Endocrinology Book

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Alpha-glucosidase Inhibitor

Aka: Alpha-glucosidase Inhibitor, 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 290:486-94
  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):49-50
    2. Chiasson (1994) Ann Intern Med 121:928-35
Medication Costs
Acarbose (on 2/9/2012 at DrugStore.com)
Acarbose 100 25mg Tablets Bottle #1 for $81.99 ($81.99/unit)
Acarbose 100 50mg Tablets Bottle #1 for $87.99 ($87.99/unit)
Acarbose 100 100mg Tablets Bottle #1 for $89.99 ($89.99/unit)
Precose (on 2/9/2012 at DrugStore.com)
Precose 25mg Tablets #90 for $85.51 ($0.95/unit)
Precose 50mg Tablets #30 for $36.99 ($1.23/unit)
Precose 100mg Tablets #90 for $109.99 ($1.22/unit)
Glyset (on 2/9/2012 at DrugStore.com)
Glyset 25mg Tablets #90 for $111.99 ($1.24/unit)
Glyset 50mg Tablets #90 for $120.00 ($1.33/unit)
Glyset 100mg Tablets #90 for $125.99 ($1.40/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

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.
Concepts Carbohydrate (T118) , Pharmacologic Substance (T121)
MSH D020909
SnomedCT 391700000, 109077006, 386965004
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 - chemical (substance), 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 (product), Acarbose (substance), Acarbose - chemical
Swedish Akarbos
Czech akarbosa
Spanish Acarbose - chemical, acarbosa (producto), acarbosa (sustancia), acarbosa, Acarbosa
Finnish Akarboosi
Russian AKARBOZA, АКАРБОЗА
Japanese アカルボース
Polish Akarboza
French Acarbose
German Acarbose
Italian Acarbosio
Portuguese Acarbose
Sources
Derived from the NIH UMLS (Unified Medical Language System)


miglitol (C0066535)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C045621
SnomedCT 386046009, 109071007
English miglitol, N-hydroxyethyl-1-desoxynojirimycin, N-hydroxyethyl-1-desoxy-nojirimycin, miglitol (medication), miglitol [Chemical/Ingredient], Miglitol (product), Miglitol (substance), Miglitol, MIGLITOL
Spanish miglitol (producto), miglitol (sustancia), miglitol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Precose (C0591572)

Concepts Carbohydrate (T118) , Pharmacologic Substance (T121)
MSH D020909
English glucobay, precose, Glucobay, Bayer Brand of Acarbose, Glucor, Prandase, Precose
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Glyset (C0720692)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C045621
English Glyset, glyset
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Alpha-glucoside inhibitor (C1299007)

Concepts Pharmacologic Substance (T121)
SnomedCT 109072000, 372565001
English Alpha-glucoside inhibitor, alpha glucosidase inhibitor, alpha glucosidase inhibitors, alpha glucoside inhibitors, alpha-glucosidase inhibitor, alpha glucosides inhibitors, Alpha-glucosidase inhibitor, Alpha-glucoside inhibitor (product), Alpha-glucoside inhibitor (substance), Alpha Glucosidase Inhibitors
Spanish inhibidor de alfa glucósido (sustancia), inhibidor de alfa glucósido, inhibidor de alfaglucosidasa (producto), inhibidor de alfaglucosidasa, inhibidor de alfaglucósido (producto), inhibidor de alfaglucósido (sustancia), inhibidor de alfaglucósido
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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