Miglitol, a new α-glucosidase inhibitor

Expert Opinion on Pharmacotherapy

Volumn 1, Issue 1, 1999, Pages 149-156

  Sels, Jean Pierre J E ^a   Maya, S P ^a   Huijberts, ^a   Wolffenbuttel, Bruce H R ^a  

^a MAASTRICHT UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

Acarbose; Clinical trials; Diabetes inellitiis; Metabolic effects; Miglitol; glucosidase

Indexed keywords

ALPHA GLUCOSIDASE; ANTIDIABETIC AGENT; DRUG DERIVATIVE; ENZYME INHIBITOR; GLUCOSAMINE; IMINOSUGAR; MIGLITOL;

ANIMAL; CLINICAL TRIAL; DIABETES MELLITUS; DRUG ANTAGONISM; ENZYMOLOGY; HUMAN; REVIEW;

ALPHA-GLUCOSIDASES; ANIMALS; CLINICAL TRIALS; DIABETES MELLITUS; ENZYME INHIBITORS; GLUCOSAMINE; HUMANS; HYPOGLYCEMIC AGENTS; IMINO PYRANOSES;

EID: 0033224332     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656566.1.1.149     Document Type: Article

References (50)

1. DCCT RESEARCH GROUP: The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulindependent diabetes mellitus. New Eugl. J. Med. (1993) 329:977-986.
2. TURNER RC, CULL C, HOLMAN RR: United Kingdom Prospective Diabetes Study 17: a 9-year update of a randomised, controlled trial on the effect of improved metabolic control on complications in non-insulindcpendent diabetes mellitus. Ann. Intern. Mecl. (1996) 124:136-145.
3. MIRANDA I'M, HORWITZ DL: High fiber diets in the treatment of diabetes mellitus. Ann. Intern. Med. (1978) 88:482-486.
4. JENKINS DJA, WOLEVERTMS, TAYLOR RM, REYNOLDS P, NINEHAM R, HOCKADAY TDR: Diabetic glucose control, lipid and trace elements on long term guar. Br. Med. J. (1980) 280:1353-1354.
5. AHR H-J, BOBERG M, BRENDEL E, KRAUSE HP, STEINKE W: Pharmacokinctics of miglitol. ArzneimForscbungJDnig Res. (.1997) 47:734-745. Extensive review of the pharmocokinetics of miglitol
6. LEMI5CKE B, FÖLSCH VR, CREUTZFELDT W: Effect of 1-deoxynojirimycin derivatives on small intestinal disaccharicla.se activities and on active transport in vitro. Digestion (1985) 31:120-127. • Interesting study showing difference of affinities of miglitol for digestive enzymes.
7. DEBOUNO JF, MICHAELIS IV OE, TULP OL: The effects of the intestinal glucosidasc inhibitor Bay M 1099 (Miglitol) on glycémie status of obese rats. Niilr. Kes. (1989) 9:1041-1042.
8. DEBOUNO JF, MICHAELIS IV OE, TULP OL: The effects of the intestinal glucosidase inhibitor Bay M 1099 (Miglitol) on glycémie status of obese rats. Gen. I'hannacol. (1993) 24:509-515.
9. TULP OL, SZEPESI B, MICHAELIS IV OE, DEBOUNO JF: The effects of low-dose Bay-m 1099 (Miglitol) on serum lip ids and liver enzyme activity of obese and obesediabetic corpulent rats. Comp. Biocbem. Pbysiol. (1991) 99C:241-246.
10. MADAR Z: The effect of acarbose and miglitol (Bay-M1099) on postprandial glucose levels following ingestion of various sources of starch by non-diabetic rats. J. Nutr. (1989) 119:2023-2029-
11. MADAR Z, HAZAN A: Effect of miglitol and acarbose on starch digestion, daily plasma profiles and cataract formation J. Basic Cbcni. Pbysiol. Pbannacol. (1993) 4:69-81. • Compares the effects of acarbose and miglitol on cataract formation in sand rats.
