donepezil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
946 120014-06-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aricept
  • donepezil
  • donepezil hydrochloride
  • donepezil HCl
  • donezpil hydrochloride
  • donezpil
  • donezpil HCl
  • donepezilium oxalate trihydrate
  • donepezilium oxalate
  • donepezil oxalate
  • E2020
  • E-2020
An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.
  • Molecular weight: 379.50
  • Formula: C24H29NO3
  • CLOGP: 4.60
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 38.77
  • ALOGS: -4.93
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
7.50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10.60 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.38 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Nov. 25, 1996 FDA EISAI INC

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
Bradycardia 529.81 12.75 400 30511 65898 46589253
Fall 354.15 12.75 713 30198 328384 46326767
Dementia 304.11 12.75 163 30748 14767 46640384
Syncope 270.91 12.75 340 30571 104463 46550688
Electrocardiogram QT prolonged 257.96 12.75 237 30674 51088 46604063
Confusional state 237.66 12.75 399 30512 159493 46495658
Sinus bradycardia 222.05 12.75 129 30782 13653 46641498
Hallucination 191.64 12.75 199 30712 49752 46605399
Agitation 169.52 12.75 196 30715 55219 46599932
Drug interaction 168.39 12.75 397 30514 202697 46452454
Dementia Alzheimer's type 158.14 12.75 50 30861 1145 46654006
Torsade de pointes 150.16 12.75 96 30815 12058 46643093
Delusion 147.30 12.75 92 30819 11096 46644055
Aggression 146.38 12.75 121 30790 22623 46632528
Abnormal behaviour 143.87 12.75 116 30795 20942 46634209
Cognitive disorder 127.36 12.75 139 30772 36744 46618407
Neuroleptic malignant syndrome 125.50 12.75 83 30828 11039 46644112
Pleurothotonus 118.74 12.75 40 30871 1125 46654026
Parkinsonism 113.90 12.75 69 30842 7879 46647272
Delirium 107.68 12.75 128 30783 37100 46618051
Drug ineffective 102.79 12.75 183 30728 677655 45977496
Hallucination, visual 102.50 12.75 89 30822 17784 46637367
Rheumatoid arthritis 102.15 12.75 18 30893 240197 46414954
Seizure 93.67 12.75 233 30678 122821 46532330
Cholinergic syndrome 90.04 12.75 25 30886 358 46654793
Extrapyramidal disorder 87.59 12.75 67 30844 11201 46643950
Arthralgia 86.48 12.75 69 30842 364534 46290617
Somnolence 85.98 12.75 263 30648 156258 46498893
Loss of consciousness 81.36 12.75 204 30707 108034 46547117
Electrocardiogram PR prolongation 80.72 12.75 26 30885 633 46654518
Altered state of consciousness 80.59 12.75 88 30823 23260 46631891
Depressed level of consciousness 80.33 12.75 126 30785 47443 46607708
Tremor 79.75 12.75 211 30700 115428 46539723
Femoral neck fracture 76.09 12.75 54 30857 8049 46647102
Sinus node dysfunction 74.01 12.75 42 30869 4247 46650904
Muscle rigidity 72.57 12.75 57 30854 9904 46645247
Torticollis 71.77 12.75 31 30880 1736 46653415
Hypothermia 70.53 12.75 61 30850 12122 46643029
Pain 69.20 12.75 132 30779 476816 46178335
Myoclonus 67.62 12.75 64 30847 14288 46640863
Disorientation 64.01 12.75 99 30812 36819 46618332
Atrioventricular block first degree 62.22 12.75 43 30868 6143 46649008
Mania 62.16 12.75 54 30857 10792 46644359
Mental status changes 61.69 12.75 99 30812 37989 46617162
Decreased appetite 60.98 12.75 272 30639 193564 46461587
Nightmare 58.04 12.75 63 30848 16535 46638616
Urinary incontinence 52.98 12.75 79 30832 28451 46626700
