repaglinide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antihyperglycaemics 2366 135062-02-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • repaglinide
  • (S)-(+)-Repaglinide
  • prandin
  • enyglid
  • surepost
  • Molecular weight: 452.60
  • Formula: C27H36N2O4
  • CLOGP: 5.66
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 78.87
  • ALOGS: -5.19
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 1.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.47 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 56 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.35 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7.80 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) 0.87 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.04 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.231 High 0.80
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.832 High 0.80
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 59.293 10^-6 cm/s High 0.80
dh-clint Dog hepatocyte intrinsic clearance 12.246 uL/min/10^6 cells High 0.80
dppb Dog plasma protein binding (% unbound) 0.980 % High 0.80
fcs-ppb Fetal calf serum protein binding (% unbound) 2.070 % High 0.80
herg hERG pIC50 4.750 pIC50 High 0.80
hh-clint Human hepatocyte intrinsic clearance 15.276 uL/min/10^6 cells High 0.80
hlm-clint Human liver microsomal intrinsic clearance 49.204 uL/min/mg protein High 0.80
hppb Human plasma protein binding (% unbound) 0.750 % High 0.80
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK,TGFBR1 25
kinase-selectivity-class AXL,BRAF,CAMK2D,CDK9,EIF2AK3,GRK2,MAPK7,STK33,TTK 9
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 9.099 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.212 High 0.80
mh-clint Mouse hepatocyte intrinsic clearance 48.865 High 0.80
mppb Mouse plasma protein binding (% unbound) 1.160 High 0.80
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 51.523 High 0.80
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 2.010 % High 0.80
rat-kpuu-brain Rat brain Kpuu 0.019 % High 1
rh-clint Rat hepatocyte intrinsic clearance 38.726 uL/min/10^6 cells High 0.80
rh-fuinc Rat hepatocyte fraction unbound in incubation 30.340 % High 0.80
rppb Rat plasma protein binding (% unbound) 1.110 % High 0.80
solubility-dd Solubility at pH 7.4 in DMSO 855.067 uM High 0.80

Approvals:

