Frati MAC, Martínez VE

Language: Spanish
References: 20
Page: 450-454
PDF size: 170.51 Kb.

ABSTRACT

Exenatide, or synthetic exendin-4, is a novel anti-diabetic drug, GLP-1 (glucagons like peptide-1) agonist, which restores the near-lost incretin effect in type 2 diabetes mellitus. Twice daily subcutaneous injection therapy increases insulin secretion mediated by glucose intake, it decreases glucagons hypersecretion, slows gastric emptying, diminishes food ingestion and body weight. The efficacy to control postprandial and fasting hyperglycemia has been consistently shown. An increase of pancreatic β-cells number in experimental animals has been found. Main adverse effect is nausea. Exenatide is indicated for the treatment of type 2 diabetics if diet and oral hypoglycemic drugs did not achieve glucose control. Its several therapeutic effects seem ideal for type 2 diabetes mellitus treatment and a possibility to change the outcome of this type of diabetes arises.

REFERENCES

1. Stonehouse A, Wintle M, Henry, et al. Exenatide (exendin-4) reduced HbA1c and weight over 52 weeks in sulphonylurea-treated patients with type 2 diabetes: P52B. Diabet Med 2005;22(2):42.

2. Baker DE. Exenatide: improves glycemic control in patients with type 2 diabetes mellitus. Advances in Pharmacy 2005;3(1)14-22.

3. Nauck MA, Zdravkovic M, Gumprecht J. Treatment with liraglutide + metformin results in significantly better glycaemic control and a greater reduction in weight than treatment with glimepiride + metformin in patients with type 2 diabetes: P68. Diabet Med 2005;22(Suppl 2):46.

4. Feinglos MN, Saad MF, Pi-Sunyer FX, et al. Effects of liraglutide (NN2211), a long-acting GLP-1 analogue, on glucaemic control and bodyweight in subjects with type 2 diabetes. Diabet Med 2005;22(8):1016-23.

5. Nielsen LL, Young AA, Parkes DG. Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes. Regul Pept 2004;117:77-88.

6. Young AA. Glucagon-like peptide-1, exendin and insulin sensitivity. In: Hansen B, Shafrir E, editors. Insulin resistance and insulin resistance syndrome. New York: Harwood Academic Press, 2002;pp:235-62.

7. Egan JM, Clocquet AR, Elahi D. The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to type 2 diabetes. J Clin Endocrinol Metab 2002;87:1282-90.

8. Kolterman OG, Buse JB, Fineman MS, et al. Synthetic exendin-4 (AC2993) significantly reduces postprandial and fasting plasma glucose in subjects with type 2 diabetes. J Clin Endocrinol Metab 2003;88(7):3082-9.

9. Zander M, Madsbad S, Madsen JL, Holst JJ. Effect of 6-week course of glucagon-like peptide 1 on glucaemic control, insulin sensitivity, and β-cell function in type 2 diabetes: a parallel-group study. Lancet 2002;359:824-30.

10. Edwards CM, Stanley SA, Davis R, et al. Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocrinol Metab 2001;281:E155-61.

11. Xu G, Stoffers DA, Habener JF, Bonner-Weir S. Exendin-4 stimulates both β-cell replication and neogenesis, resulting in increased β-cell mass and improved glucose tolerance in diabetic rats. Diabetes 1999;48:2270-6.

12. Tourrel C, Bailbé D, Meile M-J, Kergoat M, Portha B. Persistent improvement of type 2 diabetes in the Goto-Kakizaki rat model by expansion of the β-cell mass during the prediabetic period with glucagon-like peptide-1 or exendin-4. Diabetes 2002;51:1443-52.

13. Egan JM, Meneilly GS, Elahi D. Effects of 1-mo bolus subcutaneous administration of exendin 4 in type 2 diabetes. Am J Physiol Endocrinol Metab 2003;284:E1072-9.

14. Fineman MS, Bicsak TA, Shen LZ, Taylor K, et al. Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonylurea treatment in patients with type 2 diabetes. Diabetes Care 2003;26:2370-7.

15. Buse JB, Henry RR, Han J, Kim DD, et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care 2004;27:2628-35.

16. Kendall DM, Riddle MC, Rosenstock J, Zhuang D, et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and sulfonylurea. Diabetes Care 2005;28:1083-91.

17. DeFronzo RA, Ratner RE, Han J, Kim DD, et al. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care 2005;28:1092-100.

18. Kolterman OG, Kim DD, Shen L, et al. Pharmacokinetics, pharmacodynamics and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm 2005;62:173-81.

19. Degn KB, Brock B, Juhl CB, et al. Effect of intravenous infusion of exenatide (synthetic exendin-4) on glucose-dependent insulin secretion and counterregulation during hypoglycemia. Diabetes 2004;53:2397-403.

20. Calara F, Taylor K, Han J, et al. A randomized, open-label, crossover study examining the effect of injection site on bioavailability of exenatide (synthetic exendin-4). Clin Ther 2005;27:210-5.