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Identification
NameAcarbose
Accession NumberDB00284  (APRD00656)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionAn 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)
Structure
Thumb
Synonyms
Acarbosa
Acarbose
Acarbosum
Glucobay
Precose
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acarbosetablet25 mg/1oralAlvogen, Inc.2008-01-30Not applicableUs
Acarbosetablet50 mg/1oralAlvogen, Inc.2008-01-30Not applicableUs
Acarbosetablet100 mg/1oralAlvogen, Inc.2008-01-30Not applicableUs
Glucobaytablet50 mgoralBayer Inc1996-02-02Not applicableCanada
Glucobaytablet100 mgoralBayer Inc1996-02-02Not applicableCanada
Precosetablet25 mg/1oralPhysicians Total Care, Inc.2007-11-19Not applicableUs
Precosetablet50 mg/1oralAphena Pharma Solutions Tennessee, Llc2008-01-30Not applicableUs
Precosetablet50 mg/1oralBayer Health Care Pharmaceuticals Inc.2008-01-30Not applicableUs
Precosetablet100 mg/1oralBayer Health Care Pharmaceuticals Inc.2008-01-30Not applicableUs
Precosetablet25 mg/1oralBayer Health Care Pharmaceuticals Inc.2008-01-30Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acarbosetablet50 mg/1oralMylan Pharmaceuticals Inc.2011-01-06Not applicableUs
Acarbosetablet50 mg/1oralPd Rx Pharmaceuticals, Inc.2008-05-07Not applicableUs
Acarbosetablet25 mg/1oralRoxane Laboratories, Inc2008-05-07Not applicableUs
Acarbosetablet25 mg/1oralAv Kare, Inc.2013-12-24Not applicableUs
Acarbosetablet50 mg/1oralVirtus Pharmaceuticals LLC2013-10-09Not applicableUs
Acarbosetablet100 mg/1oralActavis Pharma, Inc.2008-05-07Not applicableUs
Acarbosetablet25 mg/1oralVirtus Pharmaceuticals LLC2015-02-01Not applicableUs
Acarbosetablet50 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2009-05-14Not applicableUs
Acarbosetablet50 mg/1oralLibertas Pharma, Inc.2011-07-27Not applicableUs
Acarbosetablet100 mg/1oralMylan Pharmaceuticals Inc.2011-01-06Not applicableUs
Acarbosetablet25 mg/1oralStrides Arcolab Limited2011-07-28Not applicableUs
Acarbosetablet50 mg/1oralRoxane Laboratories, Inc2008-05-07Not applicableUs
Acarbosetablet50 mg/1oralAv Kare, Inc.2013-12-24Not applicableUs
Acarbosetablet100 mg/1oralVirtus Pharmaceuticals LLC2013-10-09Not applicableUs
Acarbosetablet25 mg/1oralHeritage Pharmaceuticals Inc.2012-07-30Not applicableUs
Acarbosetablet50 mg/1oralVirtus Pharmaceuticals LLC2015-02-01Not applicableUs
Acarbosetablet100 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2009-05-14Not applicableUs
Acarbosetablet100 mg/1oralLibertas Pharma, Inc.2011-07-27Not applicableUs
Acarbosetablet25 mg/1oralActavis Pharma, Inc.2008-05-07Not applicableUs
Acarbosetablet50 mg/1oralStrides Arcolab Limited2011-07-28Not applicableUs
Acarbosetablet100 mg/1oralRoxane Laboratories, Inc2008-05-07Not applicableUs
Acarbosetablet100 mg/1oralAv Kare, Inc.2013-12-24Not applicableUs
Acarbosetablet100 mg/1oralVirtus Pharmaceuticals LLC2015-02-01Not applicableUs
Acarbosetablet50 mg/1oralHeritage Pharmaceuticals Inc.2012-07-30Not applicableUs
Acarbosetablet25 mg/1oralPhysicians Total Care, Inc.2008-10-03Not applicableUs
Acarbosetablet25 mg/1oralMylan Pharmaceuticals Inc.2011-01-06Not applicableUs
Acarbosetablet50 mg/1oralActavis Pharma, Inc.2008-05-07Not applicableUs
Acarbosetablet100 mg/1oralStrides Arcolab Limited2011-07-28Not applicableUs
Acarbosetablet25 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2009-05-14Not applicableUs
Acarbosetablet25 mg/1oralLibertas Pharma, Inc.2011-07-27Not applicableUs
Acarbosetablet100 mg/1oralHeritage Pharmaceuticals Inc.2012-07-30Not applicableUs
Acarbosetablet25 mg/1oralVirtus Pharmaceuticals LLC2013-10-09Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PrandaseBayer AG
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIT58MSI464G
CAS number56180-94-0