DateAgencyCompanyOrphan
Dec. 22, 1997 FDA NOVO NORDISK INC

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 830.39 18.26 311 10393 69537 90548206
Lactic acidosis 485.78 18.26 193 10511 50270 90567473
Acute kidney injury 446.43 18.26 339 10365 320048 90297695
Hypoglycaemic coma 228.21 18.26 56 10648 2934 90614809
Hyperkalaemia 188.40 18.26 109 10595 64855 90552888
Drug interaction 145.69 18.26 171 10533 276282 90341461
Diabetes mellitus inadequate control 99.06 18.26 47 10657 18637 90599106
Pemphigoid 81.39 18.26 33 10671 8993 90608750
Diabetic ketoacidosis 78.88 18.26 44 10660 24363 90593380
Euglycaemic diabetic ketoacidosis 74.79 18.26 28 10676 6173 90611570
Hyperglycaemia 70.60 18.26 54 10650 50916 90566827
Sopor 70.43 18.26 41 10663 24603 90593140
Rhabdomyolysis 61.71 18.26 50 10654 51206 90566537
Product prescribing error 60.38 18.26 40 10664 30105 90587638
Metabolic acidosis 56.07 18.26 49 10655 55627 90562116
Transcription medication error 53.44 18.26 11 10693 256 90617487
Pancreatitis acute 53.42 18.26 38 10666 32077 90585666
Renal failure 52.79 18.26 71 10633 130936 90486807
Blood glucose increased 51.80 18.26 60 10644 95186 90522557
Prothrombin consumption time prolonged 50.54 18.26 8 10696 37 90617706
Hepatocellular injury 49.87 18.26 35 10669 28923 90588820
Anuria 48.66 18.26 27 10677 14791 90602952
Rash maculo-papular 45.23 18.26 38 10666 40895 90576848
Anaemia 44.69 18.26 116 10588 352686 90265057
Drug ineffective 39.94 18.26 64 10640 1384234 89233509
Glomerulonephritis minimal lesion 38.95 18.26 9 10695 363 90617380
Dehydration 38.05 18.26 76 10628 194371 90423372
Septic shock 37.59 18.26 48 10656 84112 90533631
Asthenia 37.47 18.26 143 10561 533608 90084135
Abdominal discomfort 32.87 18.26 8 10696 477320 90140423
Arthropathy 32.33 18.26 3 10701 366239 90251504
Ischaemic stroke 31.82 18.26 24 10680 22142 90595601
Joint swelling 31.73 18.26 10 10694 503290 90114453
Agranulocytosis 31.66 18.26 29 10675 34973 90582770
Hypotension 29.56 18.26 95 10609 325302 90292441
Poverty of speech 29.42 18.26 7 10697 321 90617422
Hypokalaemia 29.00 18.26 54 10650 131062 90486681
Cholestasis 28.86 18.26 28 10676 36271 90581472
Drug reaction with eosinophilia and systemic symptoms 28.53 18.26 30 10674 42728 90575015
Renal impairment 27.94 18.26 47 10657 105374 90512369
Renal arteriosclerosis 27.65 18.26 6 10698 181 90617562
Soft tissue necrosis 27.61 18.26 8 10696 792 90616951
Faecal vomiting 27.47 18.26 8 10696 806 90616937
Resting tremor 26.83 18.26 8 10696 875 90616868
Confusional state 26.66 18.26 103 10601 386102 90231641
Eosinophilia 26.51 18.26 24 10680 28509 90589234
Dermatitis exfoliative generalised 26.40 18.26 13 10691 5580 90612163
Glomerulosclerosis 26.22 18.26 7 10697 513 90617230
Diabetes mellitus 25.86 18.26 35 10669 64840 90552903
Headache 25.63 18.26 39 10665 862707 89755036
Gingival abscess 25.44 18.26 8 10696 1045 90616698
Drug level increased 25.10 18.26 23 10681 27739 90590004
Rheumatoid arthritis 25.10 18.26 6 10698 362608 90255135
Infusion related reaction 25.01 18.26 9 10695 416771 90200972
Cerebellar syndrome 24.45 18.26 11 10693 3861 90613882
Hypoglycaemic encephalopathy 24.07 18.26 6 10698 335 90617408
Dermatitis bullous 23.89 18.26 15 10689 10301 90607442
Fall 23.68 18.26 116 10588 481694 90136049
Swelling 23.58 18.26 10 10694 419048 90198695
Pneumonia respiratory syncytial viral 23.48 18.26 8 10696 1343 90616400
Arthralgia 23.30 18.26 35 10669 778487 89839256
Congenital uterine anomaly 22.91 18.26 5 10699 155 90617588
Cardiac failure 22.85 18.26 44 10660 109452 90508291
Disorientation 22.65 18.26 27 10677 44087 90573656
Therapeutic product effect decreased 22.65 18.26 3 10701 277568 90340175
Cerebral haemorrhage 22.64 18.26 24 10680 34498 90583245
Vertigo 22.45 18.26 34 10670 69777 90547966
Wrong patient received product 22.34 18.26 10 10694 3467 90614276
Somnambulism 22.25 18.26 12 10692 6216 90611527
Subacute cutaneous lupus erythematosus 22.06 18.26 10 10694 3572 90614171
Bradycardia 21.71 18.26 37 10667 83810 90533933
Vascular purpura 21.51 18.26 8 10696 1730 90616013
Maternal exposure during pregnancy 21.22 18.26 8 10696 360055 90257688
Hepatitis fulminant 21.13 18.26 10 10694 3935 90613808
Pain 21.03 18.26 55 10649 996286 89621457
Altered state of consciousness 20.82 18.26 22 10682 31510 90586233
Mechanical urticaria 20.67 18.26 6 10698 598 90617145
Autoimmune haemolytic anaemia 20.51 18.26 11 10693 5634 90612109
Hypothermia 20.46 18.26 16 10688 15559 90602184
Blister 20.23 18.26 3 10701 254995 90362748
Hyponatraemia 20.14 18.26 47 10657 133491 90484252
Discomfort 20.07 18.26 4 10700 274331 90343412
Haematemesis 19.60 18.26 22 10682 33704 90584039
Contraindicated product administered 19.05 18.26 7 10697 320132 90297611
Medication error 18.88 18.26 35 10669 84617 90533126
Peripheral swelling 18.66 18.26 13 10691 413093 90204650

