carvedilol Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 522 72956-09-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • carvedilol
  • carvedilol phosphate
  • carvediol
  • carvedilol hydrochloride
  • carvedilol HCl
  • BM 14,190
A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION.
  • Molecular weight: 406.48
  • Formula: C24H26N2O4
  • CLOGP: 4.04
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 75.74
  • ALOGS: -4.96
  • ROTB: 10

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
37.50 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 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.03 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 1.30 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) 2.40 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 14, 1995 FDA SMITHKLINE BEECHAM

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
Cardiac failure congestive 1156.38 9.94 1061 86456 91696 53169853
Myocardial infarction 371.20 9.94 619 86898 98735 53162814
Cardiac failure 323.49 9.94 537 86980 85307 53176242
Rheumatoid arthritis 280.57 9.94 84 87433 314447 52947102
Hypotension 262.82 9.94 964 86553 253112 53008437
Drug ineffective 223.59 9.94 649 86868 816596 52444953
Bradycardia 216.45 9.94 405 87112 70651 53190898
Acute myocardial infarction 160.13 9.94 233 87284 33002 53228547
Cardiomyopathy 146.82 9.94 160 87357 16928 53244621
Hyperkalaemia 144.16 9.94 292 87225 53964 53207585
Acute kidney injury 136.94 9.94 796 86721 253072 53008477
Treatment failure 136.90 9.94 23 87494 128380 53133169
Synovitis 130.20 9.94 13 87504 107880 53153669
Joint swelling 126.63 9.94 119 87398 234519 53027030
Maternal exposure during pregnancy 122.41 9.94 51 87466 155588 53105961
Systemic lupus erythematosus 122.07 9.94 28 87489 125386 53136163
Infusion related reaction 119.64 9.94 53 87464 155904 53105645
Ejection fraction decreased 117.94 9.94 154 87363 19694 53241855
Gastrointestinal haemorrhage 115.24 9.94 341 87176 79989 53181560
Chronic kidney disease 114.70 9.94 233 87284 43137 53218412
Contraindicated product administered 114.04 9.94 40 87477 135589 53125960
Coronary artery disease 108.57 9.94 196 87321 33241 53228308
Atrial fibrillation 104.64 9.94 411 87106 111241 53150308
Hand deformity 102.95 9.94 10 87507 84839 53176710
Glossodynia 102.50 9.94 20 87497 100271 53161278
Lower respiratory tract infection 99.89 9.94 15 87502 90966 53170583
Renal failure 97.56 9.94 419 87098 118033 53143516
Pain 92.74 9.94 576 86941 587822 52673727
Drug intolerance 89.35 9.94 124 87393 205369 53056180
Dyspnoea 88.55 9.94 1400 86117 584832 52676717
Syncope 86.78 9.94 389 87128 111604 53149945
Therapeutic product effect decreased 84.04 9.94 51 87466 125604 53135945
Oedema peripheral 82.71 9.94 521 86996 170266 53091283
Cardiac disorder 80.75 9.94 213 87304 46753 53214796
Cerebrovascular accident 79.75 9.94 363 87154 104811 53156738
Arthropathy 79.51 9.94 69 87448 141384 53120165
International normalised ratio increased 79.48 9.94 214 87303 47547 53214002
Arthralgia 79.18 9.94 412 87105 439371 52822178
Renal impairment 76.66 9.94 305 87212 83013 53178536
Death 75.78 9.94 907 86610 356325 52905224
Off label use 72.88 9.94 465 87052 471747 52789802
Hepatic enzyme increased 72.83 9.94 60 87457 126135 53135414
Pericarditis 72.13 9.94 10 87507 64396 53197153
Musculoskeletal stiffness 72.02 9.94 58 87459 123310 53138239
Hypoglycaemia 71.22 9.94 236 87281 58777 53202772
Hypersensitivity 70.62 9.94 150 87367 210515 53051034
Chest pain 69.64 9.94 542 86975 189643 53071906
Alopecia 67.54 9.94 181 87336 234402 53027147
Wound 64.29 9.94 35 87482 91522 53170027
Pulmonary oedema 64.07 9.94 214 87303 53509 53208040
Rash 63.50 9.94 450 87067 445741 52815808
Hypertensive crisis 63.13 9.94 97 87420 14409 53247140
Exposure during pregnancy 61.95 9.94 68 87449 124792 53136757
Anaemia 61.90 9.94 710 86807 276008 52985541
Atrioventricular block 58.12 9.94 65 87452 7075 53254474
Mental status changes 55.78 9.94 167 87350 39404 53222145
Blood glucose increased 55.66 9.94 263 87254 77098 53184451
Congestive cardiomyopathy 55.40 9.94 59 87458 6079 53255470
Dehydration 54.63 9.94 467 87050 167943 53093606
Cardiomegaly 53.57 9.94 101 87416 17699 53243850
Fluid retention 52.33 9.94 202 87315 54199 53207350
Cardiac failure chronic 51.81 9.94 47 87470 3983 53257566
Cardioactive drug level increased 51.48 9.94 36 87481 2093 53259456
Cardiogenic shock 51.13 9.94 98 87419 17384 53244165
Blood creatinine increased 50.96 9.94 269 87248 82393 53179156
Full blood count decreased 50.84 9.94 118 87399 23911 53237638
Discomfort 49.59 9.94 50 87467 95422 53166127
Cardiac arrest 47.96 9.94 290 87227 93377 53168172
Blood pressure decreased 47.96 9.94 215 87302 61654 53199895
Haemoglobin decreased 46.77 9.94 385 87132 136922 53124627
Drug hypersensitivity 46.22 9.94 251 87266 264991 52996558
Abortion spontaneous 46.18 9.94 10 87507 46625 53214924
Dizziness 46.16 9.94 862 86655 371397 52890152
Helicobacter infection 43.90 9.94 6 87511 39063 53222486
Impaired healing 42.99 9.94 26 87491 64179 53197370
Gastrointestinal tract mucosal pigmentation 42.97 9.94 21 87496 619 53260930
Blood loss anaemia 42.68 9.94 62 87455 8761 53252788
Pyrexia 41.94 9.94 441 87076 402752 52858797
Drug abuse 41.86 9.94 28 87489 65498 53196051
Glomerular filtration rate decreased 41.63 9.94 75 87442 12692 53248857
Unresponsive to stimuli 41.50 9.94 135 87382 33291 53228258
Ischaemic cardiomyopathy 40.76 9.94 34 87483 2574 53258975
Folliculitis 40.47 9.94 3 87514 31706 53229843
Abdominal discomfort 39.72 9.94 207 87310 220855 53040694
Infection 39.58 9.94 147 87370 172058 53089491
