rivastigmine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
acetylcholinesterase inhibitors 2392 123441-03-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • prometax
  • rivastigmine
  • S-Rivastigmine
  • rivastigmine tartrate
  • rivastigmine hydrogen tartrate
  • rivastigmine hexal
  • exelon
A carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE.
  • Molecular weight: 250.34
  • Formula: C14H22N2O2
  • CLOGP: 2.10
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -2.09
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
9 mg O
9.50 mg TD

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.80 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 72 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 12 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.60 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.40 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.350 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.670 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 37.757 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 6.324 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 92.640 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 89.330 % High 1
herg hERG pIC50 4.213 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.009 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 2.924 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 90.100 % High 1
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IKBKB,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PLK1,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 41
kinase-selectivity-class AXL,BRAF,CDK4,DDR1,EPHB4,MAP3K7,TEK 7
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.395 High 1
mh-clint Mouse hepatocyte intrinsic clearance 41.687 High 1
mppb Mouse plasma protein binding (% unbound) 91.760 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.030 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 92.110 % High 1
rh-clint Rat hepatocyte intrinsic clearance 40.365 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 96.010 % High 1
rppb Rat plasma protein binding (% unbound) 85.710 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 926.830 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 12, 1998 EMA
April 21, 2000 FDA NOVARTIS

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
Product adhesion issue 482.60 19.01 131 21474 5011 90601831
Application site erythema 398.28 19.01 113 21492 5095 90601747
Hallucination 385.11 19.01 223 21382 65736 90541106
Dementia 366.80 19.01 156 21449 23705 90583137
Fall 341.94 19.01 492 21113 481318 90125524
Application site pruritus 297.19 19.01 86 21519 4161 90602681
Death 286.05 19.01 440 21165 456111 90150731
On and off phenomenon 253.67 19.01 68 21537 2475 90604367
Agitation 224.94 19.01 160 21445 66938 90539904
Hallucination, visual 222.20 19.01 109 21496 22983 90583859
Disorientation 192.77 19.01 124 21481 43990 90562852
Stoma site discharge 188.11 19.01 51 21554 1938 90604904
Application site rash 173.28 19.01 51 21554 2618 90604224
Aggression 171.16 19.01 96 21509 26572 90580270
Confusional state 160.76 19.01 311 21294 385894 90220948
Dyskinesia 155.43 19.01 101 21504 36433 90570409
Cognitive disorder 150.71 19.01 128 21477 69279 90537563
Wrong technique in product usage process 145.28 19.01 127 21478 71444 90535398
Stoma site erythema 144.48 19.01 39 21566 1457 90605385
Freezing phenomenon 141.60 19.01 40 21565 1772 90605070
Delusion 138.13 19.01 67 21538 13773 90593069
Bradykinesia 133.60 19.01 53 21552 6735 90600107
Abnormal behaviour 130.56 19.01 76 21529 22552 90584290
Bradycardia 128.08 19.01 127 21478 83720 90523122
Muscle rigidity 127.13 19.01 64 21541 14245 90592597
Product administration error 122.18 19.01 77 21528 26346 90580496
Restlessness 119.22 19.01 85 21520 35635 90571207
Application site hypersensitivity 117.06 19.01 24 21581 259 90606583
Blood cholinesterase decreased 112.15 19.01 22 21583 186 90606656
Syncope 109.26 19.01 146 21459 132517 90474325
Cholinergic syndrome 105.59 19.01 26 21579 670 90606172
Tremor 95.93 19.01 148 21457 153025 90453817
Dysphagia 94.64 19.01 125 21480 112153 90494689
Speech disorder 88.69 19.01 79 21526 45506 90561336
Arthralgia 87.83 19.01 38 21567 778484 89828358
Alopecia 86.13 19.01 9 21596 495062 90111780
Memory impairment 84.48 19.01 161 21444 197083 90409759
Pain 83.89 19.01 69 21536 996272 89610570
Cerebral atrophy 83.69 19.01 36 21569 5610 90601232
Application site irritation 83.00 19.01 27 21578 1934 90604908
Somnolence 82.67 19.01 165 21440 208919 90397923
Application site reaction 81.86 19.01 22 21583 808 90606034
Mini mental status examination abnormal 80.76 19.01 11 21594 0 90606842
Hyperkinesia 79.52 19.01 26 21579 1893 90604949
Vascular encephalopathy 78.73 19.01 21 21584 749 90606093
Subileus 77.15 19.01 30 21575 3614 90603228
Joint swelling 76.17 19.01 14 21591 503286 90103556
Loss of consciousness 76.14 19.01 127 21478 140111 90466731
Pneumonia aspiration 75.79 19.01 69 21536 40871 90565971
Femur fracture 74.44 19.01 72 21533 46010 90560832
Cerebrovascular accident 72.65 19.01 116 21489 123417 90483425
Drug hypersensitivity 72.10 19.01 12 21593 463597 90143245
Rheumatoid arthritis 70.31 19.01 4 21601 362610 90244232
Lack of application site rotation 68.12 19.01 10 21595 7 90606835
Posture abnormal 67.05 19.01 25 21580 2686 90604156
Arthropathy 65.40 19.01 6 21599 366236 90240606
