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
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. Safety
- Pregnancy Category B
- Avoid in Lactation
IX. Efficacy
-
Acarbose associated with cardiovascular benefits
- Reduced cardiovascular events
- Reduced Hypertension risk
- Significant weight loss
- Chiasson (2003) JAMA 290:486-94 [PubMed]