II. Indications
- Type II Diabetes Mellitus
- Close to target (Hemoglobin A1C <8% as monotherapy)
III. Contraindications
- Creatinine Clearance <25 ml/min (or Serum Creatinine >2.0 mg/dl)
- Diabetic Ketoacidosis (DKA)
- Cirrhosis (Acarbose)
- Intestinal disorder
- Inflammatory Bowel Disease
- Colonic ulceration
- Small bowl obstruction history
- Partial Intestinal Obstruction
IV. Mechanism
- Structurally similar to Glucose
- Reversible inhibitor of the enzyme alpha glucosidase
- Present in brush border of Small Intestine
- Alpha glucosidase catalyzes complex Carbohydrates
- Interferes with hydrolysis of Carbohydrates
- Complex Carbohydrates
- Dietary Disaccharides
- Delays absorption of Glucose and other Monosaccharides
- Decreases postprandial Hyperglycemia
- Benefits rely on food within the Intestine at the time of medication dosing
V. Dosing
- Acarbose (Precose)
- Start dose: 25 mg orally three times daily at start of meal
- Maintenance: 50-100 mg orally three times daily ($45/month)
- Miglitol (Glyset)
- Start dose: 25 mg orally three times daily at start of meal
- Maintenance: 50-100 mg orally three times daily ($52/month)
VI. Pharmacokinetics
- Acarbose is not absorbed from Gastrointestinal Tract
- Miglitol is absorbed from Gastrointestinal Tract
- Not metabolized
- Excreted in urine
- Elimination Half-Life: 2 hours
- Excreted in Breast Milk in small amounts
VII. Adverse Effects
- Poorly tolerated
- Decreased GI effects when taken with a high fiber, starchy diet
- Gastrointestinal side effects (unabsorbed Carbohydrate)
- Hepatotoxicity (Acarbose)
- Serum Transaminitis
-
Hypoglycemia
- If used with other Oral Hypoglycemic agent or Insulin
- Use oral Glucose (not sucrose) to treat Hypoglycemia
VIII. Efficacy
- Acarbose associated with cardiovascular benefits
- Reduced cardiovascular events
- Reduced Hypertension risk
- Significant weight loss
- Chiasson (2003) JAMA 290:486-94 [PubMed]
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acarbose (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ACARBOSE 100 MG TABLET | Generic | $0.30 each |
ACARBOSE 25 MG TABLET | Generic | $0.18 each |
ACARBOSE 50 MG TABLET | Generic | $0.22 each |