Vomiting 65.30 19.01 364 21241 787929 89818913
Abnormal dreams 62.79 19.01 37 21568 11220 90595622
Pemphigus 62.17 19.01 4 21601 326860 90279982
Infusion related reaction 62.17 19.01 12 21593 416768 90190074
Akinesia 61.89 19.01 21 21584 1715 90605127
Skin irritation 61.27 19.01 39 21566 13564 90593278
Femoral neck fracture 60.69 19.01 35 21570 10198 90596644
Dehydration 60.20 19.01 139 21466 194308 90412534
Dysstasia 60.15 19.01 49 21556 25003 90581839
Sinusitis 57.71 19.01 7 21598 343081 90263761
Stoma site irritation 57.65 19.01 14 21591 340 90606502
Dementia with Lewy bodies 54.91 19.01 14 21591 417 90606425
Dystonia 53.76 19.01 39 21566 16780 90590062
Swelling 52.95 19.01 17 21588 419041 90187801
Amyloid related imaging abnormality-oedema/effusion 52.46 19.01 16 21589 928 90605914
Therapeutic product effect variable 52.45 19.01 18 21587 1521 90605321
Gastrointestinal sounds abnormal 51.46 19.01 24 21581 4519 90602323
Aphasia 51.30 19.01 57 21548 42755 90564087
Decreased appetite 51.08 19.01 201 21404 376339 90230503
Hip fracture 50.28 19.01 50 21555 33027 90573815
Arrhythmia 50.11 19.01 56 21549 42276 90564566
Stoma site pain 49.96 19.01 17 21588 1400 90605442
Delirium 48.15 19.01 88 21517 104271 90502571
Stomatitis 47.71 19.01 5 21600 274693 90332149
Faecaloma 47.21 19.01 30 21575 10401 90596441
Unresponsive to stimuli 46.10 19.01 51 21554 38070 90568772
Marasmus 45.95 19.01 14 21591 809 90606033
Feeding disorder 45.76 19.01 36 21569 17476 90589366
Application site dermatitis 45.55 19.01 10 21595 153 90606689
Gait disturbance 45.45 19.01 151 21454 260345 90346497
Hypokinesia 44.79 19.01 34 21571 15663 90591179
Wound 44.58 19.01 9 21596 302971 90303871
Amyloid related imaging abnormality-microhaemorrhages and haemosiderin deposits 44.30 19.01 13 21592 660 90606182
Off label use 43.86 19.01 127 21478 1102125 89504717
Fibroma 43.60 19.01 14 21591 962 90605880
Dementia Alzheimer's type 43.25 19.01 14 21591 987 90605855
Urinary tract infection 42.93 19.01 165 21440 305467 90301375
Malaise 42.81 19.01 262 21343 585724 90021118
Hepatic enzyme increased 41.55 19.01 17 21588 360719 90246123
Balance disorder 41.21 19.01 79 21526 97001 90509841
Product prescribing error 41.14 19.01 43 21562 30102 90576740
Resting tremor 40.82 19.01 13 21592 870 90605972
Treatment failure 40.81 19.01 11 21594 303917 90302925
Accessory cardiac pathway 40.42 19.01 6 21599 5 90606837
Application site discolouration 40.04 19.01 13 21592 925 90605917
Hypersensitivity 40.00 19.01 30 21575 454647 90152195
Screaming 39.98 19.01 19 21586 3731 90603111
Tobacco interaction 39.57 19.01 8 21597 80 90606762
Nasopharyngitis 38.26 19.01 25 21580 407079 90199763
Concomitant disease aggravated 37.48 19.01 27 21578 11491 90595351
Ileus 36.87 19.01 31 21574 16515 90590327
Fracture 36.60 19.01 35 21570 22041 90584801
Urinary retention 36.46 19.01 45 21560 37699 90569143
Stoma site hypergranulation 36.31 19.01 10 21595 403 90606439
Application site swelling 36.10 19.01 11 21594 636 90606206
Orthostatic hypotension 35.87 19.01 47 21558 41780 90565062
Pleurothotonus 35.55 19.01 13 21592 1322 90605520
Peripheral swelling 35.38 19.01 28 21577 413078 90193764
Abdominal discomfort 35.36 19.01 37 21568 477291 90129551
Extrapyramidal disorder 35.21 19.01 30 21575 16273 90590569
Fibromyalgia 35.18 19.01 4 21601 206265 90400577
Nightmare 35.18 19.01 34 21571 21691 90585151
Discomfort 34.86 19.01 11 21594 274324 90332518
Depressed level of consciousness 34.35 19.01 62 21543 72722 90534120
Impaired healing 34.35 19.01 7 21598 234192 90372650
Stoma site inflammation 34.15 19.01 11 21594 763 90606079
Stoma site reaction 33.87 19.01 9 21596 316 90606526
Drug interaction 33.82 19.01 143 21462 276310 90330532
Salivary hypersecretion 33.50 19.01 23 21582 9069 90597773
Intentional product use issue 32.83 19.01 6 21599 216886 90389956
Psychomotor hyperactivity 32.75 19.01 26 21579 12787 90594055
Rash 32.12 19.01 91 21514 796009 89810833
Therapeutic product effect decreased 32.08 19.01 13 21592 277558 90329284
Lower respiratory tract infection 31.94 19.01 10 21595 250649 90356193
Urinary casts present 31.71 19.01 7 21598 110 90606732
Stoma site discomfort 31.53 19.01 7 21598 113 90606729
Senile dementia 31.13 19.01 8 21597 246 90606596
Dizziness 30.89 19.01 243 21362 589041 90017801
Parkinson's disease 30.46 19.01 11 21594 1079 90605763
Dyspnoea 30.43 19.01 108 21497 880847 89725995
Type 2 diabetes mellitus 29.96 19.01 6 21599 203238 90403604
Urticaria 29.65 19.01 19 21586 312715 90294127
Eating disorder 29.61 19.01 35 21570 28038 90578804
Wheezing 29.45 19.01 10 21595 238070 90368772
Blister 29.37 19.01 12 21593 254986 90351856
Apparent death 29.33 19.01 11 21594 1201 90605641
Arthritis 29.16 19.01 3 21602 167312 90439530
Blood cholesterol increased 28.93 19.01 7 21598 208005 90398837
Parkinsonism 28.59 19.01 25 21580 14040 90592802
Cerebral haemorrhage 28.38 19.01 38 21567 34484 90572358
Ill-defined disorder 28.23 19.01 5 21600 184886 90421956
Liver injury 27.42 19.01 4 21601 170563 90436279
Dermatitis contact 27.30 19.01 24 21581 13571 90593271
Headache 27.05 19.01 110 21495 862636 89744206
Pain in extremity 27.02 19.01 41 21564 450488 90156354
Application site vesicles 26.93 19.01 11 21594 1506 90605336
Fear 26.89 19.01 26 21579 16596 90590246
Neutropenia 26.87 19.01 10 21595 224894 90381948
Product administered at inappropriate site 26.77 19.01 15 21590 4136 90602706
