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DRUG RECORD

 

MIGLITOL

OVERVIEW
Miglitol

 

Introduction

Miglitol is an alpha-glucosidase inhibitor which decreases intestinal absorption of carbohydrates and is used as an adjunctive therapy in the management of type 2 diabetes.  Miglitol has not been linked to instances of clinically apparent acute liver injury.

 

Background

Miglitol is an inhibitor of intestinal alpha-glucosidase which results in a decrease in intestinal absorption of starch, disaccharides and dextrin.  The inhibition of glucosidase activity in the intestinal brush border blocks the breakdown of starch and disaccharides to absorbable monosaccharides, leading to carbohydrate malabsorption and blunting of the postprandial rise in blood glucose.  Miglitol was approved for use in the United States in 1996 and was the second α-glucosidase inhibitor (after acarbose) introduced into clinical practice.  The current indications are for management of glycemic control in type 2 diabetes used combination with diet and exercise with or without other oral hypoglycemic agents or insulin.  Miglitol is available generically and under the brand name Glyset in tablets of 25, 50 and 100 mg.  The typical initial dose in adults is 25 mg with each meal (with the first bite) followed by a gradual increase to a maximum of 100 mg three times daily.  Miglitol causes malabsorption and gastrointestinal side effects are most common and flatulence, diarrhea, abdominal boating and rash.

 

Hepatotoxicity

In several large clinical trials, serum aminotransferase elevations were no more common with miglitol than with placebo, and all elevations that occurred were asymptomatic and resolved rapidly with stopping therapy.  Neither during these studies nor since approval and wide clinical use have reports of clinically apparent liver injury due to miglitol been published.  Thus, liver injury from miglitol must be very rare if it occurs at all.  There also have been no reports of patients who developed liver injury while on acarbose being switched to miglitol.

 

Mechanism of Injury

The reason why miglitol rarely causes liver injury is not known, but is likely related to its rapid renal clearance and absence of hepatic metabolism.  While similar to acarbose (which does cause liver injury) in its mechanism of action, miglitol is a structurally distinct synthetic pseudopolysaccharide.


Drug Class:  Antidiabetic Agents

 

Other Drugs in the Subclass Alpha Glucosidase InhibitorsAcarbose

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PRODUCT INFORMATION
Miglitol

 

REPRESENTATIVE TRADE NAMES
Miglitol – Generic, Glyset®

 

DRUG CLASS
Antidiabetic Agents

 

COMPLETE LABELING

Product labeling at DailyMed, National Library of Medicine, NIH

 

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DRUG CAS REGISTRY NUMBER MOLECULAR FORMULA STRUCTURE
Miglitol 72432-03-2 C8-H17-N-O5 Miglitol Chemical Structure

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REFERENCES
Miglitol

 

References updated: 15 May 2013

  1. Zimmerman HJ. Oral hypoglycemic agents and other diabetes therapy. In, Zimmerman, HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott,1999: pp. 575-9.  (Textbook of hepatotoxicity published in 1999 mentions that several instances of serum enzyme elevations and at least two cases of liver injury with jaundice have been linked to acarbose use; no mention of miglitol).

  2. Bhardwaj SS, Chalasani NP. Antidiabetic drugs. Cardiovascular and antidiabetic medications. In, Kaplowitz N, DeLeve LD, eds. Drug-induced liver disease. 2nd ed. New York: Informa Healthcare USA, 2007, pp. 611-7.  (Review of hepatotoxicity published in 2007 mentions that acarbose has been associated with hepatocellular injury despite the fact that it is minimally absorbed, but that miglitol has not been implicated in causing liver injury).

  3. Davis SN. Endocrine pancreas and pharmacotherapy of diabetes mellitus and hypoglycemia. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilman's the pharmacological basis of therapeutics. 12th ed. New York: McGraw-Hill, 2011, pp. 1237-74.  (Textbook of pharmacology and therapeutics).

  4. Segal P, Feig PU, Schernthaner G, Ratzmann KP, Rybka J, Petzinna D, Berlin C. The efficacy and safety of miglitol therapy compared with glibenclamide in patients with NIDDM inadequately controlled by diet alone. Diabetes Care 1997; 20: 687-91. PubMed Citation  (Controlled trial of miglitol vs glyburide vs placebo for 24 weeks in 201 patients with diabetes; 4 patients had elevations of liver enzymes at the end of the study [1 on miglitol, 1 glyburide and 2 placebo], but all 4 had some degree of elevation before treatment initiation).

