U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C14H22N2O2.C4H6O6
Molecular Weight 400.4235
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RIVASTIGMINE TARTRATE

SMILES

O[C@H]([C@@H](O)C(O)=O)C(O)=O.CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C

InChI

InChIKey=GWHQHAUAXRMMOT-MBANBULQSA-N
InChI=1S/C14H22N2O2.C4H6O6/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4;5-1(3(7)8)2(6)4(9)10/h7-11H,6H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t11-;1-,2-/m01/s1

HIDE SMILES / InChI
Molecular Formula C14H22N2O2
Molecular Weight 250.3367
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED
Molecular Formula C4H6O6
Molecular Weight 150.0868
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Rivastigmine (sold under the trade name Exelon) is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. Rivastigmine, an acetylcholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase (unlike donepezil, which selectively inhibits acetylcholinesterase). It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain neurotransmitter acetylcholine. Rivastigmine capsules, liquid solution, and patches are used for the treatment of mild to moderate dementia of the Alzheimer's type and for mild to moderate dementia related to Parkinson's disease. Rivastigmine has demonstrated treatment effects on the cognitive (thinking and memory), functional (activities of daily living) and behavioral problems commonly associated with Alzheimer's and Parkinson's disease dementia. In people with either type of dementia, rivastigmine has been shown to provide meaningful symptomatic effects that may allow patients to remain independent and ‘be themselves’ for longer. In particular, it appears to show marked treatment effects in patients showing a more aggressive course of the disease, such as those with younger-onset ages, poor nutritional status, or those experiencing symptoms such as delusions or hallucinations. Side effects may include nausea and vomiting, decreased appetite and weight loss.

CNS Activity

Originator

Approval Year

2000
171
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 54.0 nM [IC50]
Inhibitor
8297
 30.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
EXELON

Approved Use

EXELON PATCH is an acetylcholinesterase inhibitor indicated for treatment of: Mild, moderate, and severe dementia of the Alzheimer’s type (1.1) Mild to moderate dementia associated with Parkinson’s disease (1.2) 1.1 Alzheimer’s Disease EXELON PATCH is indicated for the treatment of dementia of the Alzheimer’s type (AD). Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer’s disease. 1.2 Parkinson’s Disease Dementia EXELON PATCH is indicated for the treatment of mild to moderate dementia associated with Parkinson’s disease (PDD).

Launch Date

2007
Primary
Approved
8429
EXELON

Approved Use

EXELON PATCH is an acetylcholinesterase inhibitor indicated for treatment of: Mild, moderate, and severe dementia of the Alzheimer’s type (1.1) Mild to moderate dementia associated with Parkinson’s disease (1.2) 1.1 Alzheimer’s Disease EXELON PATCH is indicated for the treatment of dementia of the Alzheimer’s type (AD). Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer’s disease. 1.2 Parkinson’s Disease Dementia EXELON PATCH is indicated for the treatment of mild to moderate dementia associated with Parkinson’s disease (PDD).

Launch Date

2007
Primary
Phase IV
63
EXELON

Approved Use

EXELON PATCH is an acetylcholinesterase inhibitor indicated for treatment of: Mild, moderate, and severe dementia of the Alzheimer’s type (1.1) Mild to moderate dementia associated with Parkinson’s disease (1.2) 1.1 Alzheimer’s Disease EXELON PATCH is indicated for the treatment of dementia of the Alzheimer’s type (AD). Efficacy has been demonstrated in patients with mild, moderate, and severe Alzheimer’s disease. 1.2 Parkinson’s Disease Dementia EXELON PATCH is indicated for the treatment of mild to moderate dementia associated with Parkinson’s disease (PDD).

