothrombotic factors in naive type 2 diabetic patients treated with metformin: a 1-year, double-blind, randomized clinical trial. Intern Med 2007; 46: 1837-46. (Pubitemid 350200169)
47. Derosa G, D'Angelo A, Fogari E, et al. Nateglinide and glibenclamide metabolic effects in naive type 2 diabetic patients treated with metformin. J Clin Pharm Ther 2009; 34: 13-23.
48. Gerich J, Raskin P, Jean-Louis L, et al. PRESERVE-beta: two-year efficacy and safety of initial combination therapy with nateglinide or glyburide plus metformin. Diabetes Care 2005; 28: 2093-9. (Pubitemid 41242450)
49. Schwarz SL, Gerich JE, Marcellari A, et al. Nateglinide, alone or in combination with metformin, is effective and well tolerated in treatment-naive elderly patients with type 2 diabetes. Diabetes Obes Metab 2008; 10: 652-60. (Pubitemid 352044295)
50. Fonseca V, Grunberger G, Gupta S, et al. Addition of nateglinide to rosiglitazone monotherapy suppresses mealtime hyperglycemia and improves overall glycemic control. Diabetes Care 2003; 26: 1685-90. (Pubitemid 36929104)
51. Panelo A, Wing JR. Repaglinide/bedtime NPH insulin is comparable to twice-daily NPH insulin. Diabetes Care 2005; 28: 1789-90. (Pubitemid 40923094)
52. Civera M, Merchante A, Salvador M, et al. Safety and efficacy of repaglinide in combination with metformin and bedtime NPH insulin as an insulin treatment regimen in type 2 diabetes. Diabetes Res Clin Pract 2008; 79: 42-7.
53. Lund SS, Tarnow L, Frandsen M, et al. Combining insulin with metformin or an insulin secretagogue in non-obese patients with type 2 diabetes: 12 month, randomised, double blind trial. BMJ 2009; 339: b4324.
54. Dashora UK, Sibal L, Ashwell SG, Home PD. Insulin glargine in combination with nateglinide in people with type 2 diabetes: a randomized placebo-controlled trial. Diabet Med 2007; 24: 344-9. (Pubitemid 46452399)
55. McKillop AM, Duffy NA, Lindsay JR, et al. Insulinotropic actions of nateglinide in type 2 diabetic patients and effects on dipeptidyl peptidase-IV activity and glucose-dependent insulinotropic polypeptide degradation. Eur J Endocrinol 2009; 161: 877-85.
56. Stephens JW, Bodvarsdottir TB, Wareham K, et al. Effects of short-term therapy with glibenclamide and repaglinide on incretin hormones and oxidative damage associated with postprandial hyperglycaemia in people with type 2 dia betes mellitus. Diabetes Res Clin Pract 2011; 94: 199-206.
57. Bell PM, Cuthbertson J, Patterson S, O'Harte FP. Additive hypoglycaemic effect of nateglinide and exogenous glucagon-like peptide-1 in type 2 diabetes. Diabetes Res Clin Pract 2011; 91: e68-70.
58. Kitahara Y, Miura K, Yasuda R, et al. Nateglinide stimulates glucagon-like peptide-1 release by human intestinal L cells via a K(ATP) channel-independent mechanism. Biol Pharm Bull 2011; 34: 671-6.
59. Defronzo RA. Banting Lecture. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus. Diabetes 2009; 58: 773-95.
60. Guardado-Mendoza R, Davalli AM, Chavez AO, et al. Pancreatic islet amyloidosis, beta-cell apoptosis, and alpha-cell proliferation are determinants of islet remodeling in type-2 diabetic baboons. Proc Natl Acad Sci USA 2009; 106: 13992-7.
61. Madsbad S, Kilhovd B, Lager I, et al. Comparison between repaglinide and glipizide in type 2 diabetes mellitus: a 1-year multicentre study. Diabet Med 2001; 18: 395-401. (Pubitemid 32679389)
62. Marbury T, Huang WC, Strange P, Lebovitz H. Repaglinide versus glyburide: a one-year comparison trial. Diabetes Res Clin Pract 1999; 43: 155-66. (Pubitemid 29202125)
63. Raskin P. Oral combination therapy: repaglinide plus metformin for treatment of type 2 diabetes. Diabetes Obes Metab 2008; 10: 1167-77.