12. TORMO MA, ROPERO MF, NIETO M, MARTINEZ IM, CAMPILLO JE: lu vitro study of the effect of miglitol on carbohydrate digestion and intestinal metabolism in normal and non-insulin dependent diabetic rats. Cim. J. Physiol. I'hannacol (1996) 74:1196-1203.
13. LUDOLPH D, GROSS V, KATZ NR, GIFFMORN K, KREISEL W, HEINRICH PC, GEROK W: Effect of the cc-glucosidase inhibitor N-hydroethyl-1-desoxynojirimycin Bay m 1099 on the biosynthesis of liver secretory glycoproteins. Biocbem. Pbannacol. (1989) 38:2479-2486.
14. BOLLEN M, VANDEBROECK A, STALMANS W: 1-Dcoxynojirimycin and related compounds inhibit glycogenolysis in the liver without affecting the concentration of phosphorylase A. Biocbem. Pbannacol. (1988) 37:905-909.
15. BOLLEN M, STALMANS W: The antiglycogenolytic activity of 1-deoxynojirimycin results from a specific inhibition of the ct-1.6-glucosidase activity of the debranching enzyme. Enr. J. Biocbem. (1989) 181:775-780.
16. SALEHI A, LUNDQUIST T: Ca2 deficiency, selective a glucosidc hydrolasc inhibition and insulin secretion. Am.]. Pbysiol. (1993) 265:E1-E9.
17. REUSER AJJ, WISSELAAR HA: An evaluation of the potential side-effects of a glucosidasc inhibitors used for the management of diabetes mellitus. Eur.J. Clin. Incest. (1995) 24(Suppl. 3):19-24. • Assessment of the real risk of long-term use of miglitol.
18. WISSELAAR HA, VAN DONGEN JM, REUSER AJJ: Effects of N-hydroxyethyl-1-deoxynojirimycin (Bay m 1099) on the activity of neutral- and a-glucosidascs in human fibroblasts and HepF2 cells. Clin. Cbim. Ada (1989) 182:41-52.
19. KINGMA IJ, MENHEERE PPCA, SELS JP, NIEUWENHUIJZEN KRUSEMAN AC: a Glucosidase inhibition by miglitol in NIDDM patients. Diabetes Care (1992) 15:478-483. • This study demonstrates that for the day to day use of miglitol a dietary advice concerning the dietary starch content is not necessary.
20. JOUBERT PH, FOUKARID1S GN, BOLPAPE ML: Miglitol may have a blood glucose lowering effect unrelated to inhibitory alpha-glucosidasc. Enr. J. Clin. Pbannacol. (1987) 31:723-724.
21. JOUIiERT PH, VENTER HL, FOUKARIDIS GN: The effect of miglitol and acarbosc after oral glucose load: a novel hypoglycaemic mechanism? Br. J. Clin. Pbannacol. (1990) 30:391-396.
22. SELS JPJE, NAUTA JJP, MENHEERE PPCA, WOLFFENBUTTEL BHR, NIEUWENHUIJZEN KRUSEMAN AC: Miglitol (Bay m 1099) has no cxtraintcstinal effects on glucose control in healthy volunteers. Br. J. Clin. Pbannacol. (1996) 42:503-506. • Placebo-controlled study demonstrating that there are no extra-intestinal effects of miglitol.
23. VENTER HL, MUNTINGH G, £NNESLEY GV: Clinical trial to investigate the existence of a systemic effect of miglitol (single dose of 25 mg, 50 mg, 100 mg and 200 mg) by observing response to oral glucose load: concentration-effect and dose-effect relationship. Bayer AG Report, no R 6340. Extensive study using an important number of patients and different doses of miglitol. Systemic effects are not present.
24. HILLEBRAND I, BOEHME K, GRAEFE KH WEHLING K:The effect of new a-glucosidasc inhibitors (Bay m 1099 and Bay o 1248) on meal-stimulated increases in glucose and insulin levels in man. Klin. Wocbenscbr. (1986) 64:393-396.
