Dementia Medications - Kinder Flashcards
Donepezil
AChE inhibitor
approved for dementia
galantamine
AChE inhibitor
approved for dementia
rivastigmine
AChE inhibitor
approved for dementia
tacrine
AChE inhibitor
approved for dementia
pralidoxome
cholinesterase reactivator
prevalence of AD
20% over 85yo
AD path
tau tangles, amyloid plaques
also - loss of cholinergic neurons
-marked decrase choline acetyltransferase
also possible excess of glutamate
direct acting cholinomimetic
bind to and activate mAChR and nAChR
indirect acting cholinomimetic
AChE inhibitor
cholinesterases
butylcholinesterase
acetylcholinesterase
target of AChE inhibitors - acetylcholinesterase
AChE
hydrolysis of ACh to choline and acetate
alcohol AChE inhibitors
alcohol group and quaternary ammonium
-positive charge
noncovalent and reversible, short lived
-binding to AChE
edrophonium
AChE inhibitor - alcohol
carbamic acid ester AChE inhibitors
carbamic acid ester of alcohol
-quaternary or tertiary ammonium group
positive charge or neurtal
neostigmine
carbamic acid ester AChE inhibitor
pyridostigmine
carbamic acid ester AChE inhibitor
physostigmine
carbamic acid ester AChE inhibitor
carbaryl
carbamic acid ester AChE inhibitor
binding of carbamic acid ester AChE inhibitor
to AChE - two step oricess
covalent bond of carbamoylated enzyme - more resistant to second step hydration
organophosphates
covalent and irreversible bind to AChE
charge neutral and highly lipid soluble
-CNS toxicity
echothiophate
organophosphate
parathion and malathion
organophosphate
insectisides
sarin and soman
organophosphate
nerve gas
charged AChE inhibitor
quaternary ammonium
no CNS effects
ex/ neostigmine, pyridostigmine, edrohonium, echothiophate, ambenonium
uncharged AChE inhibitor
tertiary ammonium
CNS distribution
physostigmine, donepezil, tacrine, rivastigmine, galantamine