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

Stem definitionDrug idCAS RN
guanylate cyclase activators and stimulators 4807 625115-55-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • adempas
  • BAY 63-2521
  • riociguat
guanylate cyclase stimulator
  • Molecular weight: 422.42
  • Formula: C20H19FN8O2
  • CLOGP: 2.06
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 2
  • TPSA: 138.07
  • ALOGS: -3.79
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4.50 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.44 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.74 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9.10 hours Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.067 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.350 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 39.628 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.429 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 24.490 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 43.310 % High 1
herg hERG pIC50 4.460 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.556 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.767 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 9.440 % High 1
kinase-safety-class ACVR2B,GRK2,PDK1,PDK2,PDK4,PRKDC 6
kinase-selectivity-class ACVR2B,AXL 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 11.220 High 1
mh-clint Mouse hepatocyte intrinsic clearance 4.102 High 1
mppb Mouse plasma protein binding (% unbound) 17.320 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 23.605 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 43.590 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.692 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 81.710 % High 1
rppb Rat plasma protein binding (% unbound) 20.110 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 42.364 uM High 1

Approvals:

DateAgencyCompanyOrphan
Oct. 8, 2013 FDA BAYER HLTHCARE

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
Death 2128.56 22.56 2144 66838 454407 90105058
Hospitalisation 1964.21 22.56 1218 67764 126882 90432583
Dyspnoea 1437.08 22.56 2464 66518 878491 89680974
Hypotension 1266.62 22.56 1391 67591 324006 90235459
Fluid retention 1170.38 22.56 766 68216 87325 90472140
Dyspnoea exertional 1135.84 22.56 699 68283 71589 90487876
Pain in jaw 851.66 22.56 502 68480 47483 90511982
Pulmonary arterial hypertension 844.75 22.56 408 68574 25779 90533686
Headache 769.42 22.56 1884 67098 860862 89698603
Dizziness 657.95 22.56 1408 67574 587876 89971589
Drug ineffective 607.51 22.56 155 68827 1384143 89175322
Oedema peripheral 539.95 22.56 812 68170 257103 90302362
Oxygen saturation decreased 523.05 22.56 519 68463 106964 90452501
Right ventricular failure 471.98 22.56 249 68733 18956 90540509
Pulmonary hypertension 453.05 22.56 323 68659 42200 90517265
Hypervolaemia 449.47 22.56 291 68691 32466 90526999
Blood pressure decreased 417.78 22.56 390 68592 74505 90484960
Nausea 350.83 22.56 1717 67265 1108599 89450866
Diarrhoea 347.81 22.56 1522 67460 937668 89621797
Off label use 343.81 22.56 208 68774 1102044 89457421
Nasal congestion 296.27 22.56 341 68641 83073 90476392
Transfusion 291.92 22.56 176 68806 17312 90542153
Infusion related reaction 288.13 22.56 6 68976 416774 90142691
Epistaxis 287.32 22.56 339 68643 84786 90474679
Dyspepsia 277.90 22.56 522 68460 197638 90361827
Syncope 266.19 22.56 410 68572 132253 90427212
Catheterisation cardiac 258.13 22.56 108 68874 4848 90554617
Maternal exposure during pregnancy 238.31 22.56 8 68974 360055 90199410
Cough 235.39 22.56 715 68267 368247 90191218
Pulmonary arterial pressure increased 233.45 22.56 94 68888 3822 90555643
Palpitations 227.24 22.56 388 68594 136340 90423125
Arthropathy 223.40 22.56 14 68968 366228 90193237
Drug hypersensitivity 215.89 22.56 45 68937 463564 90095901
Treatment failure 211.48 22.56 4 68978 303924 90255541
Infusion site pain 208.01 22.56 149 68833 19589 90539876
Hepatic enzyme increased 208.01 22.56 18 68964 360718 90198747
Alopecia 207.31 22.56 60 68922 495011 90064454
Chest pain 203.36 22.56 619 68363 319026 90240439
Flushing 199.63 22.56 289 68693 88202 90471263
Rheumatoid arthritis 196.32 22.56 23 68959 362591 90196874
Rash 194.54 22.56 192 68790 795908 89763557
Haemoptysis 194.37 22.56 178 68804 33142 90526323
Dizziness postural 193.43 22.56 107 68875 8946 90550519
Lung transplant 190.76 22.56 80 68902 3612 90555853
Therapy change 190.64 22.56 103 68879 8219 90551246
Toxicity to various agents 188.32 22.56 7 68975 287839 90271626
Pulmonary endarterectomy 186.86 22.56 39 68943 118 90559347
Pericarditis 182.34 22.56 5 68977 270146 90289319
Contraindicated product administered 181.78 22.56 17 68965 320122 90239343
Catheter site erythema 178.38 22.56 83 68899 4811 90554654
Abdominal distension 175.47 22.56 338 68644 130263 90429202
Oedema 175.18 22.56 436 68546 199859 90359606
Hypoxia 169.96 22.56 241 68741 72158 90487307
Catheter management 167.70 22.56 69 68913 2967 90556498
Oxygen consumption increased 164.70 22.56 77 68905 4512 90554953
Wound 164.51 22.56 19 68963 302961 90256504
Oxygen therapy 162.90 22.56 68 68914 3034 90556431
Unevaluable event 156.84 22.56 201 68781 54647 90504818
Peripheral swelling 155.27 22.56 674 68308 412432 90147033
Catheter site pruritus 153.79 22.56 60 68922 2242 90557223
Feeling abnormal 153.59 22.56 371 68611 166864 90392601
Product use in unapproved indication 151.65 22.56 35 68947 336201 90223264
Impaired healing 148.81 22.56 7 68975 234192 90325273
Helicobacter infection 146.71 22.56 6 68976 226844 90332621
