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Identification
NameRivastigmine
Accession NumberDB00989  (APRD00321)
TypeSmall Molecule
GroupsApproved, 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
SynonymLanguageCode
(S)-3-(1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamateNot AvailableNot Available
Ena 713 Free BaseNot AvailableNot Available
m-((S)-1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamateNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Exeloncapsule1.5 mgoralNovartis Pharmaceuticals Corporation2000-04-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule3 mgoralNovartis Pharmaceuticals Corporation2000-04-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule4.5 mgoralNovartis Pharmaceuticals Corporation2000-04-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule6 mgoralNovartis Pharmaceuticals Corporation2000-04-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release4.6 mg/24htransdermalNovartis Pharmaceuticals Corporation2007-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release9.5 mg/24htransdermalNovartis Pharmaceuticals Corporation2007-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release13.3 mg/24htransdermalNovartis Pharmaceuticals Corporation2007-07-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release4.6 mg/24[USP'U]transdermalRebel Distributors Corp2009-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule1.5 mgoralPhysicians Total Care, Inc.2002-04-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule4.5 mgoralPhysicians Total Care, Inc.2005-03-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule6 mgoralPhysicians Total Care, Inc.2005-06-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule3 mgoralPhysicians Total Care, Inc.2007-12-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release9.5 mg/24[USP'U]transdermalPhysicians Total Care, Inc.2008-10-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exelonpatch, extended release4.6 mg/24[USP'U]transdermalPhysicians Total Care, Inc.2009-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exeloncapsule3 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Exeloncapsule4.5 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Exeloncapsule6 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Exelonsolution2 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rivastigminecapsule1.5 mgoralPro Doc LimiteeNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Rivastigminecapsule3 mgoralPro Doc LimiteeNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Rivastigminecapsule4.5 mgoralPro Doc LimiteeNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Rivastigminecapsule6 mgoralPro Doc LimiteeNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot Available
International Brands
NameCompany
Exelon PatchNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number123441-03-2
WeightAverage: 250.3367
Monoisotopic: 250.168127958
Chemical FormulaC14H22N2O2
InChI KeyXSVMFMHYUFZWBK-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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassAmines
Sub ClassAralkylamines
Direct ParentAralkylamines
Alternative Parents
Substituents
  • Aralkylamine
  • Benzenoid
  • Monocyclic benzene moiety
  • Tertiary aliphatic amine
  • Tertiary amine
  • Monocarboxylic acid or derivatives
  • Hydrocarbon derivative
  • Organooxygen compound
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.
PharmacodynamicsRivastigmine 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 actionRivastigmine 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.
AbsorptionNot Available
Volume of distribution
  • 1.8 to 2.7 L/kg
Protein binding40%
Metabolism

Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.

