acarbose ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.64 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 2 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.32 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.20 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 6, 1995 FDA BAYER HLTHCARE

FDA Adverse Event Reporting System (Female)

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 415.05 23.32 159 4094 53422 50547449
Hypoglycaemic coma 222.01 23.32 49 4204 2284 50598587
Lactic acidosis 130.09 23.32 61 4192 33294 50567577
Acute kidney injury 55.36 23.32 81 4172 227977 50372894
Diabetes mellitus inadequate control 54.15 23.32 25 4228 13120 50587751
Blood glucose decreased 52.10 23.32 27 4226 18184 50582687
Hyperglycaemia 46.28 23.32 32 4221 36373 50564498
Abdominal distension 45.13 23.32 42 4211 72861 50528010
Drug interaction 44.26 23.32 68 4185 199553 50401318
Pneumatosis intestinalis 43.07 23.32 13 4240 2090 50598781
Peripheral artery haematoma 38.22 23.32 6 4247 39 50600832
Glycosylated haemoglobin increased 37.02 23.32 18 4235 10588 50590283
Mucosal erosion 35.39 23.32 10 4243 1277 50599594
Ketoacidosis 35.21 23.32 13 4240 3882 50596989
Intestinal transit time abnormal 35.16 23.32 6 4247 69 50600802
Drug ineffective 32.92 23.32 14 4239 819319 49781552
Urine calcium/creatinine ratio increased 32.35 23.32 6 4247 114 50600757
Insulin-like growth factor decreased 30.88 23.32 7 4246 367 50600504
Bite 30.75 23.32 7 4246 374 50600497
Blood sodium increased 29.24 23.32 10 4243 2392 50598479
Diabetic ketoacidosis 28.24 23.32 18 4235 17854 50583017
Urethral caruncle 27.54 23.32 5 4248 84 50600787
Urinary incontinence 27.22 23.32 21 4232 28187 50572684
Hyperkalaemia 26.50 23.32 26 4227 48063 50552808
Cell death 26.10 23.32 9 4244 2206 50598665
Stevens-Johnson syndrome 25.03 23.32 18 4235 21734 50579137
Pain 24.65 23.32 9 4244 578894 50021977
Hyperleukocytosis 24.26 23.32 6 4247 458 50600413

FDA Adverse Event Reporting System (Male)

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 182.15 21.05 100 3826 48246 29522355
Hypoglycaemic coma 153.02 21.05 39 3887 2124 29568477
Lactic acidosis 85.49 21.05 52 3874 30195 29540406
Diabetes mellitus inadequate control 56.53 21.05 29 3897 12105 29558496
Hyperoxaluria 53.42 21.05 10 3916 123 29570478
Cerebral infarction 39.81 21.05 30 3896 24645 29545956
Albumin urine present 37.88 21.05 9 3917 364 29570237
Speech disorder 34.45 21.05 27 3899 23489 29547112
Drug interaction 33.63 21.05 78 3848 197307 29373294
Quadriparesis 31.41 21.05 10 3916 1209 29569392
Mouth swelling 28.89 21.05 10 3916 1566 29569035
Acute kidney injury 27.25 21.05 87 3839 265180 29305421
Mast cell degranulation present 26.60 21.05 5 3921 63 29570538
Diabetic metabolic decompensation 26.02 21.05 9 3917 1407 29569194
Pneumatosis intestinalis 25.34 21.05 11 3915 3158 29567443
Metabolic acidosis 25.31 21.05 28 3898 37634 29532967
Monoparesis 23.42 21.05 9 3917 1894 29568707
Acetonaemia 22.75 21.05 5 3921 142 29570459

FDA Adverse Event Reporting System (Geriatric)

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 533.71 19.63 247 7725 89645 64401115
Hypoglycaemic coma 368.31 19.63 89 7883 4185 64486575
Lactic acidosis 195.04 19.63 111 7861 61299 64429461
Diabetes mellitus inadequate control 96.99 19.63 49 7923 21272 64469488
Acute kidney injury 67.71 19.63 162 7810 449078 64041682
Drug interaction 67.31 19.63 142 7830 361941 64128819
Pneumatosis intestinalis 59.83 19.63 23 7949 5206 64485554
Abdominal distension 55.90 19.63 64 7908 95930 64394830
Hyperoxaluria 52.78 19.63 11 7961 260 64490500
Blood glucose decreased 50.65 19.63 33 7939 23090 64467670
Glycosylated haemoglobin increased 45.56 19.63 27 7945 15992 64474768
Ketoacidosis 44.08 19.63 20 7952 6843 64483917
Hyperkalaemia 42.11 19.63 57 7915 101072 64389688
Hyperglycaemia 39.50 19.63 43 7929 60925 64429835
Cerebral infarction 37.73 19.63 35 7937 41009 64449751
Speech disorder 36.44 19.63 37 7935 48404 64442356
Peripheral artery haematoma 35.16 19.63 6 7966 45 64490715
Diabetic ketoacidosis 34.53 19.63 29 7943 29816 64460944
Metabolic acidosis 34.21 19.63 43 7929 70915 64419845
Albumin urine present 33.40 19.63 9 7963 652 64490108
Drug ineffective 33.34 19.63 33 7939 840214 63650546
Intestinal transit time abnormal 32.85 19.63 6 7966 69 64490691
Urine calcium/creatinine ratio increased 28.78 19.63 6 7966 142 64490618
Bite 27.25 19.63 7 7965 421 64490339
Mast cell degranulation present 26.95 19.63 5 7967 63 64490697
Urethral caruncle 26.20 19.63 5 7967 74 64490686
Insulin-like growth factor decreased 25.41 19.63 7 7965 551 64490209
Acetonaemia 25.12 19.63 6 7966 267 64490493
Mucosal erosion 23.90 19.63 9 7963 1925 64488835
Quadriparesis 23.79 19.63 10 7962 2847 64487913
Portal venous gas 23.61 19.63 6 7966 346 64490414
Monoparesis 23.54 19.63 10 7962 2924 64487836
Diabetic ketosis 23.42 19.63 6 7966 357 64490403
Anuria 23.12 19.63 19 7953 18945 64471815
Arthralgia 23.10 19.63 13 7959 442247 64048513
Lacunar infarction 23.07 19.63 12 7960 5520 64485240
Chronic gastritis 22.58 19.63 10 7962 3230 64487530
Diabetic metabolic decompensation 20.90 19.63 9 7963 2719 64488041
Unresponsive to stimuli 20.34 19.63 28 7944 50365 64440395
Blood glucose increased 19.93 19.63 40 7932 98033 64392727

