Identification

Name
Rivastigmine
Accession Number
DB00989  (APRD00321)
Type
Small Molecule
Groups
Approved, Investigational
Description

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.

Structure
Thumb
Synonyms
  • (S)-3-(1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
  • m-((S)-1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
  • Rivastigmina
External IDs
ENA-713D / ONO-2540 / SDZ-212-713 / SDZ-212713
Product Ingredients
IngredientUNIICASInChI Key
Rivastigmine tartrate9IY2357JPE129101-54-8GWHQHAUAXRMMOT-MBANBULQSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Rivastigmine Patch 10Patch18 mgTransdermalActavis Pharma CompanyNot applicableNot applicableCanada
Act Rivastigmine Patch 5Patch9 mgTransdermalActavis Pharma CompanyNot applicableNot applicableCanada
ExelonPatch9.5 mg/24hoursTransdermalNovartis Europharm Limited1998-05-12Not applicableEu
ExelonPatch, extended release4.6 mg/24[USP'U]TransdermalPhysicians Total Care, Inc.2009-10-07Not applicableUs
ExelonCapsule6 mgOralNovartis2000-05-15Not applicableCanada
ExelonPatch, extended release4.6 mg/24hTransdermalNovartis Pharmaceuticals Corporation2007-07-06Not applicableUs
ExelonSolution2 mg/mlOralNovartis Europharm Limited1998-05-12Not applicableEu
ExelonPatch4.6 mg/24hoursTransdermalNovartis Europharm Limited1998-05-12Not applicableEu
ExelonPatch4.6 mg/24hoursTransdermalNovartis Europharm Limited1998-05-12Not applicableEu
ExelonCapsule4.5 mg/1OralNovartis2000-04-30Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rivastigmineCapsule3 mgOralApotex Corporation2010-04-07Not applicableCanada
Apo-rivastigmineCapsule6 mgOralApotex Corporation2010-04-07Not applicableCanada
Apo-rivastigmineCapsule4.5 mgOralApotex Corporation2010-04-07Not applicableCanada
Apo-rivastigmineCapsule1.5 mgOralApotex Corporation2010-04-07Not applicableCanada
Auro-rivastigmineCapsule6 mgOralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-rivastigmineCapsule1.5 mgOralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-rivastigmineCapsule4.5 mgOralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-rivastigmineCapsule3 mgOralAuro Pharma Inc2016-04-12Not applicableCanada
Dom-rivastigmineCapsule6.0 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-rivastigmineCapsule1.5 mgOralDominion PharmacalNot applicableNot applicableCanada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Rivastigmine 3m Health Care Ltd.Rivastigmine (9.5 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (9.5 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (4.6 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (4.6 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (4.6 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (9.5 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (9.5 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine 3m Health Care Ltd.Rivastigmine (4.6 mg/24h)PatchTransdermal3 M Pharmaceuticals2014-04-032014-09-18Eu
Rivastigmine TevaRivastigmine (6 mg)CapsuleOralTeva Pharma B.V.2009-04-172012-09-27Eu
Rivastigmine TevaRivastigmine (1.5 mg)CapsuleOralTeva Pharma B.V.2009-04-172012-09-27Eu
International/Other Brands
Exelon Patch
Categories
UNII
PKI06M3IW0
CAS number
123441-03-2
Weight
Average: 250.3367
Monoisotopic: 250.168127958
Chemical Formula
C14H22N2O2
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

Pharmacology

Indication

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

Associated Conditions
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
Human
ACholinesterase
inhibitor
Human
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Rivastigmine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Rivastigmine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Rivastigmine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Rivastigmine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Rivastigmine.
6-Deoxyerythronolide BThe metabolism of Rivastigmine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Rivastigmine.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Rivastigmine.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Rivastigmine.
AcalabrutinibThe metabolism of Rivastigmine can be decreased when combined with Acalabrutinib.
Food Interactions
Not Available

