Drug information of Miglitol


Drug group: blood sugar

GLYSET Tablets contain miglitol, an oral alpha-glucosidase inhibitor for use in the management of non-insulin-dependent diabetes mellitus
GLYSET is available as 25 mg, 50 mg and 100 mg tablets for oral use.

Mechanism of effect

 In contrast to sulfonylureas, miglitol does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia.


Miglitol, an oral alpha-glucosidase inhibitor, is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time. Because its mechanism of action is different, the effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance.


absorption:  Absorption of miglitol is saturable at high doses with 25 mg being completely absorbed
while a 100-mg dose is only 50-70% absorbed. No evidence exists to show that systemic absorption of miglitol adds to its therapeutic effect.
volume of distribution:
  • 0.18L/kg
protein binding: The protein binding of miglitol is negligible (<4.0%)

metabolism:Miglitol is not metabolized in man or in any animal species studied.

route of elimination:Miglitol is not metabolized in man or in any animal species studied. It is eliminated by renal excretion as an unchanged drug.

half-life:The elimination half-life of miglitol from plasma is approximately 2 hours.

Drug indications

diabetes mellitus type2

Type 2 DM (Monotherapy or with Sulfonylurea)


Type 2 DM (Monotherapy or with Sulfonylurea)
Initial: 25 mg PO q8hr at meals (with first bite)
Maintanance: Usually 50 mg PO q8hr, increase after 4-8 weeks
Not more than 100 mg PO q8hr

Drug contraindications

intestinal obstruction

Hypersensitivity to miglitol

Diabetic ketoacidosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction

Disorders of GI digestion or absorption

Conditions that may deteriorate due to increased GI gas

Severe renal impairment

Side effects

Diarrhea , flatulence , Abdominal pain , Rash



Concurrent use with sulfonylureas may result in hypoglycemia; treat hypoglycemia with oral glucose, not sucrose

Pregnancy level

Pregnancy Category: B
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

Breast feeding warning

Enters slightly into breast milk; nor recommended

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