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Identification
NameMiglitol
Accession NumberDB00491  (APRD01117)
TypeSmall Molecule
GroupsApproved
DescriptionMiglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not metabolized and is excreted by the kidneys.
Structure
Thumb
Synonyms
Glyset
Miglitol
Miglitolum
External Identifiers
  • Bay m 1099
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GlysetTablet, film coated25 mg/1OralPharmacia And Upjohn Company Llc1996-12-18Not applicableUs
GlysetTablet, film coated50 mg/1OralPharmacia And Upjohn Company Llc1996-12-18Not applicableUs
GlysetTablet, film coated100 mg/1OralPharmacia And Upjohn Company Llc1996-12-18Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MiglitolTablet, coated25 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated50 mg/1OralSun Pharmaceutical Industries Ltd.2016-01-04Not applicableUs
MiglitolTablet, coated50 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated100 mg/1OralSun Pharmaceutical Industries Ltd.2016-01-04Not applicableUs
MiglitolTablet, coated100 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated25 mg/1OralSun Pharmaceutical Industries Ltd.2016-01-04Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DiabanChen Ho
DiamigMicro DTF
DiasetACI
DiastabolSanofi-Aventis
ElitoxRanbaxy
EuglitolAbbott
GlycetPfizer
LaipingXinchang Pharmaceutical
MigboseStandard
MiglitBiocon
MignarGlenmark
MigtorTorrent
MisobitLupin
PlumarolLacer
SeibuleSanwa Kagaku
Brand mixturesNot Available
SaltsNot Available
Categories
UNII0V5436JAQW
CAS number72432-03-2
WeightAverage: 207.2243
Monoisotopic: 207.110672659
Chemical FormulaC8H17NO5
InChI KeyIBAQFPQHRJAVAV-ULAWRXDQSA-N
InChI
InChI=1S/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5-,6+,7-,8-/m1/s1
IUPAC Name
(2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
SMILES
OCCN1C[[email protected]](O)[C@@H](O)[[email protected]](O)[[email protected]]1CO
Pharmacology
IndicationFor use as an adjunct to diet to improve glycemic control in patients with non-insulin-dependent diabetes mellitus (NIDDM) whose hyperglycemia cannot be managed with diet alone.
Structured Indications
PharmacodynamicsMiglitol, an oral alpha-glucosidase inhibitor, 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. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time. Because its mechanism of action is different, the effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance.
Mechanism of actionIn contrast to sulfonylureas, miglitol does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia.
TargetKindPharmacological actionActionsOrganismUniProt ID
Maltase-glucoamylase, intestinalProteinyes
antagonist
inhibitor
HumanO43451 details
Lysosomal alpha-glucosidaseProteinyes
antagonist
HumanP10253 details
Neutral alpha-glucosidase ABProteinyes
antagonist
HumanQ14697 details
Neutral alpha-glucosidase CProteinyes
antagonist
HumanQ8TET4 details
Related Articles
AbsorptionAbsorption of miglitol is saturable at high doses with 25 mg being completely absorbed while a 100-mg dose is only 50-70% absorbed. No evidence exists to show that systemic absorption of miglitol adds to its therapeutic effect.
Volume of distribution
  • 0.18 L/kg
Protein bindingThe protein binding of miglitol is negligible (<4.0%).
Metabolism

Miglitol is not metabolized in man or in any animal species studied.

Route of eliminationMiglitol is not metabolized in man or in any animal species studied. It is eliminated by renal excretion as an unchanged drug.
Half lifeThe elimination half-life of miglitol from plasma is approximately 2 hours.
