Acarbose

Prescribing Information (Research Brand)

Indications

Acarbose is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Therapeutic Class

Alpha-Glucosidase inhibitor

Pharmacology

Acarbose reversibly bind to pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolases. These enzymes inhibit hydrolysis of complex starches to oligosaccharides in the lumen of the small intestine and hydrolysis of oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine.

Used to reduce blood gluose in patients with type 2 diabetes. Acarbose is a complex oligosaccharide that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. Acarbose binds to and inhibits alpha amylase and alpha-gluocside hydrolases. In diabetic patients, this enzyme inhibition results in a delayed glucose absorption and a lowering of postprandial hyperglycemia.

Dosage & Administration

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.

Interaction

May enhance effects of other antidiabetics including insulin. Diminished effects with GI adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate splitting enzymes (e.g. amylase, pancreatin). Neomycin and colestyramine may enhance effects of acarbose. May inhibit absorption of digoxin.

Contraindications

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).

Side Effects

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 & Lactation

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).

Precautions

Patient exposed to stress (e.g. fever, trauma, infection, surgery). Mild to moderate hepatic and renal impairment. Pregnancy and lactation.

Storage Conditions

Store below 25° C. Protect from moisture.