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acarbose
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(ah KAR bose)

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.

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.

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.

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.

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.

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 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).
  • 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. (Plasma glucose concentrations generally 10–15% higher than those in whole blood and may vary according to method and laboratory used.) During therapy initiation and dosage titration, obtain 1-hour postprandial glucose concentration to determine therapeutic response and minimum effective dosage. Monitor HbA1c values at approximately every 3 months to evaluate long-term glycemic control. Monitor glucose concentrations 1–2 hours after the start of a meal in those who have elevated HbA1c despite adequate preprandial glucose concentrations.

Administration

Oral Administration

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

Dosage

Adults

Diabetes Mellitus

Oral

Initially, 25 mg 3 times daily at the beginning of each main meal. 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). 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

Diabetes Mellitus

Oral

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

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

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