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

Stem definitionDrug idCAS RN
platelet aggregation inhibitors 4184 274693-27-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ticagrelor
  • brilinta
  • AZD 6140
  • possia
  • brilique
a cyclopentyltriazolopyrimidine, inhibitor of platelet activation and aggregation mediated by the P2Y12 ADP-receptor indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction
  • Molecular weight: 522.57
  • Formula: C23H28F2N6O4S
  • CLOGP: 3.35
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 4
  • TPSA: 138.44
  • ALOGS: -3.92
  • ROTB: 10

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.18 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.25 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.38 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.80 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.01 mg/mL Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 0 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.324 High 0.88
caco2-efflux Caco-2 efflux ratio (BA/AB) 7.482 High 0.88
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 29.580 10^-6 cm/s High 0.88
dh-clint Dog hepatocyte intrinsic clearance 2.612 uL/min/10^6 cells High 0.88
dppb Dog plasma protein binding (% unbound) 0.400 % High 0.88
fcs-ppb Fetal calf serum protein binding (% unbound) 0.920 % High 0.88
herg hERG pIC50 4.937 pIC50 High 0.88
hh-clint Human hepatocyte intrinsic clearance 7.603 uL/min/10^6 cells High 0.88
hlm-clint Human liver microsomal intrinsic clearance 17.258 uL/min/mg protein High 0.88
hppb Human plasma protein binding (% unbound) 0.300 % High 0.88
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK14,CDK16,CDK2,CDK3,CDK5,CDK7,CDK9,CLK4,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,IRAK4,ITK,MAP2K6,MAP3K21,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PDPK1,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ZAP70 40
kinase-selectivity-class AXL,CDK1,CDK16,CDK2,CDK7,CDK9,GRK2,MAP2K6,PDK1,TEK 10
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 20.941 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 24.547 High 0.88
mh-clint Mouse hepatocyte intrinsic clearance 17.298 High 0.88
mppb Mouse plasma protein binding (% unbound) 0.400 High 0.88
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 86.298 High 0.88
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 0.750 % High 0.88
rat-kpuu-brain Rat brain Kpuu 0.007 % High 1
rh-clint Rat hepatocyte intrinsic clearance 16.406 uL/min/10^6 cells High 0.88
rh-fuinc Rat hepatocyte fraction unbound in incubation 2.240 % High 0.88
rppb Rat plasma protein binding (% unbound) 0.280 % High 0.88
solubility-dd Solubility at pH 7.4 in DMSO 10.864 uM High 0.88

Approvals:

DateAgencyCompanyOrphan
July 20, 2011 FDA ASTRAZENECA LP

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
Rhabdomyolysis 928.01 18.69 345 15454 50911 90561737
Vascular stent thrombosis 834.76 18.69 148 15651 968 90611680
Myocardial infarction 437.25 18.69 256 15543 105716 90506932
Drug interaction 409.14 18.69 357 15442 276096 90336552
Acute myocardial infarction 318.37 18.69 144 15655 34746 90577902
Dyspnoea 316.82 18.69 555 15244 880400 89732248
Acute kidney injury 314.46 18.69 330 15469 320057 90292591
Thrombosis in device 296.29 18.69 75 15724 3000 90609648
Gastrointestinal haemorrhage 292.56 18.69 187 15612 90061 90522587
Chest discomfort 159.89 18.69 156 15643 138209 90474439
Haemorrhage 143.05 18.69 109 15690 69260 90543388
Asphyxia 139.94 18.69 51 15748 7052 90605596
Haemorrhage intracranial 133.22 18.69 61 15738 15101 90597547
Cerebral haemorrhage 117.85 18.69 74 15725 34448 90578200
Myopathy 114.43 18.69 53 15746 13465 90599183
Acute coronary syndrome 112.59 18.69 49 15750 10764 90601884
Melaena 112.33 18.69 72 15727 34725 90577923
Hypersensitivity myocarditis 112.04 18.69 22 15777 264 90612384
Angina pectoris 111.72 18.69 75 15724 39085 90573563
Coronary artery stenosis 108.18 18.69 39 15760 5227 90607421
Vascular stent stenosis 103.73 18.69 24 15775 652 90611996
Angina unstable 103.56 18.69 41 15758 7102 90605546
Atrioventricular block complete 100.66 18.69 44 15755 9767 90602881
Coronary artery disease 94.96 18.69 64 15735 33559 90579089
Anaemia 94.42 18.69 197 15602 352605 90260043
Bradycardia 86.57 18.69 89 15710 83758 90528890
Chest pain 84.93 18.69 178 15621 319467 90293181
Sinus arrest 80.45 18.69 25 15774 2121 90610527
Coronary artery occlusion 80.15 18.69 36 15763 8518 90604130
Epistaxis 80.11 18.69 86 15713 85039 90527609
Cardiogenic shock 79.88 18.69 51 15748 24417 90588231
Cholestatic liver injury 73.81 18.69 27 15772 3770 90608878
Labelled drug-drug interaction medication error 70.08 18.69 39 15760 14543 90598105
Cardiac arrest 68.68 18.69 88 15711 104847 90507801
Eosinophilia 63.59 18.69 47 15752 28486 90584162
Haematoma 60.60 18.69 52 15747 38996 90573652
Haemoglobin decreased 57.42 18.69 102 15697 161854 90450794
Infusion related reaction 54.42 18.69 5 15794 416775 90195873
Coronary artery thrombosis 54.39 18.69 16 15783 1126 90611522
Cardiac failure 52.41 18.69 79 15720 109417 90503231
Electrocardiogram ST segment elevation 51.14 18.69 21 15778 3995 90608653
Maternal exposure during pregnancy 50.76 18.69 3 15796 360060 90252588
Mixed liver injury 49.71 18.69 25 15774 7598 90605050
Upper gastrointestinal haemorrhage 49.30 18.69 37 15762 22939 90589709
Arthropathy 48.88 18.69 4 15795 366238 90246410
Breath holding 47.73 18.69 10 15789 169 90612479
Coronary artery restenosis 46.68 18.69 11 15788 324 90612324
Atrioventricular block 46.29 18.69 25 15774 8790 90603858
Arthralgia 43.57 18.69 43 15756 778479 89834169
Metabolic acidosis 43.37 18.69 51 15748 55625 90557023
Subarachnoid haemorrhage 43.32 18.69 31 15768 17873 90594775
Faeces discoloured 42.81 18.69 33 15766 21287 90591361
Death 42.76 18.69 175 15624 456376 90156272
Platelet function test abnormal 42.25 18.69 8 15791 78 90612570
Retroperitoneal haematoma 40.81 18.69 17 15782 3351 90609297