Injection site pain 39.43 9.94 79 87438 113312 53148237
Drug interaction 39.24 9.94 540 86977 218789 53042760
Mitral valve incompetence 39.17 9.94 94 87423 19457 53242092
Hypertension 39.11 9.94 552 86965 224879 53036670
Asthenia 38.30 9.94 783 86734 342807 52918742
Coronary arterial stent insertion 38.10 9.94 34 87483 2820 53258729
Arrhythmia 37.38 9.94 139 87378 36640 53224909
Pregnancy 37.36 9.94 4 87513 31437 53230112
Cardiac failure acute 37.06 9.94 59 87458 9033 53252516
Fluid overload 36.92 9.94 115 87402 27716 53233833
Sinus bradycardia 36.88 9.94 77 87440 14524 53247025
Spinal epidural haematoma 36.65 9.94 21 87496 860 53260689
Febrile neutropenia 36.58 9.94 73 87444 104863 53156686
Renal disorder 36.46 9.94 118 87399 29021 53232528
Ventricular arrhythmia 36.29 9.94 37 87480 3623 53257926
Product use issue 35.55 9.94 114 87403 139470 53122079
End stage renal disease 35.29 9.94 47 87470 6124 53255425
Myocardial ischaemia 35.13 9.94 70 87447 12774 53248775
Glycosylated haemoglobin increased 34.90 9.94 66 87451 11589 53249960
Angina pectoris 33.86 9.94 114 87403 28611 53232938
Blood potassium increased 33.85 9.94 84 87433 17757 53243792
Distributive shock 33.23 9.94 20 87497 898 53260651
Atrioventricular block first degree 33.19 9.94 47 87470 6488 53255061
Orthopnoea 32.64 9.94 45 87472 6059 53255490
Isosthenuria 32.51 9.94 11 87506 120 53261429
Extradural haematoma 32.26 9.94 25 87492 1703 53259846
Therapeutic product effect incomplete 31.86 9.94 64 87453 91720 53169829
Calcium deficiency 31.75 9.94 20 87497 975 53260574
Swelling 31.55 9.94 184 87333 190921 53070628
Pericardial effusion 31.05 9.94 107 87410 27171 53234378
Asthma 29.89 9.94 86 87431 108886 53152663
Pulse absent 29.71 9.94 40 87477 5266 53256283
Left ventricular dysfunction 29.25 9.94 60 87457 11177 53250372
Myxoedema coma 28.29 9.94 14 87503 424 53261125
Sinusitis 27.44 9.94 163 87354 168401 53093148
Coronary artery occlusion 27.43 9.94 49 87468 8238 53253311
Ventricular hypokinesia 27.40 9.94 35 87482 4377 53257172
Angina unstable 27.12 9.94 46 87471 7422 53254127
Pyelitis 26.85 9.94 11 87506 211 53261338
Bladder hypertrophy 26.25 9.94 11 87506 224 53261325
Erythema 25.97 9.94 151 87366 156818 53104731
Injection site erythema 25.85 9.94 55 87462 77194 53184355
Fall 25.83 9.94 770 86747 357670 52903879
Suicidal ideation 25.77 9.94 37 87480 60474 53201075
Left ventricular hypertrophy 25.70 9.94 37 87480 5186 53256363
Dialysis 25.49 9.94 54 87463 10288 53251261
Vessel puncture site haemorrhage 25.45 9.94 9 87508 113 53261436
Electrocardiogram PR shortened 25.42 9.94 11 87506 243 53261306
Ventricular tachycardia 25.06 9.94 75 87442 17687 53243862
Blood urea increased 24.89 9.94 97 87420 26134 53235415
Nasopharyngitis 24.85 9.94 199 87318 192096 53069453
Sleep disorder due to general medical condition, insomnia type 24.56 9.94 5 87512 24344 53237205
Blood pressure inadequately controlled 24.47 9.94 35 87482 4876 53256673
Blood glucose decreased 24.09 9.94 80 87437 19936 53241613
Blister 23.98 9.94 59 87458 78694 53182855
Gastrointestinal disorder 23.97 9.94 72 87445 89932 53171617
Diastolic dysfunction 23.93 9.94 38 87479 5806 53255743
Irritable bowel syndrome 23.64 9.94 22 87495 43610 53217939
Ill-defined disorder 23.35 9.94 28 87489 49416 53212133
Implantable defibrillator insertion 23.31 9.94 12 87505 396 53261153
Melaena 23.14 9.94 102 87415 29027 53232522
Migraine 23.14 9.94 62 87455 80355 53181194
Stomatitis 23.05 9.94 83 87434 98075 53163474
Acute respiratory failure 23.00 9.94 107 87410 31151 53230398
Respiratory failure 22.89 9.94 259 87258 100253 53161296
Arterial stenosis 22.76 9.94 14 87503 654 53260895
Peritonitis bacterial 22.71 9.94 49 87468 9456 53252093
Intracardiac thrombus 22.59 9.94 24 87493 2465 53259084
Tricuspid valve incompetence 22.44 9.94 63 87454 14333 53247216
Red blood cell sedimentation rate increased 22.35 9.94 9 87508 28048 53233501
Upper gastrointestinal haemorrhage 22.18 9.94 71 87446 17359 53244190
Blood pressure abnormal 22.00 9.94 60 87457 13423 53248126
Ischaemic stroke 21.73 9.94 72 87445 17921 53243628
Brain natriuretic peptide increased 21.52 9.94 33 87484 4892 53256657
Haemorrhage intracranial 21.37 9.94 59 87458 13293 53248256
Atrial flutter 21.28 9.94 48 87469 9543 53252006
Urticaria 21.27 9.94 133 87384 135752 53125797
Blood pressure increased 21.21 9.94 336 87181 140143 53121406
Subdural haematoma 21.09 9.94 60 87457 13753 53247796
Injection site reaction 21.09 9.94 32 87485 51134 53210415
Aortic valve incompetence 20.94 9.94 37 87480 6168 53255381
Hypovolaemia 20.82 9.94 50 87467 10352 53251197
Foetal exposure during pregnancy 20.65 9.94 16 87501 34699 53226850
Condition aggravated 20.31 9.94 354 87163 296780 52964769
Leukopenia 20.12 9.94 58 87459 73405 53188144
Neutropenia 19.98 9.94 166 87351 159019 53102530
Loss of consciousness 19.90 9.94 280 87237 113932 53147617
Headache 19.90 9.94 701 86816 536120 52725429
Cerebral infarction 19.73 9.94 86 87431 24358 53237191
Completed suicide 19.54 9.94 327 87190 137874 53123675
Pneumonia 19.50 9.94 835 86682 406334 52855215
Decreased appetite 19.21 9.94 475 87042 214499 53047050
Pleural effusion 19.16 9.94 226 87291 88353 53173196
Chronic obstructive pulmonary disease 19.06 9.94 168 87349 60905 53200644
Platelet dysfunction 18.98 9.94 7 87510 100 53261449
Arteriosclerosis 18.55 9.94 47 87470 10064 53251485
Urinary tract infection 18.52 9.94 520 86997 239383 53022166
Basal ganglia haemorrhage 18.48 9.94 12 87505 617 53260932
Lower gastrointestinal haemorrhage 18.07 9.94 39 87478 7527 53254022
Hypervolaemia 18.06 9.94 20 87497 2153 53259396
