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Acarbose (Systemic)

Introductory Information

Antidiabetic agent; an α-glucosidase inhibitor.1, 6, 30, 52

Class: 68:20.02 alpha-Glucosidase Inhibitors; hs502 (VA primary)

Brands: Precose®

Generic Name: Acarbose

CAS Number: 56180-94-0
Chemical Name: O-4,6-dideoxy-4-[[[1S-(1α,4α,5β,6α)]-4,5,6-trihydroxy-3-(hydroxymethyl)-2-
cyclohexen-1-yl]amino]-α-D -glucopyranosyl-(1 4)-O-α-d-glucopyranosyl-(1 4)-d-glucose
Molecular Formula: C25H43NO18
Investigational Drug Number: Bay g 5421

Uses

Diabetes Mellitus

Used as monotherapy as an adjunct to diet and exercise for the management of type 2 (noninsulin-
dependent) diabetes mellitus (NIDDM) in patients whose hyperglycemia cannot be controlled by diet
and exercise alone.1, 6, 14, 47

Also used as adjunct to diet and exercise in combination with metformin, a sulfonylurea, or insulin for
management of type 2 diabetes mellitus in patients whose hyperglycemia cannot be controlled with
acarbose, metformin, insulin, or sulfonylurea monotherapy, diet, and exercise.1, 3, 6, 14, 23, 26, 44, 47

Metformin generally recommended over other antidiabetic agents for initial oral antidiabetic therapy
because of absence of weight gain or hypoglycemia, relatively lower expense and greater efficacy, and
generally low adverse effect profile.110

ADA and other clinicians prefer addition of an insulin, a sulfonylurea, or a thiazolidinedione over an α-
glucosidase inhibitor (e.g., acarbose), pramlintide, exenatide, or a meglitinide (e.g., repaglinide,
nateglinide) as second-line therapy in patients inadequately controlled on metformin monotherapy
because of relatively lesser efficacy, limited clinical data, frequent GI adverse effects, and/or greater cost
with the latter agents.110

Acarbose should not be used as sole antidiabetic therapy in patients whose diabetes is complicated by
ketoacidosis with or without coma (e.g., type 1 [insulin-dependent, IDDM] diabetes mellitus); instead,
such patients should receive insulin.1, 57

Dosage and Administration

General

• Individualize treatment and adjust target blood glucose and glycosylated hemoglobin A1c (HbA1c)
concentrations based on patient's understanding and adherence to the treatment regimen, the risk of

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severe hypoglycemia, and other factors that may increase risk or decrease benefit (e.g., very young or
old age, comorbid conditions, other diseases that materially shorten life expectancy).1, 62
• Goal of therapy is to reduce both postprandial blood (or plasma) glucose and hemoglobin values to
normal or near normal using lowest effective dosage of acarbose as monotherapy or combined with a
sulfonylurea antidiabetic agent, metformin, or insulin.1 (Plasma glucose concentrations generally 10-
15% higher than those in whole blood and may vary according to method and laboratory used.)63
During therapy initiation and dosage titration, obtain 1-hour postprandial glucose concentration to
determine therapeutic response and minimum effective dosage.1, 14, 23, 52, 62 Monitor HbA1c values
at approximately every 3 months to evaluate long-term glycemic control.1, 14, 23, 52, 62 Monitor
glucose concentrations 1-2 hours after the start of a meal in those who have elevated HbA1c despite
adequate preprandial glucose concentrations.62

Administration

Oral Administration
Administer orally at the beginning (with the first bite) of each main meal.1, 23 If a dose is missed, take
the next dose at the next meal.108 Do not take a double dose to make up for the missed dose.108

Dosage

Adults
Diabetes Mellitus
Oral: Initially, 25 mg 3 times daily at the beginning of each main meal.1, 23 In patients with adverse GI
effects,2, 12, 23, 34 initiate at 25 mg once daily and increase dosage gradually as necessary to 25 mg 3
times daily.1
Once dosage of 25 mg 3 times daily has been reached, increase dosage at intervals of 4-8 weeks as
tolerated to achieve the desired 1-hour postprandial glucose concentration (i.e., <180 mg/dL).1, 23, 34, 41,
52, 62 Maintenance dosage ranges from 50-100 mg 3 times daily.1, 6, 47
Dosages higher than 100 mg 3 times daily are not recommended since such dosages have been
associated with an increased risk of elevated serum aminotransferase concentrations.1, 10, 18, 19, 20, 22,
23, 25, 27, 30, 37, 43, 52 If no further therapeutic benefit occurs at the maximum recommended dosage,

consider lowering the dosage.1

Prescribing Limits

Adults
Diabetes Mellitus
Oral: Patients ≤60 kg: maximum 50 mg 3 times daily.1, 23, 34, 41, 52
Patients >60 kg: maximum 100 mg 3 times daily.1

