candesartan cilexetil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 475 145040-37-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • candesartan cilexetil
  • TCV-116
  • TCV 116
a nonpeptide angiotensin II receptor antagonist
  • Molecular weight: 610.67
  • Formula: C33H34N6O6
  • CLOGP: 7.08
  • LIPINSKI: 3
  • HAC: 12
  • HDO: 1
  • TPSA: 143.34
  • ALOGS: -5.48
  • ROTB: 13

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
8 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.05 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.61 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
June 4, 1998 FDA ASTRAZENECA

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
Acute kidney injury 385.57 10.18 888 57803 234967 46392404
Hyponatraemia 354.36 10.18 530 58161 100802 46526569
Hyperkalaemia 163.96 10.18 256 58435 50453 46576918
Drug ineffective 148.35 10.18 404 58287 677434 45949937
General physical health deterioration 140.48 10.18 390 58301 115379 46511992
Oligohydramnios 123.30 10.18 80 58611 5385 46621986
Completed suicide 121.59 10.18 19 58672 145901 46481470
Product dose omission issue 119.65 10.18 32 58659 168488 46458883
Death 98.79 10.18 169 58522 335379 46291992
Drug interaction 98.05 10.18 509 58182 202585 46424786
Drug hypersensitivity 97.14 10.18 98 58593 243727 46383644
Bradycardia 95.28 10.18 238 58453 66060 46561311
Angina pectoris 93.30 10.18 140 58551 26635 46600736
Lactic acidosis 90.43 10.18 157 58534 33752 46593619
Cardiac failure 86.89 10.18 259 58432 79689 46547682
Pain 81.24 10.18 317 58374 476631 46150740
Syncope 80.51 10.18 302 58389 104501 46522870
Orthostatic hypotension 78.98 10.18 124 58567 24534 46602837
Blood pressure increased 75.15 10.18 337 58354 126329 46501042
Hypotension 75.14 10.18 525 58166 232064 46395307
Inappropriate antidiuretic hormone secretion 73.99 10.18 90 58601 14012 46613359
Dizziness 69.11 10.18 692 57999 339722 46287649
Hypertensive crisis 68.38 10.18 85 58606 13530 46613841
Injection site pain 67.70 10.18 25 58666 107127 46520244
Blood creatinine increased 66.17 10.18 229 58462 76174 46551197
Rheumatoid arthritis 60.99 10.18 132 58559 240083 46387288
Renal impairment 60.18 10.18 218 58473 74154 46553217
Fall 55.60 10.18 645 58046 328452 46298919
Synovitis 55.53 10.18 6 58685 61069 46566302
Arterial occlusive disease 55.49 10.18 47 58644 4757 46622614
Hypertension 53.03 10.18 425 58266 195931 46431440
Maternal exposure during pregnancy 52.41 10.18 32 58659 102517 46524854
Hypoglycaemia 49.77 10.18 166 58525 54183 46573188
Labile hypertension 49.53 10.18 20 58671 488 46626883
Disorientation 49.34 10.18 129 58562 36789 46590582
Haematochezia 48.07 10.18 129 58562 37364 46590007
Circulatory collapse 43.77 10.18 89 58602 21535 46605836
Sputum discoloured 43.35 10.18 66 58625 12712 46614659
Confusional state 42.56 10.18 345 58346 159547 46467824
Alopecia 42.23 10.18 88 58603 162326 46465045
Vertigo 41.61 10.18 152 58539 51896 46575475
Rubber sensitivity 41.16 10.18 26 58665 1670 46625701
Product use issue 40.00 10.18 36 58655 94608 46532763
Injection site erythema 39.76 10.18 22 58669 74405 46552966
Cough 39.13 10.18 452 58239 229797 46397574
Basilar artery occlusion 38.93 10.18 12 58679 127 46627244
Atrial fibrillation 37.67 10.18 241 58450 103349 46524022
Gamma-glutamyltransferase increased 37.50 10.18 106 58585 31634 46595737
Rhabdomyolysis 37.47 10.18 127 58564 41782 46585589
Swelling 37.19 10.18 62 58629 124449 46502922
Cerebral infarction 36.87 10.18 87 58604 23279 46604092
Androgenetic alopecia 36.14 10.18 12 58679 164 46627207
Arthropathy 36.06 10.18 32 58659 84668 46542703
Pemphigoid 36.01 10.18 40 58651 5651 46621720
Altered state of consciousness 34.76 10.18 85 58606 23263 46604108
Diffuse alopecia 34.68 10.18 16 58675 544 46626827
Anaemia 34.07 10.18 480 58211 255299 46372072
