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

Stem definition	Drug id	CAS RN
antihyperglycaemics	1314	10238-21-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: glyburide glibenclamide glicuformine	An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. Molecular weight: 494 Formula: C23H28ClN3O5S CLOGP: 4.24 LIPINSKI: 0 HAC: 8 HDO: 3 TPSA: 113.60 ALOGS: -5.38 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

glyburide
glibenclamide
glicuformine

An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Molecular weight: 494
Formula: C23H28ClN3O5S
CLOGP: 4.24
LIPINSKI: 0
HAC: 8
HDO: 3
TPSA: 113.60
ALOGS: -5.38
ROTB: 7

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
7	mg	O
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.58 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	82 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.08 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.82 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.20 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
May 24, 2018	EMA	Ammtek
May 1, 1984	FDA	SANOFI AVENTIS US

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	687.39	11.85	364	22527	59701	63406430
Blood glucose increased	357.34	11.85	272	22619	83484	63382647
Cardiac failure congestive	147.33	11.85	174	22717	92259	63373872
Lactic acidosis	140.70	11.85	114	22777	38173	63427958
Coronary artery disease	135.32	11.85	104	22787	32273	63433858
Myocardial infarction	134.92	11.85	173	22718	99720	63366411
Blood glucose decreased	133.30	11.85	87	22804	20865	63445266
Diabetes mellitus inadequate control	119.34	11.85	72	22819	15054	63451077
Glycosylated haemoglobin increased	97.76	11.85	59	22832	12339	63453792
Off label use	73.71	11.85	81	22810	674381	62791750
Hyperglycaemia	63.65	11.85	77	22814	41790	63424341
Hypoglycaemic coma	55.00	11.85	24	22867	2551	63463580
Contraindicated product administered	50.09	11.85	9	22882	217639	63248492
Alopecia	48.49	11.85	31	22860	337505	63128626
Glossodynia	46.79	11.85	5	22886	178871	63287260
Hyperkalaemia	42.81	11.85	73	22818	54130	63412001
Product use in unapproved indication	39.93	11.85	8	22883	179072	63287059
Pancreatitis	38.65	11.85	66	22825	48989	63417142
Drug ineffective	38.38	11.85	221	22670	1044544	62421587
Ketoacidosis	37.55	11.85	22	22869	4356	63461775
Torsade de pointes	37.30	11.85	34	22857	13317	63452814
Maternal exposure during pregnancy	36.24	11.85	17	22874	220045	63246086
Pericarditis	36.20	11.85	3	22888	131576	63334555
Synovitis	34.75	11.85	12	22879	186906	63279225
Blood glucose abnormal	34.38	11.85	26	22865	7866	63458265
Blood glucose fluctuation	34.08	11.85	21	22870	4555	63461576
Acute kidney injury	33.50	11.85	185	22706	263230	63202901
Diabetic ketoacidosis	31.62	11.85	38	22853	20467	63445664
Lower respiratory tract infection	29.30	11.85	6	22885	132301	63333830
Wound	27.83	11.85	12	22879	163251	63302880
Bradyarrhythmia	27.51	11.85	14	22877	2101	63464030
Blood urea increased	26.99	11.85	40	22851	26339	63439792
Arthropathy	26.87	11.85	27	22864	234765	63231366
Renal failure	26.55	11.85	98	22793	117554	63348577
Hypoglycaemic encephalopathy	26.23	11.85	8	22883	304	63465827
Transient ischaemic attack	26.13	11.85	48	22843	37705	63428426
Cerebrovascular accident	26.09	11.85	92	22799	107932	63358199
Intentional product use issue	25.95	11.85	7	22884	127885	63338246
Discomfort	25.94	11.85	14	22877	167360	63298771
Metabolic acidosis	25.94	11.85	53	22838	45016	63421115
Mucosal erosion	25.62	11.85	12	22879	1504	63464627
Ischaemic cardiomyopathy	25.43	11.85	14	22877	2463	63463668
