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donepezil 🐶 Veterinary Use | 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: 4.40 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: 4.40
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:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	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
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 23, 2022	PMDA	Teikoku Seiyaku Co., Ltd.
Nov. 25, 1996	FDA	EISAI INC

FDA Adverse Event Reporting System (Female)

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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	631.23	13.55	427	33815	72800	63381980
Fall	469.91	13.55	792	33450	391542	63063238
Syncope	417.25	13.55	408	33834	116977	63337803
Dementia	311.41	13.55	167	34075	18627	63436153
Sinus bradycardia	286.01	13.55	145	34097	14406	63440374
Electrocardiogram QT prolonged	267.48	13.55	236	34006	59294	63395486
Drug interaction	237.44	13.55	435	33807	228696	63226084
Hallucination	210.42	13.55	199	34043	54618	63400162
Confusional state	195.25	13.55	408	33834	235972	63218808
Torsade de pointes	194.52	13.55	109	34133	13242	63441538

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FDA Adverse Event Reporting System (Male)

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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
Hallucination	366.76	14.34	295	23783	51203	34881650
Fall	345.45	14.34	549	23529	202336	34730517
Dementia	310.81	14.34	163	23915	13585	34919268
Bradycardia	307.95	14.34	316	23762	75102	34857751
Confusional state	304.79	14.34	432	23646	143728	34789125
Delusion	177.97	14.34	110	23968	12525	34920328
Pleurothotonus	164.04	14.34	52	24026	1153	34931700
Agitation	159.43	14.34	197	23881	57202	34875651
Delirium	143.62	14.34	164	23914	43827	34889026
Cognitive disorder	136.79	14.34	131	23947	28562	34904291

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FDA Adverse Event Reporting System (Geriatric)

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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	875.75	13.19	707	49603	134850	79559228
Fall	694.55	13.19	1160	49150	486469	79207609
Dementia	499.67	13.19	264	50046	24395	79669683
Hallucination	429.69	13.19	387	49923	85358	79608720
Syncope	426.55	13.19	545	49765	178904	79515174
Confusional state	390.55	13.19	710	49600	317287	79376791
Sinus bradycardia	335.04	13.19	205	50105	25042	79669036
Agitation	288.91	13.19	335	49975	99380	79594698
Aggression	277.06	13.19	241	50069	50717	79643361
Delusion	268.85	13.19	165	50145	20258	79673820

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:38462	acetylcholinesterase inhibitors
CHEBI has role	CHEBI:37733	EC 3.1.1.8 inhibitor
CHEBI has role	CHEBI:66980	intelligence enhancer
FDA EPC	N0000175723	Cholinesterase Inhibitor
FDA MoA	N0000000177	Cholinesterase Inhibitors
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018678	Cholinergic Agents

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

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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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	11679086	May 26, 2037	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	10016372	July 26, 2037	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	11103463	July 26, 2037	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	11648214	Sept. 23, 2037	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	10835499	May 20, 2038	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	10966936	Aug. 11, 2038	A METHOD OF TRANSDERMAL DELIVERY OF DONEPEZIL FOR TREATING MILD, MODERATE AND SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG;14MG	NAMZARIC	ABBVIE	N206439	Dec. 23, 2014	RX	CAPSULE, EXTENDED RELEASE	ORAL	8173708	Nov. 22, 2025	MEMANTINE HCL/DONEPEZIL HCL COMBINATION FOR THE TREATMENT OF MODERATE TO SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG;14MG	NAMZARIC	ABBVIE	N206439	Dec. 23, 2014	RX	CAPSULE, EXTENDED RELEASE	ORAL	8283379	Nov. 22, 2025	MEMANTINE HCL/DONEPEZIL HCL COMBINATION FOR THE TREATMENT OF MODERATE TO SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG;14MG	NAMZARIC	ABBVIE	N206439	Dec. 23, 2014	RX	CAPSULE, EXTENDED RELEASE	ORAL	8338486	Nov. 22, 2025	MEMANTINE HCL/DONEPEZIL HCL COMBINATION FOR THE TREATMENT OF MODERATE TO SEVERE DEMENTIA OF THE ALZHEIMERS TYPE
10MG;14MG	NAMZARIC	ABBVIE	N206439	Dec. 23, 2014	RX	CAPSULE, EXTENDED RELEASE	ORAL	8362085	Nov. 22, 2025	MEMANTINE HCL/DONEPEZIL HCL COMBINATION FOR THE TREATMENT OF MODERATE TO SEVERE DEMENTIA OF THE ALZHEIMERS TYPE

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	March 11, 2025	NEW PRODUCT
5MG/DAY	ADLARITY	CORIUM	N212304	March 11, 2022	RX	SYSTEM	TRANSDERMAL	March 11, 2025	NEW PRODUCT

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Bioactivity Summary:

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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
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.70	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	4.46	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
Cholinesterase	Enzyme	P06276	CHLE_HUMAN		Ki	4.90	CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4D	Enzyme	Q08499	PDE4D_HUMAN		IC50	4.44	CHEMBL
Acetylcholine receptor subunit epsilon	Ion channel	Q04844	ACHE_HUMAN		IC50	7.49	CHEMBL
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		IC50	6.46	CHEMBL
Beta-secretase 1	Enzyme	P56817	BACE1_HUMAN		IC50	5.49	CHEMBL

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External reference:

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ID	Source
E20	PDB_CHEM_ID
006295	NDDF
006296	NDDF
108497001	SNOMEDCT_US
120011-70-3	SECONDARY_CAS_RN
135446	RXNORM
15004	MMSL
178540	MMSL
3152	PUBCHEM_CID
386855006	SNOMEDCT_US

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Pharmaceutical products:

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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
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	25 sections

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