Psychomotor retardation 34.04 10.18 30 58661 3203 46624168
Lung opacity 33.45 10.18 20 58671 1164 46626207
Gangrene 33.21 10.18 35 58656 4660 46622711
Hand deformity 32.46 10.18 3 58688 34571 46592800
Vasoplegia syndrome 32.30 10.18 19 58672 1073 46626298
Renal failure 31.78 10.18 248 58443 113346 46514025
Non-cardiogenic pulmonary oedema 31.49 10.18 15 58676 549 46626822
Occupational asthma 30.79 10.18 10 58681 127 46627244
Anuria 30.56 10.18 53 58638 11378 46615993
Glossodynia 30.38 10.18 9 58682 44364 46583007
Forced expiratory volume decreased 29.12 10.18 34 58657 5070 46622301
Product prescribing error 28.80 10.18 72 58619 19975 46607396
Off label use 28.05 10.18 324 58367 379517 46247854
Drug intolerance 28.04 10.18 93 58598 146956 46480415
Toxicity to various agents 28.03 10.18 154 58537 211612 46415759
Lichen planus 27.71 10.18 21 58670 1812 46625559
Therapeutic product effect incomplete 27.16 10.18 35 58656 78118 46549253
Haematoma muscle 27.05 10.18 14 58677 614 46626757
Sinusitis 26.91 10.18 79 58612 129689 46497682
Osteochondrosis 26.41 10.18 16 58675 954 46626417
Hospitalisation 25.73 10.18 25 58666 63360 46564011
Fibromyalgia 25.70 10.18 7 58684 36456 46590915
Oesophageal dilatation 25.16 10.18 11 58680 329 46627042
Gastrointestinal tract adenoma 25.16 10.18 11 58680 329 46627042
Blood hyposmosis 25.08 10.18 6 58685 21 46627350
Injection site reaction 24.34 10.18 15 58676 47834 46579537
Peripheral swelling 24.33 10.18 109 58582 157962 46469409
Carcinoid tumour of the caecum 24.26 10.18 6 58685 25 46627346
Barotrauma 23.86 10.18 9 58682 182 46627189
Pulmonary hypoplasia 23.38 10.18 10 58681 283 46627088
No adverse event 23.33 10.18 7 58684 34224 46593147
Disease progression 23.26 10.18 50 58641 91250 46536121
Multiple sclerosis relapse 23.16 10.18 12 58679 42113 46585258
Haematoma 22.92 10.18 90 58601 31782 46595589
Internal haemorrhage 22.67 10.18 28 58663 4427 46622944
Mental status changes 22.23 10.18 10 58681 38078 46589293
Abdominal discomfort 22.22 10.18 106 58585 151059 46476312
Treatment failure 22.08 10.18 53 58638 93034 46534337
Infection 21.85 10.18 90 58601 133502 46493869
Shock haemorrhagic 21.78 10.18 39 58652 8585 46618786
Abortion spontaneous 21.76 10.18 14 58677 43632 46583739
Arrhythmia 21.61 10.18 94 58597 34747 46592624
Tinnitus 21.43 10.18 80 58611 27593 46599778
Product quality issue 21.38 10.18 9 58682 35639 46591732
Purpura senile 21.32 10.18 12 58679 623 46626748
Cerebellar syndrome 21.32 10.18 24 58667 3441 46623930
Cornea verticillata 21.07 10.18 6 58685 47 46627324
Renal impairment neonatal 21.01 10.18 5 58686 17 46627354
Metastases to fallopian tube 20.96 10.18 6 58685 48 46627323
Prerenal failure 20.71 10.18 16 58675 1421 46625950
Myalgia 20.58 10.18 241 58450 122847 46504524
Interstitial lung disease 20.52 10.18 127 58564 53822 46573549
Intravascular haemolysis 20.46 10.18 9 58682 273 46627098
Gastrointestinal disorder 20.37 10.18 27 58664 59549 46567822
Palpitations 20.37 10.18 196 58495 95063 46532308
Disturbance in attention 20.23 10.18 86 58605 31474 46595897
Sinus arrest 20.12 10.18 17 58674 1714 46625657
Thyroid stimulating immunoglobulin increased 20.07 10.18 7 58684 112 46627259
Injection site swelling 20.02 10.18 13 58678 40314 46587057
Atrioventricular block complete 19.91 10.18 35 58656 7592 46619779
Dyspnoea 19.86 10.18 814 57877 514734 46112637
Melaena 19.63 10.18 78 58613 27694 46599677
Occult blood 19.61 10.18 13 58678 907 46626464
Mental status changes postoperative 19.37 10.18 8 58683 207 46627164
Renal aplasia 19.16 10.18 8 58683 213 46627158
Oedema peripheral 18.98 10.18 294 58397 159412 46467959
Histamine intolerance 18.85 10.18 5 58686 29 46627342
Confusion postoperative 18.82 10.18 8 58683 223 46627148
Intentional overdose 18.77 10.18 33 58658 64911 46562460
Neutropenia 18.47 10.18 105 58586 143099 46484272
