The effects of theα-glucosidase inhibitor BAY g 5421 (Acarbose) on meal-stimulated elevations of circulating glucose, insulin, and triglyceride levels in man

Abstract

In blind studies the effects of a new alpha-glucosidase inhibitor (BAY g 5421) were tested in normal weight and overweight male volunteers after oral application of 75, 150, or 300 mg of BAY g 5421 or placebo per os before three standardized main meals of one day. Before and three hours after each meal blood glucose, serum insulin, and serum triglyceride levels were determined. In addition, safety studies were performed. BAY g 5421 induced a statistically significant, in part dose-dependent inhibition of the postprandial increase of blood glucose- and serum insulin levels. The reduction of the postprandial increase of serum triglyceride levels was variable. Routine blood chemistry and hematology tests have revealed no adverse side effects; but the application of the drug was frequently associated with intestinal effects, such as flatulence and diarrhea, which were substrate (carbohydrate) and, in part, dose-dependent.

Improvement of metabolic control in insulin dependent diabetics treated with the ?-glucosidase inhibitor Acarbose for two months

“…As reported in previous studies [5,7,18,19], the most disturbing side-effect of Acarbose is flatulence.…”

“…Among these compounds, Acarbose has been selected for its maximal inhibitory effects on starch digestion and sucrose absorption [4]. Preliminary studies have indicated that Acarbose reduces the rise in blood glucose following a meal or an oral sucrose load [3,18,19]. Until now, the potential benefit of Acarbose in insulin treated diabetics has been investigated in two short-term studies only.…”

Activation of the gut calcium-sensing receptor by peptide agonists reduces rapid elevation of plasma glucose in response to oral glucose load in rats

“…Prevention of postprandial hyperglycemia currently involves slowing carbohydrate digestion by dietary fibers (indigestible dextrin, guar gum, etc.) or ␣-glucosidase inhibitors (15,16,29,37). Delayed glucose absorption by the peptides demonstrated in the present study could also contribute to preventing the immediate occurance of hyperglycemia in response to meal ingestion (glucose spike).…”

“…The rate of carbohydrate digestion/absorption in the small intestine also affects glycemia. ␣-Glucosidase inhibitors attenuate postprandial glycemia and insulin secretion through delayed digestion of carbohydrates (15,16). Inhibition of gastric emptying also contributes to the prevention of postprandial hyperglycemia by reducing carbohydrate/glucose delivery in the small intestine.…”

Development of Mulberry Leaf Extract for Suppressing Postprandial Blood Glucose Elevation

“…The daily intake of the ME powder did not cause hypoglycemia or abnormal lipid profiles (i.e., high cholesterol). According to previous reports, long-term ingestion of GI (acarbose, tochi extract) reduced FAG, HbA1C, TG, and Tcho levels in the subjects (Fujita et al, 2003;Hillerbrand et al, 1979), changes which may contribute to diabetes prevention and improvement. The results of our study showed no such effects, which could be attributable to the short administration period.…”