II. Indications

  1. Type II Diabetes Mellitus
  2. Close to target (Hemoglobin A1C <8% as monotherapy)

III. Contraindications

  1. Creatinine Clearance <25 ml/min (or Serum Creatinine >2.0 mg/dl)
  2. Diabetic Ketoacidosis (DKA)
  3. Cirrhosis (Acarbose specific)
  4. Intestinal disorder
    1. Inflammatory Bowel Disease
    2. Colonic ulceration
    3. Small bowl obstruction history
    4. Partial Intestinal Obstruction

IV. 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

V. Medications

  1. Acarbose (Precose) tablets: 25 mg, 50 mg, 100 mg

VI. Dosing

  1. Start dose: 25 mg orally three times daily at start of meal
    1. May start with 25 mg orally daily if gastrointestinal side effects limit use
  2. Maintenance (after first 4 to 8 weeks)
    1. May increase to 50 to 100 mg orally three times daily
  3. Maximum:
    1. Weight <60 kg: 50 mg three times daily
    2. Weight >60 kg: 100 mg three times daily

VII. Pharmacokinetics

  1. Acarbose is not absorbed from Gastrointestinal Tract (unlike Miglitol)

VIII. 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 specific)
    1. Serum Transaminitis
  4. Hypoglycemia
    1. If used with other Oral Hypoglycemic agent or Insulin
    2. Use oral Glucose (not sucrose) to treat Hypoglycemia

IX. Safety

  1. Pregnancy Category B
  2. Avoid in Lactation

X. 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]

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Related Studies

Cost: Medications

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

Ontology: Acarbose (C0050393)

Definition (NCI) A pseudotetrasaccharide and inhibitor of alpha-glucosidase and pancreatic alpha-amylase with antihyperglycemic activity. Acarbose binds to and inhibits alpha-glucosidase, an enteric enzyme found in the brush border of the small intestines that hydrolyzes oligosaccharides and disaccharides into glucose and other monosaccharides. This prevents the breakdown of larger carbohydrates into glucose and decreases the rise in postprandial blood glucose levels. In addition, acarbose inhibits pancreatic alpha-amylase which hydrolyzes complex starches to oligosaccharides in the small intestines.
Definition (MSH) An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE.
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)
Concepts Pharmacologic Substance (T121) , Carbohydrate (T118)
MSH D020909
SnomedCT 391700000, 386965004, 109077006
LNC LP171383-5
English Acarbose, O-4,6-Dideoxy-4-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-alpha-D-glucopyranosyl-(1-4)-O-alpha-D-glucopyranosyl-(1-4)-D-glucose, acarbose, acarbose (medication), oral hypoglycemics acarbose, ACARBOSE, Acarbose [Chemical/Ingredient], D-glucose, O-4,6-dideoxy-4-(((1S-(1 alpha,4 alpha,5 beta,6 alpha))-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl)amino)-alpha-D-glucopyranosyl-(1-4)-O-alpha-D-glucopyr anosyl-(1-4)-, Acarbose - chemical, Acarbose - chemical (substance), Acarbose (product), Acarbose (substance)
Swedish Akarbos
Finnish Akarboosi
Russian AKARBOZA, АКАРБОЗА
Japanese アカルボース
Polish Akarboza
Czech akarbosa, akarbóza
Spanish acarbosa (producto), acarbosa (sustancia), acarbosa, Acarbosa
French Acarbose
German Acarbose
Italian Acarbosio
Portuguese Acarbose

Ontology: Precose (C0591572)

Concepts Pharmacologic Substance (T121) , Carbohydrate (T118)
MSH D020909
English glucobay, precose, Glucobay, Bayer Brand of Acarbose, Glucor, Prandase, Precose