Acarbose is used along with proper diet and regular exercise to help improve blood sugar control in adults with type 2 diabetes mellitus.

Unlike sulfonylureas, Acarbose does not stimulate insulin secretion. Its glucose-lowering effect works by inhibiting enzymes in the digestive tract. Acarbose competitively and reversibly blocks pancreatic alpha-amylase and intestinal alpha-glucosidase enzymes. These enzymes are responsible for breaking down complex carbohydrates into simple sugars (glucose) in the small intestine. By slowing down carbohydrate digestion, Acarbose delays glucose absorption into the bloodstream, thereby reducing the rise in blood sugar levels after meals (postprandial hyperglycemia). Because of its unique mechanism, Acarbose can be used in combination with other antidiabetic medications such as sulfonylureas, insulin, or metformin for better glucose control. Additionally, it may reduce the weight gain and excessive insulin release associated with sulfonylureas. Acarbose does not affect lactase enzyme activity and therefore does not typically cause lactose intolerance.

The recommended starting dosage of Acarbose is 25 mg given orally three times daily at the start (with the first bite) of each main meal. However, some patients may benefit from more gradual dose titration to minimize gastrointestinal side effects. This may be achieved by initiating treatment at 25 mg once per day and subsequently increasing the frequency of administration to achieve 25 mg t.i.d. Maintenance Dosage Once a 25 mg t.i.d. dosage regimen is reached, dosage of Acarbose should be adjusted at 4–8 week intervals based on one-hour postprandial glucose or glycosylated hemoglobin levels, and on tolerance. The dosage can be increased from 25 mg t.i.d. to 50 mg t.i.d. Some patients may benefit from further increasing the dosage to 100 mg t.i.d. The maintenance dose ranges from 50 mg t.i.d. to 100 mg t.i.d.

Some medications can increase blood sugar levels and reduce the effectiveness of Acarbose. These include diuretics (e.g., thiazides), corticosteroids, phenothiazines, thyroid hormones, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers, and isoniazid. Patients taking these drugs with Acarbose should be carefully monitored for loss of glucose control. When these medications are stopped in patients using Acarbose with sulfonylureas or insulin, there is a risk of hypoglycemia, so close monitoring is required.

With Sulfonylureas or Insulin: Combination therapy may increase the risk of hypoglycemia. Dose adjustments of these drugs may be necessary. Rare cases of severe hypoglycemia (including shock) have been reported.

Acarbose is contraindicated in patients with known hypersensitivity to the drug. Acarbose is contraindicated in patients with diabetic ketoacidosis or cirrhosis. Acarbose is also contraindicated in patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or in patients predisposed to intestinal obstruction. In addition, Acarbose 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.

Diarrhea, gas, upset stomach, constipation, or stomach pain may occur in the first few weeks of treatment as your body adjusts to this medication, but these usually improve with time. Follow your prescribed diet to help lessen these side effects. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Pregnancy Category B. The safety of Acarbose in pregnant women has not been established. A small amount of radioactivity has been found in the milk of lactating rats after administration of radiolabeled acarbose. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, Acarbose should not be administered to a nursing woman.

Because of its mechanism of action, Acarbose when administered alone should not cause hypoglycemia in the fasted or postprandial state. Sulfonylurea agents or insulin may cause hypoglycemia. Because Acarbose given in combination with a sulfonylurea or insulin will cause a further lowering of blood glucose, it may increase the potential for hypoglycemia. Hypoglycemia does not occur in patients receiving metformin alone under usual circumstances of use, and no increased incidence of hypoglycemia was observed in patients when Acarbose was added to metformin therapy.

Oral glucose (dextrose), whose absorption is not inhibited by Acarbose, should be used instead of sucrose (cane sugar) in the treatment of mild to moderate hypoglycemia. Sucrose, whose hydrolysis to glucose and fructose is inhibited by Acarbose, is unsuitable for the rapid correction of hypoglycemia. Severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.

Pediatric Use: The safety and effectiveness of Acarbose in pediatric patients have not been established.

Geriatric Use: Of the total number of subjects in clinical studies of Acarbose in the United States, 27% were 65 and over, while 4% were 75 and over. No overall differences in safety and effectiveness were observed between these subjects and younger subjects.

Unlike sulfonylureas or insulin, an overdose of Acarbose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside. In cases of overdosage, the patient should not be given drinks or meals containing carbohydrates (polysaccharides, oligosaccharides and disaccharides) for the next 4–6 hours.

Alpha-glucosidase inhibitor.

Store below 25°C. Protect from moisture.