Oedema peripheral	25.35	11.85	135	22756	189376	63276755
Diabetes mellitus	24.62	11.85	59	22832	55751	63410380
Hepatic steatosis	24.38	11.85	40	22851	28729	63437402
Infusion related reaction	24.03	11.85	32	22859	245489	63220642
Treatment failure	23.81	11.85	22	22869	199021	63267110
Asthenia	22.96	11.85	225	22666	383379	63082752
Treatment noncompliance	22.80	11.85	45	22846	37280	63428851
Hypoglycaemic unconsciousness	22.51	11.85	9	22882	768	63465363
Autoimmune myositis	22.35	11.85	6	22885	143	63465988
Pancreatitis acute	21.99	11.85	37	22854	27129	63439002
Carcinoid tumour of the stomach	21.67	11.85	6	22885	161	63465970
Lymphocyte count increased	21.11	11.85	14	22877	3444	63462687
Product use issue	20.32	11.85	30	22861	220490	63245641
Rhabdomyolysis	19.97	11.85	47	22844	43904	63422227
Blood pressure increased	18.72	11.85	111	22780	161951	63304180
Abdominal discomfort	18.42	11.85	57	22834	320828	63145303
Diabetic retinopathy	18.15	11.85	11	22880	2316	63463815
Hyperhidrosis	18.11	11.85	82	22809	107754	63358377
Swelling	17.96	11.85	46	22845	275332	63190799
Anaphylactic reaction	17.44	11.85	58	22833	66042	63400089
Macular oedema	17.39	11.85	13	22878	3864	63462267
Myocardial ischaemia	16.90	11.85	22	22869	12837	63453294
Peripheral swelling	16.90	11.85	45	22846	265897	63200234
Angina pectoris	16.87	11.85	35	22856	30043	63436088
Hypersensitivity	16.79	11.85	52	22839	292633	63173498
Enterochromaffin cell hyperplasia	16.65	11.85	4	22887	60	63466071
Wrong product administered	15.92	11.85	15	22876	6126	63460005
Weight decreased	15.88	11.85	161	22730	276637	63189494
Condition aggravated	15.79	11.85	83	22808	402134	63063997
Hepatic artery thrombosis	15.66	11.85	4	22887	78	63466053
Fatigue	15.65	11.85	226	22665	887802	62578329
Strongyloidiasis	15.48	11.85	8	22883	1240	63464891
Alcoholism	15.23	11.85	9	22882	1809	63464322
Fibromyalgia	15.22	11.85	5	22886	80415	63385716
Psoriatic arthropathy	15.16	11.85	7	22884	91513	63374618
Gait disturbance	14.88	11.85	115	22776	183063	63283068
Necrotising myositis	14.58	11.85	6	22885	551	63465580
General physical health deterioration	14.43	11.85	32	22859	201370	63264761
Therapeutic product effect decreased	14.42	11.85	30	22861	193157	63272974
Acute coronary syndrome	14.37	11.85	18	22873	10108	63456023
Lip discolouration	14.23	11.85	6	22885	586	63465545
Hypergastrinaemia	14.22	11.85	4	22887	114	63466017
Acute myocardial infarction	14.21	11.85	34	22857	32090	63434041
Dehydration	14.17	11.85	109	22782	173245	63292886
Blood creatinine increased	14.16	11.85	66	22825	87778	63378353
Hyperventilation	14.08	11.85	14	22877	6102	63460029
Drug hypersensitivity	14	11.85	61	22830	310626	63155505
Dizziness	13.58	11.85	224	22667	429701	63036430
Drug interaction	13.48	11.85	134	22757	228997	63237134
Oral mucosal discolouration	13.37	11.85	5	22886	356	63465775
Heart rate increased	13.18	11.85	68	22823	94170	63371961
Sinusitis	13.18	11.85	40	22851	226613	63239518
Fall	12.98	11.85	206	22685	392128	63074003
Drug abuse	12.89	11.85	5	22886	72513	63393618
Diabetic neuropathy	12.88	11.85	11	22880	3953	63462178
Irritable bowel syndrome	12.61	11.85	7	22884	82405	63383726
Blood potassium increased	12.32	11.85	23	22868	18286	63447845
Benzodiazepine drug level increased	12.30	11.85	4	22887	188	63465943
Atrioventricular block complete	12.25	11.85	15	22876	8236	63457895
Brain death	12.19	11.85	10	22881	3400	63462731
Blood creatine phosphokinase increased	12.18	11.85	31	22860	30399	63435732
Febrile neutropenia	12.03	11.85	15	22876	118434	63347697

