Alpha-glucosidase inhibitors are act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. The membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. that prevents the digestion of complex carbohydrates (such as starch). Complex carbohydrates are normally converted into simple sugars (monosaccharides) which can be absorbed through the intestine. Hence, alpha-glucosidase inhibitors reduce the impact of complex carbohydrates on blood sugar and decreases the post prandial hyperglycemia in diabetes. Voglibose is a research product of Takeda Pharma , A Japan based company. Postprandial hyperglycemia (PPHG) is primarily due to first phase insulin secretion. Alpha glucosidase inhibitors delay glucose absorption at the intestine level and thereby prevent sudden surge of glucose after a meal. There are three drugs which belong to this class, acarbose, miglitol and voglibose, of which voglibose is the newest. Voglibose scores over both acarbose and miglitol in terms of side effect profile.
Indications and Usage:
For the treatment of diabetes. It is specifically used for lowering post-prandial blood glucose levels thereby reducing the risk of macrovascular complications.
Mechanism of Action:
Mechanism of action Alpha-glucosidase inhibitors are saccharides that act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. The membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. Acarbose also blocks pancreatic alpha-amylase in addition to inhibiting membrane-bound alpha-glucosidases. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine. Inhibition of these enzyme systems reduces the rate of digestion of complex carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels: the long term effect is a small reduction in hemoglobin-A1c level.
Pharmacokinetics:
Voligbose has general properties similar to acarbose and selectively inhibits a-glucosidase in the enteric canal, delaying the digestion and absorption of carbohydrate, thereby suppressing sharp increase in post-prandial plasma glucose.
Pharmacodynamics:
Voglibose, an alpha-glucosidase inhibitor, is a synthetic compound with potent and enduring therapeutic efficacies against disorders of sensory, motor and autonomic nerve systems due to diabetes mellitus. The drug was approved in Japan in 1994 for the treatment of diabetes, and it is under further investigation by Takeda for the treatment of impaired glucose tolerance. Alpha-glucosidase inhibitors are oral anti-diabetic drugs used for diabetes mellitus type 2 that work by preventing the digestion of complex carbohydrates (such as starch). Complex carbohydrates are normally converted into simple sugars (monosaccharides) which can be absorbed through the intestine. Hence, alpha-glucosidase inhibitors reduce the impact of complex carbohydrates on blood sugar.
Contraindications:
Inflammatory bowel disease; GI obstruction or patients predisposed to it; conditions which may deteriorate as a result of increased gas formation eg, hernia; severe ketosis; diabetic coma or pre-coma; severe infection; hypersensitivity; pregnancy; lactation. Not to be used as monotherapy in IDDM.