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Alpha-Glucosidase Inhibitor

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Alpha-Glucosidase Inhibitor

  • See Also
  1. Oral Hypoglycemic Agents
  2. Acarbose
  3. Miglitol
  • Indications
  1. Type II Diabetes Mellitus
  2. Close to target (Hemoglobin A1C <8% as monotherapy)
  • Contraindications
  1. Creatinine Clearance <25 ml/min (or Serum Creatinine >2.0 mg/dl)
  2. Diabetic Ketoacidosis (DKA)
  3. Cirrhosis (Acarbose)
  4. Intestinal disorder
    1. Inflammatory Bowel Disease
    2. Colonic ulceration
    3. Small bowl obstruction history
    4. Partial Intestinal Obstruction
  • Mechanism
  1. Structurally similar to Glucose
  2. Reversible inhibitor of the enzyme alpha glucosidase
    1. Present in brush border of Small Intestine
    2. Alpha glucosidase catalyzes complex Carbohydrates
  3. Interferes with hydrolysis of Carbohydrates
    1. Complex Carbohydrates
    2. Dietary Disaccharides
  4. Delays absorption of Glucose and other Monosaccharides
    1. Decreases postprandial Hyperglycemia
    2. Benefits rely on food within the Intestine at the time of medication dosing
  • Dosing
  1. Acarbose (Precose)
    1. Start dose: 25 mg orally three times daily at start of meal
    2. Maintenance: 50-100 mg orally three times daily
  2. Miglitol (Glyset)
    1. Start dose: 25 mg orally three times daily at start of meal
    2. Maintenance: 50-100 mg orally three times daily
  • Pharmacokinetics
  1. Acarbose is not absorbed from Gastrointestinal Tract
  2. Miglitol is absorbed from Gastrointestinal Tract
    1. Not metabolized
    2. Excreted in urine
    3. Elimination Half-Life: 2 hours
    4. Excreted in Breast Milk in small amounts
  • Adverse Effects
  1. Poorly tolerated
    1. Decreased GI effects when taken with a high fiber, starchy diet
  2. Gastrointestinal side effects (unabsorbed Carbohydrate)
    1. Abdominal Pain
    2. Abdominal Bloating
    3. Diarrhea
    4. Flatulence
  3. Hepatotoxicity (Acarbose)
    1. Serum Transaminitis
  4. Hypoglycemia
    1. If used with other Oral Hypoglycemic agent or Insulin
    2. Use oral Glucose (not sucrose) to treat Hypoglycemia
  • Safety
  1. Pregnancy Category B
  2. Avoid in Lactation
  • Efficacy
  1. Acarbose associated with cardiovascular benefits
    1. Reduced cardiovascular events
    2. Reduced Hypertension risk
    3. Significant weight loss
    4. Chiasson (2003) JAMA 290:486-94 [PubMed]
  • References
  1. (1999) Med Lett Drugs Ther, 41(1053):49-50 [PubMed]
  2. Chiasson (1994) Ann Intern Med 121:928-35 [PubMed]
  3. Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]