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	1170.87	12.93	633	24584	54007	34877707
Blood glucose increased	241.28	12.93	268	24949	66450	34865264
Blood glucose decreased	183.45	12.93	116	25101	13121	34918593
Myocardial infarction	152.25	12.93	295	24922	120790	34810924
Coronary artery disease	137.83	12.93	172	25045	48133	34883581
Cardiac failure congestive	136.75	12.93	228	24989	83042	34848672
Lactic acidosis	97.84	12.93	123	25094	34649	34897065
Glycosylated haemoglobin increased	92.74	12.93	72	25145	11288	34920426
Off label use	89.42	12.93	103	25114	419421	34512293
Hyperglycaemia	81.24	12.93	120	25097	39360	34892354
Blood mercury abnormal	80.47	12.93	21	25196	213	34931501
5-hydroxyindolacetic acid in urine increased	78.52	12.93	21	25196	236	34931478
Counterfeit product administered	66.48	12.93	17	25200	158	34931556
Arteriosclerosis coronary artery	53.57	12.93	55	25162	12430	34919284
Blood pressure systolic increased	51.93	12.93	73	25144	22879	34908835
Cerebrovascular accident	51.38	12.93	156	25061	84655	34847059
Low density lipoprotein decreased	51.08	12.93	22	25195	1121	34930593
Product use in unapproved indication	45.65	12.93	14	25203	117485	34814229
Drug abuse	43.91	12.93	9	25208	99087	34832627
Product contamination	42.78	12.93	17	25200	705	34931009
Hepatic neoplasm	39.63	12.93	22	25195	1955	34929759
Myocardial ischaemia	37.36	12.93	54	25163	17354	34914360
Hyperkalaemia	36.85	12.93	122	25095	69267	34862447
Hyperoxaluria	36.49	12.93	10	25207	124	34931590
Mental status changes	36.30	12.93	83	25134	38000	34893714
Drug ineffective	35.84	12.93	189	25028	456562	34475152
Pyrexia	35.17	12.93	123	25094	332890	34598824
Platelet count normal	33.96	12.93	7	25210	21	34931693
Expired product administered	33.58	12.93	24	25193	3317	34928397
Hypoglycaemic coma	32.90	12.93	21	25196	2410	34929304
Acute kidney injury	32.37	12.93	349	24868	304639	34627075
Blood creatinine increased	32.34	12.93	145	25072	94831	34836883
Diabetes mellitus inadequate control	32.21	12.93	44	25173	13420	34918294
Metabolic acidosis	31.92	12.93	86	25131	43594	34888120
Haematocrit decreased	30.47	12.93	70	25147	32146	34899568
Ischaemic cardiomyopathy	28.96	12.93	29	25188	6360	34925354
Hypoglycaemic encephalopathy	28.58	12.93	10	25207	289	34931425
COVID-19	27.09	12.93	11	25206	77539	34854175
Pancreatitis	26.85	12.93	75	25142	38816	34892898
Neutropenia	25.80	12.93	46	25171	156732	34774982
Emotional distress	25.75	12.93	42	25175	14984	34916730
Febrile neutropenia	25.49	12.93	37	25180	136812	34794902
Congenital absence of bile ducts	24.94	12.93	4	25213	0	34931714
Oedema peripheral	23.85	12.93	158	25059	119654	34812060
Chest pain	23.35	12.93	164	25053	126598	34805116
Neoplasm	23.29	12.93	24	25193	5443	34926271
Scrotal oedema	22.81	12.93	15	25202	1811	34929903
Death	22.38	12.93	182	25035	397867	34533847
Otitis externa	21.46	12.93	12	25205	1081	34930633
Oliguria	20.98	12.93	28	25189	8352	34923362
Injury	20.73	12.93	46	25171	20641	34911073
Hirsutism	20.49	12.93	7	25210	188	34931526
Angina pectoris	20.20	12.93	59	25158	31304	34900410
Hyperlipidaemia	20.17	12.93	37	25180	14492	34917222
Hospitalisation	19.99	12.93	8	25209	56894	34874820
Quadriparesis	19.87	12.93	13	25204	1556	34930158
Asthenia	19.55	12.93	266	24951	244985	34686729
Pancreatitis acute	19.15	12.93	54	25163	28087	34903627
Condition aggravated	18.90	12.93	73	25144	192123	34739591
Deafness neurosensory	18.79	12.93	16	25201	2855	34928859
Cardiovascular disorder	18.45	12.93	29	25188	10027	34921687
Hepatic pain	18.19	12.93	12	25205	1456	34930258
Nephrocalcinosis	18.09	12.93	9	25208	639	34931075
Body temperature decreased	17.85	12.93	33	25184	13001	34918713
Weight decreased	17.83	12.93	200	25017	176101	34755613
Lacunar infarction	17.77	12.93	16	25201	3074	34928640
Treatment failure	17.35	12.93	6	25211	46691	34885023
Blood pH decreased	17.34	12.93	14	25203	2320	34929394
Diabetic neuropathy	17.12	12.93	18	25199	4179	34927535
Cardiac disorder	17.10	12.93	69	25148	43057	34888657
Dizziness	17.00	12.93	236	24981	218285	34713429
Thrombocytopenia	16.91	12.93	57	25160	156190	34775524
Poor dental condition	16.69	12.93	6	25211	188	34931526
Middle ear disorder	16.63	12.93	3	25214	3	34931711
Cutaneous lupus erythematosus	16.62	12.93	9	25208	761	34930953
Cataract	16.61	12.93	49	25168	26137	34905577
Vertigo	16.41	12.93	48	25169	25488	34906226
Renal injury	16.16	12.93	29	25188	11166	34920548
Areflexia	16.08	12.93	15	25202	3016	34928698
Peripheral vascular disorder	16.07	12.93	19	25198	5017	34926697
Blood glucose fluctuation	15.89	12.93	17	25200	4027	34927687
Renal tubular necrosis	15.86	12.93	35	25182	15645	34916069
Paratracheal lymphadenopathy	15.62	12.93	5	25212	109	34931605
Dyspepsia	15.56	12.93	60	25157	36672	34895042
Renal failure	15.49	12.93	153	25064	130404	34801310
Product complaint	15.24	12.93	20	25197	5870	34925844
Nasal neoplasm	15.17	12.93	5	25212	120	34931594
Haemolytic anaemia	14.94	12.93	27	25190	10452	34921262
Blood lactic acid increased	14.62	12.93	21	25196	6707	34925007
Drug intolerance	14.45	12.93	13	25204	59557	34872157
Pneumonia	14.44	12.93	180	25037	362447	34569267
Tympanic membrane disorder	14.35	12.93	4	25213	53	34931661
Hypophagia	14.34	12.93	44	25173	23978	34907736
Intentional overdose	14.34	12.93	66	25151	43608	34888106
Blood glucose	14.31	12.93	3	25214	10	34931704
Hyperlactacidaemia	14.24	12.93	14	25203	3002	34928712
Shock	14.17	12.93	44	25173	24135	34907579
C-reactive protein increased	14.11	12.93	11	25206	54087	34877627
Leukopenia	13.77	12.93	15	25202	62841	34868873
Fibrous histiocytoma	13.33	12.93	5	25212	177	34931537
Blood follicle stimulating hormone increased	13.30	12.93	5	25212	178	34931536
Transient ischaemic attack	13.28	12.93	47	25170	27566	34904148
Pemphigoid	13.22	12.93	23	25194	8643	34923071
Sensitisation	13.17	12.93	5	25212	183	34931531
Macrosomia	13.01	12.93	4	25213	76	34931638
Loss of consciousness	12.96	12.93	103	25114	82564	34849150