ClearanceNot Available
ToxicityUnlike sulfonylureas or insulin, an overdose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdomi-nal discomfort. Because of the lack of extra-intestinal effects seen with miglitol, no serious systemic reactions are expected in the event of an overdose.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Miglitol.Experimental
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Miglitol.Approved
AripiprazoleThe therapeutic efficacy of Miglitol can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Atazanavir.Approved, Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Miglitol.Approved, Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Miglitol.Investigational
BendroflumethiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Miglitol.Withdrawn
BetamethasoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BrexpiprazoleThe therapeutic efficacy of Miglitol can be decreased when used in combination with Brexpiprazole.Approved
BumetanideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Buserelin.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Miglitol.Withdrawn
CeritinibThe therapeutic efficacy of Miglitol can be decreased when used in combination with Ceritinib.Approved
ChlorothiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideMiglitol may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Chlorthalidone.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Miglitol.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Miglitol.Approved
ClozapineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Clozapine.Approved
CorticotropinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Cortisone acetate.Approved
Cyproterone acetateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe therapeutic efficacy of Miglitol can be decreased when used in combination with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Miglitol.Investigational
DarunavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Darunavir.Approved
dersalazinedersalazine may increase the hypoglycemic activities of Miglitol.Investigational
DesogestrelThe therapeutic efficacy of Miglitol can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Miglitol.Approved
DexamethasoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Miglitol can be decreased when used in combination with Dienogest.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Miglitol.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Miglitol.Illicit
DisopyramideMiglitol may increase the hypoglycemic activities of Disopyramide.Approved
DrospirenoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Miglitol.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Miglitol.Approved
EpinephrineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Miglitol.Approved, Investigational
EstradiolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Miglitol can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Miglitol can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Miglitol.Approved
EverolimusThe therapeutic efficacy of Miglitol can be decreased when used in combination with Everolimus.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Miglitol.Approved
FludrocortisoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Miglitol.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Miglitol.Approved, Illicit
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Miglitol.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Fosamprenavir.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Furosemide.Approved, Vet Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Miglitol.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
GliclazideMiglitol may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideMiglitol may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideMiglitol may increase the hypoglycemic activities of Glipizide.Approved
GlyburideMiglitol may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Miglitol.Withdrawn
HistrelinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Miglitol.Approved
HydrochlorothiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Iloperidone.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Miglitol.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Indapamide.Approved
IndinavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Indinavir.Approved
Insulin AspartMiglitol may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirMiglitol may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineMiglitol may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineMiglitol may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanMiglitol may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproMiglitol may increase the hypoglycemic activities of Insulin Lispro.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Miglitol.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Miglitol.Withdrawn
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Miglitol.Approved
LanreotideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Miglitol.Approved
LevonorgestrelThe therapeutic efficacy of Miglitol can be decreased when used in combination with Levonorgestrel.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Miglitol.Approved, Nutraceutical
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Miglitol.Approved
LopinavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Lopinavir.Approved
LurasidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Lurasidone.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Miglitol.Withdrawn
MecaserminMiglitol may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Miglitol.Approved
MestranolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Mestranol.Approved
MethotrimeprazineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Miglitol.Investigational
MethylprednisoloneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Miglitol.Approved
MetolazoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Metolazone.Approved
MifepristoneMiglitol may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Miglitol.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Miglitol.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Miglitol.Approved
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Miglitol.Approved
NateglinideMiglitol may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Miglitol.Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Miglitol.Approved, Withdrawn
NelfinavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Miglitol.Investigational
NiacinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Miglitol.Withdrawn
NilotinibThe therapeutic efficacy of Miglitol can be decreased when used in combination with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Miglitol.Investigational
NorethisteroneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Miglitol.Approved
NorgestimateThe therapeutic efficacy of Miglitol can be decreased when used in combination with Norgestimate.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Miglitol.Withdrawn
OctreotideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Miglitol.Approved
OlanzapineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Olanzapine.Approved, Investigational
OlsalazineOlsalazine may increase the hypoglycemic activities of Miglitol.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Miglitol.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Miglitol.Approved, Illicit
PaliperidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Miglitol.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Miglitol.Approved, Investigational
PasireotideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Miglitol.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Miglitol.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Miglitol.Approved
PentamidineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Pentamidine.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Miglitol.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Miglitol.Withdrawn
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Miglitol.Withdrawn
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Miglitol.Approved
PiperazineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Miglitol.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Miglitol.Withdrawn
PolythiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Polythiazide.Approved
PrednisoloneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Prednisone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Progesterone.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Miglitol.Investigational
QuetiapineThe therapeutic efficacy of Miglitol can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Quinethazone.Approved
QuinineMiglitol may increase the hypoglycemic activities of Quinine.Approved
RasagilineRasagiline may increase the hypoglycemic activities of Miglitol.Approved
RepaglinideMiglitol may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RisperidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Ritonavir.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Miglitol.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Miglitol.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
SaquinavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Saquinavir.Approved, Investigational
SelegilineSelegiline may increase the hypoglycemic activities of Miglitol.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Miglitol.Approved
SirolimusThe therapeutic efficacy of Miglitol can be decreased when used in combination with Sirolimus.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Miglitol.Approved
StanozololStanozolol may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
SulfadiazineMiglitol may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleMiglitol may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleMiglitol may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SunitinibMiglitol may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Miglitol can be decreased when used in combination with Tacrolimus.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Miglitol.Withdrawn
TemsirolimusThe therapeutic efficacy of Miglitol can be decreased when used in combination with Temsirolimus.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Miglitol.Approved, Investigational
TipranavirThe therapeutic efficacy of Miglitol can be decreased when used in combination with Tipranavir.Approved, Investigational
TolazamideMiglitol may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideMiglitol may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Miglitol.Approved
TorasemideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Miglitol.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Miglitol.Approved
TriamcinoloneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Miglitol.Approved, Withdrawn
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Miglitol.Approved
VorinostatThe therapeutic efficacy of Miglitol can be decreased when used in combination with Vorinostat.Approved, Investigational
ZimelidineZimelidine may increase the hypoglycemic activities of Miglitol.Withdrawn
ZiprasidoneThe therapeutic efficacy of Miglitol can be decreased when used in combination with Ziprasidone.Approved
Food Interactions
  • Take with food, at beginning of each meal. Iron needs increased.