Exposure during pregnancy 145.65 22.56 9 68973 238401 90321064
Hypersensitivity 145.07 22.56 83 68899 454594 90104871
Systemic lupus erythematosus 143.97 22.56 48 68934 361848 90197617
Blood pressure systolic decreased 143.70 22.56 89 68893 9181 90550284
Blood cholesterol increased 143.61 22.56 3 68979 208009 90351456
Neutropenia 135.87 22.56 9 68973 224895 90334570
Musculoskeletal stiffness 131.47 22.56 32 68950 296500 90262965
Transplant evaluation 130.04 22.56 46 68936 1300 90558165
Cardiac failure 128.62 22.56 268 68714 109228 90450237
Pericardial effusion 128.04 22.56 149 68833 36684 90522781
Product dose omission issue 123.65 22.56 494 68488 291193 90268272
Presyncope 123.03 22.56 136 68846 31669 90527796
Vascular device infection 120.85 22.56 88 68894 11864 90547601
Endarterectomy 119.49 22.56 29 68953 200 90559265
Dyspnoea at rest 117.34 22.56 62 68920 4729 90554736
Catheter site pain 116.61 22.56 65 68917 5514 90553951
Blister 116.03 22.56 26 68956 254972 90304493
Lower respiratory tract infection 115.18 22.56 25 68957 250634 90308831
Heart rate increased 115.11 22.56 261 68721 112641 90446824
Central venous catheterisation 113.33 22.56 51 68931 2735 90556730
Vomiting 113.03 22.56 1002 67980 787291 89772174
Drug interaction 112.86 22.56 35 68947 276418 90283047
Urticaria 110.28 22.56 50 68932 312684 90246781
Irritable bowel syndrome 110.13 22.56 14 68968 207434 90352031
Ascites 106.28 22.56 155 68827 47585 90511880
Liver injury 105.49 22.56 6 68976 170561 90388904
Device related infection 104.49 22.56 113 68869 25673 90533792
Osteoarthritis 104.41 22.56 13 68969 195717 90363748
Pulmonary oedema 104.13 22.56 177 68805 61903 90497562
Hypertension 102.93 22.56 118 68864 457414 90102051
Discomfort 102.92 22.56 40 68942 274295 90285170
Catheter site haemorrhage 102.88 22.56 52 68930 3616 90555849
Emergency care 101.17 22.56 40 68942 1549 90557916
Catheter site discharge 100.86 22.56 45 68937 2364 90557101
Fibromyalgia 100.16 22.56 18 68964 206251 90353214
C-reactive protein increased 99.35 22.56 11 68971 181378 90378087
Cardiac failure congestive 99.32 22.56 227 68755 98467 90460998
Injury 98.51 22.56 16 68966 197333 90362132
Mobility decreased 96.66 22.56 35 68947 250699 90308766
Blood pressure diastolic decreased 95.72 22.56 110 68872 26716 90532749
Blood potassium decreased 94.90 22.56 147 68835 47580 90511885
Pneumonia 93.89 22.56 816 68166 637243 89922222
Blood pressure abnormal 93.81 22.56 94 68888 19551 90539914
Productive cough 92.09 22.56 190 68792 76873 90482592
Confusional state 91.94 22.56 95 68887 386110 90173355
Chest discomfort 91.60 22.56 272 68710 138093 90421372
Device alarm issue 87.96 22.56 38 68944 1847 90557618
Device occlusion 86.34 22.56 65 68917 9217 90550248
Catheter site swelling 85.84 22.56 37 68945 1788 90557677
Malaise 84.91 22.56 747 68235 585239 89974226
Therapeutic product effect incomplete 83.83 22.56 22 68960 193874 90365591
Psoriasis 83.40 22.56 8 68974 147746 90411719
Gastrooesophageal reflux disease 83.05 22.56 297 68685 166040 90393425
Acute respiratory failure 82.29 22.56 130 68852 42788 90516677
Drug intolerance 81.96 22.56 134 68848 447457 90112008
Haemoglobin decreased 79.86 22.56 288 68694 161668 90397797
Walking distance test abnormal 79.85 22.56 26 68956 567 90558898
Angioplasty 79.65 22.56 33 68949 1444 90558021
Pruritus 79.35 22.56 185 68797 541340 90018125
Brain natriuretic peptide increased 79.03 22.56 52 68930 5953 90553512
Ill-defined disorder 78.01 22.56 22 68960 184869 90374596
Localised oedema 77.56 22.56 52 68930 6142 90553323
Hypoaesthesia 76.23 22.56 76 68906 314134 90245331
Constipation 75.36 22.56 416 68566 279979 90279486
Pulmonary thrombosis 74.77 22.56 61 68921 9721 90549744
Asthma 74.61 22.56 46 68936 242114 90317351
Infusion site erythema 73.87 22.56 70 68912 13600 90545865
Catheter site rash 71.60 22.56 26 68956 794 90558671
Rehabilitation therapy 70.46 22.56 33 68949 1941 90557524
Infusion site infection 69.65 22.56 36 68946 2624 90556841
General physical health deterioration 68.13 22.56 103 68879 355012 90204453
Thrombocytopenia 66.62 22.56 38 68944 208687 90350778
Fatigue 66.53 22.56 1239 67743 1152784 89406681
Product use issue 65.92 22.56 93 68889 329826 90229639
Gastrointestinal haemorrhage 64.12 22.56 182 68800 90066 90469399
Scleroderma 63.07 22.56 46 68936 6215 90553250
Catheter site infection 62.60 22.56 44 68938 5610 90553855
Decreased appetite 62.42 22.56 495 68487 376045 90183420
Medical procedure 61.79 22.56 21 68961 525 90558940
Obesity 61.47 22.56 5 68977 105502 90453963
Myalgia 61.27 22.56 280 68702 174845 90384620
Infection 61.16 22.56 114 68868 361980 90197485
Overdose 60.78 22.56 22 68960 157687 90401778
Internal haemorrhage 58.84 22.56 44 68938 6176 90553289
Night sweats 58.80 22.56 13 68969 128753 90430712
Mineral supplementation 58.63 22.56 22 68960 738 90558727
Dizziness exertional 58.40 22.56 20 68962 512 90558953
Lip dry 58.22 22.56 5 68977 100950 90458515
Loss of consciousness 58.11 22.56 236 68746 140002 90419463
Disease complication 57.92 22.56 36 68946 3736 90555729
Injection site reaction 57.67 22.56 3 68979 92077 90467388
Prescribed overdose 55.85 22.56 5 68977 97620 90461845
Dialysis 55.55 22.56 55 68927 11274 90548191
Delirium 55.47 22.56 7 68975 104352 90455113
Intentional product use issue 55.46 22.56 50 68932 216842 90342623
Sleep disorder 55.15 22.56 42 68940 197988 90361477
Diastolic hypotension 54.70 22.56 13 68969 81 90559384
Retching 54.41 22.56 70 68912 19089 90540376
Depression 54.04 22.56 91 68891 300510 90258955
Flatulence 52.99 22.56 105 68877 41262 90518203