Launch Date

2007
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
37.23 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28670911
6 mg single, oral
dose: 6 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RIVASTIGMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
129.46 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28670911
6 mg single, oral
dose: 6 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RIVASTIGMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.76 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28670911
6 mg single, oral
dose: 6 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RIVASTIGMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
60%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020823s032%2C021025s022lbl.pdf
RIVASTIGMINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
12 mg single, oral
Overdose
Dose: 12 mg
Route: oral
Route: single
Dose: 12 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/28328690
healthy, 3 years
n = 1
Health Status: healthy
Age Group: 3 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/28328690
Other AEs: Cholinergic syndrome...
Other AEs:
Cholinergic syndrome (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28328690
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Other AEs: Respiratory depression, Dizziness...
Other AEs:
Respiratory depression (1 patient)
Dizziness (1 patient)
Nausea (1 patient)
Vomiting (1 patient)
Sweating (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
288 mg single, oral
Overdose
Dose: 288 mg
Route: oral
Route: single
Dose: 288 mg
Co-administed with::
citalopram(280 mg, single)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16440521
unknown, 59 years
n = 1
Health Status: unknown
Age Group: 59 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16440521
Other AEs: Cholinergic syndrome...
Other AEs:
Cholinergic syndrome (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16440521
9.5 mg 6 times / day multiple, transdermal
Overdose
Dose: 9.5 mg, 6 times / day
Route: transdermal
Route: multiple
Dose: 9.5 mg, 6 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
unhealthy, 87 years
n = 1
Health Status: unhealthy
Condition: dementia
Age Group: 87 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (grade 5)
Vomiting (grade 5)
Renal failure (grade 5)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
17.4 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 17.4 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 17.4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
unhealthy
n = 303
Health Status: unhealthy
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
Disc. AE: Vomiting, Nausea...
AEs leading to
discontinuation/dose reduction:
Vomiting (1.7%)
Nausea (1.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (58%)
Vomiting (38%)
Dizziness (27%)
Anorexia (18%)
Headache (16%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
6 mg 1 times / day multiple, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
unhealthy
n = 1189
Health Status: unhealthy
Population Size: 1189
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (8%)
Vomiting (4%)
Anorexia (2%)
Dizziness (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Cholinergic syndrome 1 patient
12 mg single, oral
Overdose
Dose: 12 mg
Route: oral
Route: single
Dose: 12 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/28328690
healthy, 3 years
n = 1
Health Status: healthy
Age Group: 3 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/28328690
Dizziness 1 patient
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Nausea 1 patient
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Respiratory depression 1 patient
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Sweating 1 patient
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Vomiting 1 patient
90 mg single, oral
Overdose
Dose: 90 mg
Route: oral
Route: single
Dose: 90 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
unknown, 38 years
n = 1
Health Status: unknown
Age Group: 38 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16373816
Cholinergic syndrome 1 patient
288 mg single, oral
Overdose
Dose: 288 mg
Route: oral
Route: single
Dose: 288 mg
Co-administed with::
citalopram(280 mg, single)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16440521
unknown, 59 years
n = 1
Health Status: unknown
Age Group: 59 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/16440521
Nausea grade 5
9.5 mg 6 times / day multiple, transdermal
Overdose
Dose: 9.5 mg, 6 times / day
Route: transdermal
Route: multiple
Dose: 9.5 mg, 6 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
unhealthy, 87 years
n = 1
Health Status: unhealthy
Condition: dementia
Age Group: 87 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
Renal failure grade 5
9.5 mg 6 times / day multiple, transdermal
Overdose
Dose: 9.5 mg, 6 times / day
Route: transdermal
Route: multiple
Dose: 9.5 mg, 6 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
unhealthy, 87 years
n = 1
Health Status: unhealthy
Condition: dementia
Age Group: 87 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
Vomiting grade 5
9.5 mg 6 times / day multiple, transdermal
Overdose
Dose: 9.5 mg, 6 times / day
Route: transdermal
Route: multiple
Dose: 9.5 mg, 6 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
unhealthy, 87 years
n = 1
Health Status: unhealthy
Condition: dementia
Age Group: 87 years
Sex: M
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/22663954
Nausea 1.7%
Disc. AE
17.4 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 17.4 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 17.4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
unhealthy
n = 303
Health Status: unhealthy
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
Vomiting 1.7%
Disc. AE
17.4 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 17.4 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 17.4 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
unhealthy
n = 303
Health Status: unhealthy
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022083lbl.pdf
Headache 16%
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Anorexia 18%
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Dizziness 27%
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Vomiting 38%
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Nausea 58%
10 mg 1 times / day multiple, oral (mean)
MTD
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
unhealthy
n = 45
Health Status: unhealthy
Population Size: 45
Sources:
https://pubmed.ncbi.nlm.nih.gov/10362894
Anorexia 2%
Disc. AE
6 mg 1 times / day multiple, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
unhealthy
n = 1189
Health Status: unhealthy
Population Size: 1189
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
Dizziness 2%
Disc. AE
6 mg 1 times / day multiple, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
unhealthy
n = 1189
Health Status: unhealthy
Population Size: 1189
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
Vomiting 4%
Disc. AE
6 mg 1 times / day multiple, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
unhealthy
n = 1189
Health Status: unhealthy
Population Size: 1189
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
Nausea 8%
Disc. AE
6 mg 1 times / day multiple, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
unhealthy
n = 1189
Health Status: unhealthy
Population Size: 1189
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20823lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767
inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2C8
911