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 851.83 17.03 383 11113 59471 42550368
Lactic acidosis 288.38 17.03 169 11327 45092 42564747
Hypoglycaemic coma 222.34 17.03 64 11432 2680 42607159
Acute kidney injury 196.14 17.03 352 11144 366985 42242854
Drug interaction 159.22 17.03 269 11227 266730 42343109
Pemphigoid 78.66 17.03 45 11451 11422 42598417
Diabetes mellitus inadequate control 68.87 17.03 46 11450 15344 42594495
Hyperkalaemia 61.36 17.03 91 11405 80367 42529472
Sopor 53.22 17.03 37 11459 13165 42596674
Hyperglycaemia 52.04 17.03 63 11433 45796 42564043
Cholestasis 50.71 17.03 53 11443 32826 42577013
Oesophageal perforation 50.23 17.03 17 11479 1216 42608623
Cardiac failure 43.78 17.03 92 11404 106764 42503075
Shock haemorrhagic 42.16 17.03 35 11461 16207 42593632
Hepatocellular injury 41.67 17.03 41 11455 23637 42586202
Erythromelalgia 41.26 17.03 8 11488 55 42609784
Drug ineffective 40.14 17.03 68 11428 630129 41979710
Polymerase chain reaction 38.06 17.03 8 11488 86 42609753
Bradyphrenia 37.02 17.03 21 11475 5241 42604598
Ischaemic stroke 36.37 17.03 37 11459 22196 42587643
Coronavirus infection 34.52 17.03 20 11476 5194 42604645
Anuria 34.48 17.03 27 11469 11505 42598334
Toxic skin eruption 34.42 17.03 29 11467 13701 42596138
Supraventricular extrasystoles 33.73 17.03 18 11478 3988 42605851
Extrasystoles 32.89 17.03 18 11478 4191 42605648
Cell death 32.78 17.03 16 11480 2943 42606896
Acute coronary syndrome 32.42 17.03 29 11467 14836 42595003
Renal failure 30.88 17.03 97 11399 143629 42466210
Metabolic acidosis 30.33 17.03 52 11444 51806 42558033
Hyperkinetic heart syndrome 30.22 17.03 7 11489 121 42609718
Gastroduodenal ulcer 29.68 17.03 10 11486 705 42609134
Eosinophilia 29.15 17.03 40 11456 32859 42576980
Anti factor V antibody 28.45 17.03 8 11488 307 42609532
Loss of consciousness 28.37 17.03 71 11425 92283 42517556
Pericardial haemorrhage 27.16 17.03 15 11481 3554 42606285
Agranulocytosis 26.79 17.03 37 11459 30575 42579264
Cardio-respiratory arrest 25.77 17.03 52 11444 58584 42551255
Cerebral haematoma 25.65 17.03 17 11479 5593 42604246
Urine leukocyte esterase positive 25.56 17.03 8 11488 446 42609393
Glycosylated haemoglobin increased 23.90 17.03 23 11473 12901 42596938
Hypoglycaemic encephalopathy 23.82 17.03 7 11489 315 42609524
Interstitial lung disease 23.75 17.03 60 11436 78402 42531437
Anaemia 23.31 17.03 142 11354 280136 42329703
Glomerulonephritis membranous 22.74 17.03 10 11486 1450 42608389
Hyperthermia 22.54 17.03 22 11474 12552 42597287
Haemoglobinuria 22.32 17.03 8 11488 678 42609161
Vascular purpura 21.78 17.03 11 11485 2175 42607664
Haematoma 21.76 17.03 32 11464 27991 42581848
Drug reaction with eosinophilia and systemic symptoms 20.53 17.03 39 11457 42036 42567803
Lung disorder 20.46 17.03 42 11454 47881 42561958
Glycosuria 20.11 17.03 9 11487 1361 42608478
Urine ketone body present 19.96 17.03 9 11487 1385 42608454
Anal incontinence 19.86 17.03 18 11478 9363 42600476
Arteriovenous fistula site haematoma 19.78 17.03 4 11492 35 42609804
Renal tubular necrosis 18.85 17.03 24 11472 18330 42591509
Prurigo 18.72 17.03 7 11489 669 42609170
Rash maculo-papular 18.59 17.03 35 11461 37468 42572371
Hypomagnesaemia 18.57 17.03 30 11466 28458 42581381
Gamma-glutamyltransferase increased 18.23 17.03 32 11464 32465 42577374
Off label use 17.53 17.03 101 11395 638234 41971605
Chronic kidney disease 17.40 17.03 39 11457 47202 42562637