Complication associated with device 52.03 22.56 69 68913 19380 90540085
Device leakage 51.78 22.56 50 68932 9941 90549524
Pain in extremity 51.65 22.56 547 68435 449982 90109483
Anaphylactic reaction 51.40 22.56 4 68978 87520 90471945
Head injury 51.07 22.56 88 68894 31100 90528365
Inflammation 50.86 22.56 37 68945 178555 90380910
Drug-induced liver injury 50.67 22.56 5 68977 90313 90469152
Paraesthesia 50.55 22.56 70 68912 250256 90309209
Wound infection 50.11 22.56 10 68972 106392 90453073
Pulmonary veno-occlusive disease 49.67 22.56 24 68958 1514 90557951
Paracentesis 49.53 22.56 21 68961 974 90558491
Catheter placement 48.95 22.56 28 68954 2496 90556969
Peripheral venous disease 48.82 22.56 4 68978 83917 90475548
Epilepsy 47.60 22.56 4 68978 82202 90477263
Catheter site irritation 47.30 22.56 18 68964 628 90558837
Seasonal allergy 45.97 22.56 71 68911 22912 90536553
Gastric disorder 45.51 22.56 87 68895 33297 90526168
Renal disorder 44.81 22.56 93 68889 37766 90521699
Catheter site related reaction 44.64 22.56 20 68962 1061 90558404
White blood cell count decreased 44.57 22.56 37 68945 167072 90392393
Pulmonary artery therapeutic procedure 44.23 22.56 9 68973 23 90559442
Gout 43.86 22.56 59 68923 16800 90542665
Exercise tolerance decreased 43.36 22.56 40 68942 7511 90551954
Sinusitis 42.72 22.56 127 68855 342961 90216504
Hepatitis 42.20 22.56 3 68979 70736 90488729
Cardiac disorder 41.67 22.56 116 68866 56756 90502709
Osteoporosis 41.61 22.56 11 68971 96520 90462945
Weight decreased 41.53 22.56 457 68525 379453 90180012
Pulmonary fibrosis 41.41 22.56 15 68967 107488 90451977
Cognitive disorder 41.24 22.56 3 68979 69404 90490061
Dehydration 41.04 22.56 271 68711 194176 90365289
Dermatitis contact 40.71 22.56 51 68931 13544 90545921
Rales 40.58 22.56 55 68927 15772 90543693
Medication error 39.77 22.56 8 68974 84644 90474821
Generalised oedema 39.72 22.56 60 68922 18993 90540472
Cardiac failure acute 39.36 22.56 47 68935 11882 90547583
Device dislocation 39.23 22.56 79 68903 31403 90528062
Hyponatraemia 38.89 22.56 27 68955 133511 90425954
Autoimmune disorder 38.78 22.56 6 68976 76738 90482727
Acute kidney injury 38.17 22.56 121 68861 320266 90239199
Dry mouth 37.62 22.56 51 68931 184008 90375457
Anaemia 37.46 22.56 422 68560 352380 90207085
Right ventricular dysfunction 37.41 22.56 23 68959 2341 90557124
Device infusion issue 37.36 22.56 24 68958 2638 90556827
Therapeutic response decreased 37.24 22.56 11 68971 89718 90469747
Influenza 36.95 22.56 206 68776 139058 90420407
Decreased activity 36.92 22.56 38 68944 8154 90551311
Suicidal ideation 36.81 22.56 6 68976 73849 90485616
Depressed level of consciousness 36.08 22.56 6 68976 72778 90486687
Pulmonary congestion 36.06 22.56 58 68924 19375 90540090
Pulmonary arterial wedge pressure increased 35.80 22.56 13 68969 397 90559068
Catheter site vesicles 35.80 22.56 13 68969 397 90559068
Joint swelling 35.41 22.56 231 68751 503069 90056396
No adverse event 35.08 22.56 5 68977 67977 90491488
Pyrexia 34.46 22.56 329 68653 660156 89899309
Choking 34.22 22.56 44 68938 11989 90547476
Respiratory failure 34.00 22.56 179 68803 118239 90441226
Abdominal pain upper 34.00 22.56 395 68587 332279 90227186
Lung operation 33.40 22.56 12 68970 355 90559110
Arthralgia 33.31 22.56 406 68576 778116 89781349
Hospice care 33.29 22.56 39 68943 9665 90549800
Drug titration error 33.13 22.56 17 68965 1220 90558245
Knee arthroplasty 33.08 22.56 11 68971 83171 90476294
Nasal dryness 32.89 22.56 30 68952 5553 90553912
Asthenia 32.62 22.56 579 68403 533172 90026293
Blood iron decreased 32.50 22.56 53 68929 17906 90541559
Road traffic accident 31.02 22.56 22 68960 107604 90451861
Concomitant disease aggravated 31.02 22.56 41 68941 11477 90547988
Blood pressure increased 30.76 22.56 65 68917 197152 90362313
Cardiac pacemaker insertion 30.60 22.56 26 68956 4381 90555084
Pulmonary artery occlusion 30.59 22.56 7 68975 36 90559429
Wheezing 30.44 22.56 87 68895 237993 90321472
Amnesia 30.21 22.56 23 68959 108482 90450983
Myelosuppression 29.97 22.56 3 68979 53588 90505877
Atrial fibrillation 29.88 22.56 189 68793 133422 90426043
Drug ineffective for unapproved indication 29.88 22.56 7 68975 66637 90492828
Infusion site discharge 29.43 22.56 20 68962 2415 90557050
Infusion site swelling 28.95 22.56 40 68942 11680 90547785
Cardiac operation 28.87 22.56 24 68958 3925 90555540
Sciatica 28.86 22.56 21 68961 101361 90458104
Biopsy liver 28.12 22.56 11 68971 414 90559051
Product supply issue 27.93 22.56 21 68961 2971 90556494
Arthritis 27.93 22.56 53 68929 167262 90392203
Lactic acidosis 27.77 22.56 3 68979 50460 90509005
Clostridium difficile infection 27.61 22.56 75 68907 36170 90523295
Device connection issue 27.58 22.56 14 68968 982 90558483
Intestinal obstruction 27.46 22.56 76 68906 37055 90522410
Oxygen saturation abnormal 27.15 22.56 24 68958 4264 90555201
Fall 27.10 22.56 516 68466 481294 90078171
Coma 26.54 22.56 11 68971 72621 90486844
Loss of personal independence in daily activities 26.53 22.56 39 68943 136066 90423399
Jugular vein distension 26.36 22.56 14 68968 1079 90558386
Dry eye 26.14 22.56 6 68976 57925 90501540
Infusion site haemorrhage 26.03 22.56 26 68956 5385 90554080
Haemorrhage 25.81 22.56 113 68869 69256 90490209
Liver function test abnormal 25.63 22.56 4 68978 50841 90508624
Abortion spontaneous 25.62 22.56 5 68977 54051 90505414
Right ventricular dilatation 25.54 22.56 16 68966 1683 90557782
Cor pulmonale 25.09 22.56 17 68965 2043 90557422
Pancytopenia 24.90 22.56 33 68949 120230 90439235
Incorrect product administration duration 24.69 22.56 49 68933 19273 90540192
