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

Stem definitionDrug idCAS RN
endothelin receptor antagonists 4809 441798-33-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • opsumit
  • ACT-064992
  • macitentan
an endothelin receptor antagonist that prevents the binding of ET-1 to both ETA and ETB receptors, macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells
  • Molecular weight: 588.28
  • Formula: C19H20Br2N6O4S
  • CLOGP: 4.30
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 2
  • TPSA: 128.22
  • ALOGS: -4.94
  • ROTB: 9

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 2013 EMA
Oct. 18, 2013 FDA ACTELION PHARMS LTD

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
Pulmonary arterial hypertension 3112.68 15.18 1533 139451 24395 46520683
Dyspnoea 2825.32 15.18 5320 135664 510228 46034850
Fluid retention 2545.85 15.18 1701 139283 49345 46495733
Hospitalisation 2403.16 15.18 1786 139198 61599 46483479
Drug ineffective 1456.61 15.18 174 140810 677664 45867414
Death 1452.40 15.18 3150 137834 332398 46212680
Dyspnoea exertional 1285.11 15.18 1126 139858 49163 46495915
Pain in jaw 1156.55 15.18 945 140039 37427 46507651
Nasal congestion 1131.47 15.18 1028 139956 47085 46497993
Pulmonary hypertension 1088.05 15.18 888 140096 35105 46509973
Transfusion 1063.86 15.18 599 140385 12632 46532446
Right ventricular failure 912.65 15.18 582 140402 15511 46529567
Headache 896.63 15.18 3316 137668 475036 46070042
Fluid overload 774.02 15.18 648 140336 26537 46518541
Oxygen saturation decreased 736.64 15.18 974 140010 68190 46476888
Off label use 600.93 15.18 200 140784 379641 46165437
Oedema 581.83 15.18 856 140128 66215 46478863
Catheter management 548.72 15.18 233 140751 2562 46542516
Toxicity to various agents 531.57 15.18 26 140958 211740 46333338
Product dose omission issue 512.30 15.18 1384 139600 167136 46377942
Catheter site erythema 508.67 15.18 246 140738 3737 46541341
Rheumatoid arthritis 497.98 15.18 68 140916 240147 46304931
Pneumonia 475.02 15.18 2317 138667 374003 46171075
Lung transplant 457.15 15.18 207 140777 2685 46542393
Catheter site pain 455.88 15.18 225 140759 3581 46541497
Cough 450.30 15.18 1622 139362 228627 46316451
Oedema peripheral 436.39 15.18 1262 139722 158444 46386634
Drug hypersensitivity 436.11 15.18 101 140883 243724 46301354
Catheter site pruritus 428.82 15.18 177 140807 1802 46543276
Unevaluable event 424.57 15.18 606 140378 45569 46499509
Oxygen consumption increased 419.36 15.18 210 140774 3453 46541625
Drug interaction 401.25 15.18 66 140918 203028 46342050
Infusion site pain 398.20 15.18 292 140692 9815 46535263
Pulmonary oedema 388.96 15.18 614 140370 50491 46494587
Peripheral swelling 382.63 15.18 1197 139787 156874 46388204
Neutropenia 367.65 15.18 15 140969 143189 46401889
Catheterisation cardiac 332.73 15.18 186 140798 3861 46541217
Chest pain 325.63 15.18 1220 139764 175104 46369974
Flushing 316.04 15.18 640 140344 63974 46481104
Therapy change 315.89 15.18 195 140789 4895 46540183
Hypotension 305.40 15.18 1450 139534 231139 46313939
Condition aggravated 294.11 15.18 1489 139495 243563 46301515
Pulmonary arterial pressure increased 287.24 15.18 158 140826 3174 46541904
Dialysis 275.16 15.18 235 140749 9881 46535197
Maternal exposure during pregnancy 265.67 15.18 10 140974 102539 46442539
Febrile neutropenia 264.96 15.18 4 140980 94623 46450455
Treatment failure 264.76 15.18 3 140981 93084 46451994
Catheter site discharge 255.44 15.18 123 140861 1849 46543229
Scleroderma 253.88 15.18 164 140820 4465 46540613
Malaise 247.18 15.18 1778 139206 329454 46215624
Hypoxia 243.45 15.18 505 140479 51333 46493745
Therapy non-responder 235.87 15.18 436 140548 40716 46504362
Dizziness 233.94 15.18 1792 139192 338622 46206456
Vascular device infection 229.14 15.18 139 140845 3378 46541700
Therapeutic product effect decreased 229.12 15.18 4 140980 82597 46462481
Catheter placement 227.27 15.18 113 140871 1828 46543250
Alopecia 225.69 15.18 104 140880 162310 46382768
Catheter site rash 224.99 15.18 85 140899 669 46544409
Catheter site infection 221.13 15.18 152 140832 4601 46540477
Catheter site haemorrhage 218.61 15.18 123 140861 2586 46542492
Rash 218.37 15.18 470 140514 356042 46189036
Contraindicated product administered 217.24 15.18 5 140979 79942 46465136
Palpitations 217.05 15.18 707 140277 94552 46450526
Concomitant disease aggravated 214.16 15.18 183 140801 7699 46537379
Catheter site swelling 213.37 15.18 96 140888 1225 46543853
Transplant evaluation 212.20 15.18 90 140894 986 46544092
Diarrhoea 205.26 15.18 2582 138402 557020 45988058
Device related infection 198.98 15.18 280 140704 20761 46524317
Productive cough 192.82 15.18 454 140530 50261 46494817
Overdose 188.63 15.18 39 140945 101940 46443138
Therapeutic product effect incomplete 185.50 15.18 13 140971 78140 46466938
Exposure during pregnancy 183.19 15.18 50 140934 108162 46436916
Psoriasis 181.12 15.18 15 140969 78589 46466489
Malignant neoplasm progression 180.66 15.18 3 140981 64923 46480155
Leukopenia 179.30 15.18 6 140978 68337 46476741
Syncope 176.67 15.18 705 140279 104098 46440980
Product use in unapproved indication 176.61 15.18 30 140954 90243 46454835
Drug abuse 176.14 15.18 3 140981 63405 46481673
Device alarm issue 174.91 15.18 85 140899 1305 46543773
Hospice care 173.32 15.18 137 140847 5158 46539920
Cardiac failure congestive 168.34 15.18 634 140350 91116 46453962
Device leakage 165.36 15.18 134 140850 5231 46539847
Thrombocytopenia 165.31 15.18 88 140896 126493 46418585
Cardiac pacemaker insertion 164.35 15.18 115 140869 3584 46541494
Rehabilitation therapy 162.47 15.18 77 140907 1115 46543963
Intentional overdose 159.51 15.18 9 140975 64935 46480143
Abdominal distension 157.74 15.18 534 140450 72817 46472261
Injection site pain 154.49 15.18 65 140919 107087 46437991
Infusion site erythema 153.90 15.18 150 140834 7492 46537586
Dyspnoea at rest 153.50 15.18 109 140875 3479 46541599