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesA10BF02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (68.8 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.5422
Blood Brain Barrier-0.8379
Caco-2 permeable-0.7375
P-glycoprotein substrateSubstrate0.6354
P-glycoprotein inhibitor INon-inhibitor0.7325
P-glycoprotein inhibitor IINon-inhibitor0.8248
Renal organic cation transporterNon-inhibitor0.6749
CYP450 2C9 substrateNon-substrate0.8563
CYP450 2D6 substrateNon-substrate0.8168
CYP450 3A4 substrateNon-substrate0.6208
CYP450 1A2 substrateNon-inhibitor0.927
CYP450 2C9 inhibitorNon-inhibitor0.9022
CYP450 2D6 inhibitorNon-inhibitor0.9535
CYP450 2C19 inhibitorNon-inhibitor0.9676
CYP450 3A4 inhibitorNon-inhibitor0.9931
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9968
Ames testNon AMES toxic0.79
CarcinogenicityNon-carcinogens0.9702
BiodegradationNot ready biodegradable0.5392
Rat acute toxicity1.7432 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5797
hERG inhibition (predictor II)Non-inhibitor0.8756
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
Tablet, coatedOral100 mg/1
Tablet, coatedOral25 mg/1
Tablet, coatedOral50 mg/1
Prices
Unit descriptionCostUnit
Glyset 100 mg tablet1.46USD tablet
Glyset 50 mg tablet1.24USD tablet
Glyset 25 mg tablet1.11USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point114 °CNot Available
water solubilitySolubleNot Available
logP-2.7Not Available
pKa5.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility610.0 mg/mLALOGPS
logP-2.3ALOGPS
logP-3.2ChemAxon
logS0.47ALOGPS
pKa (Strongest Acidic)12.9ChemAxon
pKa (Strongest Basic)7.6ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area104.39 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity48.16 m3·mol-1ChemAxon
Polarizability20.81 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as piperidines. These are compounds containing a piperidine ring, which is a saturated aliphatic six-member ring with one nitrogen atom and five carbon atoms.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassNot Available
Direct ParentPiperidines
Alternative Parents
Substituents
  • Piperidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary alcohol
  • Polyol
  • 1,2-diol
  • 1,2-aminoalcohol
  • Azacycle
  • Alkanolamine
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonistinhibitor
General Function:
Maltose alpha-glucosidase activity
Specific Function:
May serve as an alternate pathway for starch digestion when luminal alpha-amylase activity is reduced because of immaturity or malnutrition. May play a unique role in the digestion of malted dietary oligosaccharides used in food manufacturing.
Gene Name:
MGAM
Uniprot ID:
O43451
Molecular Weight:
209850.8 Da
References
  1. Mooradian AD, Thurman JE: Drug therapy of postprandial hyperglycaemia. Drugs. 1999 Jan;57(1):19-29. [PubMed:9951949 ]
  2. Rossi EJ, Sim L, Kuntz DA, Hahn D, Johnston BD, Ghavami A, Szczepina MG, Kumar NS, Sterchi EE, Nichols BL, Pinto BM, Rose DR: Inhibition of recombinant human maltase glucoamylase by salacinol and derivatives. FEBS J. 2006 Jun;273(12):2673-83. [PubMed:16817895 ]
  3. Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [PubMed:19818342 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Maltose alpha-glucosidase activity
Specific Function:
Essential for the degradation of glygogen to glucose in lysosomes.
Gene Name:
GAA
Uniprot ID:
P10253
Molecular Weight:
105322.935 Da
References
  1. Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [PubMed:19818342 ]
  2. Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [PubMed:19085811 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Poly(a) rna binding
Specific Function:
Cleaves sequentially the 2 innermost alpha-1,3-linked glucose residues from the Glc(2)Man(9)GlcNAc(2) oligosaccharide precursor of immature glycoproteins.
Gene Name:
GANAB
Uniprot ID:
Q14697
Molecular Weight:
106873.125 Da
References
  1. Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [PubMed:19818342 ]
  2. Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [PubMed:19085811 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Maltose alpha-glucosidase activity
Specific Function:
Has alpha-glucosidase activity.
Gene Name:
GANC
Uniprot ID:
Q8TET4
Molecular Weight:
104333.445 Da
References
  1. Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [PubMed:19818342 ]
  2. Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [PubMed:19085811 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Chloride ion binding
Specific Function:
Not Available
Gene Name:
AMY2A
Uniprot ID:
P04746
Molecular Weight:
57706.51 Da
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23