Glitazones and the metabolic syndrome: Mechanism of action, pathophysiology and therapeutic indications;Glitazonas e síndrome metabólica: Mecanismos de ação, fisiopatologia e indicações terapêuticas

Arquivos Brasileiros de Endocrinologia e Metabologia

Volumn 50, Issue 2, 2006, Pages 271-280

  De Brito Gomes, Marília ^a,b  

^a STATE UNIVERSITY OF RIO DE JANEIRO   (Brazil)

^b Disciplina de Diabetes   (Brazil)

Author keywords

DM2; Glitazones; Insulin resistance; Metabolic syndrome

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; FATTY ACID; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR;

ADIPOSE TISSUE; CHEMISTRY; DRUG EFFECT; HUMAN; INSULIN RESISTANCE; LIPID METABOLISM; METABOLIC SYNDROME X; METABOLISM; NON INSULIN DEPENDENT DIABETES MELLITUS; PATHOPHYSIOLOGY; PHYSIOLOGY; REVIEW; VASCULAR ENDOTHELIUM;

ADIPOSE TISSUE; DIABETES MELLITUS, TYPE 2; ENDOTHELIUM, VASCULAR; FATTY ACIDS, NONESTERIFIED; HUMANS; INSULIN RESISTANCE; LIPID METABOLISM; METABOLIC SYNDROME X; PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS; THIAZOLIDINEDIONES;

EID: 33744466793     PISSN: 00042730     EISSN: 16779487     Source Type: Journal    
DOI: 10.1590/S0004-27302006000200013     Document Type: Review

References (66)