Hypersensitivity 50.86 12.75 18 30893 150303 46504848
Alopecia 50.75 12.75 22 30889 162392 46492759
Rash 50.46 12.75 100 30811 356412 46298739
Sudden death 49.85 12.75 45 30866 9459 46645692
Drug hypersensitivity 49.60 12.75 53 30858 243772 46411379
Dyskinesia 49.35 12.75 77 30834 28848 46626303
Lethargy 48.87 12.75 106 30805 51065 46604086
Hypophagia 48.59 12.75 77 30834 29229 46625922
Urinary tract infection 48.12 12.75 279 30632 219987 46435164
Joint swelling 48.04 12.75 25 30886 166048 46489103
Wandering pacemaker 48.02 12.75 8 30903 3 46655148
Treatment failure 46.75 12.75 4 30907 93083 46562068
Pain in extremity 46.47 12.75 62 30849 258618 46396533
Cough 45.77 12.75 51 30860 230198 46424953
Sinusitis 44.82 12.75 15 30896 129753 46525398
Unresponsive to stimuli 44.59 12.75 78 30833 32096 46623055
Headache 43.20 12.75 167 30744 478185 46176966
Hypocapnia 42.78 12.75 14 30897 359 46654792
Tardive dyskinesia 42.11 12.75 37 30874 7506 46647645
Psychomotor hyperactivity 41.76 12.75 41 30870 9572 46645579
Anal incontinence 41.70 12.75 45 30866 11733 46643418
Pruritus 41.60 12.75 60 30851 242292 46412859
Gastrointestinal haemorrhage 41.46 12.75 129 30782 77244 46577907
Cerebral atrophy 41.01 12.75 30 30881 4686 46650465
Atrioventricular block complete 39.78 12.75 36 30875 7591 46647560
Neuropsychiatric symptoms 39.49 12.75 14 30897 460 46654691
Dehydration 39.42 12.75 209 30702 159331 46495820
Hypersexuality 38.60 12.75 14 30897 492 46654659
Febrile neutropenia 38.24 12.75 8 30903 94619 46560532
Infusion related reaction 38.04 12.75 10 30901 101198 46553953
Product administration interrupted 37.45 12.75 13 30898 401 46654750
Hypokalaemia 36.78 12.75 135 30776 87889 46567262
Memory impairment 36.08 12.75 123 30788 77214 46577937
Pneumonia aspiration 35.49 12.75 70 30841 31535 46623616
Psoriasis 35.37 12.75 5 30906 78599 46576552
Immobile 34.94 12.75 27 30884 4579 46650572
Epilepsy 34.79 12.75 59 30852 23679 46631472
Dementia with Lewy bodies 34.78 12.75 11 30900 252 46654899
Long QT syndrome 34.77 12.75 23 30888 3057 46652094
Gait disturbance 34.32 12.75 188 30723 145075 46510076
Miosis 33.89 12.75 31 30880 6626 46648525
Atrial tachycardia 31.91 12.75 19 30892 2101 46653050
Generalised tonic-clonic seizure 31.58 12.75 61 30850 27061 46628090
Atrioventricular block 31.37 12.75 30 30881 6781 46648370
Hip fracture 31.26 12.75 60 30851 26496 46628655
Lack of spontaneous speech 30.81 12.75 9 30902 156 46654995
Sinus arrest 30.00 12.75 17 30894 1714 46653437
Rhabdomyolysis 29.38 12.75 77 30834 41832 46613319
Parkinson's disease 29.08 12.75 16 30895 1523 46653628
Swelling 28.88 12.75 24 30887 124487 46530664
Arthropathy 28.87 12.75 10 30901 84690 46570461
Paratonia 28.70 12.75 6 30905 22 46655129
Sedation 28.50 12.75 53 30858 22857 46632294
Urinary retention 28.39 12.75 57 30854 26004 46629147
Fluid intake reduced 28.34 12.75 21 30890 3345 46651806
Medication error 28.33 12.75 63 30848 30848 46624303
Circulatory collapse 28.13 12.75 51 30860 21573 46633578
Systemic lupus erythematosus 27.40 12.75 5 30906 65175 46589976
Hypernatraemia 27.24 12.75 27 30884 6374 46648777
Dyspnoea 27.22 12.75 215 30696 515333 46139818
Off label use 26.83 12.75 145 30766 379696 46275455
Delusional disorder, persecutory type 26.75 12.75 8 30903 151 46655000
Oropharyngeal pain 26.62 12.75 8 30903 74160 46580991
Orthostatic hypotension 25.76 12.75 53 30858 24605 46630546