Dehydration 18.32 10.18 292 58399 159248 46468123
Urinary retention 18.26 10.18 73 58618 25988 46601383
Joint swelling 18.21 10.18 128 58563 165945 46461426
Injection site pruritus 18.16 10.18 14 58677 39729 46587642
Blood creatine phosphokinase increased 18.12 10.18 76 58615 27648 46599723
Painful respiration 18.10 10.18 19 58672 2518 46624853
Putamen haemorrhage 17.97 10.18 7 58684 155 46627216
Hypouricaemia 17.84 10.18 7 58684 158 46627213
Psoas abscess 17.64 10.18 9 58682 383 46626988
Blood uric acid increased 17.62 10.18 24 58667 4177 46623194
Glomerulonephritis chronic 17.60 10.18 7 58684 164 46627207
Vertigo positional 17.53 10.18 19 58672 2611 46624760
Acute myocardial infarction 17.46 10.18 83 58608 31841 46595530
Thirst 17.46 10.18 41 58650 10935 46616436
Total lung capacity decreased 17.42 10.18 13 58678 1096 46626275
Vital capacity decreased 17.09 10.18 10 58681 559 46626812
Tubulointerstitial nephritis 17.09 10.18 49 58642 14739 46612632
Heart rate 17.04 10.18 5 58686 44 46627327
Multiple sclerosis 17.02 10.18 5 58686 24786 46602585
Rash 16.98 10.18 331 58360 356181 46271190
Vestibular migraine 16.92 10.18 6 58685 101 46627270
Hypokalaemia 16.83 10.18 177 58514 87847 46539524
Blood pressure inadequately controlled 16.73 10.18 24 58667 4382 46622989
Hypoosmolar state 16.67 10.18 7 58684 189 46627182
Female sterilisation 16.66 10.18 10 58681 586 46626785
Productive cough 16.61 10.18 115 58576 50600 46576771
Wrong strength 16.57 10.18 5 58686 49 46627322
Transaminases increased 16.53 10.18 74 58617 27687 46599684
Intentional product misuse 16.48 10.18 21 58670 47107 46580264
Dermatosis 16.42 10.18 8 58683 308 46627063
Exposure during pregnancy 16.41 10.18 75 58616 108137 46519234
Hepatic function abnormal 16.36 10.18 86 58605 34335 46593036
Ventricular extrasystoles 16.17 10.18 40 58651 11023 46616348
Iron deficiency anaemia 16.14 10.18 53 58638 17153 46610218
Diabetic ketoacidosis 16.11 10.18 55 58636 18155 46609216
Prothrombin time shortened 15.93 10.18 15 58676 1744 46625627
Potentiating drug interaction 15.83 10.18 22 58669 3901 46623470
Sepsis 15.82 10.18 103 58588 135911 46491460
Tarsal tunnel syndrome 15.79 10.18 10 58681 645 46626726
Spider naevus 15.78 10.18 6 58685 124 46627247
International normalised ratio increased 15.77 10.18 107 58584 46776 46580595
Injection site bruising 15.72 10.18 13 58678 35623 46591748
Chromaturia 15.67 10.18 48 58643 14971 46612400
Chest wall mass 15.65 10.18 5 58686 60 46627311
Neuropathy peripheral 15.64 10.18 60 58631 90833 46536538
Serum serotonin increased 15.61 10.18 6 58685 128 46627243
Mobility decreased 15.59 10.18 33 58658 60561 46566810
Hypomagnesaemia 15.39 10.18 62 58629 22148 46605223
Plasma cell myeloma 15.36 10.18 20 58671 44458 46582913
C-reactive protein increased 15.33 10.18 126 58565 58464 46568907
Sensitivity to weather change 15.30 10.18 26 58665 5490 46621881
Adverse drug reaction 15.27 10.18 20 58671 44342 46583029
Vestibular disorder 15.03 10.18 13 58678 1353 46626018
Cor pulmonale acute 15.02 10.18 8 58683 372 46626999
Cerebral haemorrhage 14.97 10.18 73 58618 28298 46599073
Walking disability 14.94 10.18 13 58678 1365 46626006
Contraindicated product administered 14.93 10.18 51 58640 79896 46547475
Systemic lupus erythematosus 14.76 10.18 38 58653 65142 46562229
Pneumobilia 14.57 10.18 6 58685 154 46627217
Lip infection 14.34 10.18 5 58686 80 46627291
Full blood count decreased 14.33 10.18 5 58686 22206 46605165
Nasal congestion 14.31 10.18 24 58667 48089 46579282
Dyspnoea at rest 14.30 10.18 20 58671 3568 46623803
Bradyarrhythmia 14.27 10.18 15 58676 1991 46625380
Metastases to bladder 14.19 10.18 6 58685 165 46627206
Hyperuricaemia 14.11 10.18 23 58668 4694 46622677
Retroperitoneal haematoma 14.09 10.18 17 58674 2623 46624748
Gastroenteritis 14.00 10.18 64 58627 24155 46603216
Binocular eye movement disorder 13.97 10.18 4 58687 32 46627339
