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 452.58 17.99 129 19269 4590 63465034
Application site erythema 378.90 17.99 113 19285 4722 63464902
Hallucination 346.40 17.99 213 19185 54604 63415020
Dementia 284.83 17.99 131 19267 18663 63450961
Application site pruritus 281.57 17.99 86 19312 3898 63465726
Fall 280.14 17.99 459 18939 391875 63077749
Death 235.25 17.99 414 18984 373967 63095657
On and off phenomenon 193.29 17.99 54 19344 1781 63467843
Agitation 188.85 17.99 152 19246 59605 63410019
Confusional state 186.59 17.99 290 19108 236090 63233534
Hallucination, visual 177.95 17.99 96 19302 19202 63450422
Application site rash 164.13 17.99 51 19347 2447 63467177
Disorientation 163.54 17.99 118 19280 39334 63430290
Stoma site discharge 154.59 17.99 44 19354 1554 63468070
Aggression 144.93 17.99 90 19308 23408 63446216
Freezing phenomenon 127.45 17.99 36 19362 1236 63468388
Bradykinesia 120.77 17.99 49 19349 5139 63464485
Stoma site erythema 119.12 17.99 34 19364 1213 63468411
Cognitive disorder 117.98 17.99 113 19285 55702 63413922
Blood cholinesterase decreased 117.71 17.99 22 19376 104 63469520
Application site hypersensitivity 114.77 17.99 24 19374 219 63469405
Delusion 114.18 17.99 61 19337 11956 63457668
Abnormal behaviour 112.13 17.99 74 19324 21352 63448272
Dyskinesia 110.91 17.99 86 19312 31916 63437708
Wrong technique in product usage process 107.47 17.99 113 19285 62227 63407397
Memory impairment 106.94 17.99 145 19253 104113 63365511
Bradycardia 105.86 17.99 121 19277 73106 63396518
Arthralgia 91.86 17.99 30 19368 569680 62899944
Product administration error 90.52 17.99 66 19332 22331 63447293
Muscle rigidity 86.34 17.99 50 19348 11450 63458174
Syncope 82.74 17.99 137 19261 117248 63352376
Restlessness 82.69 17.99 70 19328 29383 63440241
Pain 80.88 17.99 65 19333 740563 62729061
Application site irritation 79.45 17.99 27 19371 1723 63467901
Application site reaction 78.66 17.99 22 19376 728 63468896
Tremor 78.42 17.99 143 19255 132096 63337528
Mini mental status examination abnormal 78.03 17.99 11 19387 0 63469624
Alopecia 77.54 17.99 7 19391 337529 63132095
Dysphagia 77.19 17.99 114 19284 88471 63381153
Cholinergic syndrome 76.95 17.99 20 19378 498 63469126
Cerebral atrophy 75.72 17.99 35 19363 5031 63464593
Lack of application site rotation 68.32 17.99 10 19388 3 63469621
Speech disorder 65.32 17.99 71 19327 40558 63429066
Rheumatoid arthritis 64.94 17.99 3 19395 253816 63215808
Hyperkinesia 64.66 17.99 23 19375 1681 63467943
Skin irritation 64.35 17.99 39 19359 9702 63459922
Delirium 63.87 17.99 78 19320 50463 63419161
Vomiting 63.36 17.99 337 19061 559280 62910344
Loss of consciousness 62.88 17.99 122 19276 117999 63351625
Joint swelling 62.86 17.99 12 19386 327654 63141970
Drug hypersensitivity 60.40 17.99 11 19387 310676 63158948
Stoma site irritation 60.20 17.99 14 19384 216 63469408
Pneumonia aspiration 60.19 17.99 63 19335 34477 63435147
Somnolence 59.51 17.99 153 19245 178532 63291092
Infusion related reaction 59.42 17.99 4 19394 245517 63224107
Cerebrovascular accident 59.24 17.99 113 19285 107911 63361713
Femur fracture 58.63 17.99 68 19330 41688 63427936
Akinesia 54.81 17.99 20 19378 1573 63468051
Dysstasia 54.73 17.99 48 19350 21118 63448506
Arthropathy 53.53 17.99 5 19393 234787 63234837
Swelling 52.98 17.99 10 19388 275368 63194256
Decreased appetite 52.25 17.99 182 19216 250870 63218754
Therapeutic product effect variable 52.13 17.99 18 19380 1205 63468419
Abnormal dreams 51.82 17.99 35 19363 10481 63459143
Stoma site pain 51.47 17.99 17 19381 993 63468631
Dementia with Lewy bodies 49.97 17.99 13 19385 325 63469299