Hip arthroplasty 17.67 9.94 12 87505 27850 53233699
Atrioventricular block complete 17.66 9.94 40 87477 7975 53253574
Electrocardiogram QT shortened 17.65 9.94 7 87510 123 53261426
Oropharyngeal pain 17.61 9.94 71 87446 81197 53180352
Medication error 17.60 9.94 111 87406 36254 53225295
Device expulsion 17.40 9.94 14 87503 29799 53231750
Pulseless electrical activity 17.32 9.94 38 87479 7416 53254133
Mucocutaneous haemorrhage 17.29 9.94 6 87511 71 53261478
Renal hypoplasia 17.25 9.94 5 87512 31 53261518
Femoral artery dissection 17.25 9.94 5 87512 31 53261518
Pulmonary congestion 17.20 9.94 62 87455 16094 53245455
Gout 17.16 9.94 52 87465 12347 53249202
Peripheral coldness 17.07 9.94 48 87469 10931 53250618
Genotype drug resistance test positive 16.81 9.94 11 87506 573 53260976
Left ventricular dilatation 16.68 9.94 10 87507 446 53261103
Nephropathy 16.62 9.94 31 87486 5386 53256163
Hydrothorax 16.55 9.94 12 87505 739 53260810
Hypertensive emergency 16.35 9.94 17 87500 1704 53259845
Mobility decreased 16.29 9.94 67 87450 76204 53185345
Vena cava injury 16.24 9.94 3 87514 0 53261549
Electrocardiogram ST segment 16.24 9.94 3 87514 0 53261549
Nephrogenic anaemia 16.23 9.94 18 87499 1941 53259608
Urine albumin/creatinine ratio increased 16.21 9.94 8 87509 241 53261308
Tendonitis 16.13 9.94 4 87513 17002 53244547
Electrocardiogram abnormal 16.12 9.94 39 87478 8114 53253435
Renal injury 16.09 9.94 44 87473 9860 53251689
Creatinine renal clearance increased 16.02 9.94 11 87506 621 53260928
Coronary artery bypass 15.93 9.94 20 87497 2458 53259091
Hypouricaemia 15.92 9.94 7 87510 161 53261388
Therapy cessation 15.78 9.94 89 87428 27936 53233613
Shock 15.43 9.94 77 87440 23062 53238487
Injection site swelling 15.41 9.94 29 87488 42599 53218950
Cardiac operation 15.21 9.94 21 87496 2832 53258717
Toxic neuropathy 15.16 9.94 9 87508 394 53261155
Renal artery stenosis 15.13 9.94 17 87500 1859 53259690
Haematocrit decreased 15.10 9.94 109 87408 37222 53224327
Plasma cell myeloma 15.09 9.94 132 87385 47742 53213807
Hypertensive encephalopathy 15.09 9.94 11 87506 683 53260866
Vascular stent stenosis 14.89 9.94 10 87507 544 53261005
Psoriatic arthropathy 14.75 9.94 36 87481 48154 53213395
Pernicious anaemia 14.66 9.94 11 87506 714 53260835
Intentional self-injury 14.60 9.94 12 87505 25272 53236277
Embolic stroke 14.59 9.94 24 87493 3775 53257774
Cardio-respiratory arrest 14.57 9.94 154 87363 58604 53202945
Bundle branch block left 14.35 9.94 34 87483 6979 53254570
Unevaluable event 14.34 9.94 134 87383 49364 53212185
Subdural haemorrhage 14.33 9.94 21 87496 2991 53258558
Transfusion 14.13 9.94 52 87465 13635 53247914
Chronic left ventricular failure 14.04 9.94 8 87509 324 53261225
Occult blood positive 13.98 9.94 23 87494 3619 53257930
Malignant neoplasm progression 13.97 9.94 65 87452 71476 53190073
Renal atrophy 13.67 9.94 14 87503 1378 53260171
Heart injury 13.67 9.94 13 87504 1170 53260379
Metabolic acidosis 13.59 9.94 117 87400 42125 53219424
Oral herpes 13.59 9.94 9 87508 21170 53240379
Paraplegia 13.39 9.94 19 87498 2628 53258921
Supraventricular extrasystoles 13.28 9.94 25 87492 4375 53257174
Pulmonary arterial pressure increased 13.24 9.94 22 87495 3490 53258059
Product use in unapproved indication 13.24 9.94 119 87398 112170 53149379
Insulin-requiring type 2 diabetes mellitus 13.21 9.94 5 87512 77 53261472
Arterial occlusive disease 13.19 9.94 27 87490 5022 53256527
Herbal interaction 13.10 9.94 5 87512 79 53261470
Cytomegalovirus infection 12.95 9.94 8 87509 19531 53242018
Lethargy 12.91 9.94 140 87377 53620 53207929
Ventricular fibrillation 12.90 9.94 46 87471 11879 53249670
Catheterisation cardiac 12.79 9.94 24 87493 4190 53257359
Injection site pruritus 12.78 9.94 31 87486 41558 53219991
Urine output decreased 12.71 9.94 45 87472 11578 53249971
Presyncope 12.70 9.94 80 87437 26114 53235435
Drug dependence 12.64 9.94 10 87507 21462 53240087
Cognitive disorder 12.52 9.94 35 87482 44743 53216806
Basal cell carcinoma 12.52 9.94 12 87505 23457 53238092
Diarrhoea 12.44 9.94 1189 86328 624357 52637192
Renal tubular injury 12.43 9.94 8 87509 405 53261144
Gastritis erosive 12.37 9.94 28 87489 5578 53255971
Hyperglycaemia 12.37 9.94 110 87407 39974 53221575
Bradyarrhythmia 12.36 9.94 16 87501 2027 53259522
Inflammation 12.32 9.94 50 87467 57086 53204463
Muscle spasticity 12.25 9.94 7 87510 17831 53243718
Bone marrow failure 12.25 9.94 19 87498 30096 53231453
Loss of personal independence in daily activities 12.17 9.94 66 87451 69749 53191800
Body temperature increased 12.14 9.94 22 87495 32777 53228772
Subarachnoid haemorrhage 12.12 9.94 45 87472 11848 53249701
Traumatic renal injury 12.10 9.94 3 87514 9 53261540
Anti-neutrophil cytoplasmic antibody positive vasculitis 12.08 9.94 17 87500 2334 53259215
Renin increased 12.03 9.94 6 87511 185 53261364
Gastrointestinal arteriovenous malformation 11.98 9.94 9 87508 585 53260964
C-reactive protein increased 11.93 9.94 64 87453 67822 53193727
Hospitalisation 11.93 9.94 173 87344 70839 53190710
Refractory anaemia with an excess of blasts 11.92 9.94 8 87509 435 53261114
Peripheral vascular disorder 11.84 9.94 29 87488 6079 53255470
Cardiac pacemaker insertion 11.83 9.94 22 87495 3815 53257734
Foot deformity 11.77 9.94 8 87509 18560 53242989
Breast cancer recurrent 11.75 9.94 23 87494 4142 53257407
Blood aldosterone abnormal 11.71 9.94 4 87513 45 53261504
Carbohydrate antigen 15-3 increased 11.69 9.94 12 87505 1184 53260365
N-terminal prohormone brain natriuretic peptide increased 11.66 9.94 15 87502 1889 53259660
Azotaemia 11.63 9.94 24 87493 4489 53257060
Extrapyramidal disorder 11.60 9.94 3 87514 12399 53249150