WeightAverage: 645.6048
Monoisotopic: 645.248013577
Chemical FormulaC25H43NO18
InChI KeyInChIKey=XUFXOAAUWZOOIT-JMPDRRIHSA-N
InChI
InChI=1S/C25H43NO18/c1-6-11(26-8-2-7(3-27)12(30)15(33)13(8)31)14(32)19(37)24(40-6)43-22-10(5-29)42-25(20(38)17(22)35)44-21-9(4-28)41-23(39)18(36)16(21)34/h2,6,8-39H,3-5H2,1H3/t6-,8+,9-,10-,11-,12+,13+,14+,15+,16-,17-,18-,19-,20-,21-,22-,23-,24-,25-/m1/s1
IUPAC Name
(2R,3R,4R,5S,6R)-5-{[(2R,3R,4R,5S,6R)-5-{[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-{[(1S,4S,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino}oxan-2-yl]oxy}-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-6-(hydroxymethyl)oxane-2,3,4-triol
SMILES
C[[email protected]]1O[[email protected]](O[C@@H]2[C@@H](CO)O[[email protected]](O[C@@H]3[C@@H](CO)O[C@@H](O)[[email protected]](O)[[email protected]]3O)[[email protected]](O)[[email protected]]2O)[[email protected]](O)[C@@H](O)[C@@H]1N[[email protected]]1C=C(CO)[[email protected]](O)[[email protected]](O)[[email protected]]1O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as oligosaccharides. These are carbohydrates made up of 3 to 10 monosaccharide units linked to each other through glycosidic bonds.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassCarbohydrates and carbohydrate conjugates
Sub ClassOligosaccharides
Direct ParentOligosaccharides
Alternative Parents
Substituents
  • Oligosaccharide
  • Glucosamine
  • O-glycosyl compound
  • Glycosyl compound
  • Cyclitol derivative
  • Amino saccharide
  • Oxane
  • Secondary alcohol
  • Polyol
  • Hemiacetal
  • 1,2-diol
  • 1,2-aminoalcohol
  • Oxacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Secondary aliphatic amine
  • Acetal
  • Hydrocarbon derivative
  • Primary alcohol
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor treatment and management of diabetes type II (used in combination therapy as a second or third line agent)
PharmacodynamicsUsed to reduce blood gluose in patients with type 2 diabetes. Acarbose is a complex oligosaccharide that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. Acarbose binds to and inhibits alpha amylase and alpha-gluocside hydrolases. In diabetic patients, this enzyme inhibition results in a delayed glucose absorption and a lowering of postprandial hyperglycemia.
Mechanism of actionAcarbose reversibly bind to pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolases. These enzymes inhibit hydrolysis of complex starches to oligosaccharides in the lumen of the small intestine and hydrolysis of oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine.
Related Articles
AbsorptionExtremely low bioavailability. Less than 2% of an oral dose of acarbose was absorbed as active drug. Peak plasma concentrations of the active drug were achieved 1 hour after dosing. Drug accumulation does not occur with multiple doses.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Acarbose is only metabolized within the gastrointestinal tract by intestinal bacteria and also digestive enzymes to a lesser extent. 4-methylpyrogallol derivatives (sulfate, methyl, and glucuronide conjugates) are the major metabolites. One metabolite (formed by cleavage of a glucose molecule from acarbose) also has alpha-glucosidase inhibitory activity.

Route of eliminationThe fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. A fraction of the metabolites (approximately 34% of the dose) was absorbed and subsequently excreted in the urine. The active metabolite is excreted into the urine and accounts for less than 2% of the total administered dose. When given intravenously, 89% of the dose was excreted into the urine as the active drug. When given orally, less than 2% of the oral dose was recovered into the urine as active (parent compound and active metabolite) drug.
