acarbose Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
39 56180-94-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • acarbose
  • ascarbose
  • glucobay
  • prandase
  • precose
An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE.
  • Molecular weight: 645.61
  • Formula: C25H43NO18
  • CLOGP: -6.66
  • LIPINSKI: 3
  • HAC: 19
  • HDO: 14
  • TPSA: 321.17
  • ALOGS: -0.64
  • ROTB: 9

Drug dosage:

DoseUnitRoute
0.30 g O

Approvals:

DateAgencyCompanyOrphan
Sept. 6, 1995 FDA BAYER HLTHCARE

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 648.50 54.83 136 620 18273 4619963
Hypoglycaemic coma 284.82 54.83 45 711 1150 4637086
Lactic acidosis 191.60 54.83 47 709 11909 4626327
Pneumatosis intestinalis 159.66 54.83 27 729 1047 4637189
Acute kidney injury 116.35 54.83 49 707 70382 4567854
Diarrhoea 99.94 54.83 56 700 150129 4488107
Abdominal distension 83.98 54.83 27 729 17962 4620274
Hyperkalaemia 70.73 54.83 23 733 15814 4622422
Portal venous gas 60.19 54.83 9 747 154 4638082
Hemiparesis 57.50 54.83 16 740 6468 4631768
Diabetes mellitus inadequate control 55.12 54.83 14 742 3995 4634241

Pharmacologic Action:

SourceCodeDescription
ATC A10BD17 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BF01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Alpha glucosidase inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065089 Glycoside Hydrolase Inhibitors
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:35526 hypoglycemic agent
FDA MoA N0000000166 alpha Glucosidase Inhibitors
FDA EPC N0000175559 alpha-Glucosidase Inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Cirrhosis of liver contraindication 19943007 DOID:5082
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Ulceration of colon contraindication 46040000
Kidney disease contraindication 90708001 DOID:557
Gastrointestinal obstruction contraindication 126765001
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Surgical procedure contraindication 387713003
Traumatic injury contraindication 417746004
Fever greater than 100.4 Fahrenheit contraindication 426000000
Malabsorption States contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.57 acidic
pKa2 11.95 acidic
pKa3 12.57 acidic
pKa4 13.14 acidic
pKa5 13.89 acidic
pKa6 6.99 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Maltase-glucoamylase, intestinal Enzyme INHIBITOR IC50 5.70 WOMBAT-PK CHEMBL
Pancreatic alpha-amylase Enzyme INHIBITOR CHEMBL CHEMBL
Lysosomal alpha-glucosidase Enzyme IC50 5.30 CHEMBL
Alpha-amylase 1 Enzyme IC50 6 CHEMBL
Sucrase-isomaltase, intestinal Enzyme Ki 6.61 SCIENTIFIC LITERATURE
Oligo-1,6-glucosidase Unclassified IC50 4.42 CHEMBL
Lysosomal alpha-glucosidase Enzyme Ki 5.46 CHEMBL
Alpha-amylase Enzyme Ki 6.47 CHEMBL
Sucrase-isomaltase, intestinal Enzyme IC50 6.40 CHEMBL
Pancreatic alpha-amylase Unclassified IC50 4.45 CHEMBL

External reference:

IDSource
4020940 VUID
N0000148420 NUI
C0050393 UMLSCUI
D00216 KEGG_DRUG
109077006 SNOMEDCT_US
4020940 VANDF
136765 MMSL
16681 RXNORM
386965004 SNOMEDCT_US
4117 MMSL
d03846 MMSL
004299 NDDF
CHEMBL404271 ChEMBL_ID
DB00284 DRUGBANK_ID
CHEMBL1566 ChEMBL_ID
T58MSI464G UNII
4527 INN_ID
CHEBI:2376 CHEBI
6791 IUPHAR_LIGAND_ID
D020909 MESH_DESCRIPTOR_UI
41774 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0140 TABLET 25 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0141 TABLET 50 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0142 TABLET 100 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-147 TABLET 25 mg ORAL ANDA 10 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-148 TABLET 50 mg ORAL ANDA 10 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-149 TABLET 100 mg ORAL ANDA 10 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-130 TABLET 25 mg ORAL ANDA 14 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-131 TABLET 50 mg ORAL ANDA 14 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-132 TABLET 100 mg ORAL ANDA 14 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 43353-908 TABLET 50 mg ORAL NDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 43353-951 TABLET 50 mg ORAL NDA authorized generic 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 47781-340 TABLET 25 mg ORAL NDA authorized generic 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 47781-341 TABLET 50 mg ORAL NDA authorized generic 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 47781-342 TABLET 100 mg ORAL NDA authorized generic 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4115 TABLET 50 mg ORAL NDA authorized generic 12 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4116 TABLET 100 mg ORAL NDA authorized generic 12 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4952 TABLET 50 mg ORAL ANDA 15 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-861 TABLET 50 mg ORAL NDA 11 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-862 TABLET 100 mg ORAL NDA 11 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-863 TABLET 25 mg ORAL NDA 11 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 54868-5831 TABLET 25 mg ORAL NDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 54868-5945 TABLET 25 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 63629-5697 TABLET 25 mg ORAL ANDA 15 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 63629-5698 TABLET 50 mg ORAL ANDA 15 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 64380-758 TABLET 25 mg ORAL ANDA 15 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 64380-759 TABLET 50 mg ORAL ANDA 15 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 64380-760 TABLET 100 mg ORAL ANDA 15 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 68151-0537 TABLET 50 mg ORAL ANDA 15 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 69543-120 TABLET 25 mg ORAL ANDA 11 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 69543-121 TABLET 50 mg ORAL ANDA 11 sections