Marasmus 48.73 17.99 14 19384 511 63469113
Sinusitis 48.68 17.99 6 19392 226647 63242977
Malaise 48 17.99 252 19146 415702 63053922
Posture abnormal 47.42 17.99 20 19378 2312 63467312
Gait disturbance 46.37 17.99 142 19256 183036 63286588
Off label use 46.18 17.99 85 19313 674377 62795247
Pemphigus 44.42 17.99 3 19395 183723 63285901
Femoral neck fracture 43.52 17.99 29 19369 8494 63461130
Dehydration 43.51 17.99 134 19264 173220 63296404
Fibroma 42.30 17.99 14 19384 823 63468801
Application site dermatitis 41.76 17.99 10 19388 176 63469448
Gait inability 40.24 17.99 64 19334 52895 63416729
Drug ineffective 40.18 17.99 174 19224 1044591 62425033
Concomitant disease aggravated 39.43 17.99 28 19370 9084 63460540
Dementia Alzheimer's type 39.06 17.99 14 19384 1046 63468578
Arrhythmia 38.98 17.99 53 19345 38087 63431537
Accessory cardiac pathway 38.93 17.99 6 19392 5 63469619
Hypokinesia 38.85 17.99 33 19365 13903 63455721
Treatment failure 38.76 17.99 7 19391 199036 63270588
Application site discolouration 38.58 17.99 13 19385 808 63468816
Subileus 38.48 17.99 19 19379 3160 63466464
Fatigue 37.82 17.99 142 19256 887886 62581738
Product prescribing error 37.21 17.99 43 19355 26246 63443378
General physical health deterioration 35.96 17.99 139 19259 201263 63268361
Eating disorder 35.50 17.99 36 19362 18980 63450644
Aphasia 35.47 17.99 47 19351 32953 63436671
Application site swelling 34.63 17.99 11 19387 567 63469057
Vascular encephalopathy 33.21 17.99 10 19388 431 63469193
Fracture 32.83 17.99 35 19363 19549 63450075
Pleurothotonus 32.28 17.99 13 19385 1336 63468288
Stoma site inflammation 32.11 17.99 10 19388 483 63469141
Extrapyramidal disorder 32.10 17.99 29 19369 13255 63456369
Dyspnoea 31.99 17.99 100 19298 661213 62808411
Nightmare 31.64 17.99 34 19364 19160 63450464
Unresponsive to stimuli 31.58 17.99 45 19353 33771 63435853
Completed suicide 30.91 17.99 4 19394 145669 63323955
Resting tremor 30.82 17.99 11 19387 812 63468812
Orthostatic hypotension 30.69 17.99 46 19352 36114 63433510
Abdominal discomfort 30.33 17.99 32 19366 320853 63148771
Stoma site discomfort 30.28 17.99 7 19391 105 63469519
Balance disorder 29.85 17.99 74 19324 84348 63385276
Screaming 29.42 17.99 16 19382 3246 63466378
Pain in extremity 29.21 17.99 35 19363 331451 63138173
Stoma site reaction 29.13 17.99 8 19390 247 63469377
Headache 29.06 17.99 98 19300 633143 62836481
Stomatitis 28.98 17.99 4 19394 138721 63330903
Hypersensitivity 27.86 17.99 29 19369 292656 63176968
Urinary retention 27.82 17.99 40 19358 30261 63439363
Stoma site hypergranulation 27.29 17.99 8 19390 314 63469310
Wound 27.29 17.99 8 19390 163255 63306369
Psychotic symptom 27.18 17.99 12 19386 1549 63468075
Dizziness 27.14 17.99 224 19174 429701 63039923
Rash 26.96 17.99 85 19313 560786 62908838
Nasopharyngitis 26.77 17.99 23 19375 254234 63215390
Cough 26.76 17.99 30 19368 292713 63176911
Neutropenia 26.75 17.99 10 19388 174995 63294629
Weight decreased 26.73 17.99 160 19238 276638 63192986
Parkinson's disease 26.62 17.99 11 19387 1208 63468416
Back pain 26.49 17.99 25 19373 264120 63205504
Therapeutic product effect decreased 26.41 17.99 13 19385 193174 63276450
Apparent death 26.25 17.99 11 19387 1251 63468373
Feeding disorder 26.23 17.99 26 19372 13336 63456288
Depressed level of consciousness 25.84 17.99 58 19340 62020 63407604
Febrile neutropenia 25.75 17.99 3 19395 118446 63351178
Hip fracture 25.74 17.99 38 19360 29436 63440188
Senile dementia 25.04 17.99 7 19391 231 63469393
Arthritis 25.04 17.99 3 19395 115918 63353706
Application site vesicles 24.89 17.99 11 19387 1424 63468200