Route of eliminationRivastigmine 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 life1.5 hours
Clearance
  • renal cl=2.1-2.8 L/hr
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 substrateNon-inhibitor0.8928
CYP450 2D6 substrateNon-inhibitor0.8384
CYP450 2C19 substrateNon-inhibitor0.8734
CYP450 3A4 substrateNon-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
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
  • Dr reddys laboratories inc
  • Sun pharmaceutical industries ltd
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral1.5 mg
Capsuleoral3 mg
Capsuleoral4.5 mg
Capsuleoral6 mg
Patch, extended releasetransdermal13.3 mg/24h
Patch, extended releasetransdermal4.6 mg/24h
Patch, extended releasetransdermal4.6 mg/24[USP'U]
Patch, extended releasetransdermal9.5 mg/24h
Patch, extended releasetransdermal9.5 mg/24[USP'U]
Solutionoral2 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
CountryPatent NumberApprovedExpires (estimated)
Canada23157842006-06-272019-01-08
United States49488071992-08-142012-08-14
United States63160231999-01-082019-01-08
Properties
StateSolid
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 RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot 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 Reference
  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
  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
  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
  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
  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
  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. Pubmed# 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
  7. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. Pubmed
External Links
ATC CodesN06DA03
AHFS Codes
  • 12:04.00
PDB Entries
FDA labelDownload (74 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololMay enhance the bradycardic effect of Beta-Blockers.
AcepromazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
AcetophenazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
AcetylcholineAcetylcholinesterase Inhibitors may enhance the adverse/toxic effect of Cholinergic Agonists.
AmisulprideAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
AripiprazoleAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
AtenololMay enhance the bradycardic effect of Beta-Blockers.
BendroflumethiazideMay enhance the bradycardic effect of Beta-Blockers.
BenzquinamideAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
BetaxololMay enhance the bradycardic effect of Beta-Blockers.
BisoprololMay enhance the bradycardic effect of Beta-Blockers.
BretyliumMay enhance the bradycardic effect of Bradycardia-Causing Agents. Bretylium may also enhance atrioventricular (AV) blockade in patients receiving AV blocking agents.
CarbacholAcetylcholinesterase Inhibitors may enhance the adverse/toxic effect of Cholinergic Agonists.
CarphenazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
CarteololMay enhance the bradycardic effect of Beta-Blockers.
CarvedilolMay enhance the bradycardic effect of Beta-Blockers.
ChlormezanoneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ChlorpromazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ChlorprothixeneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ClozapineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
DipyridamoleMay diminish the therapeutic effect of Acetylcholinesterase Inhibitors.
DroperidolAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
EsmololMay enhance the bradycardic effect of Beta-Blockers.
FencamfamineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
FlupentixolAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
FluphenazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
FluspirileneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
HaloperidolAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
LabetalolMay enhance the bradycardic effect of Beta-Blockers.
LacosamideBradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide.
LevobunololMay enhance the bradycardic effect of Beta-Blockers.
LoxapineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
MesoridazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
MethotrimeprazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
MetipranololMay enhance the bradycardic effect of Beta-Blockers.
MetoclopramideRivastigmine may enhance the adverse/toxic effect of Metoclopramide. Specifically, the risk of extrapyramidal adverse reactions may be increased with this combination.
MetoprololMay enhance the bradycardic effect of Beta-Blockers.
MolindoneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
NadololMay enhance the bradycardic effect of Beta-Blockers.
NebivololMay enhance the bradycardic effect of Beta-Blockers.
OlanzapineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
OndansetronAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PaliperidoneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PenbutololMay enhance the bradycardic effect of Beta-Blockers.
PerphenazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PimozideAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PindololMay enhance the bradycardic effect of Beta-Blockers.
PiperacetazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ProchlorperazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PromazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
PropranololMay enhance the bradycardic effect of Beta-Blockers.
QuetiapineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
RemoxiprideAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ReserpineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
RisperidoneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
RuxolitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
SertindoleAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
SotalolMay enhance the bradycardic effect of Beta-Blockers.
SuccinylcholineAcetylcholinesterase Inhibitors may increase the serum concentration of Succinylcholine.
SulpirideAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ThioridazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ThiothixeneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
TimololMay enhance the bradycardic effect of Beta-Blockers.
TofacitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
TrifluoperazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
TriflupromazineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ZiprasidoneAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
ZuclopenthixolAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
Food InteractionsNot Available

Targets

1. Acetylcholinesterase

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Acetylcholinesterase P22303 Details

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
  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
  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
  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
  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
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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. Pubmed# 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
  8. Lalli S, Albanese A: Rivastigmine in Parkinson’s disease dementia. Expert Rev Neurother. 2008 Aug;8(8):1181-8. Pubmed
  9. 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
  10. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. Pubmed
  11. 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

2. Cholinesterase

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Cholinesterase P06276 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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
  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
  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. Pubmed# Birks J: Cholinesterase inhibitors for Alzheimer’s disease. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005593. Pubmed# 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
  5. 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. Pubmed
  6. 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# Lalli S, Albanese A: Rivastigmine in Parkinson’s disease dement
    ia. Expert Rev Neurother. 2008 Aug;8(8):1181-8. Pubmed
  7. 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
  8. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. Pubmed
  9. 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

Enzymes

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

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. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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. Epub 2009 Nov 24. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12