Vascular device occlusion 24.64 22.56 10 68972 415 90559050
Critical illness 24.33 22.56 9 68973 290 90559175
Infusion site induration 24.24 22.56 15 68967 1544 90557921
Pain 24.18 22.56 576 68406 995765 89563700
Hip arthroplasty 24.12 22.56 14 68968 76194 90483271
Pulmonary vascular resistance abnormality 24.07 22.56 7 68975 103 90559362
Head discomfort 24.05 22.56 44 68938 16289 90543176
Alanine aminotransferase increased 23.96 22.56 33 68949 118305 90441160
Lower limb fracture 23.69 22.56 18 68964 84995 90474470
Pulmonary pain 23.55 22.56 24 68958 5090 90554375
Deep vein thrombosis 23.55 22.56 21 68961 91599 90467866
Cardioversion 23.40 22.56 14 68968 1356 90558109
Gait inability 23.06 22.56 48 68934 146408 90413057
Therapy cessation 22.64 22.56 70 68912 36291 90523174

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
Death 904.21 26.67 1147 20619 470038 42129531
Hospitalisation 682.29 26.67 441 21325 73889 42525680
Fluid retention 519.48 26.67 274 21492 31345 42568224
Dyspnoea 426.93 26.67 786 20980 441835 42157734
Dyspnoea exertional 314.75 26.67 236 21530 49912 42549657
Hypotension 302.27 26.67 500 21266 257131 42342438
Pulmonary hypertension 282.18 26.67 166 21600 23403 42576166
Pulmonary arterial hypertension 281.12 26.67 126 21640 10061 42589508
Pain in jaw 273.45 26.67 138 21628 14364 42585205
Headache 252.02 26.67 443 21323 238926 42360643
Right ventricular failure 231.61 26.67 108 21658 9447 42590122
Oedema 209.08 26.67 189 21577 51812 42547757
Dizziness 203.47 26.67 414 21352 248840 42350729
Peripheral swelling 201.27 26.67 239 21527 90031 42509538
Pulmonary endarterectomy 187.80 26.67 34 21732 64 42599505
Hypervolaemia 186.78 26.67 127 21639 22998 42576571
Oedema peripheral 172.37 26.67 274 21492 135802 42463767
Oxygen saturation decreased 153.62 26.67 177 21589 64510 42535059
Dyspepsia 150.07 26.67 142 21624 41210 42558359
Drug ineffective 137.54 26.67 76 21690 630121 41969448
Off label use 135.01 26.67 80 21686 638255 41961314
Nasal congestion 98.86 26.67 97 21669 29404 42570165
Toxicity to various agents 90.58 26.67 7 21759 229129 42370440
Endarterectomy 83.70 26.67 19 21747 149 42599420
Haemoptysis 78.58 26.67 107 21659 46060 42553509
Syncope 77.03 26.67 162 21604 99244 42500325
Abdominal distension 76.63 26.67 134 21632 71601 42527968
Blood pressure decreased 74.40 26.67 118 21648 58214 42541355
Drug interaction 72.71 26.67 23 21743 266976 42332593
Lung transplant 70.57 26.67 31 21735 2355 42597214
Weight increased 70.16 26.67 164 21602 107819 42491750
Infusion site pain 67.14 26.67 39 21727 5356 42594213
Epistaxis 66.45 26.67 121 21645 66705 42532864
Catheterisation cardiac 65.88 26.67 31 21735 2763 42596806
Catheter management 64.39 26.67 23 21743 1009 42598560
Nausea 63.57 26.67 382 21384 396417 42203152
Transfusion 62.56 26.67 48 21718 10466 42589103
Oxygen consumption increased 60.48 26.67 25 21741 1634 42597935
Pain in extremity 58.13 26.67 189 21577 150415 42449154
Swelling 56.62 26.67 101 21665 54784 42544785
Product use in unapproved indication 55.61 26.67 13 21753 184443 42415126
Therapy change 54.69 26.67 31 21735 4064 42595505
Blood pressure systolic decreased 54.10 26.67 33 21733 4954 42594615
Thrombocytopenia 52.46 26.67 16 21750 190263 42409306
Pulmonary arterial pressure increased 52.11 26.67 22 21744 1516 42598053
Cough 48.82 26.67 200 21566 177903 42421666
Oxygen therapy 47.94 26.67 20 21746 1338 42598231
Diarrhoea 47.60 26.67 399 21367 460450 42139119
Gastrooesophageal reflux disease 46.62 26.67 83 21683 44940 42554629
Blood pressure abnormal 45.43 26.67 39 21727 9959 42589610
Chest pain 44.16 26.67 164 21602 139366 42460203
Abdominal discomfort 43.18 26.67 109 21657 75146 42524423
Angioplasty 42.40 26.67 17 21749 1027 42598542
Infusion site erythema 41.96 26.67 25 21741 3597 42595972
Transplant evaluation 41.70 26.67 14 21752 509 42599060
Pulmonary thrombosis 40.88 26.67 34 21732 8314 42591255
Dizziness postural 40.80 26.67 33 21733 7762 42591807
Blood pressure diastolic decreased 40.23 26.67 37 21729 10338 42589231
Gastrointestinal disorder 39.59 26.67 79 21687 46574 42552995
Flushing 39.28 26.67 69 21697 36959 42562610
Drug abuse 39.19 26.67 4 21762 104767 42494802
Unevaluable event 39.14 26.67 66 21700 34222 42565347
Feeling abnormal 38.91 26.67 100 21666 69686 42529883
Thrombectomy 37.08 26.67 9 21757 97 42599472
Lung operation 36.43 26.67 9 21757 105 42599464
Cardiac operation 36.41 26.67 23 21743 3672 42595897
Dyspnoea at rest 35.86 26.67 24 21742 4225 42595344
Dialysis 35.71 26.67 37 21729 11949 42587620
Malaise 35.58 26.67 207 21559 211949 42387620
Surgery 34.87 26.67 44 21722 17572 42581997
Loss of consciousness 34.77 26.67 115 21651 92239 42507330
Overdose 34.65 26.67 6 21760 105258 42494311
Catheter site pain 34.38 26.67 17 21749 1690 42597879
Pyrexia 33.70 26.67 97 21669 393945 42205624
Seizure 33.45 26.67 10 21756 120551 42479018
Terminal state 32.64 26.67 23 21743 4400 42595169
Rash 31.01 26.67 59 21707 276895 42322674
Acute kidney injury 30.26 26.67 92 21674 367245 42232324
Pulmonary artery therapeutic procedure 29.97 26.67 5 21761 4 42599565
Cardiac failure congestive 29.07 26.67 103 21663 85499 42514070
Device occlusion 28.69 26.67 28 21738 8422 42591147
Hypertension 27.38 26.67 27 21739 167177 42432392
Ascites 27.34 26.67 77 21689 56601 42542968
Paracentesis 27.25 26.67 10 21756 474 42599095
Lung disorder 27.04 26.67 69 21697 47854 42551715

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 2777.80 19.94 2958 78123 695911 109812307
Hospitalisation 2301.44 19.94 1382 79699 141111 110367107