Systemic lupus erythematosus 40.80 18.69 7 15792 361889 90250759
Ventricular asystole 40.22 18.69 8 15791 103 90612545
Cerebral haematoma 40.02 18.69 18 15781 4271 90608377
Coronary artery dissection 39.52 18.69 12 15787 942 90611706
Diabetic macroangiopathy 38.78 18.69 8 15791 125 90612523
Treatment failure 38.72 18.69 4 15795 303924 90308724
Pyrexia 38.67 18.69 35 15764 660450 89952198
Joint swelling 38.31 18.69 20 15779 503280 90109368
Alopecia 37.20 18.69 20 15779 495051 90117597
Blood creatine phosphokinase increased 36.70 18.69 37 15762 33986 90578662
Capillary fragility test 35.18 18.69 6 15793 30 90612618
Subcutaneous haematoma 35.16 18.69 13 15786 1870 90610778
Intentional product misuse 35.09 18.69 59 15740 89545 90523103
Brain natriuretic peptide increased 34.26 18.69 18 15781 5987 90606661
Stent placement 34.08 18.69 16 15783 4187 90608461
Myocardial ischaemia 33.60 18.69 24 15775 13790 90598858
Renal failure 33.59 18.69 72 15727 130935 90481713
Pain 33.54 18.69 78 15721 996263 89616385
Syncope 32.97 18.69 72 15727 132591 90480057
Haemorrhagic stroke 32.93 18.69 18 15781 6478 90606170
Arterial restenosis 32.78 18.69 5 15794 10 90612638
Sinusitis 32.00 18.69 10 15789 343078 90269570
Stomatitis 31.65 18.69 5 15794 274693 90337955
Cholestasis 31.22 18.69 35 15764 36264 90576384
Myositis 31.22 18.69 29 15770 24099 90588549
Eosinophil cationic protein increased 31.12 18.69 6 15793 65 90612583
Drug intolerance 30.91 18.69 20 15779 447571 90165077
Acid base balance abnormal 30.85 18.69 8 15791 352 90612296
Restenosis 30.62 18.69 4 15795 0 90612648
Therapeutic product effect decreased 29.92 18.69 6 15793 277565 90335083
Troponin increased 29.86 18.69 22 15777 13259 90599389
Drug reaction with eosinophilia and systemic symptoms 29.76 18.69 37 15762 42721 90569927
Subdural haematoma 29.62 18.69 24 15775 16621 90596027
Abdominal discomfort 29.48 18.69 24 15775 477304 90135344
Forced vital capacity decreased 29.06 18.69 10 15789 1168 90611480
Hepatitis acute 29.01 18.69 20 15779 10867 90601781
Helicobacter infection 28.85 18.69 3 15796 226847 90385801
Musculoskeletal stiffness 28.83 18.69 8 15791 296524 90316124
Tachypnoea 28.32 18.69 26 15773 21283 90591365
Rheumatoid arthritis 28.19 18.69 14 15785 362600 90250048
Muscle necrosis 28.17 18.69 9 15790 835 90611813
Drug ineffective 27.68 18.69 136 15663 1384162 89228486
Coma acidotic 27.50 18.69 6 15793 124 90612524
Product name confusion 27.45 18.69 6 15793 125 90612523
Swelling 27.23 18.69 20 15779 419038 90193610
Ventricular fibrillation 26.59 18.69 21 15778 14023 90598625
Labelled drug-drug interaction issue 26.03 18.69 11 15788 2247 90610401
Pulmonary alveolar haemorrhage 26.00 18.69 15 15784 5983 90606665
Hepatitis cholestatic 25.86 18.69 17 15782 8544 90604104
Mobility decreased 25.84 18.69 6 15793 250728 90361920
Retroperitoneal haemorrhage 25.82 18.69 12 15787 3068 90609580
Irritable bowel syndrome 25.73 18.69 3 15796 207445 90405203
Blood loss anaemia 25.55 18.69 18 15781 10122 90602526
Impaired healing 25.37 18.69 5 15794 234194 90378454
Vascular stent occlusion 25.31 18.69 5 15794 62 90612586
Electrocardiogram Q wave abnormal 25.26 18.69 6 15793 183 90612465
Capillary fragility increased 25.08 18.69 4 15795 12 90612636
Aortic valve stenosis 25.02 18.69 13 15786 4227 90608421
Shock haemorrhagic 24.68 18.69 19 15780 12226 90600422
Progressive multiple sclerosis 24.41 18.69 9 15790 1285 90611363
Catheter site thrombosis 24.34 18.69 7 15792 455 90612193
Potentiating drug interaction 24.12 18.69 14 15785 5648 90607000
Contraindicated product administered 23.93 18.69 13 15786 320126 90292522
Myalgia 23.91 18.69 76 15723 175049 90437599
Alveolar proteinosis 23.82 18.69 8 15791 868 90611780
Hypovolaemic shock 23.68 18.69 15 15784 7079 90605569
Stent malfunction 23.67 18.69 5 15794 88 90612560
Drug-induced liver injury 23.56 18.69 50 15749 90268 90522380
Nasopharyngitis 23.28 18.69 22 15777 407082 90205566
Spinal cord haemorrhage 22.98 18.69 6 15793 271 90612377
Fibroma 22.98 18.69 8 15791 968 90611680
Myoglobin blood increased 22.81 18.69 9 15790 1543 90611105
Sinoatrial block 22.75 18.69 8 15791 997 90611651
Agranulocytosis 22.32 18.69 29 15770 34973 90577675
Device occlusion 22.29 18.69 16 15783 9266 90603382
Intraventricular haemorrhage 21.89 18.69 10 15789 2459 90610189
Haemoptysis 21.86 18.69 28 15771 33292 90579356
Rectal haemorrhage 21.80 18.69 46 15753 82698 90529950
Intermittent claudication 21.41 18.69 9 15790 1814 90610834
Haemoperitoneum 21.34 18.69 11 15788 3517 90609131
Pericardial haemorrhage 21.16 18.69 9 15790 1867 90610781
Toxicity to various agents 21.06 18.69 12 15787 287834 90324814
Hypotension 21.01 18.69 112 15687 325285 90287363
Muscle injury 20.83 18.69 3 15796 176651 90435997
Type 2 diabetes mellitus 20.67 18.69 5 15794 203239 90409409
Iron deficiency anaemia 20.66 18.69 23 15776 23639 90589009
Lower gastrointestinal haemorrhage 20.60 18.69 15 15784 8877 90603771
Petechiae 20.52 18.69 19 15780 15722 90596926
Stenosis 20.25 18.69 9 15790 2075 90610573
Delayed graft function 20.03 18.69 8 15791 1417 90611231
Hypochromic anaemia 19.90 18.69 9 15790 2162 90610486
Cell death 19.86 18.69 10 15789 3045 90609603
Osteoarthritis 19.55 18.69 5 15794 195725 90416923
Catheter site haematoma 19.46 18.69 5 15794 212 90612436
Hepatitis 19.42 18.69 40 15759 70699 90541949
Bundle branch block right 19.38 18.69 12 15787 5441 90607207
Drug-disease interaction 19.38 18.69 7 15792 943 90611705
Hyperkalaemia 19.35 18.69 38 15761 64926 90547722
Haematuria 19.31 18.69 27 15772 34910 90577738
Electrocardiogram ST segment depression 19.12 18.69 10 15789 3293 90609355
Infection 19.07 18.69 21 15778 362073 90250575
Suffocation feeling 19.00 18.69 8 15791 1620 90611028
Atrioventricular block second degree 18.94 18.69 11 15788 4441 90608207
Exposure during pregnancy 18.83 18.69 9 15790 238401 90374247
Migraine 18.75 18.69 5 15794 190387 90422261

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
Vascular stent thrombosis 1706.28 15.22 406 29326 2836 42588767