Discomfort 24.86 17.99 10 19388 167364 63302260
Peripheral swelling 24.58 17.99 27 19371 265915 63203709
Product administered at inappropriate site 24.45 17.99 14 19384 3135 63466489
Agnosia 24.29 17.99 6 19392 121 63469503
Hepatic enzyme increased 24.25 17.99 16 19382 202312 63267312
Intentional product use issue 23.83 17.99 5 19393 127887 63341737
Dystonia 23.70 17.99 25 19373 13794 63455830
Psychotic disorder 23.69 17.99 34 19364 25678 63443946
Parkinsonian gait 23.53 17.99 8 19390 511 63469113
Psychomotor hyperactivity 23.29 17.99 22 19376 10641 63458983
Salivary hypersecretion 23.12 17.99 19 19379 7647 63461977
Dermatitis contact 22.69 17.99 22 19376 10986 63458638
Fear 22.66 17.99 26 19372 15740 63453884
Fluid intake reduced 22.57 17.99 14 19384 3627 63465997
Faecaloma 22.54 17.99 19 19379 7922 63461702
Anxiety 22.45 17.99 128 19270 217413 63252211
Urinary tract infection 22.43 17.99 148 19250 264536 63205088
Incorrect product administration duration 21.81 17.99 22 19376 11524 63458100
Parkinsonism 21.78 17.99 21 19377 10418 63459206
Medical device site dryness 21.76 17.99 5 19393 73 63469551
Atrioventricular block second degree 21.64 17.99 14 19384 3900 63465724
Paranoia 21.59 17.99 22 19376 11657 63457967
Myalgia 21.36 17.99 9 19389 146520 63323104
Medical device site injury 21.28 17.99 3 19395 0 63469624
Product administration interrupted 21.25 17.99 15 19383 4821 63464803
Drug interaction 20.56 17.99 130 19268 229001 63240623
Cerebral haemorrhage 20.46 17.99 35 19363 30694 63438930
Pyrexia 20.08 17.99 75 19323 470403 62999221
Neuropathy peripheral 20.06 17.99 5 19393 113662 63355962
Hypophagia 20.02 17.99 35 19363 31224 63438400
Mental impairment 19.78 17.99 23 19375 14128 63455496
Abnormal faeces 19.57 17.99 15 19383 5465 63464159
Lower respiratory tract infection 19.49 17.99 8 19390 132299 63337325
Tension 19.16 17.99 12 19386 3163 63466461
Apathy 18.93 17.99 18 19380 8776 63460848
Transient ischaemic attack 18.86 17.99 38 19360 37715 63431909
Platelet count decreased 18.84 17.99 6 19392 116116 63353508
Gastrointestinal sounds abnormal 18.81 17.99 13 19385 4038 63465586
Cardiac failure 18.81 17.99 65 19333 89077 63380547
Stoma site extravasation 18.71 17.99 6 19392 319 63469305
Altered state of consciousness 18.49 17.99 30 19368 25200 63444424
Paraesthesia 18.02 17.99 13 19385 156953 63312671

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 485.08 17.81 303 16377 51195 34889056
Product adhesion issue 398.35 17.81 102 16578 1498 34938753
Confusional state 297.20 17.81 354 16326 143806 34796445
Application site erythema 258.91 17.81 79 16601 2257 34937994
Aggression 257.18 17.81 184 16496 38780 34901471
Fall 238.87 17.81 380 16300 202505 34737746
On and off phenomenon 224.65 17.81 72 16608 2425 34937826
Freezing phenomenon 213.99 17.81 62 16618 1474 34938777
Dementia 195.80 17.81 106 16574 13642 34926609
Stoma site discharge 182.56 17.81 52 16628 1161 34939090
Abnormal behaviour 178.77 17.81 124 16556 24845 34915406
Application site pruritus 165.23 17.81 50 16630 1387 34938864
Agitation 159.27 17.81 165 16515 57234 34883017
Bradykinesia 143.54 17.81 58 16622 3835 34936416
Hallucination, visual 138.33 17.81 93 16587 17698 34922553
Gait disturbance 136.71 17.81 185 16495 84955 34855296
Stoma site erythema 134.84 17.81 38 16642 815 34939436
Cognitive disorder 126.95 17.81 107 16573 28586 34911665
Dyskinesia 121.22 17.81 94 16586 22319 34917932
Blood cholinesterase decreased 115.18 17.81 24 16656 129 34940122
Death 114.72 17.81 432 16248 397617 34542634
Muscle rigidity 109.18 17.81 66 16614 10452 34929799
