A szulfanilureavegyületek hosszú ideje a 2-es típusú diabetes vércukorcsökkentő kezelésének alapgyógyszerei. Az inkretin mechanizmusú antidiabetikumok megjelenésével azonban időről időre felmerül, van-e helye továbbra is e gyógyszercsoportnak napjaink terápiájában. A szerző áttekinti a szulfanilureák általános hatástani jellemzőit, s a Magyarországon forgalomban lévő második generációs származékok főbb sajátosságait. Kitér az inkretin hatású szerek, elsősorban a dipeptidil-peptidáz-gátlók és a szulfanilureák különbségeire. Megállapítja, hogy amint azt a legújabb kezelési irányelvek is tükrözik, a szulfanilureáknak ma is helye van a vércukorcsökkentő kezelésben, bár az inzulinszekretagóg szerek között a korábbinál hátrébb szorultak. Rendelésük esetén fontos a megfelelő készítményválasztás – rendezett vesefunkció esetén elsősorban gliclazid vagy glimepirid adása −, a cukorbeteg megfelelő edukálása, valamint a kívánt anyagcserehatást biztosító legkisebb dózis választása. Orv. Hetil., 2015, 156(13), 511–515.
Del Prato, S., Pulizzi, N.: The place of sulfonylureas in the therapy for type 2 diabetes mellitus. Metabolism, 2006, 55(Suppl. 1), S20–S27.
Makkar, B. M., Gupta, D., Gainda, A.: Clinical trials to clinical practice: role of sulfonylureas in today’s practice. In: Muruganathan, A. (ed.): Medicine Update, Vol. 23, 2013, Chapter 87, 393–398. www.apiindia.org/medicine_update_2013
Abrahamson, M. J.: Should sulfonylureas remain an acceptable first-line add-on to metformin therapy in patients with type 2 diabetes? Yes, they continue to serve us well! Diabetes Care, 2015, 38(1), 166–169.
Kalra, S., Gupta, Y.: Sulfonylureas. Recent Advances in Endocrinology, 2015, 65(1), 101–104.
Winkler, G.: The place of sulphonylurea compounds in the blood glucose lowering therapy of type 2 diabetes. [A szulfanilureák helye a 2-es típusú diabetes vércukorszint-csökkentő kezelésében.] Lege Artis Medicinæ, 2011, 21(5), 345–349. [Hungarian]
Gribble, F. M., Reimann, F.: Sulphonylurea action revisited: the post-cloning area. Diabetologia, 2003, 46(7), 875–891.
Karagiannis, T., Paschos, P., Paletas, K., et al.: Dipeptidyl peptidase-4 inhibitors for treatment of type 2 diabetes mellitus in the clinical setting: systematic review and meta-analysis. BMJ, 2012, 344, e1369.
Li, Y., Hu, Y., Ley, S. H., et al.: Sulfonylurea use and incident cardiovascular disease among patients with type 2 diabetes: prospective cohort study among women. Diabetes Care, 2014, 37(11), 3106–3113.
Monami, M., Genovese, S., Mannucci, E.: Cardiovascular safety of sulfonylureas: a meta-analysis of randomized clinical trials. Diabetes Obes. Metab., 2013, 15(10), 938–953.
Inzucchi, S. E., Bergenstal, R. M., Buse, J. B., et al.: Management of hyperglycemia in type 2 diabetes: a patient-centered approach: position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetes Care, 2012, 35(6), 1364–1379.
UK 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(9131), 837–853. Erratum: Lancet, 1999, 354(9178), 602.
Holman, R. R.: Long-term efficacy of sulfonylureas: a United Kingdom Prospective Diabetes Study perspective. Metabolism, 2006, 55(Suppl. 1), S2–S5.
Fowler, M. J.: Diabetes treatment, Part 2: Oral agents for glycemic management. Clin. Diabetes, 2007, 25(4), 131–134.
The ADVANCE Collaborative Group: Intensive blood glucose control and vascular outcomes in patients with type 2 diabetes. N. Engl. J. Med., 2008, 358(24), 2560–2572.
Hassanein, M., Abdallah, K., Schweizer, A.: A double-blind, randomized trial, including frequent patient-physician contacts and Ramadan-focused advice, assessing vildagliptin and gliclazide in patients with type 2 diabetes fasting during Ramadan: the STEADFAST study. Vasc. Health Risk. Manag., 2014, 10, 319–326.
Schramm, T. K., Gislason, G. H., 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(15), 1900–1908. Erratum: Eur. Heart J., 2012, 33(10), 1183.
Sarkar, A., Tiwari, A., Bhasin, P. S., et al.: Pharmacological and pharmaceutical profile of gliclazide: a review. J. Appl. Pharmaceutical Sci., 2011, 1(9), 11–19.
Winkler, M., Stephan, D., Bieger, S., et al.: Testing the bipartite model of the sulfonylurea receptor binding site: binding of A-, B-, and A+B-site ligands. J. Pharmacol. Exp. Ther., 2007, 322(2), 701–708.