Accidental overdose 25.69 12.75 47 30864 20019 46635132
Restlessness 25.65 12.75 54 30857 25470 46629681
Dysarthria 25.37 12.75 68 30843 37430 46617721
Overconfidence 25.28 12.75 4 30907 0 46655151
Speech disorder 24.89 12.75 66 30845 36101 46619050
Chorea 24.76 12.75 13 30898 1127 46654024
Wrong patient received product 24.68 12.75 15 30896 1722 46653429
Drug intolerance 24.62 12.75 37 30874 147012 46508139
Hyperhidrosis 24.12 12.75 120 30791 89188 46565963
Fatigue 23.96 12.75 273 30638 608424 46046727
Posture abnormal 23.87 12.75 16 30895 2174 46652977
Dizziness 23.75 12.75 336 30575 340078 46315073
Myalgia 23.63 12.75 28 30883 123060 46532091
Suspiciousness 23.61 12.75 9 30902 364 46654787
Salivary hypersecretion 23.47 12.75 25 30886 6420 46648731
Hypotension 23.36 12.75 246 30665 232343 46422808
Injection site erythema 23.35 12.75 10 30901 74417 46580734
Colitis microscopic 23.12 12.75 25 30886 6531 46648620
Cerebral haemorrhage 22.89 12.75 55 30856 28316 46626835
Encephalopathy 22.81 12.75 61 30850 33528 46621623
Cerebrovascular accident 22.67 12.75 129 30782 100910 46554241
Drooling 22.59 12.75 18 30893 3191 46651960
Weight increased 22.47 12.75 47 30864 164426 46490725
Social avoidant behaviour 22.32 12.75 17 30894 2822 46652329
Incontinence 22.28 12.75 30 30881 9832 46645319
Anger 22.26 12.75 33 30878 11819 46643332
Therapeutic product effect incomplete 22.23 12.75 12 30899 78141 46577010
Ventricular tachycardia 22.05 12.75 40 30871 16927 46638224
Food refusal 22.00 12.75 8 30903 283 46654868
Skull fracture 21.83 12.75 11 30900 875 46654276
Hypomania 21.49 12.75 20 30891 4368 46650783
Grandiosity 21.12 12.75 7 30904 187 46654964
Drug level increased 20.89 12.75 41 30870 18400 46636751
Psychotic disorder 20.61 12.75 46 30865 22575 46632576
Antisocial behaviour 20.22 12.75 7 30904 214 46654937
Nasopharyngitis 20.21 12.75 45 30866 153953 46501198
Brain compression 20.20 12.75 8 30903 359 46654792
Chest discomfort 20.19 12.75 18 30893 90251 46564900
Catatonia 20.09 12.75 18 30893 3744 46651407
Executive dysfunction 19.93 12.75 6 30905 116 46655035
Sinoatrial block 19.70 12.75 10 30901 808 46654343
Lower respiratory tract infection 19.66 12.75 6 30905 55083 46600068
Hyponatraemic syndrome 19.60 12.75 9 30902 583 46654568
Inappropriate affect 19.34 12.75 10 30901 840 46654311
Hypertonia 19.31 12.75 19 30892 4447 46650704
Infection 19.25 12.75 37 30874 133555 46521596
Adams-Stokes syndrome 19.22 12.75 5 30906 55 46655096
Paranoia 19.18 12.75 29 30882 10568 46644583
Incoherent 19.14 12.75 19 30892 4493 46650658
Non-24-hour sleep-wake disorder 19.06 12.75 4 30907 15 46655136
Therapeutic product effect decreased 19.05 12.75 16 30895 82585 46572566
Blood pressure orthostatic decreased 18.90 12.75 5 30906 59 46655092
Injection site pain 18.88 12.75 26 30885 107126 46548025
Discomfort 18.73 12.75 4 30907 46666 46608485
Normal pressure hydrocephalus 18.58 12.75 7 30904 274 46654877
Pyrexia 18.58 12.75 145 30766 348657 46306494
Herbal interaction 18.52 12.75 5 30906 64 46655087
Malignant neoplasm progression 18.42 12.75 10 30901 64916 46590235
Emotional poverty 18.34 12.75 7 30904 284 46654867
Atrial fibrillation 18.07 12.75 124 30787 103466 46551685
Fracture 17.91 12.75 36 30875 16435 46638716
Vomiting 17.72 12.75 408 30503 452386 46202765
Urticaria 17.56 12.75 32 30879 117860 46537291
Aphasia 17.54 12.75 50 30861 28517 46626634