White blood cell count increased 26.44 19.01 53 21552 67188 90539654
Abdominal tenderness 26.17 19.01 20 21585 9304 90597538
Hypoaesthesia 26.02 19.01 22 21583 314188 90292654
Psychotic symptom 25.80 19.01 12 21593 2244 90604598
Hypophagia 25.72 19.01 37 21568 35900 90570942
Paraesthesia 25.43 19.01 14 21591 250312 90356530
Vitamin B12 deficiency 25.39 19.01 18 21587 7468 90599374
Weight decreased 25.28 19.01 166 21439 379744 90227098
Psychotic disorder 25.10 19.01 34 21571 31196 90575646
Agnosia 24.98 19.01 6 21599 139 90606703
Mental impairment 24.90 19.01 25 21580 16695 90590147
Febrile neutropenia 24.80 19.01 4 21601 158345 90448497
Urinary incontinence 24.46 19.01 37 21568 37529 90569313
Parkinsonian gait 24.44 19.01 8 21597 584 90606258
Paranoia 24.36 19.01 22 21583 12886 90593956
Fluid intake reduced 24.08 19.01 14 21591 4138 90602704
Labelled drug-drug interaction medication error 23.95 19.01 23 21582 14559 90592283
Unmasking of previously unidentified disease 23.83 19.01 10 21595 1466 90605376
Fatigue 23.54 19.01 170 21435 1153853 89452989
Device issue 23.50 19.01 32 21573 29505 90577337
Medical device site dryness 23.46 19.01 5 21600 66 90606776
Atrioventricular block second degree 23.18 19.01 14 21591 4438 90602404
Seizure 22.72 19.01 84 21521 152545 90454297
Cough 22.68 19.01 33 21572 368929 90237913
Abnormal faeces 22.51 19.01 16 21589 6666 90600176
Therapy non-responder 22.45 19.01 3 21602 136701 90470141
Oedema 22.15 19.01 10 21595 200285 90406557
Medical device site injury 22.03 19.01 3 21602 0 90606842
Completed suicide 21.97 19.01 4 21601 145054 90461788
Neuroleptic malignant syndrome 21.44 19.01 22 21583 15074 90591768
Torticollis 21.43 19.01 11 21594 2547 90604295
Stoma site haemorrhage 21.38 19.01 9 21596 1329 90605513
Cardiac failure 21.36 19.01 66 21539 109430 90497412
Anger 21.33 19.01 21 21584 13699 90593143
Apathy 21.20 19.01 19 21586 11021 90595821
Transient ischaemic attack 20.65 19.01 37 21568 43139 90563703
Weight increased 20.57 19.01 43 21562 417884 90188958
Altered state of consciousness 20.45 19.01 31 21574 31501 90575341
Stoma site extravasation 20.38 19.01 6 21599 308 90606534
Anxiety 20.38 19.01 135 21470 309637 90297205
Drug ineffective 20.27 19.01 222 21383 1384076 89222766
Tension 20.26 19.01 12 21593 3670 90603172
Sopor 20.06 19.01 27 21578 24617 90582225
Joint range of motion decreased 20.00 19.01 4 21601 135639 90471203
Osteoarthritis 19.80 19.01 11 21594 195719 90411123
Pancreatitis 19.50 19.01 48 21557 69778 90537064
Movement disorder 19.49 19.01 29 21576 28990 90577852

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
Hallucination 587.20 17.79 352 19316 57155 42544512
Product adhesion issue 398.11 17.79 103 19565 1636 42600031
On and off phenomenon 332.01 17.79 104 19564 3363 42598304
Confusional state 330.70 17.79 396 19272 167201 42434466
Fall 330.32 17.79 469 19199 234051 42367616
Aggression 308.19 17.79 213 19455 43950 42557717
Freezing phenomenon 278.06 17.79 79 19589 1810 42599857
Dementia 255.59 17.79 133 19535 16347 42585320
Application site erythema 254.18 17.79 79 19589 2487 42599180
Stoma site discharge 200.54 17.79 58 19610 1418 42600249
Agitation 196.83 17.79 192 19476 64122 42537545
Abnormal behaviour 190.09 17.79 130 19538 26321 42575346
Dyskinesia 185.34 17.79 126 19542 25264 42576403
Gait disturbance 174.05 17.79 220 19448 97780 42503887
Hallucination, visual 169.52 17.79 111 19557 20909 42580758
Cognitive disorder 162.45 17.79 131 19537 34041 42567626
Bradykinesia 162.32 17.79 69 19599 5367 42596300
Application site pruritus 162.25 17.79 50 19618 1528 42600139
Stoma site erythema 156.61 17.79 44 19624 966 42600701
Muscle rigidity 141.63 17.79 81 19587 11978 42589689
Memory impairment 122.87 17.79 133 19535 50089 42551578
Parkinsonism 118.47 17.79 69 19599 10554 42591113
Blood cholinesterase decreased 116.17 17.79 25 19643 167 42601500
Mobility decreased 107.14 17.79 105 19563 35201 42566466
Death 106.71 17.79 464 19204 470721 42130946
Speech disorder 104.41 17.79 95 19573 29026 42572641
Akinesia 103.47 17.79 40 19628 2432 42599235
Delusion 100.12 17.79 70 19598 14664 42587003
Application site rash 99.64 17.79 31 19637 978 42600689
Hyperkinesia 98.80 17.79 37 19631 2061 42599606
Restlessness 98.23 17.79 92 19576 29157 42572510
Delirium 98.04 17.79 121 19547 52398 42549269
General physical health deterioration 97.23 17.79 215 19453 151031 42450636
Disorientation 97.19 17.79 101 19567 36288 42565379
Somnolence 96.88 17.79 206 19462 140899 42460768
Tremor 95.48 17.79 165 19503 96764 42504903
Device dislocation 90.33 17.79 52 19616 7779 42593888
Dementia with Lewy bodies 86.35 17.79 27 19641 866 42600801
Stoma site reaction 83.20 17.79 21 19647 300 42601367
Fibroma 82.57 17.79 22 19646 393 42601274
Stoma site inflammation 72.61 17.79 21 19647 513 42601154
Pneumonia aspiration 66.84 17.79 98 19570 49980 42551687
Febrile neutropenia 66.65 17.79 5 19663 185698 42415969
Abnormal dreams 64.99 17.79 43 19625 8228 42593439
Paranoia 62.88 17.79 52 19616 13974 42587693
Dysphagia 61.61 17.79 116 19552 72603 42529064
Reduced facial expression 61.30 17.79 24 19644 1509 42600158
Gait inability 58.49 17.79 62 19606 22771 42578896
Motor dysfunction 58.38 17.79 40 19628 8106 42593561
Application site irritation 57.71 17.79 19 19649 721 42600946
Eyelid function disorder 56.90 17.79 14 19654 179 42601488
Stoma site pain 56.19 17.79 19 19649 784 42600883