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 1593.86 15.56 658 20819 115446 110452376
Lactic acidosis 741.75 15.56 361 21116 92450 110475372
Acute kidney injury 602.59 15.56 675 20802 634755 109933067
Hypoglycaemic coma 461.48 15.56 123 21354 5410 110562412
Drug interaction 313.95 15.56 433 21044 499750 110068072
Hyperkalaemia 224.18 15.56 196 21281 135600 110432222
Pemphigoid 164.12 15.56 79 21398 19628 110548194
Diabetes mellitus inadequate control 136.09 15.56 80 21397 29695 110538127
Hyperglycaemia 113.35 15.56 109 21368 84981 110482841
Sopor 111.40 15.56 76 21401 36470 110531352
Hepatocellular injury 87.30 15.56 75 21402 50567 110517255
Renal failure 87.01 15.56 157 21320 226417 110341405
Metabolic acidosis 86.97 15.56 102 21375 99642 110468180
Anuria 79.88 15.56 53 21424 24288 110543534
Cholestasis 79.10 15.56 79 21398 64439 110503383
Cardiac failure 73.27 15.56 131 21346 187495 110380327
Ischaemic stroke 70.89 15.56 61 21416 41202 110526620
Drug ineffective 70.73 15.56 117 21360 1520423 109047399
Anaemia 68.94 15.56 248 21229 546838 110020984
Diabetic ketoacidosis 63.92 15.56 58 21419 42000 110525822
Shock haemorrhagic 60.98 15.56 47 21430 27200 110540622
Rash maculo-papular 58.30 15.56 72 21405 74150 110493672
Pancreatitis acute 58.20 15.56 65 21412 60209 110507613
Euglycaemic diabetic ketoacidosis 57.80 15.56 33 21444 11590 110556232
Agranulocytosis 55.22 15.56 64 21413 61696 110506126
Eosinophilia 55.12 15.56 62 21415 57874 110509948
Product prescribing error 52.41 15.56 57 21420 51274 110516548
Blood glucose increased 52.33 15.56 93 21384 132403 110435419
Bradyphrenia 52.23 15.56 31 21446 11697 110556125
Joint swelling 48.57 15.56 13 21464 442832 110124990
Coronavirus infection 47.19 15.56 27 21450 9518 110558304
Oesophageal perforation 46.81 15.56 16 21461 1643 110566179
Prothrombin consumption time prolonged 46.39 15.56 8 21469 38 110567784
Hypoglycaemic encephalopathy 46.19 15.56 13 21464 700 110567122
Drug reaction with eosinophilia and systemic symptoms 45.19 15.56 67 21410 82028 110485794
Toxic skin eruption 43.89 15.56 39 21438 27476 110540346
Headache 43.62 15.56 65 21412 882312 109685510
Vascular purpura 40.37 15.56 18 21459 3753 110564069
Off label use 38.96 15.56 155 21322 1500030 109067792
Arthropathy 38.83 15.56 5 21472 287517 110280305
Glycosylated haemoglobin increased 38.71 15.56 34 21443 23585 110544237
Polymerase chain reaction 38.54 15.56 8 21469 115 110567707
Transcription medication error 38.16 15.56 11 21466 646 110567176
Arthralgia 37.96 15.56 58 21419 779574 109788248
Pain 37.62 15.56 81 21396 954874 109612948
Chronic kidney disease 37.39 15.56 59 21418 76232 110491590
Loss of consciousness 36.60 15.56 102 21375 196204 110371618
Lower respiratory tract infection 35.99 15.56 3 21474 243103 110324719
Maternal exposure during pregnancy 35.49 15.56 4 21473 254879 110312943
Swelling 35.40 15.56 12 21465 351029 110216793
Renal impairment 35.22 15.56 98 21379 188347 110379475
Infusion related reaction 35.16 15.56 15 21462 381147 110186675
Interstitial lung disease 33.84 15.56 80 21397 139254 110428568