Stomatitis 152.06 15.18 15 140969 68282 46476796
Musculoskeletal stiffness 151.98 15.18 53 140931 97940 46447138
Cardiac failure 151.27 15.18 558 140426 79390 46465688
Infusion site infection 147.71 15.18 77 140907 1382 46543696
Acute kidney injury 143.28 15.18 312 140672 235543 46309535
Oxygen therapy 140.92 15.18 81 140903 1776 46543302
Catheter site irritation 139.10 15.18 53 140931 428 46544650
Cardiac operation 137.76 15.18 91 140893 2575 46542503
Disease progression 137.21 15.18 593 140391 90707 46454371
Epistaxis 136.37 15.18 466 140518 63839 46481239
Paracentesis 134.82 15.18 63 140921 882 46544196
Infusion site discharge 131.92 15.18 54 140930 537 46544541
Suicide attempt 131.04 15.18 9 140975 55027 46490051
Ascites 130.96 15.18 320 140664 36264 46508814
Device infusion issue 128.73 15.18 64 140920 1035 46544043
Infusion site swelling 128.35 15.18 119 140865 5580 46539498
Chest discomfort 127.84 15.18 576 140408 89693 46455385
Blood pressure increased 125.98 15.18 118 140866 126548 46418530
Injection site erythema 124.80 15.18 35 140949 74392 46470686
Dermatitis contact 123.23 15.18 137 140847 7986 46537092
Injection site reaction 122.75 15.18 5 140979 47844 46497234
Cardiac disorder 122.73 15.18 350 140634 43508 46501570
Anaphylactic reaction 122.72 15.18 10 140974 53102 46491976
Depression 122.56 15.18 203 140781 169901 46375177
Urticaria 121.81 15.18 106 140878 117786 46427292
Nasopharyngitis 121.62 15.18 839 140145 153159 46391919
Emergency care 119.71 15.18 56 140928 786 46544292
White blood cell count decreased 119.53 15.18 98 140886 112133 46432945
Arthropathy 119.50 15.18 53 140931 84647 46460431
Pericardial effusion 118.87 15.18 248 140736 25295 46519783
Electrocardiogram QT prolonged 117.66 15.18 10 140974 51315 46493763
Product use issue 116.10 15.18 71 140913 94573 46450505
Internal haemorrhage 116.09 15.18 101 140883 4354 46540724
Wrong technique in product usage process 113.52 15.18 15 140969 54407 46490671
Rhabdomyolysis 112.39 15.18 3 140981 41906 46503172
Brain natriuretic peptide increased 112.35 15.18 101 140883 4549 46540529
Seizure 110.63 15.18 125 140859 122929 46422149
Abortion spontaneous 110.50 15.18 5 140979 43641 46501437
Hypertension 110.14 15.18 271 140713 196085 46348993
Neutrophil count decreased 109.86 15.18 5 140979 43421 46501657
Influenza 109.19 15.18 546 140438 88724 46456354
Aspiration pleural cavity 108.74 15.18 52 140932 769 46544309
Hyponatraemia 108.50 15.18 88 140896 101244 46443834
Suicidal ideation 107.51 15.18 20 140964 56362 46488716
Central venous catheterisation 106.61 15.18 70 140914 1960 46543118
Presyncope 104.10 15.18 229 140755 24225 46520853
Disease complication 102.75 15.18 80 140904 2945 46542133
Osteoarthritis 102.45 15.18 30 140954 61995 46483083
Pancytopenia 101.30 15.18 66 140918 84992 46460086
Glossodynia 100.75 15.18 9 140975 44364 46500714
Plasma cell myeloma 98.40 15.18 10 140974 44468 46500610
Feeling abnormal 97.89 15.18 680 140304 124380 46420698
Packed red blood cell transfusion 97.86 15.18 68 140916 2095 46542983
Acute respiratory failure 97.06 15.18 248 140736 28890 46516188
Psoriatic arthropathy 96.10 15.18 3 140981 36376 46508702
Infusion site haemorrhage 95.21 15.18 67 140917 2107 46542971
Confusional state 94.97 15.18 214 140770 159678 46385400
Coma 94.96 15.18 29 140955 58320 46486758
N-terminal prohormone brain natriuretic peptide increased 94.76 15.18 61 140923 1650 46543428
Joint swelling 94.05 15.18 228 140756 165845 46379233
Respiratory failure 93.65 15.18 547 140437 94269 46450809
Drug intolerance 90.47 15.18 193 140791 146856 46398222
Device dislocation 90.36 15.18 202 140782 21600 46523478
Catheter site inflammation 89.85 15.18 43 140941 637 46544441
Mineral supplementation 89.56 15.18 41 140943 546 46544532
Hypersensitivity 89.42 15.18 201 140783 150120 46394958
Intentional product misuse 89.25 15.18 17 140967 47111 46497967
Dyspepsia 88.14 15.18 425 140559 68047 46477031
Product quality issue 87.34 15.18 5 140979 35643 46509435
Deep vein thrombosis 87.00 15.18 68 140916 79705 46465373
Dizziness postural 86.43 15.18 102 140882 6344 46538734
Catheter site related reaction 86.32 15.18 44 140940 752 46544326
Angioedema 84.10 15.18 10 140974 39332 46505746
Hepatic enzyme increased 82.70 15.18 75 140909 81712 46463366
Weight increased 82.70 15.18 809 140175 163664 46381414
Depressed level of consciousness 82.32 15.18 21 140963 47548 46497530
Walking distance test abnormal 81.62 15.18 37 140947 481 46544597
Intentional product use issue 81.03 15.18 29 140955 52751 46492327
Pulmonary veno-occlusive disease 80.28 15.18 44 140940 877 46544201
Sinus congestion 79.01 15.18 142 140842 12967 46532111
Seasonal allergy 78.53 15.18 143 140841 13191 46531887
Abdominal cavity drainage 78.50 15.18 33 140951 353 46544725
Bradycardia 78.19 15.18 52 140932 66246 46478832
Device occlusion 77.94 15.18 93 140891 5852 46539226
Adverse event 77.11 15.18 253 140731 33931 46511147
Myalgia 76.47 15.18 634 140350 122454 46422624
Bone marrow failure 76.43 15.18 3 140981 29666 46515412
Endarterectomy 75.82 15.18 26 140958 149 46544929
Renal disorder 75.65 15.18 214 140770 26472 46518606
Atrial septal defect repair 75.39 15.18 28 140956 209 46544869
Terminal state 75.24 15.18 59 140925 2195 46542883
Pulmonary endarterectomy 73.70 15.18 24 140960 114 46544964
Rhinorrhoea 73.41 15.18 312 140672 47353 46497725
Hepatocellular injury 72.76 15.18 4 140980 29518 46515560
Exercise tolerance decreased 72.55 15.18 79 140905 4498 46540580
Pulmonary pain 71.89 15.18 51 140933 1625 46543453
Lung disorder 71.83 15.18 290 140694 43014 46502064
C-reactive protein increased 71.77 15.18 44 140940 58546 46486532
Liver transplant 71.61 15.18 59 140925 2358 46542720
Catheter site vesicles 70.94 15.18 28 140956 251 46544827
Blood pressure decreased 70.85 15.18 351 140633 56808 46488270
Hallucination 70.85 15.18 31 140953 49920 46495158
Infusion site warmth 70.54 15.18 45 140939 1198 46543880
