rivastigmine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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 440.17 17.72 129 18185 4263 50582547
Application site erythema 367.12 17.72 113 18201 4425 50582385
Hallucination 319.65 17.72 203 18111 46454 50540356
Application site pruritus 272.16 17.72 86 18228 3673 50583137
Fall 260.49 17.72 447 17867 334485 50252325
Dementia 256.02 17.72 122 18192 15875 50570935
Death 214.07 17.72 404 17910 324975 50261835
Confusional state 186.33 17.72 279 18035 185649 50401161
Agitation 160.98 17.72 142 18172 53242 50533568
Application site rash 158.55 17.72 51 18263 2306 50584504
Hallucination, visual 149.14 17.72 86 18228 16496 50570314
On and off phenomenon 143.74 17.72 42 18272 1370 50585440
Disorientation 135.07 17.72 108 18206 35376 50551434
Aggression 129.99 17.72 86 18228 21030 50565780
Stoma site discharge 117.00 17.72 35 18279 1240 50585570
Application site hypersensitivity 114.44 17.72 24 18290 184 50586626
Cognitive disorder 112.73 17.72 107 18207 44016 50542794
Blood cholinesterase decreased 110.12 17.72 21 18293 92 50586718
Delusion 109.08 17.72 60 18254 10509 50576301
Abnormal behaviour 106.54 17.72 74 18240 19584 50567226
Memory impairment 106.09 17.72 137 18177 79223 50507587
Bradykinesia 98.15 17.72 41 18273 3902 50582908
Wrong technique in product usage process 97.34 17.72 110 18204 55400 50531410
Bradycardia 87.30 17.72 112 18202 64314 50522496
Product administration error 85.88 17.72 65 18249 19634 50567176
Dyskinesia 85.70 17.72 75 18239 27786 50559024
Freezing phenomenon 85.14 17.72 26 18288 989 50585821
Stoma site erythema 84.11 17.72 25 18289 866 50585944
Arthralgia 82.65 17.72 28 18286 438674 50148136
Application site reaction 77.30 17.72 22 18292 652 50586158
Application site irritation 77.09 17.72 27 18287 1588 50585222
Mini mental status examination abnormal 76.17 17.72 11 18303 0 50586810
Cerebral atrophy 70.25 17.72 34 18280 4567 50582243
Syncope 69.91 17.72 130 18184 102872 50483938
Cholinergic syndrome 69.79 17.72 18 18296 364 50586446
Pain 69.01 17.72 65 18249 578838 50007972
Restlessness 68.02 17.72 63 18251 25110 50561700
Lack of application site rotation 66.63 17.72 10 18304 3 50586807
Dysphagia 64.47 17.72 107 18207 77411 50509399
Alopecia 64.09 17.72 7 18307 245040 50341770
Tremor 63.45 17.72 133 18181 114770 50472040
Muscle rigidity 62.83 17.72 41 18273 9788 50577022
Vomiting 62.06 17.72 329 17985 460429 50126381
Rheumatoid arthritis 60.85 17.72 3 18311 202547 50384263
Skin irritation 58.81 17.72 36 18278 7691 50579119
Speech disorder 58.17 17.72 68 18246 35480 50551330
Delirium 57.47 17.72 70 18244 38122 50548688
Hyperkinesia 56.98 17.72 21 18293 1431 50585379
Drug hypersensitivity 56.79 17.72 11 18303 250999 50335811
Stoma site irritation 55.85 17.72 13 18301 168 50586642
Loss of consciousness 55.53 17.72 119 18195 104234 50482576
Cerebrovascular accident 53.90 17.72 111 18203 94569 50492241
Femur fracture 53.68 17.72 67 18247 37397 50549413
Joint swelling 52.92 17.72 12 18302 245274 50341536
Akinesia 52.70 17.72 20 18294 1479 50585331
Pneumonia aspiration 51.88 17.72 60 18254 30944 50555866
Dementia with Lewy bodies 49.85 17.72 13 18301 275 50586535
Somnolence 49.03 17.72 145 18169 154840 50431970
Marasmus 48.83 17.72 14 18300 426 50586384
Malaise 48.82 17.72 245 18069 335287 50251523