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	1754.83	11.40	903	39010	100691	79603784
Blood glucose increased	478.02	11.40	422	39491	114553	79589922
Myocardial infarction	267.35	11.40	391	39522	183738	79520737
Lactic acidosis	239.19	11.40	231	39682	70128	79634347
Coronary artery disease	237.86	11.40	223	39690	65251	79639224
Cardiac failure congestive	237.16	11.40	323	39590	142079	79562396
Blood glucose decreased	223.86	11.40	148	39765	26086	79678389
Glycosylated haemoglobin increased	162.71	11.40	108	39805	19152	79685323
Off label use	145.91	11.40	144	39769	907071	78797404
Hyperglycaemia	133.12	11.40	170	39743	70165	79634310
Diabetes mellitus inadequate control	108.55	11.40	93	39820	24171	79680304
Blood mercury abnormal	88.09	11.40	21	39892	213	79704262
5-hydroxyindolacetic acid in urine increased	85.97	11.40	21	39892	238	79704237
Drug ineffective	85.70	11.40	268	39645	1080645	78623830
Hyperkalaemia	83.62	11.40	180	39733	114218	79590257
Acute kidney injury	82.51	11.40	492	39421	518912	79185563
Product use in unapproved indication	78.62	11.40	15	39898	250344	79454131
Cerebrovascular accident	77.67	11.40	211	39702	155081	79549394
Counterfeit product administered	77.04	11.40	17	39896	118	79704357
Hypoglycaemic coma	69.64	11.40	38	39875	4722	79699753
Low density lipoprotein decreased	57.45	11.40	22	39891	1199	79703276
Metabolic acidosis	57.04	11.40	127	39786	82402	79622073
Hypoglycaemic encephalopathy	54.27	11.40	18	39895	643	79703832
Arteriosclerosis coronary artery	52.20	11.40	54	39859	17762	79686713
Blood creatinine increased	50.87	11.40	182	39731	154875	79549600
Hepatic neoplasm	49.15	11.40	27	39886	3399	79701076
Drug abuse	48.47	11.40	11	39902	162680	79541795
Alopecia	48.14	11.40	28	39885	231327	79473148
Myocardial ischaemia	47.18	11.40	61	39852	25458	79679017
Renal failure	46.80	11.40	212	39701	200756	79503719
Blood pressure systolic increased	46.19	11.40	103	39810	66883	79637592
Synovitis	45.29	11.40	10	39903	150724	79553751
Contraindicated product administered	40.70	11.40	14	39899	157524	79546951
Product contamination	39.64	11.40	17	39896	1243	79703232
Mental status changes	38.59	11.40	96	39817	66863	79637612
Pancreatitis	38.15	11.40	97	39816	68478	79635997
Blood glucose fluctuation	36.99	11.40	29	39884	6653	79697822
Condition aggravated	36.90	11.40	128	39785	500996	79203479
Haematocrit decreased	36.50	11.40	89	39824	61223	79643252
Treatment failure	36.37	11.40	20	39893	170466	79534009
Transient ischaemic attack	36.30	11.40	81	39832	52614	79651861
Platelet count normal	36.27	11.40	7	39906	22	79704453
Asthenia	35.62	11.40	402	39511	511287	79193188
Ischaemic cardiomyopathy	35.44	11.40	30	39883	7665	79696810
Pyrexia	34.53	11.40	199	39714	678510	79025965
Angina pectoris	33.94	11.40	78	39835	51654	79652821
Pemphigus	33.37	11.40	5	39908	99577	79604898
Arthropathy	33.34	11.40	24	39889	177087	79527388
Pericarditis	33.22	11.40	6	39907	104230	79600245
Oedema peripheral	33.13	11.40	228	39685	252060	79452415
Pancreatitis acute	32.78	11.40	75	39838	49529	79654946
Peripheral swelling	32.50	11.40	53	39860	269564	79434911
Drug hypersensitivity	32.22	11.40	63	39850	298853	79405622
Hyperoxaluria	31.41	11.40	10	39903	313	79704162
Hyperhidrosis	31.02	11.40	154	39759	151338	79553137
Maternal exposure during pregnancy	30.63	11.40	15	39898	136523	79567952
Blood urea increased	30.30	11.40	72	39841	48718	79655757
Scrotal oedema	29.89	11.40	15	39898	1570	79702905
Intentional product use issue	29.44	11.40	20	39893	152092	79552383
Torsade de pointes	29.38	11.40	42	39871	19270	79685205