Dehydration 33.66 15.56 125 21352 279386 110288436
Dysarthria 33.14 15.56 59 21418 84062 110483760
Drug hypersensitivity 33.05 15.56 24 21453 454066 110113756
Supraventricular extrasystoles 32.50 15.56 20 21457 8053 110559769
Rheumatoid arthritis 32.45 15.56 9 21468 299604 110268218
Dermatitis bullous 32.33 15.56 27 21450 17502 110550320
Fatigue 31.92 15.56 125 21352 1215833 109351989
Confusional state 31.91 15.56 177 21300 468503 110099319
Soft tissue necrosis 31.65 15.56 11 21466 1187 110566635
Dermatitis exfoliative generalised 31.50 15.56 22 21455 10950 110556872
Hyperkinetic heart syndrome 31.50 15.56 7 21470 141 110567681
Acute coronary syndrome 31.49 15.56 30 21447 23082 110544740
Hypocalcaemia 31.27 15.56 50 21427 65316 110502506
Wheezing 30.94 15.56 6 21471 255224 110312598
Anti factor V antibody 30.88 15.56 8 21469 314 110567508
Blister 30.59 15.56 4 21473 227372 110340450
Septic shock 30.50 15.56 83 21394 157445 110410377
Cell death 30.30 15.56 17 21460 5774 110562048
Sinusitis 30.16 15.56 10 21467 296678 110271144
Gastroduodenal ulcer 29.90 15.56 10 21467 961 110566861
Bradycardia 29.17 15.56 81 21396 155436 110412386
Pericardial haemorrhage 29.17 15.56 16 21461 5201 110562621
Therapeutic product effect decreased 29.08 15.56 6 21471 244310 110323512
Altered state of consciousness 28.84 15.56 45 21432 57581 110510241
Hypomagnesaemia 28.63 15.56 46 21431 60324 110507498
Peripheral swelling 28.56 15.56 22 21455 404012 110163810
Abdominal discomfort 28.42 15.56 21 21456 393837 110173985
Erythromelalgia 28.35 15.56 8 21469 435 110567387
Hypotension 28.13 15.56 186 21291 523663 110044159
Drug level increased 27.79 15.56 40 21437 47679 110520143
Psoriatic arthropathy 27.61 15.56 3 21474 196758 110371064
Hepatic cytolysis 27.56 15.56 43 21434 55010 110512812
Hypokinesia 27.24 15.56 27 21450 21799 110546023
Nasopharyngitis 27.21 15.56 22 21455 394339 110173483
Extrasystoles 27.02 15.56 18 21459 8300 110559522
Drug intolerance 26.44 15.56 24 21453 406488 110161334
Anxiety 25.41 15.56 18 21459 345060 110222762
Product use in unapproved indication 25.06 15.56 30 21447 447347 110120475
Glomerulonephritis minimal lesion 24.95 15.56 9 21468 1082 110566740
Renal tubular necrosis 24.63 15.56 30 21447 30445 110537377
Haematoma 24.31 15.56 42 21435 58434 110509388
Hyperthermia 24.15 15.56 25 21452 21247 110546575
Rhabdomyolysis 23.86 15.56 64 21413 120337 110447485
Cerebellar syndrome 23.82 15.56 15 21462 6287 110561535
Pancreatic carcinoma 23.56 15.56 21 21456 14851 110552971
Cardio-respiratory arrest 23.39 15.56 62 21415 115774 110452048
Wrong patient received product 23.03 15.56 15 21462 6659 110561163
Hepatitis acute 23.03 15.56 23 21454 18743 110549079
Haemoglobinuria 22.97 15.56 8 21469 869 110566953
Glomerulonephritis membranous 22.86 15.56 10 21467 1993 110565829
Stomatitis 22.81 15.56 12 21465 270230 110297592
Mobility decreased 22.44 15.56 9 21468 237413 110330409
Folliculitis 22.43 15.56 3 21474 167650 110400172
Cerebral haematoma 22.39 15.56 17 21460 9615 110558207
Asthenia 22.38 15.56 218 21259 688781 109879041