Intentional medical device removal by patient 54.23 17.79 16 19652 420 42601247
Bradycardia 53.12 17.79 120 19548 85364 42516303
Urinary incontinence 50.53 17.79 56 19612 21612 42580055
Parkinson's disease 50.42 17.79 20 19648 1302 42600365
Sinus bradycardia 50.39 17.79 47 19621 14806 42586861
Neutropenia 49.97 17.79 15 19653 199416 42402251
Arthralgia 48.66 17.79 17 19651 205221 42396446
Psychotic disorder 47.69 17.79 63 19605 29145 42572522
Syncope 46.34 17.79 125 19543 99281 42502386
Stoma site infection 45.58 17.79 17 19651 936 42600731
Orthostatic hypotension 45.45 17.79 63 19605 30507 42571160
Tension 44.33 17.79 22 19646 2442 42599225
Joint warmth 44.06 17.79 15 19653 632 42601035
Disturbance in attention 43.58 17.79 61 19607 29805 42571862
Device kink 43.44 17.79 14 19654 496 42601171
Balance disorder 42.84 17.79 78 19590 47567 42554100
Application site reaction 42.00 17.79 13 19655 403 42601264
Device issue 40.62 17.79 40 19628 13469 42588198
Hangover 39.20 17.79 16 19652 1122 42600545
Stoma site extravasation 39.16 17.79 9 19659 84 42601583
Stoma site hypergranulation 38.87 17.79 11 19657 248 42601419
Malignant neoplasm progression 38.64 17.79 3 19665 108397 42493270
Loss of consciousness 37.99 17.79 111 19557 92243 42509424
Application site hypersensitivity 37.26 17.79 9 19659 106 42601561
Drug abuse 37.06 17.79 3 19665 104768 42496899
Acute kidney injury 36.10 17.79 72 19596 367265 42234402
Mini mental status examination abnormal 35.93 17.79 6 19662 6 42601661
Application site discolouration 35.38 17.79 11 19657 346 42601321
Urinary tract infection 34.04 17.79 112 19556 99172 42502495
Screaming 33.89 17.79 17 19651 1930 42599737
Product administration error 33.77 17.79 42 19626 18301 42583366
Dystonia 33.23 17.79 35 19633 12755 42588912
Hypokinesia 33.02 17.79 31 19637 9840 42591827
Cogwheel rigidity 32.16 17.79 16 19652 1785 42599882
Salivary hypersecretion 32.15 17.79 32 19636 10911 42590756
Psychomotor hyperactivity 32.12 17.79 32 19636 10926 42590741
Neuroleptic malignant syndrome 31.53 17.79 44 19624 21428 42580239
Nonspecific reaction 30.91 17.79 15 19653 1586 42600081
Parkinsonian gait 30.11 17.79 11 19657 571 42601096
Prescribed underdose 30.09 17.79 30 19638 10252 42591415
Dyschezia 29.37 17.79 15 19653 1769 42599898
Embedded device 29.13 17.79 10 19658 432 42601235
Dyspnoea 28.97 17.79 106 19562 442515 42159152
Marasmus 28.80 17.79 12 19656 887 42600780
Clavicle fracture 28.78 17.79 17 19651 2666 42599001
Malaise 28.31 17.79 181 19487 211975 42389692
White blood cell count decreased 28.18 17.79 8 19660 110388 42491279
Stoma site odour 28.02 17.79 6 19662 39 42601628
Cerebellar atrophy 27.28 17.79 11 19657 747 42600920
Underdose 27.28 17.79 36 19632 16630 42585037
Platelet count decreased 27.26 17.79 15 19653 138566 42463101
Headache 26.07 17.79 44 19624 239325 42362342
Pancytopenia 25.81 17.79 11 19657 117732 42483935
Dizziness postural 25.16 17.79 24 19644 7771 42593896
Cholinergic syndrome 25.06 17.79 10 19658 661 42601006
Middle insomnia 25.06 17.79 24 19644 7809 42593858
Hip fracture 25.04 17.79 31 19637 13441 42588226
Aphasia 24.98 17.79 42 19626 24041 42577626
Application site vesicles 24.90 17.79 10 19658 672 42600995
Neuropathy peripheral 24.87 17.79 8 19660 101845 42499822
Myalgia 24.45 17.79 7 19661 96073 42505594
Stoma site irritation 24.40 17.79 7 19661 166 42601501
Back pain 24.25 17.79 18 19650 141758 42459909
Cough 24.11 17.79 28 19640 178075 42423592
Therapeutic product effect variable 24.03 17.79 16 19652 3093 42598574
Femur fracture 23.98 17.79 26 19642 9786 42591881
Sputum increased 23.78 17.79 16 19652 3147 42598520
Condition aggravated 23.67 17.79 203 19465 260551 42341116
Apathy 23.63 17.79 24 19644 8382 42593285
Miosis 23.50 17.79 30 19638 13416 42588251
Device alarm issue 23.47 17.79 10 19658 781 42600886
Hypersomnia 23.04 17.79 31 19637 14587 42587080
Hypophagia 22.80 17.79 43 19625 26913 42574754
Device difficult to use 22.62 17.79 18 19650 4578 42597089
Stoma site induration 22.02 17.79 5 19663 44 42601623
Sleep disorder 21.90 17.79 60 19608 48035 42553632
Terminal state 21.08 17.79 17 19651 4406 42597261
Insomnia 21.06 17.79 109 19559 118144 42483523
Thrombocytopenia 20.69 17.79 35 19633 190244 42411423
Pyrexia 20.45 17.79 103 19565 393939 42207728
Initial insomnia 20.30 17.79 16 19652 4014 42597653
Extrapyramidal disorder 20.28 17.79 31 19637 16381 42585286
Depressed level of consciousness 20.04 17.79 58 19610 47912 42553755
Food refusal 20.03 17.79 7 19661 319 42601348
Hyporesponsive to stimuli 19.81 17.79 11 19657 1535 42600132
Off label use 19.80 17.79 194 19474 638141 41963526
Concomitant disease progression 19.63 17.79 13 19655 2490 42599177
Posture abnormal 19.54 17.79 13 19655 2508 42599159
Neutrophil count decreased 19.45 17.79 3 19665 63412 42538255
Rash 18.96 17.79 65 19603 276889 42324778
Rhinitis allergic 18.81 17.79 15 19653 3827 42597840
Incorrect product administration duration 18.78 17.79 18 19650 5862 42595805
Intentional product use issue 18.71 17.79 5 19663 71828 42529839
Urinary retention 18.56 17.79 52 19616 42162 42559505
Application site inflammation 18.47 17.79 5 19663 95 42601572
Toxicity to various agents 18.37 17.79 50 19618 229086 42372581
Infusion related reaction 18.37 17.79 3 19665 60803 42540864
Incontinence 18.29 17.79 19 19649 6811 42594856
Suspiciousness 18.16 17.79 7 19661 422 42601245
Anal incontinence 18.10 17.79 22 19646 9359 42592308
