Identification

Summary

Rivastigmine is a cholinesterase inhibitor used to treat mild to moderate dementia in Alzheimer's and Parkinson's.

Brand Names
Exelon, Nimvastid, Prometax
Generic Name
Rivastigmine
DrugBank Accession Number
DB00989
Background

Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 250.3367
Monoisotopic: 250.168127958
Chemical Formula
C14H22N2O2
Synonyms
  • (S)-3-(1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
  • m-((S)-1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
  • Rivastigmina
  • Rivastigmine
External IDs
  • ENA-713D
  • ONO-2540
  • SDZ-212-713
  • SDZ-212713

Pharmacology

Indication

For the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Rivastigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. While the precise mechanism of rivastigmine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, rivastigmine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact.

Mechanism of action

Rivastigmine is a carbamate derivative that is structurally related to physostigmine, but not to donepezil and tacrine. The precise mechanism of rivastigmine has not been fully determined, but it is suggested that rivastigmine binds reversibly with and inactivates chlolinesterase (eg. acetylcholinesterase, butyrylcholinesterase), preventing the hydrolysis of acetycholine, and thus leading to an increased concentration of acetylcholine at cholinergic synapses. The anticholinesterase activity of rivastigmine is relatively specific for brain acetylcholinesterase and butyrylcholinesterase compared with those in peripheral tissues.

TargetActionsOrganism
AAcetylcholinesterase
inhibitor
Humans
ACholinesterase
inhibitor
Humans
Absorption

Not Available

Volume of distribution
  • 1.8 to 2.7 L/kg
Protein binding

40%

Metabolism

Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.

Route of elimination

Rivastigmine is extensively metabolized primarily via cholinesterase-mediated hydrolysis to the decarbamylated metabolite NAP226-90. Renal excretion of the metabolites is the major route of elimination. Less than 1% of the administered dose is excreted in the feces.

Half-life

1.5 hours

Clearance
  • renal cl=2.1-2.8 L/hr
Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcebutololAcebutolol may increase the bradycardic activities of Rivastigmine.
AcetylcholineThe risk or severity of adverse effects can be increased when Rivastigmine is combined with Acetylcholine.
AclidiniumRivastigmine may increase the neuromuscular blocking activities of Aclidinium.
AlfentanilAlfentanil may increase the bradycardic activities of Rivastigmine.
AmantadineThe therapeutic efficacy of Amantadine can be decreased when used in combination with Rivastigmine.
AmifampridineThe risk or severity of adverse effects can be increased when Rivastigmine is combined with Amifampridine.
AmiodaroneRivastigmine may increase the bradycardic activities of Amiodarone.
AmitriptylineThe therapeutic efficacy of Amitriptyline can be decreased when used in combination with Rivastigmine.
AmlodipineAmlodipine may increase the bradycardic activities of Rivastigmine.
AmobarbitalThe therapeutic efficacy of Amobarbital can be decreased when used in combination with Rivastigmine.
Interactions
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Food Interactions
  • Take with food. Administering rivastigmine capsules with food delays absorption but increases the AUC.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Rivastigmine tartrate9IY2357JPE129101-54-8GWHQHAUAXRMMOT-MBANBULQSA-N
Product Images
International/Other Brands
Exelon Patch
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act Rivastigmine Patch 10Patch18 mg / 10 sq cmTransdermalActavis Pharma CompanyNot applicableNot applicableCanada flag
Act Rivastigmine Patch 5Patch9 mg / 5 sq cmTransdermalActavis Pharma CompanyNot applicableNot applicableCanada flag
ExelonPatch4.6 mg/24hoursTransdermalNovartis Europharm Limited2020-12-16Not applicableEU flag
ExelonPatch13.3 mg/24hoursTransdermalNovartis Europharm Limited2016-09-08Not applicableEU flag
ExelonCapsule1.5 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
ExelonCapsule4.5 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
ExelonCapsule6 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
ExelonCapsule4.5 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
ExelonCapsule4.5 mg/1OralPhysicians Total Care, Inc.2005-03-03Not applicableUS flag
ExelonPatch9.5 mg/24hoursTransdermalNovartis Europharm Limited2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-rivastigmineCapsule6 mgOralApotex Corporation2010-04-07Not applicableCanada flag
Apo-rivastigmineCapsule1.5 mgOralApotex Corporation2010-04-07Not applicableCanada flag
Apo-rivastigmineCapsule4.5 mgOralApotex Corporation2010-04-07Not applicableCanada flag
Apo-rivastigmineCapsule3 mgOralApotex Corporation2010-04-07Not applicableCanada flag
Auro-rivastigmineCapsule4.5 mgOralAuro Pharma Inc2016-04-12Not applicableCanada flag
Auro-rivastigmineCapsule3 mgOralAuro Pharma Inc2016-04-12Not applicableCanada flag
Auro-rivastigmineCapsule6 mgOralAuro Pharma Inc2016-04-12Not applicableCanada flag
Auro-rivastigmineCapsule1.5 mgOralAuro Pharma Inc2016-04-12Not applicableCanada flag
Dom-rivastigmineCapsule4.5 mgOralDominion PharmacalNot applicableNot applicableCanada flag
Dom-rivastigmineCapsule3.0 mgOralDominion PharmacalNot applicableNot applicableCanada flag