Poverty of speech 21.78 15.56 7 21470 594 110567228
Musculoskeletal stiffness 21.39 15.56 14 21463 279808 110288014
Gingival abscess 21.29 15.56 8 21469 1079 110566743
Arteriovenous fistula site haematoma 20.89 15.56 4 21473 37 110567785
Melaena 20.66 15.56 43 21434 68714 110499108
Blood glucose decreased 20.61 15.56 27 21450 29461 110538361
Haematuria 20.52 15.56 48 21429 82957 110484865
Therapeutic product effect incomplete 20.32 15.56 9 21468 223796 110344026
Glycosuria 20.26 15.56 10 21467 2620 110565202
Jaundice 20.14 15.56 39 21438 59197 110508625
Fall 20.11 15.56 192 21285 603290 109964532
Anal incontinence 20.03 15.56 23 21454 21941 110545881
Hypoaesthesia 19.90 15.56 19 21458 314204 110253618
Diabetes mellitus 19.87 15.56 53 21424 99328 110468494
Overdose 19.86 15.56 94 21383 233700 110334122
Alopecia 19.85 15.56 25 21452 364728 110203094
Product dose omission issue 19.75 15.56 20 21457 321762 110246060
Hepatitis fulminant 19.66 15.56 15 21462 8545 110559277
Sleep disorder 19.65 15.56 7 21470 198637 110369185
Lipase increased 19.52 15.56 21 21456 18651 110549171
Prurigo 19.33 15.56 8 21469 1392 110566430
Depression 19.16 15.56 20 21457 317315 110250507
Nephrotic syndrome 18.93 15.56 18 21459 13813 110554009
Medication error 18.89 15.56 54 21423 105312 110462510
Thrombocytopenia 18.77 15.56 124 21353 348761 110219061
Disorientation 18.72 15.56 42 21435 70629 110497193
Renal arteriosclerosis 18.56 15.56 6 21471 518 110567304
Flatulence 18.55 15.56 35 21442 52114 110515708
Faecal vomiting 18.46 15.56 8 21469 1558 110566264
Diarrhoea 18.44 15.56 317 21160 1139188 109428634
Arthritis 18.20 15.56 5 21472 167581 110400241
Mechanical urticaria 17.94 15.56 6 21471 577 110567245
Atrial fibrillation 17.84 15.56 90 21387 229552 110338270
Haematemesis 17.80 15.56 37 21440 59071 110508751
Resting tremor 17.73 15.56 8 21469 1715 110566107
Acute pulmonary oedema 17.56 15.56 19 21458 16977 110550845
Completed suicide 17.37 15.56 13 21464 242368 110325454
Migraine 17.06 15.56 6 21471 171646 110396176
Acute generalised exanthematous pustulosis 16.98 15.56 21 21456 21643 110546179
Hypoglycaemic unconsciousness 16.94 15.56 7 21470 1213 110566609
Hypokalaemia 16.71 15.56 75 21402 182373 110385449
Hyponatraemia 16.69 15.56 85 21392 217568 110350254
Glomerulosclerosis 16.63 15.56 7 21470 1270 110566552
Atrioventricular block complete 16.60 15.56 20 21457 20062 110547760
Somnambulism 16.45 15.56 12 21465 6393 110561429
Pharyngeal perforation 16.41 15.56 3 21474 21 110567801
Type 2 diabetes mellitus 16.29 15.56 7 21470 177225 110390597
Impaired healing 16.21 15.56 9 21468 196708 110371114
Weight increased 16.13 15.56 36 21441 419608 110148214
Pancreatic carcinoma metastatic 15.96 15.56 10 21467 4154 110563668
Contraindicated product administered 15.73 15.56 15 21462 248252 110319570
Drug level above therapeutic 15.71 15.56 15 21462 11573 110556249
Muscle haemorrhage 15.70 15.56 12 21465 6857 110560965
Infection 15.69 15.56 29 21448 362171 110205651
Left ventricular dysfunction 15.63 15.56 21 21456 23472 110544350
Osteoarthritis 15.57 15.56 8 21469 182615 110385207