Long QT syndrome 11.57 9.94 20 87497 3276 53258273
Premature labour 11.55 9.94 3 87514 12359 53249190
Cholestatic liver injury 11.53 9.94 17 87500 2434 53259115
Torsade de pointes 11.46 9.94 47 87470 12958 53248591
Intercepted product dispensing error 11.45 9.94 5 87512 113 53261436
Aortic stenosis 11.45 9.94 24 87493 4539 53257010
Bursitis 11.42 9.94 12 87505 22480 53239069
Electrocardiogram QRS complex shortened 11.40 9.94 8 87509 468 53261081
Electrocardiogram T wave inversion 11.39 9.94 21 87496 3618 53257931
Glomerulonephritis rapidly progressive 11.35 9.94 10 87507 815 53260734
Hypovolaemic shock 11.31 9.94 27 87490 5570 53255979
Palpitations 11.27 9.94 233 87284 102115 53159434
Aortic dissection 11.25 9.94 14 87503 1706 53259843
Multiple sclerosis relapse 11.15 9.94 37 87480 44816 53216733
Arteriovenous fistula thrombosis 11.10 9.94 6 87511 219 53261330
Diarrhoea infectious 11.08 9.94 11 87506 1043 53260506
Epinephrine increased 11.06 9.94 3 87514 14 53261535
Hypophagia 11.05 9.94 88 87429 30974 53230575
Vascular pseudoaneurysm 11.00 9.94 13 87504 1501 53260048
Atrial tachycardia 10.98 9.94 16 87501 2268 53259281
Haematuria 10.97 9.94 82 87435 28307 53233242
Breath sounds 10.95 9.94 5 87512 126 53261423
Ischaemia 10.94 9.94 24 87493 4684 53256865
Blood blister 10.92 9.94 14 87503 1757 53259792
Left ventricular enlargement 10.92 9.94 4 87513 56 53261493
Phaeochromocytoma crisis 10.81 9.94 6 87511 231 53261318
Carcinoembryonic antigen increased 10.71 9.94 13 87504 1544 53260005
Premature baby 10.70 9.94 10 87507 19791 53241758
Fibromyalgia 10.52 9.94 37 87480 44038 53217511
Sinus arrest 10.48 9.94 14 87503 1830 53259719
Oral cavity fistula 10.47 9.94 9 87508 710 53260839
Cardiac murmur 10.46 9.94 43 87474 11870 53249679
Agitation 10.45 9.94 55 87462 58571 53202978
Hepatic vein dilatation 10.44 9.94 3 87514 18 53261531
Abdominal pain 10.42 9.94 330 87187 255573 53005976
Obstructive airways disorder 10.41 9.94 8 87509 17421 53244128
Post procedural hypothyroidism 10.34 9.94 5 87512 144 53261405
Photophobia 10.31 9.94 7 87510 16251 53245298
Angioedema 10.30 9.94 110 87407 41966 53219583
Quadriplegia 10.28 9.94 14 87503 1864 53259685
Anaphylactic reaction 10.24 9.94 55 87462 58271 53203278
Retinopathy hypertensive 10.21 9.94 6 87511 258 53261291
Heart rate decreased 10.19 9.94 99 87418 36848 53224701
Thrombosis 10.17 9.94 148 87369 60645 53200904
Fear 10.14 9.94 54 87463 16587 53244962
Injection site urticaria 10.11 9.94 4 87513 12603 53248946
Arthritis 10.08 9.94 93 87424 87205 53174344
Ventricular extrasystoles 10.04 9.94 42 87475 11682 53249867
Hip fracture 10.02 9.94 80 87437 28177 53233372
Sudden cardiac death 9.96 9.94 15 87502 2189 53259360

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
Cardiac failure congestive 1142.21 10.91 1359 99394 83493 32329280
Cardiac failure 467.46 10.91 937 99816 90736 32322037
Myocardial infarction 385.04 10.91 1052 99701 124624 32288149
Hypotension 367.40 10.91 1481 99272 214629 32198144
Bradycardia 272.76 10.91 651 100102 70911 32341862
Ejection fraction decreased 178.67 10.91 246 100507 17412 32395361
Coronary artery disease 156.70 10.91 421 100332 49285 32363488
Cardiac failure chronic 138.85 10.91 140 100613 7100 32405673
Hyperkalaemia 136.72 10.91 501 100252 69249 32343524
Acute myocardial infarction 134.32 10.91 426 100327 54723 32358050
Syncope 131.78 10.91 591 100162 89533 32323240
Ischaemic cardiomyopathy 124.46 10.91 125 100628 6309 32406464
Off label use 120.87 10.91 514 100239 305806 32106967
Mitral valve incompetence 118.32 10.91 185 100568 14686 32398087
Drug abuse 115.48 10.91 52 100701 80191 32332582
Dizziness 112.99 10.91 1067 99686 208551 32204222
Atrial fibrillation 109.63 10.91 677 100076 116027 32296746
Dyspnoea 105.14 10.91 1638 99115 360407 32052366
Ventricular tachycardia 104.31 10.91 239 100514 25317 32387456
Cardiac failure acute 103.19 10.91 142 100611 10042 32402731
Foetal exposure during pregnancy 97.88 10.91 8 100745 41293 32371480
Gastrointestinal haemorrhage 97.19 10.91 528 100225 86354 32326419
Cardiac disorder 97.02 10.91 318 100435 41548 32371225
Pyrexia 95.00 10.91 592 100161 319376 32093397
Blood pressure decreased 91.84 10.91 357 100396 50723 32362050
Cardiomyopathy 87.80 10.91 169 100584 15844 32396929
Neutropenia 87.75 10.91 194 100559 141981 32270792
Febrile neutropenia 81.54 10.91 154 100599 119412 32293361
International normalised ratio increased 78.04 10.91 330 100423 48705 32364068
Drug ineffective 74.54 10.91 795 99958 382682 32030091
Rheumatoid arthritis 73.88 10.91 23 100730 44521 32368252
Cardiomegaly 70.62 10.91 149 100604 14922 32397851
Chronic kidney disease 65.92 10.91 272 100481 39703 32373070
Cerebrovascular accident 61.48 10.91 468 100285 85852 32326921
Left ventricular dilatation 58.53 10.91 33 100720 678 32412095
Pulmonary oedema 52.23 10.91 282 100471 45985 32366788
Blood potassium increased 51.57 10.91 141 100612 16663 32396110
Completed suicide 51.19 10.91 474 100279 92043 32320730
Treatment failure 50.89 10.91 29 100724 39134 32373639
Bundle branch block left 50.34 10.91 75 100678 5704 32407069
Orthopnoea 48.65 10.91 69 100684 5018 32407755
Tricuspid valve incompetence 47.25 10.91 95 100658 9192 32403581
Congestive cardiomyopathy 47.05 10.91 82 100671 7120 32405653
Angina pectoris 46.54 10.91 207 100546 31219 32381554
Blood creatinine increased 46.09 10.91 478 100275 95654 32317119
N-terminal prohormone brain natriuretic peptide abnormal 45.41 10.91 19 100734 195 32412578
Coronary artery bypass 44.39 10.91 66 100687 5010 32407763
Drug reaction with eosinophilia and systemic symptoms 43.74 10.91 23 100730 32462 32380311