Paraesthesia 69.85 15.18 157 140827 117280 46427798
Nausea 68.97 15.18 2629 138355 684825 45860253
Injury 67.91 15.18 24 140960 44003 46501075
Injection site pruritus 67.90 15.18 18 140966 39725 46505353
Heart rate increased 67.79 15.18 422 140562 74369 46470709
Stent placement 66.42 15.18 67 140917 3489 46541589
Cognitive disorder 66.34 15.18 15 140969 36868 46508210
Pain in extremity 65.47 15.18 1121 139863 257559 46287519
Neuropathy peripheral 64.91 15.18 109 140875 90784 46454294
Blood creatine phosphokinase increased 64.65 15.18 5 140979 27719 46517359
Transplant 64.59 15.18 34 140950 623 46544455
Right ventricular dilatation 64.41 15.18 38 140946 876 46544202
Haemoglobin decreased 64.16 15.18 633 140351 128316 46416762
Impaired healing 64.01 15.18 16 140968 36727 46508351
Injection site swelling 63.91 15.18 21 140963 40306 46504772
Metabolic acidosis 63.59 15.18 19 140965 38761 46506317
Hypoglycaemia 63.58 15.18 43 140941 54306 46490772
Pulmonary arterial pressure abnormal 62.59 15.18 30 140954 446 46544632
Chemotherapy 62.33 15.18 43 140941 1309 46543769
Blood iron decreased 61.57 15.18 116 140868 10981 46534097
Blood cholesterol increased 61.39 15.18 22 140962 39991 46505087
Cardioversion 61.17 15.18 40 140944 1112 46543966
Cardiac ablation 60.31 15.18 41 140943 1218 46543860
Cholestasis 59.60 15.18 6 140978 26887 46518191
Illness 59.59 15.18 121 140863 12103 46532975
Pulmonary embolism 59.15 15.18 152 140832 108433 46436645
Atrial flutter 58.88 15.18 102 140882 9046 46536032
Left ventricular failure 58.85 15.18 74 140910 4916 46540162
Blood potassium decreased 58.49 15.18 249 140735 37814 46507264
Product supply issue 57.96 15.18 35 140949 843 46544235
Right ventricular dysfunction 57.85 15.18 43 140941 1475 46543603
Chronic obstructive pulmonary disease 57.85 15.18 334 140650 57299 46487779
Infusion site irritation 57.72 15.18 29 140955 480 46544598
Decreased appetite 57.26 15.18 862 140122 192974 46352104
Dysarthria 56.88 15.18 21 140963 37477 46507601
Hypocalcaemia 56.78 15.18 7 140977 26778 46518300
Therapeutic response decreased 56.27 15.18 30 140954 43115 46501963
Emotional distress 56.22 15.18 12 140972 30695 46514383
Pulmonary arterial wedge pressure increased 56.10 15.18 24 140960 269 46544809
Gout 56.06 15.18 113 140871 11243 46533835
Generalised tonic-clonic seizure 55.31 15.18 8 140976 27114 46517964
Toxic epidermal necrolysis 54.96 15.18 3 140981 22275 46522803
Stevens-Johnson syndrome 54.90 15.18 4 140980 23293 46521785
Diagnostic procedure 54.85 15.18 18 140966 88 46544990
Haemoptysis 54.79 15.18 189 140795 26000 46519078
Nasal dryness 54.76 15.18 60 140924 3440 46541638
Oropharyngeal pain 54.33 15.18 397 140587 73771 46471307
Sinus disorder 53.12 15.18 139 140845 16424 46528654
Angioplasty 53.07 15.18 38 140946 1229 46543849
Infusion site induration 53.02 15.18 32 140952 770 46544308
Biopsy 52.56 15.18 25 140959 365 46544713
Arthralgia 52.53 15.18 780 140204 363823 46181255
Catheter site warmth 52.37 15.18 21 140963 197 46544881
Inappropriate schedule of product administration 52.16 15.18 72 140912 64941 46480137
Hepatotoxicity 51.89 15.18 7 140977 25002 46520076
Hyperkalaemia 51.85 15.18 46 140938 50663 46494415
Hyperhidrosis 51.79 15.18 121 140863 89187 46455891
Agranulocytosis 51.74 15.18 4 140980 22181 46522897
Lymphocyte count decreased 51.15 15.18 8 140976 25581 46519497
Swollen tongue 50.39 15.18 13 140971 29219 46515859
Pericardial drainage 50.25 15.18 21 140963 221 46544857
Biopsy lung 49.38 15.18 19 140965 158 46544920
Blood pressure systolic increased 49.25 15.18 13 140971 28774 46516304
Somnolence 48.86 15.18 275 140709 156246 46388832
Hypercalcaemia 48.51 15.18 4 140980 21042 46524036
Bone disorder 48.50 15.18 3 140981 20030 46525048
Delirium 48.38 15.18 26 140958 37202 46507876
Drug dependence 48.12 15.18 3 140981 19898 46525180
Extra dose administered 48.03 15.18 65 140919 4642 46540436
Orthopnoea 47.97 15.18 73 140911 5807 46539271
Catheter site scab 47.88 15.18 19 140965 173 46544905
Psychotic disorder 47.73 15.18 6 140978 22615 46522463
Drug withdrawal syndrome 47.55 15.18 12 140972 27372 46517706
Hepatitis 47.28 15.18 19 140965 32196 46512882
Pulmonary congestion 47.26 15.18 124 140860 14675 46530403
Osteonecrosis 47.25 15.18 10 140974 25734 46519344
Pleural effusion 47.14 15.18 419 140565 82533 46462545
Pruritus 47.12 15.18 486 140498 241866 46303212
Respiration abnormal 47.00 15.18 63 140921 4458 46540620
Asthma 46.94 15.18 132 140852 91410 46453668
Agitation 46.88 15.18 59 140925 55356 46489722
Lactic acidosis 46.59 15.18 22 140962 33887 46511191
Concomitant disease progression 46.48 15.18 44 140940 2118 46542960
Blood glucose increased 46.38 15.18 92 140892 71921 46473157
Hyperglycaemia 46.30 15.18 24 140960 35047 46510031
Epilepsy 46.16 15.18 8 140976 23730 46521348
Mouth ulceration 46.13 15.18 12 140972 26820 46518258
Red blood cell sedimentation rate increased 46.11 15.18 7 140977 22882 46522196
Aggression 45.71 15.18 7 140977 22737 46522341
Medical device change 45.55 15.18 22 140962 333 46544745
Catheterisation cardiac abnormal 43.94 15.18 19 140965 219 46544859
Respiratory tract congestion 43.92 15.18 110 140874 12654 46532424
Fibromyalgia 43.80 15.18 28 140956 36435 46508643
Anaemia 43.53 15.18 1045 139939 254734 46290344
Cytomegalovirus infection 43.09 15.18 3 140981 18141 46526937
Medical procedure 42.78 15.18 18 140966 193 46544885
Medication error 42.55 15.18 20 140964 30891 46514187
Multiple allergies 42.08 15.18 78 140906 7293 46537785
Basal cell carcinoma 41.88 15.18 6 140978 20481 46524597
Blood count abnormal 41.83 15.18 134 140850 17744 46527334
Premature delivery 41.70 15.18 8 140976 22061 46523017
Oxygen saturation abnormal 41.50 15.18 46 140938 2672 46542406
Drug level increased 41.16 15.18 4 140980 18437 46526641
Mobility decreased 41.13 15.18 75 140909 60519 46484559
Wrong dose 41.06 15.18 27 140957 758 46544320
