Endocrinology Book

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Alpha-glucosidase inhibitorAka: Acarbose, Precose, Miglitol, Glyset

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  1. See Also
    1. Oral Hypoglycemic Agents
  2. Indications
    1. Type II Diabetes Mellitus
    2. Close to target (Hemoglobin A1C <8% as monotherapy)
  3. Contraindications
    1. Diabetic Ketoacidosis (DKA)
    2. Intestinal disorder
      1. Inflammatory Bowel Disease
      2. Colonic Ulceration
      3. Partial Intestinal Obstruction
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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)
  9. References
    1. (1999) Med Lett Drugs Ther 41(1053):49
    2. Chiasson (1994) Ann Intern Med 121:928

Acarbose (C0050393)

Definition (MSH)An inhibitor of alpha glucosidase that retards the digestion and absorption of carbohydrates in the small intestine and hence reduces the increase in blood-glucose concentrations after a carbohydrate load. It is given orally to non-insulin dependent diabetes mellitus patients where diet modification or oral hypoglycemic agents do not control their condition. (From Martindale The Extra Pharmacopoeia, 31st ed)
Definition (PDQ)A complex oligosaccharide used as a hypoglycemic agent in diabetes management. Acarbose inhibits enzymes required in catabolism of carbohydrates, specifically pancreatic alpha-amylase, which hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, and the membrane-bound intestinal alpha-glucosidases, which hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. When acarbose is orally administered, less digestion of complex carbohydrates occur and less glucose is absorbed in the small intestine, thereby producing a smaller rise in postprandial blood glucose levels after a carbohydrate load. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42140&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42140&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C983" NCI Thesaurus)
Definition (NCI)A complex oligosaccharide used as a hypoglycemic agent in diabetes management. Acarbose inhibits enzymes required in catabolism of carbohydrates, specifically pancreatic alpha-amylase, which hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, and the membrane-bound intestinal alpha-glucosidases, which hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. When acarbose is orally administered, less digestion of complex carbohydrates occur and less glucose is absorbed in the small intestine, thereby producing a smaller rise in postprandial blood glucose levels after a carbohydrate load.
ConceptsCarbohydrate (T118) , Pharmacologic Substance (T121)
EnglishAcarbose, ACARBOSE PREPARATION
Spanishacarbosa
CreditsDerived from the NIH UMLS (Unified Medical Language System)


miglitol (C0066535)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishmiglitol, MIGLITOL PREPARATION
Spanishmiglitol
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Precose (C0591572)

ConceptsCarbohydrate (T118) , Pharmacologic Substance (T121)
EnglishBayer Brand of Acarbose, Glucobay, Glucor, Prandase, Precose
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Glyset (C0720692)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishGlyset
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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