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Acarbose (Monograph)

Drug class: alpha-Glucosidase Inhibitors
VA class: HS502
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
CAS number: 56180-94-0

Medically reviewed by Drugs.com on Jun 11, 2024. Written by ASHP.

Introduction

Antidiabetic agent; an α-glucosidase inhibitor.

Uses for Acarbose

Type 2 Diabetes Mellitus

Used as monotherapy as an adjunct to diet and exercise for the management of type 2 diabetes mellitus in patients whose hyperglycemia cannot be controlled by diet and exercise alone.

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 monotherapy with these agents, diet, and exercise.

Current guidelines for the treatment of type 2 diabetes mellitus generally recommend metformin as first-line therapy in addition to lifestyle modifications in patients with recent-onset type 2 diabetes mellitus or mild hyperglycemia because of its well-established safety and efficacy (i.e., beneficial effects on glycosylated hemoglobin [hemoglobin A1c; HbA1c], weight, and cardiovascular mortality).

In patients with metformin contraindications or intolerance (e.g., risk of lactic acidosis, GI intolerance) or in selected other patients, some experts suggest that initial therapy with a drug from another class of antidiabetic agents (e.g., a glucagon-like peptide-1 [GLP-1] receptor agonist, sodium-glucose cotransporter 2 [SGLT2] inhibitor, dipeptidyl peptidase-4 [DPP-4] inhibitor, sulfonylurea, thiazolidinedione, basal insulin) may be acceptable based on patient factors.

May need to initiate therapy with 2 agents (e.g., metformin plus another drug) in patients with high initial HbA1c (>7.5% or ≥1.5% above target). In such patients with metformin intolerance, some experts suggest initiation of therapy with 2 drugs from other antidiabetic drug classes with complementary mechanisms of action.

An α-glucosidase inhibitor (acarbose, miglitol) generally not recommended as second-line therapy after failure of metformin monotherapy because of comparatively lesser efficacy, frequent adverse GI effects, and greater cost, but may be appropriate therapy in selected patients.

Consider early initiation of combination therapy for the treatment of type 2 diabetes mellitus to extend the time to treatment failure and more rapidly attain glycemic goals.

For patients with inadequate glycemic control on metformin monotherapy, consider patient comorbidities (e.g., atherosclerotic cardiovascular disease [ASCVD], established kidney disease, heart failure), hypoglycemia risk, impact on weight, cost, risk of adverse effects, and patient preferences when selecting additional antidiabetic agents for combination therapy.

Consider early introduction of insulin for severe hyperglycemia (e.g., blood glucose ≥300 mg/dL or HbA1c >9–10%), especially if accompanied by catabolic manifestations (e.g., weight loss, hypertriglyceridemia, ketosis) or symptoms of hyperglycemia.

Acarbose Dosage and Administration

General

Administration

Oral Administration

Administer orally at the beginning (with the first bite) of each main meal.

To minimize adverse GI effects, closely follow diabetic diet as prescribed. (See Adherence to Prescribed Diet under Cautions.)

Dosage

Adults

Type 2 Diabetes Mellitus
Oral

Initially, 25 mg at the beginning of each main meal (with first bite) 3 times daily. In patients with adverse GI effects, initiate at 25 mg once daily and increase dosage gradually as necessary to 25 mg 3 times daily.

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) or until maximum dosage (according to weight) is reached. (See Prescribing Limits under Dosage and Administration.) Maintenance dosage ranges from 50–100 mg 3 times daily.

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. If no further therapeutic benefit occurs at the maximum recommended dosage, consider lowering the dosage.

Prescribing Limits

Adults

Type 2 Diabetes Mellitus
Oral

Patients ≤60 kg: maximum 50 mg 3 times daily.

Patients >60 kg: maximum 100 mg 3 times daily.

Cautions for Acarbose

Contraindications

Warnings/Precautions

General Precautions

Metabolic Effects

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

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).

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). Jaundice and fatal hepatitis reported during postmarketing experience.

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

Adherence to Prescribed Diet

If prescribed diet not followed closely, adverse GI effects may be intensified. If symptoms are strongly distressing despite adherence to prescribed diabetic diet, temporarily or permanently reduce acarbose dosage.

Specific Populations

Pregnancy

Category B.

Lactation

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

Pediatric Use

Safety and efficacy in children <18 years of age not established.

