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miglitol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihyperglycaemics	1806	72432-03-2

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.30	g	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	80 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	610 mg/mL	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	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
t_half (Half-life)	2.30 hours	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
Vd (Volume of distribution)	0.28 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 18, 1996	FDA	PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BF02	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Alpha glucosidase inhibitors
FDA EPC	N0000175559	alpha-Glucosidase Inhibitor
FDA MoA	N0000000166	alpha Glucosidase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D065089	Glycoside Hydrolase Inhibitors
MeSH PA	D007004	Hypoglycemic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Lysosomal alpha-glucosidase	Enzyme	P10253	LYAG_HUMAN	INHIBITOR	IC50	6.46	CHEMBL	CHEMBL
Maltase-glucoamylase, intestinal	Enzyme	O43451	MGA_HUMAN	INHIBITOR	Ki	6	CHEMBL	CHEMBL
Glucosylceramidase	Enzyme	P04062	GLCM_HUMAN		IC50	4.08	CHEMBL
Sucrase-isomaltase, intestinal	Enzyme	P14410	SUIS_HUMAN		IC50	6.30	CHEMBL
Lactase-phlorizin hydrolase	Enzyme	P09848	LPH_HUMAN		IC50	4.30	CHEMBL
Pancreatic alpha-amylase	Enzyme	P04746	AMYP_HUMAN				WOMBAT-PK
Sucrase-isomaltase, intestinal	Enzyme		SUIS_RAT		IC50	6.96	CHEMBL
Lysosomal alpha-glucosidase	Enzyme		LYAG_RAT		Ki	6.34	CHEMBL
Glycogen debranching enzyme	Enzyme		GDE_RABIT		IC50	6.41	CHEMBL
Beta-galactosidase	Enzyme		BGAL_BOVIN		Ki	4	CHEMBL

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External reference:

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ID	Source
MIG	PDB_CHEM_ID
007635	NDDF
0V5436JAQW	UNII
109071007	SNOMEDCT_US
14051	MMSL
217372	RXNORM
241455	MMSL
386046009	SNOMEDCT_US
4021063	VUID
4021063	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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