Cerebral haematoma 13.89 10.18 19 58672 3320 46624051
Cardiorenal syndrome 13.80 10.18 9 58682 611 46626760
Unevaluable event 13.77 10.18 23 58668 46152 46581219
Blood sodium decreased 13.76 10.18 59 58632 21667 46605704
Glomerular filtration rate decreased 13.76 10.18 39 58652 11655 46615716
Therapy non-responder 13.71 10.18 19 58672 41133 46586238
Decreased appetite 13.51 10.18 329 58362 193507 46433864
Staphylococcal infection 13.51 10.18 15 58676 35756 46591615
Aortic dissection 13.33 10.18 13 58678 1579 46625792
Aphasia 13.32 10.18 71 58620 28496 46598875
Hypochloraemia 13.31 10.18 14 58677 1859 46625512
Glossitis 13.28 10.18 17 58674 2786 46624585
Hallucinations, mixed 13.22 10.18 20 58671 3829 46623542
Cardiac murmur functional 13.18 10.18 4 58687 40 46627331
Accidental exposure to product 13.17 10.18 5 58686 21076 46606295
Miosis 13.00 10.18 27 58664 6630 46620741
Crystal arthropathy 12.95 10.18 6 58685 206 46627165
Retroperitoneal fibrosis 12.94 10.18 7 58684 336 46627035
Subarachnoid haemorrhage 12.93 10.18 37 58654 11116 46616255
Treatment noncompliance 12.93 10.18 11 58680 29720 46597651
Drug metabolising enzyme decreased 12.89 10.18 3 58688 9 46627362
Pericarditis 12.88 10.18 7 58684 23920 46603451
Eczema nummular 12.77 10.18 6 58685 213 46627158
Device capturing issue 12.76 10.18 4 58687 45 46627326
Polyuria 12.69 10.18 28 58663 7167 46620204
Clostridium difficile infection 12.58 10.18 8 58683 25095 46602276
Blood urea increased 12.50 10.18 64 58627 25288 46602083
Febrile neutropenia 12.40 10.18 69 58622 94558 46532813
Tenderness 12.36 10.18 3 58688 16878 46610493
Gastrointestinal haemorrhage 12.27 10.18 150 58541 77223 46550148
Endometrial cancer stage I 12.27 10.18 6 58685 233 46627138
Arthralgia 12.23 10.18 357 58334 364246 46263125
Wrong technique in product usage process 12.11 10.18 32 58659 54390 46572981
Malaise 12.03 10.18 520 58171 330712 46296659
Seizure 11.99 10.18 98 58593 122956 46504415
Drug monitoring procedure not performed 11.92 10.18 7 58684 394 46626977
Anaemia folate deficiency 11.90 10.18 6 58685 249 46627122
Pharyngeal enanthema 11.89 10.18 4 58687 57 46627314
Electrolyte imbalance 11.87 10.18 48 58643 17178 46610193
Pregnancy 11.85 10.18 10 58681 27127 46600244
Ischaemic stroke 11.84 10.18 47 58644 16675 46610696
Drug therapeutic incompatibility 11.83 10.18 4 58687 58 46627313
Gastroenteritis viral 11.82 10.18 4 58687 18115 46609256
Thrombosis 11.71 10.18 34 58657 56035 46571336
Loss of personal independence in daily activities 11.71 10.18 35 58656 57148 46570223
Hepatic enzyme increased 11.63 10.18 58 58633 81729 46545642
Pain in jaw 11.54 10.18 19 58672 38353 46589018
Foetal malformation 11.48 10.18 5 58686 148 46627223
Brain stem stroke 11.45 10.18 6 58685 270 46627101
Labelled drug-drug interaction medication error 11.43 10.18 31 58660 9030 46618341
Therapy cessation 11.40 10.18 10 58681 26619 46600752
Intraventricular haemorrhage 11.39 10.18 13 58678 1892 46625479
Retinopathy of prematurity 11.37 10.18 6 58685 274 46627097
Transient ischaemic attack 11.34 10.18 79 58612 34824 46592547
Proteinuria 11.30 10.18 46 58645 16507 46610864
Anti-thyroid antibody positive 11.25 10.18 7 58684 438 46626933
Iron deficiency 11.24 10.18 23 58668 5590 46621781
Base excess decreased 11.19 10.18 4 58687 69 46627302
Product impurity 11.19 10.18 4 58687 69 46627302
Lordosis 11.19 10.18 6 58685 283 46627088
Aplasia pure red cell 11.16 10.18 20 58671 4405 46622966
Carcinoid tumour 11.09 10.18 6 58685 288 46627083
Blood pressure systolic increased 11.09 10.18 68 58623 28719 46598652
Delayed fontanelle closure 11.09 10.18 3 58688 19 46627352
Blood sodium abnormal 11.05 10.18 8 58683 644 46626727
Polyneuropathy 11.04 10.18 36 58655 11608 46615763
Visual acuity reduced transiently 11.03 10.18 5 58686 163 46627208