Decreased appetite 48.21 17.72 171 18143 200752 50386058
Gait inability 47.98 17.72 63 18251 36964 50549846
Infusion related reaction 46.53 17.72 4 18310 169553 50417257
Dysstasia 45.07 17.72 43 18271 17776 50569034
Posture abnormal 43.02 17.72 19 18295 2070 50584740
Swelling 42.97 17.72 10 18304 200862 50385948
Femoral neck fracture 42.46 17.72 29 18285 7461 50579349
Gait disturbance 42.45 17.72 135 18179 149870 50436940
Sinusitis 41.82 17.72 6 18308 170552 50416258
General physical health deterioration 41.05 17.72 129 18185 142305 50444505
Product administration interrupted 40.82 17.72 15 18299 1014 50585796
Fatigue 40.48 17.72 127 18187 707474 49879336
Arthropathy 40.04 17.72 5 18309 157901 50428909
Subileus 37.98 17.72 19 18295 2740 50584070
Accessory cardiac pathway 37.91 17.72 6 18308 5 50586805
Dehydration 37.61 17.72 131 18183 152318 50434492
Application site discolouration 37.57 17.72 13 18301 737 50586073
Product prescribing error 37.50 17.72 42 18272 20919 50565891
Dementia Alzheimer's type 37.09 17.72 14 18300 1020 50585790
Stoma site pain 36.71 17.72 13 18301 790 50586020
Abnormal dreams 36.63 17.72 29 18285 9348 50577462
Drug ineffective 35.88 17.72 164 18150 819169 49767641
Hypokinesia 35.78 17.72 32 18282 12185 50574625
Application site dermatitis 35.47 17.72 9 18305 170 50586640
Eating disorder 34.89 17.72 35 18279 15374 50571436
Off label use 34.84 17.72 75 18239 474351 50112459
Application site swelling 34.41 17.72 11 18303 487 50586323
Dyspnoea 34.37 17.72 94 18220 547514 50039296
Completed suicide 33.87 17.72 4 18310 131885 50454925
Concomitant disease aggravated 33.72 17.72 26 18288 8065 50578745
Therapeutic product effect variable 32.84 17.72 13 18301 1077 50585733
Vascular encephalopathy 32.75 17.72 10 18304 380 50586430
Pemphigus 32.51 17.72 3 18311 120163 50466647
Stoma site inflammation 32.33 17.72 10 18304 397 50586413
Fracture 32.31 17.72 35 18279 16798 50570012
Arrhythmia 32.01 17.72 49 18265 33083 50553727
Extrapyramidal disorder 30.90 17.72 29 18285 11741 50575069
Pain in extremity 30.81 17.72 32 18282 272833 50313977
Pleurothotonus 30.61 17.72 13 18301 1288 50585522
Orthostatic hypotension 30.47 17.72 45 18269 29436 50557374
Screaming 28.25 17.72 16 18298 2962 50583848
Neutropenia 26.82 17.72 10 18304 147955 50438855
Nightmare 26.68 17.72 31 18283 16055 50570755
Resting tremor 26.66 17.72 10 18304 716 50586094
Dizziness 26.57 17.72 215 18099 346154 50240656
Balance disorder 26.16 17.72 70 18244 70520 50516290
Back pain 25.75 17.72 25 18289 220005 50366805
Urinary retention 25.67 17.72 39 18275 26151 50560659
Headache 25.43 17.72 96 18218 506439 50080371
Cough 25.35 17.72 30 18284 241234 50345576
Unresponsive to stimuli 25.08 17.72 42 18272 30567 50556243
Parkinson's disease 25.03 17.72 11 18303 1184 50585626
Febrile neutropenia 24.98 17.72 3 18311 97664 50489146
Apparent death 24.90 17.72 11 18303 1199 50585611
Psychotic symptom 24.88 17.72 11 18303 1201 50585609
Stoma site discomfort 24.76 17.72 6 18308 93 50586717
Aphasia 24.56 17.72 40 18274 28454 50558356
Weight decreased 24.37 17.72 150 18164 221095 50365715
Senile dementia 24.26 17.72 7 18307 218 50586592
Dermatitis contact 24.05 17.72 22 18292 8624 50578186
Stomatitis 23.84 17.72 4 18310 101340 50485470
Application site vesicles 23.71 17.72 11 18303 1344 50585466
Agnosia 23.57 17.72 6 18308 115 50586695