Muscle contracture 17.53 12.75 11 30900 1336 46653815
Upper gastrointestinal haemorrhage 17.51 12.75 36 30875 16702 46638449
Cerebral infarction 17.47 12.75 44 30867 23322 46631829
Dyspepsia 17.40 12.75 12 30899 68460 46586691
Obsessive thoughts 17.35 12.75 8 30903 523 46654628
Leukaemoid reaction 16.99 12.75 6 30905 195 46654956
Anaphylactic reaction 16.88 12.75 7 30904 53105 46602046
Rash papulosquamous 16.74 12.75 5 30906 94 46655057
Pressure of speech 16.68 12.75 8 30903 572 46654579
Paraesthesia 16.51 12.75 33 30878 117404 46537747
Anorgasmia 16.44 12.75 8 30903 590 46654561
Product dispensing error 16.33 12.75 25 30886 9208 46645943
Language disorder 16.30 12.75 11 30900 1512 46653639
Intercepted product dispensing error 16.17 12.75 5 30906 106 46655045
Pemphigus 16.03 12.75 5 30906 45269 46609882
Duodenal ulcer haemorrhage 15.88 12.75 13 30898 2395 46652756
Nasal congestion 15.85 12.75 6 30905 48107 46607044
Communication disorder 15.76 12.75 13 30898 2420 46652731
Injection site reaction 15.71 12.75 6 30905 47843 46607308
Dysphagia 15.59 12.75 96 30815 77216 46577935
Cholesteatoma 15.59 12.75 5 30906 120 46655031
Glossodynia 15.54 12.75 5 30906 44368 46610783
Heart rate increased 15.46 12.75 16 30895 74775 46580376
Hypoaesthesia 15.37 12.75 35 30876 118834 46536317
Hypoglycaemia 15.36 12.75 74 30837 54275 46600876
Drop attacks 15.14 12.75 8 30903 703 46654448
Haematoma 15.12 12.75 51 30860 31821 46623330
Injection site swelling 15.12 12.75 4 30907 40323 46614828
Neuropathy peripheral 15.08 12.75 23 30888 90870 46564281
Thrombocytopenia 15.01 12.75 39 30872 126542 46528609
Neutropenia 14.87 12.75 47 30864 143157 46511994
Stomatitis 14.82 12.75 14 30897 68283 46586868
Impaired self-care 14.82 12.75 11 30900 1757 46653394
Erythema 14.74 12.75 47 30864 142773 46512378
Product use issue 14.71 12.75 25 30886 94619 46560532
Muscle twitching 14.69 12.75 31 30880 14641 46640510
Hyponatraemia 14.64 12.75 116 30795 101216 46553935
Delusion of grandeur 14.57 12.75 5 30906 149 46655002
Gastric ulcer haemorrhage 14.50 12.75 17 30894 4851 46650300
Haematemesis 14.47 12.75 47 30864 28759 46626392
Nonspecific reaction 14.37 12.75 11 30900 1839 46653312
Disease progression 14.30 12.75 24 30887 91276 46563875
Gastric ulcer 14.14 12.75 39 30872 21824 46633327
Opisthotonus 13.97 12.75 6 30905 331 46654820
Crying 13.96 12.75 38 30873 21103 46634048
Pemphigoid 13.92 12.75 18 30893 5673 46649478
Acute abdomen 13.90 12.75 10 30901 1522 46653629
Visuospatial deficit 13.77 12.75 3 30908 14 46655137
Bundle branch block left 13.75 12.75 19 30892 6380 46648771
Progressive supranuclear palsy 13.71 12.75 4 30907 69 46655082
Subdural haematoma 13.65 12.75 28 30883 12969 46642182
Heart rate decreased 13.53 12.75 49 30862 31674 46623477
Herpes zoster 13.49 12.75 15 30896 67857 46587294
Blunted affect 13.44 12.75 5 30906 189 46654962
Arthritis 13.38 12.75 19 30892 77297 46577854
Product blister packaging issue 13.34 12.75 5 30906 193 46654958
Theft 13.25 12.75 4 30907 78 46655073
Senile dementia 13.22 12.75 5 30906 198 46654953
Hypoglycaemic coma 13.13 12.75 12 30899 2562 46652589
Apraxia 13.10 12.75 10 30901 1665 46653486
Abnormal dreams 13.06 12.75 24 30887 10255 46644896
Gait inability 13.05 12.75 52 30859 35151 46620000
Fibromyalgia 12.96 12.75 4 30907 36459 46618692
Balance disorder 12.93 12.75 80 30831 64441 46590710
Hepatic function abnormal 12.88 12.75 51 30860 34370 46620781