Winkler, G.: The use of gliclazide in individualized solfonylurea therapy. [A gliclazid használata a differenciált szulfanilureaalkalmazás tükrében.] Orv. Hetil., 2014, 155(14), 541–548. [Hungarian]
Jarrard, R. E., Wang, Y., Salyer, A. E., et al.: Potentiation of sulfonylurea action by an EPAC-selective cAMP analog in INS-1 cells: comparison of tolbutamide and gliclazide, and a potential role for EPAC activation of a 2-APB-sensitive Ca2+ influx. Mol. Pharmacol., 2013, 83(1), 191–205.
Holz, G. G., Chepurny, O. G., Leech, C. A.: Epac2A makes a new impact in β-cell biology. Diabetes, 2013, 62(8), 2665–2666.
Kai, A. K., Lam, A. K., Chen, Y., et al.: Exchange protein activated by cAMP 1 (Epac1)-deficient mice develop β-cell dysfunction and metabolic syndrome. FASEB J., 2013, 27(10), 4122–4135.
Herbst, K. J., Coltharp, C., Amzel, L. M., et al.: Direct activation of Epac by sulfonylurea is isoform selective. Chem. Biol., 2011, 18(2), 243–251.
O’Brien, R. C., Luo, M., Balázs, N., et al.: In vitro and in vivo antioxidant properties of gliclazide. J. Diab. Compl., 2000, 14(4), 201–206.
Sena, C. M., Louro, T., Matafome, P., et al.: Antioxidant and vascular effects of gliclazide in type 2 diabetic rats fed high-fat diet. Physiol. Res., 2009, 58(2), 203–209.
Räkel, A., Renier, G., Roussin, A., et al.: Beneficial effects of gliclazide modified release compared with glibenclamide on endothelial activation and low-grade inflammation in patients with type 2 diabetes. Diabetes Obes. Metab., 2007, 9(1), 127–129.
Chen, L. L., Yu, F., Zheng, T. S., et al.: Effects of gliclazide on endothelial function in patients with newly diagnosed type 2 diabetes. Eur. J. Pharmacol., 2011, 659(2–3), 296–301.
Jennings, P. E.: Vascular benefits of gliclazide beyond glycemic control. Metabolism, 2000, 49(10 Suppl. 2), 17–20.
Del Guerra, S., D’Aleo, V., Lupi, R., et al.: Effects of exposure of human islet beta-cells to normal and high glucose levels with or without gliclazide or glibenclamide. Diabetes Metab., 2009, 35(4), 293–298.
Schernthaner, G., Grimaldi, A., DiMario, 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(8), 535–542.
Skyler, J. S., Bergenstal, R., Bonow, R. O., et al.: Intensive glycemic control and the prevention of cardiovascular events: implications of the ACCORD, ADVANCE and VA Diabetes Trials. A Position Statement of the American Diabetes Association and a Scientific Statement of the American College of Cardiology Foundation and the American Heart Association. J. Am. Coll. Cardiol., 2009, 53(3), 298–304.
Zoungas, S., Chalmers, J., Kengne, A. P., et al.: The efficacy of lowering glycated haemoglobin with a gliclazide modified release-based intensive glucose lowering regimen in the ADVANCE trial. Diabetes Res. Clin. Pract., 2010, 89(2), 126–133.
Al Sifri, S., Basiounny, A., Echtay, A., et al.: The incidence of hypoglycaemia in Muslim patients with type 2 diabetes treated with sitagliptin or a sulphonylurea during Ramadan: a randomised trial. Int. J. Clin. Pract., 2011, 65(11), 1132–1140.
Aravind, S. R., Ismail, S. B., Balamurugan, R., et al.: Hypoglycemia in patients with type 2 diabetes from India and Malaysia treated with sitagliptin or a sulfonylurea during Ramadan: a randomized, pragmatic study. Curr. Med. Res. Opin., 2012, 28(8), 1289–1296.
Harrower, A.: Gliclazide modified release: from once-daily administration to 24-hour blood glucose control. Metabolism, 2000, 49(10 Suppl. 2), 7–11.
Gore, M. O., McGuire, D. K.: Resolving drug effects from class effects among drugs for type 2 diabetes mellitus: more support for cardiovascular outcome assessments. Eur. Heart J., 2011, 32(15), 1832–1834.
Zhang, Y., McCoy, R. G., Mason, J. E., et al.: Second-line agents for glycemic control for type 2 diabetes: are newer agents better? Diabetes Care, 2014, 37(5), 1338–1345.
Saisho, Y.: Importance of beta cell function for the treatment of type 2 diabetes. J. Clin. Med., 2014, 3(3), 923–943.
Inzucchi, S. E., Bergenstal, R. M., Buse, J. B., et al.: Management of hyperglycemia in type 2 diabetes, 2015: a patient-centered approach: update to a position statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care, 2015, 38(1), 140–149.