Anti-Alzheimer's Drugs Flashcards
Pathophysiology of Alzheimers:
Depletion of levels of ACh
Persistent activation of NMDA receptors by glutamate
»Neurodegeneration
Two types of drugs used for symptom management of Alzheimers:
ACh-esterase inhibitors
NMDA receptor antagonists
ACh-esterase inhibitors include:
Tacrine (Cognex)
Donepezil (Aricept)
Rivastigmine(Exelon)
Galantamine (Razadyne)
MOA of ACh-esterase inhibitors:
Centrally acting, reversible inhibition of Ach-esterase which increases the amount of ACh available in post-synaptic neurons
What AE is common with all ACh-esterase inhibitors?
GI intolerance: N/V/D Fatigue Insomnia Loss of appetite Weight loss
Tacrine can lead to elevated _____ and is not used much.
LFTs
Which drug causes the least AE and is approved for all stages of Alzheimers?
Donepezil
AE of Rivastigmine incldue:
HA, dizziness
avail-IR, skin patch, capsules
Which ACh-esterase inhibitors has the highest incidence of N/V?
Galantamine
avail- IR capsule, ER capsule, liquid
DI of ACh-esterase inhibitors:
Synergistic effects with cholinergic agonists
Antagonistic effects with anticholinergics
CYP 2D6 and 3A4 inducers decrease levels of donepezil
Excess glutamate can lead to excess activation of NDMA receptors and ion channels opening and lead to what symptom of Alzheimers?
Memory loss
MOA of Mermatine (Namenda):
NMDA receptor antagonist= helps to regulate glutamate which is produced in excess in Alzheimer’s patients
AE of Mermatine (Namenda):
GI intolerance
HTN
Dizziness
HA
Memantine is the only drug it is class approved for use with ________ ______ .
ACh-esterase inhibitors
Memantine is usually used for which type of Alzheimer’s disease?
Moderate to severe