CYP2C19
1478

CYP3A5
73
esterase
72
P-gp
257

BCRP
75
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP3A4
1925
 no
CYP3A5
130
 no
BCRP
773
 yes
P-gp
1650
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
esterase
72
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:8874
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8874
ChemicalBook
CB92656938
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB92656938
MolPort
MolPort-003-666-662
https://www.molport.com/shop/molecule-link/MolPort-003-666-662
ZINC
ZINC000000004413
http://zinc15.docking.org/substances/ZINC000000004413
eMolecules
902424
https://www.emolecules.com/cgi-bin/more?vid=902424
PubMed

PubMed

TitleDatePubMed
Galantamine for Alzheimer's disease.
2001
Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine.
2001
Clinical and cost-effectiveness of donepezil, rivastigmine and galantamine for Alzheimer's disease: a rapid and systematic review.
2001
Cholinesterase inhibitors for Alzheimer's disease.
2001
Review of rivastigmine and its clinical applications in Alzheimer's disease and related disorders.
2001 Apr
[Alzheimer dementia. Comparison of the effectiveness of cholinesterase inhibitors and gingko].
2001 Dec 13
Use of cholinesterase inhibitors for treatment of Alzheimer disease.
2001 Jul
Long-Term use of rivastigmine in patients with dementia with Lewy bodies: an open-label trial.
2001 Jun
Alzheimer's disease and related disorders.
2001 May
[Anticholinesterase agents in Alzheimer's disease].
2001 Sep
Brain metabolic and clinical effects of rivastigmine in Alzheimer's disease.
2001 Sep
Rivastigmine for the treatment of dementia and visual hallucinations associated with Parkinson's disease: a case series.
2002
Rivastigmine antagonizes deficits in prepulse inhibition induced by selective immunolesioning of cholinergic neurons in nucleus basalis magnocellularis.
2002
Cholinergic medication for neuroleptic-induced tardive dyskinesia.
2002
Clinical use of cholinomimetic agents: a review.
2002 Aug
Sustained cholinesterase inhibition in AD patients receiving rivastigmine for 12 months.
2002 Aug 27
Cerebral blood flow and cognitive responses to rivastigmine treatment in Alzheimer's disease.
2002 Jan 21
[Rivastigmine for Alzheimer disease; evaluation of preliminary results and of structured assessment of efficacy].
2002 Jan 5
Medical treatment of Alzheimer's disease: past, present, and future.
2002 Jul
Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats.
2002 Jul
Inhibition of acetyl- and butyryl-cholinesterase in the cerebrospinal fluid of patients with Alzheimer's disease by rivastigmine: correlation with cognitive benefit.
2002 Jul
Switching cholinesterase inhibitors in patients with Alzheimer's disease.
2002 Jun
Do cholinesterase inhibitors slow progression of Alzheimer's disease?
2002 Jun
Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.
2002 Mar 19
Centrally acting antiemetics mitigate nausea and vomiting in patients with Alzheimer's disease who receive rivastigmine.
2002 Mar-Apr
Long-term effects of rivastigmine in moderately severe Alzheimer's disease: does early initiation of therapy offer sustained benefits?
2002 May
Prolonged QT interval with rivastigmine.
2002 May
The nicotinic allosteric potentiating ligand galantamine facilitates synaptic transmission in the mammalian central nervous system.
2002 May
Patents