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
Dementia 347.49 13.53 176 22714 12285 29917303
Hallucination 344.22 13.53 291 22599 48768 29880820
Fall 308.30 13.53 520 22370 181352 29748236
Bradycardia 292.13 13.53 302 22588 65224 29864364
Confusional state 244.78 13.53 398 22492 134436 29795152
Agitation 163.63 13.53 204 22686 53869 29875719
Delusion 153.16 13.53 102 22788 11887 29917701
Delirium 143.73 13.53 166 22724 40465 29889123
Aggression 141.10 13.53 157 22733 36750 29892838
Pleurothotonus 130.14 13.53 43 22847 980 29928608
Cognitive disorder 119.64 13.53 117 22773 23573 29906015
Abnormal behaviour 119.17 13.53 121 22769 25502 29904086
Cholinergic syndrome 101.30 13.53 30 22860 470 29929118
Depressed level of consciousness 95.03 13.53 131 22759 38091 29891497
Hallucination, visual 87.80 13.53 83 22807 16030 29913558
Somnolence 84.59 13.53 211 22679 96552 29833036
Syncope 74.04 13.53 185 22705 84718 29844870
Neuroleptic malignant syndrome 72.20 13.53 75 22815 16220 29913368
Sinus node dysfunction 67.43 13.53 40 22850 3803 29925785
Urinary incontinence 66.29 13.53 73 22817 16867 29912721
Dementia Alzheimer's type 65.66 13.53 21 22869 430 29929158
Mania 65.46 13.53 55 22835 9099 29920489
Sinus bradycardia 63.24 13.53 60 22830 11635 29917953
Gait disturbance 63.15 13.53 161 22729 74616 29854972
Memory impairment 59.49 13.53 104 22786 37070 29892518
Febrile neutropenia 57.47 13.53 7 22883 106686 29822902
Blood cholinesterase decreased 54.85 13.53 14 22876 121 29929467
Nightmare 54.25 13.53 56 22834 12020 29917568
Serotonin syndrome 48.51 13.53 64 22826 17827 29911761
Parkinsonism 46.54 13.53 41 22849 7228 29922360
Unresponsive to stimuli 46.34 13.53 77 22813 26342 29903246
Balance disorder 45.79 13.53 92 22798 36401 29893187
Pneumonia aspiration 43.58 13.53 92 22798 37688 29891900
Myoclonus 41.43 13.53 51 22839 13261 29916327
Poriomania 41.39 13.53 11 22879 113 29929475
Tremor 41.21 13.53 139 22751 75224 29854364
Extrapyramidal disorder 39.97 13.53 45 22845 10648 29918940
Loss of consciousness 39.58 13.53 142 22748 79233 29850355
Libido increased 39.27 13.53 17 22873 827 29928761
Neutropenia 39.14 13.53 25 22865 128515 29801073
Product prescribing issue 36.23 13.53 16 22874 817 29928771
Orthostatic hypotension 35.67 13.53 65 22825 23914 29905674
Hyperhidrosis 35.14 13.53 122 22768 66968 29862620
Dyskinesia 34.80 13.53 61 22829 21773 29907815
Anal incontinence 34.57 13.53 34 22856 6888 29922700
Restlessness 34.56 13.53 62 22828 22537 29907051
Disorientation 34.49 13.53 75 22815 31343 29898245
Automatism 34.36 13.53 9 22881 87 29929501
Prescribed underdose 33.09 13.53 35 22855 7724 29921864
Arthralgia 33.08 13.53 33 22857 135758 29793830
Jealous delusion 32.83 13.53 11 22879 262 29929326
Rhabdomyolysis 32.76 13.53 115 22775 63465 29866123
Dizziness 32.39 13.53 257 22633 194652 29734936
Paranoia 31.65 13.53 39 22851 10149 29919439
Somatic delusion 31.52 13.53 9 22881 123 29929465
Mental status changes 31.43 13.53 80 22810 36999 29892589
Salivary hypersecretion 30.28 13.53 33 22857 7533 29922055
Electrocardiogram QT prolonged 30.04 13.53 77 22813 35758 29893830
Lethargy 29.17 13.53 81 22809 39438 29890150
Dyspnoea 28.28 13.53 145 22745 333150 29596438
Muscle rigidity 28.27 13.53 37 22853 10224 29919364
Dementia with Lewy bodies 28.03 13.53 12 22878 568 29929020
Miosis 27.83 13.53 32 22858 7744 29921844
Drug abuse 27.78 13.53 14 22876 82058 29847530