Spinal osteoarthritis 11.03 10.18 41 58650 14110 46613261
Hypoaesthesia 10.98 10.18 96 58595 118773 46508598
Resorption bone increased 10.96 10.18 10 58681 1117 46626254
Congestive cardiomyopathy 10.95 10.18 23 58668 5690 46621681
Stasis dermatitis 10.95 10.18 8 58683 653 46626718
Gastritis bacterial 10.93 10.18 4 58687 74 46627297
Device dislocation 10.86 10.18 7 58684 21795 46605576
Complication associated with device 10.81 10.18 3 58688 15438 46611933
Procalcitonin increased 10.81 10.18 8 58683 666 46626705
Dyscalculia 10.71 10.18 3 58688 22 46627349
Hepatitis cholestatic 10.68 10.18 25 58666 6652 46620719
Infusion related reaction 10.60 10.18 79 58612 101129 46526242
Incarcerated incisional hernia 10.59 10.18 3 58688 23 46627348
Chemotherapeutic drug level increased 10.57 10.18 5 58686 180 46627191
Laboratory test abnormal 10.50 10.18 8 58683 22839 46604532
Blood pressure decreased 10.49 10.18 114 58577 57045 46570326
Drug dependence 10.45 10.18 6 58685 19895 46607476
Vitamin B12 decreased 10.37 10.18 15 58676 2760 46624611
Skin texture abnormal 10.36 10.18 6 58685 329 46627042
Necrotising myositis 10.34 10.18 6 58685 330 46627041
Stress urinary incontinence 10.29 10.18 13 58678 2103 46625268
Agranulocytosis 10.25 10.18 55 58636 22130 46605241
White blood cell count decreased 10.21 10.18 91 58600 112140 46515231

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
Hyperkalaemia 150.84 10.50 320 45449 65690 29841019
General physical health deterioration 146.36 10.50 408 45361 99536 29807173
Acute kidney injury 135.24 10.50 795 44974 273047 29633662
Death 133.69 10.50 213 45556 357070 29549639
Completed suicide 126.87 10.50 6 45763 99486 29807223
Product monitoring error 126.54 10.50 59 45710 1682 29905027
Haematochezia 86.44 10.50 173 45596 34049 29872660
Product dose omission issue 75.62 10.50 23 45746 91608 29815101
Drug abuse 72.60 10.50 18 45751 82054 29824655
Toxicity to various agents 72.47 10.50 99 45670 177084 29729625
Bradycardia 62.43 10.50 231 45538 65295 29841414
Hypertension 58.06 10.50 350 45419 121004 29785705
Neutropenia 50.34 10.50 74 45695 128466 29778243
Dizziness 49.22 10.50 484 45285 194425 29712284
Pulmonary hypoplasia 48.93 10.50 20 45749 411 29906298
Cardiac failure 48.08 10.50 253 45516 83165 29823544
Product prescribing error 46.38 10.50 88 45681 16645 29890064
Angina pectoris 44.56 10.50 122 45647 29396 29877313
Renal impairment 44.25 10.50 249 45520 83935 29822774
Interstitial lung disease 43.62 10.50 195 45574 60002 29846707
Pemphigoid 37.97 10.50 52 45717 7476 29899233
Plasma cell myeloma 36.51 10.50 18 45751 53444 29853265
Electrolyte imbalance 36.32 10.50 64 45705 11436 29895273
Vitamin D deficiency 36.09 10.50 42 45727 5128 29901581
Presyncope 34.49 10.50 76 45693 15980 29890729
Anencephaly 33.87 10.50 11 45758 113 29906596
Nipple inflammation 33.80 10.50 10 45759 73 29906636
Lymphocyte count abnormal 33.61 10.50 17 45752 581 29906128
Renal artery thrombosis 33.25 10.50 14 45755 311 29906398
Drug ineffective 32.60 10.50 348 45421 340039 29566670
Cerebral infarction 31.22 10.50 100 45669 26273 29880436
Drug interaction 30.28 10.50 450 45319 199118 29707591
Patient dissatisfaction with treatment 30.27 10.50 9 45760 67 29906642
Disease progression 30.26 10.50 47 45722 79827 29826882
Myalgia 29.81 10.50 210 45559 76457 29830252
C-reactive protein decreased 29.06 10.50 22 45747 1556 29905153
Blood pressure increased 28.54 10.50 198 45571 71730 29834979
Seizure 28.54 10.50 68 45701 98407 29808302
Agitation 27.78 10.50 25 45744 54048 29852661
Labelled drug-drug interaction medication error 27.46 10.50 54 45715 10484 29896225
Hospitalisation 27.25 10.50 17 45752 44302 29862407
Oedema peripheral 27.22 10.50 264 45505 105568 29801141
Neuropathy peripheral 27.15 10.50 41 45728 70434 29836275
Arrhythmia 26.74 10.50 111 45658 33058 29873651
Blood creatinine increased 26.55 10.50 234 45535 91141 29815568