Categories

ATC Codes
N06DA03 — Rivastigmine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenoxy compounds. These are aromatic compounds contaning a phenoxy group.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Phenoxy compounds
Direct Parent
Phenoxy compounds
Alternative Parents
Aralkylamines / Carbamate esters / Trialkylamines / Organic carbonic acids and derivatives / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Amine / Aralkylamine / Aromatic homomonocyclic compound / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Hydrocarbon derivative / Organic nitrogen compound / Organic oxide / Organic oxygen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
carbamate ester, tertiary amino compound (CHEBI:8874)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
PKI06M3IW0
CAS number
123441-03-2
InChI Key
XSVMFMHYUFZWBK-NSHDSACASA-N
InChI
InChI=1S/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1
IUPAC Name
3-[(1S)-1-(dimethylamino)ethyl]phenyl N-ethyl-N-methylcarbamate
SMILES
CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C

References

Synthesis Reference

Venkata Naga Brahmeswara Rao Mandava, Venkata Reddy Vajrala, Ganesh Varanasi, Vijay Kumar Adla, Mukund Reddy Jambula, Vijaypal Reddy Kanumathi Reddy, "PREPARATION OF RIVASTIGMINE AND ITS SALTS." U.S. Patent US20080255383, issued October 16, 2008.

US20080255383
General References
  1. Camps P, Munoz-Torrero D: Cholinergic drugs in pharmacotherapy of Alzheimer's disease. Mini Rev Med Chem. 2002 Feb;2(1):11-25. [Article]
  2. Rosler M, Anand R, Cicin-Sain A, Gauthier S, Agid Y, Dal-Bianco P, Stahelin HB, Hartman R, Gharabawi M: Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. BMJ. 1999 Mar 6;318(7184):633-8. [Article]
  3. Finkel SI: Effects of rivastigmine on behavioral and psychological symptoms of dementia in Alzheimer's disease. Clin Ther. 2004 Jul;26(7):980-90. [Article]
  4. Rosler M, Retz W, Retz-Junginger P, Dennler HJ: Effects of two-year treatment with the cholinesterase inhibitor rivastigmine on behavioural symptoms in Alzheimer's disease. Behav Neurol. 1998;11(4):211-216. [Article]
  5. Emre M, Aarsland D, Albanese A, Byrne EJ, Deuschl G, De Deyn PP, Durif F, Kulisevsky J, van Laar T, Lees A, Poewe W, Robillard A, Rosa MM, Wolters E, Quarg P, Tekin S, Lane R: Rivastigmine for dementia associated with Parkinson's disease. N Engl J Med. 2004 Dec 9;351(24):2509-18. [Article]
  6. Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE: Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2. [Article]
  7. Naik RS, Hartmann J, Kiewert C, Duysen EG, Lockridge O, Klein J: Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice. J Pharm Pharm Sci. 2009;12(1):79-85. [Article]
  8. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [Article]
Human Metabolome Database
HMDB0015124
KEGG Drug
D03822
KEGG Compound
C11766
PubChem Compound
77991
PubChem Substance
46507452
ChemSpider
70377
BindingDB
10620
RxNav
183379
ChEBI
8874
ChEMBL
CHEMBL636
ZINC
ZINC000000004413
Therapeutic Targets Database
DAP000149
PharmGKB
PA451262
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rivastigmine
FDA label
Download (74 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableTraumatic Brain Injury With Persistent Cognitive Deficits1
4CompletedOtherAlzheimer's Disease (AD)1
4CompletedPreventionDelirium1
4CompletedPreventionDelirium / POCD - Postoperative Cognitive Dysfunction1
4CompletedTreatmentAlzheimer's Disease (AD)12
4CompletedTreatmentAlzheimer's Disease (AD) / Cerebrovascular Accident1
4CompletedTreatmentCognitive Impairment (CI)1
4CompletedTreatmentDementia of the Alzheimer's Type1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Neurocognitive Disturbance1
4CompletedTreatmentMild Cognitive Impairment (MCI) / Parkinson's Disease (PD)1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
  • Dr reddys laboratories inc
  • Sun pharmaceutical industries ltd
  • Watson laboratories inc
Packagers
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Doctor Reddys Laboratories Ltd.
  • LTS Lohmann Therapy Systems Corp.
  • Novartis AG
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Sandoz
  • Sun Pharmaceutical Industries Ltd.
  • Vangard Labs Inc.