Half lifeHealthy volunteers = 2 hours
ClearanceNot Available
ToxicityGastrointestinal symptoms are the most common reactions to acarbose.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8467
Blood Brain Barrier-0.9723
Caco-2 permeable-0.725
P-glycoprotein substrateSubstrate0.5316
P-glycoprotein inhibitor IInhibitor0.5421
P-glycoprotein inhibitor IINon-inhibitor0.8656
Renal organic cation transporterNon-inhibitor0.8647
CYP450 2C9 substrateNon-substrate0.7581
CYP450 2D6 substrateNon-substrate0.8505
CYP450 3A4 substrateNon-substrate0.5683
CYP450 1A2 substrateNon-inhibitor0.8791
CYP450 2C9 inhibitorNon-inhibitor0.8677
CYP450 2D6 inhibitorNon-inhibitor0.8974
CYP450 2C19 inhibitorNon-inhibitor0.8392
CYP450 3A4 inhibitorNon-inhibitor0.986
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7163
Ames testNon AMES toxic0.8054
CarcinogenicityNon-carcinogens0.967
BiodegradationNot ready biodegradable0.6447
Rat acute toxicity1.4610 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8586
hERG inhibition (predictor II)Non-inhibitor0.8288
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Impax laboratories inc
  • Roxane laboratories inc
  • Watson laboratories inc
  • Bayer healthcare pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg/1
Tabletoral25 mg/1
Tabletoral50 mg/1
Tabletoral100 mg
Tabletoral50 mg
Prices
Unit descriptionCostUnit
Acarbose 100 100 mg tablet Bottle120.62USD bottle
Acarbose 100 50 mg tablet Bottle100.71USD bottle
Acarbose 100 25 mg tablet Bottle93.54USD bottle
Precose 100 mg tablet1.28USD tablet
Acarbose 100 mg tablet1.17USD tablet
Precose 50 mg tablet1.11USD tablet
Precose 25 mg tablet1.01USD tablet
Acarbose 25 mg tablet0.91USD tablet
Acarbose 50 mg tablet0.88USD tablet
Glucobay 100 mg Tablet0.4USD tablet
Glucobay 50 mg Tablet0.29USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP-6.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility148.0 mg/mLALOGPS
logP-2.7ALOGPS
logP-7.6ChemAxon
logS-0.64ALOGPS
pKa (Strongest Acidic)11.23ChemAxon
pKa (Strongest Basic)7.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count19ChemAxon
Hydrogen Donor Count14ChemAxon
Polar Surface Area321.17 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity137.6 m3·mol-1ChemAxon
Polarizability62.39 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Anneliese Crueger, Wolfgang Piepersberg, Jurgen Distler, Ansgar Stratmann, “Acarbose biosynthesis genes from actinoplanes sp., process for the isolation thereof and the use thereof.” U.S. Patent US5753501, issued December, 1977.

US5753501
General References
  1. Clissold SP, Edwards C: Acarbose. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs. 1988 Mar;35(3):214-43. [PubMed:3286212 ]
External Links
ATC CodesA10BD17A10BF01
AHFS Codes
  • 68:20.02
PDB EntriesNot Available
FDA labelDownload (268 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Acarbose.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Acarbose.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Acarbose.
AmoxapineAmoxapine may increase the hypoglycemic activities of Acarbose.
AripiprazoleThe therapeutic efficacy of Acarbose can be decreased when used in combination with Aripiprazole.
Arsenic trioxideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Atazanavir.
BendroflumethiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Bendroflumethiazide.
BenmoxinBenmoxin may increase the hypoglycemic activities of Acarbose.
BetamethasoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Betamethasone.
BrexpiprazoleThe therapeutic efficacy of Acarbose can be decreased when used in combination with Brexpiprazole.
BumetanideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Bumetanide.
BuserelinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Buserelin.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Acarbose.
CeritinibThe therapeutic efficacy of Acarbose can be decreased when used in combination with Ceritinib.
ChlorothiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Chlorothiazide.
ChlorpropamideAcarbose may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Chlorthalidone.
CitalopramCitalopram may increase the hypoglycemic activities of Acarbose.
ClomipramineClomipramine may increase the hypoglycemic activities of Acarbose.
ClozapineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Clozapine.
CorticotropinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Cortisone acetate.
Cyproterone acetateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Acarbose can be decreased when used in combination with Dabrafenib.
DanazolThe therapeutic efficacy of Acarbose can be decreased when used in combination with Danazol.
DapoxetineDapoxetine may increase the hypoglycemic activities of Acarbose.
DarunavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Darunavir.
DesogestrelThe therapeutic efficacy of Acarbose can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Dexamethasone.
DiazoxideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Diazoxide.
DienogestThe therapeutic efficacy of Acarbose can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the hypoglycemic activities of Acarbose.
DigoxinThe serum concentration of Digoxin can be decreased when it is combined with Acarbose.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Acarbose.