Catheter site discolouration 40.85 15.18 15 140969 108 46544970
Hernia repair 40.62 15.18 31 140953 1107 46543971
Premature baby 40.24 15.18 4 140980 18108 46526970
Dependence on oxygen therapy 39.92 15.18 20 140964 329 46544749
Infusion site pruritus 39.36 15.18 48 140936 3090 46541988
Pancreatitis acute 39.32 15.18 13 140971 24859 46520219
Skin lesion 38.80 15.18 16 140968 26697 46518381
Pericarditis 38.73 15.18 12 140972 23915 46521163
Cardiac output increased 38.65 15.18 15 140969 128 46544950
Head discomfort 38.59 15.18 92 140892 10259 46534819
Metastases to bone 38.46 15.18 4 140980 17472 46527606
Peritonitis 38.11 15.18 8 140976 20706 46524372
Hypokalaemia 38.07 15.18 137 140847 87887 46457191
Liver function test abnormal 37.77 15.18 51 140933 46436 46498642
Drug eruption 37.71 15.18 9 140975 21320 46523758
Choking 37.42 15.18 80 140904 8296 46536782
Encephalopathy 37.41 15.18 28 140956 33561 46511517
Polypectomy 37.33 15.18 23 140961 575 46544503
Cerebral infarction 37.32 15.18 12 140972 23354 46521724
Cardio-respiratory arrest 37.26 15.18 78 140906 59791 46485287
Drug-induced liver injury 37.16 15.18 15 140969 25353 46519725
Device connection issue 37.16 15.18 24 140960 653 46544425
Accidental exposure to product 37.07 15.18 9 140975 21072 46524006
Chronic respiratory failure 36.56 15.18 35 140949 1709 46543369
Dyskinesia 36.43 15.18 21 140963 28904 46516174
Ischaemic stroke 36.36 15.18 4 140980 16718 46528360
Infusion site discolouration 36.28 15.18 22 140962 534 46544544
Eosinophilia 36.24 15.18 7 140977 19210 46525868
Jugular vein distension 36.07 15.18 26 140958 850 46544228
Visual acuity reduced 35.95 15.18 11 140973 22102 46522976
Bronchitis 35.92 15.18 483 140501 105496 46439582
Hypoaesthesia 35.92 15.18 211 140773 118658 46426420
Heart valve replacement 35.72 15.18 21 140963 481 46544597
Diabetic ketoacidosis 35.71 15.18 6 140978 18204 46526874
Tremor 35.62 15.18 204 140780 115435 46429643
Hepatic steatosis 35.57 15.18 14 140970 24028 46521050
Withdrawal syndrome 35.50 15.18 6 140978 18128 46526950
Complication associated with device 35.46 15.18 115 140869 15326 46529752
Erythema 35.40 15.18 269 140715 142551 46402527
Blister 35.22 15.18 50 140934 44581 46500497
Hypoacusis 35.22 15.18 141 140843 20828 46524250
Pregnancy 35.19 15.18 19 140965 27118 46517960
Pyelonephritis 35.17 15.18 3 140981 15354 46529724
Abnormal behaviour 35.10 15.18 10 140974 21048 46524030
Nocturnal dyspnoea 34.91 15.18 27 140957 984 46544094
Pneumocystis jirovecii pneumonia 34.86 15.18 3 140981 15245 46529833
Hallucination, visual 34.80 15.18 6 140978 17867 46527211
Osteopenia 34.59 15.18 5 140979 16956 46528122
Pancreatitis 34.31 15.18 49 140935 43578 46501500
Coronary artery disease 34.05 15.18 31 140953 33721 46511357
No adverse event 33.87 15.18 32 140952 34199 46510879
Acute myocardial infarction 33.80 15.18 28 140956 31896 46513182
Swelling 33.78 15.18 546 140438 123965 46421113
Acute myeloid leukaemia 33.74 15.18 4 140980 15774 46529304
Skin exfoliation 33.53 15.18 30 140954 32908 46512170
Cor pulmonale 33.38 15.18 35 140949 1908 46543170
Metastases to liver 33.21 15.18 9 140975 19576 46525502
Cardiac failure high output 32.79 15.18 16 140968 248 46544830
Mood swings 32.67 15.18 5 140979 16247 46528831
Product prescribing error 32.54 15.18 10 140974 20037 46525041
Hepatic cirrhosis 32.44 15.18 113 140871 15619 46529459
Lymphopenia 32.40 15.18 4 140980 15289 46529789
Myoclonus 32.34 15.18 3 140981 14349 46530729
Altered state of consciousness 32.30 15.18 15 140969 23333 46521745
Oxygen consumption 32.14 15.18 12 140972 91 46544987
Endotracheal intubation 31.95 15.18 36 140948 2129 46542949
Spinal osteoarthritis 31.77 15.18 3 140981 14148 46530930
Osteoporosis 31.55 15.18 46 140938 40562 46504516
Catheter removal 31.37 15.18 17 140967 331 46544747
Paranasal sinus discomfort 30.99 15.18 39 140945 2593 46542485
Ejection fraction decreased 30.87 15.18 8 140976 17929 46527149
Heart and lung transplant 30.86 15.18 12 140972 103 46544975
Biopsy liver 30.78 15.18 18 140966 408 46544670
Sinus bradycardia 30.74 15.18 3 140981 13779 46531299
Foot deformity 30.43 15.18 5 140979 15420 46529658
Tracheostomy 30.43 15.18 20 140964 561 46544517
Cardiac failure acute 30.33 15.18 72 140912 8006 46537072
Biopsy bone marrow 30.31 15.18 16 140968 295 46544783
Hypertensive crisis 30.27 15.18 3 140981 13612 46531466
Device related sepsis 29.97 15.18 43 140941 3244 46541834
Catheter site nodule 29.97 15.18 10 140974 52 46545026
Catheter site dermatitis 29.66 15.18 10 140974 54 46545024
Disturbance in attention 29.50 15.18 31 140953 31529 46513549
Injection site rash 29.31 15.18 6 140978 15807 46529271
Proteinuria 29.23 15.18 7 140977 16546 46528532
Diplopia 29.21 15.18 11 140973 19394 46525684
Dysphagia 29.18 15.18 127 140857 77185 46467893
Cholecystectomy 29.11 15.18 76 140908 8966 46536112
Poisoning 28.84 15.18 4 140980 13990 46531088
Therapeutic response unexpected 28.79 15.18 6 140978 15610 46529468
Tubulointerstitial nephritis 28.72 15.18 5 140979 14783 46530295
Type 2 diabetes mellitus 28.71 15.18 12 140972 19863 46525215
Blood lactate dehydrogenase increased 28.63 15.18 13 140971 20487 46524591
Rash erythematous 28.60 15.18 37 140947 34313 46510765
Platelet transfusion 28.57 15.18 21 140963 708 46544370
Colitis ulcerative 28.51 15.18 9 140975 17723 46527355
Catheter site erosion 28.24 15.18 10 140974 64 46545014
Balance disorder 28.17 15.18 100 140884 64421 46480657
Localised oedema 28.14 15.18 53 140931 5016 46540062
Chest tube insertion 27.94 15.18 9 140975 41 46545037
Cardiac flutter 27.92 15.18 42 140942 3307 46541771
Haematuria 27.89 15.18 24 140960 26834 46518244
Femur fracture 27.68 15.18 43 140941 36954 46508124
Respiratory arrest 27.57 15.18 37 140947 33779 46511299
Carbon dioxide increased 27.38 15.18 25 140959 1149 46543929
Anxiety 27.27 15.18 386 140598 181571 46363507
Upper respiratory tract congestion 27.26 15.18 31 140953 1852 46543226