Psychotic disorder 23.56 17.72 34 18280 21778 50565032
Parkinsonian gait 23.46 17.72 8 18306 434 50586376
Hip fracture 23.16 17.72 37 18277 25894 50560916
Fibroma 22.96 17.72 9 18305 726 50586084
Product administered at inappropriate site 22.83 17.72 13 18301 2430 50584380
Rash 22.53 17.72 82 18232 437389 50149421
Abdominal discomfort 22.07 17.72 31 18283 231610 50355200
Paraesthesia 22.00 17.72 8 18306 120235 50466575
Parkinsonism 21.71 17.72 21 18293 8826 50577984
Faecaloma 21.57 17.72 19 18295 7089 50579721
Myalgia 21.54 17.72 9 18305 124310 50462500
Arthritis 21.36 17.72 3 18311 86718 50500092
Nasopharyngitis 21.34 17.72 23 18291 192904 50393906
Hypersensitivity 21.30 17.72 28 18286 215133 50371677
Peripheral swelling 21.21 17.72 26 18288 205910 50380900
Incorrect product administration duration 20.87 17.72 21 18293 9254 50577556
Depressed level of consciousness 20.76 17.72 53 18261 51900 50534910
Paranoia 20.71 17.72 22 18292 10326 50576484
Atrioventricular block second degree 20.48 17.72 14 18300 3607 50583203
Neuropathy peripheral 20.31 17.72 5 18309 96752 50490058
Stoma site reaction 20.18 17.72 6 18308 208 50586602
Pyrexia 19.74 17.72 71 18243 380132 50206678
Platelet count decreased 19.65 17.72 6 18308 100720 50486090
Stoma site extravasation 19.12 17.72 6 18308 250 50586560
Psychomotor hyperactivity 19.01 17.72 20 18294 9281 50577529
Medication error 18.97 17.72 41 18273 36063 50550747
Therapeutic product effect decreased 18.96 17.72 13 18301 136037 50450773
Apathy 18.68 17.72 18 18296 7530 50579280
Cerebral haemorrhage 18.14 17.72 34 18280 27018 50559792
Drug interaction 18.12 17.72 129 18185 199492 50387318
Mental impairment 17.98 17.72 22 18292 12022 50574788
Altered state of consciousness 17.86 17.72 30 18284 21880 50564930
Wound 17.79 17.72 8 18306 105786 50481024

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 460.65 17.68 288 15188 44424 29514627
Product adhesion issue 397.54 17.68 102 15374 1369 29557682
Confusional state 277.10 17.68 337 15139 127540 29431511
Application site erythema 260.07 17.68 79 15397 2020 29557031
Aggression 250.31 17.68 181 15295 35360 29523691
Fall 212.52 17.68 352 15124 176826 29382225
Dementia 188.87 17.68 101 15375 11557 29547494
Abnormal behaviour 165.48 17.68 119 15357 23008 29536043
Stoma site discharge 164.44 17.68 46 15430 871 29558180
On and off phenomenon 162.03 17.68 54 15422 1874 29557177
Application site pruritus 161.44 17.68 49 15427 1248 29557803
Freezing phenomenon 158.43 17.68 48 15428 1215 29557836
Agitation 147.67 17.68 157 15319 51147 29507904
Hallucination, visual 125.45 17.68 85 15391 14930 29544121
Stoma site erythema 123.78 17.68 34 15442 600 29558451
Cognitive disorder 120.03 17.68 99 15377 23400 29535651
Death 118.23 17.68 419 15057 341665 29217386
Bradykinesia 114.67 17.68 49 15427 3398 29555653
Gait disturbance 114.53 17.68 165 15311 73184 29485867
Application site rash 104.31 17.68 31 15445 733 29558318
Somnolence 102.02 17.68 179 15297 93776 29465275
General physical health deterioration 88.02 17.68 177 15299 102680 29456371
Muscle rigidity 87.59 17.68 57 15419 9354 29549697
Fibroma 85.22 17.68 21 15455 236 29558815
Blood cholinesterase decreased 84.07 17.68 18 15458 101 29558950
Dyskinesia 83.11 17.68 75 15401 19986 29539065
Disorientation 82.49 17.68 89 15387 29426 29529625