Patents

JP2002524498A
2
JP2007508290A
21

Sample Use Guides

In Vivo Use Guide
Oral (Indicated for mild-to-moderate dementia of the Alzheimer's type): Initial: 1.5 mg PO q12hr; Increase by 1.5 mg/dose q2Weeks; not to exceed 6 mg PO q12hr; Maintenance: 3-6 mg PO q12hr (higher end may be more beneficial); Transdermal (Indicated for mild, moderate, and severe dementia of the Alzheimer's type): Initial: Apply 4.6 mg q24hr; Dose titration: May increase dose to 9.5 mg q24hr after a minimum 4 weeks if well tolerated; after an additional 4 weeks, may further increase to 13.3 mg patch if needed; Mild-to-moderate Alzheimer disease: Effective dosage range is 9.5-13.3 mg/24 hr; Moderate-to-severe Alzheimer disease: Effective dose is 13.3 mg/24 hr; Replace with new patch q24hr
Route of Administration: Other
In Vitro Use Guide
The cytotoxicity of empty and Rivastigmine-loaded PHEA-EDASq17-PS80 micelles was evaluated on mouse neuroblastoma (Neuro2a) cell lines. cCells were seeded in 96 well plate at a density of 5×104 cells/well and grown in Minimum Essential Medium (MEM) with 10% FBS (fetal bovine serum) and 1% of penicillin/streptomycin (10,000U mL−1 penicillin and 10mg mL−1 streptomycin) at 37°C in 5% CO2 humidified atmosphere. After 72h of incubation, cells were treated with Riv-loaded micelles solutions in bidistilled water, having micelle concentrations of 1, 0.5 and 0.25mg/mL. Aliquots of micelle solutions (10 µL) were added to the cells in 100 µL fresh medium and incubated for 6, 24 and 48h. After incubation, 20 µL of MTT reagent solution [3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide, Sigma; 0.5mg mL−1)] were added to each well and plates were incubated at 37°C for 2h; the absorbance was then measured by a multiwell plate reader (Multiskan Ex, Thermo absystems, Finland), at 490nm after background correction. Cells treated with Riv (Rivastigmine) solutions in DMSO, with drug concentration of 0.1, 0.2 and 0.05mg/mL, were used as positive control
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:30:29 GMT 2023
Edited
by admin
on Fri Dec 15 15:30:29 GMT 2023
Record UNII
9IY2357JPE
Record Status Validated (UNII)
Record Version
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RIVASTIGMINE TARTRATE
ORANGE BOOK   USP-RS   VANDF  
Common Name English
RIVASTIGMINE (AS HYDROGEN TARTRATE)
Common Name English
CARBAMIC ACID, N-ETHYL-N-METHYL-, 3-((1S)-1-(DIMETHYLAMINO)ETHYL)PHENYL ESTER, (2R,3R)-2,3-DIHYDROXYBUTANEDIOATE (1:1)
Common Name English
RIVASTIGMINE HYDROGEN TARTRATE [MART.]
Common Name English
SDZ-ENA-713
Code English
RIVASTIGMINE TARTRATE [ORANGE BOOK]
Common Name English
RIVASTIGMINE TARTRATE [USP MONOGRAPH]
Common Name English
ENA-713
Code English
RIVASTIGMINE HYDROGEN TARTRATE [EMA EPAR]
Common Name English
RIVASTIGMINE HYDROGENTARTRATE
Common Name English
RIVASTIGMINE HYDROGEN TARTRATE [EP MONOGRAPH]
Common Name English
RIVASTIGMINE HYDROGEN TARTRATE [MI]
Common Name English
SDZ-ENA 713
Common Name English
RIVASTIGMINE TARTRATE [USP-RS]
Common Name English
ENA 713
Code English
RIVASTIGMINE ACTAVIS
Brand Name English
Rivastigmine hydrogen tartrate [WHO-DD]
Common Name English
RIVASTIGMINE BITARTRATE
Common Name English
RIVASTIGMINE HYDROGEN TARTRATE
EMA EPAR   MART.   MI   WHO-DD  
