A pseudotetrasaccharide and inhibitor of alpha-glucosidase and pancreatic alpha-amylase with antihyperglycemic activity. Acarbose binds to and inhibits alpha-glucosidase, an enteric enzyme found in the brush border of the small intestines that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents the breakdown of larger carbohydrates into glucose and decreases the rise in postprandial blood glucose levels. In addition, acarbose inhibits pancreatic alpha-amylase which hydrolyzes complex starches to oligosaccharides in the small intestines.
Information about Acarbose
Acarbose 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. Acarbose has been linked to rare instances of clinically apparent acute liver injury.
Mechanism of action of Acarbose
Acarbose (ay' kar bose) is an inhibitor of intestinal alpha-glucosidase, an enzyme responsible for digestion and absorption of starch, disaccharides and dextrin. The inhibition of the 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. Acarbose
FDA approval information for Acarbose
Acarbose was approved for use in the United States in 1995 and was the first alpha-glucosidase inhibitor introduced into clinical practice. A similar alpha glucosidase inhibitor, miglitol, was approved the following year. The current indications for acarbose are for management of glycemic control in type 2 diabetes used in combination with diet and exercise, with or without other oral hypoglycemic agents or insulin. Acarbose is available generically and under the brand name Precose in tablets of 25, 50 and 100 mg.
Dosage and administration for Acarbose
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. Acarbose causes malabsorption and gastrointestinal side effects of flatulence, diarrhea and abdominal boating are not uncommon.
- Alpha-Glucosidase Inhibitors
- Incretin-Based Drugs
- Metiglinide Analogues
- Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitors
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