Acne 27.25 15.18 13 140971 19906 46525172
Biopsy lymph gland 27.18 15.18 8 140976 25 46545053
Dialysis related complication 27.11 15.18 10 140974 73 46545005
Hyperlipidaemia 27.09 15.18 11 140973 18528 46526550
Myelodysplastic syndrome 27.06 15.18 7 140977 15704 46529374
Disseminated intravascular coagulation 26.62 15.18 12 140972 18993 46526085
Systemic lupus erythematosus 26.52 15.18 104 140880 65076 46480002
Device physical property issue 26.51 15.18 27 140957 1422 46543656
Wound 26.43 15.18 56 140928 42746 46502332
Diet noncompliance 26.38 15.18 14 140970 261 46544817
Lower respiratory tract infection 26.38 15.18 82 140902 55007 46490071
Urinary retention 26.21 15.18 24 140960 26037 46519041
Dizziness exertional 26.17 15.18 15 140969 327 46544751
Cardiomyopathy 26.12 15.18 8 140976 16065 46529013
Ventilation perfusion mismatch 26.10 15.18 13 140971 211 46544867
Abdominal pain upper 26.00 15.18 598 140386 144707 46400371
Oral herpes 26.00 15.18 13 140971 19377 46525701
Myocardial infarction 25.94 15.18 180 140804 97348 46447730
Muscular weakness 25.68 15.18 167 140817 91677 46453401
Unevaluable investigation 25.67 15.18 8 140976 32 46545046
Joint range of motion decreased 25.55 15.18 7 140977 15117 46529961
Thrombectomy 25.49 15.18 12 140972 171 46544907
Medical device implantation 25.41 15.18 18 140966 572 46544506
Systemic scleroderma 25.36 15.18 21 140963 845 46544233
Palliative care 25.32 15.18 14 140970 284 46544794
Echocardiogram abnormal 25.23 15.18 22 140962 951 46544127
Drug ineffective for unapproved indication 25.22 15.18 9 140975 16404 46528674
Hip surgery 25.15 15.18 34 140950 2426 46542652
Infusion site vesicles 24.93 15.18 15 140969 359 46544719
Lip swelling 24.82 15.18 24 140960 25371 46519707
Critical illness 24.75 15.18 11 140973 136 46544942
Pulmonary vascular resistance abnormality 24.74 15.18 8 140976 37 46545041
Pulmonary artery aneurysm 24.74 15.18 8 140976 37 46545041
Cancer surgery 24.65 15.18 16 140968 439 46544639
Pericardial excision 24.51 15.18 7 140977 19 46545059
Iron deficiency anaemia 24.47 15.18 110 140874 17096 46527982
Infusion site abscess 24.42 15.18 12 140972 189 46544889
Sinus tachycardia 24.17 15.18 18 140966 21631 46523447
Right ventricular systolic pressure increased 24.09 15.18 17 140967 537 46544541
Heart valve operation 23.99 15.18 11 140973 147 46544931
Metastases to central nervous system 23.62 15.18 3 140981 11218 46533860
Aphasia 23.55 15.18 31 140953 28536 46516542
Treatment noncompliance 23.41 15.18 162 140822 29569 46515509
Discomfort 23.40 15.18 68 140916 46602 46498476
Secretion discharge 23.32 15.18 71 140913 9148 46535930
Cerebrovascular accident 23.31 15.18 194 140790 100845 46444233
Platelet count increased 23.12 15.18 8 140976 14866 46530212
Tenderness 23.12 15.18 11 140973 16870 46528208
Body temperature decreased 23.04 15.18 6 140978 13403 46531675
Transaminases increased 23.02 15.18 30 140954 27731 46517347
Haematoma 22.95 15.18 38 140946 31834 46513244
Dry eye 22.92 15.18 35 140949 30287 46514791
Right-to-left cardiac shunt 22.86 15.18 11 140973 165 46544913
Blood triglycerides increased 22.84 15.18 4 140980 11779 46533299
Bursitis 22.80 15.18 16 140968 19826 46525252
Joint stiffness 22.78 15.18 29 140955 27079 46517999
Pulmonary arterial pressure decreased 22.77 15.18 9 140975 81 46544997
Hypervolaemia 22.68 15.18 27 140957 1695 46543383
Catheter site extravasation 22.65 15.18 12 140972 223 46544855
Colonoscopy 22.64 15.18 23 140961 1208 46543870
Heart transplant 22.63 15.18 15 140969 427 46544651
Speech disorder 22.60 15.18 47 140937 36120 46508958
Brain natriuretic peptide abnormal 22.58 15.18 14 140970 354 46544724
Gastrointestinal tube insertion 22.53 15.18 22 140962 1101 46543977
Respiratory depression 22.35 15.18 4 140980 11596 46533482
Catheter site induration 22.35 15.18 8 140976 53 46545025
Hallucination, auditory 22.34 15.18 3 140981 10753 46534325
Application site pruritus 22.33 15.18 42 140942 3971 46541107
Arteriovenous malformation 22.29 15.18 23 140961 1230 46543848
Hypercholesterolaemia 22.17 15.18 4 140980 11526 46533552
Paranasal sinus hypersecretion 22.14 15.18 37 140947 3187 46541891
Jaundice 22.09 15.18 33 140951 28812 46516266
Paranoia 21.90 15.18 3 140981 10594 46534484
Breast cancer metastatic 21.88 15.18 7 140977 13671 46531407
CREST syndrome 21.87 15.18 14 140970 375 46544703
Cardiovascular disorder 21.83 15.18 5 140979 12182 46532896
Dysgeusia 21.79 15.18 57 140927 40434 46504644
Mydriasis 21.78 15.18 3 140981 10550 46534528
Catheter culture positive 21.72 15.18 10 140974 135 46544943
Tendonitis 21.64 15.18 8 140976 14269 46530809
Neutrophil count increased 21.58 15.18 8 140976 14245 46530833
Cor pulmonale chronic 21.53 15.18 11 140973 189 46544889
Spinal operation 21.48 15.18 50 140934 5490 46539588
Fear 21.45 15.18 11 140973 16161 46528917
Lymphadenopathy 21.37 15.18 43 140941 33445 46511633
Infusion site discomfort 21.32 15.18 17 140967 648 46544430
Atrial fibrillation 21.30 15.18 435 140549 103155 46441923
Delusion 21.25 15.18 4 140980 11184 46533894
Anhedonia 21.19 15.18 3 140981 10332 46534746
Ear congestion 21.13 15.18 26 140958 1689 46543389
Vitamin D deficiency 21.11 15.18 4 140980 11130 46533948
Drug therapy 21.09 15.18 6 140978 16 46545062
Cardiac monitoring 21.09 15.18 6 140978 16 46545062
Exostosis 20.99 15.18 3 140981 10260 46534818
Muscle twitching 20.97 15.18 9 140975 14663 46530415
Injection site haemorrhage 20.91 15.18 19 140965 20690 46524388
Sickle cell anaemia 20.86 15.18 16 140968 576 46544502
Gastrointestinal surgery 20.73 15.18 11 140973 205 46544873
Carpal tunnel syndrome 20.72 15.18 11 140973 15848 46529230
Pulmonary artery dilatation 20.63 15.18 11 140973 207 46544871
Pharyngeal oedema 20.48 15.18 9 140975 14462 46530616
Head injury 20.45 15.18 136 140848 24500 46520578
Injection site warmth 20.41 15.18 8 140976 13764 46531314
Irritability 20.39 15.18 35 140949 28911 46516167