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. [PubMed:12369954]
  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. [PubMed:10066203]
  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. [PubMed:15336465]
  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. [PubMed:11568422]
  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. [PubMed:15590953]
  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. [PubMed:19370562]
  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. [PubMed:19470293]
  8. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [PubMed:14587496]
External Links
Human Metabolome Database
HMDB0015124
KEGG Drug
D03822
KEGG Compound
C11766
PubChem Compound
77991
PubChem Substance
46507452
ChemSpider
70377
BindingDB
11682
ChEBI
8874
ChEMBL
CHEMBL636
Therapeutic Targets Database
DAP000149
PharmGKB
PA451262
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rivastigmine
ATC Codes
N06DA03 — Rivastigmine
AHFS Codes
  • 12:04.00 — Parasympathomemetic (Cholinergic) Agents
FDA label
Download (74 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAutonomic Failure / Idiopathic orthostatic hypotension1
1CompletedNot AvailableCocaine Abuse / Dependence, Cocaine / Substance Abuse1
1CompletedNot AvailableMethamphetamine Abuse / Methamphetamine Dependence / Substance Abuse1
1CompletedTreatmentAlzheimer's Disease (AD) / Central Nervous System Diseases1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentSubstance-Related Disorders1
1RecruitingOtherBioequivalence1
1, 2CompletedTreatmentDown Syndrome (DS)1
2Unknown StatusTreatmentDementias / Progressive Supranuclear Palsy (PSP)1
3CompletedTreatmentAlzheimer's Disease (AD)5
3CompletedTreatmentAlzheimer's Disease (AD) / Cognition Disorders1
3CompletedTreatmentAlzheimer's Disease (AD) / Dementia, Alzheimer Type1
3CompletedTreatmentAlzheimer's Disease (AD) / Dementias1
3CompletedTreatmentApathy / No Dementia / Parkinson's Disease (PD)1
3CompletedTreatmentCognitive Impairments / Traumatic Brain Injury (TBI)1
3CompletedTreatmentDelirium1
3CompletedTreatmentDementia, Vascular2
3CompletedTreatmentParkinson's Disease Dementia (PDD)1
3CompletedTreatmentTraumatic Brain Injury (TBI)1
3RecruitingTreatmentProgressive Supranuclear Palsy (PSP)1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentCognitive Symptoms1
3TerminatedTreatmentDelirium1
4CompletedNot AvailableTraumatic Brain Injury With Persistent Cognitive Deficits1
4CompletedOtherAlzheimer's Disease (AD)1
4CompletedPreventionDelirium1
4CompletedPreventionDelirium / Postoperative Cognitive Dysfunction1
4CompletedTreatmentAlzheimer Dementia (AD)1
4CompletedTreatmentAlzheimer's Disease (AD)11
4CompletedTreatmentCognitive Impairments1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Neurocognitive Disturbance1
4CompletedTreatmentMild Cognitive Impairment (MCI) / Parkinson's Disease (PD)1
4CompletedTreatmentMild to Moderate Alzheimer's Disease1
4Not Yet RecruitingTreatmentAlzheimer's Disease (AD)1
4RecruitingTreatmentAlzheimer's Disease (AD) / CVA (Cerebrovascular Accident)1
4SuspendedTreatmentHealthy Volunteers1
4TerminatedPreventionParkinson's Disease (PD)1
4TerminatedTreatmentCognitive Impairments / Disseminated Sclerosis1
4TerminatedTreatmentDelirium1
4TerminatedTreatmentHealthy Volunteers1
4Unknown StatusTreatmentParkinson's Disease (PD)1
Not AvailableActive Not RecruitingBasic ScienceAlzheimer's Disease (AD)1
Not AvailableCompletedNot AvailableAlzheimer's Disease (AD)1
Not AvailableCompletedNot AvailableDiffuse Lewy Body Disease1
Not AvailableCompletedBasic ScienceAlzheimer's Disease (AD)1
Not AvailableCompletedTreatmentAlzheimer's Disease (AD)1
Not AvailableCompletedTreatmentDown Syndrome (DS)1
Not AvailableCompletedTreatmentRivastigmine Toxicity1
Not AvailableTerminatedNot AvailableMild Cognitive Disorder / Mild Cognitive Impairment (MCI)1
Not AvailableTerminatedTreatmentAlzheimer's Disease (AD) / Dementias1