Parkinson's disease 27.76 13.53 17 22873 1711 29927877
Death 27.31 13.53 403 22487 356880 29572708
Hypothermia 27.14 13.53 35 22855 9532 29920056
Sexually inappropriate behaviour 26.77 13.53 10 22880 330 29929258
Flight of ideas 26.29 13.53 10 22880 347 29929241
Abdominal pain 25.66 13.53 40 22850 135614 29793974
Thrombocytopenia 25.37 13.53 41 22849 137003 29792585
Muscle contractions involuntary 24.86 13.53 16 22874 1757 29927831
Dysstasia 24.58 13.53 35 22855 10470 29919118
Seizure 24.16 13.53 143 22747 98332 29831256
Blood glucose fluctuation 24.14 13.53 21 22869 3640 29925948
Nonspecific reaction 23.98 13.53 14 22876 1292 29928296
Neuropathy peripheral 23.88 13.53 12 22878 70463 29859125
Drug interaction 23.83 13.53 245 22645 199323 29730265
Daydreaming 23.63 13.53 10 22880 460 29929128
Altered state of consciousness 23.53 13.53 49 22841 19870 29909718
Drooling 23.45 13.53 19 22871 2986 29926602
Irritability 23.02 13.53 53 22837 22997 29906591
Executive dysfunction 22.63 13.53 7 22883 128 29929460
Atrioventricular block complete 22.47 13.53 30 22860 8447 29921141
Pain 22.47 13.53 63 22827 172578 29757010
Skin swelling 22.43 13.53 12 22878 935 29928653
Intestinal haemorrhage 22.40 13.53 19 22871 3182 29926406
Inappropriate antidiuretic hormone secretion 22.35 13.53 35 22855 11387 29918201
Cold sweat 22.35 13.53 31 22859 9051 29920537
Paraesthesia 22.08 13.53 7 22883 54320 29875268
Gait inability 21.85 13.53 46 22844 18795 29910793
Psychomotor hyperactivity 21.64 13.53 29 22861 8195 29921393
Dehydration 21.64 13.53 165 22725 123374 29806214
Contusion 21.03 13.53 62 22828 31218 29898370
Hangover 20.97 13.53 12 22878 1066 29928522
Subdural haematoma 20.49 13.53 45 22845 18927 29910661
Gastrointestinal ulcer 20.35 13.53 14 22876 1718 29927870
Hip fracture 20.27 13.53 33 22857 11091 29918497
Neutrophil count decreased 20.09 13.53 4 22886 42450 29887138
Intention tremor 19.89 13.53 8 22882 323 29929265
Atrioventricular block first degree 19.67 13.53 23 22867 5665 29923923
Femoral neck fracture 19.65 13.53 17 22873 2925 29926663
Pruritus 19.49 13.53 38 22852 118166 29811422
Posture abnormal 19.42 13.53 14 22876 1850 29927738
Gastrointestinal haemorrhage 19.07 13.53 119 22771 83327 29846261
Cerebral atrophy 18.91 13.53 20 22870 4413 29925175
Duodenal ulcer 18.90 13.53 30 22860 9871 29919717
Bradyarrhythmia 18.84 13.53 14 22876 1938 29927650
Hypersomnia 18.53 13.53 32 22858 11284 29918304
Septic shock 18.49 13.53 13 22877 63594 29865994
Gastroenteritis pseudomonas 18.49 13.53 4 22886 15 29929573
Condition aggravated 18.25 13.53 173 22717 137693 29791895
Malignant neoplasm progression 18.24 13.53 17 22873 72270 29857318
Potentiating drug interaction 18.18 13.53 20 22870 4611 29924977
Hiccups 17.21 13.53 28 22862 9406 29920182
Multiple organ dysfunction syndrome 17.14 13.53 14 22876 63473 29866115
Underdose 16.91 13.53 32 22858 12109 29917479
Foaming at mouth 16.91 13.53 9 22881 694 29928894
Speech disorder 16.87 13.53 49 22841 24463 29905125
Loss of personal independence in daily activities 16.74 13.53 45 22845 21490 29908098
Defect conduction intraventricular 16.66 13.53 6 22884 178 29929410
Impulsive behaviour 16.56 13.53 13 22877 1952 29927636
Post-traumatic stress disorder 16.53 13.53 12 22878 1603 29927985
Urinary tract infection 16.18 13.53 104 22786 73555 29856033
Chest pain 15.98 13.53 42 22848 117585 29812003
