Identification

Name
Miglitol
Accession Number
DB00491  (APRD01117)
Type
Small Molecule
Groups
Approved
Description

Miglitol 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
  • Miglitol
  • Miglitolum
External IDs
Bay m 1099
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GlysetTablet, film coated25 mg/1OralPharmacia & Upjohn Inc1996-12-18Not applicableUs00009 5012 01 nlmimage10 8f15c7be
GlysetTablet, film coated100 mg/1OralPharmacia & Upjohn Inc1996-12-18Not applicableUs
GlysetTablet, film coated50 mg/1OralPharmacia & Upjohn Inc1996-12-18Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MiglitolTablet, coated25 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated100 mg/1OralSun Pharmaceutical Industries Limited2016-01-04Not applicableUs
MiglitolTablet, coated100 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated50 mg/1OralSun Pharmaceutical Industries Limited2016-01-04Not applicableUs
MiglitolTablet, coated50 mg/1OralOrient Pharma Co., Ltd.2015-07-31Not applicableUs
MiglitolTablet, coated25 mg/1OralSun Pharmaceutical Industries Limited2016-01-04Not applicableUs
International/Other Brands
Diaban (Chen Ho) / Diamig (Micro DTF) / Diaset (ACI) / Diastabol (Sanofi-Aventis) / Elitox (Ranbaxy) / Euglitol (Abbott) / Glycet (Pfizer) / Glyset / Laiping (Xinchang Pharmaceutical) / Migbose (Standard) / Miglit (Biocon) / Mignar (Glenmark) / Migtor (Torrent) / Misobit (Lupin) / Plumarol (Lacer) / Seibule (Sanwa Kagaku)
Categories
UNII
0V5436JAQW
CAS number
72432-03-2
Weight
Average: 207.2243
Monoisotopic: 207.110672659
Chemical Formula
C8H17NO5
InChI Key
IBAQFPQHRJAVAV-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

Pharmacology

Indication

For 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
Pharmacodynamics

Miglitol, 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 action

In 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.

TargetActionsOrganism
AMaltase-glucoamylase, intestinal
antagonist
inhibitor
Human
ALysosomal alpha-glucosidase
antagonist
Human
ANeutral alpha-glucosidase AB
antagonist
Human
ANeutral alpha-glucosidase C
antagonist
Human
Absorption

Absorption 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 binding

The protein binding of miglitol is negligible (<4.0%).

Metabolism

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

Route of elimination

Miglitol is not metabolized in man or in any animal species studied. It is eliminated by renal excretion as an unchanged drug.

Half life

The elimination half-life of miglitol from plasma is approximately 2 hours.

Clearance
Not Available
Toxicity

Unlike 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
AlaproclateAlaproclate may increase the hypoglycemic activities of Miglitol.Experimental
AloxiprinAloxiprin may increase the hypoglycemic activities of Miglitol.Experimental
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Miglitol.Approved
AmphetamineAmphetamine may increase the hypoglycemic activities of Miglitol.Approved, Illicit
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
BCG vaccineThe therapeutic efficacy of BCG vaccine 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
BrofaromineBrofaromine may increase the hypoglycemic activities of Miglitol.Experimental
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, Investigational, Withdrawn
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
CyclopenthiazideThe therapeutic efficacy of Miglitol can be decreased when used in combination with Cyclopenthiazide.Experimental
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, Investigational
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.Withdrawn
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, Investigational, 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
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Miglitol.Investigational
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.Investigational, Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Miglitol.Experimental
HarmalineHarmaline may increase the hypoglycemic activities of Miglitol.Experimental
Hemoglobin crosfumarilHemoglobin crosfumaril may increase the hypoglycemic activities of Miglitol.Experimental
HistrelinThe therapeutic efficacy of Miglitol can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Miglitol.Experimental
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, Investigational
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
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
MesteroloneMesterolone may increase the hypoglycemic activities of Miglitol.Experimental
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
Methyl salicylateMethyl salicylate may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Miglitol.Approved, 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
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Miglitol.Approved, Investigational
NandroloneNandrolone may increase the hypoglycemic activities of Miglitol.Experimental, Investigational
Nandrolone decanoateNandrolone decanoate may increase the hypoglycemic activities of Miglitol.Approved, Illicit
NateglinideMiglitol may increase the hypoglycemic activities of Nateglinide.Approved, 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
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
Oxolinic acidOxolinic acid may increase the hypoglycemic activities of Miglitol.Experimental
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
Pipemidic acidPipemidic acid may increase the hypoglycemic activities of Miglitol.Experimental
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, Investigational
PirlindolePirlindole may increase the hypoglycemic activities of Miglitol.Approved
Piromidic acidPiromidic acid may increase the hypoglycemic activities of Miglitol.Experimental
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
ProcarbazineProcarbazine may increase the hypoglycemic activities of Miglitol.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, Investigational
RufloxacinRufloxacin may increase the hypoglycemic activities of Miglitol.Experimental
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
SitafloxacinSitafloxacin may increase the hypoglycemic activities of Miglitol.Experimental, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational
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
Testosterone PropionateTestosterone Propionate may increase the hypoglycemic activities of Miglitol.Approved, Vet Approved
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
Trolamine salicylateTrolamine salicylate may increase the hypoglycemic activities of Miglitol.Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Miglitol.Approved, Investigational, 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

General References
Not Available
External Links
Human Metabolome Database
HMDB14634
KEGG Drug
D00625
KEGG Compound
C07708
PubChem Compound
441314
PubChem Substance
46504492
ChemSpider
390074
BindingDB
50242271
ChEBI
6935
ChEMBL
CHEMBL1561
Therapeutic Targets Database
DAP000712
PharmGKB
PA164776726
HET
MIG
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Miglitol
ATC Codes
A10BF02 — Miglitol
PDB Entries
3l4w / 5nn6
MSDS
Download (68.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of ASP19411
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
3CompletedTreatmentType 2 Diabetes Mellitus6
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus3

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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)114 °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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Piperidines
Sub Class
Not Available
Direct Parent
Piperidines
Alternative Parents
Trialkylamines / Secondary alcohols / 1,2-aminoalcohols / Polyols / Azacyclic compounds / Primary alcohols / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Piperidine / 1,2-aminoalcohol / Tertiary aliphatic amine / Tertiary amine / Secondary alcohol / Alkanolamine / Polyol / Azacycle / Organic nitrogen compound / Primary alcohol
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
piperidines (CHEBI:6935)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
Inhibitor
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 dietar...
Gene Name
MGAM
Uniprot ID
O43451
Uniprot Name
Maltase-glucoamylase, intestinal
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
Uniprot Name
Lysosomal alpha-glucosidase
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
Uniprot Name
Neutral alpha-glucosidase AB
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
Uniprot Name
Neutral alpha-glucosidase C
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
Uniprot Name
Pancreatic alpha-amylase
Molecular Weight
57706.51 Da

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:38