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

Stem definitionDrug idCAS RN
antihyperglycaemics 1806 72432-03-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • miglitol
  • diastabol
  • seibule
  • glyset
Miglitol is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus.
  • Molecular weight: 207.23
  • Formula: C8H17NO5
  • CLOGP: -1.26
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 5
  • TPSA: 104.39
  • ALOGS: 0.47
  • ROTB: 3

  • 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) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 80 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 20.68 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.28 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.30 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 18, 1996 FDA PHARMACIA AND UPJOHN

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 78.91 34.13 29 665 53552 50550878
Hepatic function abnormal 64.45 34.13 22 672 32659 50571771
Cerebral infarction 56.45 34.13 18 676 21586 50582844
Pemphigoid 38.31 34.13 10 684 5897 50598533
Hypoglycaemic encephalopathy 38.20 34.13 6 688 272 50604158

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 80.68 26.84 41 1340 48305 29524841
Hepatic function abnormal 55.98 26.84 30 1351 39229 29533917
Diabetes mellitus inadequate control 48.43 26.84 19 1362 12115 29561031
Liver disorder 44.63 26.84 23 1358 27726 29545420
Cerebral infarction 35.52 26.84 19 1362 24656 29548490
Pneumatosis intestinalis 28.15 26.84 9 1372 3160 29569986

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 134.69 26.95 64 2125 89828 64406715
Hepatic function abnormal 131.84 26.95 57 2132 64256 64432287
Cerebral infarction 76.26 26.95 34 2155 41010 64455533
Diabetes mellitus inadequate control 75.25 26.95 28 2161 21293 64475250
Liver disorder 56.22 26.95 30 2159 53321 64443222
Pneumatosis intestinalis 47.37 26.95 14 2175 5215 64491328
Pemphigoid 45.60 26.95 17 2172 12969 64483574
Anti-insulin antibody positive 39.06 26.95 7 2182 280 64496263
Ketosis 36.13 26.95 8 2181 945 64495598
Glycosylated haemoglobin increased 35.35 26.95 15 2174 16004 64480539
Renal impairment 34.95 26.95 32 2157 134985 64361558
Hyperglycaemia 32.17 26.95 22 2167 60946 64435597
Platelet count decreased 29.11 26.95 32 2157 167679 64328864
Altered state of consciousness 28.23 26.95 17 2172 37885 64458658
Hypoglycaemic encephalopathy 28.03 26.95 6 2183 606 64495937
Rectal cancer 27.56 26.95 8 2181 2798 64493745

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BF02 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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Infectious disease contraindication 40733004
Ulcerative colitis contraindication 64766004 DOID:8577
Ulceration of intestine contraindication 85942002
Kidney disease contraindication 90708001 DOID:557
Gastrointestinal obstruction contraindication 126765001
Hypoglycemic disorder contraindication 237630007
Surgical procedure contraindication 387713003
Traumatic injury contraindication 417746004
Prolonged-Severe Nausea and Vomiting 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 13.55 acidic
pKa2 7.11 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
Lysosomal alpha-glucosidase Enzyme INHIBITOR IC50 6.46 CHEMBL CHEMBL
Maltase-glucoamylase, intestinal Enzyme INHIBITOR Ki 6 CHEMBL CHEMBL
Glucosylceramidase Enzyme IC50 4.08 CHEMBL
Sucrase-isomaltase, intestinal Enzyme IC50 6.30 CHEMBL
Lactase-phlorizin hydrolase Enzyme IC50 4.30 CHEMBL
Pancreatic alpha-amylase Enzyme WOMBAT-PK
Sucrase-isomaltase, intestinal Enzyme IC50 6.96 CHEMBL
Lysosomal alpha-glucosidase Enzyme Ki 6.34 CHEMBL
Glycogen debranching enzyme Enzyme IC50 6.41 CHEMBL
Beta-galactosidase Enzyme Ki 4 CHEMBL
Alpha-mannosidase Enzyme IC50 4.12 CHEMBL
Alpha-glucosidase Enzyme IC50 4.24 CHEMBL

External reference:

IDSource
4021063 VUID
N0000148526 NUI
D00625 KEGG_DRUG
4021063 VANDF
C0066535 UMLSCUI
CHEBI:6935 CHEBI
MIG PDB_CHEM_ID
CHEMBL1561 ChEMBL_ID
DB00491 DRUGBANK_ID
441314 PUBCHEM_CID
5879 INN_ID
C045621 MESH_SUPPLEMENTAL_RECORD_UI
4842 IUPHAR_LIGAND_ID
0V5436JAQW UNII
217372 RXNORM
14051 MMSL
241455 MMSL
7945 MMSL
d04110 MMSL
007635 NDDF
109071007 SNOMEDCT_US
386046009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 57664-684 TABLET, COATED 25 mg ORAL ANDA 24 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 57664-685 TABLET, COATED 50 mg ORAL ANDA 24 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 57664-686 TABLET, COATED 100 mg ORAL ANDA 24 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 69367-303 TABLET, COATED 25 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 69367-304 TABLET, COATED 50 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 69367-305 TABLET, COATED 100 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-935 TABLET, COATED 25 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-935 TABLET, COATED 25 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-936 TABLET, COATED 50 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-936 TABLET, COATED 50 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-937 TABLET, COATED 100 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 71205-937 TABLET, COATED 100 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 76333-125 TABLET, COATED 25 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 76333-126 TABLET, COATED 50 mg ORAL ANDA 25 sections
Miglitol HUMAN PRESCRIPTION DRUG LABEL 1 76333-127 TABLET, COATED 100 mg ORAL ANDA 25 sections