Thrombosis in device 737.07 15.22 207 29525 2939 42588664
Dyspnoea 548.35 15.22 1046 28686 441575 42150028
Acute myocardial infarction 519.35 15.22 383 29349 57782 42533821
Myocardial infarction 438.57 15.22 484 29248 123525 42468078
Rhabdomyolysis 366.68 15.22 355 29377 77664 42513939
Chest discomfort 353.89 15.22 318 29414 63298 42528305
Drug interaction 287.51 15.22 597 29135 266402 42325201
Chest pain 271.36 15.22 405 29327 139125 42452478
Angina pectoris 260.85 15.22 202 29530 32694 42558909
Gastrointestinal haemorrhage 251.87 15.22 325 29407 97401 42494202
Sinus arrest 243.50 15.22 81 29651 2075 42589528
Melaena 215.87 15.22 194 29538 38552 42553051
Vascular stent stenosis 195.34 15.22 59 29673 1093 42590510
Angina unstable 181.44 15.22 108 29624 11340 42580263
Asphyxia 168.09 15.22 92 29640 8234 42583369
Haemorrhage intracranial 163.97 15.22 118 29614 17074 42574529
Coronary artery occlusion 151.86 15.22 95 29637 10902 42580701
Cerebral haemorrhage 149.32 15.22 159 29573 38807 42552796
Sinoatrial block 134.16 15.22 37 29695 488 42591115
Coronary artery stenosis 131.70 15.22 85 29647 10294 42581309
Acute coronary syndrome 114.96 15.22 90 29642 14775 42576828
Haemorrhage 110.60 15.22 171 29561 60392 42531211
Bradycardia 105.66 15.22 203 29529 85281 42506322
Coronary artery thrombosis 100.29 15.22 43 29689 2243 42589360
Rectal haemorrhage 99.00 15.22 146 29586 49460 42542143
Labelled drug-drug interaction medication error 94.66 15.22 82 29650 15500 42576103
Shock haemorrhagic 93.70 15.22 83 29649 16159 42575444
Febrile neutropenia 91.65 15.22 11 29721 185692 42405911
Pulmonary haemorrhage 90.29 15.22 70 29662 11327 42580276
Cardiac arrest 88.63 15.22 219 29513 109101 42482502
Vascular stent occlusion 85.77 15.22 22 29710 215 42591388
Toxicity to various agents 85.12 15.22 27 29705 229109 42362494
Haematuria 82.38 15.22 146 29586 57653 42533950
Coronary artery restenosis 82.11 15.22 29 29703 893 42590710
Anaemia 79.68 15.22 396 29336 279882 42311721
Coronary artery disease 76.94 15.22 136 29596 53584 42538019
Epistaxis 76.84 15.22 154 29578 66672 42524931
Cardiac ventricular thrombosis 72.52 15.22 32 29700 1790 42589813
Pyrexia 72.27 15.22 102 29630 393940 42197663
Atrioventricular block complete 69.42 15.22 60 29672 11304 42580299
Blood loss anaemia 68.97 15.22 56 29676 9680 42581923
Upper gastrointestinal haemorrhage 67.50 15.22 94 29638 30205 42561398
Haemorrhagic stroke 66.46 15.22 49 29683 7353 42584250
Platelet aggregation inhibition 65.96 15.22 12 29720 14 42591589
Subarachnoid haemorrhage 64.34 15.22 64 29668 14408 42577195
Neutropenia 61.78 15.22 31 29701 199400 42392203
Atrioventricular block 57.18 15.22 50 29682 9565 42582038
Disease progression 54.98 15.22 16 29716 143640 42447963
Subdural haematoma 54.88 15.22 74 29658 23064 42568539
Malignant neoplasm progression 54.50 15.22 6 29726 108394 42483209
Gastric haemorrhage 53.33 15.22 50 29682 10465 42581138
Device dislocation 53.28 15.22 44 29688 7787 42583816
Coronary artery dissection 52.78 15.22 16 29716 300 42591303
Haematoma 52.34 15.22 80 29652 27943 42563660
Pneumonia 51.54 15.22 139 29593 422010 42169593
Muscle necrosis 50.31 15.22 21 29711 1024 42590579
Rash maculo-papular 49.92 15.22 92 29640 37411 42554192
Breath holding 48.71 15.22 12 29720 98 42591505
Electrocardiogram ST segment elevation 48.17 15.22 37 29695 5902 42585701
Loss of control of legs 47.50 15.22 19 29713 830 42590773
White blood cell count decreased 46.67 15.22 10 29722 110386 42481217
Brain herniation 45.73 15.22 33 29699 4790 42586813
Arterial restenosis 44.97 15.22 10 29722 49 42591554
Intentional product misuse 44.91 15.22 119 29613 61781 42529822
Cheyne-Stokes respiration 44.43 15.22 14 29718 300 42591303
Drug abuse 43.26 15.22 10 29722 104761 42486842
Heparin-induced thrombocytopenia 42.67 15.22 36 29696 6561 42585042
Arterial thrombosis 42.54 15.22 22 29710 1754 42589849
Mixed liver injury 41.03 15.22 30 29702 4444 42587159
Haemoglobin decreased 40.98 15.22 192 29540 132279 42459324
Ventricular asystole 40.89 15.22 13 29719 287 42591316
Suffocation feeling 40.55 15.22 16 29716 674 42590929
Gastritis erosive 39.04 15.22 34 29698 6469 42585134
Haematemesis 38.84 15.22 73 29659 30126 42561477
Device occlusion 38.73 15.22 38 29694 8412 42583191
Sepsis 38.05 15.22 50 29682 199284 42392319
Pancytopenia 36.88 15.22 18 29714 117725 42473878
Faeces discoloured 36.72 15.22 52 29680 16962 42574641
Gastric ulcer haemorrhage 36.71 15.22 32 29700 6095 42585508
Gastroduodenal ulcer 36.56 15.22 15 29717 700 42590903
Device malfunction 36.45 15.22 44 29688 12283 42579320
Retroperitoneal haematoma 36.28 15.22 24 29708 3027 42588576
Sinus bradycardia 34.45 15.22 47 29685 14806 42576797
Diarrhoea 34.02 15.22 186 29546 460663 42130940
Hepatitis cholestatic 33.96 15.22 38 29694 9786 42581817
Myocardial ischaemia 33.58 15.22 51 29681 17711 42573892
Electrocardiogram P wave abnormal 33.37 15.22 10 29722 180 42591423
Pericardial haemorrhage 32.88 15.22 24 29708 3545 42588058
Chronic coronary syndrome 32.76 15.22 11 29721 290 42591313
Lower gastrointestinal haemorrhage 32.65 15.22 39 29693 10769 42580834
Gastric ulcer 32.51 15.22 51 29681 18211 42573392
Base excess decreased 32.38 15.22 10 29722 200 42591403
Thrombosis 32.10 15.22 113 29619 68398 42523205
Constipation 31.69 15.22 40 29692 162251 42429352
Miller Fisher syndrome 31.62 15.22 9 29723 134 42591469
Cardiogenic shock 31.62 15.22 74 29658 35566 42556037
Iron deficiency anaemia 31.37 15.22 42 29690 12997 42578606
Completed suicide 31.36 15.22 14 29718 96451 42495152
Hepatic cytolysis 30.99 15.22 62 29670 26782 42564821
Haemoptysis 30.72 15.22 86 29646 46081 42545522
Stent placement 30.13 15.22 27 29705 5333 42586270
Atrioventricular block second degree 29.48 15.22 24 29708 4163 42587440
Diastolic dysfunction 29.42 15.22 30 29702 6953 42584650
Infusion related reaction 29.00 15.22 4 29728 60802 42530801
Duodenal ulcer 28.70 15.22 39 29693 12240 42579363
Tachypnoea 28.64 15.22 53 29679 21609 42569994
