Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose hyperglycemia cannot be managed on diet alone

Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination.

Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in 15% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction.

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: Transaminases increased

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

Calcium channel blocking agents: May decrease the efficacy of acarbose due to hyperglycemic effects.

Corticosteroids: May decrease the efficacy of acarbose due to hyperglycemic effects.

Digoxin: Acarbose decreases the bioavailability of digoxin, resulting in lower serum concentrations.

Diuretics (including thiazides): May decrease the efficacy of acarbose due to hyperglycemic effects.

Enzyme replacement (pancrelipase, amylase): May decrease the efficacy of acarbose due to effects on carbohydrate metabolism.

Estrogens: May decrease the efficacy of acarbose due to hyperglycemic effects.

Isoniazid: May decrease the efficacy of acarbose due to hyperglycemic effects.

Nicotinic acid: May decrease the efficacy of acarbose due to hyperglycemic effects.

Oral contraceptives: May decrease the efficacy of acarbose due to hyperglycemic effects.

Phenothiazines: May decrease the efficacy of acarbose due to hyperglycemic effects.

Sulfonylureas: 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.

Thyroid hormones: May decrease the efficacy of acarbose due to hyperglycemic effects.

Absorption: <2% as active drug

Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified

Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract

Excretion: Urine (~34%)

Adults: Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose

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:

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: Clcr<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.

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

Bischoff H, "Pharmacology of -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 -Glucosidase Inhibitor Acarbose in Normal Man,"Eur J Clin Invest, 1994, 24(Suppl 3):50-4.