Blood glucose abnormal	29.12	11.40	31	39882	10535	79693940
Glossodynia	28.81	11.40	8	39905	103329	79601146
Hypersensitivity	28.49	11.40	55	39858	262184	79442291
Hypophagia	28.23	11.40	67	39846	45300	79659175
Diabetic retinopathy	27.64	11.40	18	39895	3088	79701387
Renal injury	27.51	11.40	38	39875	16889	79687586
Chest pain	27.51	11.40	238	39675	282066	79422409
Neutropenia	27.38	11.40	65	39848	287645	79416830
Febrile neutropenia	27.28	11.40	46	39867	230953	79473522
Oliguria	27.09	11.40	37	39876	16272	79688203
Joint swelling	26.84	11.40	66	39847	288580	79415895
Lower respiratory tract infection	26.36	11.40	16	39897	129204	79575271
Infusion related reaction	26.14	11.40	47	39866	230190	79474285
Cardiac disorder	25.80	11.40	82	39831	65675	79638800
Rhabdomyolysis	25.65	11.40	111	39802	103020	79601455
Poor dental condition	25.62	11.40	10	39903	574	79703901
Product use issue	25.51	11.40	41	39872	209781	79494694
Angina unstable	25.23	11.40	36	39877	16491	79687984
Ketoacidosis	25.19	11.40	25	39888	7829	79696646
Blood pH decreased	25.12	11.40	20	39893	4691	79699784
Headache	24.70	11.40	209	39704	653563	79050912
Loss of consciousness	24.59	11.40	156	39757	167787	79536688
Helicobacter infection	24.54	11.40	3	39910	69701	79634774
COVID-19	24.09	11.40	26	39887	157648	79546827
Expired product administered	23.65	11.40	23	39890	7028	79697447
Bladder cancer	23.39	11.40	38	39875	19488	79684987
Rash	23.16	11.40	182	39731	578176	79126299
Peripheral vascular disorder	22.91	11.40	24	39889	8006	79696469
Emotional distress	22.71	11.40	57	39856	39912	79664563
Atrial fibrillation	22.60	11.40	173	39740	197713	79506762
Shock	22.57	11.40	60	39853	43488	79660987
Acute myocardial infarction	22.38	11.40	87	39826	76949	79627526
Weight decreased	21.99	11.40	273	39640	354925	79349550
Diabetic ketoacidosis	21.89	11.40	51	39862	34071	79670404
Cardiovascular disorder	21.48	11.40	35	39878	17990	79686485
Gastrointestinal disorder	21.17	11.40	18	39895	122187	79582288
Macular oedema	20.54	11.40	19	39894	5455	79699020
Bladder transitional cell carcinoma	20.32	11.40	14	39899	2636	79701839
Syncope	20.00	11.40	156	39757	179293	79525182
Discomfort	19.99	11.40	20	39893	125597	79578878
Therapeutic product effect incomplete	19.86	11.40	25	39888	141620	79562855
Dehydration	19.55	11.40	200	39713	247987	79456488
Nephrocalcinosis	19.27	11.40	11	39902	1491	79702984
Hepatic enzyme increased	19.22	11.40	39	39874	182571	79521904
Lacunar infarction	19.17	11.40	19	39894	5938	79698537
Hepatic pain	19.01	11.40	16	39897	4056	79700419
Cardiomegaly	18.70	11.40	41	39872	26311	79678164
Carcinoid tumour of the stomach	18.69	11.40	6	39907	193	79704282
Haemodialysis	18.64	11.40	33	39880	18135	79686340
Ventricular hypertrophy	18.49	11.40	20	39893	6918	79697557
Diabetes mellitus	18.45	11.40	83	39830	78307	79626168
Body temperature decreased	18.42	11.40	46	39867	32099	79672376
Blood pressure increased	17.94	11.40	173	39740	211187	79493288
Hyperlipidaemia	17.84	11.40	40	39873	26053	79678422
Hospitalisation	17.43	11.40	13	39900	94223	79610252
Coronary artery occlusion	17.26	11.40	29	39884	15286	79689189
Neoplasm	17.18	11.40	22	39891	9094	79695381
Rheumatoid arthritis	16.87	11.40	51	39862	208419	79496056
Blood glucose	16.83	11.40	4	39909	40	79704435
Wound	16.82	11.40	20	39893	116159	79588316
Bradyarrhythmia	16.75	11.40	15	39898	4131	79700344
Diabetic neuropathy	16.71	11.40	18	39895	6198	79698277
Renal tubular necrosis	16.69	11.40	38	39875	25001	79679474
Hepatic steatosis	16.61	11.40	49	39864	37689	79666786
Haemolytic anaemia	16.55	11.40	31	39882	17789	79686686