1. Wild S, Roglic G, Green A, Sicree R, King H. Global prevalences of diabetes. Estimates for the year 2000 and projections for 2030. Diabetes Care 2004;27:1047-153.
2. http:/www.kenes.com/prediabetes/summary. Acessado em Outubro/2005.
3. Malerbi DA, Franco LJ; The Brazilian Cooperative Group on the Study of Diabetes Prevalence. Multicenter study of the prevalence of diabetes mellitus and impaired glucose tolerance in the urban Brazilian population aged 30-69 yr. Diabetes Care 1992;15:1509-16.
4. Torquato MTCG, Montenegro RM, Viana LAL, Souza RAGH, Lanna CM, Lucas JCB, et al. Prevalence of diabetes mellitus, impaired glucose tolerance and cardiovascular risk factors in the urban adult population of Ribeirão Preto. Diab Res Clin Pract 2000;50(suppl.1):S140.
5. DATASUS. http://tabnet.datasus.gov.br/tabnet/tabnet. htm#Morbidade. Acessado em Setembro/2004.
6. Ferrannini E, Gastaldelli A, Miyazaki Y, Matsuda M, Mari A, DeFronzo RA. β-cell function in subjects spanning the range from normal glucose tolerance to overt diabetes: a new analysis. J Clin Endocrinol Metab 2005;90:493-500.
7. Alberti KGMM, Zimmet P, Shaw J; IDF Epidemiology Task Force Consensus Group. The metabolic syndrome - a new worldwide definition. Lancet 2005;366:1059-62.
8. Eckel RH, Grundy SM, Zimmet PZ. The metabolic syndrome. Lancet 2005;365:1415-28.
9. Isomaa B, Almgren P, Tuomi T, Forsén B, Lahti K, Nissén M, et al. Cardiovascular morbidity and mortality associated with the metabolic syndrome. Diab Care 2001;24(4):686-9.
10. Ilane-Parikka P, Eriksson JG, Lindström J, Hämäläinen H, Kiukaanniemi SK, Laakso M, et al; The Finnish Diabetes Prevention Study Group. Prevalence of the metabolic syndrome and its components. Diabetes Care 2004;27(9):2135-40.
11. Haffner SM, Lehto S, Ronemaa T, Pyorala K, Laakso M. Mortality from coronary heart disease in subjects with type 2 diabetes and non diabetic subjects with and without prior myocardial infarction. N Engl J Med 1998;339:229-34.
12. American Diabetes Association. Economic costs of diabetes in the US in 2002. Diabetes Care 2003;26:917-32.
13. UK Prospective Diabetes Study 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.
14. Saydah SH, Fradkin J, Cowie CC. Poor control of risk factors for vascular disease among adults with previously diagnosed diabetes. JAMA 2004;291:335-42.
15. Brown JB, Nichols GA, Perry AP. The burden of treatment failure in type 2 diabetes. Diabetes Care 2004;27:1535-40.
16. Matthaei S, Stumvoll M, Kellerer M, Häring HU. Pathophysiology and pharmacological treatment of insulin resistance. Endocr Rev 2000;21:585-618.
17. Yki-Jarvinen H. The PROactive study: some answers, many questions. Lancet 2005;366:1240-1.
18. Fürnsinn C, Waldhäusl W. Thiazolidinediones: metabolic actions in vitro. Diabetologia 2002;45:1211-23.
19. Yki-Jarvinen H. Thiazolidinediones. N Engl J Med 2004;351:1106-18.
20. Zhang X, Young HA. PPAR and immune system-what do we know. Int Immunopharmacol 2002;2:1029-44.
21. Feinstein DL, Spagnolo A, Akar C, Weinberg G, Murphy P, Gavrilyuk V, et al. Receptor-independent actions of PPAR thiazolidinedione agonists: is mitochondrial function the key? Biochem Pharmacol 2005;15;70:177-88.
22. WilsonTM, Brown PJ, Sternbach DD, Hence BR. The PPARs: from orphan receptors to drug discovery. J Med Chem 2000;43:527-50.
23. Akbiyik F, Ray DM, Gettings KF, Blumberg N, Francis CW, Phipps RP. Human bone marrow megakaryocytes and platelets express PPARγ, and PPARγ agonists blunt platelet release of CD40 ligand and thromboxanes. Blood 2004;104:1361-8.
24. Koshiyama H, Shimono, D, Kuwamura N, Minamikawa, J, Nakamura Y. Inhibitory effect of pioglitzone on carotid arterial wall thickness in type 2 diabetes. J Clin Endocrinol Metab 2001;86(7):3452-60.
25. Martens F, Visseren FLJ, Lemay J, Koning EJP, Rabelink TJ. Metabolic and additional vascular effects of thiazolidinediones. Drugs 2002;62:1463-80.
26. Miyazaki Y, Mahankali A, Wajcberg E, Bajaj M, Mandarino LJ, Defronzo RA. Effect of pioglitazone on circulating adipocytokine levels and insulin sensitivity in type 2 diabetic patients. J Clin Endocrinol Metab 2004;89:4312-9.
27. Bajaj M, Suraamornkull S, Hardies LJ, Pratipanawatr T, DeFronzo RA. Plasma resistin concentration, hepatic fat content, and hepatic and peripheral insulin resistance in pioglitazone-treated type II diabetic patients. Int J Obes 2004;1-7.
28. McGarry JD. Dysregulation of fatty acid metabolism in the etiology of type 2 diabetes. Diabetes 2002;51:7-18.
29. Tan MH, Galtzer B, Johns D, Gilmore KJ. Pioglitazone as monotherapy or in combination with sulfonylurea o metformin enhances insulin sensitivity (HOMA-S or QUICKI) in patients with type 2 diabetes. Curr Med Res Opin 2004;20:723-4.
30. Larsen TM, Toubro S, Astrup A. PPARg agonists in the treatment of type II diabetes is increased fatness commensurate with long-term efficacy? Int J Obes Relat Metab Disord 2003;27:147-61.
31. Moller DE. New drug targets for type 2 diabetes and the metabolic syndrome. Nature 2001;414:821-7.
32. Guan HP. A futile metabolic cycle activated in adipocytes by antidiabetic agents. Nat Med 2002;8:1122-8.
33. Chui PC, Guan HP, Leherke M, Lazar MA. PPARg regulates adipocyte cholesterol metabolism via oxidized LDL receptor 1. J Clin Invest 2005;115:2244-56.
34. Tannock LR, Little PJ, Barret PHR, Wight TN, Chait A. Thiazolidinedionas reduce the LDL binding affinity of non-human primate vascular cell proteoglycans. Diabetologia 2004;47:837-43.
35. Chinetti G, Lestavel S, Bocher V, Remaley AT, Neve B, Torra IP, et al. PPAR-α and PPAR-γ activators induce cholesterol removal from human macrofage foam cells through stimulation of the ABCA1 pathway. Nat Med 2001;7(1):53-8.
36. Chiquette E, Ramirez G, DeFronzo R. A meta-analysis comparing the effect of thiazolidinediones on cardiovascular risk factors. Arch Intern Med 2004;164:2097-14.