Incontinence 15.92 13.53 20 22870 5306 29924282
Leukopenia 15.65 13.53 12 22878 56147 29873441
Rheumatoid arthritis 15.55 13.53 6 22884 41191 29888397
Tardive dyskinesia 15.13 13.53 19 22871 5038 29924550
Frontotemporal dementia 15.02 13.53 6 22884 238 29929350
Hypomania 14.99 13.53 13 22877 2243 29927345
Hypernatraemia 14.73 13.53 23 22867 7461 29922127
Decreased appetite 14.65 13.53 177 22713 149733 29779855
Pressure of speech 14.56 13.53 7 22883 435 29929153
Blood glucose abnormal 14.54 13.53 19 22871 5240 29924348
Headache 14.47 13.53 81 22809 182225 29747363
Musculoskeletal pain 14.46 13.53 3 22887 30937 29898651
Drug hypersensitivity 14.13 13.53 19 22871 68500 29861088
Fracture 14.03 13.53 20 22870 5986 29923602
Sudden death 13.72 13.53 34 22856 15458 29914130
Accidental poisoning 13.69 13.53 7 22883 497 29929091
Urticaria 13.59 13.53 13 22877 54593 29874995

Pharmacologic Action:

SourceCodeDescription
ATC N06DA02 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTI-DEMENTIA DRUGS
Anticholinesterases
ATC N06DA52 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTI-DEMENTIA DRUGS
Anticholinesterases
ATC N06DA53 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTI-DEMENTIA DRUGS
Anticholinesterases
FDA MoA N0000000177 Cholinesterase Inhibitors
FDA EPC N0000175723 Cholinesterase Inhibitor
CHEBI has role CHEBI:38462 acetylcholinesterase 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 D018377 Neurotransmitter Agents
MeSH PA D018697 Nootropic Agents
CHEBI has role CHEBI:37733 bche inhibitor
CHEBI has role CHEBI:66980 nootropics

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Alzheimer's disease indication 26929004 DOID:10652
Moderate to Severe Alzheimer's Type Dementia indication
Diffuse Lewy body disease off-label use 80098002
Sick sinus syndrome contraindication 36083008 DOID:13884
Gastrointestinal ulcer contraindication 40845000
Sinus bradycardia contraindication 49710005
Gastrointestinal hemorrhage contraindication 74474003
Epilepsy contraindication 84757009 DOID:1826
Asthma contraindication 195967001 DOID:2841
Atrioventricular block contraindication 233917008 DOID:0050820
Bladder outflow obstruction contraindication 236645006
NSAID-Induced Gastric Ulcer contraindication
Chronic Obstructive Pulmonary Disease with Bronchospasms contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.4 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 Ki 7.80 WOMBAT-PK CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 5.05 WOMBAT-PK
Amine oxidase [flavin-containing] B Enzyme IC50 4.82 CHEMBL
Beta-secretase 1 Enzyme IC50 5.49 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.84 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.70 CHEMBL
Cholinesterase Enzyme Ki 4.90 CHEMBL
Histamine H3 receptor GPCR IC50 6.46 CHEMBL
Multidrug resistance protein 1 Transporter IC50 4.46 CHEMBL
Acetylcholinesterase Enzyme Ki 8.54 CHEMBL
Acetylcholinesterase Enzyme IC50 8.24 CHEMBL
Choline O-acetyltransferase Enzyme IC50 8.28 CHEMBL
Butyrylcholinesterase; Protein Bche Enzyme IC50 5.56 CHEMBL
Acetylcholinesterase Enzyme IC50 8.77 CHEMBL
Acetylcholinesterase Enzyme IC50 8.24 CHEMBL
Cholinesterase Enzyme IC50 6.08 CHEMBL
Amine oxidase [flavin-containing] B Enzyme IC50 4.82 CHEMBL
Butyrylcholinesterase Enzyme Ki 6.19 CHEMBL
Acetylcholinesterase Enzyme Ki 7.25 CHEMBL

External reference:

IDSource
D00670 KEGG_DRUG
120011-70-3 SECONDARY_CAS_RN
4021006 VANDF