Incorrect product dosage form administered 18.02 17.79 6 19662 236 42601431
Cholinesterase inhibition 17.97 17.79 3 19665 3 42601664
Dysstasia 17.96 17.79 27 19641 14059 42587608
Sepsis 17.92 17.79 41 19627 199293 42402374

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
Hallucination 727.09 16.40 404 28374 101028 110459493
Fall 528.23 16.40 713 28065 602769 109957752
On and off phenomenon 434.35 16.40 119 28659 4305 110556216
Dementia 399.34 16.40 185 28593 31488 110529033
Confusional state 344.26 16.40 510 28268 468170 110092351
Hallucination, visual 337.07 16.40 177 28601 39428 110521093
Aggression 328.69 16.40 200 28578 59010 110501511
Freezing phenomenon 302.33 16.40 80 28698 2529 110557992
Stoma site discharge 287.49 16.40 78 28700 2717 110557804
Agitation 283.48 16.40 235 28543 112816 110447705
Dyskinesia 245.74 16.40 158 28620 51288 110509233
Blood cholinesterase decreased 214.56 16.40 44 28734 432 110560089
Stoma site erythema 212.69 16.40 58 28720 2059 110558462
Bradykinesia 211.23 16.40 86 28692 10702 110549819
Cognitive disorder 203 16.40 174 28604 87337 110473184
Application site erythema 202.45 16.40 70 28708 5540 110554981
Delusion 198.75 16.40 105 28673 23650 110536871
Disorientation 185.62 16.40 151 28627 70520 110490001
Product adhesion issue 184.01 16.40 56 28722 2950 110557571
Abnormal behaviour 181.74 16.40 118 28660 38921 110521600
Muscle rigidity 161.74 16.40 92 28686 23939 110536582
Application site pruritus 158.25 16.40 54 28724 4106 110556415
Death 154.80 16.40 465 28313 698404 109862117
Somnolence 152.99 16.40 276 28502 297173 110263348
Akinesia 148.94 16.40 50 28728 3617 110556904
Tremor 143.52 16.40 217 28561 202015 110358506
Gait disturbance 139.05 16.40 255 28523 277953 110282568
Parkinsonism 130.93 16.40 78 28700 22109 110538412
Delirium 130.32 16.40 168 28610 134857 110425664
Bradycardia 129.44 16.40 180 28598 155337 110405184
Restlessness 128.66 16.40 111 28667 56148 110504373
Pneumonia aspiration 127.48 16.40 130 28648 81103 110479418
Speech disorder 114.25 16.40 108 28670 61461 110499060
Cholinergic syndrome 113.17 16.40 32 28746 1300 110559221
Syncope 102.84 16.40 187 28591 202349 110358172
Hyperkinesia 100.63 16.40 36 28742 3148 110557373
Application site rash 97.90 16.40 33 28745 2417 110558104
Dysphagia 96.63 16.40 156 28622 153444 110407077
Arthralgia 92.07 16.40 44 28734 779588 109780933
Loss of consciousness 88.15 16.40 172 28606 196134 110364387
Abnormal dreams 86.18 16.40 49 28729 12731 110547790
Dystonia 84.81 16.40 63 28715 25742 110534779
Stoma site inflammation 84.04 16.40 24 28754 1011 110559510
Paranoia 81.20 16.40 58 28720 22316 110538205
Cerebral atrophy 78.37 16.40 41 28737 9044 110551477
Orthostatic hypotension 77.73 16.40 91 28687 66158 110494363
Drug hypersensitivity 76.67 16.40 13 28765 454077 110106444
Vascular encephalopathy 75.49 16.40 21 28757 803 110559718
Mini mental status examination abnormal 74.38 16.40 11 28767 7 110560514
Alopecia 72.49 16.40 6 28772 364747 110195774
Memory impairment 70.21 16.40 157 28621 196787 110363734
Pain 69.60 16.40 88 28690 954867 109605654
Stoma site pain 68.92 16.40 24 28754 1939 110558582
Therapeutic product effect variable 68.43 16.40 26 28752 2692 110557829
Psychotic disorder 68.31 16.40 75 28703 50862 110509659
Stoma site hypergranulation 67.50 16.40 18 28760 586 110559935
Amyloid related imaging abnormality-oedema/effusion 66.04 16.40 22 28756 1553 110558968
Dementia with Lewy bodies 65.85 16.40 20 28758 1046 110559475
Neuroleptic malignant syndrome 65.58 16.40 61 28717 33998 110526523
Balance disorder 64.75 16.40 112 28666 116448 110444073
Posture abnormal 62.44 16.40 28 28750 4410 110556111
Stoma site reaction 62.31 16.40 16 28762 448 110560073
Wrong technique in product usage process 62.26 16.40 94 28684 87254 110473267
Rheumatoid arthritis 62.18 16.40 4 28774 299609 110260912
Subileus 61.15 16.40 31 28747 6406 110554115
Device dislocation 59.54 16.40 56 28722 31648 110528873
General physical health deterioration 59.10 16.40 243 28535 425052 110135469
Infusion related reaction 57.90 16.40 14 28764 381148 110179373
Amyloid related imaging abnormality-microhaemorrhages and haemosiderin deposits 56.96 16.40 19 28759 1347 110559174
Psychomotor hyperactivity 56.76 16.40 45 28733 20232 110540289
Pleurothotonus 56.14 16.40 22 28756 2476 110558045
Febrile neutropenia 55.87 16.40 8 28770 316759 110243762
Femur fracture 55.38 16.40 63 28715 44406 110516115
Salivary hypersecretion 53.84 16.40 41 28737 17380 110543141
Fibroma 53.79 16.40 17 28761 1015 110559506
Arthropathy 53.76 16.40 6 28772 287516 110273005
Urinary incontinence 52.48 16.40 64 28714 48523 110511998
Stomatitis 52.18 16.40 5 28773 270237 110290284
Application site hypersensitivity 51.66 16.40 13 28765 335 110560186
Sinus bradycardia 51.42 16.40 50 28728 29433 110531088
Eyelid function disorder 50.49 16.40 14 28764 529 110559992
Extrapyramidal disorder 50.43 16.40 49 28729 28818 110531703
Disturbance in attention 50.40 16.40 71 28707 61924 110498597
Headache 50.21 16.40 96 28682 882281 109678240
Marasmus 49.25 16.40 18 28760 1673 110558848
Urinary tract infection 48.95 16.40 191 28587 326091 110234430
Sinusitis 48.94 16.40 9 28769 296679 110263842
Reduced facial expression 48.09 16.40 22 28756 3629 110556892
Rash 47.86 16.40 88 28690 820876 109739645
Screaming 47.81 16.40 24 28754 4857 110555664
Hip fracture 47.55 16.40 52 28726 35099 110525422
