Acarbose

U.S. BRAND NAMES — Precose®
PHARMACOLOGIC CATEGORY Antidiabetic Agent, Alpha-Glucosidase Inhibitor
DOSING: ADULTS — Type 2 diabetes: Oral:
Initial: 25 mg 3 times/day
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance until maintenance dose is reached; maintenance dose: 50-100 mg 3 times/day. Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose.
Maximum: 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: ELDERLY — Refer to adult dosing.
DOSING: 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
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
DOSAGE FORMS: CONCISE Tablet: Precose®: 25 mg, 50 mg, 100 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered with the first bite of each main meal.
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.
ADVERSE REACTIONS SIGNIFICANT >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% (Limited to important or life-threatening): Severe gastrointestinal distress
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 Concerns related to adverse effects: Elevated serum transaminases: 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.
Disease-related concerns: Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues: Sulfonylureas: In combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
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.
Insulin: Acarbose may increase the hypoglycemic potential of insulin. 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.
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.
PREGNANCY RISK FACTOR — B (show table)
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/use caution
PRICING — (data from drugstore.com)Tablets (Precose) 25 mg (90): $79.17 50 mg (90): $81.95 100 mg (90): $94.45
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.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — 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. In cases of overdosage, the patient should not be given fluids or food containing carbohydrates (polysaccharides, oligosaccharides, or disaccharides) for 4-6 hours following overdose.
CANADIAN BRAND NAMES — Prandase®
INTERNATIONAL BRAND NAMES — Deglu (TW); Glibose (TW); Glicobase (IT); Glucobay (AE, AN, AR, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Gluconase (PH); Glucor (FR); Glumida (ES); Prandase (CA, IL); Rebose (IN)
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border 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 / 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%)
PATIENT INFORMATION — Take this medication exactly as directed, 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.
(For additional information see "Acarbose: Patient drug information")