Neutrophil count decreased 28.36 15.22 5 29727 63410 42528193
Ventricular tachycardia 28.27 15.22 64 29668 30096 42561507
Myopathy 28.14 15.22 41 29691 13720 42577883
Muscle enzyme increased 28.10 15.22 10 29722 315 42591288
Off label use 27.97 15.22 298 29434 638037 41953566
Orthopnoea 27.93 15.22 26 29706 5391 42586212
Intrapericardial thrombosis 27.91 15.22 7 29725 62 42591541
Cardiac tamponade 27.38 15.22 28 29704 6512 42585091
Neuropathy peripheral 27.04 15.22 19 29713 101834 42489769
Blood urine present 27.02 15.22 37 29695 11696 42579907
Overdose 26.19 15.22 21 29711 105243 42486360
Cardiac failure 26.11 15.22 145 29587 106711 42484892
Nasopharyngitis 26.06 15.22 13 29719 83983 42507620
Dizziness 26.05 15.22 277 29455 248977 42342626
Mallory-Weiss syndrome 25.80 15.22 15 29717 1506 42590097
Leukopenia 25.66 15.22 10 29722 74736 42516867
Vasospasm 25.63 15.22 11 29721 575 42591028
Myelofibrosis 25.60 15.22 16 29716 1831 42589772
Dehydration 25.58 15.22 37 29695 141730 42449873
Ejection fraction decreased 25.47 15.22 51 29681 22036 42569567
Seizure 25.36 15.22 28 29704 120533 42471070
Left ventricular enlargement 24.93 15.22 12 29720 820 42590783
Oxygen consumption decreased 24.75 15.22 9 29723 302 42591301
Sinus node dysfunction 24.63 15.22 23 29709 4789 42586814
Anterior interosseous syndrome 24.42 15.22 5 29727 15 42591588
ECG signs of myocardial ischaemia 24.34 15.22 8 29724 197 42591406
Decreased appetite 23.93 15.22 63 29669 193074 42398529
Intracardiac thrombus 23.88 15.22 17 29715 2415 42589188
Sleep apnoea syndrome 23.86 15.22 49 29683 21559 42570044
Overlap syndrome 23.84 15.22 9 29723 336 42591267
Intestinal haematoma 23.82 15.22 8 29724 211 42591392
Therapeutic product effect incomplete 23.52 15.22 10 29722 70929 42520674
Gingival bleeding 23.01 15.22 29 29703 8456 42583147
Ventricular fibrillation 22.95 15.22 59 29673 30064 42561539
Foetal exposure during pregnancy 22.83 15.22 3 29729 47308 42544295
Hiatus hernia 22.81 15.22 29 29703 8531 42583072
Diverticulum intestinal haemorrhagic 22.73 15.22 18 29714 3001 42588602
Stomatitis 22.44 15.22 4 29728 50325 42541278
Oedema peripheral 22.19 15.22 38 29694 136038 42455565
Platelet aggregation abnormal 21.93 15.22 5 29727 28 42591575
Somnolence 21.58 15.22 41 29691 141064 42450539
Reperfusion injury 21.36 15.22 6 29726 85 42591518
Dyspnoea at rest 21.15 15.22 20 29712 4229 42587374
Thrombotic thrombocytopenic purpura 21.06 15.22 19 29713 3785 42587818
Accelerated idioventricular rhythm 20.72 15.22 7 29725 188 42591415
Ischaemic stroke 20.64 15.22 47 29685 22186 42569417
Bronchial haemorrhage 20.63 15.22 10 29722 694 42590909
Microcytic anaemia 20.53 15.22 17 29715 3018 42588585
Infection 20.46 15.22 29 29703 112039 42479564
Ascites 20.44 15.22 7 29725 56671 42534932
Acute kidney injury 20.21 15.22 364 29368 366973 42224630
Haemorrhagic infarction 20.17 15.22 9 29723 517 42591086
Coronary ostial stenosis 20.13 15.22 6 29726 106 42591497
Palpitations 19.81 15.22 79 29653 50718 42540885
Syncope 19.25 15.22 127 29605 99279 42492324
Circumstance or information capable of leading to medication error 18.88 15.22 15 29717 2513 42589090
Dropped head syndrome 18.86 15.22 7 29725 249 42591354
Platelet aggregation decreased 18.85 15.22 4 29728 15 42591588
Plasma cell myeloma 18.74 15.22 5 29727 47573 42544030
Influenza 18.72 15.22 10 29722 62165 42529438
Weight increased 18.68 15.22 29 29703 107954 42483649
Urinary bladder haemorrhage 18.34 15.22 13 29719 1834 42589769
Walking disability 18.05 15.22 11 29721 1203 42590400
Apheresis related complication 17.92 15.22 4 29728 20 42591583
Mitral valve incompetence 17.74 15.22 37 29695 16452 42575151
Gout 17.44 15.22 51 29681 28004 42563599
Troponin increased 17.36 15.22 40 29692 19022 42572581
Electrocardiogram PR prolongation 17.25 15.22 10 29722 998 42590605
Hypertrophy 17.22 15.22 8 29724 505 42591098
Deep vein thrombosis 17.16 15.22 17 29715 76940 42514663
Acquired haemophilia 17.12 15.22 12 29720 1663 42589940
Eosinophilia 16.92 15.22 56 29676 32843 42558760
Stenosis 16.84 15.22 13 29719 2088 42589515
Haematochezia 16.81 15.22 83 29649 58353 42533250
Decompressive craniectomy 16.73 15.22 3 29729 3 42591600
Large intestine polyp 16.66 15.22 26 29706 9239 42582364
Cerebral haematoma 16.54 15.22 20 29712 5590 42586013
Delirium 16.48 15.22 8 29724 52511 42539092
Myelosuppression 16.42 15.22 4 29728 40457 42551146
Myasthenic syndrome 16.37 15.22 9 29723 812 42590791
Weight decreased 16.35 15.22 82 29650 207866 42383737
Electrocardiogram RR interval prolonged 16.27 15.22 3 29729 4 42591599
Cerebellar haematoma 16.26 15.22 6 29726 210 42591393
Pruritus allergic 16.25 15.22 7 29725 369 42591234
Product administration error 16.17 15.22 38 29694 18305 42573298
Scar pain 16.05 15.22 5 29727 103 42591500
Procalcitonin increased 15.92 15.22 13 29719 2263 42589340
Gastrointestinal ulcer 15.82 15.22 12 29720 1878 42589725
Ventricular tachyarrhythmia 15.59 15.22 7 29725 408 42591195
Upper respiratory tract infection 15.57 15.22 5 29727 42168 42549435
Bladder tamponade 15.56 15.22 8 29724 630 42590973
Depressed level of consciousness 15.52 15.22 7 29725 47963 42543640
Therapy cessation 15.52 15.22 40 29692 20410 42571193
Paroxysmal atrioventricular block 15.51 15.22 3 29729 6 42591597
Platelet function test abnormal 15.45 15.22 5 29727 117 42591486
Spinal epidural haematoma 15.40 15.22 7 29725 420 42591183

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
Vascular stent thrombosis 1999.65 15.30 431 40645 3730 110544493
Rhabdomyolysis 1171.37 15.30 662 40414 119739 110428484
Acute myocardial infarction 834.06 15.30 468 40608 83309 110464914
Myocardial infarction 756.70 15.30 602 40474 191481 110356742
Drug interaction 704.13 15.30 895 40181 499288 110048935
Thrombosis in device 652.37 15.30 184 40892 5143 110543080
Dyspnoea 644.70 15.30 1323 39753 1105549 109442674
Chest discomfort 493.96 15.30 452 40624 173396 110374827
Gastrointestinal haemorrhage 489.19 15.30 440 40636 165078 110383145
Melaena 371.87 15.30 261 40815 68496 110479727
