No

Antidiabetic Agent (Miscellaneous)

Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with noninsulin-dependent diabetes mellitus (NIDDM) whose hyperglycemia cannot be managed on diet alone

Combination with a sulfonylurea, metformin, or insulin in patients with NIDDM when diet plus acarbose do not result in adequate glycemic control

B

Breast-feeding/lactation: It is not known whether acarbose is excreted in human milk

Known hypersensitivity to the drug 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; 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

Hypoglycemia: Acarbose may increase the hypoglycemic potential of sulfonylureas. Oral glucose (dextrose) should be used in the treatment of mild to moderate hypoglycemia. Severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.

When diabetic patients are exposed to stress such as fever, trauma, infection, or surgery, a temporary loss of control of blood glucose may occur. At such times, temporary insulin therapy may be necessary.

>10%:

Gastrointestinal: Abdominal pain (21%) and diarrhea (33%) tend to return to pretreatment levels over time, and the frequency and intensity of flatulence (77%) tend to abate with time

Hepatic: Elevated liver transaminases

<1%: Sleepiness, headache, vertigo, erythema, urticaria, severe gastrointestinal distress, weakness

An overdose will not result in hypoglycemia; an overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside

Decreased effect: Thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel-blocking drugs, isoniazid, intestinal adsorbents (eg, charcoal), digestive enzyme preparations (eg, amylase, pancreatin)

Store at <25°C (77°F) and protect from moisture

Competitive inhibitor of pancreatic a-amylase and intestinal brush border a-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose

Absorption: <2% absorbed as active drug

Metabolism: Metabolized exclusively within the gastrointestinal tract, principally by intestinal bacteria and by digestive enzymes; ~34% of dose is metabolized, absorbed, and subsequently excreted in the urine; 13 metabolites have been identified

Bioavailability: Low systemic bioavailability of parent compound because acarbose acts locally within the gastrointestinal tract

Elimination: The fraction that is absorbed as intact drug is almost completely excreted by the kidney

Oral:

Initial dose: 25 mg 3 times/day with the first bite of each main meal

Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance. Dosage may be increased from 25 mg 3 times/day to 50 mg 3 times/day. Some patients may benefit from increasing the dose to 100 mg 3 times/day.

Maintenance dose ranges: 50-100 mg 3 times/day.

Maximum dose:

less than or equal to 60 kg: 50 mg 3 times/day

>60 kg: 100 mg 3 times/day

Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.

Dosing adjustment in renal impairment: Cl_cr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended

Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter

May cause drowsiness

Antipsychotics and tricyclic antidepressants may decrease the effects of acarbose. Monoamine oxidase inhibitors, SSRIs, and nefazodone may increase the effects of acarbose.

No information available to require special precautions

No effects or complications reported

Take this medication exactly as directed, with the first bite of each main meal. Do not change dosage or discontinue without first consulting prescriber. Do not take other medications with or within 2 hours of this medication unless so advised by prescriber. It is important to follow dietary and lifestyle recommendations of prescriber. You will be instructed in signs of hypo-/hyperglycemia by prescriber or diabetic educator. If combining acarbose with other diabetic medication (eg, sulfonylureas, insulin), keep source of glucose (sugar) on hand in case hypoglycemia occurs. You may experience mild side effects during first weeks of acarbose therapy (eg, bloating, flatulence, diarrhea, abdominal discomfort); these should diminish over time. Report severe or persistent side effects, fever, extended vomiting or flu, or change in color of urine or stool. Breast-feeding precautions: Consult prescriber if breast-feeding.

Administer acarbose 3 times/day at the start (with the first bite) of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. A source of glucose (dextrose) should be readily available to treat symptoms of low blood glucose when taking acarbose in combination with a sulfonylurea or insulin. If side effects occur, they usually develop during the first few weeks of therapy and are most often mild to moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.

Tablet: 50 mg, 100 mg

Balfour JA and McTavish D, "Acarbose: A Reappraisal," Drugs, 1993, 46(6):1025-54.

Bischoff H, "Pharmacology of a-Glucosidase Inhibition," Eur J Clin Invest, 1994, 24(Suppl 3):3-10.

Scheen AJ, de Magalhaes AC, Salvatore T, et al, "Reduction of the Acute Bioavailability of Metformin by the a-Glucosidase Inhibitor Acarbose in Normal Man," Eur J Clin Invest, 1994, 24(Suppl 3):50-4.