Acarbose is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Alpha-Glucosidase inhibitor
In contrast to sulfonylureas, Acarbose does not enhance insulin secretion. The antihyperglycemic action of acarbose results from a competitive, reversible inhibition of pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolase enzymes. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, while the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in a delayed glucose absorption and a lowering of postprandial hyperglycemia. Because its mechanism of action is different, the effect of Acarbose to enhance glycemic control is additive to that of sulfonylureas, insulin or metformin when used in combination. In addition, Acarbose diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Acarbose has no inhibitory activity against lactase and consequently would not be expected to induce lactose intolerance.
Since acarbose prevents the digestion of complex carbohydrates, the drug should be taken at the start of main meals (taken with first bite of meal). Moreover, the amount of complex carbohydrates in the meal will determine the effectiveness of acarbose in decreasing postprandial hyperglycemia. Adults may take doses of 25 mg 3 times daily, increasing to 100 mg 3 times a day.
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 When such drugs are withdrawn from patients receiving Acarbose in combination with sulfonylureas or insulin, patients should be observed closely for any evidence of hypoglycemia.
Patients Receiving Sulfonylureas or Insulin: Sulfonylurea agents or insulin may cause hypoglycemia. Acarbose given in combination with a sulfonylurea or insulin may cause a further lowering of blood glucose and may increase the potential for hypoglycemia. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made. Very rarely, individual cases of hypoglycemic shock have been reported in patients receiving Acarbose therapy in combination with sulfonylureas and/or insulin.
Patient with inflammatory bowel disease, diabetic ketoacidosis or cirrhosis, colonic ulceration, partial intestinal obstruction or predisposition to this condition, chronic intestinal diseases associated with marked disorders of digestion or absorption and state/s which may deteriorate as a result of increased gas formation in the intestine (e.g. larger hernias). Severe hepatic and renal impairment (CrCl <25 mL/min). Patient exposed to stress (e.g. fever, trauma, infection, surgery). Mild to moderate hepatic and renal impairment. Pregnancy and lactation.
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 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. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
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.
Store below 25° C. Protect from moisture.
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