Application site rash 103.61 17.81 31 16649 826 34939425
Somnolence 99.74 17.81 185 16495 110931 34829320
General physical health deterioration 91.54 17.81 194 16486 128075 34812176
Device dislocation 88.42 17.81 48 16632 6201 34934050
Memory impairment 84.91 17.81 104 16576 43214 34897037
Akinesia 82.10 17.81 33 16647 2151 34938100
Restlessness 81.13 17.81 79 16601 25403 34914848
Disorientation 80.64 17.81 89 16591 33099 34907152
Mobility decreased 80.58 17.81 85 16595 30043 34910208
Fibroma 78.55 17.81 21 16659 367 34939884
Dementia with Lewy bodies 78.44 17.81 24 16656 691 34939560
Pneumonia aspiration 74.78 17.81 96 16584 41807 34898444
Delusion 70.49 17.81 54 16626 12581 34927670
Delirium 66.58 17.81 93 16587 43898 34896353
Speech disorder 66.08 17.81 71 16609 25615 34914636
Stoma site inflammation 64.38 17.81 19 16661 482 34939769
Hyperkinesia 64.00 17.81 26 16654 1742 34938509
Dysphagia 58.57 17.81 106 16574 62275 34877976
Stoma site reaction 58.00 17.81 15 16665 229 34940022
Abnormal dreams 57.40 17.81 39 16641 7539 34932712
Reduced facial expression 57.18 17.81 21 16659 1070 34939181
Gait inability 56.26 17.81 59 16621 20699 34919552
Tremor 55.48 17.81 122 16558 82465 34857786
Application site irritation 54.24 17.81 18 16662 677 34939574
Febrile neutropenia 53.17 17.81 3 16677 136846 34803405
Arthralgia 52.50 17.81 9 16671 170032 34770219
Paranoia 49.25 17.81 43 16637 12025 34928226
Parkinson's disease 48.33 17.81 20 16660 1404 34938847
Sinus bradycardia 46.60 17.81 43 16637 12920 34927331
Syncope 45.20 17.81 120 16560 91331 34848920
Bradycardia 44.65 17.81 106 16574 75312 34864939
Urinary incontinence 43.06 17.81 49 16631 18825 34921426
Neutropenia 42.84 17.81 11 16669 156767 34783484
Device kink 41.15 17.81 13 16667 417 34939834
Prescribed underdose 40.89 17.81 34 16646 8899 34931352
Intentional medical device removal by patient 40.79 17.81 12 16668 301 34939950
Stoma site pain 38.96 17.81 14 16666 670 34939581
Balance disorder 38.03 17.81 69 16611 40585 34899666
Stoma site extravasation 37.94 17.81 9 16671 94 34940157
Psychotic disorder 37.43 17.81 52 16628 24400 34915851
Application site discolouration 36.76 17.81 11 16669 293 34939958
Stoma site infection 36.65 17.81 14 16666 796 34939455
Product administration error 36.55 17.81 42 16638 16302 34923949
Hangover 36.48 17.81 15 16665 1036 34939215
Loss of consciousness 36.40 17.81 104 16576 82563 34857688
Urinary tract infection 36.27 17.81 105 16575 83976 34856275
Drug abuse 36.07 17.81 3 16677 99093 34841158
Application site hypersensitivity 35.66 17.81 9 16671 124 34940127
Disturbance in attention 35.06 17.81 52 16628 25893 34914358
Motor dysfunction 34.98 17.81 28 16652 6946 34933305
Tension 34.41 17.81 18 16662 2157 34938094
Mini mental status examination abnormal 34.01 17.81 6 16674 10 34940241
Marasmus 33.16 17.81 12 16668 586 34939665
Stoma site hypergranulation 32.33 17.81 9 16671 184 34940067
Off label use 30.38 17.81 101 16579 419423 34520828
Sleep disorder 29.91 17.81 54 16626 31634 34908617
Parkinsonism 29.26 17.81 27 16653 8111 34932140
Application site reaction 29.19 17.81 10 16670 415 34939836
Dyspnoea 29.17 17.81 88 16592 376694 34563557
Nonspecific reaction 29.16 17.81 14 16666 1397 34938854
Acute kidney injury 29.15 17.81 64 16616 304924 34635327
Hypokinesia 29.13 17.81 28 16652 8852 34931399
Device issue 28.67 17.81 29 16651 9748 34930503
Stoma site odour 28.38 17.81 6 16674 35 34940216
Malaise 27.58 17.81 167 16513 185658 34754593
Therapeutic product effect variable 27.00 17.81 16 16664 2440 34937811
Cholinergic syndrome 26.04 17.81 10 16670 577 34939674