Dyspnoea 1602.42 19.94 2877 78204 1103995 109404223
Fluid retention 1488.17 19.94 902 80179 93405 110414813
Dyspnoea exertional 1209.37 19.94 821 80260 103239 110404979
Hypotension 1171.43 19.94 1665 79416 522184 109986034
Pulmonary arterial hypertension 946.66 19.94 467 80614 32101 110476117
Pain in jaw 933.73 19.94 538 80543 50639 110457579
Headache 931.78 19.94 2014 79067 880363 109627855
Dizziness 760.07 19.94 1615 79466 696578 109811640
Right ventricular failure 645.49 19.94 335 80746 25619 110482599
Oedema peripheral 639.20 19.94 980 80101 327680 110180538
Pulmonary hypertension 632.18 19.94 432 80649 54788 110453430
Drug ineffective 567.82 19.94 205 80876 1520335 108987883
Oxygen saturation decreased 550.90 19.94 626 80455 156356 110351862
Hypervolaemia 547.41 19.94 379 80702 49081 110459137
Off label use 485.51 19.94 249 80832 1499936 109008282
Blood pressure decreased 398.57 19.94 456 80625 114635 110393583
Nausea 373.66 19.94 1838 79243 1233852 109274366
Dyspepsia 369.98 19.94 569 80512 190396 110317822
Diarrhoea 334.94 19.94 1682 79399 1137823 109370395
Pulmonary endarterectomy 331.59 19.94 68 81013 193 110508025
Oedema 327.23 19.94 567 80514 209409 110298809
Transfusion 319.51 19.94 211 80870 25261 110482957
Nasal congestion 319.48 19.94 377 80704 97905 110410313
Toxicity to various agents 300.49 19.94 12 81069 480543 110027675
Peripheral swelling 297.61 19.94 805 80276 403229 110104989
Syncope 292.46 19.94 529 80552 202007 110306211
Catheterisation cardiac 290.77 19.94 124 80957 6067 110502151
Epistaxis 283.21 19.94 410 80671 129962 110378256
Infusion related reaction 250.87 19.94 6 81075 381156 110127062
Cough 240.19 19.94 814 80267 460827 110047391
Chest pain 236.21 19.94 708 80373 375667 110132551
Neutropenia 231.96 19.94 10 81071 374610 110133608
Pulmonary arterial pressure increased 228.64 19.94 99 80982 5028 110503190
Abdominal distension 221.15 19.94 432 80649 174671 110333547
Drug interaction 211.81 19.94 53 81028 500130 110008088
Unevaluable event 205.47 19.94 235 80846 58992 110449226
Dizziness postural 205.31 19.94 130 80951 14479 110493739
Infusion site pain 203.32 19.94 138 80943 17281 110490937
Product use in unapproved indication 200.19 19.94 42 81039 447335 110060883
Palpitations 200.07 19.94 392 80689 158820 110349398
Lung transplant 196.98 19.94 90 80991 5196 110503022
Haemoptysis 196.74 19.94 252 80829 71102 110437116
Feeling abnormal 192.96 19.94 416 80665 180295 110327923
Catheter management 192.75 19.94 80 81001 3655 110504563
Drug hypersensitivity 192.47 19.94 48 81033 454042 110054176
Flushing 190.02 19.94 303 80778 104433 110403785
Treatment failure 183.79 19.94 4 81077 277230 110230988
Therapy change 179.25 19.94 104 80977 9893 110498325
Stomatitis 178.76 19.94 4 81077 270238 110237980
Oxygen consumption increased 178.52 19.94 86 80995 5599 110502619
Hepatic enzyme increased 173.90 19.94 17 81064 320875 110187343
Oxygen therapy 171.59 19.94 76 81005 4077 110504141
Product dose omission issue 169.43 19.94 570 80511 321212 110187006
Catheter site erythema 164.88 19.94 83 80998 5945 110502273
Catheter site pruritus 163.04 19.94 62 81019 2244 110505974
Blood pressure systolic decreased 162.89 19.94 109 80972 13332 110494886
Arthropathy 159.08 19.94 14 81067 287508 110220710
Endarterectomy 156.83 19.94 40 81041 361 110507857
Rash 153.44 19.94 228 80853 820736 109687482
Rheumatoid arthritis 151.99 19.94 20 81061 299593 110208625
Maternal exposure during pregnancy 150.77 19.94 9 81072 254874 110253344
Glossodynia 147.94 19.94 3 81078 222001 110286217
Hypoxia 144.96 19.94 304 80777 129211 110379007
Transplant evaluation 143.06 19.94 53 81028 1782 110506436
Blood pressure abnormal 139.03 19.94 122 80959 22302 110485916
Pericarditis 138.45 19.94 5 81076 219109 110289109
Catheter site pain 131.58 19.94 73 81008 6373 110501845
Blood pressure diastolic decreased 125.48 19.94 143 80938 35742 110472476
Thrombocytopenia 124.44 19.94 50 81031 348835 110159383
Cardiac failure congestive 124.31 19.94 314 80767 150686 110357532
Fatigue 121.78 19.94 1393 79688 1214565 109293653
Blood cholesterol increased 121.16 19.94 3 81078 184782 110323436
Emergency care 120.80 19.94 44 81037 1409 110506809
Contraindicated product administered 120.25 19.94 19 81062 248248 110259970
Vomiting 116.52 19.94 1097 79984 909578 109598640
Type 2 diabetes mellitus 115.74 19.94 3 81078 177229 110330989
Blood potassium decreased 115.69 19.94 169 80912 53945 110454273
Alopecia 115.06 19.94 62 81019 364691 110143527
Heart rate increased 114.14 19.94 295 80786 143539 110364679
C-reactive protein increased 111.82 19.94 14 81067 217905 110290313
Drug abuse 108.88 19.94 5 81076 177406 110330812
Overdose 108.59 19.94 20 81061 233774 110274444
Confusional state 107.53 19.94 111 80970 468569 110039649
Pericardial effusion 107.15 19.94 168 80913 57049 110451169
Hypertension 106.98 19.94 130 80951 509954 109998264
Urticaria 106.87 19.94 50 81031 318807 110189411
Dyspnoea at rest 106.74 19.94 70 81011 8276 110499942
Catheter site discharge 105.62 19.94 49 81032 2930 110505288
Impaired healing 105.03 19.94 11 81070 196706 110311512
Musculoskeletal stiffness 104.96 19.94 37 81044 279785 110228433
Malaise 104.40 19.94 845 80236 670974 109837244
Presyncope 103.53 19.94 152 80929 48735 110459483
Helicobacter infection 102.94 19.94 8 81073 181869 110326349
Lower respiratory tract infection 100.42 19.94 27 81054 243079 110265139
Central venous catheterisation 99.54 19.94 51 81030 3791 110504427
Acute kidney injury 98.05 19.94 199 80882 635231 109872987
Pain in extremity 96.32 19.94 649 80432 486469 110021749