Blood cholesterol 26.37 10.50 9 45760 109 29906600
Hyperuricaemia 25.78 10.50 43 45726 7351 29899358
Cardiac arrest 25.43 10.50 66 45703 92784 29813925
Off label use 25.41 10.50 251 45518 249039 29657670
Nipple disorder 25.04 10.50 10 45759 193 29906516
Peripheral arterial occlusive disease 25.02 10.50 35 45734 5133 29901576
Respiratory arrest 24.74 10.50 7 45762 29251 29877458
Joint contracture 24.29 10.50 21 45748 1794 29904915
Lactic acidosis 24.03 10.50 103 45666 31110 29875599
Colitis 23.96 10.50 102 45667 30718 29875991
Hypertensive crisis 23.21 10.50 44 45725 8313 29898396
Intentional product misuse 23.17 10.50 12 45757 34655 29872054
Dyspnoea 22.50 10.50 667 45102 332628 29574081
Pain 22.44 10.50 163 45606 172478 29734231
Intestinal haemorrhage 22.33 10.50 26 45743 3175 29903534
Hemiataxia 22.21 10.50 6 45763 30 29906679
Hyponatraemia 22.12 10.50 177 45592 67025 29839684
Mucosal haemorrhage 21.84 10.50 18 45751 1440 29905269
Mental status changes 21.74 10.50 15 45754 37064 29869645
Sepsis 21.64 10.50 133 45636 146262 29760447
Acute cutaneous lupus erythematosus 21.54 10.50 7 45762 72 29906637
Diabetes mellitus inadequate control 21.54 10.50 55 45714 12707 29894002
Pneumonia 21.39 10.50 371 45398 333935 29572774
Blood glucose fluctuation 21.10 10.50 27 45742 3634 29903075
Gastrointestinal ischaemia 21.08 10.50 9 45760 207 29906502
Food aversion 21.07 10.50 10 45759 297 29906412
Febrile neutropenia 20.83 10.50 88 45681 106605 29800104
Haematoma 20.77 10.50 82 45687 23871 29882838
Hypoxia 20.26 10.50 26 45743 47828 29858881
Urinary hesitation 20.18 10.50 21 45748 2263 29904446
Nervous system neoplasm 20.05 10.50 8 45761 154 29906555
Oral lichen planus 19.37 10.50 8 45761 169 29906540
Vasculitic rash 19.28 10.50 14 45755 929 29905780
Duodenal ulcer 19.19 10.50 45 45724 9856 29896853
Eczema eyelids 19.03 10.50 5 45764 22 29906687
Gamma-glutamyltransferase increased 18.98 10.50 92 45677 29258 29877451
Mixed liver injury 18.83 10.50 19 45750 1974 29904735
Basilar artery thrombosis 18.35 10.50 7 45762 119 29906590
Jaundice 18.32 10.50 98 45671 32388 29874321
Pallor 18.20 10.50 72 45697 20977 29885732
Tonsillar ulcer 18.16 10.50 8 45761 199 29906510
Anxiety disorder due to a general medical condition 17.91 10.50 4 45765 7 29906702
Atrioventricular block second degree 17.85 10.50 23 45746 3117 29903592
Congenital renal disorder 17.63 10.50 6 45763 72 29906637
Macular ischaemia 17.20 10.50 6 45763 78 29906631
Unevaluable event 17.17 10.50 14 45755 31771 29874938
Blood creatine phosphokinase increased 16.97 10.50 120 45649 43728 29862981
Hepatic function abnormal 16.94 10.50 116 45653 41829 29864880
Blood pressure fluctuation 16.89 10.50 62 45707 17441 29889268
Cerebral haematoma 16.75 10.50 27 45742 4487 29902222
Paresis cranial nerve 16.66 10.50 6 45763 86 29906623
Congenital vas deferens absence 16.61 10.50 5 45764 39 29906670
Congenital muscle absence 16.61 10.50 5 45764 39 29906670
Hallucination 16.61 10.50 31 45738 49028 29857681
Skull malformation 16.54 10.50 9 45760 358 29906351
Choroidal detachment 16.52 10.50 9 45760 359 29906350
Supine hypertension 16.51 10.50 8 45761 249 29906460
Blood pressure inadequately controlled 16.49 10.50 20 45749 2550 29904159
Device lead damage 16.46 10.50 3 45766 0 29906709
Incarcerated inguinal hernia 16.41 10.50 6 45763 90 29906619
Xanthopsia 16.36 10.50 7 45762 162 29906547
Syncope 16.35 10.50 200 45569 84703 29822006
Muscle rupture 16.10 10.50 18 45751 2103 29904606
Fracture 15.92 10.50 31 45738 5975 29900734
Retinal artery occlusion 15.81 10.50 16 45753 1668 29905041
Oliguria 15.74 10.50 35 45734 7404 29899305
Hepatic ischaemia 15.71 10.50 9 45760 396 29906313
Sedation 15.66 10.50 3 45766 16370 29890339
Treatment failure 15.57 10.50 18 45751 34661 29872048
Pancreatitis acute 15.51 10.50 79 45690 25616 29881093