Angina pectoris 333.44 15.30 235 40841 62060 110486163
Angina unstable 330.23 15.30 148 40928 16284 110531939
Asphyxia 324.39 15.30 140 40936 14075 110534148
Sinus arrest 312.60 15.30 99 40977 4143 110544080
Chest pain 294.14 15.30 512 40564 375863 110172360
Cerebral haemorrhage 279.81 15.30 215 40861 64753 110483470
Acute kidney injury 279.08 15.30 681 40395 634749 109913474
Vascular stent stenosis 248.48 15.30 66 41010 1463 110546760
Coronary artery stenosis 242.12 15.30 113 40963 13645 110534578
Haemorrhage intracranial 225.05 15.30 138 40938 28831 110519392
Acute coronary syndrome 223.92 15.30 127 40949 22985 110525238
Coronary artery occlusion 221.52 15.30 111 40965 15661 110532562
Anaemia 220.69 15.30 568 40508 546518 110001705
Bradycardia 180.40 15.30 254 40822 155263 110392960
Cardiac arrest 175.13 15.30 284 40792 196469 110351754
Sinoatrial block 163.13 15.30 47 41029 1418 110546805
Labelled drug-drug interaction medication error 162.45 15.30 113 40963 29189 110519034
Haemorrhage 162.08 15.30 199 40877 106493 110441730
Atrioventricular block complete 159.39 15.30 97 40979 19985 110528238
Coronary artery disease 146.63 15.30 156 40920 71534 110476689
Shock haemorrhagic 141.58 15.30 101 40975 27146 110521077
Epistaxis 140.99 15.30 206 40870 130166 110418057
Myopathy 130.79 15.30 93 40983 24867 110523356
Upper gastrointestinal haemorrhage 129.94 15.30 124 40952 49972 110498251
Coronary artery thrombosis 122.77 15.30 46 41030 3198 110545025
Haemoglobin decreased 116.67 15.30 274 40802 248453 110299770
Rectal haemorrhage 116.24 15.30 180 40896 119653 110428570
Haematuria 113.60 15.30 147 40929 82858 110465365
Breath holding 108.04 15.30 22 41054 139 110548084
Infusion related reaction 107.99 15.30 9 41067 381153 110167070
Subarachnoid haemorrhage 107.92 15.30 89 40987 29613 110518610
Haematoma 106.95 15.30 120 40956 58356 110489867
Coronary artery restenosis 105.43 15.30 32 41044 1160 110547063
Pulmonary haemorrhage 104.40 15.30 69 41007 16387 110531836
Cardiogenic shock 103.73 15.30 117 40959 57221 110491002
Blood loss anaemia 103.40 15.30 71 41005 17954 110530269
Electrocardiogram ST segment elevation 98.72 15.30 54 41022 9106 110539117
Atrioventricular block 95.68 15.30 66 41010 16811 110531412
Hypersensitivity myocarditis 90.84 15.30 22 41054 331 110547892
Subdural haematoma 88.45 15.30 87 40989 36367 110511856
Mixed liver injury 87.36 15.30 55 41021 12024 110536199
Muscle necrosis 84.84 15.30 30 41046 1767 110546456
Myocardial ischaemia 84.73 15.30 74 41002 26610 110521613
Coronary artery dissection 83.22 15.30 27 41049 1221 110547002
Cardiac ventricular thrombosis 81.77 15.30 34 41042 3113 110545110
Eosinophilia 81.45 15.30 104 40972 57832 110490391
Alopecia 81.32 15.30 18 41058 364735 110183488
Faeces discoloured 80.47 15.30 80 40996 33868 110514355
Toxicity to various agents 80.41 15.30 39 41037 480516 110067707
Haemorrhagic stroke 78.35 15.30 54 41022 13735 110534488
Retroperitoneal haematoma 76.93 15.30 40 41036 6091 110542132
Pyrexia 76.07 15.30 136 40940 898129 109650094
Cardiac failure 74.50 15.30 194 40882 187432 110360791
Arthropathy 73.23 15.30 10 41066 287512 110260711
Stomatitis 72.24 15.30 8 41068 270234 110277989
Ventricular asystole 72.01 15.30 19 41057 410 110547813
Febrile neutropenia 69.86 15.30 16 41060 316751 110231472
Platelet aggregation inhibition 69.26 15.30 16 41060 194 110548029
Nasopharyngitis 67.50 15.30 31 41045 394330 110153893
Rash maculo-papular 65.76 15.30 107 40969 74115 110474108
Brain herniation 65.72 15.30 41 41035 8822 110539401
Haematemesis 64.72 15.30 94 40982 59014 110489209
Pemphigus 63.80 15.30 4 41072 214566 110333657
Haemoptysis 63.39 15.30 103 40973 71251 110476972
Stent placement 62.74 15.30 37 41039 7197 110541026
Ventricular fibrillation 62.59 15.30 77 40999 41236 110506987
Hepatitis cholestatic 62.49 15.30 52 41024 17514 110530709
Lower gastrointestinal haemorrhage 62.21 15.30 53 41023 18433 110529790
Systemic lupus erythematosus 62.10 15.30 10 41066 254328 110293895
Sinusitis 61.53 15.30 17 41059 296671 110251552
Gastric haemorrhage 60.57 15.30 49 41027 15866 110532357
Psoriatic arthropathy 60.56 15.30 3 41073 196758 110351465
Wound 60.05 15.30 8 41068 234429 110313794
Pain 59.35 15.30 171 40905 954784 109593439
Vascular stent occlusion 59.16 15.30 15 41061 275 110547948
Duodenal ulcer 57.74 15.30 52 41024 19462 110528761
Tachypnoea 57.40 15.30 72 41004 39323 110508900
Gastric ulcer 56.77 15.30 72 41004 39755 110508468
Syncope 55.95 15.30 184 40892 202352 110345871
Synovitis 54.47 15.30 17 41059 274075 110274148
Sinus bradycardia 53.04 15.30 60 41016 29423 110518800
Iron deficiency anaemia 53.03 15.30 62 41014 31497 110516726
Drug reaction with eosinophilia and systemic symptoms 52.93 15.30 103 40973 81992 110466231
Brain natriuretic peptide increased 52.43 15.30 39 41037 11170 110537053
Gastritis erosive 52.25 15.30 40 41036 11960 110536263
Gastric ulcer haemorrhage 51.47 15.30 37 41039 10057 110538166
Swelling 50.80 15.30 34 41042 351007 110197216
Cerebral haematoma 50.71 15.30 36 41040 9596 110538627
Joint swelling 50.49 15.30 54 41022 442791 110105432
Mobility decreased 50.37 15.30 13 41063 237409 110310814
Cholestatic liver injury 49.40 15.30 32 41044 7344 110540879
Treatment failure 48.67 15.30 21 41055 277213 110271010
Fibromyalgia 48.47 15.30 4 41072 170905 110377318
Device malfunction 47.66 15.30 53 41023 25505 110522718
Impaired healing 47.42 15.30 8 41068 196709 110351514
Heparin-induced thrombocytopenia 47.38 15.30 37 41039 11387 110536836
Ventricular tachycardia 46.90 15.30 74 41002 49935 110498288
Pericarditis 46.47 15.30 12 41064 219102 110329121
Suffocation feeling 45.75 15.30 20 41056 2071 110546152
Cardiac tamponade 45.56 15.30 36 41040 11271 110536952
Injury 45.51 15.30 6 41070 177259 110370964
Cheyne-Stokes respiration 45.49 15.30 14 41062 532 110547691
Loss of control of legs 45.38 15.30 20 41056 2112 110546111
Troponin increased 44.32 15.30 55 41021 29711 110518512
Hepatic cytolysis 44.26 15.30 76 41000 54977 110493246