Ascites 95.96 19.94 211 80870 92597 110415621
Exposure during pregnancy 95.78 19.94 7 81074 167417 110340801
Gastrooesophageal reflux disease 95.65 19.94 320 80761 179656 110328562
Pulmonary thrombosis 95.25 19.94 80 81001 13783 110494435
Hypersensitivity 94.57 19.94 94 80987 403904 110104314
Angioplasty 94.28 19.94 40 81041 1931 110506287
Cardiac failure 93.93 19.94 327 80754 187299 110320919
Device occlusion 92.90 19.94 82 80999 15103 110493115
Vascular device infection 92.80 19.94 85 80996 16427 110491791
Therapeutic product effect incomplete 92.17 19.94 25 81056 223780 110284438
Device related infection 91.20 19.94 128 80953 39391 110468827
Infusion site erythema 90.51 19.94 73 81008 11886 110496332
Muscle injury 89.68 19.94 3 81078 140804 110367414
Wound 89.64 19.94 30 81051 234407 110273811
Catheter site haemorrhage 89.37 19.94 55 81026 5825 110502393
Productive cough 89.20 19.94 233 80848 114072 110394146
Rehabilitation therapy 87.52 19.94 39 81042 2122 110506096
Walking distance test abnormal 86.70 19.94 29 81052 717 110507501
Device alarm issue 85.99 19.94 40 81041 2406 110505812
Constipation 85.19 19.94 500 80581 357286 110150932
Liver injury 84.05 19.94 7 81074 150406 110357812
Medical procedure 83.78 19.94 26 81055 502 110507716
Intentional overdose 83.77 19.94 3 81078 132498 110375720
Mobility decreased 83.05 19.94 35 81046 237387 110270831
Fibromyalgia 82.93 19.94 13 81068 170896 110337322
Chest discomfort 82.73 19.94 298 80783 173550 110334668
Dialysis 80.42 19.94 85 80996 19534 110488684
Pneumonia 79.38 19.94 986 80095 875728 109632490
Blister 78.76 19.94 34 81047 227342 110280876
Brain natriuretic peptide increased 77.66 19.94 65 81016 11144 110497074
General physical health deterioration 77.45 19.94 120 80961 425175 110083043
Irritable bowel syndrome 76.34 19.94 14 81067 164201 110344017
Pulmonary oedema 76.31 19.94 203 80878 100456 110407762
Systemic lupus erythematosus 76.21 19.94 46 81035 254292 110253926
Osteoarthritis 75.95 19.94 20 81061 182603 110325615
Localised oedema 75.59 19.94 59 81022 9164 110499054
Acute respiratory failure 74.31 19.94 168 80913 75092 110433126
Bursitis 72.71 19.94 6 81075 129912 110378306
Injury 72.61 19.94 20 81061 177245 110330973
Catheter site swelling 72.50 19.94 35 81046 2289 110505929
Psoriasis 71.79 19.94 9 81072 139984 110368234
Pruritus 71.56 19.94 205 80876 581355 109926863
Loss of consciousness 71.18 19.94 309 80772 195997 110312221
Anaphylactic reaction 70.85 19.94 3 81078 114297 110393921
Infusion site infection 70.22 19.94 34 81047 2238 110505980
Hyponatraemia 70.07 19.94 36 81045 217617 110290601
Electrocardiogram QT prolonged 67.08 19.94 3 81078 108957 110399261
Myalgia 66.60 19.94 331 80750 222050 110286168
Catheter site rash 66.53 19.94 26 81055 1014 110507204
Pyrexia 65.75 19.94 388 80693 897877 109610341
Paracentesis 65.60 19.94 28 81053 1372 110506846
Pancytopenia 65.52 19.94 36 81045 209577 110298641
Asthma 64.79 19.94 53 81028 250238 110257980
Intentional product use issue 63.54 19.94 53 81028 247853 110260365
White blood cell count decreased 62.64 19.94 46 81035 229344 110278874
Flatulence 62.54 19.94 126 80955 52023 110456195
Gastric disorder 62.52 19.94 98 80983 33259 110474959
Drug-induced liver injury 60.88 19.94 8 81073 120059 110388159
Internal haemorrhage 60.84 19.94 54 81027 10017 110498201
Pulmonary artery therapeutic procedure 60.81 19.94 12 81069 26 110508192
Mineral supplementation 60.23 19.94 23 81058 842 110507376
Scleroderma 59.55 19.94 44 81037 6297 110501921
Night sweats 58.99 19.94 13 81068 133970 110374248
Obesity 58.82 19.94 7 81074 113344 110394874
Catheter placement 58.09 19.94 34 81047 3286 110504932
Drug intolerance 57.90 19.94 133 80948 406379 110101839
Weight increased 57.72 19.94 514 80567 419130 110089088
Delirium 57.66 19.94 14 81067 135011 110373207
Lung operation 57.64 19.94 18 81063 355 110507863
Suicide attempt 57.24 19.94 5 81076 103389 110404829
Catheter site infection 56.69 19.94 47 81034 7953 110500265
Renal disorder 56.32 19.94 117 80964 49362 110458856
Discomfort 56.15 19.94 45 81036 214662 110293556
Ill-defined disorder 55.04 19.94 23 81058 156830 110351388
Lip dry 54.98 19.94 5 81076 100078 110408140
Abdominal pain upper 54.54 19.94 440 80641 348671 110159547
Myelosuppression 53.79 19.94 4 81077 94336 110413882
Injection site reaction 53.09 19.94 3 81078 89067 110419151
Decreased appetite 52.74 19.94 557 80524 475289 110032929
Lactic acidosis 52.74 19.94 4 81077 92807 110415411
Epilepsy 52.47 19.94 6 81075 100203 110408015
Inflammation 52.43 19.94 39 81042 193199 110315019
Concomitant disease aggravated 51.84 19.94 62 81019 16302 110491916
Retching 51.64 19.94 73 81008 22609 110485609
Disease complication 51.53 19.94 39 81042 5788 110502430
Pulmonary veno-occlusive disease 51.30 19.94 27 81054 2121 110506097
Hepatitis 50.83 19.94 4 81077 90050 110418168
Complication associated with device 50.81 19.94 68 81013 20005 110488213
Cardiac operation 50.54 19.94 39 81042 5956 110502262
Diastolic hypotension 50.47 19.94 16 81065 332 110507886
Drug ineffective for unapproved indication 49.48 19.94 8 81073 102830 110405388
Head injury 49.29 19.94 102 80979 42915 110465303
Depressed level of consciousness 49.21 19.94 11 81070 112267 110395951
Catheter site related reaction 48.72 19.94 23 81058 1431 110506787
Dizziness exertional 48.26 19.94 19 81062 756 110507462
Suicidal ideation 48.25 19.94 6 81075 93931 110414287
Cardiac disorder 48.17 19.94 144 80937 76136 110432082
Terminal state 48.07 19.94 37 81044 5630 110502588
Hypoaesthesia 47.87 19.94 99 80982 314124 110194094
