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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:

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

Approvals:

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

FDA Adverse Event Reporting System (Female)

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
Hyperglycaemia	45.90	22.74	33	5052	41834	63442103
Hyperkalaemia	44.59	22.74	36	5049	54167	63429770
Peripheral artery haematoma	38.51	22.74	6	5079	39	63483898
Ketoacidosis	37.99	22.74	14	5071	4364	63479573
Intestinal transit time abnormal	35.37	22.74	6	5079	70	63483867
Glycosylated haemoglobin increased	35.18	22.74	18	5067	12380	63471557
Mucosal erosion	34.24	22.74	10	5075	1506	63482431
Urine calcium/creatinine ratio increased	32.63	22.74	6	5079	114	63483823
Urinary incontinence	32.28	22.74	24	5061	31990	63451947
Insulin-like growth factor decreased	30.81	22.74	7	5078	389	63483548
Cold sweat	29.92	22.74	16	5069	12031	63471906
Bite	29.46	22.74	7	5078	474	63483463
Unresponsive to stimuli	28.95	22.74	23	5062	33793	63450144
Blood sodium increased	28.45	22.74	10	5075	2722	63481215
Urethral caruncle	27.78	22.74	5	5080	84	63483853
Protein urine present	26.88	22.74	12	5073	6108	63477829
Peptic ulcer	26.77	22.74	11	5074	4576	63479361
Cardiogenic shock	26.47	22.74	17	5068	17915	63466022
Cell death	25.11	22.74	9	5076	2592	63481345
Blood glucose increased	24.77	22.74	32	5053	83724	63400213
Melaena	24.60	22.74	20	5065	30345	63453592
Neuroglycopenia	24.37	22.74	6	5079	472	63483465
Dizziness	23.81	22.74	82	5003	429843	63054094
Stevens-Johnson syndrome	23.59	22.74	18	5067	24932	63459005
Drug ineffective	23.19	22.74	30	5055	1044735	62439202

FDA Adverse Event Reporting System (Male)

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
Quadriparesis	29.26	20.87	10	4477	1559	34950885
Abdominal distension	28.03	20.87	36	4451	58456	34893988
Mouth swelling	27.62	20.87	10	4477	1846	34950598
Mast cell degranulation present	26.41	20.87	5	4482	68	34952376
Diabetic metabolic decompensation	24.37	20.87	9	4478	1757	34950687
Acute kidney injury	23.52	20.87	89	4398	304899	34647545
Metabolic acidosis	22.69	20.87	28	4459	43652	34908792
Acetonaemia	22.38	20.87	5	4482	159	34952285
Monoparesis	21.89	20.87	9	4478	2337	34950107
Ketosis	21.32	20.87	6	4481	492	34951952

FDA Adverse Event Reporting System (Geriatric)