Therapeutic product effect incomplete 44.25 15.30 14 41062 223791 110324432
Atrioventricular block second degree 44.05 15.30 31 41045 8150 110540073
Arterial thrombosis 43.93 15.30 22 41054 3097 110545126
Arthralgia 43.85 15.30 146 40930 779486 109768737
Ill-defined disorder 43.58 15.30 4 41072 156849 110391374
Irritable bowel syndrome 43.53 15.30 5 41071 164210 110384013
Pericardial haemorrhage 43.46 15.30 26 41050 5191 110543032
Neutropenia 43.45 15.30 45 41031 374575 110173648
Diastolic dysfunction 42.63 15.30 36 41040 12368 110535855
Drug intolerance 42.62 15.30 53 41023 406459 110141764
Dry mouth 42.31 15.30 11 41065 199937 110348286
Therapeutic product effect decreased 42.10 15.30 19 41057 244297 110303926
Gingival bleeding 42.01 15.30 44 41032 19795 110528428
Infection 41.46 15.30 44 41032 362156 110186067
Gastroduodenal ulcer 41.28 15.30 15 41061 956 110547267
White blood cell count decreased 40.86 15.30 17 41059 229373 110318850
Muscle injury 40.75 15.30 3 41073 140804 110407419
Rheumatoid arthritis 40.74 15.30 31 41045 299582 110248641
Malignant neoplasm progression 40.14 15.30 8 41068 174559 110373664
ECG signs of myocardial ischaemia 40.05 15.30 12 41064 416 110547807
Off label use 39.99 15.30 361 40715 1499824 109048399
Platelet function test abnormal 39.98 15.30 10 41066 173 110548050
Sinus node dysfunction 39.04 15.30 30 41046 9017 110539206
Lower respiratory tract infection 38.73 15.30 21 41055 243085 110305138
Ischaemic stroke 38.61 15.30 61 41015 41202 110507021
Migraine 37.17 15.30 9 41067 171643 110376580
Intraventricular haemorrhage 37.15 15.30 24 41052 5483 110542740
Microcytic anaemia 36.86 15.30 25 41051 6193 110542030
Exposure during pregnancy 35.82 15.30 9 41067 167415 110380808
Subcutaneous haematoma 35.79 15.30 19 41057 3017 110545206
Night sweats 35.71 15.30 4 41072 133979 110414244
Abdominal discomfort 35.66 15.30 57 41019 393801 110154422
Device dislocation 35.55 15.30 51 41025 31653 110516570
Helicobacter infection 34.86 15.30 12 41064 181865 110366358
Pulmonary alveolar haemorrhage 34.54 15.30 40 41036 20110 110528113
Stenosis 34.04 15.30 19 41057 3332 110544891
Lymphorrhoea 33.73 15.30 9 41067 203 110548020
Pneumonia 33.50 15.30 190 40886 876524 109671699
Myositis 33.36 15.30 49 41027 31067 110517156
Weight increased 33.25 15.30 66 41010 419578 110128645
Retroperitoneal haemorrhage 32.70 15.30 23 41053 6042 110542181
Intrapericardial thrombosis 32.30 15.30 7 41069 62 110548161
Intracardiac thrombus 32.29 15.30 20 41056 4248 110543975
Mitral valve incompetence 32.20 15.30 50 41026 33279 110514944
Electrocardiogram P wave abnormal 32.19 15.30 10 41066 392 110547831
Base excess decreased 32.14 15.30 10 41066 394 110547829
Orthopnoea 31.88 15.30 29 41047 10992 110537231
Diabetic macroangiopathy 31.69 15.30 8 41068 144 110548079
Left ventricular enlargement 31.69 15.30 12 41064 859 110547364
Blood creatine phosphokinase increased 31.51 15.30 78 40998 72999 110475224
Cholestasis 31.20 15.30 72 41004 64446 110483777
Peripheral swelling 30.77 15.30 65 41011 403969 110144254
Chronic coronary syndrome 30.73 15.30 9 41067 288 110547935
Capillary fragility test 30.65 15.30 6 41070 30 110548193
Blister 30.30 15.30 24 41052 227352 110320871
Thrombosis 30.23 15.30 99 40977 108563 110439660
Osteoarthritis 30.23 15.30 15 41061 182608 110365615
Myelofibrosis 30.18 15.30 17 41059 3034 110545189
Hepatocellular injury 29.60 15.30 61 41015 50581 110497642
Muscle enzyme increased 29.44 15.30 10 41066 522 110547701
Hypotension 29.12 15.30 310 40766 523539 110024684
Miller Fisher syndrome 29.09 15.30 9 41067 348 110547875
Toxic skin eruption 29.02 15.30 43 41033 27472 110520751
Neutrophil count decreased 28.96 15.30 5 41071 120936 110427287
Arthritis 28.92 15.30 13 41063 167573 110380650
Sleep disorder due to general medical condition, insomnia type 28.54 15.30 3 41073 105640 110442583
Gastrointestinal disorder 28.11 15.30 29 41047 241923 110306300
Musculoskeletal stiffness 27.75 15.30 38 41038 279784 110268439
Constipation 27.71 15.30 57 41019 357729 110190494
Intentional product misuse 27.55 15.30 110 40966 132794 110415429
Ecchymosis 27.37 15.30 33 41043 17305 110530918
Drug abuse 27.28 15.30 16 41060 177395 110370828
Ejection fraction decreased 27.21 15.30 52 41024 40828 110507395
Intermittent claudication 27.13 15.30 17 41059 3684 110544539
Subacute cutaneous lupus erythematosus 27.06 15.30 19 41057 4975 110543248
Ischaemic cardiomyopathy 27.02 15.30 23 41053 7988 110540235
Pancytopenia 26.85 15.30 23 41053 209590 110338633
Confusional state 26.83 15.30 87 40989 468593 110079630
Haematochezia 26.72 15.30 99 40977 115425 110432798
Electrocardiogram RR interval prolonged 26.66 15.30 5 41071 19 110548204
Eosinophil cationic protein increased 26.59 15.30 6 41070 65 110548158
Gout 26.20 15.30 48 41028 36518 110511705
Anterior interosseous syndrome 25.89 15.30 5 41071 23 110548200
Device occlusion 25.79 15.30 30 41046 15155 110533068
Oxygen consumption decreased 25.63 15.30 9 41067 519 110547704
Diverticulum intestinal haemorrhagic 25.53 15.30 18 41058 4745 110543478
Contraindicated product administered 25.35 15.30 33 41043 248234 110299989
Intentional product use issue 25.26 15.30 33 41043 247873 110300350
Vascular pseudoaneurysm 25.21 15.30 17 41059 4173 110544050
Completed suicide 24.97 15.30 32 41044 242349 110305874
Intestinal haematoma 24.89 15.30 8 41068 351 110547872
Vasospasm 24.69 15.30 12 41064 1584 110546639
Haemorrhagic infarction 24.44 15.30 10 41066 879 110547344
Neuropathy peripheral 23.79 15.30 19 41057 179258 110368965
Cardiac aneurysm 23.67 15.30 12 41064 1733 110546490
Urinary tract infection 23.59 15.30 54 41022 326228 110221995
Dizziness 23.55 15.30 377 40699 697816 109850407
Immune-mediated myositis 23.44 15.30 19 41057 6167 110542056
Bronchial haemorrhage 23.19 15.30 11 41065 1376 110546847
Labelled drug-drug interaction issue 23.15 15.30 16 41060 4085 110544138
Dyspnoea exertional 23.08 15.30 88 40988 103972 110444251