Fear	16.51	11.40	35	39878	21951	79682524
Hyperlactacidaemia	16.46	11.40	17	39896	5578	79698897
Musculoskeletal stiffness	16.27	11.40	40	39873	174968	79529507
Autoimmune myositis	16.22	11.40	6	39907	297	79704178
Unresponsive to stimuli	16.20	11.40	63	39850	55725	79648750
Hypoglycaemic unconsciousness	16.09	11.40	9	39904	1174	79703301
General physical health deterioration	16.02	11.40	77	39836	275161	79429314
Metabolic alkalosis	15.73	11.40	15	39898	4474	79700001
Middle ear disorder	15.65	11.40	3	39910	9	79704466
Irritable bowel syndrome	15.28	11.40	6	39907	62235	79642240
Intentional overdose	15.24	11.40	98	39815	105862	79598613
Paratracheal lymphadenopathy	15.01	11.40	5	39908	181	79704294
Mucosal erosion	14.90	11.40	11	39902	2307	79702168
Areflexia	14.83	11.40	16	39897	5518	79698957
Swelling	14.83	11.40	57	39856	216654	79487821
Quadriparesis	14.81	11.40	13	39900	3488	79700987
Cataract	14.79	11.40	66	39847	62054	79642421
Hirsutism	14.79	11.40	9	39904	1373	79703102
Pemphigoid	14.67	11.40	27	39886	15288	79689187
Otitis externa	14.60	11.40	11	39902	2379	79702096
Fibromyalgia	14.53	11.40	7	39906	64333	79640142
Brain death	14.50	11.40	16	39897	5661	79698814
Lymphocyte count decreased	14.48	11.40	3	39910	47286	79657189
Nasal neoplasm	14.32	11.40	5	39908	209	79704266
Dilatation atrial	14.18	11.40	13	39900	3691	79700784
Renal cyst	14.14	11.40	26	39887	14706	79689769
Enterochromaffin cell hyperplasia	13.90	11.40	4	39909	88	79704387
Mobility decreased	13.81	11.40	25	39888	122150	79582325
Deafness neurosensory	13.56	11.40	17	39896	6881	79697594
Chronic obstructive pulmonary disease	13.53	11.40	81	39832	85338	79619137
Blood creatine phosphokinase increased	13.38	11.40	67	39846	66023	79638452
Leukocytosis	13.38	11.40	50	39863	43405	79661070
Lung infiltration	13.35	11.40	33	39880	22879	79681596
Bundle branch block left	13.24	11.40	22	39891	11491	79692984
Fatigue	13.08	11.40	360	39553	929367	78775108
Depressed level of consciousness	13.05	11.40	88	39825	96564	79607911
Abdominal discomfort	12.98	11.40	73	39840	250654	79453821
Blood lactic acid increased	12.88	11.40	23	39890	12721	79691754
Arthralgia	12.88	11.40	205	39708	571598	79132877
Treatment noncompliance	12.79	11.40	56	39857	52212	79652263
Sedation	12.74	11.40	5	39908	51890	79652585
Anhedonia	12.71	11.40	25	39888	14873	79689602
Insulin C-peptide increased	12.66	11.40	4	39909	122	79704353
Accidental exposure to product by child	12.65	11.40	11	39902	2915	79701560
Arteriosclerosis	12.53	11.40	28	39885	18199	79686276
Stomatitis	12.53	11.40	35	39878	146722	79557753
Mitral valve incompetence	12.49	11.40	37	39876	28528	79675947
Drug ineffective for unapproved indication	12.48	11.40	5	39908	51233	79653242
Drug resistance	12.28	11.40	3	39910	42210	79662265
Duodenal ulcer	12.22	11.40	26	39887	16343	79688132
Alcoholism	12.22	11.40	12	39901	3711	79700764
Leukopenia	12.16	11.40	25	39888	116488	79587987
Tricuspid valve incompetence	12.14	11.40	29	39884	19683	79684792
Electrocardiogram T wave peaked	12.13	11.40	7	39906	968	79703507
Halo vision	12.11	11.40	6	39907	611	79703864
Blood follicle stimulating hormone increased	12.04	11.40	5	39908	337	79704138
Myiasis	11.98	11.40	3	39910	38	79704437
Hepatomegaly	11.87	11.40	28	39885	18846	79685629
Oral mucosal discolouration	11.85	11.40	5	39908	351	79704124
Mitral valve disease	11.81	11.40	11	39902	3186	79701289
Psoriatic arthropathy	11.75	11.40	13	39900	77986	79626489
Arrhythmia	11.63	11.40	61	39852	61211	79643264
Full blood count abnormal	11.53	11.40	3	39910	40471	79664004
Drug-disease interaction	11.43	11.40	7	39906	1080	79703395

