miglitol 🐶 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 µM/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
S (Water solubility) 610 mg/mL Bocci G, Oprea TI, Benet LZ

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 87.84 34.32 31 709 60034 63428248
Hepatic function abnormal 65.17 34.32 22 718 37120 63451162
Cerebral infarction 61.75 34.32 19 721 23874 63464408
Hypoglycaemic encephalopathy 45.98 34.32 7 733 305 63487977
Pemphigoid 37.76 34.32 10 730 7334 63480948

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 82.50 26.77 42 1442 54598 34900849
Hepatic function abnormal 60.84 26.77 32 1452 44331 34911116
Diabetes mellitus inadequate control 51.80 26.77 20 1464 13444 34942003
Liver disorder 42.92 26.77 23 1461 32974 34922473
Cerebral infarction 38.14 26.77 20 1464 27435 34928012
Pneumatosis intestinalis 27.10 26.77 9 1475 3914 34951533
Anti-insulin antibody positive 26.96 26.77 5 1479 193 34955254

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 145.09 26.67 67 2284 101527 79640510
Hepatic function abnormal 139.12 26.67 59 2292 73048 79668989
Cerebral infarction 83.90 26.67 36 2315 45640 79696397
Diabetes mellitus inadequate control 82.98 26.67 30 2321 24234 79717803
Liver disorder 51.58 26.67 30 2321 72387 79669650
Pneumatosis intestinalis 46.53 26.67 14 2337 6383 79735654
Pemphigoid 45.19 26.67 17 2334 15298 79726739
Anti-insulin antibody positive 39.83 26.67 7 2344 289 79741748
Glycosylated haemoglobin increased 38.04 26.67 16 2335 19244 79722793
Hyperglycaemia 36.95 26.67 24 2327 70311 79671726
Ketosis 35.93 26.67 8 2343 1118 79740919
Renal impairment 34.52 26.67 32 2319 157751 79584286
Hypoglycaemic encephalopathy 34.22 26.67 7 2344 654 79741383
Platelet count decreased 32.40 26.67 34 2317 194630 79547407
Interstitial lung disease 28.90 26.67 25 2326 112575 79629462
Decreased appetite 28.19 26.67 42 2309 342376 79399661
Altered state of consciousness 28.16 26.67 17 2334 43805 79698232
Rectal cancer 26.89 26.67 8 2343 3505 79738532

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 | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 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
C045621 MESH_SUPPLEMENTAL_RECORD_UI
4842 IUPHAR_LIGAND_ID
5879 INN_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