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Alpha-glucosidase Inhibitor

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Alpha-glucosidase Inhibitor, Acarbose, Precose, Miglitol, Glyset

  • See Also
  1. Oral Hypoglycemic Agents
  • Indications
  1. Type II Diabetes Mellitus
  2. Close to target (Hemoglobin A1C <8% as monotherapy)
  • Contraindications
  1. Diabetic Ketoacidosis (DKA)
  2. Intestinal disorder
    1. Inflammatory Bowel Disease
    2. Colonic ulceration
    3. Partial Intestinal Obstruction
  • Mechanism
  1. Structurally similar to Glucose
  2. Reversible inhibitor of alpha glucosidase
    1. Present in brush border of Small Intestine
  3. Interferes with hydrolysis of Carbohydrates
    1. Complex Carbohydrates
    2. Dietary Disaccharides
  4. Delays absorption of Glucose and other Monosaccharides
  • 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
  2. Gastrointestinal side effects (unabsorbed Carbohydrate)
    1. Abdominal Pain
    2. Diarrhea
    3. Flatulence
  3. Hypoglycemia
    1. If used with other Oral Hypoglycemic agent or Insulin
    2. Use oral Glucose (not sucrose) to treat Hypoglycemia
  • 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]
  • Dosages
  1. Acarbose (Precose)
    1. Start dose: 25 mg PO tid at start of meal
    2. Maintenance: 50-100 mg PO tid ($45/month)
  2. Miglitol (Glyset)
    1. Start dose: 25 mg PO tid at start of meal
    2. Maintenance: 50-100 mg PO tid ($52/month)
  • References
  1. (1999) Med Lett Drugs Ther, 41(1053):49-50 [PubMed]
  2. Chiasson (1994) Ann Intern Med 121:928-35 [PubMed]