Renal impairment 43.47 10.91 456 100297 91516 32321257
Coronary arterial stent insertion 42.74 10.91 59 100694 4183 32408590
Computerised tomogram coronary artery abnormal 42.21 10.91 17 100736 157 32412616
Ventricular hypokinesia 41.84 10.91 63 100690 4837 32407936
Chest pain 41.80 10.91 577 100176 123560 32289213
Heart rate decreased 41.16 10.91 171 100582 25029 32387744
Hypoglycaemia 41.05 10.91 299 100454 54083 32358690
Suicidal ideation 40.51 10.91 35 100718 38048 32374725
Premature baby 40.20 10.91 5 100748 18513 32394260
Blood loss anaemia 39.98 10.91 81 100672 7881 32404892
Leukopenia 39.59 10.91 79 100674 60043 32352730
Fluid retention 38.64 10.91 174 100579 26376 32386397
Cardiac arrest 38.55 10.91 464 100289 96312 32316461
Toxicity to various agents 38.20 10.91 360 100393 177681 32235092
Product use in unapproved indication 37.59 10.91 141 100612 87063 32325710
Presyncope 37.03 10.91 128 100625 17173 32395600
Agitation 37.01 10.91 76 100677 57160 32355613
Acute kidney injury 36.09 10.91 1176 99577 292292 32120481
Malignant neoplasm progression 35.77 10.91 124 100629 78372 32334401
Sinus bradycardia 35.25 10.91 104 100649 12834 32399939
Suicide attempt 35.10 10.91 40 100713 38204 32374569
Depression 35.02 10.91 168 100585 96892 32315881
Diastolic dysfunction 34.80 10.91 60 100693 5164 32407609
Carotid sinus syndrome 34.54 10.91 10 100743 28 32412745
Drug dependence 34.10 10.91 15 100738 23469 32389304
Atrioventricular block 33.92 10.91 74 100679 7581 32405192
Oedema peripheral 33.54 10.91 518 100235 113573 32299200
Aggression 33.20 10.91 44 100709 39345 32373428
Fractured coccyx 32.69 10.91 14 100739 153 32412620
Hepatocellular injury 32.53 10.91 19 100734 25299 32387474
Left ventricular dysfunction 32.43 10.91 84 100669 9611 32403162
Blood pressure inadequately controlled 32.27 10.91 41 100712 2681 32410092
Mucosal inflammation 31.75 10.91 34 100719 33400 32379373
Renal failure 31.32 10.91 588 100165 133890 32278883
Cardiogenic shock 31.27 10.91 137 100616 20525 32392248
Cholestasis 31.06 10.91 23 100730 27010 32385763
Asthenia 30.67 10.91 952 99801 234992 32177781
Brain natriuretic peptide abnormal 30.47 10.91 17 100736 342 32412431
Ventricular internal diameter abnormal 30.46 10.91 12 100741 104 32412669
Cardioactive drug level increased 30.14 10.91 32 100721 1724 32411049
Arthralgia 29.79 10.91 305 100448 148143 32264630
Rales 29.68 10.91 71 100682 7730 32405043
Bradyarrhythmia 29.67 10.91 35 100718 2119 32410654
N-terminal prohormone brain natriuretic peptide increased 29.64 10.91 34 100719 1998 32410775
Mouth breathing 29.58 10.91 11 100742 80 32412693
Suspected suicide 28.85 10.91 41 100712 2987 32409786
Generalised tonic-clonic seizure 28.70 10.91 14 100739 20625 32392148
Nodal rhythm 28.50 10.91 29 100724 1486 32411287
Arrhythmia 27.73 10.91 196 100557 35107 32377666
Lower respiratory tract infection 27.47 10.91 30 100723 29213 32383560
Jugular vein distension 27.31 10.91 19 100734 571 32412202
Nodal arrhythmia 27.24 10.91 22 100731 832 32411941
Seizure 27.24 10.91 199 100554 103655 32309118
Sudden cardiac death 27.16 10.91 45 100708 3749 32409024
Alanine aminotransferase increased 27.06 10.91 138 100615 78341 32334432
Thrombocytopenia 26.84 10.91 312 100441 147987 32264786
Blood thyroid stimulating hormone abnormal 26.83 10.91 14 100739 245 32412528
Rash 26.76 10.91 472 100281 208861 32203912
Pulmonary arterial pressure abnormal 26.64 10.91 13 100740 196 32412577
Therapeutic product effect incomplete 26.63 10.91 55 100698 41286 32371487
Sinus arrest 26.53 10.91 29 100724 1615 32411158
Electrocardiogram QRS complex abnormal 26.48 10.91 15 100738 311 32412462
Blood glucose decreased 26.29 10.91 97 100656 13437 32399336
Infusion related reaction 25.86 10.91 65 100688 45534 32367239
Pancytopenia 25.80 10.91 171 100582 91064 32321709
Agranulocytosis 25.67 10.91 21 100732 23456 32389317
Neutrophil count decreased 25.35 10.91 69 100684 47070 32365703
Electrocardiogram abnormal 25.33 10.91 67 100686 7763 32405010
Rash maculo-papular 24.97 10.91 30 100723 27992 32384781
Blood urea increased 24.66 10.91 178 100575 32095 32380678
Shock 24.56 10.91 143 100610 23971 32388802
Pulmonary hypertension 24.54 10.91 127 100626 20367 32392406
Brain natriuretic peptide increased 24.33 10.91 46 100707 4254 32408519
Dyspnoea exertional 24.30 10.91 205 100548 38756 32374017
Fall 24.25 10.91 787 99966 195414 32217359
Orthostatic hypotension 24.14 10.91 149 100604 25501 32387272
Cytomegalovirus infection 24.06 10.91 26 100727 25438 32387335
Candida infection 23.98 10.91 11 100742 16792 32395981
Intentional overdose 23.82 10.91 59 100694 41542 32371231
Haemorrhage intracranial 23.78 10.91 105 100648 15782 32396991
Ventricular arrhythmia 23.54 10.91 50 100703 5029 32407744
Oxygen saturation increased 23.46 10.91 13 100740 258 32412515
Drug resistance 23.35 10.91 22 100731 22943 32389830
Nonalcoholic fatty liver disease 23.31 10.91 14 100739 325 32412448
Coma 23.20 10.91 62 100691 42550 32370223
Pericardial disease 23.12 10.91 14 100739 330 32412443
Pulmonary valve disease 22.97 10.91 13 100740 269 32412504
Oesophageal discomfort 22.68 10.91 8 100745 49 32412724
Neuroleptic malignant syndrome 22.66 10.91 13 100740 17482 32395291
Blood glucose increased 22.64 10.91 305 100448 64936 32347837
Glomerular filtration rate decreased 22.56 10.91 89 100664 12722 32400051
Neutrophil count increased 22.30 10.91 11 100742 16103 32396670
Sedation 22.29 10.91 15 100738 18511 32394262
End stage renal disease 22.27 10.91 65 100688 7972 32404801
Hypertensive crisis 22.25 10.91 69 100684 8748 32404025