  • Watson Pharmaceuticals
Dosage Forms
FormRouteStrength
PatchTransdermal18 mg / 10 sq cm
PatchTransdermal9 mg / 5 sq cm
PatchTransdermal
Drug delivery systemTransdermal18 mg
CapsuleOral1.5 mg/1
CapsuleOral3 mg/1
CapsuleOral4.5 mg/1
PatchTransdermal13.3 mg/24hours
PatchTransdermal13.3 MG/24ORE
PatchTransdermal4.6 MG/24ORE
PatchTransdermal4.6 mg/24hours
PatchTransdermal9.5 mg/24hours
PatchTransdermal9.5 MG/24ORE
Patch, extended releaseTransdermal13.3 MG/24hr
Patch, extended releaseTransdermal4.6 MG/24hr
Patch, extended releaseTransdermal4.6 mg/24[USP'U]
Patch, extended releaseTransdermal9.5 MG/24hr
Patch, extended releaseTransdermal9.5 mg/24[USP'U]
SolutionOral2 mg/1mL
SolutionOral2 mg/ml
SolutionOral2 mg / mL
Capsule, coatedOral3 mg
Capsule, coatedOral6 mg
PlasterCutaneous13.3 MG
CapsuleOral3.0 MG
CapsuleOral4.5 mg
PlasterCutaneous4.6 MG
CapsuleOral6 mg
CapsuleOral6.0 MG
PlasterCutaneous9.5 MG
SyrupOral2 mg/1ml
SolutionOral
PatchTransdermal9.5 mg / 24 hour
Patch, extended releaseTransdermal18.00 mg/10cm2
PatchTransdermal13.3 mg / 24 hour
Patch, extended releaseTransdermal27.000 mg
PatchTransdermal4.6 mg / 24 hour
Patch, extended releaseTransdermal9 mg/5cm2
Tablet, effervescent
Capsule, coatedOral4.5 mg
PatchTransdermal18 mg
PatchTransdermal9 mg
Tablet, orally disintegratingOral1.5 mg
Tablet, orally disintegratingOral3 mg
Tablet, orally disintegratingOral4.5 mg
Tablet, orally disintegratingOral6 mg
PlasterTransdermal
Capsule, coatedOral1.5 mg
CapsuleOral
PatchTopical; Transdermal13.3 mg
PatchTransdermal4.6 mg/24hr
PatchTransdermal9.5 mg/24hr
PatchTransdermal13.3 mg/24h
PatchTransdermal4.6 mg/24h
PatchTransdermal9.5 mg/24h
Patch, extended releaseTransdermal13.3 mg/24h
Patch, extended releaseTransdermal4.6 mg/24h
Patch, extended releaseTransdermal9.5 mg/24h
CapsuleOral6 mg/1
Patch, extended releaseTransdermal13.3 mg/1
Patch, extended releaseTransdermal4.6 mg/1
Patch, extended releaseTransdermal9.5 mg/1
CapsuleOral1.5 mg
CapsuleOral3 mg
Prices
Unit descriptionCostUnit
Exelon 30 4.6 mg/24hr Patches Box252.18USD box
Exelon 30 9.5 mg/24hr Patches Box252.18USD box
Exelon 4.6 mg/24hr patch8.08USD patch
Exelon 9.5 mg/24hr patch8.08USD patch
Exelon 1.5 mg capsule4.81USD capsule
Exelon 3 mg capsule4.81USD capsule
Exelon 4.5 mg capsule4.81USD capsule
Exelon 6 mg capsule4.81USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US4948807No1990-08-142012-08-14US flag
CA2315784No2006-06-272019-01-08Canada flag
US6335031No2002-01-012019-01-08US flag
US6316023No2001-11-132019-01-08US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.04 mg/mLALOGPS
logP2.45ALOGPS
logP2.41ChemAxon
logS-2.1ALOGPS
pKa (Strongest Basic)8.89ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.78 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity73.37 m3·mol-1ChemAxon
Polarizability28.53 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9853
Caco-2 permeable+0.7001
P-glycoprotein substrateNon-substrate0.6571
P-glycoprotein inhibitor INon-inhibitor0.7919
P-glycoprotein inhibitor IINon-inhibitor0.8756
Renal organic cation transporterNon-inhibitor0.8406
CYP450 2C9 substrateNon-substrate0.7993
CYP450 2D6 substrateNon-substrate0.6659
CYP450 3A4 substrateSubstrate0.5932
CYP450 1A2 substrateNon-inhibitor0.609
CYP450 2C9 inhibitorNon-inhibitor0.8928
CYP450 2D6 inhibitorNon-inhibitor0.8384
CYP450 2C19 inhibitorNon-inhibitor0.8734
CYP450 3A4 inhibitorNon-inhibitor0.9545
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8062
Ames testNon AMES toxic0.5279
CarcinogenicityNon-carcinogens0.5858
BiodegradationNot ready biodegradable0.9463
Rat acute toxicity3.4167 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9355
hERG inhibition (predictor II)Non-inhibitor0.8986
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-0090000000-cb0be842083fd5bb182c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-1090000000-d7335c9ff57f34335d3c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052r-9050000000-2739573cc72accdb3593
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052r-9010000000-827dd9cfa5e61c705617
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052r-9000000000-42e62adc5ba35b92f991
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9000000000-717721d4d1b05cfae7d9