Common Name English
RIVASTIGMINE TARTRATE [VANDF]
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS RIVASTIGMINE ACTAVIS (AUTHORIZED: PARKINSON DISEASE)
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
NCI_THESAURUS C47792
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
EMA ASSESSMENT REPORTS RIVASTIGMINE ACTAVIS (AUTHORIZED: DEMENTIA)
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
EMA ASSESSMENT REPORTS RIVASTIGMINE ACTAVIS (AUTHORIZED: ALZHEIMER DISEASE)
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
Code System Code Type Description
PUBCHEM
6918078
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
DRUG BANK
DBSALT001252
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
DAILYMED
9IY2357JPE
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
RS_ITEM_NUM
1604858
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
CAS
129101-54-8
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
FDA UNII
9IY2357JPE
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
ChEMBL
CHEMBL636
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
MERCK INDEX
m9639
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY Merck Index
EVMPD
SUB04257MIG
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
SMS_ID
100000093043
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
EPA CompTox
DTXSID8047840
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
RXCUI
994808
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY RxNorm
NCI_THESAURUS
C47707
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
CHEBI
64358
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
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WIKIPEDIA
Rivastigmine tartrate
Created by admin on Fri Dec 15 15:30:29 GMT 2023 , Edited by admin on Fri Dec 15 15:30:29 GMT 2023
PRIMARY
Related Record Type Details
Structure of RIVASTIGMINE TARTRATE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
USP
Structure of RIVASTIGMINE TARTRATE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
EP
Structure of RIVASTIGMINE
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of RIVASTIGMINE, (R)-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 3-METHOXYACETOPHENONE
IMPURITY -> PARENT
UNSPECIFIED
EP
Structure of 3-NITROPHENYL ETHYL(METHYL)CARBAMATE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 3-(1-(DIMETHYLAMINO)ETHYL)PHENYL DIMETHYLCARBAMATE, (1S)-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of NAP-226-90
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of N,N-DIMETHYL-1-(3-(4-NITROPHENOXY)PHENYL)ETHANAMINE, (S)-
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 3-METHOXY-.ALPHA.-METHYLBENZYL ALCOHOL, (±)-
IMPURITY -> PARENT
UNSPECIFIED
EP
Structure of 3-(1-(DIMETHYLAMINO)ETHYL)PHENYL DIMETHYLCARBAMATE, (1S)-
IMPURITY -> PARENT
UNSPECIFIED
EP
Structure of 1-(3-METHOXYPHENYL)-N,N-DIMETHYLETHANAMINE, (1S)-
IMPURITY -> PARENT
UNSPECIFIED
EP
Structure of NAP-226-90
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of Di-p-toluoyl-D-tartaric acid
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 3-(1-(METHYLAMINO)ETHYL)PHENYL ETHYL(METHYL)CARBAMATE, (1S)-
IMPURITY -> PARENT
UNSPECIFIED
EP
Related Record Type Details
Structure of RIVASTIGMINE
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