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
Cerebral infarction	54.47	17.81	44	9219	45632	79689493
Diabetic ketoacidosis	51.92	17.81	38	9225	34084	79701041
Hyperoxaluria	51.53	17.81	11	9252	312	79734813
Ketoacidosis	45.80	17.81	21	9242	7833	79727292
Glycosylated haemoglobin increased	45.03	17.81	28	9235	19232	79715893
Unresponsive to stimuli	44.93	17.81	43	9220	55745	79679380
Speech disorder	38.33	17.81	39	9224	54406	79680719
Hyperglycaemia	38.32	17.81	44	9219	70291	79664834
Albumin urine present	33.56	17.81	9	9254	682	79734443
Intestinal transit time abnormal	33.14	17.81	6	9257	70	79735055
Metabolic acidosis	32.70	17.81	44	9219	82485	79652640
Blood glucose abnormal	31.58	17.81	18	9245	10548	79724577
Peripheral artery haematoma	29.88	17.81	6	9257	125	79735000
Urine calcium/creatinine ratio increased	29.15	17.81	6	9257	142	79734983
Hepatic function abnormal	29.00	17.81	39	9224	73068	79662057
Cold sweat	28.84	17.81	21	9242	18678	79716447
Arthralgia	27.78	17.81	16	9247	571787	79163338
Hyperhidrosis	27.67	17.81	57	9206	151435	79583690
Flatulence	27.19	17.81	29	9234	42695	79692430
Drug ineffective	27.13	17.81	53	9210	1080860	78654265
Mast cell degranulation present	26.91	17.81	5	9258	68	79735057
Urethral caruncle	26.51	17.81	5	9258	74	79735051
Bite	26.02	17.81	7	9256	537	79734588
Insulin-like growth factor decreased	25.52	17.81	7	9256	578	79734547
Melaena	24.94	17.81	33	9230	60857	79674268
Urinary incontinence	24.69	17.81	27	9236	40882	79694243
Acetonaemia	24.15	17.81	6	9257	336	79734789
Chronic gastritis	24.10	17.81	11	9252	4057	79731068
Portal venous gas	23.04	17.81	6	9257	406	79734719
Lacunar infarction	22.94	17.81	12	9251	5945	79729180
Mucosal erosion	22.86	17.81	9	9254	2309	79732816
Anuria	22.49	17.81	19	9244	20944	79714181
Peptic ulcer	22.44	17.81	12	9251	6211	79728914
Quadriparesis	22.44	17.81	10	9253	3491	79731634
Monoparesis	22.41	17.81	10	9253	3501	79731624
Neuroglycopenia	22.08	17.81	6	9257	478	79734647
Diabetic ketosis	21.89	17.81	6	9257	494	79734631
Protein urine present	21.88	17.81	14	9249	10098	79725027
Blood glucose fluctuation	21.64	17.81	12	9251	6670	79728455
Glucose urine present	21.56	17.81	8	9255	1748	79733377
Dizziness	21.56	17.81	119	9144	526322	79208803
Altered state of consciousness	21.51	17.81	26	9237	43796	79691329
Ketosis	20.99	17.81	7	9256	1119	79734006
Blood glucose increased	20.68	17.81	43	9220	114932	79620193
Diabetic metabolic decompensation	19.71	17.81	9	9254	3323	79731802
Chronic kidney disease	18.57	17.81	30	9233	66124	79669001
Hypoproteinaemia	18.05	17.81	9	9254	4037	79731088

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
FDA MoA	N0000000166	alpha Glucosidase Inhibitors
FDA EPC	N0000175559	alpha-Glucosidase Inhibitor
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
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D065089	Glycoside Hydrolase Inhibitors
MeSH PA	D007004	Hypoglycemic Agents

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

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
Traumatic injury	contraindication	417746004
Fever greater than 100.4 Fahrenheit	contraindication	426000000
Malabsorption States	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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
Pancreatic alpha-amylase	Enzyme		AMYP_PIG		IC50	4.45	CHEMBL

External reference:

ID	Source
4020940	VUID
N0000148420	NUI
D00216	KEGG_DRUG
151826	RXNORM
C0050393	UMLSCUI
CHEBI:84363	CHEBI
CHEMBL1566	ChEMBL_ID
CHEMBL404271	ChEMBL_ID
D020909	MESH_DESCRIPTOR_UI
DB00284	DRUGBANK_ID
6791	IUPHAR_LIGAND_ID
4527	INN_ID
T58MSI464G	UNII
444254	PUBCHEM_CID
109077006	SNOMEDCT_US
386965004	SNOMEDCT_US
4020940	VANDF
136765	MMSL
4117	MMSL
4644	MMSL
d03846	MMSL
004299	NDDF

Pharmaceutical products:

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
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-147	TABLET	25 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-147	TABLET	25 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-148	TABLET	50 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-148	TABLET	50 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-148	TABLET	50 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-149	TABLET	100 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-149	TABLET	100 mg	ORAL	ANDA	20 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	23155-149	TABLET	100 mg	ORAL	ANDA	20 sections
acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	42291-130	TABLET	25 mg	ORAL	ANDA	22 sections
acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	42291-131	TABLET	50 mg	ORAL	ANDA	22 sections
acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	42291-132	TABLET	100 mg	ORAL	ANDA	22 sections
Precose	HUMAN PRESCRIPTION DRUG LABEL	1	43353-908	TABLET	50 mg	ORAL	NDA	22 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	43353-951	TABLET	50 mg	ORAL	NDA authorized generic	21 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4115	TABLET	50 mg	ORAL	NDA authorized generic	22 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4116	TABLET	100 mg	ORAL	NDA authorized generic	22 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4952	TABLET	50 mg	ORAL	ANDA	17 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4952	TABLET	50 mg	ORAL	ANDA	17 sections
ACARBOSE	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5088	TABLET	100 mg	ORAL	ANDA	24 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5829	TABLET	100 mg	ORAL	ANDA	17 sections
Precose	HUMAN PRESCRIPTION DRUG LABEL	1	50419-861	TABLET	50 mg	ORAL	NDA	22 sections