Geriatric Use

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

Hepatic Impairment

Contraindicated in patients with cirrhosis. Not studied in other conditions associated with hepatic impairment.

Renal Impairment

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

Common Adverse Effects

Flatulence, diarrhea, abdominal discomfort/pain.

Digestive Enzyme Supplements

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

Intestinal Adsorbents

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

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

1,5-Anhydroglucitol assay

Unreliable results in patients taking acarbose

Manufacturer recommends use of alternative method to monitor glycemic control

Amylase (digestive enzyme preparation)

Possible reduction in glycemic effects of acarbose

Avoid concomitant use

Calcium-channel blocking agents

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

No effect of acarbose on the pharmacokinetic or pharmacodynamics of nifedipine

Monitor for loss of glycemic control

When calcium-channel blocking agents are withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Charcoal (intestinal adsorbent)

Possible reduction in glycemic effects of acarbose

Avoid concomitant use

Corticosteroids

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When corticosteroids are withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Contraceptives, oral

Potential exacerbation of hyperglycemia/loss of glycemic control

Monitor for loss of glycemic control

When oral contraceptives are withdrawn in patients receiving concurrent sulfonylureas or insulin, observe for evidence of hypoglycemia

Digoxin

Decreased blood concentrations of digoxin

May require increased digoxin dosage

Diuretics (e.g., thiazides)

Potential exacerbation of hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When diuretics are withdrawn in patients receiving concurrent sulfonylureas or insulin, observe for evidence of hypoglycemia

Estrogens

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When estrogens are withdrawn in patients receiving concurrent sulfonylureas or insulin, observe for evidence of hypoglycemia

Glyburide

No effect on absorption or disposition of concomitant glyburide

Pharmacokinetic interaction with glyburide unlikely

Insulin

Increased risk of hypoglycemia, rarely hypoglycemic shock, with concomitant insulin

If hypoglycemia occurs, reduce insulin dosage

Isoniazid

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When isoniazid is withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Metformin

Possible decreased peak plasma concentration of metformin

Pharmacokinetic interaction not considered clinically important

Nicotinic acid

Potential to exacerbate diabetes mellitus, resulting in loss of glycemic control

Monitor for loss of glycemic control

When nicotinic acid is withdrawn in patients receiving concurrent sulfonylureas or insulin, observe for evidence of hypoglycemia

Pancreatin (digestive enzyme preparation; no longer commercially available in the US)

Possible reduction in glycemic effects of acarbose

Avoid concomitant use

Phenothiazines

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When phenothiazines are withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Phenytoin

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When phenytoin is withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Pramlintide

Delayed gastric emptying caused by α-glucosidase inhibitors may alter effects of pramlintide on GI absorption of nutrients

Avoid concomitant pramlintide; safety/efficacy of combination therapy not established

Propranolol

Pharmacokinetic or pharmacodynamic interaction unlikely

Ranitidine

Pharmacokinetic or pharmacodynamic interaction unlikely

Rosiglitazone

Reduced extent of absorption and prolonged half-life of rosiglitazone

Potential for altered glycemic control is uncertain

Pharmacokinetic interaction not considered clinically important

Sulfonylureas

Increased risk of hypoglycemia, hypoglycemic shock with sulfonylureas

If hypoglycemia occurs, reduce sulfonylurea dosage

Sympathomimetic agents

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When sympathomimetic agents are withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia.

Thyroid agents

Potential to exacerbate hyperglycemia, resulting in loss of glycemic control

Monitor for loss of glycemic control

When thyroid agents are withdrawn in patients receiving concurrent sulfonylureas or insulin, monitor for evidence of hypoglycemia

Acarbose Pharmacokinetics

Absorption

Bioavailability

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

Onset

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

Special Populations

In geriatric patients, mean AUC and peak blood concentrations of the drug were higher compared with younger adults; differences not statistically significant.

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.

Distribution

Extent

Distributed into milk in rats.

Elimination

Metabolism

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

Elimination Route

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

Half-life

Approximately 2 hours.

Stability

Storage

Oral

Tablets

≤25°C. Protect from moisture.

Actions

Advice to Patients

Preparations

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

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Acarbose

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

25 mg*

Acarbose Tablets

50 mg*

Acarbose Tablets

100 mg*

Acarbose Tablets

AHFS DI Essentials™. © Copyright 2024, Selected Revisions June 21, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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