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
PatchTransdermal9 mg
CapsuleOral6.0 mg
CapsuleOral1.5 mg/1
CapsuleOral3 mg
CapsuleOral3 mg/1
CapsuleOral4.5 mg/1
CapsuleOral4.5 mg
CapsuleOral6 mg
PatchTransdermal13.3 mg/24hours
PatchTransdermal4.6 mg/24hours
PatchTransdermal9.5 mg/24hours
Patch, extended releaseTransdermal4.6 mg/24[USP'U]
Patch, extended releaseTransdermal9.5 mg/24[USP'U]
SolutionOral2 mg/1mL
SolutionOral2 mg/ml
SolutionOral2 mg
CapsuleOral1.5 mg
PatchTransdermal9.5 mg
PatchTransdermal13.3 mg
PatchTransdermal4.6 mg
Tablet, orally disintegratingOral1.5 mg
Tablet, orally disintegratingOral3 mg
Tablet, orally disintegratingOral4.5 mg
Tablet, orally disintegratingOral6 mg
CapsuleOral3.0 mg
PatchTransdermal13.3 mg/24h
Patch, extended releaseTransdermal13.3 mg/24h
Patch, extended releaseTransdermal4.6 mg/24h
Patch, extended releaseTransdermal9.5 mg/24h
PatchTransdermal4.6 mg/24h
PatchTransdermal9.5 mg/24h
CapsuleOral6 mg/1
Patch, extended releaseTransdermal13.3 mg/1
Patch, extended releaseTransdermal4.6 mg/1
Patch, extended releaseTransdermal9.5 mg/1
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)
US4948807No1990-08-142012-08-14Us
CA2315784No2006-06-272019-01-08Canada
US6335031No2002-01-012019-01-08Us
US6316023No2001-11-132019-01-08Us

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

Taxonomy

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
Phenoxy compound / Aralkylamine / Carbamic acid ester / Carbonic acid derivative / Tertiary amine / Tertiary aliphatic amine / Amine / Hydrocarbon derivative / Organic oxide / Organopnictogen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
carbamate ester, tertiary amino compound (CHEBI:8874)

Targets

Details
1. Acetylcholinesterase
Kind
Protein
Organism
Human
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. [PubMed:10587286]
  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. [PubMed:10673128]
  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. [PubMed:10713582]
  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. [PubMed:11078030]
  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. [PubMed:11139819]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  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. [PubMed:19370562]
  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. [PubMed:19470293]
  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. [PubMed:18671661]
  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. [PubMed:18044073]
  11. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [PubMed:14587496]
  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. [PubMed:12636181]
Kind
Protein
Organism
Human
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. [PubMed:11752352]
  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. [PubMed:11078030]
  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. [PubMed:11139819]
  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. [PubMed:19370562]
  5. Birks J: Cholinesterase inhibitors for Alzheimer's disease. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593. [PubMed:16437532]
  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. [PubMed:19470293]
  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. [PubMed:19420308]
  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. [PubMed:19374459]
  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. [PubMed:18671661]
  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. [PubMed:18044073]
  11. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. [PubMed:14587496]
  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. [PubMed:12636181]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Jann MW, Shirley KL, Small GW: Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors. Clin Pharmacokinet. 2002;41(10):719-39. doi: 10.2165/00003088-200241100-00003. [PubMed:12162759]

Drug created on June 13, 2005 07:24 / Updated on November 18, 2018 04:47