Dyschezia 25.59 17.81 13 16667 1465 34938786
Screaming 25.54 17.81 13 16667 1471 34938780
White blood cell count decreased 25.48 17.81 7 16673 95438 34844813
Application site vesicles 25.47 17.81 10 16670 612 34939639
Underdose 25.23 17.81 32 16648 13748 34926503
Aspiration 25.04 17.81 30 16650 12164 34928087
Myalgia 24.76 17.81 5 16675 84105 34856146
Salivary hypersecretion 24.19 17.81 25 16655 8619 34931632
Stoma site irritation 23.85 17.81 7 16673 174 34940077
Embedded device 23.56 17.81 8 16672 323 34939928
Pancytopenia 23.56 17.81 8 16672 95149 34845102
Parkinsonian gait 23.47 17.81 9 16671 517 34939734
Aphasia 23.43 17.81 39 16641 21415 34918836
Middle insomnia 23.36 17.81 22 16658 6780 34933471
Hypersomnia 23.02 17.81 29 16651 12378 34927873
Apathy 23.00 17.81 22 16658 6910 34933341
Orthostatic hypotension 22.98 17.81 43 16637 25876 34914375
Neuroleptic malignant syndrome 22.88 17.81 35 16645 17899 34922352
Miosis 22.16 17.81 25 16655 9510 34930741
Device difficult to use 22.15 17.81 15 16665 2882 34937369
Platelet count decreased 22.12 17.81 15 16665 119702 34820549
Pain 22.06 17.81 40 16640 204635 34735616
Dysstasia 21.82 17.81 28 16652 12167 34928084
Headache 21.81 17.81 39 16641 200596 34739655
Concomitant disease progression 21.58 17.81 14 16666 2504 34937747
Back pain 21.53 17.81 16 16664 121773 34818478
Incorrect product administration duration 21.37 17.81 18 16662 4793 34935458
Depressed level of consciousness 20.92 17.81 56 16624 42785 34897466
Condition aggravated 20.90 17.81 160 16520 192036 34748215
Psychomotor hyperactivity 20.30 17.81 24 16656 9598 34930653
Toxicity to various agents 19.98 17.81 41 16639 200321 34739930
Urinary retention 19.32 17.81 49 16631 36239 34904012
Confusional arousal 19.27 17.81 4 16676 21 34940230
Hip fracture 19.21 17.81 26 16654 11899 34928352
Neuropathy peripheral 18.94 17.81 8 16672 83255 34856996
Choking 18.73 17.81 17 16663 4998 34935253
Wrong technique in product usage process 18.54 17.81 48 16632 35938 34904313
Incorrect product dosage form administered 18.38 17.81 6 16674 214 34940037
Oesophageal dilatation 18.35 17.81 6 16674 215 34940036
Dystonia 18.01 17.81 24 16656 10821 34929430
Application site inflammation 17.97 17.81 5 16675 102 34940149
Hypophagia 17.84 17.81 37 16643 23985 34916266

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 601.64 15.59 356 23986 85389 79634657
Fall 390.89 15.59 601 23741 487028 79233018
Confusional state 336.78 15.59 448 23894 317549 79402497
On and off phenomenon 303.64 15.59 87 24255 3153 79716893
Dementia 274.20 15.59 139 24203 24520 79695526
Freezing phenomenon 256.15 15.59 68 24274 1846 79718200
Hallucination, visual 255.94 15.59 146 24196 32583 79687463
Aggression 243.04 15.59 166 24176 50792 79669254
Stoma site discharge 237.29 15.59 66 24276 2143 79717903
Blood cholinesterase decreased 224.46 15.59 43 24299 238 79719808
Agitation 213.25 15.59 203 24139 99512 79620534
Application site erythema 197.93 15.59 70 24272 5040 79715006
Bradykinesia 190.88 15.59 77 24265 7966 79712080
Stoma site erythema 177.45 15.59 50 24292 1703 79718343
Product adhesion issue 176.84 15.59 55 24287 2649 79717397
Cognitive disorder 172.03 15.59 154 24188 69772 79650274
Dyskinesia 163.38 15.59 124 24218 44649 79675397
Abnormal behaviour 160.36 15.59 113 24229 36308 79683738
Application site pruritus 154.47 15.59 54 24288 3756 79716290
Delusion 148.69 15.59 87 24255 20336 79699710
Disorientation 148.00 15.59 135 24207 62641 79657405
Death 124.21 15.59 417 23925 566097 79153949
Somnolence 122.95 15.59 243 24099 238738 79481308
Akinesia 119.31 15.59 43 24299 3269 79716777