Depressed level of consciousness 47.50 16.40 96 28682 112182 110448339
Stoma site odour 46.93 16.40 10 28768 120 110560401
Product administration error 46.80 16.40 53 28725 37164 110523357
Femoral neck fracture 46.57 16.40 33 28745 12534 110547987
Urticaria 45.96 16.40 13 28765 318844 110241677
Stoma site irritation 45.84 16.40 12 28766 363 110560158
Stoma site extravasation 45.50 16.40 12 28766 374 110560147
Joint swelling 44.99 16.40 30 28748 442815 110117706
Stoma site infection 44.58 16.40 17 28761 1778 110558743
Urinary retention 44.09 16.40 71 28707 69612 110490909
Hypokinesia 43.78 16.40 40 28738 21786 110538735
Application site dermatitis 43.63 16.40 10 28768 171 110560350
Dysstasia 43.24 16.40 48 28730 32938 110527583
Unresponsive to stimuli 43.13 16.40 67 28711 63723 110496798
Device issue 43.12 16.40 49 28729 34486 110526035
Gastrointestinal sounds abnormal 43.08 16.40 24 28754 5994 110554527
Dehydration 43.04 16.40 165 28613 279346 110281175
Intentional product use issue 42.02 16.40 7 28771 247899 110312622
Motor dysfunction 41.84 16.40 41 28737 24365 110536156
Miosis 41.60 16.40 39 28739 21944 110538577
Faecaloma 41.54 16.40 33 28745 14875 110545646
Neutropenia 41.37 16.40 23 28755 374597 110185924
Swelling 41.06 16.40 20 28758 351021 110209500
Application site reaction 40.23 16.40 13 28765 834 110559687
Contraindicated product administered 39.95 16.40 8 28770 248259 110312262
Application site irritation 39.83 16.40 16 28762 1921 110558600
Hand deformity 39.75 16.40 5 28773 218501 110342020
Decreased appetite 39.61 16.40 235 28543 475611 110084910
Hepatic enzyme increased 39.52 16.40 17 28761 320875 110239646
Feeding disorder 38.71 16.40 37 28741 21325 110539196
Abdominal discomfort 38.26 16.40 28 28750 393830 110166691
Intentional medical device removal by patient 37.77 16.40 11 28767 497 110560024
Accessory cardiac pathway 37.28 16.40 6 28772 11 110560510
Hyporesponsive to stimuli 36.94 16.40 17 28761 2843 110557678
Hangover 35.88 16.40 16 28762 2486 110558035
Wheezing 35.69 16.40 11 28767 255219 110305302
Joint warmth 35.36 16.40 15 28763 2067 110558454
Injection site pain 35.12 16.40 3 28775 177919 110382602
Wound 34.83 16.40 9 28769 234428 110326093
Concomitant disease aggravated 34.81 16.40 31 28747 16333 110544188
Anger 34.59 16.40 33 28745 18974 110541547
Clavicle fracture 34.58 16.40 20 28758 5364 110555157
Tobacco interaction 34.57 16.40 8 28770 143 110560378
Hypersomnia 33.66 16.40 39 28739 28022 110532499
Fibromyalgia 33.42 16.40 3 28775 170906 110389615
Dyspnoea 33.09 16.40 162 28616 1106710 109453811
Apathy 33.04 16.40 30 28748 16209 110544312
Cogwheel rigidity 32.79 16.40 17 28761 3681 110556840
Parkinson's disease 32.64 16.40 13 28765 1526 110558995
Pemphigus 32.33 16.40 8 28770 214562 110345959
Aphasia 31.85 16.40 56 28722 58941 110501580
Hypersensitivity 31.72 16.40 35 28743 403963 110156558
Unevaluable event 31.69 16.40 56 28722 59171 110501350
Inflammation 31.56 16.40 6 28772 193232 110367289
Altered state of consciousness 31.50 16.40 55 28723 57571 110502950
Lower respiratory tract infection 31.36 16.40 12 28766 243094 110317427
Resting tremor 31.22 16.40 13 28765 1710 110558811
Sputum increased 30.79 16.40 19 28759 5732 110554789
Urinary casts present 30.63 16.40 7 28771 118 110560403
Treatment failure 30.62 16.40 17 28761 277217 110283304
Neuropathy peripheral 30.52 16.40 5 28773 179272 110381249
Back pain 30.40 16.40 31 28747 370965 110189556
Myalgia 30.35 16.40 10 28768 222371 110338150
Tension 30.34 16.40 18 28760 5060 110555461
Cerebellar atrophy 29.87 16.40 12 28766 1441 110559080
Hypophagia 29.78 16.40 51 28727 52575 110507946
Blister 29.70 16.40 11 28767 227365 110333156
Parkinsonian gait 29.70 16.40 11 28767 1061 110559460
Stoma site discomfort 29.70 16.40 7 28771 136 110560385
Blood cholesterol increased 29.63 16.40 6 28772 184779 110375742
Malignant neoplasm progression 29.42 16.40 5 28773 174562 110385959
Device kink 29.06 16.40 13 28765 2036 110558485
Movement disorder 28.56 16.40 41 28737 36363 110524158
Impaired healing 28.37 16.40 8 28770 196709 110363812
Incorrect product dosage form administered 28.20 16.40 8 28770 329 110560192
Cough 28.19 16.40 48 28730 461593 110098928
Ileus 27.69 16.40 37 28741 30692 110529829
Product prescribing error 26.78 16.40 48 28730 51283 110509238
Migraine 26.65 16.40 6 28772 171646 110388875
Arrhythmia 26.50 16.40 57 28721 69518 110491003
Atrioventricular block 26.44 16.40 27 28751 16850 110543671
Mental impairment 26.38 16.40 31 28747 22608 110537913
Hypoaesthesia 26.03 16.40 26 28752 314197 110246324
Psoriasis 25.96 16.40 3 28775 139990 110420531
Type 2 diabetes mellitus 25.95 16.40 7 28771 177225 110383296
Product administration interrupted 25.23 16.40 22 28756 11270 110549251
Choking 25.18 16.40 25 28753 15085 110545436
Completed suicide 25.17 16.40 16 28762 242365 110318156
Fluid intake reduced 25.09 16.40 18 28760 6968 110553553
Medical device site injury 24.97 16.40 4 28774 7 110560514
Agnosia 24.83 16.40 7 28771 281 110560240
Device connection issue 24.40 16.40 10 28768 1264 110559257
Weight increased 24.38 16.40 45 28733 419599 110140922
Atrioventricular block complete 24.24 16.40 28 28750 20054 110540467
Platelet count decreased 24.22 16.40 15 28763 230428 110330093
Stoma site induration 24.21 16.40 5 28773 51 110560470
Discomfort 23.95 16.40 13 28765 214694 110345827
Liver injury 23.87 16.40 5 28773 150408 110410113
