week 4- Drugs used in the treatment of Alzheimer's Disease - Pharmacology

Question 1

what are te 2 drugs used to treat alzehmiers?

Answer 1

• Anticholinesterases (donepezil,
rivastigmine, galantamine)
• NMDA antagonist (memantine)

Question 2

-why do we use antiaceteylcholine esterase ?

Answer 2

-theres a selective loss of cholinergic receptors so we use antiaceteylcholine esterase so by boostering the amount of acetylcholine that is present this will allow activity at the cholinergic synapses, to replace the neuronal loss

Question 3

how do Acetylcholinesterase inhibitors work?

Answer 3

All AChEIs primarily work by enhancing the action of ACh by inhibiting the enzyme AChE from breaking down AChImproves cognitive function (small but measurable) in mildmoderate AD
Relies on some intact cholinergic neurones to synthesise
ACh. Hence, they are more beneficial in early stages of the
disease
All inhibit AChE. Galantamine also a BuChE inhibitor and
positive allosteric modulator at nicotinic receptors
Side effects can be limiting

Question 4

how does memantine work?

Answer 4

Memantine is a non-competitive
NMDA antagonist
Glutamate toxicity
(excitotoxicity) is proposed to
play a role in neuronal cell
death in AD
- neuronal function deteriorates
and cells die, glutamate is
released
Cognitive improvement in
moderate-severe AD

Question 5

what are some future developments for treatment of alzhemiers?

Answer 5

Anti-amyloid therapies
- Inhibition or modulation of β and γ secretase
Anti-aggregation therapy
- Reduction in the formation of β-amyloid plaques
- Reduction or inhibition of phosphorylation of tau
- Numerous failed clinical trials
- But many more ongoing…