glibenclamide ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihyperglycaemics 1314 10238-21-8

Description:

MoleculeDescription

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:

DoseUnitRoute
7 mg O
10 mg O

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
May 24, 2018 EMA Ammtek
May 1, 1984 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Insulin resistance 24.06 8.84 3 4 3 89782

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 1, Kir6.2 Ion channel BLOCKER Kd 9.52 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Bile salt export pump Transporter IC50 5.28 CHEMBL
Cytochrome P450 2C9 Enzyme INHIBITOR IC50 5.80 DRUG MATRIX
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor Ki 6.18 CHEMBL
Cystic fibrosis transmembrane conductance regulator Ion channel BLOCKER Ki 4.66 IUPHAR
Sulfonylurea receptor 2, Kir6.2 Ion channel BLOCKER Ki 8.21 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.13 CHEMBL
NACHT, LRR and PYD domains-containing protein 3 Unclassified IC50 4.92 CHEMBL
CDGSH iron-sulfur domain-containing protein 1 Unclassified Ki 5.78 CHEMBL
ATP-sensitive inward rectifier potassium channel 11 Ion channel BLOCKER IC50 5.70 IUPHAR
NACHT, LRR and PYD domains-containing protein 3 Unclassified IC50 5 CHEMBL
Sur1-Trpm4; Sulfonylurea receptor 1 - Transient receptor potential melastatin 4 Ion channel INHIBITOR EC50 7.32 SCIENTIFIC LITERATURE
Bile salt export pump Transporter IC50 5.55 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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