37. Henke BR, Blanchard SG, Brackeen MF, Brown KK, Cobb JE, Collins JL, et al. N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. J Med Chem 1998;41:5020-36.
38. Koshiyama H, Shimono D, Kuwamura N, Minamikawa J, Nakamura Y. Inhibitory effect of pioglitzone on carotid arterial wall thickness in type 2 diabetes. J Clin Endocrinol Metab 2001;86(7);3452-60.
39. Haffner SM, Greenberg AS, Weston WM, Chen H, Williams K, Freed MI. Effect of rosiglitazone treatment on non traditional markers of cardiovascular disease in patients with type 2 diabetes mellitus. Circulation 2002;106:679-84.
40. Kurebayashi S, Xu X, Ishii S, Shiraishi M, Kouhara H, Kasayama S. A novel thiazolidinedione MCC-555 down-regulates tumor necrosis factor-alpha-induced expression of vascular cell adhesion molecule-1 in vascular endothelial cells. Atherosclerosis 2005;182:71-7.
41. Liu HB, Medcalf RL, Simpson RW, Dear AE. Thiazolidinediones inhibit TNFα induction of PAI-1 independent of PPARγ activation. Biochem Biophys Res Commun 2005;334:30-7.
42. Escandon JC, Cipolla M. Diabetes and endothelial dysfunction: a clinical perspective. Endocr Rev 2001;22:36-52.
43. Dandona P, Aljada A. Endothelial dysfunction in patients with type diabetes and the effects of thiazolidinedione antidiabetic agents. J Diab Complic 2004;18:91-102.
44. Wang CCL, Goalstone ML, Draznin B. Molecular mechanisms of insulin resistance that impact cardiovascular biology. Diabetes 2005;53:2735-40.
45. Brownlee M. Biochemistry and molecular cell biology of diabetic complications. Nature 2001;414:813-20.
46. Schrauwen P, Hesselink MKC. Oxidative capacity, liptoxicity, and mitochondrial damage in type 2 diabetes. Diabetes 2004;53:1412-7.
47. Natali A, Baldweg S, Toschi A, Capaldo B, Barbaro D, Gastaldelli A, et al. Vascular effects of improving metabolic control with metformin or rosiglitazone in type 2 diabetes. Diabetes Care 2004;27:1349-57.
48. Choi D, Kim SK, Choi SH, Ko YG, Ahn CW, Jang Y, et al. Preventative effects of rosiglitazone on restenosis after coronary stent implantation in patients with type 2 diabetes. Diabetes Care 2004;27:2654-60.
49. Tavares V, Hirata RD, Rodrigues AC, Monte O, Salles JE, Scalissi N, et al. Association between Pro12Ala polymorphism of the PPAR-gamma2 gene and insulin sensitivity in Brazilian patients with type 2 diabetes mellitus. Diabetes Obes Metab 2005;7:605-11.
50. Strowig S, Aviles-Santa ML, Raskin P. Improved glycemic control without weight gain using triple therapy in type 2 diabetes. Diabetes Care 2004;27:1577-83.
51. Berria R, Belfort R, DeFillippis E, Cusi K, Mahankali A, Miyasaki Y, et al. Fluid retention and hemodilution are not associated with reduction in hematocrit and hemoglobin following pioglitazone and rosiglitazone treatment in type 2 diabetes mellitus. Diabetologia 2005;48(suppl.1):A17.
52. Nesto RW, Bell D, Bonow RO, Fonseca V, Grundy SM, Horton ES, et al. Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association. Diabetes Care 2004;27:256-63.
53. Husein Z, Wentworth J, Nankervis A, Proietto J, Colman PG. Effectiveness and side effects of thiazolidinediones for type 2 diabetes: real-life experience from a tertiary hospital. MJA 2004;181:536-9.
54. Nichols GA, Gullion CM, Koro CE, Ephross AS, Brown JB. The incidence of congestive heart failure in type 2 diabetes. Diabetes Care 2004;27:1879-84.
55. Dormandy JA, Charbonnel B, Eckland DJ, Erdmann E, Massi-Benedetti M, Moules IK, et al; The PROactive investigators. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive (PROspective pioglitAzone Clinical Trial In macroVascular Events): a randomized controlled trial. Lancet 2005;366:1279-89.
56. Digman C, Klein AK, Pittas A. Leukopenia and thrombocitopenia caused by thiazolinediones. Ann Intern Med 2005;143:465-6.
57. Lebovitz HE, Kreider M, Freed MI. Evaluation of liver function in type 2 diabetic patients during clinical trials. Evidence that rosiglitazone does not cause hepatic dysfunction. Diabetes Care 2002;25:815-21.
58. Schoff C, Lubben G. Post-marketing surveillance study of the efficacy and tolerability of pioglitazone in insulin resistant patients with type 2 diabetes in general practice. Clin Drug Invest 2003;23:725-34.
59. Promrat K, Lutchman G, Uwaifo GI, Freedman RJ, Soza A, Heller T. A pilot study of pioglitazona treatment for nonalcoholic steatohepatitis. Hepatology 2004;39:188-96.
60. Guo Q, Sahoo SP, Wang PR, Milot DP, Ippolito MC, Wu MS, et al. A novel peroxisome proliferator-activated receptor α/γ dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology 2004;145:1640-8.
61. Buse JB, Rubin CJ, Friederich R, Viraswami-Appanna K, Lin KC, Montoro R, et al. Muraglitazar, a dual (alpha/gamma) PPAR activator: A randomized, doubleblind, placebo-controlled, 24-week monotherapy trial in adult patients with type 2 diabetes. Clin Ther 2005;27:1181-95.
62. Fargerberg B, Edwards S, Halmos T, Lopatynski J, Schuster H, Stender S, et al. Tesaglitazar, a novel dual peroxima γ/α proliferators- activated receptor agonist, dose dependently improves the metabolic abnormalities associated with insulin resistance in a nodiabetic population. Diabetologia 2005;48:1716-25.
63. Pegorier JP. PPAR receptors and insulin sensitivity: new agonists in development. Ann Endocrinol 2005;66:1S10-7.
64. Buchanan TA, Xiang AH, Peters RK, Kjos SL, Marroquin A, Goico J, et al. Preservation of pancreatic α-cell function and prevention of type 2 diabetes by pharmacological treatment of insulin resistance in high-risk Hispanic women. Diabetes 2002;51:2796-803.
65. http.www.diabetes.org.br/consenso_atual_2002. Acessado em Outubro/2005.
66. American Diabetes Association. Prevention or delay of T2DM. Diabetes Care 2004;1:S47-S54.