acarbose indications/contra

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

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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 476.88 56.65 100 448 14218 3371093
Hypoglycaemic coma 185.04 56.65 30 518 957 3384354
Pneumatosis intestinalis 177.74 56.65 28 520 740 3384571
Abdominal distension 62.93 56.65 20 528 13556 3371755

Pharmacologic Action:

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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
FDA MoA N0000000166 alpha Glucosidase Inhibitors
FDA EPC N0000175559 alpha-Glucosidase Inhibitor
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065089 Glycoside Hydrolase Inhibitors
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:35526 hypoglycemic agent

Drug Use (View source of the data)

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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:2527
Gastrointestinal obstruction contraindication 126765001
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007 DOID:9993
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

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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:

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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:

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IDSource
DB00284 DRUGBANK_ID
4020940 VUID
N0000148420 NUI
C0050393 UMLSCUI
6791 IUPHAR_LIGAND_ID
D00216 KEGG_DRUG
4020940 VANDF
136765 MMSL
N0000148420 NDFRT
N0000007005 NDFRT
16681 RXNORM
109077006 SNOMEDCT_US
386965004 SNOMEDCT_US
4117 MMSL
d03846 MMSL
004299 NDDF
CHEMBL1566 ChEMBL_ID
41774 PUBCHEM_CID
T58MSI464G UNII
4527 INN_ID
D020909 MESH_DESCRIPTOR_UI
CHEBI:2376 CHEBI
ACR PDB_CHEM_ID
QPS PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
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 16252-523 TABLET 25 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 16252-524 TABLET 50 mg ORAL ANDA 11 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 16252-525 TABLET 100 mg ORAL ANDA 11 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
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 55289-171 TABLET 50 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 64380-760 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
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 69543-122 TABLET 100 mg ORAL ANDA 11 sections