Alopecia universalis 15.51 10.50 5 45764 50 29906659
Shock hypoglycaemic 15.36 10.50 6 45763 109 29906600
Hypotension 15.33 10.50 408 45361 200157 29706552
Gastrointestinal disorder 15.27 10.50 84 45685 28053 29878656
Oligohydramnios 15.09 10.50 8 45761 302 29906407
Aortic valve incompetence 15.03 10.50 27 45742 4896 29901813
Abdominal pain lower 14.94 10.50 38 45731 8760 29897949
Prolonged expiration 14.93 10.50 7 45762 202 29906507
Primary hyperaldosteronism 14.85 10.50 5 45764 58 29906651
Drug dependence 14.79 10.50 7 45762 21288 29885421
Full blood count decreased 14.78 10.50 3 45766 15714 29890995
Rhabdomyolysis 14.60 10.50 155 45614 63425 29843284
Renin increased 14.55 10.50 5 45764 62 29906647
Papillary renal cell carcinoma 14.52 10.50 6 45763 127 29906582
Coronavirus infection 14.48 10.50 22 45747 3476 29903233
Desmoplastic melanoma 14.38 10.50 3 45766 3 29906706
Eczema 14.31 10.50 49 45720 13320 29893389
Therapeutic product effect decreased 14.27 10.50 14 45755 29062 29877647
Sinusitis 14.24 10.50 18 45751 33327 29873382
White blood cell count decreased 14.16 10.50 73 45696 83874 29822835
Melaena 13.87 10.50 91 45678 32346 29874363
COVID-19 13.83 10.50 5 45764 17873 29888836
Multiple drug therapy 13.82 10.50 7 45762 240 29906469
Excessive eye blinking 13.71 10.50 7 45762 244 29906465
Cardiovascular insufficiency 13.66 10.50 14 45755 1482 29905227
Vasoplegia syndrome 13.66 10.50 13 45756 1258 29905451
Basal ganglia haemorrhage 13.65 10.50 11 45758 852 29905857
Total cholesterol/HDL ratio increased 13.59 10.50 6 45763 150 29906559
Therapy non-responder 13.54 10.50 15 45754 29438 29877271
Hypozincaemia 13.52 10.50 3 45766 5 29906704
Hepatitis acute 13.52 10.50 32 45737 7051 29899658
Condition aggravated 13.42 10.50 290 45479 137576 29769133
Drug resistance 13.41 10.50 7 45762 20126 29886583
Brain stem infarction 13.36 10.50 13 45756 1293 29905416
Vertebral artery stenosis 13.31 10.50 6 45763 158 29906551
Product quality issue 13.31 10.50 6 45763 18768 29887941
Orthostatic hypotension 13.29 10.50 72 45697 23907 29882802
No adverse event 13.26 10.50 5 45764 17414 29889295
Renal ischaemia 13.26 10.50 9 45760 536 29906173
Prothrombin time shortened 13.21 10.50 14 45755 1541 29905168
Rhinalgia 13.20 10.50 8 45761 391 29906318
Periorbital discomfort 13.20 10.50 4 45765 32 29906677
Vascular stent thrombosis 13.07 10.50 17 45752 2326 29904383
Palmar-plantar erythrodysaesthesia syndrome 12.96 10.50 51 45718 14819 29891890
Cranial sutures widening 12.95 10.50 5 45764 88 29906621
Mechanical urticaria 12.84 10.50 5 45764 90 29906619
Hepatocellular carcinoma 12.82 10.50 38 45731 9572 29897137
Neurologic neglect syndrome 12.71 10.50 6 45763 176 29906533
Thrombocytopenia 12.69 10.50 141 45628 136903 29769806
Adrenal insufficiency 12.68 10.50 40 45729 10423 29896286
Unresponsive to stimuli 12.65 10.50 13 45756 26406 29880303
Hypoglycaemia 12.51 10.50 126 45643 50855 29855854
Product use in unapproved indication 12.47 10.50 64 45705 73629 29833080
Myopia 12.43 10.50 9 45760 594 29906115
Aortic valve disease mixed 12.36 10.50 5 45764 100 29906609
Lip ulceration 12.32 10.50 10 45759 783 29905926
Mesenteric artery thrombosis 12.24 10.50 8 45761 447 29906262
Coronary artery stenosis 12.23 10.50 36 45733 9034 29897675
Hypochromic anaemia 12.20 10.50 10 45759 794 29905915
Subileus 12.19 10.50 19 45750 3068 29903641
Glycosylated haemoglobin increased 12.16 10.50 37 45732 9454 29897255
Renal failure 12.14 10.50 270 45499 128696 29778013
Pterygium 11.96 10.50 5 45764 109 29906600
Anti-erythropoietin antibody negative 11.95 10.50 6 45763 202 29906507
Neuroleptic malignant syndrome 11.88 10.50 5 45764 16290 29890419
Stomal hernia 11.88 10.50 5 45764 111 29906598
Antinuclear antibody increased 11.68 10.50 6 45763 212 29906497
Neonatal hypotension 11.55 10.50 5 45764 119 29906590