Mania 20.35 15.18 4 140980 10842 46534236
Device breakage 20.31 15.18 70 140914 9622 46535456
Diabetes mellitus 20.29 15.18 80 140904 49985 46495093
Vasculitis 20.26 15.18 8 140976 13703 46531375
Thrombosis in device 20.20 15.18 34 140950 2945 46542133
Sensory disturbance 20.13 15.18 6 140978 12261 46532817
Renal tubular necrosis 20.12 15.18 4 140980 10755 46534323
Portopulmonary hypertension 20.06 15.18 9 140975 114 46544964
Abdominal pain 20.03 15.18 535 140449 229496 46315582
Injection site discharge 19.83 15.18 13 140971 363 46544715
Cardiac septal defect 19.80 15.18 12 140972 291 46544787
Blood pressure abnormal 19.60 15.18 81 140903 12136 46532942
Acute right ventricular failure 19.46 15.18 10 140974 174 46544904
Dialysis device insertion 19.45 15.18 6 140978 23 46545055
Living in residential institution 19.43 15.18 13 140971 376 46544702
Gastrointestinal haemorrhage 19.39 15.18 335 140649 77038 46468040
Infusion site rash 19.37 15.18 19 140965 956 46544122
Catheter site bruise 19.37 15.18 12 140972 303 46544775
Oral pain 19.35 15.18 28 140956 24769 46520309
Body height decreased 19.33 15.18 3 140981 9649 46535429
Congestive hepatopathy 19.32 15.18 30 140954 2428 46542650
Hypophagia 19.24 15.18 37 140947 29269 46515809
Joint dislocation 19.23 15.18 5 140979 11181 46533897
Liver ablation 19.22 15.18 4 140980 0 46545078
Immune tolerance induction 19.22 15.18 4 140980 0 46545078
Intervertebral disc degeneration 19.14 15.18 8 140976 13244 46531834
Live birth 18.98 15.18 4 140980 10326 46534752
Bronchospasm 18.94 15.18 12 140972 15695 46529383
Drug titration 18.91 15.18 5 140979 9 46545069
Gastroenteritis viral 18.82 15.18 106 140878 18013 46527065
Clostridium difficile infection 18.73 15.18 135 140849 24968 46520110
Medical device site haemorrhage 18.69 15.18 6 140978 27 46545051
Coordination abnormal 18.62 15.18 5 140979 10944 46534134
Laboratory test abnormal 18.62 15.18 25 140959 22822 46522256
Nervous system disorder 18.54 15.18 13 140971 16116 46528962
Drug titration error 18.47 15.18 15 140969 587 46544491
Mechanical ventilation 18.44 15.18 21 140963 1257 46543821
Hypothermia 18.18 15.18 7 140977 12176 46532902
Obstructive airways disorder 17.97 15.18 9 140975 13403 46531675
Right ventricular enlargement 17.75 15.18 11 140973 278 46544800
Labelled drug-drug interaction medication error 17.73 15.18 3 140981 9058 46536020
Drain placement 17.71 15.18 7 140977 63 46545015
Ecchymosis 17.67 15.18 5 140979 10571 46534507
Breast cancer 17.65 15.18 74 140910 45444 46499634
Oesophageal motility disorder 17.51 15.18 11 140973 285 46544793
Diabetes mellitus inadequate control 17.50 15.18 9 140975 13205 46531873
Retching 17.48 15.18 82 140902 12975 46532103
Viral infection 17.30 15.18 153 140831 30082 46514996
Brain oedema 17.29 15.18 8 140976 12470 46532608
Circulatory collapse 17.28 15.18 24 140960 21600 46523478
Catheter site dryness 17.27 15.18 6 140978 36 46545042
Myopathy 17.25 15.18 3 140981 8878 46536200
General physical health deterioration 17.18 15.18 246 140738 115523 46429555
Walking disability 17.16 15.18 21 140963 1357 46543721
Arthritis 17.14 15.18 150 140834 77166 46467912
Nightmare 17.03 15.18 15 140969 16583 46528495
Conjunctivitis 16.99 15.18 13 140971 15411 46529667
Respiratory syncytial virus infection 16.98 15.18 42 140942 4793 46540285
Cataract operation 16.98 15.18 38 140946 4065 46541013
Biopsy kidney 16.87 15.18 8 140976 116 46544962
Oxygen saturation increased 16.81 15.18 8 140976 117 46544961
Cardiac pacemaker replacement 16.78 15.18 11 140973 307 46544771
Sluggishness 16.74 15.18 41 140943 4650 46540428
Upper-airway cough syndrome 16.73 15.18 57 140927 7790 46537288
Adverse drug reaction 16.66 15.18 73 140911 44289 46500789
Blood bilirubin increased 16.58 15.18 167 140817 34017 46511061
Tooth disorder 16.57 15.18 28 140956 23275 46521803
Skin necrosis 16.51 15.18 3 140981 8601 46536477
Cardiac septal defect repair 16.46 15.18 4 140980 4 46545074
Full blood count decreased 16.44 15.18 26 140958 22185 46522893
Hypomagnesaemia 16.44 15.18 26 140958 22184 46522894
Throat irritation 16.41 15.18 146 140838 28755 46516323
Rales 16.36 15.18 65 140919 9566 46535512
Suture related complication 16.35 15.18 9 140975 181 46544897
Hemiparesis 16.32 15.18 22 140962 20047 46525031
Acute left ventricular failure 16.28 15.18 16 140968 807 46544271
Disorientation 16.26 15.18 57 140927 36861 46508217
Fluid intake restriction 16.24 15.18 5 140979 19 46545059
Petechiae 16.24 15.18 9 140975 12661 46532417
Metastases to lung 16.20 15.18 6 140978 10690 46534388
Life support 16.20 15.18 10 140974 251 46544827
Inflammation 16.14 15.18 84 140900 48697 46496381
Ear discomfort 16.11 15.18 51 140933 6710 46538368
Transient ischaemic attack 15.97 15.18 53 140931 34850 46510228
Fatigue 15.97 15.18 2084 138900 606613 45938465
Eczema 15.95 15.18 23 140961 20377 46524701
Spinal stenosis 15.95 15.18 9 140975 12534 46532544
Right atrial enlargement 15.94 15.18 7 140977 84 46544994
Acute respiratory distress syndrome 15.91 15.18 26 140958 21896 46523182
Leukocytosis 15.84 15.18 29 140955 23369 46521709
Haemolytic anaemia 15.81 15.18 5 140979 9837 46535241
Large intestinal polypectomy 15.79 15.18 9 140975 194 46544884
Oesophagogastroduodenoscopy 15.69 15.18 6 140978 49 46545029
Product storage error 15.67 15.18 8 140976 11784 46533294
Gastrointestinal endoscopic therapy 15.66 15.18 5 140979 22 46545056
Bronchial artery embolisation 15.58 15.18 4 140980 6 46545072
Infusion site inflammation 15.55 15.18 9 140975 200 46544878
Immune thrombocytopenia 15.54 15.18 3 140981 8238 46536840
Arteriosclerosis 15.54 15.18 5 140979 9728 46535350
Feeding tube user 15.48 15.18 5 140979 23 46545055
Bronchoscopy 15.48 15.18 6 140978 51 46545027
Mixed connective tissue disease 15.46 15.18 11 140973 352 46544726
Endoscopy 15.39 15.18 10 140974 275 46544803
Dysentery 15.37 15.18 15 140969 750 46544328
Arteriosclerosis coronary artery 15.32 15.18 3 140981 8153 46536925
