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

Stem definition	Drug id	CAS RN
	946	120014-06-4

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
7.50	mg	O

ADMET properties:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Nov. 25, 1996	FDA	EISAI INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	8.4	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN	INHIBITOR	Ki	7.80	WOMBAT-PK	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.05	WOMBAT-PK
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN		IC50	4.82	CHEMBL
Beta-secretase 1	Enzyme	P56817	BACE1_HUMAN		IC50	5.49	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	7.84	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.70	CHEMBL
Cholinesterase	Enzyme	P06276	CHLE_HUMAN		Ki	4.90	CHEMBL
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		IC50	6.46	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	4.46	CHEMBL
Acetylcholinesterase	Enzyme		ACES_BOVIN		Ki	8.54	CHEMBL
Acetylcholinesterase	Enzyme		ACES_TORCA		IC50	8.24	CHEMBL
Choline O-acetyltransferase	Enzyme		CLAT_RAT		IC50	8.28	CHEMBL
Butyrylcholinesterase; Protein Bche	Enzyme		Q9JKC1_RAT		IC50	5.56	CHEMBL
Acetylcholinesterase	Enzyme		ACES_RAT		IC50	8.77	CHEMBL
Acetylcholinesterase	Enzyme		ACES_MOUSE		IC50	8.24	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		IC50	6.08	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_RAT		IC50	4.82	CHEMBL
Butyrylcholinesterase	Enzyme		Q9N1N9_HORSE		Ki	6.19	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	7.25	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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