FDA Adverse Event Reporting System (Pediatric)

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
Insulin resistance	24.06	8.84	3	4	3	89782

Pharmacologic Action:

Source	Code	Description
ATC	A10BB01	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sulfonylureas
FDA CS	M0020795	Sulfonylurea Compounds
CHEBI has role	CHEBI:35526	antidiabetic
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:77194	ATP:pantothenate 4-phosphotransferase inhibitor
CHEBI has role	CHEBI:131770	CFTR inhibitors
MeSH PA	D007004	Hypoglycemic Agents
FDA EPC	N0000175608	Sulfonylurea

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
Neonatal diabetes mellitus	indication	49817004	DOID:11717
Alcoholism	contraindication	7200002
Asthenia	contraindication	13791008
Myocardial infarction	contraindication	22298006	DOID:5844
Acute vomiting	contraindication	23971007
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Dehydration	contraindication	34095006
Infectious disease	contraindication	40733004
Hepatic porphyria	contraindication	55056006	DOID:3133
Ketoacidosis	contraindication	56051008
Acute nephropathy	contraindication	58574008
Metabolic acidosis	contraindication	59455009
Hepatic failure	contraindication	59927004
Hemolytic anemia	contraindication	61261009	DOID:583
Glucose-6-phosphate dehydrogenase deficiency anemia	contraindication	62403005
Hypopituitarism	contraindication	74728003	DOID:9406
Cardiogenic shock	contraindication	89138009
Kidney disease	contraindication	90708001	DOID:557
Lactic acidosis	contraindication	91273001	DOID:3650
Cobalamin deficiency	contraindication	190634004
Decompensated cardiac failure	contraindication	195111005
Disease of liver	contraindication	235856003	DOID:409
Hypoglycemic disorder	contraindication	237630007
Sepsis syndrome	contraindication	238150007
Primary adrenocortical insufficiency	contraindication	373662000
Adrenal cortical hypofunction	contraindication	386584007	DOID:10493
Fever	contraindication	386661006
Surgical procedure	contraindication	387713003
Severe diarrhea	contraindication	409587002
Traumatic injury	contraindication	417746004
Fever greater than 100.4 Fahrenheit	contraindication	426000000
Severe Autonomic Insufficiency	contraindication
Severe Hypoxemia	contraindication
Radiography with IV Iodinated Contrast Agent	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	5.31	acidic
pKa2	12.71	acidic

