Acarbose

U.S. BRAND NAMES — Precose®
CANADIAN BRAND NAMES — Prandase®
THERAPEUTIC CATEGORY Antidiabetic Agent, Alpha-glucosidase InhibitorAntidiabetic Agent, Oral
DOSING — Oral:
(For additional information see "Acarbose: Drug information")
Adolescents and Adults: Dosage must be individualized on the basis of effectiveness and tolerance; do not exceed the maximum recommended dose (use slow titration to prevent or minimize GI effects): Initial: 25 mg 3 times/day; increase in 25 mg/day increments in 2-4 week intervals to maximum dose Maximum dose: Patients 60 kg: 50 mg 3 times/day Patients >60 kg: 100 mg 3 times/day
Dosing adjustment in renal impairment: See Warnings
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
GENERIC AVAILABLE — No
ADMINISTRATION — Oral: Administer with first bite of each main meal
USE — Management of type II diabetes mellitus (noninsulin-dependent, NIDDM) when hyperglycemia cannot be managed by diet alone; may be used concomitantly with metformin, a sulfonylurea, or insulin to improve glycemic control
ADVERSE REACTIONS Central nervous system: Headache, vertigo, drowsiness
Dermatologic: Urticaria, erythema
Endocrine & metabolic: Hypoglycemia
Gastrointestinal: Abdominal pain, diarrhea, flatulence
Hepatic: Elevated liver enzymes
Neuromuscular & skeletal: Weakness
CONTRAINDICATIONS — Hypersensitivity to acarbose or any component; diabetic ketoacidosis; cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption; patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
PRECAUTIONS — Hypoglycemia may occur when used in combination with sulfonylureas or insulin; oral glucose (absorption is not affected by acarbose) should be used instead of sucrose (table sugar) for the treatment of mild to moderate hypoglycemia
WARNINGS — Dose-related elevations in serum transaminases occurred in 15% of acarbose-treated patients in long-term studies; these elevations were asymptomatic, reversible, more common in females, and not associated with other evidence of liver dysfunction; acarbose serum levels are proportionately higher in patients with renal dysfunction (Scr >2 mg/dL); until long term clinical studies are completed, use in renally-compromised patients is not recommended
DRUG INTERACTIONS — Drugs that produce hyperglycemia (eg, diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, rifampin, and isoniazid) may lead to a loss of glycemic control; intestinal adsorbents; digestive enzyme preparations; decreases bioavailability of digoxin resulting in decreased serum levels
PREGNANCY RISK FACTOR — B (show table)
MONITORING PARAMETERS — Fasting blood glucose; hemoglobin A1c; liver enzymes every 3 months for the first year of therapy and periodically thereafter
REFERENCE RANGE — Target range:
Blood glucose: Fasting and preprandial: 80-120 mg/dL; bedtime: 100-140 mg/dL
Glycosylated hemoglobin (hemoglobin A1c): <7%
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-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 — Average decrease in fasting blood sugar: 20-30 mg/dL
PHARMACOKINETICS Absorption: <2% absorbed as active drug
Metabolism: Metabolized exclusively within the GI tract, principally by intestinal bacteria and by digestive enzymes; 13 metabolites have been identified
Bioavailability: Low systemic bioavailability of parent compound
Elimination: Fraction absorbed as intact drug is almost completely excreted in urine
ADDITIONAL INFORMATION — Acarbose has been used successfully to treat postprandial hypoglycemia in children with Nissen fundoplications. Six children (4-25 months) initially received 12.5 mg before each bolus feeding of formula containing complex carbohydrates. The dosage was increased in 12.5 mg increments (dosage range: 12.5-50 mg per dose) until postprandial serum glucose was stable 60 mg/dL. Most commonly reported side effects were flatulence, abdominal distension, and diarrhea (Ng, 2001).