Catheter site irritation 47.85 19.94 18 81063 632 110507586
Seizure 47.77 19.94 55 81026 221130 110287088
Hyperkalaemia 47.50 19.94 20 81061 135776 110372442
Infection 47.25 19.94 124 80957 362076 110146142
Seasonal allergy 47.17 19.94 65 81016 19657 110488561
Gout 47.05 19.94 91 80990 36475 110471743
Prescribed overdose 46.47 19.94 5 81076 87576 110420642
Metabolic acidosis 45.30 19.94 9 81072 99735 110408483
Haemoglobin decreased 45.29 19.94 325 80756 248402 110259816
Medication error 44.84 19.94 11 81070 105355 110402863
Device dislocation 44.64 19.94 82 80999 31622 110476596
Hospice care 44.10 19.94 50 81031 12423 110495795
Grip strength decreased 44.05 19.94 4 81077 80170 110428048
Exercise tolerance decreased 43.73 19.94 49 81032 12018 110496200
Catheter site vesicles 43.56 19.94 15 81066 406 110507812
Blood pressure increased 43.19 19.94 77 81004 258296 110249922
Paraesthesia 42.22 19.94 87 80994 276434 110231784
Coma 41.81 19.94 17 81064 117852 110390366
Cognitive disorder 41.67 19.94 7 81074 87504 110420714
Nasal dryness 41.43 19.94 34 81047 5672 110502546
Thrombectomy 41.19 19.94 14 81067 364 110507854
Product use issue 41.19 19.94 106 80975 311589 110196629
Bradycardia 40.15 19.94 33 81048 155484 110352734
Sleep disorder 40.14 19.94 52 81029 198592 110309626
No adverse event 39.73 19.94 4 81077 73835 110434383
Sedation 39.60 19.94 3 81078 69680 110438538
Surgery 39.46 19.94 91 80990 41192 110467026
Peripheral venous disease 39.46 19.94 7 81074 84110 110424108
Alanine aminotransferase increased 39.35 19.94 46 81035 183727 110324491
Wound infection 39.28 19.94 11 81070 96454 110411764
Angioedema 38.70 19.94 12 81069 98488 110409730
Rales 38.70 19.94 67 81014 24672 110483546
Weight decreased 38.23 19.94 517 80564 467540 110040678
Device infusion issue 37.63 19.94 25 81056 3020 110505198
Drug titration error 37.35 19.94 20 81061 1627 110506591
Infusion site swelling 37.33 19.94 41 81040 9836 110498382
Pulmonary arterial wedge pressure increased 37.31 19.94 15 81066 631 110507587
Cardiac failure high output 37.09 19.94 14 81067 496 110507722
Incorrect product administration duration 36.73 19.94 59 81022 20439 110487779
Vascular device occlusion 36.69 19.94 15 81066 659 110507559
Multiple allergies 36.47 19.94 45 81036 12218 110496000
Fall 36.38 19.94 633 80448 602849 109905369
Diuretic therapy 36.17 19.94 11 81070 198 110508020
Depression 36.01 19.94 116 80965 317219 110190999
Hyperglycaemia 35.98 19.94 9 81072 85081 110423137
Dry mouth 35.80 19.94 57 81024 199891 110308327
Blood iron decreased 35.38 19.94 56 81025 19158 110489060
Osteoporosis 35.37 19.94 10 81071 87142 110421076
Influenza 34.34 19.94 227 80854 168874 110339344
Agranulocytosis 34.15 19.94 3 81078 61757 110446461
Hypocalcaemia 34.00 19.94 4 81077 65362 110442856
Infusion site discharge 33.98 19.94 20 81061 1953 110506265
Pulmonary congestion 33.82 19.94 72 81009 30894 110477324
Disease recurrence 33.48 19.94 3 81078 60781 110447437
Deep vein thrombosis 33.32 19.94 32 81049 139855 110368363
Generalised oedema 33.08 19.94 71 81010 30633 110477585
Infusion site abscess 33.04 19.94 12 81069 381 110507837
Right ventricular dilatation 32.93 19.94 21 81060 2366 110505852
Device leakage 32.68 19.94 49 81032 15999 110492219
Infusion site haemorrhage 32.55 19.94 27 81054 4571 110503647
Myocardial infarction 32.32 19.94 57 81024 192026 110316192
Intestinal obstruction 32.21 19.94 99 80982 53128 110455090
Decreased activity 32.20 19.94 40 81041 10934 110497284
Skin exfoliation 32.14 19.94 12 81069 87639 110420579
Choking 32.01 19.94 47 81034 15063 110493155
Agitation 31.73 19.94 22 81059 113029 110395189
Abnormal weight gain 31.68 19.94 24 81057 3567 110504651
Sickle cell anaemia with crisis 31.62 19.94 37 81044 9508 110498710
Eosinophilia 31.54 19.94 3 81078 57933 110450285
Bone marrow failure 31.48 19.94 3 81078 57845 110450373
Abdominal discomfort 31.31 19.94 433 80648 393425 110114793
Cor pulmonale 31.20 19.94 20 81061 2274 110505944
Right ventricular dysfunction 31.07 19.94 23 81058 3300 110504918
Cardiac failure acute 31.07 19.94 60 81021 24018 110484200
Lymphocyte count decreased 31.06 19.94 3 81078 57240 110450978
Therapeutic response decreased 30.98 19.94 16 81065 96483 110411735
Product supply issue 30.55 19.94 24 81057 3762 110504456
Intra-abdominal fluid collection 30.39 19.94 24 81057 3790 110504428
Eczema 29.89 19.94 8 81073 72285 110435933
Hallucination 29.46 19.94 19 81062 101413 110406805
Multiple organ dysfunction syndrome 29.34 19.94 41 81040 151669 110356549
Asthenia 29.28 19.94 686 80395 688313 109819905
Injection site infection 28.97 19.94 20 81061 2573 110505645
Cholestasis 28.92 19.94 6 81075 64512 110443706
Cardiac pacemaker insertion 28.90 19.94 29 81052 6272 110501946
Diabetes mellitus 28.34 19.94 19 81062 99362 110408856
Acute myocardial infarction 28.25 19.94 13 81068 83764 110424454
Aspartate aminotransferase increased 28.25 19.94 46 81035 159890 110348328
Sickle cell disease 28.20 19.94 9 81072 191 110508027
Oxygen saturation abnormal 27.92 19.94 27 81054 5584 110502634
Liver function test abnormal 27.82 19.94 8 81073 68942 110439276
Sickle cell anaemia 27.76 19.94 13 81068 794 110507424
Cerebrovascular accident 27.69 19.94 57 81024 181227 110326991
Device connection issue 27.58 19.94 15 81066 1259 110506959
Autoimmune disorder 27.54 19.94 7 81074 65476 110442742
Haemorrhage 27.23 19.94 152 80929 106540 110401678
Atrial septal defect 27.00 19.94 18 81063 2187 110506031
Bendopnoea 26.62 19.94 7 81074 72 110508146
Head discomfort 26.57 19.94 49 81032 18951 110489267