Akinesia 82.12 17.68 33 15443 1957 29557094
Pneumonia aspiration 77.80 17.68 96 15380 36641 29522410
Device dislocation 75.47 17.68 40 15436 4487 29554564
Dementia with Lewy bodies 74.70 17.68 23 15453 615 29558436
Memory impairment 71.97 17.68 92 15384 36378 29522673
Restlessness 67.59 17.68 70 15406 22075 29536976
Mobility decreased 65.56 17.68 74 15402 25706 29533345
Delusion 65.20 17.68 51 15425 11165 29547886
Stoma site reaction 62.82 17.68 15 15461 146 29558905
Speech disorder 58.94 17.68 67 15409 23449 29535602
Dysphagia 58.67 17.68 104 15372 54822 29504229
Stoma site inflammation 56.64 17.68 17 15459 416 29558635
Delirium 54.75 17.68 84 15392 39313 29519738
Application site irritation 54.23 17.68 18 15458 616 29558435
Reduced facial expression 52.33 17.68 18 15458 688 29558363
Gait inability 50.60 17.68 55 15421 18320 29540731
Arthralgia 49.78 17.68 7 15469 139610 29419441
Parkinson's disease 47.43 17.68 20 15456 1341 29557710
Sinus bradycardia 47.29 17.68 43 15433 11560 29547491
Paranoia 47.06 17.68 40 15436 9837 29549214
Febrile neutropenia 46.91 17.68 3 15473 112237 29446814
Tremor 45.24 17.68 111 15365 73427 29485624
Prescribed underdose 42.24 17.68 34 15442 7752 29551299
Abnormal dreams 41.37 17.68 32 15444 6888 29552163
Urinary incontinence 41.36 17.68 47 15429 16434 29542617
Hyperkinesia 41.18 17.68 19 15457 1580 29557471
Syncope 41.01 17.68 114 15362 81257 29477794
Neutropenia 39.73 17.68 10 15466 131701 29427350
Application site discolouration 39.08 17.68 11 15465 213 29558838
Stoma site pain 37.57 17.68 13 15463 506 29558545
Product administration error 36.23 17.68 41 15435 14269 29544782
Hangover 36.20 17.68 15 15461 962 29558089
Application site hypersensitivity 35.39 17.68 9 15467 116 29558935
Stoma site extravasation 34.58 17.68 8 15468 67 29558984
Marasmus 34.29 17.68 12 15464 483 29558568
Bradycardia 34.10 17.68 93 15383 65536 29493515
Device kink 33.72 17.68 11 15465 356 29558695
Stoma site infection 33.72 17.68 13 15463 690 29558361
Mini mental status examination abnormal 33.46 17.68 6 15470 10 29559041
Stoma site hypergranulation 33.07 17.68 9 15467 153 29558898
Psychotic disorder 31.99 17.68 46 15430 20308 29538743
Balance disorder 31.75 17.68 63 15413 36107 29522944
Acute kidney injury 31.30 17.68 57 15419 265210 29293841
Sleep disorder 31.09 17.68 50 15426 24336 29534715
Intentional medical device removal by patient 30.76 17.68 9 15467 201 29558850
Nonspecific reaction 30.65 17.68 14 15462 1137 29557914
Urinary tract infection 30.36 17.68 95 15381 72259 29486792
Motor dysfunction 30.28 17.68 25 15451 5905 29553146
Application site reaction 28.54 17.68 10 15466 404 29558647
Malaise 28.39 17.68 161 15315 159441 29399610
White blood cell count decreased 27.84 17.68 5 15471 83357 29475694
Parkinsonism 27.77 17.68 26 15450 7252 29551799
Condition aggravated 26.95 17.68 149 15327 146146 29412905
Therapeutic product effect variable 26.88 17.68 15 15461 1862 29557189
Tension 26.61 17.68 15 15461 1898 29557153
Screaming 26.33 17.68 13 15463 1257 29557794
Dyspnoea 26.11 17.68 86 15390 326646 29232405
Application site vesicles 25.91 17.68 10 15466 532 29558519
Salivary hypersecretion 25.49 17.68 25 15451 7384 29551667
Hypokinesia 25.08 17.68 25 15451 7529 29551522
Disturbance in attention 24.71 17.68 42 15434 21382 29537669
Loss of consciousness 24.67 17.68 90 15386 73966 29485085