Erythema 21.90 10.91 159 100594 82946 32329827
Cerebral infarction 21.50 10.91 153 100600 27461 32385312
Musculoskeletal stiffness 21.47 10.91 57 100696 39207 32373566
Conjunctival scar 21.30 10.91 8 100745 60 32412713
Ventricular fibrillation 21.24 10.91 108 100645 17202 32395571
Cardio-respiratory arrest 21.21 10.91 266 100487 55723 32357050
Angina unstable 21.09 10.91 85 100668 12270 32400503
Fluid overload 21.06 10.91 118 100635 19503 32393270
Death 21.02 10.91 1414 99339 381103 32031670
Drug withdrawal syndrome 21.02 10.91 19 100734 20212 32392561
Graft versus host disease 20.99 10.91 4 100749 10802 32401971
Full blood count decreased 20.78 10.91 106 100647 16904 32395869
Osteonecrosis 20.62 10.91 13 100740 16609 32396164
Epilepsy 20.42 10.91 23 100730 22086 32390687
Neutropenic sepsis 20.27 10.91 7 100746 12692 32400081
Mitral valve calcification 20.02 10.91 16 100737 596 32412177
Bone marrow failure 19.96 10.91 40 100713 30364 32382409
C-reactive protein increased 19.93 10.91 79 100674 48023 32364750
Serotonin syndrome 19.81 10.91 18 100735 19099 32393674
Injection site pain 19.63 10.91 46 100707 33012 32379761
Hepatitis 19.42 10.91 27 100726 23666 32389107
Type V hyperlipidaemia 19.31 10.91 17 100736 725 32412048
Bundle branch block 19.27 10.91 19 100734 937 32411836
Lymphadenopathy 19.21 10.91 34 100719 27048 32385725
Gingival hypertrophy 19.21 10.91 25 100728 1674 32411099
Nephrogenic anaemia 19.09 10.91 29 100724 2244 32410529
Intentional product use issue 19.00 10.91 67 100686 42144 32370629
Schizophrenia 18.76 10.91 4 100749 9980 32402793
Torsade de pointes 18.69 10.91 58 100695 7357 32405416
Myocardial ischaemia 18.53 10.91 106 100647 17653 32395120
Lymphopenia 18.36 10.91 11 100742 14445 32398328
Cardiac pacemaker insertion 18.27 10.91 31 100722 2634 32410139
Oedema 18.19 10.91 217 100536 44930 32367843
Vomiting 18.11 10.91 574 100179 234983 32177790
Abnormal behaviour 18.09 10.91 34 100719 26432 32386341
Loss of personal independence in daily activities 17.88 10.91 35 100718 26798 32385975
Concomitant disease progression 17.69 10.91 30 100723 2548 32410225
Gallbladder oedema 17.62 10.91 10 100743 208 32412565
Immune reconstitution inflammatory syndrome 17.62 10.91 4 100749 9555 32403218
Ejection fraction abnormal 17.58 10.91 18 100735 929 32411844
Conduction disorder 17.58 10.91 26 100727 1964 32410809
Progressive multifocal leukoencephalopathy 17.54 10.91 4 100749 9527 32403246
Implantable defibrillator insertion 17.53 10.91 16 100737 716 32412057
Pathogen resistance 17.49 10.91 4 100749 9506 32403267
Aspergillus infection 17.43 10.91 7 100746 11567 32401206
Atrioventricular block second degree 17.34 10.91 35 100718 3395 32409378
Left atrial dilatation 17.32 10.91 25 100728 1847 32410926
Atrioventricular block complete 17.28 10.91 64 100689 8880 32403893
Acute pulmonary oedema 17.20 10.91 58 100695 7683 32405090
Pulmonary embolism 17.13 10.91 171 100582 83488 32329285
Fatigue 17.10 10.91 1284 99469 349417 32063356
Intentional self-injury 17.06 10.91 11 100742 13889 32398884
Vascular graft 17.05 10.91 22 100731 1461 32411312
Pneumocystis jirovecii pneumonia 17.03 10.91 20 100733 18850 32393923
Haemophagocytic lymphohistiocytosis 16.84 10.91 7 100746 11328 32401445
Upper gastrointestinal haemorrhage 16.78 10.91 129 100624 23720 32389053
Hallucination 16.76 10.91 95 100658 52524 32360249
Cardiac discomfort 16.70 10.91 13 100740 466 32412307
Tremor 16.69 10.91 166 100587 81111 32331662
Bronchopulmonary aspergillosis 16.57 10.91 11 100742 13676 32399097
Arterial spasm 16.43 10.91 8 100745 120 32412653
Psychotic disorder 16.24 10.91 29 100724 22991 32389782
Pulmonary renal syndrome 16.22 10.91 9 100744 179 32412594
Asthma 16.04 10.91 76 100677 43989 32368784
Hypovolaemia 15.90 10.91 62 100691 8815 32403958
Urticaria 15.73 10.91 114 100639 59500 32353273
Mitral valve thickening 15.71 10.91 12 100741 418 32412355
Osteonecrosis of jaw 15.55 10.91 22 100731 19144 32393629
Periodontitis 15.51 10.91 24 100729 1887 32410886
Respiratory depression 15.49 10.91 11 100742 13200 32399573
Drug hypersensitivity 15.46 10.91 149 100604 73251 32339522
Ventricular extrasystoles 15.44 10.91 76 100677 11950 32400823
Extrapyramidal disorder 15.18 10.91 9 100744 11886 32400887
Overdose 15.04 10.91 185 100568 86892 32325881
Dizziness postural 14.86 10.91 46 100707 5826 32406947
Tumour lysis syndrome 14.71 10.91 14 100739 14533 32398240
Subdural haematoma 14.64 10.91 109 100644 19844 32392929
Cardioversion 14.52 10.91 16 100737 899 32411874
Mitral valve disease 14.45 10.91 19 100734 1285 32411488
Pulse waveform abnormal 14.43 10.91 4 100749 9 32412764
Colitis ulcerative 14.41 10.91 19 100734 17032 32395741
Physical examination abnormal 14.39 10.91 9 100744 225 32412548
Arteriosclerosis 14.35 10.91 70 100683 10964 32401809
Dyspnoea at rest 14.35 10.91 32 100721 3327 32409446
Cardioactive drug level above therapeutic 14.31 10.91 6 100747 62 32412711
Intracardiac thrombus 14.30 10.91 27 100726 2494 32410279
Pulmonary arterial pressure increased 14.26 10.91 18 100735 1169 32411604
Stenosis 14.23 10.91 17 100736 1043 32411730
Disturbance in attention 14.14 10.91 33 100720 23720 32389053
Gastrointestinal endoscopic therapy 14.14 10.91 4 100749 10 32412763
Oral candidiasis 14.12 10.91 10 100743 12017 32400756
Mouth ulceration 14.03 10.91 9 100744 11392 32401381
Embolic stroke 13.98 10.91 34 100719 3740 32409033
Aspartate aminotransferase increased 13.92 10.91 135 100618 66294 32346479
Anger 13.84 10.91 10 100743 11894 32400879
Infective pulmonary exacerbation of cystic fibrosis 13.74 10.91 5 100748 8774 32403999