DisopyramideAcarbose may increase the hypoglycemic activities of Disopyramide.
DrospirenoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Drospirenone.
EpinephrineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Epinephrine.
EscitalopramEscitalopram may increase the hypoglycemic activities of Acarbose.
EstradiolThe therapeutic efficacy of Acarbose can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Acarbose can be decreased when used in combination with Etacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Acarbose can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Acarbose can be decreased when used in combination with Etonogestrel.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Acarbose.
EverolimusThe therapeutic efficacy of Acarbose can be decreased when used in combination with Everolimus.
FenfluramineFenfluramine may increase the hypoglycemic activities of Acarbose.
FludrocortisoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Fludrocortisone.
FluoxetineFluoxetine may increase the hypoglycemic activities of Acarbose.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Acarbose.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Acarbose.
FosamprenavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Fosamprenavir.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Acarbose.
FurosemideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Furosemide.
GliclazideAcarbose may increase the hypoglycemic activities of Gliclazide.
GlimepirideAcarbose may increase the hypoglycemic activities of Glimepiride.
GlipizideAcarbose may increase the hypoglycemic activities of Glipizide.
GlyburideAcarbose may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.
HistrelinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Histrelin.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Acarbose.
HydrochlorothiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Iloperidone.
IndalpineIndalpine may increase the hypoglycemic activities of Acarbose.
IndapamideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Indinavir.
Insulin AspartAcarbose may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirAcarbose may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineAcarbose may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineAcarbose may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanAcarbose may increase the hypoglycemic activities of Insulin Human.
Insulin LisproAcarbose may increase the hypoglycemic activities of Insulin Lispro.
IproclozideIproclozide may increase the hypoglycemic activities of Acarbose.
IproniazidIproniazid may increase the hypoglycemic activities of Acarbose.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Acarbose.
LanreotideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Lanreotide.
LanreotideAcarbose may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Acarbose.
LevonorgestrelThe therapeutic efficacy of Acarbose can be decreased when used in combination with Levonorgestrel.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Acarbose.
LopinavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Lopinavir.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Acarbose.
LurasidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Lurasidone.
MebanazineMebanazine may increase the hypoglycemic activities of Acarbose.
MecaserminAcarbose may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Medroxyprogesterone acetate.
Megestrol acetateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Megestrol acetate.
MesalazineMesalazine may increase the hypoglycemic activities of Acarbose.
MestranolThe therapeutic efficacy of Acarbose can be decreased when used in combination with Mestranol.
MethotrimeprazineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Methyclothiazide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Acarbose.
MethylprednisoloneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Methylprednisolone.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Acarbose.
MetolazoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Metolazone.
MifepristoneAcarbose may increase the hypoglycemic activities of Mifepristone.
MilnacipranMilnacipran may increase the hypoglycemic activities of Acarbose.
MinaprineMinaprine may increase the hypoglycemic activities of Acarbose.
MoclobemideMoclobemide may increase the hypoglycemic activities of Acarbose.
NateglinideAcarbose may increase the hypoglycemic activities of Nateglinide.
NelfinavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Nelfinavir.
NeomycinThe risk or severity of adverse effects can be increased when Neomycin is combined with Acarbose.
NiacinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Niacin.
NialamideNialamide may increase the hypoglycemic activities of Acarbose.
NilotinibThe therapeutic efficacy of Acarbose can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Acarbose can be decreased when used in combination with Norgestimate.
OctamoxinOctamoxin may increase the hypoglycemic activities of Acarbose.
OctreotideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Octreotide.
OctreotideAcarbose may increase the hypoglycemic activities of Octreotide.
OlanzapineOlanzapine may increase the hypoglycemic activities of Acarbose.
OxandroloneOxandrolone may increase the hypoglycemic activities of Acarbose.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Acarbose.
PaliperidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Paliperidone.
PargylinePargyline may increase the hypoglycemic activities of Acarbose.
ParoxetineParoxetine may increase the hypoglycemic activities of Acarbose.
PasireotideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.
PasireotideAcarbose may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Acarbose.
PentamidineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Pentamidine.
PentamidineAcarbose may increase the hypoglycemic activities of Pentamidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Acarbose.
PheniprazinePheniprazine may increase the hypoglycemic activities of Acarbose.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Acarbose.
PiperazineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Pipotiazine.
PirlindolePirlindole may increase the hypoglycemic activities of Acarbose.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Acarbose.
PolythiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Polythiazide.
PrednisoloneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Prednisone.
ProgesteroneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Progesterone.
QuetiapineThe therapeutic efficacy of Acarbose can be decreased when used in combination with Quetiapine.
QuinethazoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Quinethazone.
QuinineAcarbose may increase the hypoglycemic activities of Quinine.
RasagilineRasagiline may increase the hypoglycemic activities of Acarbose.
RepaglinideAcarbose may increase the hypoglycemic activities of Repaglinide.
RisperidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Ritonavir.
SafrazineSafrazine may increase the hypoglycemic activities of Acarbose.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Acarbose.
SaquinavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Saquinavir.
SelegilineSelegiline may increase the hypoglycemic activities of Acarbose.
SertralineSertraline may increase the hypoglycemic activities of Acarbose.
SirolimusThe therapeutic efficacy of Acarbose can be decreased when used in combination with Sirolimus.
StanozololStanozolol may increase the hypoglycemic activities of Acarbose.
SulfadiazineAcarbose may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleAcarbose may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleAcarbose may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibAcarbose may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Acarbose can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Acarbose can be decreased when used in combination with Temsirolimus.
TestosteroneTestosterone may increase the hypoglycemic activities of Acarbose.
TipranavirThe therapeutic efficacy of Acarbose can be decreased when used in combination with Tipranavir.
TolazamideAcarbose may increase the hypoglycemic activities of Tolazamide.
TolbutamideAcarbose may increase the hypoglycemic activities of Tolbutamide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Acarbose.
TorasemideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Torasemide.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Acarbose.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Acarbose.
TrazodoneTrazodone may increase the hypoglycemic activities of Acarbose.
TriamcinoloneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Triamcinolone.
TrichlormethiazideThe therapeutic efficacy of Acarbose can be decreased when used in combination with Trichlormethiazide.
TriptorelinThe therapeutic efficacy of Acarbose can be decreased when used in combination with Triptorelin.
VilazodoneVilazodone may increase the hypoglycemic activities of Acarbose.
VorinostatThe therapeutic efficacy of Acarbose can be decreased when used in combination with Vorinostat.
VortioxetineVortioxetine may increase the hypoglycemic activities of Acarbose.
ZimelidineZimelidine may increase the hypoglycemic activities of Acarbose.
ZiprasidoneThe therapeutic efficacy of Acarbose can be decreased when used in combination with Ziprasidone.
Food Interactions
  • Take with food, at beginning of each meal.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Maltose alpha-glucosidase activity
Specific Function:
May serve as an alternate pathway for starch digestion when luminal alpha-amylase activity is reduced because of immaturity or malnutrition. May play a unique role in the digestion of malted dietary oligosaccharides used in food manufacturing.
Gene Name:
MGAM
Uniprot ID:
O43451
Molecular Weight:
209850.8 Da
References
  1. Okumiya T, Keulemans JL, Kroos MA, Van der Beek NM, Boer MA, Takeuchi H, Van Diggelen OP, Reuser AJ: A new diagnostic assay for glycogen storage disease type II in mixed leukocytes. Mol Genet Metab. 2006 May;88(1):22-8. Epub 2005 Dec 15. [PubMed:16359900 ]
  2. Zhang H, Kallwass H, Young SP, Carr C, Dai J, Kishnani PS, Millington DS, Keutzer J, Chen YT, Bali D: Comparison of maltose and acarbose as inhibitors of maltase-glucoamylase activity in assaying acid alpha-glucosidase activity in dried blood spots for the diagnosis of infantile Pompe disease. Genet Med. 2006 May;8(5):302-6. [PubMed:16702880 ]
  3. Gelb MH, Turecek F, Scott CR, Chamoles NA: Direct multiplex assay of enzymes in dried blood spots by tandem mass spectrometry for the newborn screening of lysosomal storage disorders. J Inherit Metab Dis. 2006 Apr-Jun;29(2-3):397-404. [PubMed:16763908 ]
  4. Yamagishi S, Matsui T, Ueda S, Fukami K, Okuda S: Clinical utility of acarbose, an alpha-glucosidase inhibitor in cardiometabolic disorders. Curr Drug Metab. 2009 Feb;10(2):159-63. [PubMed:19275550 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Maltose alpha-glucosidase activity
Specific Function:
Essential for the degradation of glygogen to glucose in lysosomes.