Stoma site odour 24.00 17.68 5 15471 24 29559027
Miosis 23.85 17.68 25 15451 7984 29551067
Pain 23.81 17.68 33 15443 171399 29387652
Parkinsonian gait 23.69 17.68 9 15467 459 29558592
Myalgia 23.53 17.68 5 15471 74014 29485037
Neuroleptic malignant syndrome 23.21 17.68 35 15441 16113 29542938
Dysstasia 23.16 17.68 28 15448 10446 29548605
Platelet count decreased 23.13 17.68 13 15463 104659 29454392
Orthostatic hypotension 23.05 17.68 42 15434 22587 29536464
Incorrect product administration duration 22.67 17.68 18 15458 4023 29555028
Aphasia 22.63 17.68 38 15438 19160 29539891
Hypersomnia 22.57 17.68 28 15448 10726 29548325
Pancytopenia 22.01 17.68 8 15468 83160 29475891
Underdose 21.92 17.68 29 15447 11840 29547211
Apathy 21.56 17.68 21 15455 6150 29552901
Off label use 21.47 17.68 83 15393 300717 29258334
Concomitant disease progression 21.23 17.68 14 15462 2347 29556704
Drug dispensed to wrong patient 20.34 17.68 7 15469 268 29558783
Oesophageal dilatation 20.30 17.68 6 15470 139 29558912
Skin irritation 19.09 17.68 17 15459 4444 29554607
Headache 19.08 17.68 39 15437 173968 29385083
Toxicity to various agents 18.97 17.68 39 15437 173622 29385429
Urinary retention 18.38 17.68 47 15429 31851 29527200
Back pain 18.25 17.68 16 15460 102268 29456783
Psychomotor hyperactivity 18.23 17.68 22 15454 8191 29550860
Dyschezia 18.21 17.68 10 15466 1203 29557848
Wrong technique in product usage process 17.79 17.68 46 15430 31382 29527669

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 561.62 16.11 337 22185 72451 64403759
Fall 363.27 16.11 574 21948 416252 64059958
Confusional state 329.07 16.11 429 22093 260715 64215495
Dementia 247.05 16.11 128 22394 20638 64455572
Aggression 223.59 16.11 160 22362 46072 64430138
Hallucination, visual 219.79 16.11 131 22391 27703 64448507
On and off phenomenon 215.65 16.11 65 22457 2454 64473756
Application site erythema 194.62 16.11 70 22452 4619 64471591
Stoma site discharge 186.28 16.11 53 22469 1629 64474581
Blood cholinesterase decreased 183.44 16.11 36 22486 197 64476013
Freezing phenomenon 181.56 16.11 51 22471 1495 64474715
Agitation 181.33 16.11 187 22335 88180 64388030
Product adhesion issue 174.71 16.11 55 22467 2404 64473806
Cognitive disorder 167.48 16.11 145 22377 54942 64421268
Bradykinesia 154.84 16.11 65 22457 6495 64469715
Abnormal behaviour 148.08 16.11 110 22412 33512 64442698
Application site pruritus 147.50 16.11 53 22469 3486 64472724
Delusion 140.14 16.11 84 22438 17930 64458280
Stoma site erythema 132.53 16.11 38 22484 1201 64475009
Disorientation 128.88 16.11 126 22396 55702 64420508
Akinesia 116.73 16.11 43 22479 3036 64473174
Death 114.57 16.11 399 22123 482306 63993904
Dyskinesia 114.30 16.11 101 22421 39287 64436923
Somnolence 112.84 16.11 231 22291 203414 64272796
Pneumonia aspiration 111.82 16.11 120 22402 59151 64417059
Gait disturbance 102.18 16.11 201 22321 171954 64304256
Application site rash 95.71 16.11 33 22489 1921 64474289
Restlessness 86.62 16.11 87 22435 39698 64436512
Delirium 85.65 16.11 113 22409 69081 64407129
Arthralgia 82.48 16.11 26 22496 442234 64033976
General physical health deterioration 81.99 16.11 204 22318 204221 64271989
Bradycardia 77.43 16.11 144 22378 118075 64358135
Muscle rigidity 76.53 16.11 57 22465 17416 64458794
Cholinergic syndrome 73.21 16.11 22 22500 821 64475389
