Brand Name: Glyset
Active Ingredient: miglitol
Approved uses: Glyset is indicated as monotherapy for the treatment of non-insulin dependent diabetes mellitus as an adjunct to diet to improve glycemic control in patients whose hyperglycemia can not be controlled by diet alone. Glyset is also approved for combination therapy with a sulfonylurea.
Company Name: Pharmacia & Upjohn Inc.
Availability: Prescription only
Glyset: Introduction
Glyset (miglitol) is an oral alpha-glucosidase inhibitor that is similar to acarbose (Precose®). Glyset has not yet demonstrated hepatotoxicity, which has occurred with the use of Precose. Although Glyset was first approved by the FDA in 1996, Pharmacia & Upjohn recently acquired the rights to Glyset and launched its sale in the US.
Glyset: How It Works
Glyset is a reversible inhibitor of membrane-bound intestinal alpha-glucoside hydrolase enzymes. These enzymes hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the small intestine. In patients with diabetes, inhibition of this enzyme results in delayed glucose absorption and lowering of postprandial hyperglycemia. Glyset can be used in combination with sulfonylureas to enhance glycemic control.
Glyset: Clinical Study Results
Several controlled, fixed-dose studies have been conducted to demonstrate the efficacy of Glyset monotherapy. The first study was one year in duration and evaluated a combination of Glyset and a sulfonylurea, in addition to Glyset as monotherapy. The results indicated that there was a statistically smaller increase in mean glycosylated hemoglobin (HbA1c) over time in the Glyset 50 mg three times a day arm when compared to placebo. Mean fasting and postprandial plasma glucose levels as well as mean postprandial insulin levels were significantly reduced in the Glyset group in comparison to the placebo group. In a 14-week study, patients in the Glyset group had a significant decrease in HbA1c in comparison to those taking placebo. The dose of Glyset used in this study was either 50 mg 0or 100 mg three times a day. Significant decreases in postprandial plasma glucose levels and postprandial insulin levels were seen in the Glyset group.
Several studies have also examined the use of Glyset in combination with sulfonylureas. The first study was 14 weeks’ duration and enrolled patients already on maximal doses of sulfonylureas. The patients received either Glyset 50 mg or 100 mg three times a day or placebo. Patients in the Glyset group had significantly reduced HbA1c levels at the end of the study period. A second study enrolled patients on maximum doses of glyburide and added either Glyset 25 mg, 50 mg or 100 mg three times a day or placebo to the regimen. At the end of the study, patients in both of the Glyset groups had significantly reduced HbA1c levels.
Glyset: What The Patient Should Know
Glyset is contraindicated in patients with diabetic ketoacidosis, inflammatory bowel disease, colonic ulceration or partial intestinal obstruction, and in patients predisposed to intestinal obstruction. Glyset should also be avoided in patients who suffer from chronic intestinal diseases associated with marked disorders of digestion or absorption, or those with conditions that may deteriorate as a result of increased gas formation in the intestine.
Glyset should be taken three times a day at the start of each main meal with the first bite of food.
Glyset does not cause hypoglycemia when administered alone, even in the fasted state. However, sulfonylureas and insulin can lower blood sugar levels enough to cause hypoglycemia. When Glyset is given in combination with a sulfonylurea or insulin it may increase the hypoglycemic potential of these agents. It is important that the patient and other family members recognize and understand the symptoms, predisposing factors, and treatment of hypoglycemia. Because Glyset prevents the breakdown of table sugar, a source of glucose should be kept available to be administered if the patient is taking Glyset in addition to sulfonylureas and insulin.
The most common adverse effects of Glyset are primarily dose-related gastrointestinal effects including flatulence, soft stools, diarrhea, or abdominal discomfort. Side effects, if they occur, usually develop in the first few weeks of therapy and generally diminish in frequency and intensity with time.