  5. Miglitol for type 2 diabetes mellitus. Med Lett Drugs Ther 1999; 41 (1053): 49-50. PubMed Citation  (Brief review of role of miglitol in type 2 diabetes; "increased aminotransferase activity has not been reported with miglitol"; otherwise, the average cost, efficacy and tolerance of miglitol are similar to acarbose).

  6. Sels JP, Huijberts MS, Wolffenbuttel BH. Miglitol, a new alpha-glucosidase inhibitor. Expert Opin Pharmacother 1999; 1: 149-56. PubMed Citation  (Review of the mechanism of action of miglitol and summary of results of clinical trials; no discussion of side effects).

  7. Campbell LK, Baker DE, Campbell RK. Miglitol: assessment of its role in the treatment of patients with diabetes mellitus. Ann Pharmacother 2000; 34: 1291-301. PubMed Citation  (Systematic review of miglitol therapy of diabetes; rates of serum enzyme elevations during therapy with miglitol were low and similar to placebo).

  8. Scott LJ, Spencer CM. Miglitol: a review of its therapeutic potential in type 2 diabetes mellitus. Drugs 2000; 59: 521-49. PubMed Citation  (Systematic review of literature on miglitol; side effects of flatulence [15-24%], diarrhea [7-13%], and abdominal pain [1-3%] were common, partially dose related, and similar to rates with acarbose; "Unlike acarbose, treatment with miglitol was not associated with elevated serum transaminase levels").

  9. Carlson RF. Miglitol and hepatotoxicity in type 2 diabetes mellitus. Am Fam Physician 2000; 62: 315, 318. PubMed Citation  (Letter in response to a review article on treatment of diabetes correcting the statement that miglitol causes liver injury similar to that described with acarbose; in studies for up to 12 months, ALT elevations above 3 times the ULN occurred in 3% of acarbose-, but only 1% of miglitol treated patients with diabetes).

  10. Chiasson JL, Naditch L; Miglitol Canadian University Investigator Group. The synergistic effect of miglitol plus metformin combination therapy in the treatment of type 2 diabetes. Diabetes Care 2001; 24: 989-94. PubMed Citation  (Controlled trial of 8 weeks of miglitol vs placebo with or without metformin in 324 patients with diabetes; there were no differences in biochemical test results among the treatment groups and no liver related serious adverse event).

  11. Chitturi S, George J. Hepatotoxicity of commonly used drugs: nonsteroidal anti-inflammatory drugs, antihypertensives, antidiabetic agents, anticonvulsants, lipid-lowering agents, psychotropic drugs. Semin Liver Dis 2002; 22: 169-83. PubMed Citation  (Overview of hepatotoxicity of antidiabetic medications mentions that acarbose has been incriminated in hepatotoxicity, generally arising within 2 to 8 months of starting therapy with an acute hepatitis-like clinical picture, but that miglitol has not).

  12. van de Laar FA, Lucassen PL, Akkermans RP, van de Lisdonk EH, Rutten GE, van Weel C. Alpha-glucosidase inhibitors for patients with type 2 diabetes: results from a Cochrane systematic review and meta-analysis. Diabetes Care 2005; 28: 154-63. PubMed Citation  (Review of 41 studies, 30 of acarbose, 7 miglitol, 1 voglibose and 3 combined; discusses relative rates of side effects in comparison to placebo overall, but does not mention hepatic effects specifically).

  13. Chalasani N, Fontana RJ, Bonkovsky HL, Watkins PB, Davern T, Serrano J, Yang H, Rochon J; Drug Induced Liver Injury Network (DILIN). Causes, clinical features, and outcomes from a prospective study of drug-induced liver injury in the United States. Gastroenterology 2008; 135: 1924-34. PubMed Citation  (Among 300 cases of drug induced liver injury in the US collected from 2004 to 2008, none were attributed to miglitol or acarbose).

  14. Reuben A, Koch DG, Lee WM; Acute Liver Failure Study Group. Drug-induced acute
    liver failure: results of a U.S. multicenter, prospective study. Hepatology 2010;
    52: 2065-76. PubMed Citation  (Among 1198 patients with acute liver failure enrolled in a US prospective study between 1998 and 2007, 133 [11%] were attributed to drug induced liver injury, of which 4 were due to troglitazone, but none were attributed to miglitol or other antidiabetic medications).

  15. Drugs for type 2 diabetes. Treat Guidel Med Lett 2011; 9 (108): 47-54. PubMed Citation  (Concise review of the role of current antidiabetes medications in management of type 2 diabetes).

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OTHER REFERENCE LINKS
Miglitol
  1. PubMed logoRecent References on Miglitol

  2. Clinical Trials logoTrials on Miglitol

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