25. LEMBCKE B, FÖLSCH UK, GATZEMEIER W, EBERT R, SIEGEL E, CREUTZFELDT W: Inhibition of glycémie and hormonal responses after repetitive sucrose and starch loads by different doses of the α-glucosidasc inhibitor miglitol (Bay m 1099) in man. Pbannacology (1991)43:318-328.
26. HEINZ G, KOMJATI M, KORN A, WALDHÄUSL W: Reduction of postprandial blood glucose by the a-glucosidasc inhibitor miglitol (Bay m 1099) in Type II diabetes. Eur.J. Clin. Pbannacol. (1989) 37:33-36.
27. SCHNACK CH, RÖGGLA G, LUGER A, SCHERNTHANER G: Effects of the a-glucosidase inhibitor 1 desoxynojirimycin (Bay M 1099) on postprandial blood glucose, serum insulin and C-pcptide levels in Type II diabetic patients. Eur.J. din. Phannacol. (1986) 30:417-419.
28. REQUEJO F, UTTENTHAL LO, I3LOOM SU: Effects of α-glucosidasc inhibition and viscous fibre on diabetic control and postprandial gut hormone responses. Diabetic Med. (1990) 7:515-520.
29. KATSILAMBROS N. PHILIPPIDES PU, TOSKAS A et cil.: A double-blind study on the efficacy and tolerance of a new a-glucosidase Inhibitor in type-2 diabetics. Arzneim. Foi-schSDnig Res. (1986) 36:1136-1138.
30. ARENDS J, WILLMS IJHL: Smoothing effect of a new a-glucosidase inhibitor Bay m 1099 on blood glucose profiles on sulphonylurea-treated Type II diabetic patients. Harm. Metab. Res. (1986) 18:761-761.
31. WILLMS B, KÜBKE AHRENS K, ARENDS J: Kesorptionsverzögcrung de Kohlenhydrate in der Therapie de Typ-II-Diabetcs: Vergleich zwisschen diätetischer (Müsli) und pharmacologischcr (a-Glucosidasehcnunung) Beeinflussing. Schweiz. Med. Wscbr. (1991) 121:1379-1382.
32. JOUDERT PH, BAM WJ, MANYANE N: Effect of an alphaglucosidasc inhibitor (Bay m 1099) on postprandial blood glucose and insulin in Type II diabetics. Enr.J. Clin. Pharmacol. (1986) 30:253-255.
33. SELS JPJE, KINGMA PJ, WOLFFENBUTTEL BHR, MENHEERE PPCA, BRANOLTE JH, NIEUWENHUIJZEN KRUSEMAN AC: Effect of miglitol (Bay m 1099) on fasting blood glucose in Type 2 diabetes mcllitus. Ketb. J. Meil. (1994) 44:198-201. This study demonstrates that miglitol cannot prevent the noctural rise of blood glucose in Type 2 diabetes patients.
34. 3. RENARD E, PARER-R1CHARD C. RICHARD J-L, JUREIDINIS, ORSETTI A, MIROUZE J: Effect of miglitol (Bay m 1099) a new a-glucosidasc inhibitor, on glucose, insulin, C-pcptide and GIF responses to an oral sucrose load hi patients with post-prandial hypoglycaemic symptoms. Diab. Metabol. (1991) 17:355-362.
35. LEMBCKE B, DIEDEKICH M, FÖLSCH UR, CREUTZFELDT W: Postprandial glycémie control, hormonal effects and carbohydrate malabsorption during long-term administration of the alplia-glucosida.se inhibitor miglitol. Digestion (1990) 47:47-55.
36. JOHNSTON PS, FEIG PU, CONIFF RF, KROL A, DAVIDSON JA, HAFFNER SM: Long-term titrated dose a-glucosidasc inhibition in non-insulin-rcquiring hispanic NIDDM patients. Diabetes Can? (.1998) 21:409-415.
37. JOHNSTON PS, FEIG PU, CONIFF RF, KKOL A, KELLEY DE, MOORADIAN AD: Chronic treatment of africanamerican Type 2 diabetic patients with α-glucosidase inhibition. Diabetes Can? (1998) 21:416-422. Placebo-controlled study in a population with high prevalence of Type 2 diabetes.