Wrong dose 11.46 10.50 7 45762 347 29906362
Neurotoxicity 11.43 10.50 3 45766 13179 29893530
Breast pain 11.37 10.50 12 45757 1315 29905394
Generalised tonic-clonic seizure 11.34 10.50 8 45761 19543 29887166
Gastric dilatation 11.28 10.50 8 45761 511 29906198
Nocturnal dyspnoea 11.24 10.50 8 45761 514 29906195
Acute on chronic liver failure 11.22 10.50 5 45764 128 29906581
Respiratory failure 11.22 10.50 99 45670 100543 29806166
Depersonalisation/derealisation disorder 11.17 10.50 8 45761 519 29906190
Anxiety 11.11 10.50 86 45683 89785 29816924
Costovertebral angle tenderness 11.10 10.50 3 45766 15 29906694
Aortic dissection 11.03 10.50 16 45753 2426 29904283
Lymphocyte count 11.00 10.50 4 45765 59 29906650
Skull fracture 10.94 10.50 10 45759 919 29905790
Cytomegalovirus infection 10.94 10.50 12 45757 23662 29883047
Fatigue 10.86 10.50 391 45378 320282 29586427
Fluid overload 10.83 10.50 8 45761 19084 29887625
Idiopathic pulmonary fibrosis 10.78 10.50 21 45748 4048 29902661
Septic encephalopathy 10.76 10.50 4 45765 63 29906646
Influenza like illness 10.75 10.50 14 45755 25591 29881118
Sinus rhythm 10.71 10.50 6 45763 253 29906456
Catheter site cellulitis 10.67 10.50 5 45764 144 29906565
Tongue haematoma 10.61 10.50 5 45764 146 29906563
Toxic skin eruption 10.61 10.50 39 45730 10976 29895733
Tetany 10.53 10.50 9 45760 757 29905952
Facial paresis 10.51 10.50 17 45752 2833 29903876

Pharmacologic Action:

SourceCodeDescription
ATC C09CA06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN
Angiotensin II receptor blockers (ARBs), plain
ATC C09DA06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and diuretics
ATC C09DB07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and calcium channel blockers
ATC C09DX06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs), other combinations
MeSH PA D047228 Angiotensin II Type 1 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
FDA MoA N0000000070 Angiotensin 2 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic heart failure indication 48447003
Atrial fibrillation off-label use 49436004 DOID:0060224
Diabetic renal disease off-label use 127013003
Diastolic heart failure off-label use 418304008 DOID:9775
Nondiabetic Proteinuric Nephropathy off-label use
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Oliguria contraindication 83128009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Surgical procedure contraindication 387713003
Azotemia contraindication 445009001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.25 acidic
pKa2 3.2 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
Type-1 angiotensin II receptor GPCR ANTAGONIST UNKNOWN CHEMBL
Adenosine receptor A3 GPCR Ki 6.16 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 5.76 CHEMBL
Cytochrome P450 2C9 Enzyme IC50 5.52 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 5.52 CHEMBL
Thromboxane-A synthase Enzyme IC50 5.51 CHEMBL
Beta-3 adrenergic receptor GPCR Ki 5.49 CHEMBL
Epidermal growth factor receptor Kinase IC50 5.48 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 5.23 CHEMBL
Cytochrome P450 3A4 Enzyme IC50 5.05 CHEMBL
Cruzipain Enzyme IC50 4.38 CHEMBL
Type-1 angiotensin II receptor GPCR IC50 6.96 CHEMBL
Type-1 angiotensin II receptor GPCR Ki 9.19 CHEMBL

External reference:

IDSource
4021148 VUID
N0000179517 NUI
D00522 KEGG_DRUG
139481-59-7 SECONDARY_CAS_RN
4021148 VANDF
4021151 VANDF
C0527379 UMLSCUI
C0717550 UMLSCUI
CHEBI:3348 CHEBI
CHEBI:149509 CHEBI
CHEMBL1014 ChEMBL_ID
DB00796 DRUGBANK_ID
C077793 MESH_SUPPLEMENTAL_RECORD_UI
2540 PUBCHEM_CID
8352 IUPHAR_LIGAND_ID
C081643 MESH_SUPPLEMENTAL_RECORD_UI
7239 INN_ID
S8Q36MD2XX UNII
2541 PUBCHEM_CID
587 IUPHAR_LIGAND_ID
DB13919 DRUGBANK_ID
135481 RXNORM
188909 MMSL
7490 MMSL
d04322 MMSL
007275 NDDF
007276 NDDF
108587008 SNOMEDCT_US
372512008 SNOMEDCT_US
386878000 SNOMEDCT_US

Pharmaceutical products:

None