Gait disturbance 119.02 15.59 221 24121 207285 79512761
Pneumonia aspiration 116.60 15.59 122 24220 66845 79653201
Muscle rigidity 107.32 15.59 70 24272 19812 79700234
Restlessness 105.70 15.59 98 24244 46394 79673652
Bradycardia 100.78 15.59 162 24180 135395 79584651
Delirium 98.12 15.59 125 24217 84502 79635544
Application site rash 97.23 15.59 33 24309 2099 79717947
Arthralgia 93.93 15.59 29 24313 571774 79148272
Cholinergic syndrome 87.74 15.59 26 24316 1061 79718985
Tremor 87.45 15.59 173 24169 169910 79550136
Syncope 82.18 15.59 174 24168 179275 79540771
General physical health deterioration 79.10 15.59 223 24119 275015 79445031
Dysphagia 78.79 15.59 137 24205 121999 79598047
Abnormal dreams 76.23 15.59 46 24296 11366 79708680
Stoma site inflammation 75.69 15.59 21 24321 675 79719371
Memory impairment 75.57 15.59 128 24214 111606 79608440
Cerebral atrophy 73.96 15.59 40 24302 8035 79712011
Mini mental status examination abnormal 73.26 15.59 11 24331 6 79720040
Loss of consciousness 72.48 15.59 159 24183 167784 79552262
Therapeutic product effect variable 72.05 15.59 26 24316 1983 79718063
Hyperkinesia 67.77 15.59 27 24315 2702 79717344
Pain 66.77 15.59 70 24272 703732 79016314
Speech disorder 62.42 15.59 80 24262 54365 79665681
Paranoia 60.43 15.59 49 24293 19383 79700663
Drug hypersensitivity 59.27 15.59 10 24332 298906 79421140
Fibroma 57.66 15.59 18 24324 877 79719169
Stoma site pain 56.56 15.59 20 24322 1438 79718608
Stoma site hypergranulation 55.71 15.59 15 24327 430 79719616
Device dislocation 55.67 15.59 53 24289 25917 79694129
Alopecia 55.23 15.59 4 24338 231351 79488695
Marasmus 55.21 15.59 18 24324 1010 79719036
Wrong technique in product usage process 54.46 15.59 88 24254 73787 79646259
Pleurothotonus 52.59 15.59 22 24320 2494 79717552
Febrile neutropenia 52.37 15.59 5 24337 230994 79489052
Stoma site irritation 52.36 15.59 13 24329 268 79719778
Infusion related reaction 52.15 15.59 5 24337 230232 79489814
Rheumatoid arthritis 51.55 15.59 3 24339 208467 79511579
Psychotic disorder 50.90 15.59 63 24279 41339 79678707
Dementia with Lewy bodies 50.29 15.59 16 24326 830 79719216
Application site hypersensitivity 50.13 15.59 13 24329 321 79719725
Stoma site reaction 47.55 15.59 13 24329 395 79719651
Reduced facial expression 47.35 15.59 21 24321 2744 79717302
Balance disorder 46.53 15.59 97 24245 98760 79621286
Orthostatic hypotension 45.68 15.59 70 24272 56094 79663952
Joint swelling 44.92 15.59 16 24326 288630 79431416
Stoma site extravasation 44.27 15.59 12 24330 353 79719693
Sinus bradycardia 43.92 15.59 46 24296 25201 79694845
Dysstasia 43.77 15.59 48 24294 27698 79692348
Stoma site odour 43.06 15.59 9 24333 82 79719964
Neuroleptic malignant syndrome 42.30 15.59 47 24295 27512 79692534
Product administration error 41.64 15.59 50 24292 31796 79688250
Headache 41.44 15.59 86 24256 653686 79066360
Application site dermatitis 41.35 15.59 10 24332 184 79719862
Stoma site infection 41.12 15.59 16 24326 1504 79718542
Urinary tract infection 40.85 15.59 179 24163 274333 79445713
Extrapyramidal disorder 40.67 15.59 42 24300 22637 79697409
Posture abnormal 40.65 15.59 21 24321 3845 79716201
Urinary incontinence 40.56 15.59 56 24286 40853 79679193
Product administration interrupted 40.48 15.59 21 24321 3878 79716168
Femur fracture 39.97 15.59 54 24288 38598 79681448
Neutropenia 39.83 15.59 19 24323 287691 79432355
Arthropathy 39.70 15.59 4 24338 177107 79542939
Hypokinesia 39.15 15.59 38 24304 19022 79701024
Application site irritation 38.99 15.59 16 24326 1728 79718318
Depressed level of consciousness 38.85 15.59 89 24253 96563 79623483