Infusion site dryness 15.20 15.18 4 140980 7 46545071

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
Pulmonary arterial hypertension 1466.39 20.31 532 40733 8769 29902444
Fluid retention 1150.10 20.31 599 40666 24399 29886814
Dyspnoea 1012.85 20.31 1707 39558 331588 29579625
Hospitalisation 863.37 20.31 612 40653 43707 29867506
Death 809.27 20.31 1613 39652 355670 29555543
Pulmonary hypertension 592.23 20.31 353 40912 18683 29892530
Right ventricular failure 578.81 20.31 262 41003 7774 29903439
Pain in jaw 506.56 20.31 273 40992 11883 29899330
Dyspnoea exertional 431.55 20.31 371 40894 35059 29876154
Transfusion 431.32 20.31 209 41056 7252 29903961
Headache 370.01 20.31 790 40475 181516 29729697
Oxygen saturation decreased 325.48 20.31 348 40917 43092 29868121
Nasal congestion 318.99 20.31 238 41027 18328 29892885
Fluid overload 295.54 20.31 230 41035 18862 29892351
Oedema 295.23 20.31 329 40936 42664 29868549
Drug ineffective 247.55 20.31 81 41184 340306 29570907
Peripheral swelling 245.45 20.31 358 40907 60716 29850497
Drug interaction 232.66 20.31 10 41255 199558 29711655
Lung transplant 230.36 20.31 90 41175 1826 29909387
Toxicity to various agents 216.56 20.31 6 41259 177177 29734036
Condition aggravated 204.20 20.31 529 40736 137337 29773876
Oxygen consumption increased 203.90 20.31 74 41191 1214 29909999
Catheter management 201.09 20.31 67 41198 840 29910373
Oedema peripheral 165.79 20.31 415 40850 105417 29805796
Neutropenia 162.22 20.31 3 41262 128537 29782676
Catheterisation cardiac 158.21 20.31 72 41193 2159 29909054
Product dose omission issue 157.00 20.31 372 40893 91259 29819954
Catheter site erythema 143.23 20.31 56 41209 1138 29910075
Therapy non-responder 141.09 20.31 188 41077 29265 29881948
Flushing 133.29 20.31 183 41082 29309 29881904
Concomitant disease aggravated 126.15 20.31 82 41183 5047 29906166
Transplant evaluation 120.96 20.31 40 41225 489 29910724
Dialysis 119.39 20.31 108 41157 10888 29900325
Infusion site pain 117.29 20.31 62 41203 2588 29908625
Unevaluable event 115.63 20.31 178 41087 31607 29879606
Catheter site pain 110.42 20.31 45 41220 1023 29910190
Off label use 104.36 20.31 114 41151 249176 29662037
Weight increased 100.05 20.31 277 40988 74636 29836577
Hypoxia 98.32 20.31 209 41056 47645 29863568
Acute kidney injury 97.19 20.31 142 41123 273700 29637513
Thrombocytopenia 96.81 20.31 34 41231 137010 29774203
Catheter site pruritus 93.76 20.31 29 41236 281 29910932
Pulmonary arterial pressure increased 92.32 20.31 40 41225 1064 29910149
Pain in extremity 89.61 20.31 344 40921 109877 29801336
Drug abuse 89.59 20.31 6 41259 82066 29829147
Cough 89.28 20.31 376 40889 125266 29785947
Oxygen therapy 87.41 20.31 34 41231 681 29910532
Swelling 85.60 20.31 167 41098 35808 29875405
Malaise 85.32 20.31 454 40811 166508 29744705
Therapy change 85.25 20.31 50 41215 2559 29908654
Brain natriuretic peptide increased 83.60 20.31 58 41207 3977 29907236
Catheter site rash 82.91 20.31 24 41241 181 29911032
Pneumonia 79.80 20.31 755 40510 333551 29577662
Catheter site discharge 77.26 20.31 29 41236 525 29910688
Overdose 74.85 20.31 13 41252 84324 29826889
Pulmonary oedema 73.51 20.31 177 41088 43798 29867415
Dizziness 71.43 20.31 486 40779 194423 29716790
Aspiration pleural cavity 69.69 20.31 30 41235 785 29910428
Abdominal distension 68.02 20.31 176 41089 45533 29865680
Pancytopenia 67.48 20.31 17 41248 85035 29826178
Catheter site irritation 67.20 20.31 18 41247 98 29911115
Catheter placement 66.34 20.31 28 41237 697 29910516
Liver transplant 64.53 20.31 43 41222 2759 29908454
Productive cough 62.85 20.31 132 41133 29821 29881392
Leukopenia 61.59 20.31 4 41261 56155 29855058
Hypotension 58.05 20.31 473 40792 200092 29711121
Product use in unapproved indication 57.93 20.31 15 41250 73678 29837535
Disease complication 57.73 20.31 39 41226 2560 29908653
Paracentesis 56.42 20.31 21 41244 371 29910842
Syncope 56.31 20.31 249 41016 84654 29826559
Diarrhoea 56.17 20.31 704 40561 333399 29577814
Adverse event 55.88 20.31 86 41179 15255 29895958
Endarterectomy 53.08 20.31 16 41249 141 29911072
Rash 53.08 20.31 116 41149 191773 29719440
Cardiac pacemaker insertion 51.36 20.31 36 41229 2509 29908704
Packed red blood cell transfusion 51.24 20.31 30 41235 1530 29909683
Hyperkalaemia 50.82 20.31 14 41251 65996 29845217
Confusional state 50.61 20.31 67 41198 134767 29776446
Disease progression 50.52 20.31 231 41034 79643 29831570
Abdominal discomfort 50.50 20.31 165 41100 48626 29862587
Plasma cell myeloma 50.23 20.31 7 41258 53455 29857758
Drug hypersensitivity 50.07 20.31 16 41249 68503 29842710
Device dislocation 49.92 20.31 47 41218 4984 29906229
Vascular device infection 49.65 20.31 31 41234 1778 29909435
Cardiac operation 48.96 20.31 35 41230 2517 29908696
Nasopharyngitis 47.18 20.31 183 41082 58666 29852547
Hospice care 46.89 20.31 43 41222 4409 29906804
Sinus congestion 46.63 20.31 44 41221 4678 29906535
Pulmonary veno-occlusive disease 46.61 20.31 19 41246 432 29910781
Chronic obstructive pulmonary disease 45.96 20.31 154 41111 45972 29865241
Emergency care 45.76 20.31 15 41250 178 29911035
Lung operation 45.32 20.31 12 41253 62 29911151
Catheter site haemorrhage 44.48 20.31 31 41234 2141 29909072
Infusion site infection 44.15 20.31 17 41248 331 29910882
Acute respiratory failure 43.12 20.31 104 41161 25746 29885467
Chest pain 42.79 20.31 293 40972 117334 29793879
Cardiac failure 42.59 20.31 227 41038 83191 29828022
Cardiac ablation 41.61 20.31 19 41246 574 29910639
Walking distance test abnormal 41.40 20.31 13 41252 133 29911080
Cardiac disorder 41.36 20.31 135 41130 39758 29871455
Acute myocardial infarction 41.17 20.31 11 41254 52928 29858285
Seizure 41.11 20.31 45 41220 98430 29812783
Hallucination 40.48 20.31 9 41256 49050 29862163
Feeling abnormal 40.32 20.31 170 41095 56586 29854627
Pulmonary endarterectomy 40.31 20.31 11 41254 65 29911148
Hypertension 39.97 20.31 66 41199 121288 29789925
