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Alpha-glucosidase inhibitors and lipase inhibitors for treatment of diabetes mellitus

David K McCulloch, MD
Section Editor
David M Nathan, MD
Deputy Editor
Jean E Mulder, MD


Two oral classes of drugs lower blood glucose by modifying the intestinal absorption of carbohydrates and fat: alpha-glucosidase inhibitors and lipase inhibitors. The pharmacology and use of these drugs will be discussed here. Other oral hypoglycemic drugs are reviewed separately. (See "Metformin in the treatment of adults with type 2 diabetes mellitus" and "Thiazolidinediones in the treatment of diabetes mellitus" and "Sulfonylureas and meglitinides in the treatment of diabetes mellitus".)


The alpha-glucosidase inhibitors (acarbose, miglitol, voglibose) have been studied extensively in Europe and Japan; two of them, acarbose and miglitol, are available in the United States. Taken orally, they inhibit the upper gastrointestinal enzymes (alpha-glucosidases) that convert complex polysaccharide carbohydrates into monosaccharides in a dose-dependent fashion. These drugs slow absorption of glucose; the slower rise in postprandial blood glucose concentrations is potentially beneficial in both type 1 and type 2 diabetes. In older patients with type 2 diabetes, acarbose may also increase insulin sensitivity [1].

Acarbose and voglibose have also been evaluated for the prevention of type 2 diabetes. (See "Prevention of type 2 diabetes mellitus", section on 'Drugs not recommended for prevention'.)

Efficacy — Several trials have demonstrated the efficacy of acarbose in patients with type 2 diabetes [2-4]. In one trial, 96 patients who were inadequately controlled by diet alone were randomly assigned to receive either glyburide or acarbose [2]. The A1C values and fasting blood glucose concentrations fell by a similar amount in both groups; postprandial blood glucose concentrations, however, remained high in the glyburide group but fell in the acarbose group. A second trial evaluated 354 patients treated with diet alone or diet plus a sulfonylurea, metformin, or insulin [3]. As compared with placebo, the addition of acarbose in each of these groups reduced the mean postprandial blood glucose concentration by 63 mg/dL (3.5 mmol/L) and lowered A1C values by 0.4 to 0.9 percentage points; furthermore, more than 50 percent of patients responded to acarbose. In general, acarbose has resulted in greater improvement in A1C values than in fasting blood glucose concentrations, consistent with its predominant effect on postprandial hyperglycemia [4].

Miglitol has similar efficacy, based upon studies in which it was given alone or combined with insulin or a sulfonylurea, as compared with placebo [5-9]. There are no studies that compare miglitol with acarbose, but they appear to have comparable effects. Miglitol is also effective when combined with metformin [10].

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Literature review current through: Nov 2017. | This topic last updated: Jun 19, 2017.
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