Duodenal ulcer haemorrhage 22.96 15.30 21 41055 8016 110540207
Hypoaesthesia 22.72 15.30 52 41024 314171 110234052
Bradyarrhythmia 22.70 15.30 17 41059 4917 110543306
Large intestine polyp 22.61 15.30 28 41048 15089 110533134
Acid base balance abnormal 22.59 15.30 8 41068 473 110547750
Diarrhoea 22.33 15.30 294 40782 1139211 109409012
Headache 22.26 15.30 215 40861 882162 109666061
Arterial restenosis 22.09 15.30 5 41071 55 110548168
Bundle branch block right 22.08 15.30 25 41051 12266 110535957
Coronary arterial stent insertion 22.06 15.30 18 41058 5897 110542326
Capillary fragility increased 22.05 15.30 4 41072 12 110548211
Coma acidotic 22.01 15.30 6 41070 147 110548076
Hyperlipidaemia 21.92 15.30 44 41032 35804 110512419
Mallory-Weiss syndrome 21.88 15.30 14 41062 3147 110545076
Ventricular tachyarrhythmia 21.79 15.30 8 41068 525 110547698
Oedema peripheral 21.72 15.30 57 41019 328603 110219620
Acquired haemophilia 21.62 15.30 13 41063 2618 110545605
Myalgia 21.56 15.30 149 40927 222232 110325991
Blood urine present 21.53 15.30 35 41041 24210 110524013
Peripheral venous disease 21.22 15.30 3 41073 84114 110464109
Hypersensitivity 21.08 15.30 78 40998 403920 110144303
Oropharyngeal pain 21.08 15.30 12 41064 135264 110412959
Wound infection 21.00 15.30 5 41071 96460 110451763
Procalcitonin increased 20.98 15.30 15 41061 4041 110544182
Fatigue 20.90 15.30 322 40754 1215636 109332587
Arteriospasm coronary 20.74 15.30 21 41055 9079 110539144
Injection site reaction 20.64 15.30 4 41072 89066 110459157
Pancreatitis acute 20.58 15.30 59 41017 60215 110488008
Thrombocytopenia 20.56 15.30 209 40867 348676 110199547
Post procedural haemorrhage 20.47 15.30 27 41049 15485 110532738
Cerebellar haematoma 20.44 15.30 8 41068 626 110547597
Apheresis related complication 20.44 15.30 4 41072 20 110548203
Dyspnoea at rest 20.39 15.30 20 41056 8326 110539897
Abnormal loss of weight 20.39 15.30 22 41054 10235 110537988
Cardiac failure acute 20.36 15.30 34 41042 24044 110524179
Oedema 20.33 15.30 29 41047 209947 110338276
Myelosuppression 20.32 15.30 5 41071 94335 110453888
Somnolence 20.10 15.30 51 41025 297398 110250825
Reperfusion injury 19.97 15.30 6 41070 210 110548013
Injection site pain 19.91 15.30 22 41054 177900 110370323
Coronary revascularisation 19.91 15.30 5 41071 88 110548135
Sciatica 19.70 15.30 5 41071 92394 110455829
Arteriosclerosis 19.65 15.30 34 41042 24733 110523490
Disease progression 19.64 15.30 38 41038 243996 110304227
Forced vital capacity decreased 19.55 15.30 11 41065 1959 110546264
Metabolic acidosis 19.43 15.30 81 40995 99663 110448560
Herpes zoster 19.34 15.30 8 41068 108371 110439852
Haemoperitoneum 19.27 15.30 16 41060 5372 110542851
Chronic gastritis 19.21 15.30 16 41060 5395 110542828
Splenic rupture 19.05 15.30 12 41064 2625 110545598
Gait inability 18.67 15.30 14 41062 136362 110411861
Head injury 18.63 15.30 46 41030 42971 110505252
Epilepsy 18.54 15.30 7 41069 100202 110448021
Petechiae 18.49 15.30 32 41044 23285 110524938
Blood cholesterol increased 18.41 15.30 25 41051 184760 110363463
Cardiac flutter 18.34 15.30 16 41060 5741 110542482
Gastrointestinal angiodysplasia 18.23 15.30 9 41067 1229 110546994
Accelerated idioventricular rhythm 18.19 15.30 6 41070 286 110547937
Myocardial rupture 18.17 15.30 6 41070 287 110547936
Cardiac failure chronic 18.17 15.30 24 41052 13787 110534436
Osteoporosis 18.04 15.30 5 41071 87147 110461076
Myasthenic syndrome 17.97 15.30 9 41067 1267 110546956
Dropped head syndrome 17.97 15.30 7 41069 541 110547682
Ventricular extrasystoles 17.86 15.30 31 41045 22610 110525613
Decompressive craniectomy 17.76 15.30 3 41073 5 110548218
Progressive multiple sclerosis 17.66 15.30 9 41067 1315 110546908
Coronary artery reocclusion 17.54 15.30 5 41071 145 110548078
Drug hypersensitivity 17.52 15.30 98 40978 453992 110094231
Hypertensive crisis 17.47 15.30 32 41044 24340 110523883
Overdose 17.46 15.30 38 41038 233756 110314467
Hypertrophy 17.44 15.30 8 41068 927 110547296
Hepatic enzyme increased 17.37 15.30 61 41015 320831 110227392
Spinal cord haemorrhage 17.26 15.30 7 41069 601 110547622
Sleep apnoea syndrome 17.25 15.30 43 41033 40404 110507819
Haemorrhoidal haemorrhage 17.23 15.30 18 41058 8075 110540148
Myocardial necrosis marker increased 17.04 15.30 13 41063 3867 110544356
Cardiac discomfort 17.01 15.30 9 41067 1419 110546804
Catheter site thrombosis 16.98 15.30 7 41069 627 110547596
Hyperkalaemia 16.90 15.30 97 40979 135699 110412524
Intestinal haemorrhage 16.84 15.30 17 41059 7324 110540899
Gastritis 16.84 15.30 51 41025 53648 110494575
Palpitations 16.82 15.30 109 40967 159103 110389120
Lipid metabolism disorder 16.77 15.30 7 41069 647 110547576
Immune thrombocytopenia 16.71 15.30 30 41046 22464 110525759
Fibroma 16.69 15.30 8 41068 1024 110547199
Back pain 16.62 15.30 76 41000 370920 110177303
Post procedural haematoma 16.58 15.30 11 41065 2628 110545595
Subdural haemorrhage 16.56 15.30 16 41060 6542 110541681
Arrhythmia 16.40 15.30 60 41016 69515 110478708
Live birth 16.36 15.30 3 41073 69481 110478742
Ascites 16.32 15.30 7 41069 92801 110455422
Cell death 16.29 15.30 15 41061 5776 110542447
Myocardial haemorrhage 16.29 15.30 4 41072 64 110548159
Atrial fibrillation 16.23 15.30 143 40933 229499 110318724
Deep vein thrombosis 15.98 15.30 17 41059 139870 110408353
Gastrointestinal ulcer 15.96 15.30 13 41063 4247 110543976
Catheter site haematoma 15.96 15.30 6 41070 421 110547802
Discomfort 15.95 15.30 35 41041 214672 110333551
Urinary bladder haemorrhage 15.91 15.30 11 41065 2811 110545412
Allergic eosinophilia 15.84 15.30 4 41072 72 110548151
Type 2 diabetes mellitus 15.70 15.30 26 41050 177206 110371017
Vomiting 15.67 15.30 241 40835 910434 109637789
Abdominal pain 15.58 15.30 119 40957 512870 110035353
Wheezing 15.57 15.30 46 41030 255184 110293039
Thrombotic thrombocytopenic purpura 15.47 15.30 16 41060 7095 110541128
Renal failure 15.45 15.30 140 40936 226434 110321789
Percutaneous coronary intervention 15.44 15.30 6 41070 461 110547762