Mini mental status examination abnormal 71.78 16.11 11 22511 6 64476204
Dysphagia 71.07 16.11 131 22391 106681 64369529
Syncope 70.35 16.11 164 22358 157471 64318739
Tremor 69.22 16.11 157 22365 148073 64328137
Stoma site inflammation 67.69 16.11 19 22503 555 64475655
Memory impairment 65.91 16.11 112 22410 85570 64390640
Product administration interrupted 62.72 16.11 21 22501 1117 64475093
Cerebral atrophy 61.96 16.11 36 22486 7249 64468961
Pain 58.92 16.11 64 22458 553447 63922763
Loss of consciousness 57.27 16.11 146 22376 148219 64327991
Marasmus 55.82 16.11 18 22504 850 64475360
Paranoia 55.72 16.11 46 22476 16306 64459904
Drug hypersensitivity 54.16 16.11 9 22513 237806 64238404
Speech disorder 52.20 16.11 74 22448 48367 64427843
Pleurothotonus 51.62 16.11 22 22500 2280 64473930
Therapeutic product effect variable 51.60 16.11 20 22502 1624 64474586
Wrong technique in product usage process 51.37 16.11 86 22436 64888 64411322
Abnormal dreams 50.37 16.11 36 22486 10320 64465890
Application site hypersensitivity 50.31 16.11 13 22509 275 64475935
Hyperkinesia 49.49 16.11 22 22500 2524 64473686
Device dislocation 49.21 16.11 48 22474 21130 64455080
Febrile neutropenia 47.74 16.11 5 22517 187652 64288558
Dementia with Lewy bodies 46.86 16.11 15 22507 692 64475518
Rheumatoid arthritis 45.58 16.11 3 22519 164291 64311919
Orthostatic hypotension 45.42 16.11 68 22454 46670 64429540
Stoma site extravasation 45.04 16.11 12 22510 287 64475923
Stoma site irritation 43.84 16.11 11 22511 206 64476004
Stoma site pain 43.60 16.11 16 22506 1117 64475093
Psychotic disorder 43.58 16.11 57 22465 34521 64441689
Alopecia 43.23 16.11 4 22518 165686 64310524
Sinus bradycardia 42.52 16.11 46 22476 22847 64453363
Product administration error 41.93 16.11 50 22472 27593 64448617
Stoma site hypergranulation 41.70 16.11 12 22510 384 64475826
Balance disorder 41.50 16.11 91 22431 83835 64392375
Neuroleptic malignant syndrome 40.89 16.11 47 22475 24949 64451261
Prescribed underdose 40.31 16.11 40 22482 17975 64458235
Infusion related reaction 40.29 16.11 5 22517 164462 64311748
Reduced facial expression 40.24 16.11 18 22504 2095 64474115
Stoma site reaction 39.81 16.11 11 22511 303 64475907
Toxicity to various agents 39.76 16.11 41 22481 363472 64112738
Extrapyramidal disorder 39.35 16.11 41 22481 19511 64456699
Fibroma 39.11 16.11 13 22509 676 64475534
Gait inability 38.85 16.11 60 22462 42308 64433902
Completed suicide 38.65 16.11 15 22507 224399 64251811
Urinary incontinence 38.61 16.11 55 22467 36096 64440114
Application site irritation 38.47 16.11 16 22506 1560 64474650
Neutropenia 38.11 16.11 18 22504 239606 64236604
Stoma site odour 37.59 16.11 8 22514 69 64476141
Accessory cardiac pathway 37.13 16.11 6 22516 7 64476203
Joint swelling 36.11 16.11 15 22507 215367 64260843
Parkinsonism 36.09 16.11 34 22488 14339 64461871
Application site dermatitis 35.50 16.11 9 22513 176 64476034
Dysstasia 35.22 16.11 42 22480 23173 64453037
Headache 34.84 16.11 84 22438 529383 63946827
Urinary retention 34.79 16.11 62 22460 49139 64427071
Dyspnoea 34.46 16.11 132 22390 718542 63757668
Concomitant disease aggravated 34.27 16.11 30 22492 11512 64464698
Screaming 34.22 16.11 19 22503 3510 64472700
Decreased appetite 33.77 16.11 190 22332 281099 64195111
Hypokinesia 33.76 16.11 35 22487 16561 64459649