Anal incontinence 23.82 16.40 29 28749 21935 110538586
Nightmare 23.77 16.40 39 28739 38824 110521697
Drug interaction 23.70 16.40 216 28562 499967 110060554
Terminal state 23.63 16.40 16 28762 5651 110554870
Medical device site dryness 23.46 16.40 5 28773 60 110560461
Oesophageal dilatation 23.43 16.40 8 28770 609 110559912
Aspiration 23.39 16.40 34 28744 30499 110530022
Abdominal tenderness 23.38 16.40 22 28756 12435 110548086
Ill-defined disorder 23.33 16.40 6 28772 156847 110403674
Bradyarrhythmia 23.16 16.40 15 28763 4919 110555602
Stoma complication 22.72 16.40 9 28769 1042 110559479
White blood cell count decreased 22.66 16.40 16 28762 229374 110331147
Condition aggravated 22.58 16.40 291 28487 734545 109825976
Fracture 22.57 16.40 30 28748 24758 110535763
Nasopharyngitis 22.28 16.40 43 28735 394318 110166203
Dizziness postural 22.21 16.40 23 28755 14586 110545935
Mobility decreased 22.18 16.40 121 28657 237301 110323220
Circulatory collapse 22.16 16.40 40 28738 42953 110517568
Basal ganglia infarction 22.01 16.40 8 28770 732 110559789
Pain in extremity 21.96 16.40 60 28718 487058 110073463
Toxicity to various agents 21.81 16.40 59 28719 480496 110080025
Hypotension 21.74 16.40 220 28558 523629 110036892
Hallucinations, mixed 21.60 16.40 18 28760 8675 110551846
Dyschezia 21.46 16.40 13 28765 3794 110556727
Myoclonus 21.39 16.40 34 28744 32964 110527557
Peripheral swelling 21.18 16.40 46 28732 403988 110156533
Hallucination, auditory 21.10 16.40 30 28748 26367 110534154
Sedation 20.94 16.40 52 28726 69631 110490890
Senile dementia 20.87 16.40 6 28772 259 110560262
Torticollis 20.78 16.40 12 28766 3209 110557312
Therapeutic product effect decreased 20.48 16.40 20 28758 244296 110316225
Oropharyngeal pain 20.46 16.40 5 28773 135271 110425250
Drooling 20.31 16.40 16 28762 7123 110553398
Subdural haematoma 20.19 16.40 35 28743 36419 110524102
Incoherent 20.13 16.40 17 28761 8341 110552180
Skin irritation 20.11 16.40 23 28755 16296 110544225
Psychotic behaviour 20.08 16.40 9 28769 1416 110559105
Illusion 20.05 16.40 10 28768 1997 110558524
Dizziness 20.00 16.40 273 28505 697920 109862601
White blood cell count increased 19.95 16.40 63 28715 96779 110463742
Gastrooesophageal reflux disease 19.92 16.40 11 28767 179965 110380556
Hallucination, olfactory 19.85 16.40 7 28771 587 110559934
Cholinesterase inhibition 19.68 16.40 3 28775 3 110560518
Cerebral haemorrhage 19.01 16.40 48 28730 64920 110495601
Middle insomnia 18.96 16.40 25 28753 20477 110540044
Anxiety 18.94 16.40 154 28624 344924 110215597
Abdominal pain upper 18.92 16.40 39 28739 349072 110211449
Psychotic symptom 18.75 16.40 12 28766 3855 110556666
Nonspecific reaction 18.63 16.40 11 28767 3063 110557458
Medical device site hyperaesthesia 18.47 16.40 3 28775 6 110560515
Atrioventricular block second degree 18.40 16.40 16 28762 8165 110552356
Stoma site haemorrhage 18.37 16.40 10 28768 2388 110558133
Night sweats 18.32 16.40 6 28772 133977 110426544
Facial bones fracture 18.29 16.40 13 28765 4958 110555563
Embedded device 18.29 16.40 12 28766 4021 110556500
Drug dispensed to wrong patient 18.26 16.40 7 28771 742 110559779
Suspiciousness 18.10 16.40 7 28771 760 110559761
Fear 18.01 16.40 26 28752 23167 110537354
Pruritus 17.97 16.40 84 28694 581476 109979045
Libido increased 17.83 16.40 10 28768 2529 110557992
Oedema 17.82 16.40 17 28761 209959 110350562
Musculoskeletal pain 17.77 16.40 13 28765 183010 110377511
Vomiting 17.76 16.40 334 28444 910341 109650180
Neuropsychiatric symptoms 17.72 16.40 8 28770 1280 110559241
Lacunar infarction 17.70 16.40 14 28764 6272 110554249
Time perception altered 17.64 16.40 5 28773 205 110560316
Joint range of motion decreased 17.48 16.40 5 28773 121827 110438694
Lack of application site rotation 17.42 16.40 4 28774 69 110560452
Cerebrovascular accident 17.33 16.40 93 28685 181191 110379330
Grimacing 17.25 16.40 7 28771 863 110559658
Poriomania 17.23 16.40 5 28773 223 110560298
Mania 17.17 16.40 24 28754 20772 110539749
Pulmonary fibrosis 17.02 16.40 3 28775 102039 110458482
Initial insomnia 16.97 16.40 17 28761 10372 110550149
Drug intolerance 16.91 16.40 52 28726 406460 110154061
Pyrexia 16.89 16.40 151 28627 898114 109662407
Dementia Alzheimer's type 16.80 16.40 7 28771 922 110559599
Unmasking of previously unidentified disease 16.70 16.40 10 28768 2858 110557663
Food refusal 16.65 16.40 7 28771 943 110559578
Underdose 16.60 16.40 45 28733 63509 110497012

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N06DA03 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTI-DEMENTIA DRUGS
Anticholinesterases
FDA MoA N0000000177 Cholinesterase Inhibitors
MeSH PA D002800 Cholinesterase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018696 Neuroprotective Agents
MeSH PA D020011 Protective Agents
FDA EPC N0000175723 Cholinesterase Inhibitor
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:37733 EC 3.1.1.8 (cholinesterase) inhibitor
CHEBI has role CHEBI:38323 cholinergic drug
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:50514 vasoconstrictor agent

Related Drugs by ATC class:

N06DA Anticholinesterases 5 drugs

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

DiseaseRelationSNOMED_IDDOID
Alzheimer's disease indication 26929004 DOID:10652
Dementia associated with Parkinson's Disease indication 425390006
Diffuse Lewy body disease off-label use 80098002
Moderate to Severe Alzheimer's Type Dementia off-label use