Targets

Drugtargets2
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Details
1. Acetylcholinesterase
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine hydrolase activity
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P22303
Uniprot Name
Acetylcholinesterase
Molecular Weight
67795.525 Da
References
  1. Kennedy JS, Polinsky RJ, Johnson B, Loosen P, Enz A, Laplanche R, Schmidt D, Mancione LC, Parris WC, Ebert MH: Preferential cerebrospinal fluid acetylcholinesterase inhibition by rivastigmine in humans. J Clin Psychopharmacol. 1999 Dec;19(6):513-21. [Article]
  2. Goldblum D, Garweg JG, Bohnke M: Topical rivastigmine, a selective acetylcholinesterase inhibitor, lowers intraocular pressure in rabbits. J Ocul Pharmacol Ther. 2000 Feb;16(1):29-35. [Article]
  3. Grossberg GT, Stahelin HB, Messina JC, Anand R, Veach J: Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medications. Int J Geriatr Psychiatry. 2000 Mar;15(3):242-7. [Article]
  4. Stahl SM: The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different. J Clin Psychiatry. 2000 Oct;61(10):710-1. [Article]
  5. Gottwald MD, Rozanski RI: Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer's disease: review and current status. Expert Opin Investig Drugs. 1999 Oct;8(10):1673-1682. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE: Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2. [Article]
  8. Naik RS, Hartmann J, Kiewert C, Duysen EG, Lockridge O, Klein J: Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice. J Pharm Pharm Sci. 2009;12(1):79-85. [Article]
  9. Lalli S, Albanese A: Rivastigmine in Parkinson's disease dementia. Expert Rev Neurother. 2008 Aug;8(8):1181-8. doi: 10.1586/14737175.8.8.1181. [Article]
  10. Onor ML, Trevisiol M, Aguglia E: Rivastigmine in the treatment of Alzheimer's disease: an update. Clin Interv Aging. 2007;2(1):17-32. [Article]
  11. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [Article]
  12. Greig NH, Lahiri DK, Sambamurti K: Butyrylcholinesterase: an important new target in Alzheimer's disease therapy. Int Psychogeriatr. 2002;14 Suppl 1:77-91. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Identical protein binding
Specific Function
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name
BCHE
Uniprot ID
P06276
Uniprot Name
Cholinesterase
Molecular Weight
68417.575 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Stahl SM: The new cholinesterase inhibitors for Alzheimer's disease, Part 1: their similarities are different. J Clin Psychiatry. 2000 Oct;61(10):710-1. [Article]
  3. Gottwald MD, Rozanski RI: Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer's disease: review and current status. Expert Opin Investig Drugs. 1999 Oct;8(10):1673-1682. [Article]
  4. Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE: Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2. [Article]
  5. Birks J: Cholinesterase inhibitors for Alzheimer's disease. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593. [Article]
  6. Naik RS, Hartmann J, Kiewert C, Duysen EG, Lockridge O, Klein J: Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice. J Pharm Pharm Sci. 2009;12(1):79-85. [Article]
  7. Smith DA: Treatment of Alzheimer's disease in the long-term-care setting. Am J Health Syst Pharm. 2009 May 15;66(10):899-907. doi: 10.2146/ajhp070622. [Article]
  8. Bassil N, Grossberg GT: Novel regimens and delivery systems in the pharmacological treatment of Alzheimer's disease. CNS Drugs. 2009;23(4):293-307. [Article]
  9. Lalli S, Albanese A: Rivastigmine in Parkinson's disease dementia. Expert Rev Neurother. 2008 Aug;8(8):1181-8. doi: 10.1586/14737175.8.8.1181. [Article]
  10. Onor ML, Trevisiol M, Aguglia E: Rivastigmine in the treatment of Alzheimer's disease: an update. Clin Interv Aging. 2007;2(1):17-32. [Article]
  11. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [Article]
  12. Greig NH, Lahiri DK, Sambamurti K: Butyrylcholinesterase: an important new target in Alzheimer's disease therapy. Int Psychogeriatr. 2002;14 Suppl 1:77-91. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 04, 2021 10:27