Alpha-glucosidase Inhibitor

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

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II. Indications

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

III. Contraindications

  1. Diabetic Ketoacidosis (DKA)
  2. Intestinal disorder
    1. Inflammatory Bowel Disease
    2. Colonic ulceration
    3. Partial Intestinal Obstruction

IV. 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

V. 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

VI. 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

VII. 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]

VIII. 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)

IX. References

  1. (1999) Med Lett Drugs Ther, 41(1053):49-50 [PubMed]
  2. Chiasson (1994) Ann Intern Med 121:928-35 [PubMed]

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Cost: Medications

acarbose (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ACARBOSE 100 MG TABLET Generic $0.25 each
ACARBOSE 25 MG TABLET Generic $0.20 each
ACARBOSE 50 MG TABLET Generic $0.23 each
glyset (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
GLYSET 100 MG TABLET $3.16 each
GLYSET 25 MG TABLET $2.48 each
GLYSET 50 MG TABLET $2.70 each
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.

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
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: miglitol (C0066535)

Definition (NCI) A desoxynojirimycin derivative and inhibitor of alpha-glucosidase with antihyperglycemic activity. Miglitol 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. Compared to acarbose, miglitol is systemically absorbed.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045621
SnomedCT 386046009, 109071007
English miglitol, N-hydroxyethyl-1-desoxynojirimycin, N-hydroxyethyl-1-desoxy-nojirimycin, miglitol (medication), miglitol [Chemical/Ingredient], MIGLITOL, Miglitol (product), Miglitol (substance), Miglitol
Spanish miglitol (producto), miglitol (sustancia), miglitol
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Precose (C0591572)

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

Ontology: Glyset (C0720692)

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

Ontology: alpha-Glucosidase Inhibitors (C1299007)

Definition (MSH) Compounds that inhibit ALPHA-GLUCOSIDASE.
Concepts Pharmacologic Substance (T121)
MSH D065089
SnomedCT 109072000, 372565001
English alpha glucosidase inhibitor, alpha glucosidase inhibitors, alpha glucoside inhibitors, alpha-glucosidase inhibitor, alpha glucosides inhibitors, Inhibitors, alpha-Glucosidase, alpha Glucosidase Inhibitors, alpha-Glucosidase Inhibitors, Alpha-glucosidase inhibitor, Alpha-glucoside inhibitor (product), Alpha-glucoside inhibitor (substance), Alpha-glucoside inhibitor, 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
Derived from the NIH UMLS (Unified Medical Language System)

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