Femur fracture 33.64 16.11 50 22472 34085 64442125
Urinary tract infection 32.98 16.11 164 22358 231432 64244778
Miosis 32.58 16.11 31 22491 13235 64462975
Back pain 32.44 16.11 24 22498 250147 64226063
Hangover 32.44 16.11 15 22507 1886 64474324
Posture abnormal 32.10 16.11 18 22504 3388 64472822
Stoma site infection 31.71 16.11 13 22509 1222 64474988
Dehydration 31.21 16.11 154 22368 216609 64259601
Altered state of consciousness 31.06 16.11 51 22471 37851 64438359
Femoral neck fracture 30.68 16.11 25 22497 8699 64467511
Subileus 30.61 16.11 20 22502 4957 64471253
Hypersomnia 30.46 16.11 36 22486 19681 64456529
Myalgia 30.08 16.11 9 22513 158608 64317602
Stoma site discomfort 29.48 16.11 7 22515 103 64476107
Salivary hypersecretion 29.16 16.11 28 22494 12085 64464125
Arthropathy 28.84 16.11 4 22518 120963 64355247
Malignant neoplasm progression 28.72 16.11 3 22519 112868 64363342
Mobility decreased 28.57 16.11 80 22442 85760 64390450
Psychomotor hyperactivity 28.54 16.11 30 22492 14421 64461789
Parkinson's disease 28.47 16.11 13 22509 1588 64474622
Product prescribing error 28.29 16.11 47 22475 35222 64440988
Sinusitis 28.19 16.11 8 22514 145920 64330290
Disturbance in attention 28.07 16.11 51 22471 41023 64435187
Application site reaction 27.15 16.11 10 22512 705 64475505
Hip fracture 27.15 16.11 40 22482 27059 64449151
Apathy 27.11 16.11 26 22496 11206 64465004
Rash 26.90 16.11 77 22445 458472 64017738
Urticaria 26.79 16.11 9 22513 147308 64328902
Dystonia 26.78 16.11 33 22489 18832 64457378
Intentional medical device removal by patient 26.53 16.11 8 22514 302 64475908
Anger 26.42 16.11 30 22492 15711 64460499
Depressed level of consciousness 26.22 16.11 75 22447 81361 64394849
Pain in extremity 26.05 16.11 41 22481 303044 64173166
Platelet count decreased 26.04 16.11 13 22509 167698 64308512
Drug ineffective 25.75 16.11 180 22342 840067 63636143
Neuropathy peripheral 25.54 16.11 5 22517 117520 64358690
Parkinsonian gait 25.48 16.11 10 22512 839 64475371
Vascular encephalopathy 25.47 16.11 9 22513 563 64475647
Stomatitis 25.27 16.11 4 22518 109601 64366609
Agnosia 25.19 16.11 7 22515 197 64476013
Choking 24.69 16.11 24 22498 10514 64465696
Unresponsive to stimuli 24.18 16.11 54 22468 50339 64425871
Swelling 24.01 16.11 13 22509 160205 64316005
Cough 24.00 16.11 43 22479 302105 64174105
Vomiting 22.84 16.11 293 22229 550824 63925386
Hypersensitivity 22.79 16.11 21 22501 196431 64279779
Aphasia 22.10 16.11 46 22476 40860 64435350
Lack of application site rotation 22.06 16.11 4 22518 13 64476197
White blood cell count decreased 21.97 16.11 14 22508 157823 64318387
Oesophageal dilatation 21.62 16.11 7 22515 335 64475875
Underdose 21.49 16.11 35 22487 25794 64450416
Nightmare 21.04 16.11 31 22491 20962 64455248
Oropharyngeal pain 21.04 16.11 3 22519 88864 64387346
Drug dispensed to wrong patient 20.95 16.11 7 22515 370 64475840
Fracture 20.71 16.11 29 22493 18726 64457484
Fatigue 20.71 16.11 165 22357 748565 63727645
Circulatory collapse 20.70 16.11 40 22482 33692 64442518
Faecaloma 20.66 16.11 21 22501 9707 64466503
Contraindicated product administered 20.66 16.11 6 22516 107823 64368387
Resting tremor 20.58 16.11 10 22512 1404 64474806
Bradyarrhythmia 20.46 16.11 14 22508 3744 64472466
Arrhythmia 20.29 16.11 52 22470 52892 64423318
Off label use 20.11 16.11 134 22388 632672 63843538