Restenosis 15.33 15.30 3 41073 15 110548208

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC24 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA PE N0000008832 Decreased Platelet Aggregation
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058921 Purinergic P2Y Receptor Antagonists
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA EPC N0000182142 P2Y12 Platelet Inhibitor
FDA MoA N0000182143 P2Y12 Receptor Antagonists
FDA MoA N0000185503 P-Glycoprotein Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:68563 P2Y<small><sub>12</sub></small> receptor antagonist
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

B01AC Platelet aggregation inhibitors excl. heparin 24 drugs

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

DiseaseRelationSNOMED_IDDOID
Acute coronary syndrome indication 394659003
Peripheral vascular disease indication 400047006
Percutaneous coronary intervention indication 415070008
Myocardial Reinfarction Prevention indication
Intracranial hemorrhage contraindication 1386000
Hepatic failure contraindication 59927004
Disease of liver contraindication 235856003 DOID:409
Surgical procedure contraindication 387713003
Significant Bleeding contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.07 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
60MG BRILINTA ASTRAZENECA N022433 Sept. 3, 2015 RX TABLET ORAL 10300065 Jan. 27, 2036 REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY AND HAVING OR WHO HAD ACUTE CORONARY SYNDROME BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY
60MG BRILINTA ASTRAZENECA N022433 Sept. 3, 2015 RX TABLET ORAL 10300065 Jan. 27, 2036 REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION (MI), AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY WITH A HISTORY OF MI BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY
90MG BRILINTA ASTRAZENECA N022433 July 20, 2011 RX TABLET ORAL 10300065 Jan. 27, 2036 REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY AND HAVING OR WHO HAD ACUTE CORONARY SYNDROME BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY
90MG BRILINTA ASTRAZENECA N022433 July 20, 2011 RX TABLET ORAL 10300065 Jan. 27, 2036 REDUCING THE RATE OF CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION (MI), AND STROKE IN A PATIENT RECEIVING 75-100 MG ASPIRIN DAILY WITH A HISTORY OF MI BY ADMINISTERING 60 MG TICAGRELOR TWICE DAILY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
P2Y purinoceptor 12 GPCR NEGATIVE ALLOSTERIC MODULATOR Ki 7.85 CHEMBL CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 6.29 CHEMBL
Equilibrative nucleoside transporter 1 Transporter INHIBITOR Ki 7.30 IUPHAR
Transmembrane protein 97 Enzyme Ki 5.89 CHEMBL
P2Y purinoceptor 12 GPCR IC50 5.38 CHEMBL

External reference:

IDSource
4030908 VUID
N0000182973 NUI
D09017 KEGG_DRUG
4030908 VANDF
C1999375 UMLSCUI
CHEBI:68558 CHEBI
TIQ PDB_CHEM_ID
CHEMBL398435 ChEMBL_ID
D000077486 MESH_DESCRIPTOR_UI
DB08816 DRUGBANK_ID
1765 IUPHAR_LIGAND_ID
8772 INN_ID
GLH0314RVC UNII
9871419 PUBCHEM_CID
1116632 RXNORM
182026 MMSL
235692 MMSL
256501 MMSL
27677 MMSL
d07721 MMSL
013611 NDDF
698805004 SNOMEDCT_US
704464003 SNOMEDCT_US
GLH0314RVC INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 0186-0776 TABLET 60 mg ORAL NDA 30 sections
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 0186-0777 TABLET 90 mg ORAL NDA 30 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 0378-2214 TABLET, FILM COATED 60 mg ORAL ANDA 29 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 0378-2215 TABLET, FILM COATED 90 mg ORAL ANDA 29 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 0480-2688 TABLET, FILM COATED 60 mg ORAL ANDA 28 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 0480-2695 TABLET, FILM COATED 90 mg ORAL ANDA 28 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 11788-157 TABLET 60 mg ORAL ANDA 26 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 11788-158 TABLET 90 mg ORAL ANDA 26 sections
Ticagrelor Human Prescription Drug Label 1 33342-431 TABLET, FILM COATED 60 mg ORAL ANDA 27 sections
Ticagrelor Human Prescription Drug Label 1 33342-432 TABLET, FILM COATED 90 mg ORAL ANDA 27 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 42658-115 TABLET, FILM COATED 90 mg ORAL ANDA 28 sections
TICAGRELOR HUMAN PRESCRIPTION DRUG LABEL 1 43547-657 TABLET, FILM COATED 90 mg ORAL ANDA 20 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 43598-480 TABLET 90 mg ORAL ANDA 27 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 43598-480 TABLET 90 mg ORAL ANDA 27 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 43598-629 TABLET 60 mg ORAL ANDA 27 sections
Ticagrelor Human Prescription Drug Label 1 46708-241 TABLET, FILM COATED 90 mg ORAL ANDA 28 sections
Ticagrelor Human Prescription Drug Label 1 46708-241 TABLET, FILM COATED 90 mg ORAL ANDA 28 sections
Ticagrelor Human Prescription Drug Label 1 46708-500 TABLET, FILM COATED 60 mg ORAL ANDA 28 sections
ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 50228-521 TABLET 60 mg ORAL ANDA 28 sections
ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 50228-522 TABLET 90 mg ORAL ANDA 28 sections
TICAGRELOR HUMAN PRESCRIPTION DRUG LABEL 1 50268-826 TABLET 90 mg ORAL ANDA 26 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 51407-861 TABLET 90 mg ORAL ANDA 27 sections
BRILINTA HUMAN PRESCRIPTION DRUG LABEL 1 55154-9618 TABLET 90 mg ORAL NDA 30 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 55488-0543 TABLET 90 mg ORAL ANDA 30 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 55488-0544 TABLET 60 mg ORAL ANDA 30 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 60505-4452 TABLET 90 mg ORAL ANDA 28 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 60505-4452 TABLET 90 mg ORAL ANDA 28 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 60505-4453 TABLET 60 mg ORAL ANDA 28 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 60687-928 TABLET 90 mg ORAL ANDA 27 sections
Ticagrelor HUMAN PRESCRIPTION DRUG LABEL 1 60687-935 TABLET 60 mg ORAL ANDA 27 sections