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QuickView for Rivastigmine (compound)


PubChem
Name: rivastigmine
PubChem Compound ID: 10586926
Molecular formula: C14H22N2O2
Molecular weight: 252.345 g/mol
DrugBank
Identification
Name: rivastigmine
Name (isomeric): DB00989
Drug Type: small molecule
Synonyms:
Ena 713 Free Base; Rivastigmine Hydrogen Tartrate
Brand: Exelon Patch, Exelon
Category: Parasympathomimetics, Nootropic Agents, Cholinesterase Inhibitors, Cholinergic Agents, Neuroprotective Agents
CAS number: 123441-03-2
Pharmacology
Indication: For the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.
Pharmacology:
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...
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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 hyd...
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Protein binding: 40%
Biotransformation: 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
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TizanidinePossible antagonism of action
OxybutyninPossible antagonism of action
ChlorprothixenePossible antagonism of action
MesoridazinePossible antagonism of action
LoxapinePossible antagonism of action
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Targets


Enzymes