Toxicity to various agents 38.70 15.59 43 24299 421497 79298549
Disturbance in attention 38.09 15.59 61 24281 50740 79669306
Parkinsonism 37.75 15.59 35 24307 16549 79703497
Dystonia 37.24 15.59 39 24303 21360 79698686
Urinary retention 37.11 15.59 64 24278 56566 79663480
Gait inability 36.55 15.59 65 24277 58852 79661194
Concomitant disease aggravated 36.36 15.59 31 24311 13136 79706910
Salivary hypersecretion 36.28 15.59 32 24310 14192 79705854
Accessory cardiac pathway 35.98 15.59 6 24336 12 79720034
Completed suicide 35.95 15.59 15 24327 245752 79474294
Rash 35.86 15.59 77 24265 578281 79141765
Sinusitis 35.66 15.59 8 24334 195493 79524553
Dehydration 35.52 15.59 160 24182 248027 79472019
Psychomotor hyperactivity 35.38 15.59 34 24308 16815 79703231
Decreased appetite 35.15 15.59 201 24141 342217 79377829
Back pain 35.14 15.59 25 24317 304155 79415891
Screaming 34.68 15.59 19 24323 3914 79716132
Intentional medical device removal by patient 34.51 15.59 10 24332 377 79719669
Dyspnoea 34.39 15.59 140 24202 856885 78863161
Hangover 32.85 15.59 15 24327 2097 79717949
Swelling 32.06 15.59 13 24329 216698 79503348
Altered state of consciousness 32.01 15.59 52 24290 43770 79676276
Hip fracture 31.84 15.59 43 24299 30718 79689328
Miosis 31.53 15.59 31 24311 15758 79704288
Mobility decreased 31.19 15.59 95 24247 122080 79597966
Stomatitis 31.17 15.59 4 24338 146753 79573293
Myalgia 31.15 15.59 9 24333 185632 79534414
Urticaria 31.04 15.59 9 24333 185192 79534854
Subileus 30.73 15.59 20 24322 5634 79714412
Femoral neck fracture 30.67 15.59 25 24317 9959 79710087
Off label use 30.56 15.59 158 24184 907057 78812989
Vascular encephalopathy 29.82 15.59 10 24332 613 79719433
Hypersomnia 29.78 15.59 36 24306 23050 79696996
Hypersensitivity 29.70 15.59 22 24320 262217 79457829
Contraindicated product administered 29.64 15.59 6 24336 157532 79562514
Parkinson's disease 29.61 15.59 13 24329 1658 79718388
Aphasia 29.55 15.59 52 24290 46680 79673366
Amyloid related imaging abnormality-oedema/effusion 29.25 15.59 9 24333 418 79719628
Unresponsive to stimuli 28.93 15.59 57 24285 55731 79664315
Apathy 28.79 15.59 27 24315 12950 79707096
Prescribed underdose 28.65 15.59 40 24302 29474 79690572
Stoma site discomfort 28.64 15.59 7 24335 135 79719911
Aspiration 28.59 15.59 33 24309 20125 79699921
Choking 28.44 15.59 26 24316 12075 79707971
Abdominal discomfort 28.44 15.59 21 24321 250706 79469340
Drug ineffective 28.19 15.59 204 24138 1080709 78639337
Intentional product use issue 28.19 15.59 6 24336 152106 79567940
Malignant neoplasm progression 28.18 15.59 4 24338 135986 79584060
Incorrect product dosage form administered 27.67 15.59 8 24334 299 79719747
Application site reaction 27.67 15.59 10 24332 766 79719280
Anger 27.61 15.59 30 24312 17132 79702914
Tension 27.48 15.59 17 24325 4387 79715659
Neuropathy peripheral 27.39 15.59 5 24337 141300 79578746
Product prescribing error 27.23 15.59 49 24293 44764 79675282
Cough 26.04 15.59 45 24297 366744 79353302
Parkinsonian gait 25.72 15.59 10 24332 938 79719108
Agnosia 25.35 15.59 7 24335 221 79719825
Device kink 24.97 15.59 12 24330 1883 79718163
Oesophageal dilatation 24.57 15.59 8 24334 447 79719599
Medical device site injury 24.34 15.59 4 24338 7 79720039
Resting tremor 24.28 15.59 11 24331 1510 79718536
Vomiting 23.93 15.59 309 24033 665519 79054527
Hyporesponsive to stimuli 23.86 15.59 12 24330 2076 79717970
Pain in extremity 23.85 15.59 47 24295 364491 79355555
Platelet count decreased 23.81 15.59 15 24327 194649 79525397
Device issue 23.76 15.59 35 24307 27073 79692973