38. SEGAL P, FEIG PU, SCHERTNTHALER G et al.: The efficacy and safety of miglitol therapy compared with glibenclamide in patients with NIDDM inadequately controlled by diet alone. Diabetes Care (1997) 20:687-691.
39. JONHNSTON PS, LEBOVITZ HE. CONIFF RF, SIMONSON DC, RASKIN P, MUNERA C: Advantages of a-glucosidase inhibition as monothcrapy in elderly Type 2 diabetic patients..J. Clin. Eiirlocriiiot. Métal). (1998) 83:1515-1522. • This study demonstrated the usefulness of miglitol in this particular population
40. JOHNSTON PS, CONIFF RF, HOOGWERF IiJ, SANTIAGO JV, XAVIER I'I-SUNYER, KROL A: Effects of the carbohydrase inhibitor miglitol in sulphonylurea-treated NIDDM patients. Diabetes Care (1994) 17:20-29.
41. MITKAKOU A. TOUNTAS N, RAPTIS AE, BAUER RJ, SCHULZ H, RAPTIS SA: Long-term effectiveness of a new cc-glucosidasc inhibitor (Bay ml099-Miglitol) in insulin-treated Type 2 diabetes mcllitus. Diabetic Mecl. (1998) 15:657-660.
42. PAGANO G, MARENA S, CORGIAT-MANSIN L et al.: Comparison of miglitol and glibcnclamidc in diet-treated Type 2 diabetic patients. Diab. Metabol. (1995) 21:162-167. • This study demonstarted that miglitol was not superior to a frequently-used sulphonylurea compound. Glibenclamide gave a greater reduction of HbAlc.
43. SCHNACK C, PRAGER RJF, WINKLER J, KLAUSER RM, SCHNEIDER I3G, SCHERNTHANER G: Effects of 8-wk α-glucosidasc inhibition on metabolic control, C-peptide secretion, hepatic glucose output, and peripheral insulin sensitivity in poorly controlled Type II diabetic patients. Diabetes Care (1989) 12:537-543.
44. JOHNSON AB, TAYLOR R: Does suppression of postprandial blood glucose excursions by the a-glucosidasc inhibitor miglitol improve insulin sensitivity in diet-treated Type II diabetic patients? Diabetes Care (1996) 19:559-563. • Improvement of glycaemic control could increase insulin sensitivity. Smoothing postprandial blood glucose levels by miglitol could have this consequence. This study could not demonstrate a change in insulin sensitivity, probably caused by the limited reduction of blood glucose levels by miglitol.
45. MAISLOS M, VAN GAAL L, SEGAL P: Miglitol in combination with mctformin improves glucaemic control in Type 2 diabetics. Diabetologia (1999) 45:A223.
46. STANDL E, SCHERNTHANER G, RYBKA J, HANEFELD M: Improved glycaemic control with miglitol In Type 2 diabetics insufficiently controlled on oral hypiglycacmics. Diabetologia (1999) 45:A223
47. RYBKA J, GOKE B, SISSMANN J: European comparative study of 2 alpha-glucosidasc inhibitors, miglitol and acarbose. Diabetes (.1999) 48(SuppI. 1):A101.
48. WING J, KALK WJ, BERZIN M et al.: The acute effects of glucosidase inhibition on post-meal glucose increments in insulin-dependent diabetics. S. Afric. Mecl.J. (1990) 77:286-288.
49. HILLMAN RJ, SCOTT M, GRAY RS: Effect of alphaglucosidasc inhibition on glucose profiles in insulin dependent diabetes. Diabetes Res. (1989) 10:81-84.
50. DIMITRIADES G, HATZIAGELLAKI E, ALEXOPOULOS E et al.: Effects of a-glucosidasc inhibition on meal glucose tolerance and timing of insulin administration in patients with Type I diabetes mcllitus. Diabetes Care (1991) 14:393-398.