Gene Name:
GAA
Uniprot ID:
P10253
Molecular Weight:
105322.935 Da
References
  1. Salehi A, Fan BG, Ekelund M, Nordin G, Lundquist I: TPN-evoked dysfunction of islet lysosomal activity mediates impairment of glucose-stimulated insulin release. Am J Physiol Endocrinol Metab. 2001 Jul;281(1):E171-9. [PubMed:11404235 ]
  2. Li Y, Scott CR, Chamoles NA, Ghavami A, Pinto BM, Turecek F, Gelb MH: Direct multiplex assay of lysosomal enzymes in dried blood spots for newborn screening. Clin Chem. 2004 Oct;50(10):1785-96. Epub 2004 Aug 3. [PubMed:15292070 ]
  3. Lundquist I, Panagiotidis G: The relationship of islet amyloglucosidase activity and glucose-induced insulin secretion. Pancreas. 1992;7(3):352-7. [PubMed:1594557 ]
  4. Zhang H, Kallwass H, Young SP, Carr C, Dai J, Kishnani PS, Millington DS, Keutzer J, Chen YT, Bali D: Comparison of maltose and acarbose as inhibitors of maltase-glucoamylase activity in assaying acid alpha-glucosidase activity in dried blood spots for the diagnosis of infantile Pompe disease. Genet Med. 2006 May;8(5):302-6. [PubMed:16702880 ]
  5. Gelb MH, Turecek F, Scott CR, Chamoles NA: Direct multiplex assay of enzymes in dried blood spots by tandem mass spectrometry for the newborn screening of lysosomal storage disorders. J Inherit Metab Dis. 2006 Apr-Jun;29(2-3):397-404. [PubMed:16763908 ]
  6. Lullmann-Rauch R, Watermann D: Fusion of storage lysosomes in experimental lipidosis and glycogenosis. Exp Mol Pathol. 1987 Feb;46(1):136-43. [PubMed:3467980 ]
  7. Bourbon JR, Doucet E, Rieutort M: Role of alpha-glucosidase in fetal lung maturation. Biochim Biophys Acta. 1987 Jan 13;917(1):203-10. [PubMed:3539207 ]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Sucrose alpha-glucosidase activity
Specific Function:
Plays an important role in the final stage of carbohydrate digestion. Isomaltase activity is specific for both alpha-1,4- and alpha-1,6-oligosaccharides.
Gene Name:
SI
Uniprot ID:
P14410
Molecular Weight:
209451.49 Da
References
  1. Juretic D, Bernik S, Cop L, Hadzija M, Petlevski R, Lukac-Bajalo J: Short-term effect of acarbose on specific intestinal disaccharidase activities and hyperglycaemia in CBA diabetic mice. J Anim Physiol Anim Nutr (Berl). 2003 Aug;87(7-8):263-8. [PubMed:12864906 ]
  2. Meyer H, Wieczorek H, Zeiske W: K+ transport in the caterpillar intestine epithelium: role of osmolytes for the K+-secretory capacity of the tobacco hornworm midgut. J Comp Physiol B. 2004 Oct;174(7):527-39. Epub 2004 Aug 20. [PubMed:15322845 ]
  3. Karley AJ, Ashford DA, Minto LM, Pritchard J, Douglas AE: The significance of gut sucrase activity for osmoregulation in the pea aphid, Acyrthosiphon pisum. J Insect Physiol. 2005 Dec;51(12):1313-9. Epub 2005 Sep 15. [PubMed:16169004 ]
  4. Samulitis BK, Goda T, Lee SM, Koldovsky O: Inhibitory mechanism of acarbose and 1-deoxynojirimycin derivatives on carbohydrases in rat small intestine. Drugs Exp Clin Res. 1987;13(8):517-24. [PubMed:2962844 ]
  5. Newbrun E, Hoover CI, Walker GJ: Inhibition by acarbose, nojirimycin and 1-deoxynojirimycin of glucosyltransferase produced by oral streptococci. Arch Oral Biol. 1983;28(6):531-6. [PubMed:6226260 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Chloride ion binding
Specific Function:
Not Available
Gene Name:
AMY2A
Uniprot ID:
P04746
Molecular Weight:
57706.51 Da
References
  1. Jonas L, Mikkat U, Lehmann R, Schareck W, Walzel H, Schroder W, Lopp H, Pussa T, Toomik P: Inhibitory effects of human and porcine alpha-amylase on CCK-8-stimulated lipase secretion of isolated rat pancreatic acini. Pancreatology. 2003;3(4):342-8. [PubMed:12890998 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23