Acarbose is an oligosaccharide antidiabetic agent.
Pharmacology: Mechanism of Action: The antihyperglycemic action of acarbose results from a competitive, reversible inhibition of pancreatic α-amylase complex starches to oligosaccharides in the lumen of the small intestine, while the membrane-bound intestinal and membrane-bound intestinal α-glucoside hydrolase enzymes. Pancreatic α-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, while the membrane-bound intestinal α-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.
Pharmacokinetics: Following oral dosing of healthy volunteers with 14C-labeled acarbose, peak plasma concentrations of radioactivity were attained 14-24 hrs after dosing, while peak plasma acarbose, concentrations of active drug were attained at approximately 1 hr. The delayed absorption of acarbose-related radioactivity reflects the absorption of metabolites that may be formed by either intestinal bacteria or intestinal enzymatic hydrolysis.
Acarbose is metabolized exclusively within the gastrointestinal tract, principally by intestinal bacteria.
The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys.
As monotherapy, as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus whose hyperglycemia cannot be managed on diet alone. Acarbose may also be used in combination with a sulfonylurea when diet plus either acarbose or a sulfonylurea does not result in adequate glycemic control. Also, acarbose may be used in combination with insulin or metformin.
Recommended Starting Dosage: 25 mg given orally 3 times daily at the start of each main meal. The dosage can be increased from 25-50 mg 3 times daily. Some patients may benefit from further increasing the dosage to 100 mg 3 times daily. Maintenance Dose: 50-100 mg 3 times daily.
Symptoms and Treatment: 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.
Patients with known hypersensitivity to acarbose, and in patients with diabetic ketoacidosis or cirrhosis. 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.
Use in lactation: It is known whether acarbose is excreted in human milk. Because many drugs are excreted in human milk, acarbose should not be administered to a nursing woman.
Acarbose itself does not cause hypoglycemia even when administered to patients in the fasted state. Sulfonylurea drugs and insulin, however, can lower blood sugar levels enough to cause symptoms or sometimes life-threatening hypoglycemia. Because acarbose given in combination with sulfonylurea or insulin will cause a further lowering of blood sugar, it may increase the hypoglycemic potential of these agents.
Use in lactation: It is known whether acarbose is excreted in human milk. Because many drugs are excreted in human milk, acarbose should not be administered to a nursing woman.
Abdominal pain, diarrhea and flatulence are some of the common adverse reactions observed.
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.
Intestinal adsorbents (eg, charcoal) and digestive enzyme preparations containing carbohydrate-splitting enzymes (eg, amylase, pancreatin) may reduce the effect of acarbose and should not be taken concomitantly.
Store below 25°C, in a dry place. Protect from direct sunlight.
A10BF01 - acarbose ; Belongs to the class of alpha glucosidase inhibitors. Used in the treatment of diabetes.
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