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Pronunciation:

(AY car bose)

U.S. Brand Names:

Precose®

Generic Available:

Canadian Brand Names:

Prandase®

Use:

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.

Pregnancy Risk Factor:

Pregnancy Implications:

Abnormal blood glucose levels are associated with a higher incidence of congenital abnormalities. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.

Lactation:

Excretion in breast milk unknown

Contraindications:

Hypersensitivity to acarbose or any component of the formulation; 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

Warnings/Precautions:

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.

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.

Adverse Reactions:

>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

Overdosage/Toxicology:

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. However, acarbose may complicate the treatment of hypoglycemia from other causes, since it will inhibit the absorption of oral disaccharides (sucrose). Oral glucose (dextrose) should be used in mild to moderate hypoglycemia; severe hypoglycemia should be treated with I.V. glucose.

Drug Interactions:

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.

Ethanol/Nutrition/Herb Interactions:

Ethanol: Limit ethanol.

Stability:

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

Mechanism of Action:

Competitive inhibitor of pancreatic -amylase and intestinal brush border -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

Pharmacodynamics/Kinetics:

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%)

Dosage:

Oral:

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.

Administration:

Should be administered with the first bite of each main meal.

Monitoring Parameters:

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

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. 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 advised by prescriber. Avoid alcohol. It is important to follow dietary and lifestyle recommendations of prescriber. You will be instructed in signs of hypo- or 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. May cause 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 precaution: Consult prescriber if breast-feeding.

Nursing Implications:

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 mild to moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.

Cardiovascular Considerations:

Acarbose produces a slight but statistically significant reduction in Hb A1c (~1%) and fasting plasma glucose (~25 mg/dL). In general, acarbose may be used in combination with other agents (eg, sulfonylurea, metformin) or as monotherapy for patients with Type 2 diabetes. Therapy should be titrated slowly to minimize gastrointestinal side effects.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

May cause drowsiness

Mental Health: Effects on Psychiatric Treatment:

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

Dosage Forms:

Tablet: 25 mg, 50 mg, 100 mg

International Brand Names:

Asucrose® (IN); Glicobase® (IT); Glucobay® (AR, AT, AU, BE, BR, CH, CL, CO, CY, CZ, DE, DK, EC, EG, ES, GB, HR, HU, ID, IE, IN, IT, JO, JP, KW, LB, LU, MT, MX, NL, NO, NZ, PL, PT, RO, RU, SE, SG, SI, TH, TR, YU, ZA); Glucor® (FR); Glumida® (ES); Prandase® (CA, IL)

References

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.

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