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

Stem definition	Drug id	CAS RN
	39	56180-94-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: acarbose ascarbose glucobay prandase precose	An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE. Molecular weight: 645.61 Formula: C25H43NO18 CLOGP: -6.66 LIPINSKI: 3 HAC: 19 HDO: 14 TPSA: 321.17 ALOGS: -0.64 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

acarbose
ascarbose
glucobay
prandase
precose

An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE.

Molecular weight: 645.61
Formula: C25H43NO18
CLOGP: -6.66
LIPINSKI: 3
HAC: 19
HDO: 14
TPSA: 321.17
ALOGS: -0.64
ROTB: 9

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
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.64 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	2.70 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	2 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	129 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.32 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Sept. 6, 1995	FDA	BAYER HLTHCARE

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	531.60	22.74	194	4891	59871	63424066
Hypoglycaemic coma	315.35	22.74	66	5019	2509	63481428
Lactic acidosis	140.02	22.74	66	5019	38221	63445716
Diabetes mellitus inadequate control	84.05	22.74	35	5050	15091	63468846
Blood glucose decreased	55.39	22.74	29	5056	20923	63463014
Acute kidney injury	52.16	22.74	83	5002	263332	63220605
Diabetic ketoacidosis	50.30	22.74	27	5058	20478	63463459
Drug interaction	49.25	22.74	75	5010	229056	63254881
Abdominal distension	48.11	22.74	46	5039	86569	63397368
Pneumatosis intestinalis	46.17	22.74	14	5071	2399	63481538

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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	223.50	20.87	118	4369	54522	34897922
Hypoglycaemic coma	194.29	20.87	48	4439	2383	34950061
Lactic acidosis	87.88	20.87	55	4432	34717	34917727
Diabetes mellitus inadequate control	72.14	20.87	35	4452	13429	34939015
Hyperoxaluria	53.68	20.87	10	4477	124	34952320
Cerebral infarction	53.65	20.87	37	4450	27418	34925026
Drug interaction	37.95	20.87	87	4400	225859	34726585
Albumin urine present	37.92	20.87	9	4478	375	34952069
Speech disorder	33.14	20.87	27	4460	25659	34926785
Pneumatosis intestinalis	29.78	20.87	13	4474	3910	34948534

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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	677.23	17.81	297	8966	101297	79633828
Hypoglycaemic coma	500.07	17.81	115	9148	4645	79730480
Lactic acidosis	208.56	17.81	119	9144	70240	79664885
Diabetes mellitus inadequate control	138.87	17.81	64	9199	24200	79710925
Drug interaction	78.38	17.81	158	9105	415025	79320100
Abdominal distension	72.40	17.81	79	9184	119571	79615554
Pneumatosis intestinalis	67.21	17.81	26	9237	6371	79728754
Acute kidney injury	62.95	17.81	166	9097	519238	79215887
Hyperkalaemia	58.12	17.81	69	9194	114329	79620796
Blood glucose decreased	56.00	17.81	36	9227	26198	79708927

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BD17	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BF01	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Alpha glucosidase inhibitors
CHEBI has role	CHEBI:35526	antidiabetic
CHEBI has role	CHEBI:50627	Taka-amylase A inhibitor
CHEBI has role	CHEBI:67239	glucosidoinvertase inhibitor
CHEBI has role	CHEBI:176497	geroprotectors
FDA EPC	N0000175559	alpha-Glucosidase Inhibitor
FDA MoA	N0000000166	alpha Glucosidase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D065089	Glycoside Hydrolase Inhibitors

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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
Cirrhosis of liver	contraindication	19943007	DOID:5082
Inflammatory bowel disease	contraindication	24526004	DOID:0050589
Ulceration of colon	contraindication	46040000
Kidney disease	contraindication	90708001	DOID:557
Gastrointestinal obstruction	contraindication	126765001
Liver function tests abnormal	contraindication	166603001
Disease of liver	contraindication	235856003	DOID:409
Hypoglycemic disorder	contraindication	237630007
Surgical procedure	contraindication	387713003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.57	acidic
pKa2	11.95	acidic
pKa3	12.57	acidic
pKa4	13.14	acidic
pKa5	13.89	acidic
pKa6	6.99	Basic

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Maltase-glucoamylase, intestinal	Enzyme	O43451	MGA_HUMAN	INHIBITOR	IC50	5.70	WOMBAT-PK	CHEMBL
Pancreatic alpha-amylase	Enzyme	P04746	AMYP_HUMAN	INHIBITOR			CHEMBL	CHEMBL
Alpha-amylase 1	Enzyme	P04745	AMY1_HUMAN		IC50	6	CHEMBL
Lysosomal alpha-glucosidase	Enzyme	P10253	LYAG_HUMAN		IC50	5.30	CHEMBL
Alpha-amylase 1A	Enzyme	P0DUB6	AMY1A_HUMAN		IC50	6.30	CHEMBL
Sucrase-isomaltase, intestinal	Enzyme	P14410	SUIS_HUMAN		Ki	6.61	SCIENTIFIC LITERATURE
Sucrase-isomaltase, intestinal	Enzyme		SUIS_RAT		IC50	6.40	CHEMBL
Lysosomal alpha-glucosidase	Enzyme		LYAG_RAT		Ki	5.46	CHEMBL
Alpha-amylase	Enzyme		P94451_GEOSE		Ki	6.47	CHEMBL
Oligo-1,6-glucosidase	Enzyme		MALX3_YEAST		IC50	4.42	CHEMBL

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External reference:

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ID	Source
004299	NDDF
109077006	SNOMEDCT_US
136765	MMSL
151826	RXNORM
386965004	SNOMEDCT_US
4020940	VUID
4020940	VANDF
4117	MMSL
444254	PUBCHEM_CID
4527	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0140	TABLET	25 mg	ORAL	ANDA	10 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0140	TABLET	25 mg	ORAL	ANDA	10 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0141	TABLET	50 mg	ORAL	ANDA	10 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0141	TABLET	50 mg	ORAL	ANDA	10 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0142	TABLET	100 mg	ORAL	ANDA	10 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0142	TABLET	100 mg	ORAL	ANDA	10 sections
ACARBOSE	HUMAN PRESCRIPTION DRUG LABEL	1	11788-039	TABLET	25 mg	ORAL	ANDA	24 sections
ACARBOSE	HUMAN PRESCRIPTION DRUG LABEL	1	11788-040	TABLET	50 mg	ORAL	ANDA	24 sections
ACARBOSE	HUMAN PRESCRIPTION DRUG LABEL	1	11788-041	TABLET	100 mg	ORAL	ANDA	24 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-147	TABLET	25 mg	ORAL	ANDA	20 sections

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