64. Wang W, Bu R, Su Q, et al. Randomized study of repaglinide alone and in combination with metformin in Chinese subjects with type 2 diabetes naive to oral anti-diabetes therapy. Expert Opin Pharmacother 2011; 12: 2791-9.
65. Meneilly GS. Effect of repaglinide versus glyburide on postprandial glucose and insulin values in elderly patients with type 2 diabetes. Diabetes Technol Ther 2011; 13: 63-5.
66. Bellomo Damato A, Stefanelli G, Laviola L, et al. Nateglinide provides tighter glycaemic control than gly buride in patients with type 2 diabetes with prevalent postprandial hyperglycaemia. Diabet Med 2011; 28: 560-6.
67. Raskin P, Klaff L, McGill J, et al. Efficacy and safety of combination therapy: repaglinide plus metformin versus nateglinide plus metformin. Diabetes Care 2003; 26: 2063-8. (Pubitemid 41184253)
68. Moses R, Slobodniuk R, Boyages S, et al. Effect of repaglinide addition to metformin monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 1999; 22: 119-24. (Pubitemid 29028307)
69. Saloranta C, Hershon K, Ball M, et al. Efficacy and safety of nateglinide in type 2 diabetic patients with modest fasting hyperglycemia. J Clin Endocrinol Metab 2002; 87: 4171-6.
70. Derosa G, Salvadeo SA, D'Angelo A, et al. Metabolic effect of repaglinide or acarbose when added to a double oral antidiabetic treatment with sulphonylureas and metformin: a double-blind, cross-over, clinical trial. Curr Med Res Opin 2009; 25: 607-15.
71. Holman RR, Haffner SM, McMurray JJ, et al. Effect of nateglinide on the incidence of diabetes and cardiovascular events. N Engl J Med 2010; 362: 1463-76.
72. Quast U, Stephan D, Bieger S, Russ U. The impact of ATP-sensitive K+ channel subtype selectivity of insulin secretagogues for the coronary vasculature and the myocardium. Diabetes 2004; 53: S156-64. (Pubitemid 39564538)
73. Muhlhauser I, Sawicki PT, Berger M. Possible risk of sulfonylureas in the treatment of non-insulin-dependent diabetes mellitus and coronary artery disease. Diabetologia 1997; 40: 1492-3. (Pubitemid 28004946)
74. Derosa G, Mugellini A, Ciccarelli L, et al. Comparison of glycaemic control and cardiovascular risk profile in patients with type 2 diabetes during treatment with either repaglinide or metformin. Diabetes Res Clin Pract 2003; 60: 161-9. (Pubitemid 36561617)
75. 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.
76. Derosa G. Nateglinide does not reduce the incidence of diabetes or cardiovascular outcomes in people with impaired glucose tolerance and cardiovascular disease or risk factors. Evid Based Med 2011; 16: 7-8.
77. Efanova IB, Zaitsev SV, Zhivotovsky B, et al. Glucose and tolbutamide induce apoptosis in pancreatic beta-cells. A process dependent on intracellular Ca2+ concentration. J Biol Chem 1998; 273: 33501-7.
78. Maedler K, Carr RD, Bosco D, et al. Sulfonylurea induced beta-cell apoptosis in cultured human islets. J Clin Endocrinol Metab 2005; 90: 501-6. (Pubitemid 40116700)
79. Blickle JF. Meglitinide analogues: a review of clinical data focused on recent trials. Diabetes Metab 2006; 32: 113-20.
80. Laghmich A, Ladriere L, Malaisse-Lagae F, Malaisse WJ. Long-term effects of glibenclamide and nateglinide upon pancreatic islet function in normal and diabetic rats. Pharmacol Res 1999; 40: 475-82.
81. Kalbag JB, Walter YH, Nedelman JR, McLeod JF. Mealtime glucose regulation with nateglinide in healthy volunteers: comparison with repaglinide and placebo. Diabetes Care 2001; 24: 73-7.
82. Schumacher S, Abbasi I, Weise D, et al. Single- and multiple-dose pharmacokinetics of repaglinide in patients with type 2 diabetes and renal impairment. Eur J Clin Pharmacol 2001; 57: 147-52. (Pubitemid 32449136)