Nonspecific reaction 20.01 16.11 11 22511 1992 64474218
Abdominal discomfort 19.41 16.11 21 22501 182301 64293909
Device kink 18.88 16.11 10 22512 1683 64474527
Fluid intake reduced 18.49 16.11 15 22507 5185 64471025
Aspiration 18.48 16.11 26 22496 16859 64459351
Hyporesponsive to stimuli 18.32 16.11 10 22512 1787 64474423
Condition aggravated 18.02 16.11 204 22318 372222 64103988
Skin irritation 18.00 16.11 19 22503 9175 64467035
Mental impairment 17.65 16.11 25 22497 16318 64459892
Atrioventricular block second degree 17.62 16.11 16 22506 6438 64469772
Medical device site hyperaesthesia 17.59 16.11 3 22519 6 64476204
Hypophagia 17.42 16.11 41 22481 39546 64436664
Feeding disorder 17.34 16.11 22 22500 12927 64463283
Arthritis 17.32 16.11 4 22518 83810 64392400
Paraesthesia 17.30 16.11 13 22509 134509 64341701
Medical device site injury 17.27 16.11 3 22519 7 64476203
Movement disorder 17.22 16.11 29 22493 21971 64454239
Grimacing 17.08 16.11 7 22515 658 64475552
Intentional product use issue 17.03 16.11 6 22516 95358 64380852
Psychotic symptom 16.70 16.11 10 22512 2128 64474082
Haematuria traumatic 16.68 16.11 5 22517 185 64476025
Hallucinations, mixed 16.51 16.11 15 22507 6037 64470173
Dyspnoea exertional 16.31 16.11 3 22519 73727 64402483
Incoherent 16.28 16.11 16 22506 7102 64469108
Epilepsy 16.16 16.11 36 22486 33495 64442715

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 D002491 Central Nervous System Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D002800 Cholinesterase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018696 Neuroprotective Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:37733 EC 3.1.1.8 inhibitor
CHEBI has role CHEBI:38323 cholinergic drugs
CHEBI has role CHEBI:63726 neuroprotective agents
FDA EPC N0000175723 Cholinesterase Inhibitor

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
Acetylcholinesterase Enzyme INHIBITOR IC50 7.43 CHEMBL IUPHAR
Cholinesterase Enzyme INHIBITOR IC50 7.52 CHEMBL IUPHAR
Acetylcholinesterase Enzyme IC50 5.95 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

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
DB00989 DRUGBANK_ID
CHEMBL215645 ChEMBL_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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0501 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL NDA 30 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0501 PATCH, EXTENDED RELEASE 4.60 mg TRANSDERMAL NDA 30 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0502 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL NDA 30 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0502 PATCH, EXTENDED RELEASE 9.50 mg TRANSDERMAL NDA 30 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0503 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL NDA 30 sections
Exelon HUMAN PRESCRIPTION DRUG LABEL 1 0078-0503 PATCH, EXTENDED RELEASE 13.30 mg TRANSDERMAL NDA 30 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9070 PATCH 4.60 mg TRANSDERMAL ANDA 27 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9071 PATCH 9.50 mg TRANSDERMAL ANDA 27 sections
Rivastigmine HUMAN PRESCRIPTION DRUG LABEL 1 0378-9072 PATCH 13.30 mg TRANSDERMAL ANDA 27 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 0904-6587 CAPSULE 1.50 mg ORAL ANDA 24 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