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9 Cards in this Set

  • Front
  • Back
What are the cholinesterase inhibitors used in dementia?
donepezil, rivastigmine, galantamine
(DON'T take me RIVER GALLON)
donepezil: uses, half-life, SEs, metabolism
used in mild, moderate and severe AD, other types of dementia
reversible AchE inhib
long half-life
SEs are muscarinic in nature: bradycardia, GI upset, muscle cramps, urinary incont
metab is hepatic
rivastigmine: uses, half-life, SEs, metabolism
used in mild/moderate dementia
non-competitive inhibitor (STIGMATIZE)
shorter 1/2 life, BID dosing
metabolized via ChE hydrolysis, no DDIs
SEs muscarinic
(METABOLIZED IN THE RIVER (BLOODSTREAM))
galantamine
mild-moderate AD, vascular dementia
reversible competitor of AChE
BID dosing
metabolized by CYP and excreted unchanged
cholinesterase inhibitros: general effect on AD
significant but modest improvements
do not slow ultimate progression of MCI --> AD
not disease modifying drugs
memantine
blocks NMDA receptors (when glutamate bound), uncompetitive agonist
used in moderate - severe AD, vascular dementia
Safe and well tolerated
excreted unchanged in urine, so no metabolic interactions
What is a new anti-amyloid therapy?
anti Abeta clearance, by passive or acvitve immunization
which new therapy works by decreaseing Abeta generation?
inhibiting gamma-secretase (semagacestat)
lowered amyloid production but decreased cog function
how might methylthioninium chloride work? (methylene blue)
disrupts tau-mediated tangle formation