4024045 VANDF
C0527315 UMLSCUI
CHEBI:53289 CHEBI
E20 PDB_CHEM_ID
CHEMBL502 ChEMBL_ID
CHEMBL1678 ChEMBL_ID
DB00843 DRUGBANK_ID
D000077265 MESH_DESCRIPTOR_UI
3152 PUBCHEM_CID
6599 IUPHAR_LIGAND_ID
7517 INN_ID
8SSC91326P UNII
135446 RXNORM
15004 MMSL
178540 MMSL
4631 MMSL
6432 MMSL
d04099 MMSL
006295 NDDF
006296 NDDF
108497001 SNOMEDCT_US
386855006 SNOMEDCT_US
386856007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9747 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9748 TABLET, FILM COATED 10 mg ORAL ANDA 24 sections
Namzaric HUMAN PRESCRIPTION DRUG LABEL 2 0456-1207 CAPSULE 10 mg ORAL NDA 26 sections
Namzaric HUMAN PRESCRIPTION DRUG LABEL 2 0456-1214 CAPSULE 10 mg ORAL NDA 26 sections
Namzaric HUMAN PRESCRIPTION DRUG LABEL 2 0456-1221 CAPSULE 10 mg ORAL NDA 26 sections
Namzaric HUMAN PRESCRIPTION DRUG LABEL 2 0456-1228 CAPSULE 10 mg ORAL NDA 26 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7951 TABLET, FILM COATED 5 mg ORAL ANDA 18 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-7952 TABLET, FILM COATED 10 mg ORAL ANDA 18 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8313 TABLET, FILM COATED 10 mg ORAL ANDA 19 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-5276 TABLET, ORALLY DISINTEGRATING 5 mg ORAL ANDA 26 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-5277 TABLET, ORALLY DISINTEGRATING 10 mg ORAL ANDA 26 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6477 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6478 TABLET, FILM COATED 10 mg ORAL ANDA 24 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 13668-102 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 13668-103 TABLET, FILM COATED 10 mg ORAL ANDA 24 sections
Donepezil Hydrochloride Human Prescription Drug Label 1 16571-778 TABLET, FILM COATED 5 mg ORAL ANDA 26 sections
Donepezil Hydrochloride Human Prescription Drug Label 1 16571-779 TABLET, FILM COATED 10 mg ORAL ANDA 26 sections
DONEPEZIL HYDROCHLORIDE Human Prescription Drug Label 1 24724-028 TABLET, FILM COATED 5 mg ORAL ANDA 25 sections
DONEPEZIL HYDROCHLORIDE Human Prescription Drug Label 1 24724-029 TABLET, FILM COATED 10 mg ORAL ANDA 25 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24979-004 TABLET, FILM COATED 23 mg ORAL ANDA 16 sections
donepezil hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 29300-248 TABLET, FILM COATED 5 mg ORAL ANDA 23 sections
donepezil hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 29300-249 TABLET, FILM COATED 10 mg ORAL ANDA 23 sections
donepezil hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 29300-250 TABLET, ORALLY DISINTEGRATING 5 mg ORAL ANDA 23 sections
donepezil hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 29300-251 TABLET, ORALLY DISINTEGRATING 10 mg ORAL ANDA 23 sections
Donepezil hydrochloride Human Prescription Drug Label 1 31722-139 TABLET, FILM COATED 5 mg ORAL ANDA 25 sections
Donepezil hydrochloride Human Prescription Drug Label 1 31722-140 TABLET, FILM COATED 10 mg ORAL ANDA 25 sections
Donepezil Human Prescription Drug Label 1 31722-737 TABLET 5 mg ORAL ANDA 19 sections
Donepezil Human Prescription Drug Label 1 31722-738 TABLET 10 mg ORAL ANDA 19 sections
Donepezil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 33261-817 TABLET, FILM COATED 10 mg ORAL ANDA 19 sections
Donepezil Hydrochloride Human Prescription Drug Label 1 33342-027 TABLET, FILM COATED 5 mg ORAL ANDA 18 sections