Cautions

Contraindications

• Known hypersensitivity to the drug.1

• Diabetic ketoacidosis.1

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• Cirrhosis.1
• Inflammatory bowel disease, colonic ulceration, existing partial intestinal obstruction or predisposition
to this condition.1
• Chronic intestinal diseases associated with marked disorders of digestion or absorption.1
• Co-existing conditions that may deteriorate as a result of increased intestinal gas formation.1

Warnings/Precautions

General Precautions
Metabolic Effects
Should not cause hypoglycemia when administered alone in the fasted or postprandial state.1 However,
hypoglycemia (rarely hypoglycemic shock) may occur when used concomitantly with a sulfonylurea
antidiabetic agent and/or insulin.1 If hypoglycemia occurs, adjust dosage of these agents appropriately.1
Use oral glucose (dextrose) for the treatment of mild to moderate hypoglycemia instead of sucrose (table
sugar);1 the absorption of oral glucose is not inhibited by acarbose.1 Severe hypoglycemia may require
the use of either IV glucose or parenteral glucagon.1

Insulin may be required for correction of temporary hyperglycemia that is not controlled by dietary
regulation or oral antidiabetic agents during periods of severe stress (e.g., acute infection, trauma,
surgery, fever).1, 57, 59

Hepatic Effects
Elevations in serum aminotransferase (i.e., ALT, AST) concentrations and, in rare instances,
hyperbilirubinemia may occur, particularly with dosages exceeding 150 mg daily (50 mg 3 times
daily).1, 23 Jaundice and fatal hepatitis reported during postmarketing experience.1

Determine serum aminotransferase concentrations every 3 months during the first year of therapy and
periodically thereafter.1 If elevations in serum aminotransferase concentrations occur, reduce dosage.1
May be necessary to withdraw the drug, particularly if elevated serum aminotransferase concentrations
persist.1

Adherence to Prescribed Diet

If prescribed diet not followed closely, adverse GI effects may be intensified.1, 108 To minimize adverse
GI effects, avoid rich foods, sauces, and certain beverages, including beer and carbonated soft drinks.108
Limit intake of gas-producing foods such as beans, nuts, bran cereals, broccoli, and cabbage.108
Consume low-fat meals and snacks.108 Drink plenty of water, especially in the early morning,
midmorning, and afternoon.108 Avoid overeating; food portions should be small to moderate in size.108
Eat food slowly and chew thoroughly.108 Keep food diary to identify problem foods.108

Specific Populations
Pregnancy
Category B.1

Lactation
Distributed into milk in rats.1 Not known whether distributed into human milk.1 Use not recommended
in nursing women.1

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Pediatric Use
Safety and efficacy in children <18 years of age not established.1, 23

Geriatric Use
Safety and efficacy in those ≥65 years of age similar to that in younger adults.1 (See Special Populations
under Pharmacokinetics: Absorption.)

Hepatic Impairment
Contraindicated in patients with cirrhosis.1, 23, 52 Not studied in other conditions associated with hepatic
impairment.1, 23, 52

Renal Impairment
Not recommended for use in diabetic patients with appreciable renal impairment (Scr >2 mg/dL).1, 23

Common Adverse Effects

Flatulence, diarrhea, abdominal discomfort/pain.1

Interactions

Digestive Enzyme Supplements

Possible reduction in the glycemic effects of acarbose.1 Avoid concomitant use.1

Intestinal Adsorbents

Possible reduction in the glycemic effects of acarbose.1 Avoid concomitant use.1

Specific Drugs

Drug Interaction Comments

Amylase (digestive Possible reduction in glycemic effects
Avoid concomitant use1
enzyme preparation) of acarbose1

Potential to exacerbate
hyperglycemia, resulting in loss of Monitor for loss of glycemic control1
When calcium-channel blocking agents
Calcium-channel glycemic control1
are withdrawn in patients receiving
blocking agents No effect of acarbose on the
concurrent sulfonylureas or insulin,
pharmacokinetic or
monitor for evidence of hypoglycemia1
pharmacodynamics of nifedipine1
Charcoal (intestinal Possible reduction in glycemic effects
Avoid concomitant use1
adsorbent) of acarbose1

