Classification: Antidiabetic agent
Action/Kinetics: An oligosaccharide obtained from a fermentation process using the microorganism Actinoplans utahensis. Causes a competitive, reversible inhibition of pancreatic alpha-amylase and membrane-bound intestinal alpha-glucosidase hydrolase enzymes. This causes delayed glucose absorption resulting in a smaller increase in blood glucose following meals. Glycosylated hemoglobin levels are decreased in those with non-insulin-dependent diabetes mellitus. Because the mechanism of action is different from sulfonylureas (i.e., enhance insulin secretion), acarbose is additive to the effect of sulfonylureas. Approximately 65% of an oral dose of acarbose remains in the GI tract, which is the site of action. Metabolized in the GI tract by both intestinal bacteria and intestinal enzymes. The acarbose and metabolites that are absorbed are excreted in the urine.
Uses: Used alone, with insulin or metformin, or with a sulfonylurea to treat type 2 diabetes mellitus. Diet control is essential.
Contraindications: Diabetic ketoacidosis, cirrhosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or predisposition to intestinal obstruction, chronic intestinal diseases associated with marked disorders of digestion or absorption, conditions that may deteriorate as a result of increased gas formation in the intestine. In significant renal dysfunction. Severe, persistent bradycardia. Lactation.
Special Concerns: Safety and efficacy have not been determined in children. Acarbose does not cause hypoglycemia; however, sulfonylureas and insulin can lower blood glucose sufficiently to cause symptoms or even life-threatening hypoglycemia.
Side Effects: GI: Abdominal pain, diarrhea, flatulence. GI side effects may be severe and be confused with paralytic ileus.
Laboratory Test Alterations: Serum transaminases (especially with doses greater than 50 mg t.i.d.). Small in hematocrit. Low plasma B 6 levels.
Overdose Management: Symptoms: Flatulence, diarrhea, abdominal discomfort. Treatment: Reduce dose; symptoms will subside.
How Supplied: Tablet: 25 mg, 50 mg, 100 mg