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Drugs
Erschienen in: Drugs 9/2002

01.06.2002 | Adis New Formulation Profile

Gliclazide Modified Release

verfasst von: Jane K. McGavin, Caroline M. Perry, Karen L. Goa

Erschienen in: Drugs | Ausgabe 9/2002

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Abstract

  • ▴ Gliclazide modified release (MR) is a new formulation of the drug gliclazide and is given once daily. The hydrophilic matrix ofhypromellose-based polymer in the new formulation effects a progressive release of the drug which parallels the 24-hour glycaemic profile in untreated patients with type 2 diabetes mellitus.
  • ▴ The formulation shows high bioavailability and its absorption profile is unaffected by coadministration with food. Mean plasma glucose levels are significantly reduced over a 24-hour period in patients with type 2 diabetes mellitus treated with gliclazide MR once daily, in both fasting and postprandial states.
  • ▴ No cardiovascular ATP-sensitive potassium channel interaction has been observed at therapeutic concentrations of gliclazide MR. Gliclazide MR has also demonstrated antioxidant properties that are independent of glycaemic control.
  • ▴ In a randomised, double-blind, multicentre study, gliclazide MR 30 to 120mg once daily showed similar efficacy to gliclazide immediate release (IR) 80 to 320 mg/day (in divided doses for doses >80ms) in patients with type 2 diabetes mellitus over a 10-montn period, reducing glycosylated haemoglobin (HbA1c) and fasting plasma glucose (FPG) to a similar extent.
  • ▴ The drug appeared most efficacious in patients who had previously been treated by diet alone, where significant reductions in HbAic from baseline of 0.9% and 0.95% were seen at 10 and 24 months. Similarly, a sustained effect of gliclazide MR was observed in a subgroup of elderly patients defined a priori; HbAic was decreased to a similar degree to that observed in the general study population.
  • ▴ Gliclazide MR showed similar tolerability to gliclazide IR after 10 months’ treatment in the randomised trial. The most commonly observed adverse events were arthralgia, arthritis, back pain and bronchitis (each <5%). Bodyweight remained stable.
  • ▴ In this study no episodes of nocturnal hypoglycaemia or hypoglycaemia requiring third party assistance were observed during treatment with gliclazide MR. Episodes of symptomatic hypoglycaemia were infrequent, occurring in approximately 5% of patients.
Literatur
1.
Harris MI, Flegal KM, Cowie CC, et al. Prevalence of diabetes, impaired fasting glucose, and impaired glucose tolerance in U.S. adults. Third National Health and Nutrition Examination Survey, 1988–1994. Diabetes Care 1998 Apr; 21(4): 518–24PubMedCrossRef
2.
Winter WE. Type 2 diabetes mellitus: the challenge of a metabolic epidemic. J Clin Ligand Assay 1998; 21 (No. 3): 293–308
3.
Meltzer S, Leiter L, Daneman D, et al. 1998 clinical practice guidelines for the management of diabetes in Canada. Can Med Assoc J 1998; 159 Suppl. 8: S1–29
4.
5.
ADVANCE Management Committee. Study rationale and design of ADVANCE: action in diabetes and vascular disease — preterax and diamicron MR controlled evaluation. Diabetologia 2001 Sep; 44: 1118–20CrossRef
6.
European Diabetes Policy Group. A desktop guide to Type 2 diabetes mellitus. Diabet Med 1999 Sep; 16: 716–30CrossRef
7.
American Diabetes Association. Standards of medical care for patients with diabetes mellitus. Diabetes Care 1999 Jan; 22 Suppl. 1:S32–41
8.
O’Keefe Jr JH, Miles JM, Harris WH, et al. Improving the adverse cardiovascular prognosis of type 2 diabetes. Mayo Clin Proc 1999 Feb; 74: 171–80PubMedCrossRef
9.
Harrower A. Gliclazide modified release: from once-daily administration to 24-hour blood glucose control. Metabolism 2000 Oct; 49 (10 Suppl. 2): 7–11PubMedCrossRef
10.
Gribble FM, Ashcroft FM. Differential sensitivity of beta-cell and extrapancreatic K(atp) channels to gliclazide. Diabetologia 1999 Jul; 42(7): 845–8PubMedCrossRef
11.
Gregorio F, Ambrosi F, Filipponi P, et al. Glucose modulates the amount, but not the kinetics, of insulin released by sulfonylureas. J Diabetes Complications 1994 Oct 31; 8: 204–12PubMedCrossRef
12.
Gregorio F, Ambrosi F, Cristallini S, et al. Therapeutical concentrations of tolbutamide, glibenclamide, gliclazide and gliquidone at different glucose levels: in vitro effects on pancreatic A- and B-cell function. Diabetes Res Clin Pract 1992 Dec; 18: 197–206PubMedCrossRef
13.
Pulido N, Suarez A, Casanova B, et al. Gliclazide treatment of streptozotocin diabetic rats restores GLUT4 protein content and basal glucose uptake in skeletal muscle. Metabolism 1997 Dec; 46: 10–3PubMedCrossRef
14.
Guillausseau PJ, Greb W. 24-Hour glycemic profile in type 2 diabetic patients treated with gliclazide modified release once daily. Diabetes Metab 2001 Apr; 27 (2 Pt 1): 133–7PubMed
15.
Lawrence CL, Proks P, Rodrigo GC, et al. Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia 2001 Aug; 44(8): 1019–25PubMedCrossRef