Potential to exacerbate Monitor for loss of glycemic control1

Corticosteroids hyperglycemia, resulting in loss of When corticosteroids are withdrawn in
glycemic control1 patients receiving concurrent
sulfonylureas or insulin, monitor for

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Potential exacerbation of
Contraceptives, oral hyperglycemia/loss of glycemic
control1
Decreased blood concentrations of
Digoxin
digoxin1
Potential exacerbation of
Diuretics (e.g., hyperglycemia, resulting in loss of
thiazides)
glycemic control1
Potential to exacerbate
Estrogens hyperglycemia, resulting in loss of
glycemic control 1
No effect on absorption or disposition Pharmacokinetic interaction with
Glyburide
of concomitant glyburide1
Increased risk of hypoglycemia,
Insulin rarely hypoglycemic shock, with
concomitant insulin1
Potential to exacerbate
Isoniazid hyperglycemia, resulting in loss of
glycemic control1
Possible decreased peak plasma
Metformin
concentration of metformin1
Potential to exacerbate diabetes
Nicotinic acid mellitus, resulting in loss of glycemic patients receiving concurrent
control1
Pancreatin (digestive Possible reduction in glycemic effects
enzyme preparation) of acarbose1
Potential to exacerbate
Phenothiazines hyperglycemia, resulting in loss of
glycemic control1
Potential to exacerbate
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evidence of hypoglycemia1
Monitor for loss of glycemic control1
When oral contraceptives are withdrawn
in patients receiving concurrent
sulfonylureas or insulin, observe for
evidence of hypoglycemia1
May require increased digoxin dosage1
Monitor for loss of glycemic control1
When diuretics are withdrawn in patients
receiving concurrent sulfonylureas or
insulin, observe for evidence of
hypoglycemia1
Monitor for loss of glycemic control1
When estrogens are withdrawn in
patients receiving concurrent
sulfonylureas or insulin, observe for
evidence of hypoglycemia1
glyburide unlikely1
If hypoglycemia occurs, reduce insulin
dosage1
Monitor for loss of glycemic control1
When isoniazid is withdrawn in patients
receiving concurrent sulfonylureas or
insulin, monitor for evidence of
hypoglycemia1
Pharmacokinetic interaction not
considered clinically important1
Monitor for loss of glycemic control1
When nicotinic acid is withdrawn in
sulfonylureas or insulin, observe for
evidence of hypoglycemia1
Avoid concomitant use1
Monitor for loss of glycemic control1
When phenothiazines are withdrawn in
patients receiving concurrent
sulfonylureas or insulin, monitor for
evidence of hypoglycemia1
Monitor for loss of glycemic control1
When phenytoin is withdrawn in patients
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hyperglycemia, resulting in loss of receiving concurrent sulfonylureas or

Phenytoin glycemic control1 insulin, monitor for evidence of
hypoglycemia1
Delayed gastric emptying caused by
Avoid concomitant pramlintide;
α-glucosidase inhibitors may alter
Pramlintide safety/efficacy of combination therapy
effects of pramlintide on GI
not established112
absorption of nutrients112
Pharmacokinetic or
Propranolol pharmacodynamic interaction
unlikely1
Pharmacokinetic or
Ranitidine pharmacodynamic interaction
unlikely1
Reduced extent of absorption and
prolonged half-life of rosiglitazone113 Pharmacokinetic interaction not
Rosiglitazone
Potential for altered glycemic control considered clinically important113
is uncertain114
Increased risk of hypoglycemia,
If hypoglycemia occurs, reduce
Sulfonylureas hypoglycemic shock with
sulfonylurea dosage1
sulfonylureas1
Monitor for loss of glycemic control1
Potential to exacerbate When sympathomimetic agents are
Sympathomimetic hyperglycemia, resulting in loss of withdrawn in patients receiving
agents
glycemic control1 concurrent sulfonylureas or insulin,
monitor for evidence of hypoglycemia.1
Monitor for loss of glycemic control1
Potential to exacerbate When thyroid agents are withdrawn in
Thyroid agents hyperglycemia, resulting in loss of patients receiving concurrent
glycemic control1 sulfonylureas or insulin, monitor for
evidence of hypoglycemia1

Pharmacokinetics

Absorption

Bioavailability
Low systemic bioavailability of parent compound; <2% of dose is absorbed as active drug (parent
compound and active metabolite).1 Peak plasma concentrations of active drug attained at approximately
1 hour.1 Approximately 34% of dose absorbed as numerous metabolites.1

Onset
Satisfactory control of blood glucose concentrations achieved within a few days after dosage
adjustment; however18, 23 maximum response may be delayed for up to 2 weeks.18, 23

