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rivastigmine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
acetylcholinesterase inhibitors	2392	123441-03-2

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
9	mg	O
9.50	mg	TD

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	72 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	12 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.40 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.30 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.80 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.60 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
April 21, 2000	FDA	NOVARTIS
May 12, 1998	EMA

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
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

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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	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

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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
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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06DA03	NERVOUS SYSTEM PSYCHOANALEPTICS ANTI-DEMENTIA DRUGS Anticholinesterases
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
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

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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
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

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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	8.32	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

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	IC50	7.43	CHEMBL	IUPHAR
Cholinesterase	Enzyme	P06276	CHLE_HUMAN	INHIBITOR	IC50	7.52	CHEMBL	IUPHAR
Acetylcholinesterase	Enzyme		ACES_MOUSE		IC50	5.95	CHEMBL
Butyrylcholinesterase; Protein Bche	Enzyme		Q9JKC1_RAT		IC50	6.46	CHEMBL
Acetylcholinesterase	Enzyme		ACES_RAT		IC50	5.74	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		IC50	5.38	CHEMBL
Acetylcholinesterase	Enzyme		ACES_BOVIN		IC50	6.21	CHEMBL
Cholinesterase	Enzyme		CHLE_MOUSE		IC50	5.80	CHEMBL
Butyrylcholinesterase	Enzyme		Q9N1N9_HORSE		IC50	6.80	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		IC50	6.08	CHEMBL

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External reference:

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ID	Source
007559	NDDF
007560	NDDF
126131008	SNOMEDCT_US
129101-54-8	SECONDARY_CAS_RN
174208	MMSL
183379	RXNORM
23978	MMSL
31947	MMSL
323368009	SNOMEDCT_US
395868008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
Exelon	HUMAN PRESCRIPTION DRUG LABEL	1	21695-357	PATCH, EXTENDED RELEASE	4.60 mg	TRANSDERMAL	NDA	16 sections

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