Infusion site erythema 39.70 20.31 26 41239 1620 29909593
Neuropathy peripheral 39.61 20.31 24 41241 70451 29840762
Deep vein thrombosis 39.38 20.31 17 41248 60484 29850729
Intentional product use issue 38.78 20.31 3 41262 36437 29874776
Device leakage 37.59 20.31 35 41230 3659 29907554
Atrial septal defect repair 37.00 20.31 11 41254 92 29911121
Abdominal cavity drainage 36.80 20.31 15 41250 341 29910872
Blood iron decreased 36.78 20.31 36 41229 4004 29907209
Psoriasis 36.72 20.31 7 41258 42499 29868714
Exercise tolerance decreased 36.65 20.31 35 41230 3777 29907436
White blood cell count decreased 36.56 20.31 37 41228 83910 29827303
Epistaxis 35.56 20.31 156 41109 52825 29858388
Cardiac failure congestive 35.41 20.31 218 41047 84189 29827024
Metabolic acidosis 34.96 20.31 5 41260 37456 29873757
Ascites 34.96 20.31 119 41146 35802 29875411
Stomatitis 34.74 20.31 5 41260 37274 29873939
Bradycardia 34.53 20.31 24 41241 65502 29845711
Dizziness exertional 34.48 20.31 11 41254 119 29911094
Internal haemorrhage 34.06 20.31 36 41229 4386 29906827
Device alarm issue 33.85 20.31 18 41247 760 29910453
Respiratory failure 33.84 20.31 246 41019 100396 29810817
Palpitations 33.36 20.31 112 41153 33461 29877752
Myocardial infarction 33.02 20.31 78 41187 125547 29785666
Stent placement 32.91 20.31 36 41229 4560 29906653
Delirium 32.44 20.31 8 41257 40623 29870590
Catheter site infection 32.23 20.31 27 41238 2454 29908759
Rehabilitation therapy 32.16 20.31 16 41249 587 29910626
Aggression 32.05 20.31 6 41259 36901 29874312
Wrong technique in product usage process 31.96 20.31 3 41262 31152 29880061
Rhinorrhoea 30.94 20.31 80 41185 20674 29890539
Terminal state 30.75 20.31 31 41234 3573 29907640
Coronary artery disease 30.74 20.31 15 41250 49697 29861516
Hernia repair 30.50 20.31 19 41246 1085 29910128
Device infusion issue 30.44 20.31 15 41250 539 29910674
Suture insertion 30.43 20.31 8 41257 40 29911173
Pyrexia 30.28 20.31 260 41005 294229 29616984
Hyperglycaemia 29.98 20.31 6 41259 35194 29876019
Heart rate increased 29.88 20.31 119 41146 38602 29872611
Hyperhidrosis 29.86 20.31 29 41236 67061 29844152
Rheumatoid arthritis 29.42 20.31 10 41255 41187 29870026
Platelet count decreased 29.42 20.31 64 41201 106065 29805148
Intentional product misuse 29.34 20.31 6 41259 34661 29876552
Biopsy liver 28.68 20.31 10 41255 145 29911068
Haemoptysis 28.54 20.31 101 41164 30977 29880236
Complication associated with device 28.11 20.31 37 41228 5683 29905530
Catheter site warmth 27.89 20.31 7 41258 28 29911185
Blood pressure increased 27.72 20.31 35 41230 71893 29839320
Catheter site swelling 27.66 20.31 11 41254 234 29910979
Dizziness postural 27.53 20.31 36 41229 5494 29905719
Infusion site haemorrhage 26.75 20.31 13 41252 453 29910760
Hypoglycaemia 26.43 20.31 19 41246 50962 29860251
Catheter removal 25.81 20.31 10 41255 198 29911015
Oxygen saturation abnormal 25.56 20.31 17 41248 1087 29910126
Lung disorder 25.32 20.31 98 41167 31371 29879842
Abnormal behaviour 24.92 20.31 3 41262 25620 29885593
Influenza 24.85 20.31 122 41143 43276 29867937
Device related infection 24.76 20.31 65 41200 16950 29894263
Hyponatraemia 24.57 20.31 34 41231 67168 29844045
Therapeutic product effect incomplete 24.53 20.31 8 41257 33826 29877387
Cardiac index increased 24.11 20.31 6 41259 23 29911190
Cholestasis 24.07 20.31 3 41262 24947 29886266
Gout 24.03 20.31 65 41200 17250 29893963
Suicidal ideation 23.73 20.31 10 41255 36104 29875109
Right ventricular dysfunction 23.70 20.31 15 41250 881 29910332
Diuretic therapy 23.53 20.31 6 41259 26 29911187
Agitation 23.34 20.31 24 41241 54049 29857164
Myalgia 23.28 20.31 183 41082 76484 29834729
Dyspepsia 23.22 20.31 93 41172 30236 29880977
Scleroderma 22.74 20.31 17 41248 1310 29909903
Urticaria 22.72 20.31 25 41240 54581 29856632
N-terminal prohormone brain natriuretic peptide increased 22.52 20.31 17 41248 1329 29909884
Chemotherapy 22.11 20.31 12 41253 528 29910685
Presyncope 22.01 20.31 60 41205 15996 29895217
Heart and lung transplant 22.00 20.31 7 41258 75 29911138
Cardioversion 21.67 20.31 14 41251 852 29910361
Depressed level of consciousness 21.49 20.31 13 41252 38209 29873004
Cerebral infarction 21.43 20.31 5 41260 26368 29884845
Spontaneous intrahepatic portosystemic venous shunt 21.03 20.31 5 41260 15 29911198
Heart valve operation 20.99 20.31 6 41259 43 29911170
Pneumonitis 20.79 20.31 6 41259 27448 29883765

Pharmacologic Action:

SourceCodeDescription
ATC C02KX04 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
OTHER ANTIHYPERTENSIVES
Antihypertensives for pulmonary arterial hypertension
FDA MoA N0000175364 Endothelin Receptor Antagonists
FDA EPC N0000175581 Endothelin Receptor Antagonist
MeSH PA D065130 Endothelin A Receptor Antagonists
MeSH PA D065131 Endothelin B Receptor Antagonists
MeSH PA D065128 Endothelin Receptor Antagonists
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:51451 era
CHEBI has role CHEBI:71031 orphan drugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pulmonary arterial hypertension indication 11399002
Pregnancy, function contraindication 289908002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.83 acidic
pKa2 10.58 acidic
pKa3 2.37 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
Endothelin-1 receptor GPCR ANTAGONIST IC50 9.30 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Endothelin B receptor GPCR ANTAGONIST IC50 6.41 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
D10135 KEGG_DRUG
4032833 VANDF
C2606557 UMLSCUI
CHEBI:76607 CHEBI
CHEMBL2103873 ChEMBL_ID
16004692 PUBCHEM_CID
DB08932 DRUGBANK_ID
C533860 MESH_SUPPLEMENTAL_RECORD_UI
7352 IUPHAR_LIGAND_ID
9018 INN_ID
Z9K9Y9WMVL UNII
1442132 RXNORM
206622 MMSL
29714 MMSL
d08126 MMSL
015242 NDDF
710283008 SNOMEDCT_US
715555005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
OPSUMIT HUMAN PRESCRIPTION DRUG LABEL 1 66215-501 TABLET, FILM COATED 10 mg ORAL NDA 32 sections