Urinary tract obstruction contraindication 7163005 DOID:5200
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Parkinsonism contraindication 32798002
Sick sinus syndrome contraindication 36083008 DOID:13884
Gastrointestinal ulcer contraindication 40845000
Conduction disorder of the heart contraindication 44808001
Neuromuscular block, function contraindication 55394004
Anorexia nervosa contraindication 56882008 DOID:8689
Diarrhea contraindication 62315008
Gastrointestinal hemorrhage contraindication 74474003
Extrapyramidal disease contraindication 76349003
Weight loss contraindication 89362005
Seizure disorder contraindication 128613002
Asthma contraindication 195967001 DOID:2841
Atrioventricular block contraindication 233917008 DOID:0050820
Vomiting contraindication 422400008
Nausea contraindication 422587007




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.32 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cholinesterase Enzyme INHIBITOR IC50 7.52 CHEMBL IUPHAR
Acetylcholinesterase Enzyme INHIBITOR IC50 7.43 CHEMBL IUPHAR
MAP/microtubule affinity-regulating kinase 4 Kinase IC50 5.17 CHEMBL
Fatty-acid amide hydrolase 1 Enzyme IC50 4.85 CHEMBL
Butyrylcholinesterase; Protein Bche Enzyme IC50 6.46 CHEMBL
Acetylcholinesterase Enzyme IC50 5.74 CHEMBL
Acetylcholinesterase Enzyme IC50 5.38 CHEMBL
Acetylcholinesterase Enzyme IC50 6.21 CHEMBL
Cholinesterase Enzyme IC50 5.80 CHEMBL
Butyrylcholinesterase Enzyme IC50 6.80 CHEMBL
Cholinesterase Enzyme IC50 6.08 CHEMBL
Acetylcholine receptor subunit epsilon Ion channel IC50 5.05 CHEMBL
Cholinesterase Enzyme IC50 5.20 CHEMBL
Acetylcholinesterase Enzyme IC50 5.95 CHEMBL

External reference:

IDSource
4021219 VUID
N0000148665 NUI
D03822 KEGG_DRUG
129101-54-8 SECONDARY_CAS_RN
4021219 VANDF
4021220 VANDF
C0649350 UMLSCUI
CHEBI:8874 CHEBI
CHEMBL636 ChEMBL_ID
CHEMBL1201092 ChEMBL_ID
DB00989 DRUGBANK_ID
D000068836 MESH_DESCRIPTOR_UI
77991 PUBCHEM_CID
6602 IUPHAR_LIGAND_ID
7562 INN_ID
PKI06M3IW0 UNII
183379 RXNORM
174208 MMSL
23978 MMSL
31947 MMSL
79573 MMSL
8887 MMSL
d04537 MMSL
007559 NDDF
007560 NDDF
126131008 SNOMEDCT_US
323368009 SNOMEDCT_US
395868008 SNOMEDCT_US
PKI06M3IW0 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0501 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL NDA 28 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0502 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL NDA 28 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0503 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL NDA 28 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9070 PATCH 4.60 mg TRANSDERMAL ANDA 28 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9071 PATCH 9.50 mg TRANSDERMAL ANDA 28 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9072 PATCH 13.30 mg TRANSDERMAL ANDA 28 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0781-7304 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL NDA authorized generic 27 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0781-7309 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL NDA authorized generic 27 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0781-7313 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL NDA authorized generic 27 sections
Rivastigmine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7107 CAPSULE 1.50 mg ORAL ANDA 25 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 16714-115 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL ANDA 25 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 16714-116 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL ANDA 25 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 16714-117 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL ANDA 25 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 21695-357 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL NDA 16 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 27241-090 CAPSULE 1.50 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 27241-091 CAPSULE 3 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 27241-092 CAPSULE 4.50 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 27241-093 CAPSULE 6 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 33342-089 CAPSULE 1.50 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 33342-090 CAPSULE 3 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 33342-091 CAPSULE 4.50 mg ORAL ANDA 25 sections
RIVASTIGMINE TARTRATE Human Prescription Drug Label 1 33342-092 CAPSULE 6 mg ORAL ANDA 25 sections
Rivastigmine Tartrate Human Prescription Drug Label 1 46708-063 CAPSULE 1.50 mg ORAL ANDA 26 sections
Rivastigmine Tartrate Human Prescription Drug Label 1 46708-064 CAPSULE 3 mg ORAL ANDA 26 sections
Rivastigmine Tartrate Human Prescription Drug Label 1 46708-065 CAPSULE 4.50 mg ORAL ANDA 26 sections
Rivastigmine Tartrate Human Prescription Drug Label 1 46708-066 CAPSULE 6 mg ORAL ANDA 26 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 51956-0001 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL ANDA 25 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 51956-0002 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL ANDA 25 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 51956-0003 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL ANDA 25 sections
Rivastigmine Transdermal System HUMAN PRESCRIPTION DRUG LABEL 1 51991-897 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL ANDA 31 sections