Tachycardia induced cardiomyopathy 13.65 10.91 7 100746 118 32412655
Cerebral haemorrhage 13.55 10.91 166 100587 34581 32378192
Shunt occlusion 13.54 10.91 14 100739 731 32412042
Gravitational oedema 13.43 10.91 13 100740 627 32412146
Toxic skin eruption 13.19 10.91 10 100743 11604 32401169
Haematochezia 13.06 10.91 182 100571 39026 32373747
Substance abuse 13.05 10.91 3 100750 7104 32405669
Epstein-Barr virus infection 13.00 10.91 3 100750 7087 32405686
Lower gastrointestinal haemorrhage 12.99 10.91 58 100695 8759 32404014
Heart rate abnormal 12.97 10.91 21 100732 1716 32411057
Symblepharon 12.95 10.91 7 100746 132 32412641
Atrial flutter 12.93 10.91 86 100667 15097 32397676
Cardiac output decreased 12.89 10.91 15 100738 895 32411878
Azotaemia 12.60 10.91 41 100712 5333 32407440
Dyskinesia 12.35 10.91 35 100718 23568 32389205
Eosinophilia 12.34 10.91 38 100715 24920 32387853
Cerebellar haemorrhage 12.32 10.91 19 100734 1489 32411284
Human ehrlichiosis 12.28 10.91 8 100745 215 32412558
Coronary artery occlusion 12.28 10.91 69 100684 11416 32401357
Headache 12.12 10.91 491 100262 195706 32217067
Acute respiratory distress syndrome 12.10 10.91 39 100714 25214 32387559
Stomatitis 12.08 10.91 74 100679 40155 32372618
Dilatation atrial 12.08 10.91 23 100730 2138 32410635
Hypoglycaemic unconsciousness 12.08 10.91 14 100739 832 32411941
Blood pressure abnormal 12.03 10.91 51 100702 7529 32405244
Miosis 11.96 10.91 6 100747 8698 32404075
Supraventricular tachycardia 11.95 10.91 66 100687 10850 32401923
Tubulointerstitial nephritis 11.81 10.91 27 100726 19550 32393223
Acute generalised exanthematous pustulosis 11.73 10.91 3 100750 6610 32406163
Internal haemorrhage 11.72 10.91 37 100716 4735 32408038
Delusion 11.71 10.91 14 100739 13094 32399679
Anti-neutrophil cytoplasmic antibody positive vasculitis 11.66 10.91 13 100740 740 32412033
Hypertension 11.57 10.91 509 100244 131241 32281532
Colitis 11.52 10.91 60 100693 33891 32378882
Glycosylated haemoglobin increased 11.50 10.91 63 100690 10326 32402447
Sepsis 11.48 10.91 390 100363 158444 32254329
Goitre 11.45 10.91 19 100734 1585 32411188
Toxic goitre 11.41 10.91 3 100750 5 32412768
Large intestinal haemorrhage 11.41 10.91 19 100734 1590 32411183
Somnolence 11.40 10.91 240 100513 103557 32309216
Confusional state 11.40 10.91 347 100406 142768 32270005
Eczema 11.37 10.91 18 100735 14962 32397811
Blood pressure systolic decreased 11.36 10.91 34 100719 4229 32408544
Hydrothorax 11.30 10.91 11 100742 534 32412239
Chills 11.29 10.91 172 100581 77912 32334861
Inspiratory capacity decreased 11.25 10.91 6 100747 110 32412663
Jaundice 11.24 10.91 61 100692 34097 32378676
Injection site swelling 11.21 10.91 8 100745 9576 32403197
Procedural hypotension 11.20 10.91 15 100738 1033 32411740
Posterior reversible encephalopathy syndrome 11.19 10.91 8 100745 9568 32403205
Labile blood pressure 11.14 10.91 12 100741 657 32412116
Cholangitis sclerosing 11.13 10.91 15 100738 1039 32411734
Multiple organ dysfunction syndrome 11.10 10.91 151 100602 69703 32343070
Blood pressure increased 11.02 10.91 323 100430 79031 32333742
Hepatitis B 11.01 10.91 3 100750 6338 32406435
Atrial septal defect 10.99 10.91 4 100749 7021 32405752
Thyroiditis 10.98 10.91 21 100732 1959 32410814
Periorbital haemorrhage 10.97 10.91 6 100747 116 32412657
Myelosuppression 10.94 10.91 12 100741 11664 32401109

Pharmacologic Action:

SourceCodeDescription
ATC C07AG02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Alpha and beta blocking agents
ATC C07FX06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents, other combinations
FDA MoA N0000000099 Adrenergic alpha-Antagonists
FDA MoA N0000009923 Adrenergic beta1-Antagonists
FDA MoA N0000009924 Adrenergic beta2-Antagonists
FDA EPC N0000175553 alpha-Adrenergic Blocker
FDA EPC N0000175556 beta-Adrenergic Blocker
CHEBI has role CHEBI:35530 beta-adrenoceptor antagonists
CHEBI has role CHEBI:35554 cardiovascular drugs
CHEBI has role CHEBI:35620 vasodilator
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:37890 alpha-adrenoceptor antagonists
MeSH PA D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D000975 Antioxidants
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic heart failure indication 48447003
Left ventricular cardiac dysfunction indication 429589006
Atrial fibrillation off-label use 49436004 DOID:0060224
Diastolic heart failure off-label use 418304008 DOID:9775
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation off-label use
Bronchospasm contraindication 4386001
Complete atrioventricular block contraindication 27885002
Sick sinus syndrome contraindication 36083008 DOID:13884
Anaphylaxis contraindication 39579001
Low blood pressure contraindication 45007003
Sinus bradycardia contraindication 49710005
Hepatic failure contraindication 59927004
Chronic bronchitis contraindication 63480004 DOID:6132
Diabetes mellitus contraindication 73211009 DOID:9351
Prinzmetal angina contraindication 87343002
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Second degree atrioventricular block contraindication 195042002
Asthma contraindication 195967001 DOID:2841
Pregnancy, function contraindication 289908002
Peripheral vascular disease contraindication 400047006
Intraoperative floppy iris syndrome contraindication 418801006
Acutely Decompensated HF Requiring Parenteral Inotropic Therapy contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.13 acidic
pKa2 7.88 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF CONGESTIVE HEART FAILURE
10MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF HYPERTENSION
20MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF CONGESTIVE HEART FAILURE
20MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF HYPERTENSION
40MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF CONGESTIVE HEART FAILURE
40MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF HYPERTENSION
80MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF CONGESTIVE HEART FAILURE
80MG COREG CR WOODWARD N022012 Oct. 20, 2006 RX CAPSULE, EXTENDED RELEASE ORAL 7268156 June 27, 2023 TREATMENT OF HYPERTENSION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR ANTAGONIST Ki 9.90 IUPHAR CHEMBL
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 9.50 IUPHAR CHEMBL
D(1A) dopamine receptor GPCR Ki 6.13 DRUG MATRIX
D(2) dopamine receptor GPCR Ki 7.31 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 7.40 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.46 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 6.93 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 6.27 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR Ki 8.48 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.93 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 7.82 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 7.22 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 6.15 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 7.37 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.71 DRUG MATRIX
Beta-3 adrenergic receptor GPCR ANTAGONIST Ki 9.40 IUPHAR
Alpha-2C adrenergic receptor GPCR Ki 7.89 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 6.17 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 9.05 DRUG MATRIX
Potassium channel subfamily K member 2 Ion channel IC50 5.80 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 5.47 CHEMBL
Potassium channel subfamily K member 10 Ion channel IC50 5.12 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.12 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 4.03 CHEMBL
Toll-like receptor 4 Membrane receptor IC50 4.49 CHEMBL
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 8.66 WOMBAT-PK
Amyloid beta A4 protein Unclassified IC50 4.52 CHEMBL
Ryanodine receptor 2 Ion channel INHIBITOR IC50 4.80 IUPHAR
5-hydroxytryptamine receptor 4 GPCR Ki 6.74 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 8.71 DRUG MATRIX
5-hydroxytryptamine receptor 1B GPCR Ki 6.23 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 8.11 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 8.50 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 9.09 CHEMBL

External reference:

IDSource
4021041 VUID
N0000148505 NUI
D00255 KEGG_DRUG
610309-89-2 SECONDARY_CAS_RN
C0054836 UMLSCUI
CHEBI:3441 CHEBI
CVD PDB_CHEM_ID
CHEMBL723 ChEMBL_ID
CHEMBL1201167 ChEMBL_ID
D000077261 MESH_DESCRIPTOR_UI
DB01136 DRUGBANK_ID
2585 PUBCHEM_CID
551 IUPHAR_LIGAND_ID
5333 INN_ID
0K47UL67F2 UNII
20352 RXNORM
119032 MMSL
22339 MMSL
265288 MMSL
4363 MMSL
d03847 MMSL
004167 NDDF
011844 NDDF
108551001 SNOMEDCT_US
386870007 SNOMEDCT_US
426471008 SNOMEDCT_US
4021041 VANDF
4026028 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3370 CAPSULE, EXTENDED RELEASE 10 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3371 CAPSULE, EXTENDED RELEASE 20 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3372 CAPSULE, EXTENDED RELEASE 40 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3373 CAPSULE, EXTENDED RELEASE 80 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3383 CAPSULE, EXTENDED RELEASE 10 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3385 CAPSULE, EXTENDED RELEASE 20 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3387 CAPSULE, EXTENDED RELEASE 40 mg ORAL NDA 26 sections
COREGCR HUMAN PRESCRIPTION DRUG LABEL 1 0007-3388 CAPSULE, EXTENDED RELEASE 80 mg ORAL NDA 26 sections
COREG HUMAN PRESCRIPTION DRUG LABEL 1 0007-4139 TABLET, FILM COATED 3.13 mg ORAL NDA 26 sections
COREG HUMAN PRESCRIPTION DRUG LABEL 1 0007-4140 TABLET, FILM COATED 6.25 mg ORAL NDA 26 sections
COREG HUMAN PRESCRIPTION DRUG LABEL 1 0007-4141 TABLET, FILM COATED 12.50 mg ORAL NDA 26 sections
COREG HUMAN PRESCRIPTION DRUG LABEL 1 0007-4142 TABLET, FILM COATED 25 mg ORAL NDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0093-0051 TABLET, FILM COATED 3.13 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0093-0135 TABLET, FILM COATED 6.25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7295 TABLET, FILM COATED 12.50 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7296 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0378-3631 TABLET, FILM COATED 3.13 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0378-3632 TABLET, FILM COATED 6.25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0378-3633 TABLET, FILM COATED 12.50 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0378-3634 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-7944 TABLET, FILM COATED 3.13 mg ORAL ANDA 27 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-7945 TABLET, FILM COATED 12.50 mg ORAL ANDA 27 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-7946 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8018 TABLET, FILM COATED 6.25 mg ORAL ANDA 27 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8387 TABLET, FILM COATED 3.13 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8388 TABLET, FILM COATED 6.25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8389 TABLET, FILM COATED 12.50 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0615-8390 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0781-5221 TABLET, FILM COATED 3.13 mg ORAL ANDA 25 sections
Carvedilol HUMAN PRESCRIPTION DRUG LABEL 1 0781-5222 TABLET, FILM COATED 6.25 mg ORAL ANDA 25 sections