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
Sulfonylurea receptor 1, Kir6.2	Ion channel	Q09428 Q14654	ABCC8_HUMAN KCJ11_HUMAN	BLOCKER	Kd	9.52	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Bile salt export pump	Transporter	O95342	ABCBB_HUMAN		IC50	5.28	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN	INHIBITOR	IC50	5.80	DRUG MATRIX
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN		Ki	6.18	CHEMBL
Cystic fibrosis transmembrane conductance regulator	Ion channel	P13569	CFTR_HUMAN	BLOCKER	Ki	4.66	IUPHAR
Sulfonylurea receptor 2, Kir6.2	Ion channel	O60706 Q14654	ABCC9_HUMAN KCJ11_HUMAN	BLOCKER	Ki	8.21	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.13	CHEMBL
NACHT, LRR and PYD domains-containing protein 3	Unclassified	Q96P20	NLRP3_HUMAN		IC50	4.92	CHEMBL
CDGSH iron-sulfur domain-containing protein 1	Unclassified	Q9NZ45	CISD1_HUMAN		Ki	5.78	CHEMBL
ATP-sensitive inward rectifier potassium channel 11	Ion channel		KCJ11_MOUSE	BLOCKER	IC50	5.70	IUPHAR
NACHT, LRR and PYD domains-containing protein 3	Unclassified		NLRP3_MOUSE		IC50	5	CHEMBL
Sur1-Trpm4; Sulfonylurea receptor 1 - Transient receptor potential melastatin 4	Ion channel		ABCC8_RAT TRPM4_RAT	INHIBITOR	EC50	7.32	SCIENTIFIC LITERATURE
Bile salt export pump	Transporter		ABCBB_RAT		IC50	5.55	CHEMBL

External reference:

ID	Source
4018078	VUID
N0000146417	NUI
D00336	KEGG_DRUG
4018078	VANDF
CHEBI:5441	CHEBI
GBM	PDB_CHEM_ID
CHEMBL472	ChEMBL_ID
2414	IUPHAR_LIGAND_ID
DB01016	DRUGBANK_ID
4815	RXNORM
4790	MMSL
597	MMSL
d00248	MMSL
000912	NDDF
384978002	SNOMEDCT_US
80870001	SNOMEDCT_US
C0017628	UMLSCUI
D005905	MESH_DESCRIPTOR_UI
2386	INN_ID
3488	PUBCHEM_CID
SX6K58TVWC	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-0341	TABLET	1.50 mg	ORAL	NDA	26 sections
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-0341	TABLET	1.50 mg	ORAL	NDA	26 sections
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-0352	TABLET	3 mg	ORAL	NDA	26 sections
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-0352	TABLET	3 mg	ORAL	NDA	26 sections
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3449	TABLET	6 mg	ORAL	NDA	26 sections
Glynase	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3449	TABLET	6 mg	ORAL	NDA	26 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8034	TABLET	1.50 mg	ORAL	ANDA	24 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8035	TABLET	3 mg	ORAL	ANDA	24 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8036	TABLET	6 mg	ORAL	ANDA	24 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8342	TABLET	1.25 mg	ORAL	ANDA	26 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8343	TABLET	2.50 mg	ORAL	ANDA	26 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-8344	TABLET	5 mg	ORAL	ANDA	26 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9364	TABLET	5 mg	ORAL	NDA AUTHORIZED GENERIC	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9433	TABLET	2.50 mg	ORAL	NDA AUTHORIZED GENERIC	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9477	TABLET	1.25 mg	ORAL	NDA AUTHORIZED GENERIC	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1742	TABLET	1.25 mg	ORAL	ANDA	22 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1743	TABLET	2.50 mg	ORAL	ANDA	22 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1744	TABLET	5 mg	ORAL	ANDA	22 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0929	TABLET	1.25 mg	ORAL	ANDA	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0930	TABLET	2.50 mg	ORAL	ANDA	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0931	TABLET	5 mg	ORAL	ANDA	25 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9918	TABLET	1.50 mg	ORAL	ANDA	20 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9919	TABLET	3 mg	ORAL	ANDA	20 sections
Glyburide	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9920	TABLET	6 mg	ORAL	ANDA	20 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2751	TABLET, FILM COATED	1.25 mg	ORAL	ANDA	27 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2751	TABLET, FILM COATED	1.25 mg	ORAL	ANDA	27 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2752	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	27 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2752	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	27 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2753	TABLET, FILM COATED	5 mg	ORAL	ANDA	27 sections
Glyburide and Metformin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0228-2753	TABLET, FILM COATED	5 mg	ORAL	ANDA	27 sections