Brands, Medical Use, Clinical Data
- Hypoglycemic Agents
- Alpha-glucosidase Inhibitors
Brands / Synonyms
For treatment and management of diabetes type II (used in combination therapy as a second or third line agent)
Used to reduce blood gluose in patients with type 2 diabetes. Acarbose is a complex oligosaccharide that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. Acarbose binds to and inhibits alpha amylase and alpha-gluocside hydrolases. In diabetic patients, this enzyme inhibition results in a delayed glucose absorption and a lowering of postprandial hyperglycemia.
Mechanism of Action
Acarbose reversibly bind to pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolases. These enzymes inhibit hydrolysis of complex starches to oligosaccharides in the lumen of the small intestine and hydrolysis of oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine.
Biotrnasformation / Drug Metabolism
PRECOSE ® is contraindicated in patients with known hypersensitivity to the drug and in patients with diabetic
ketoacidosis or cirrhosis. PRECOSE ® is also contraindicated in patients with inflammatory bowel disease, colonic
ulceration, partial intestinal obstruction or in patients predisposed to intestinal obstruction. In addition, PRECOSE
® is contraindicated in patients who have chronic intestinal diseases associated with marked disorders of
digestion or absorption and in patients who have conditions that may deteriorate as a result of increased gas
formation in the intestine.
Certain drugs tend to produce hyperglycemia and may lead to loss of blood glucose control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel-blocking drugs, and isoniazid. When such drugs are administered to a patient receiving Acarbose, the patient should be closely observed for loss of blood glucose control. When such drugs are withdrawn from patients receiving Acarbose in combination with sulfonylureas or insulin, patients should be observed closely for any evidence of hypoglycemia.
Intestinal adsorbents (e. g., charcoal) and digestive enzyme preparations containing carbohydrate-splitting enzymes (e. g., amylase, pancreatin) may reduce the effect of Acarbose and should not be taken concomitantly.
Acarbose has been shown to change the bioavailabillty digoxin when they are co-administered, which may require digoxin dose adjustment.
Studies in healthy volunteers have shown that Acarbose has no effect on either the pharmacokinetics or pharmacodynamics of digoxin, nifedipine, propranolol, or ranitidine. Acarbose did not interfere with the absorption or disposition of the sulfonylurea glyburide in diabetic patients. Acarbose may affect digoxin bioavailabillty and may require dose adjustment of digoxin by 16% (90% confidence interval: 8-23%), decrease mean C max digoxin by 26% (90% confidence interval: 16-34%) and decrease mean trough concentrations of digoxin by 9% (90% confidence limit: 19% decrease to 2% increase).
The amount of metformin absorbed while taking Acarbose was bioequivalent to the amount absorbed when taking placebo, as indicated by the plasma AUC values. However, the peak plasma level of metformin was reduced by approximately 20% when taking Acarbose due to a slight delay in the absorption of metformin. There is little if any clinically significant interaction between Acarbose and metformin.