16.
Gribble FM, Tucker SJ, Scino S, et al. Tissue specificity of sulfonylureas: studies on cloned cardiac and beta cell K(atp) channels. Diabetes 1998 Sep; 47(9): 1412–8PubMedCrossRef
17.
Reimann F, Ashcroft FM, Gribble FM. Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes 2001 Oct; 50(10): 2253–9PubMedCrossRef
18.
Ravel D, Félétou M, Bouskela E. Differential effects of sulphonylureas on the vasodilatory response of KATPChannel openers in the rat and guinea-pig isolated aorta and the hamster cheek pouch [abstract]. J Physiol (Lond) 2001; 533: 117P
19.
Noda Y, Mori A, Cossins E, et al. Gliclazide scavenges hydroxyl and Superoxide radicals: an electron spin resonance study. Metabolism 2000 Feb; 49 (2 Suppl. 1): 14–6PubMedCrossRef
20.
Scott NA, Jennings PE, Brown J, et al. Gliclazide: a general free radical scavenger. Eur J Pharmacol 1991 Oct 14; 208(2): 175–7PubMedCrossRef
21.
O’Brien RC, Luo M, Balazs N, et al. In vitro and in vivo anti-oxidant properties of gliclazide. J Diabetes Complications 2000 Jul 31; 14(4): 201–6PubMedCrossRef
22.
O’Brien RC, Luo M. The effects of gliclazide and other sulfonylureas on low-density lipoprotein oxidation in vitro. Metabolism 1997 Dec; 46 (12 Suppl. 1): 22–5PubMedCrossRef
23.
Mamputu JC, Renier G. Gliclazide decreases vascular smooth muscle cell dysfunction induced by cell-mediated oxidized low-density lipoprotein. Metabolism 2001 Jun; 50(6): 688–95PubMedCrossRef
24.
Vallejo S, Angulo J, Peiro C, et al. Highly glycated oxyhaemoglobin impairs nitric oxide relaxations in human mesenteric microvessels. Diabetologia 2000 Jan; 43(1): 83–90PubMedCrossRef
25.
Vallejo S, Angulo J, Peiro C, et al. Correction of glycosylated oxyhemoglobin-induced impairment of endothelium-dependent vasodilatation by gliclazide. J Diabetes Complications 2000 Jul 31; 14(4): 207–14PubMedCrossRef
26.
Vallejo S, Angulo J, Peiro C, et al. Prevention of endothelial dysfunction in streptozotocin-induced diabetic rats by gliclazide treatment. J Diabetes Complications 2000 Jul 31; 14(4): 224–33PubMedCrossRef
27.
Desfaits AC, Serri O, Renier G. Gliclazide reduces the induction of human monocyte adhesion to endothelial cells by glycated albumin. Diabetes Obes Metab 1999 Mar; 1(2): 113–20PubMedCrossRef
28.
Desfaits AC, Serri O, Renier G. Gliclazide decreases cell-mediated low-density lipoprotein (LDL) oxidation and reduces monocyte adhesion to endothelial cells induced by oxidatively modified LDL. Metabolism 1997 Oct; 46(10): 1150–6PubMedCrossRef
29.
Omi H, Okayama N, Shimizu M, et al. Participation of high glucose concentrations in neutrophil adhesion and surface expression of adhesion molecules on cultured human endothelial cells: effect of antidiabetic medicines. J Diabetes Complications 2002. In press
30.
Kinoshita N, Kakehashi A, Inoda S, et al. Effective and selective prevention of retinal leukostasis in streptozotocin-induced diabetic rats using gliclazide. Diabetologia 2002. In press
31.
Delrat P, Paraire M, Jochemsen R. Complete bioavailability and lack of food-effect on pharmacokinetics of glicazide 30 mg modified release in healthy volunteers. Biopharm Drug Dispos 2002; 22. In press
32.
Francillard M, Frey N, Paraire M, et al. Pharmacokinetics of Diamicron modified release (MR) in 1007 type 2 diabetic patients [abstract]. Presented at the European Union Geriatric Medicine Society Annual Meeting; 2001 Aug 29–Sep 01; Paris.
33.
Frey N, Laveille C, Paraire M, et al. Effect of gliclazide in a new once-a-day formulation. In: Danhof M, Karlsson M, Powell RJ, editors. Measurement and kinetics of in vivo drug effects: advances in simultaneous pharmacokinetic/pharmacodynamic modelling; 2002 Apr 24–27; Noordwijkerhout. Amsterdam: Leiden University, 2002: 154–60
34.
Campbell DB, Lavielle R, Nathan C. The mode of action and clinical pharmacology of glicazide: a review. Diabetes Res Clin Pract 1991; 14: S21–36PubMedCrossRef
35.
Diamicron MR Study Group, Drouin P. Diamicron MR once daily is effective and well tolerated in type 2 diabetes: a double-blind, randomised, multinational study. J Diabetes Complications 2000; 14(4): 185–91CrossRef
36.
Drouin P. Two year efficacy and safety of Diamicron MR in inadequately controlled patients with type 2 diabetes [abstract. J Nutr Health Aging 2001; 5 (1 Special issue 31): F14
37.
Drouin P. Two year efficacy and safety of Diamicron® MR in inadequately controlled patients with type 2 diabetes. Presented at the European Union Geriatric Medicine Society Annual Meeting; 2001 Aug 29–Sep 01; Paris.
38.
Diamicron MR prescribing information. European summary of product characteristics. Servier, France. 2002
Metadaten
Titel
Gliclazide Modified Release
verfasst von
Jane K. McGavin
Caroline M. Perry
Karen L. Goa
Publikationsdatum
01.06.2002
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 9/2002
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.2165/00003495-200262090-00010

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