Anti diabetic drug – Acarbose

Acarbose is used as anti-diabetic drug for treating Type 2 Diabetes. It inhibits Alpha Glucosidase which is an enteric enzyme that releases glucose from larger carbohydrates by digesting starches in food. Acarbose is used in condition in which the body does not use insulin normally and therefore cannot control the amount of sugar in the blood . Acarbose works by slowing the action of certain chemicals that break down food to release glucose (sugar) into the blood. Slowing food digestion helps keep blood glucose from rising very high after meals.

Acarbose belongs to the class of drugs termed Alpha-Glycosidase Inhibitors.

It is very important to take each dose with the first bite of each main meal

Acarbose is Prescribed for:
It is known that strict sugar control in diabetics decreases the risk of eye, kidney, and nerve damage. The use of Alpha-glycosidase inhibitors help to  lower blood sugar levels that are not controlled by diet and exercise. Acarbose can be used alone to treat type II diabetes or can be combined with sulfonylureas such as glyburide (Diabeta) or metformin (Glucophage) or with insulin..

Mechanism of action:
Acarbose inhibits enzymes (glycoside hydrolases) needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines and pancreatic alpha-amylase. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, whereas the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in 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 HbA1c.

Dosage Form:
The initial acarbose dose may start 25 mg three times daily and then increase after four to eight weeks to 50-100 mg three times daily. Acarbose is  be taken at the first bite of each meal.

Smaller doses may be adequate for patients with severe kidney dysfunction or liver disease. Acarbose is not recommended if cirrhosis is present. Acarbose therapy is not advised in the presence of certain medical conditions such as inflammatory bowel disease or intestinal obstruction and chronic intestinal diseases that interfere with digestion or absorption such as Crohn’s disease.
Acarbose doses should be adjusted based upon blood glucose levels taken one hour after a meal and blood HbA1c levels taken about three months after starting or changing the dose. (HbA1c is a chemical in the blood that is a good indicator of blood glucose control.)
Acarbose is the only agent approved for the treatment of prediabetes. The excellent safety, efficacy profile along with cardioprotective action makes acarbose a valuable option to treat type II diabetes.
Acarbose is more effective in post meal endothelial dysfunction

Drug Interactions:
Acarbose may interfere with digoxin absorption thereby decreasing digoxin blood levels and its effect. Therefore, the digoxin dose may need to be increased if acarbose is begun. Since adding insulin or a sulfonylurea to acarbose therapy may lower blood glucose more than acarbose alone, the risk for developing hypoglycemia is greater when these drugs are combined. Caution should be used when combining these drugs. If mild to moderate hypoglycemia occurs while taking acarbose in combination with another anti-diabetic agent, the hypoglycemia should be treated with oral glucose (dextrose) instead of sucrose (table sugar) because acarbose blocks the digestion of sucrose to glucose, and hypoglycemia will not be corrected rapidly with sucrose. Acarbose alone does not produce hypoglycemia.

Pregnancy:
.Acarbose is not harmful to an unborn baby. Do not take acarbose without first talking to doctor during pregnancy.

Nursing Mothers:
Acarbose passes into breast milk and may affect a nursing infant. Hence it is advised to first consult the doctor before giving to nursing mothers.

Possible Side Effects:
The most common side effects with acarbose therapy are abdominal pain, diarrhea and flatulence. There is a rare possibility that these gastrointestinal side effects may become severe and progress to paralytic ileus. Other possible but rare side effects are an increase in liver enzymes, and decreases in hematocrit, calcium or vitamin B6 levels.

Storage:
Acarbose should be stored at room temperature, 59-86°F (15-30°C) away from moisture and heat in he container it came in, tightly closed, and out of reach of children.

Conclusion: Acarbose is the only agent approved for the treatment of prediabetes. The excellent safety, efficacy profile along with cardioprotective action makes acarbose a valuable option to treat type II diabetes.

Reference

Acarbose

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