Feeding disorder 23.71 15.59 27 24315 16227 79703819
Nightmare 23.56 15.59 34 24308 25827 79694219
Bradyarrhythmia 23.36 15.59 15 24327 4131 79715915
Hypophagia 23.09 15.59 46 24296 45321 79674725
Treatment failure 22.47 15.59 12 24330 170474 79549572
Medical device site dryness 22.37 15.59 5 24337 64 79719982
Skin irritation 22.32 15.59 22 24320 11218 79708828
Fluid intake reduced 22.00 15.59 17 24325 6271 79713775
Arrhythmia 21.98 15.59 54 24288 61218 79658828
Circulatory collapse 21.38 15.59 40 24302 37628 79682418
Device connection issue 21.35 15.59 9 24333 1039 79719007
Underdose 21.10 15.59 37 24305 33114 79686932
White blood cell count decreased 21.05 15.59 16 24326 188272 79531774
Oropharyngeal pain 20.91 15.59 4 24338 109349 79610697
Movement disorder 20.80 15.59 33 24309 27226 79692820
Fracture 20.35 15.59 29 24313 21772 79698274
Arthritis 20.35 15.59 5 24337 114875 79605171
Nasopharyngitis 20.04 15.59 29 24313 253852 79466194
Faecaloma 19.98 15.59 21 24321 11543 79708503
Stoma complication 19.98 15.59 8 24334 811 79719235
Fatigue 19.84 15.59 185 24157 929542 78790504
Hepatic enzyme increased 19.80 15.59 16 24326 182594 79537452
Hand deformity 19.45 15.59 4 24338 103915 79616131
Incoherent 19.01 15.59 17 24325 7675 79712371
Nonspecific reaction 18.99 15.59 11 24331 2521 79717525
Mental impairment 18.78 15.59 26 24316 19010 79701036
Anxiety 18.75 15.59 135 24207 248377 79471669
Hallucinations, mixed 18.56 15.59 16 24326 6883 79713163
Drooling 18.53 15.59 15 24327 5919 79714127
Psychotic symptom 18.34 15.59 11 24331 2686 79717360
Medical device site hyperaesthesia 17.99 15.59 3 24339 6 79720040
Stoma site induration 17.98 15.59 4 24338 50 79719996
Atrioventricular block second degree 17.75 15.59 16 24326 7296 79712750
Grimacing 17.73 15.59 7 24335 684 79719362
Drug dispensed to wrong patient 17.58 15.59 7 24335 699 79719347
Middle insomnia 17.45 15.59 23 24319 16046 79704000
Time perception altered 17.27 15.59 5 24337 188 79719858
Haematuria traumatic 17.16 15.59 5 24337 192 79719854
Migraine 17.16 15.59 3 24339 87490 79632556
Wound 17.12 15.59 7 24335 116172 79603874
Dyspnoea exertional 17.05 15.59 3 24339 87070 79632976
Epilepsy 16.82 15.59 38 24304 40822 79679224
Head injury 16.79 15.59 36 24306 37333 79682713
Amyloid related imaging abnormality-microhaemorrhages and haemosiderin deposits 16.64 15.59 5 24337 214 79719832
Poriomania 16.57 15.59 5 24337 217 79719829
Urinary casts present 16.47 15.59 4 24338 75 79719971
Confusional arousal 16.42 15.59 4 24338 76 79719970
Pancytopenia 16.20 15.59 16 24326 165729 79554317
Facial bones fracture 16.19 15.59 13 24329 5069 79714977
Fear 15.93 15.59 26 24316 21960 79698086
Lack of application site rotation 15.86 15.59 4 24338 88 79719958
Libido increased 15.82 15.59 9 24333 1992 79718054
Senile dementia 15.81 15.59 5 24337 254 79719792
Concomitant disease progression 15.80 15.59 11 24331 3462 79716584
Neuropsychiatric symptoms 15.79 15.59 8 24334 1407 79718639
Lower respiratory tract infection 15.74 15.59 10 24332 129210 79590836
Hallucination, auditory 15.72 15.59 25 24317 20668 79699378
Application site vesicles 15.65 15.59 8 24334 1432 79718614

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 0078-0501 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 0078-0502 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
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 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 16714-115 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 16714-116 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
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