FDA Adverse Event Reporting System (Pediatric)

None

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
FDA MoA N0000000166 alpha Glucosidase Inhibitors
FDA EPC N0000175559 alpha-Glucosidase Inhibitor
CHEBI has role CHEBI:35526 antidiabetic
CHEBI has role CHEBI:50627 Taka-amylase A inhibitor
CHEBI has role CHEBI:67239 glucosidoinvertase inhibitor
CHEBI has role CHEBI:176497 geroprotectors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065089 Glycoside Hydrolase Inhibitors
MeSH PA D007004 Hypoglycemic Agents

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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
Alpha-amylase 1 Enzyme IC50 6 CHEMBL
Lysosomal alpha-glucosidase Enzyme IC50 5.30 CHEMBL
Alpha-amylase 1A Enzyme IC50 6.30 CHEMBL
Sucrase-isomaltase, intestinal Enzyme Ki 6.61 SCIENTIFIC LITERATURE
Sucrase-isomaltase, intestinal Enzyme IC50 6.40 CHEMBL
Lysosomal alpha-glucosidase Enzyme Ki 5.46 CHEMBL
Alpha-amylase Enzyme Ki 6.47 CHEMBL
Oligo-1,6-glucosidase Enzyme IC50 4.42 CHEMBL
Pancreatic alpha-amylase Enzyme IC50 4.45 CHEMBL

External reference:

IDSource
4020940 VUID
N0000148420 NUI
D00216 KEGG_DRUG
151826 RXNORM
C0050393 UMLSCUI
CHEBI:84363 CHEBI
CHEMBL1566 ChEMBL_ID
CHEMBL404271 ChEMBL_ID
D020909 MESH_DESCRIPTOR_UI
DB00284 DRUGBANK_ID
6791 IUPHAR_LIGAND_ID
4527 INN_ID
T58MSI464G UNII
444254 PUBCHEM_CID
136765 MMSL
4117 MMSL
4644 MMSL
d03846 MMSL
004299 NDDF
4020940 VANDF
109077006 SNOMEDCT_US
386965004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0140 TABLET 25 mg ORAL ANDA 10 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0141 TABLET 50 mg ORAL ANDA 10 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 0054-0142 TABLET 100 mg ORAL ANDA 10 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 11788-039 TABLET 25 mg ORAL ANDA 24 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 11788-040 TABLET 50 mg ORAL ANDA 24 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 11788-041 TABLET 100 mg ORAL ANDA 24 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-147 TABLET 25 mg ORAL ANDA 20 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-147 TABLET 25 mg ORAL ANDA 20 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-148 TABLET 50 mg ORAL ANDA 20 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-148 TABLET 50 mg ORAL ANDA 20 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-149 TABLET 100 mg ORAL ANDA 20 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 23155-149 TABLET 100 mg ORAL ANDA 20 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-130 TABLET 25 mg ORAL ANDA 22 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-131 TABLET 50 mg ORAL ANDA 22 sections
acarbose HUMAN PRESCRIPTION DRUG LABEL 1 42291-132 TABLET 100 mg ORAL ANDA 22 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 43353-908 TABLET 50 mg ORAL NDA 22 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 43353-951 TABLET 50 mg ORAL NDA authorized generic 21 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4115 TABLET 50 mg ORAL NDA authorized generic 22 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4116 TABLET 100 mg ORAL NDA authorized generic 22 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-4952 TABLET 50 mg ORAL ANDA 17 sections
ACARBOSE HUMAN PRESCRIPTION DRUG LABEL 1 50090-5088 TABLET 100 mg ORAL ANDA 24 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 50090-5829 TABLET 100 mg ORAL ANDA 17 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-861 TABLET 50 mg ORAL NDA 22 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-862 TABLET 100 mg ORAL NDA 22 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 50419-863 TABLET 25 mg ORAL NDA 22 sections
Precose HUMAN PRESCRIPTION DRUG LABEL 1 54868-5831 TABLET 25 mg ORAL NDA 22 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 54868-5945 TABLET 25 mg ORAL ANDA 19 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 63629-5697 TABLET 25 mg ORAL ANDA 17 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 63629-5698 TABLET 50 mg ORAL ANDA 17 sections
Acarbose HUMAN PRESCRIPTION DRUG LABEL 1 64380-758 TABLET 25 mg ORAL ANDA 17 sections