Special Populations
In geriatric patients, mean AUC and peak blood concentrations of the drug were higher compared with

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younger adults;1 differences not statistically significant.1

In individuals with severe renal impairment (CLcr <25 mL/minute), peak plasma drug concentrations
and AUC increased compared with those values in individuals with normal renal function.1

Distribution

Extent
Distributed into milk in rats.1

Elimination

Metabolism
Metabolized exclusively in GI tract, principally by intestinal bacteria but also by digestive enzymes to
numerous metabolites, one of which is active.1

Elimination Route
Excreted principally in feces (51% of dose) as unabsorbed drug and in urine as metabolites (34% of
dose).1 No accumulation with recommended dosing frequency.1

Half-life
Approximately 2 hours.1

Stability

Storage

Oral
Tablets
≤25°C.1 Protect from moisture.1

Actions

• Small inhibitory effect on α-glucosidase enzymes (e.g., glucoamylase, sucrase, maltase, isomaltase)
that hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other
monosaccharides in the intestinal brush-border.2, 6, 14, 24, 29, 30, 52 Small inhibitory effect on
pancreatic α-amylase, which hydrolyzes starch into maltose, maltotriose, and dextrins in the lumen of
the small intestine.2, 14, 30, 33 No inhibitory effect on lactase and would not be expected to produce
lactose intolerance.1
• Delays carbohydrate breakdown and glucose absorption and reduces postprandial hyperglycemia in
diabetic patients.1, 2, 6, 7, 10, 14, 23, 24, 30
• Reduces fluctuations in the daily blood glucose concentration-time profile in patients with type 2
diabetes mellitus and in lean or obese nondiabetic individuals.1, 2, 3, 6, 7, 19, 20, 21, 23, 24, 35, 37, 39, 47
Fasting blood glucose concentrations either not affected or mildly decreased.1, 2, 3, 6, 7, 19, 20, 21, 23,
24, 35, 37, 39, 47

• In contrast to sulfonylurea antidiabetic agents, acarbose does not enhance insulin secretion.1 Does not
produce hypoglycemia when given as monotherapy in fasting individuals.1

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• When used in combination with sulfonylurea antidiabetic agents are used in combination, acarbose
reduces the insulinotropic and weight-increasing effects of sulfonylureas.1 No clinically important
loss of calories or weight loss occurs in either diabetic or nondiabetic individuals.2, 6, 13, 14, 18, 21, 23,
28, 35, 37, 39

Advice to Patients

• Importance of adherence to diet and exercise regimen.1, 23 54

• Importance of adherence to dietary precautions designed to minimize adverse GI effects.1, 108
Importance of consulting a clinician for dosage adjustments if adverse GI effects occur despite
adherence to such dietary precautions.1 (See Adherence to Prescribed Diet under Cautions.)
• Importance of regular monitoring of blood glucose concentrations.1, 14, 23, 52, 62
• Importance of avoiding infection.23
• Provide instruction on the management of hyperglycemia or hypoglycemia.23, 62 Advise of the risk of
hypoglycemia, its symptoms, and conditions that predispose to the development of hypoglycemia.1
Importance of keeping a readily available source of glucose (dextrose) to treat symptoms of
hypoglycemia when used in combination with a sulfonylurea agent or insulin.1
• Importance of informing clinicians of existing or contemplated concomitant therapy, including
prescription and OTC drugs.1
• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-
feed.1
• Importance of advising patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some
individuals; consult specific product labeling for details.

Acarbose
Routes Dosage Forms Strengths Brand Names Manufacturer
Oral Tablets 25 mg Precose® Bayer
50 mg Precose® Bayer
100 mg Precose® Bayer

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing
information was updated 03/2011. For the most current and up-to-date pricing information, please visit
www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-
order locations and health insurance copays.

Acarbose 100MG Tablets (WATSON LABS): 100/$89.99 or 300/$239.97

Acarbose 25MG Tablets (WATSON LABS): 100/$81.99 or 300/$223.9

Acarbose 50MG Tablets (WATSON LABS): 100/$87.99 or 300/$235.96

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Precose 100MG Tablets (BAYER HEALTHCARE PHARMA): 90/$109.99 or 270/$299.97

Precose 25MG Tablets (BAYER PHARMACEUTICAL): 90/$85.51 or 270/$238.56

Precose 50MG Tablets (BAYER PHARMACEUTICAL): 90/$88.49 or 270/$250.48

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54. National Institutes of Health Office of Medical Applications of Research. Consensus development
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