Vascular resistance pulmonary decreased 26.36 19.94 7 81074 75 110508143
Abdominal cavity drainage 26.26 19.94 13 81068 898 110507320
Drug dependence 26.17 19.94 3 81078 50017 110458201
Coronary artery disease 25.98 19.94 10 81071 71680 110436538
Pulmonary fibrosis 25.90 19.94 22 81059 102020 110406198
Infusion site irritation 25.90 19.94 14 81067 1161 110507057
Sinus disorder 25.81 19.94 67 81014 32661 110475557
Wheezing 25.79 19.94 98 80983 255132 110253086
Jaundice 25.56 19.94 6 81075 59230 110448988
Choking sensation 25.25 19.94 23 81058 4413 110503805
Product availability issue 25.17 19.94 30 81051 7860 110500358
Mouth ulceration 24.91 19.94 3 81078 48135 110460083
Nocturnal dyspnoea 24.65 19.94 16 81065 1859 110506359
Transaminases increased 24.41 19.94 8 81073 63382 110444836
Gastrointestinal haemorrhage 24.41 19.94 206 80875 165312 110342906
Drug dose titration not performed 24.34 19.94 13 81068 1052 110507166
N-terminal prohormone brain natriuretic peptide increased 24.17 19.94 26 81055 6095 110502123
Ear discomfort 23.84 19.94 35 81046 11214 110497004
Cardioversion 23.82 19.94 17 81064 2306 110505912
Accidental exposure to product 23.81 19.94 4 81077 50004 110458214
Dehydration 23.73 19.94 311 80770 279200 110229018
COVID-19 23.54 19.94 96 80985 244964 110263254
Dermatitis contact 23.43 19.94 39 81042 13914 110494304
Cardiac discomfort 23.35 19.94 14 81067 1414 110506804
Onychomadesis 23.25 19.94 3 81078 45660 110462558
Colitis ulcerative 23.15 19.94 14 81067 77349 110430869
Traumatic fracture 23.11 19.94 13 81068 1165 110507053
Hepatic steatosis 23.04 19.94 4 81077 48827 110459391
Infusion site warmth 22.99 19.94 15 81066 1758 110506460
Amnesia 22.98 19.94 26 81055 105382 110402836
Pulmonary artery occlusion 22.97 19.94 6 81075 60 110508158
Emotional distress 22.70 19.94 3 81078 44844 110463374
Hypomagnesaemia 22.58 19.94 8 81073 60362 110447856
Product prescribing error 22.55 19.94 5 81076 51326 110456892
Hernia repair 22.48 19.94 17 81064 2519 110505699
Psychotic disorder 22.30 19.94 5 81076 50932 110457286
Colonoscopy 22.20 19.94 16 81065 2204 110506014
Arthritis 22.12 19.94 57 81024 167529 110340689
Drug eruption 22.07 19.94 6 81075 53653 110454565
Pulmonary pain 21.86 19.94 25 81056 6268 110501950
Jugular vein distension 21.76 19.94 14 81067 1602 110506616
Dry eye 21.56 19.94 7 81074 55786 110452432
Chronic right ventricular failure 21.47 19.94 6 81075 79 110508139
Liver function test increased 21.39 19.94 20 81061 88528 110419690
Sluggishness 21.28 19.94 27 81054 7540 110500678
Infusion site induration 21.24 19.94 13 81068 1363 110506855
Sinusitis 21.17 19.94 129 80952 296559 110211659
Faeces soft 21.10 19.94 33 81048 11177 110497041
Sciatica 21.01 19.94 22 81059 92377 110415841
Cardiac arrest 20.89 19.94 74 81007 196679 110311539
Biopsy liver 20.87 19.94 10 81071 643 110507575
Aspiration pleural cavity 20.84 19.94 14 81067 1723 110506495
Road traffic accident 20.79 19.94 29 81052 107369 110400849
Sinus congestion 20.66 19.94 59 81022 30400 110477818
Eructation 20.60 19.94 37 81044 14020 110494198
Loss of personal independence in daily activities 20.59 19.94 50 81031 149970 110358248
Hypokalaemia 20.47 19.94 67 81014 182381 110325837
Oral candidiasis 20.40 19.94 4 81077 44756 110463462
Disseminated intravascular coagulation 20.34 19.94 3 81078 41283 110466935
Hepatocellular injury 20.20 19.94 6 81075 50636 110457582
Catheter site warmth 20.16 19.94 8 81073 325 110507893
Blood lactate dehydrogenase increased 20.13 19.94 4 81077 44330 110463888

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02KX05 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
OTHER ANTIHYPERTENSIVES
Antihypertensives for pulmonary arterial hypertension
MeSH PA D020536 Enzyme Activators
FDA MoA N0000190484 Guanylate Cyclase Stimulators
FDA EPC N0000190485 Soluble Guanylate Cyclase Stimulator
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:76022 soluble guanylate cyclase activator

Related Drugs by ATC class:

C02KX Antihypertensives for pulmonary arterial hypertension 6 drugs
ambrisentanbosentanmacitentansitaxentansotatercept-csrktadalafil

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

DiseaseRelationSNOMED_IDDOID
Pulmonary arterial hypertension indication 11399002
Chronic thromboembolic pulmonary hypertension indication 233947005
Pregnancy, function contraindication 289908002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.68 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 12503469 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Guanylate cyclase soluble subunit beta-1 Enzyme POSITIVE ALLOSTERIC MODULATOR MEC 7.52 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
cAMP-specific 3',5'-cyclic phosphodiesterase 7B Enzyme IC50 5.54 SCIENTIFIC LITERATURE

External reference:

IDSource
D09572 KEGG_DRUG
4032785 VANDF
CHEBI:76018 CHEBI
CHEMBL2107834 ChEMBL_ID
C542595 MESH_SUPPLEMENTAL_RECORD_UI
5257 IUPHAR_LIGAND_ID
DB08931 DRUGBANK_ID
RU3FE2Y4XI UNII
1439816 RXNORM
207043 MMSL
29792 MMSL
d08140 MMSL
015236 NDDF
713333001 SNOMEDCT_US
715490004 SNOMEDCT_US
C2717561 UMLSCUI
GZO PDB_CHEM_ID
8857 INN_ID
11304743 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-250 TABLET, FILM COATED 0.50 mg ORAL NDA 28 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-251 TABLET, FILM COATED 1 mg ORAL NDA 28 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-252 TABLET, FILM COATED 1.50 mg ORAL NDA 28 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-253 TABLET, FILM COATED 2 mg ORAL NDA 28 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-254 TABLET, FILM COATED 2.50 mg ORAL NDA 28 sections