Scroll

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)	1	Benet LZ, Broccatelli F, Oprea TI
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

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	415.05	23.32	159	4094	53422	50547449
Hypoglycaemic coma	222.01	23.32	49	4204	2284	50598587
Lactic acidosis	130.09	23.32	61	4192	33294	50567577
Acute kidney injury	55.36	23.32	81	4172	227977	50372894
Diabetes mellitus inadequate control	54.15	23.32	25	4228	13120	50587751
Blood glucose decreased	52.10	23.32	27	4226	18184	50582687
Hyperglycaemia	46.28	23.32	32	4221	36373	50564498
Abdominal distension	45.13	23.32	42	4211	72861	50528010
Drug interaction	44.26	23.32	68	4185	199553	50401318
Pneumatosis intestinalis	43.07	23.32	13	4240	2090	50598781
Peripheral artery haematoma	38.22	23.32	6	4247	39	50600832
Glycosylated haemoglobin increased	37.02	23.32	18	4235	10588	50590283
Mucosal erosion	35.39	23.32	10	4243	1277	50599594
Ketoacidosis	35.21	23.32	13	4240	3882	50596989
Intestinal transit time abnormal	35.16	23.32	6	4247	69	50600802
Drug ineffective	32.92	23.32	14	4239	819319	49781552
Urine calcium/creatinine ratio increased	32.35	23.32	6	4247	114	50600757
Insulin-like growth factor decreased	30.88	23.32	7	4246	367	50600504
Bite	30.75	23.32	7	4246	374	50600497
Blood sodium increased	29.24	23.32	10	4243	2392	50598479
Diabetic ketoacidosis	28.24	23.32	18	4235	17854	50583017
Urethral caruncle	27.54	23.32	5	4248	84	50600787
Urinary incontinence	27.22	23.32	21	4232	28187	50572684
Hyperkalaemia	26.50	23.32	26	4227	48063	50552808
Cell death	26.10	23.32	9	4244	2206	50598665
Stevens-Johnson syndrome	25.03	23.32	18	4235	21734	50579137
Pain	24.65	23.32	9	4244	578894	50021977
Hyperleukocytosis	24.26	23.32	6	4247	458	50600413

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	182.15	21.05	100	3826	48246	29522355
Hypoglycaemic coma	153.02	21.05	39	3887	2124	29568477
Lactic acidosis	85.49	21.05	52	3874	30195	29540406
Diabetes mellitus inadequate control	56.53	21.05	29	3897	12105	29558496
Hyperoxaluria	53.42	21.05	10	3916	123	29570478
Cerebral infarction	39.81	21.05	30	3896	24645	29545956
Albumin urine present	37.88	21.05	9	3917	364	29570237
Speech disorder	34.45	21.05	27	3899	23489	29547112
Drug interaction	33.63	21.05	78	3848	197307	29373294
Quadriparesis	31.41	21.05	10	3916	1209	29569392
Mouth swelling	28.89	21.05	10	3916	1566	29569035
Acute kidney injury	27.25	21.05	87	3839	265180	29305421
Mast cell degranulation present	26.60	21.05	5	3921	63	29570538
Diabetic metabolic decompensation	26.02	21.05	9	3917	1407	29569194
Pneumatosis intestinalis	25.34	21.05	11	3915	3158	29567443
Metabolic acidosis	25.31	21.05	28	3898	37634	29532967
Monoparesis	23.42	21.05	9	3917	1894	29568707
Acetonaemia	22.75	21.05	5	3921	142	29570459

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	533.71	19.63	247	7725	89645	64401115
Hypoglycaemic coma	368.31	19.63	89	7883	4185	64486575
Lactic acidosis	195.04	19.63	111	7861	61299	64429461
Diabetes mellitus inadequate control	96.99	19.63	49	7923	21272	64469488
Acute kidney injury	67.71	19.63	162	7810	449078	64041682
Drug interaction	67.31	19.63	142	7830	361941	64128819
Pneumatosis intestinalis	59.83	19.63	23	7949	5206	64485554
Abdominal distension	55.90	19.63	64	7908	95930	64394830
Hyperoxaluria	52.78	19.63	11	7961	260	64490500
Blood glucose decreased	50.65	19.63	33	7939	23090	64467670
Glycosylated haemoglobin increased	45.56	19.63	27	7945	15992	64474768
Ketoacidosis	44.08	19.63	20	7952	6843	64483917
Hyperkalaemia	42.11	19.63	57	7915	101072	64389688
Hyperglycaemia	39.50	19.63	43	7929	60925	64429835
Cerebral infarction	37.73	19.63	35	7937	41009	64449751
Speech disorder	36.44	19.63	37	7935	48404	64442356
Peripheral artery haematoma	35.16	19.63	6	7966	45	64490715
Diabetic ketoacidosis	34.53	19.63	29	7943	29816	64460944
Metabolic acidosis	34.21	19.63	43	7929	70915	64419845
Albumin urine present	33.40	19.63	9	7963	652	64490108
Drug ineffective	33.34	19.63	33	7939	840214	63650546
Intestinal transit time abnormal	32.85	19.63	6	7966	69	64490691
Urine calcium/creatinine ratio increased	28.78	19.63	6	7966	142	64490618
Bite	27.25	19.63	7	7965	421	64490339
Mast cell degranulation present	26.95	19.63	5	7967	63	64490697
Urethral caruncle	26.20	19.63	5	7967	74	64490686
Insulin-like growth factor decreased	25.41	19.63	7	7965	551	64490209
Acetonaemia	25.12	19.63	6	7966	267	64490493
Mucosal erosion	23.90	19.63	9	7963	1925	64488835
Quadriparesis	23.79	19.63	10	7962	2847	64487913
Portal venous gas	23.61	19.63	6	7966	346	64490414
Monoparesis	23.54	19.63	10	7962	2924	64487836
Diabetic ketosis	23.42	19.63	6	7966	357	64490403
Anuria	23.12	19.63	19	7953	18945	64471815
Arthralgia	23.10	19.63	13	7959	442247	64048513
Lacunar infarction	23.07	19.63	12	7960	5520	64485240
Chronic gastritis	22.58	19.63	10	7962	3230	64487530
Diabetic metabolic decompensation	20.90	19.63	9	7963	2719	64488041
Unresponsive to stimuli	20.34	19.63	28	7944	50365	64440395
Blood glucose increased	19.93	19.63	40	7932	98033	64392727

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
136765	MMSL
4117	MMSL
4644	MMSL
d03846	MMSL
004299	NDDF
4020940	VANDF
109077006	SNOMEDCT_US
386965004	SNOMEDCT_US

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	0054-0141	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	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	23155-148	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	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	50090-5088	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
Precose	HUMAN PRESCRIPTION DRUG LABEL	1	50419-862	TABLET	100 mg	ORAL	NDA	22 sections
Precose	HUMAN PRESCRIPTION DRUG LABEL	1	50419-863	TABLET	25 mg	ORAL	NDA	22 sections
Precose	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5831	TABLET	25 mg	ORAL	NDA	22 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5945	TABLET	25 mg	ORAL	ANDA	19 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	63629-5697	TABLET	25 mg	ORAL	ANDA	17 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	63629-5698	TABLET	50 mg	ORAL	ANDA	17 sections
Acarbose	HUMAN PRESCRIPTION DRUG LABEL	1	64380-758	TABLET	25 mg	ORAL	ANDA	17 sections