Introduction
Acarbose (Precose)
and miglitol (Glycet) are the currently available
a-glucosidase
inhibitor class of oral anti-hyperglycemic agents. In general, these
drugs lower glucose levels without risk for weight gain or hypoglycemia.
Unfortunately, these drugs have gastrointestinal side effects that often
limit their acceptance.
Mechanism of
Action
a-Glucosidase
inhibitors are competitive, reversible inhibitors of pancreatic
a-amylase
and membrane-bound intestinal
a-glucosidase
hydrolase enzymes. Use of these drugs leads to blocking the
enzymatic degradation of complex carbohydrates in the small intestine.
Thus, less carbohydrate is absorbed and the carbohydrate that is absorbed
is delayed. Acarbose binding affinity for the
a-glucosidase
enzymes is: glycoamylase > sucrase > maltase > dextranase and has no
affinity for the
b-glucosidase
enzymes, such as lactase. Miglitol is a more potent inhibitor of
sucrase and maltase that acarbose, has no effect on
a-amylase.