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BD14 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BX02 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Other blood glucose lowering drugs, excl. insulins
FDA EPC N0000175428 Glinide
FDA MoA N0000175448 Potassium Channel Antagonists
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:38068 antimalarial
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:145947 antiatherosclerotic agent

Related Drugs by ATC class:

A10BD Combinations of oral blood glucose lowering drugs 19 drugs
acarbosealogliptincanagliflozindapagliflozinempagliflozinertugliflozinevogliptingemigliptinglimepiridelinagliptinlobeglitazonemetformin show all 19 →
A10BX Other blood glucose lowering drugs, excl. insulins 6 drugs
benfluoreximegliminmitiglinidenateglinidepramlintidetirzepatide

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

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Alcoholism contraindication 7200002
Asthenia contraindication 13791008
Myocardial infarction contraindication 22298006 DOID:5844
Acute vomiting contraindication 23971007
Severe adrenal insufficiency contraindication 24867002
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Dehydration contraindication 34095006
Infectious disease contraindication 40733004
Ketoacidosis contraindication 56051008
Acute nephropathy contraindication 58574008
Metabolic acidosis contraindication 59455009
Acute infectious disease contraindication 63171007
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
Breastfeeding (mother) contraindication 413712001
Traumatic injury contraindication 417746004
Radiography with IV Iodinated Contrast Agent contraindication
Severe Hypoxemia contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.43 acidic
pKa2 3.8 Basic

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 Ki 9.14 WOMBAT-PK CHEMBL
ATP-binding cassette sub-family C member 8 Ion channel Kd 7.30 CHEMBL
Solute carrier organic anion transporter family member 1B1 Transporter WOMBAT-PK
Solute carrier family 22 member 1 Transporter IC50 5.04 CHEMBL
Sulfonylurea receptor 2, Kir6.2 Ion channel BLOCKER Ki 8.81 WOMBAT-PK

External reference:

IDSource
4021119 VUID
N0000148573 NUI
D00594 KEGG_DRUG
4021119 VANDF
C0246689 UMLSCUI
CHEBI:8805 CHEBI
BJX PDB_CHEM_ID
CHEMBL1272 ChEMBL_ID
DB00912 DRUGBANK_ID
C072379 MESH_SUPPLEMENTAL_RECORD_UI
6841 IUPHAR_LIGAND_ID
6818 INN_ID
668Z8C33LU UNII
65981 PUBCHEM_CID
219335 RXNORM
11576 MMSL
120643 MMSL
5416 MMSL
d04267 MMSL
007421 NDDF
109074004 SNOMEDCT_US
386964000 SNOMEDCT_US
668Z8C33LU INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Repaglinide Human Prescription Drug Label 1 33342-248 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 33342-249 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 33342-250 TABLET 2 mg ORAL ANDA 25 sections
Prandin HUMAN PRESCRIPTION DRUG LABEL 1 54868-5381 TABLET 2 mg ORAL NDA 21 sections
Prandin HUMAN PRESCRIPTION DRUG LABEL 1 54868-6439 TABLET 1 mg ORAL NDA 21 sections
Repaglinide Human Prescription Drug Label 1 57237-157 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 57237-158 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 57237-159 TABLET 2 mg ORAL ANDA 25 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 60687-560 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 62135-946 TABLET 0.50 mg ORAL ANDA 17 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 62135-947 TABLET 1 mg ORAL ANDA 17 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 62135-948 TABLET 2 mg ORAL ANDA 17 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 63629-4866 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 65862-670 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 65862-671 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 65862-672 TABLET 2 mg ORAL ANDA 25 sections
Prandin HUMAN PRESCRIPTION DRUG LABEL 1 68151-3565 TABLET 0.50 mg ORAL NDA 25 sections
Prandin HUMAN PRESCRIPTION DRUG LABEL 1 68151-3566 TABLET 1 mg ORAL NDA 21 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 71335-2554 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 71335-2598 TABLET 2 mg ORAL ANDA 25 sections
Repaglinide HUMAN PRESCRIPTION DRUG LABEL 1 72162-2558 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 72603-810 TABLET 0.50 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 72603-811 TABLET 1 mg ORAL ANDA 25 sections
Repaglinide Human Prescription Drug Label 1 72603-812 TABLET 2 mg ORAL ANDA 25 sections